Notice of Pre-AIA or AIA Status
The present application is being examined under the pre-AIA first to invent provisions.
Continued Examination Under 37 CFR 1.114
A request for continued examination under 37 CFR 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR 1.114, and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114. Applicant's submission filed on 07/08/2026 has been entered.
Status of the Claims
Per Applicant’s amendment to the claims, submitted on 07/08/2026, claims 78-79 are amended. Currently, claims 1, 33-38, 45-46, 48-51, 54, 56-60, 62-66, and 68-79 are pending in the instant application.
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 07/08/2026 is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Affidavit
Applicant has submitted an Affidavit penned by Dr. Ronald Kaminsky, traversing the outstanding rejections. The Affidavit is insufficient to overcome the outstanding rejections in view of Lahm (previously referenced). Applicant’s arguments traversing rejections utilizes the aforementioned Affidavit, and will accordingly be addressed in responses to Remarks below.
Interference
As indicated in previous Office Actions, claims 1, 46, 54, 60, and 66 were indicated as being rejected under pre-AIA 35 USC 135(b)(1). As a matter of clerical correction and clarification, claims 1, 33-38, 45-46, 48-51, 54, 56-60, 62-66, and 68-79 are all subject to rejection under pre-AIA 35 USC 135(b)(1). The rejections of the claims were inadvertently only applied to the independent claims 1, 46, 54, 60, and 66. As the dependent claims do not overcome the interfering subject matter, they are also subject to rejections under pre-AIA 35 USC 135(b)(1).
Claim Rejections - 35 USC § 112 Second Paragraph – Withdrawn
Rejection of claim 79:
In light of Applicant’s amendment to the claim, the rejection is hereby withdrawn. Claim 79 has been amended to be dependent upon claim 78. The claim no longer provides improper antecedence.
Claim Rejections - 35 USC § 103 - Maintained
Claim(s) 1, 33-38, 45-46, 48-51, 54, 56-60, 62-66, and 68-79 is/are rejected under pre-AIA 35 U.S.C. 102 (e) as anticipated by or, in the alternative, under pre-AIA 35 U.S.C. 103(a) as obvious over Lahm (US Patent 11278533).
Rejections of claims 1, 33-38, 45-46, 48-51, 54, 56-60, 62-66, and 68-79:
Applicant’s arguments are not persuasive. Accordingly, rejections are hereby maintained. Applicant contends that the claims of the instant application are non-obvious over the teachings of Lahm (previously referenced). Applicant’s arguments appear to mainly be drawn towards the biological differences between fleas and ticks. More specifically, that a person of ordinary skill in the art would not expect (Remarks page 13):
That a compound effective for treating or protecting a mammal from fleas would also be effective for controlling a tick infestation
That the dose of a compound effective for treating or protecting a mammal from fleas would be an effective dose for controlling a tick infestation
With regards to element (1), Applicant contends that ticks are significantly differentiated from fleas in morphology, development, feeding behavior, and disease transmission. Applicant further indicates that such differences exist despite both ticks and fleas being considered as ectoparasites. In support of said contention, Applicant provides examples supported by the Declaration of Dr. Kaminsky, wherein lufenuron and imidacloprid were effective against fleas, but not ticks (Remarks page 15). Applicant provides a further example wherein Spinosad treatments were not totally effective against ticks (Remarks page 16). While Examiner does not explicitly deny the factual claims raised by the Declaration of Dr. Kaminsky, the examples provided are not persuasive in establishing non-obviousness of the instant claims. Firstly, lufenuron and imidacloprid do not appear to be structurally or mechanically analogous to the compound of claim 1 (i.e., fluralaner). Per Applicant’s provided Appendix G (Meinke page 650), lufenuron is represented by the following structure:
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Lufenuron is considered as an insect growth regulator (IGR), and derives its pesticidal effect by inhibiting chitin synthesis. Both the structure of lufenuron and its mechanism of action appear to be unaffiliated with those of fluralaner.
The structure of imidacloprid is also provided below as disclosed in the same Appendix G (Meinke page 650):
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Imidacloprid is considered as a neonicotinoid compound. Such compounds derive their pesticidal properties from their ability to bind nicotinic acetylcholine receptors. It appears that, similarly to lufenuron above, that the structure and function of imidacloprid are not analogous to fluralaner.
Regarding Spinosad, Examiner disagrees with the conclusion that lack of total efficacy against ticks (Appendix K) provides support for Applicant’s argument of non-obviousness and unpredictability. Appendix K (Davey, 2001), as provided by Dr. Kaminsky, details the testing of topically sprayed Spinosad on boophilus microplus infested cattle. While Applicant is correct in that Davey indicates Spinosad treatment as being not “totally effective against ticks” (Remarks page 15), this misunderstands the goal of Davey’s testing and results. The testing of Spinosad by Davey was not just for assessing efficacy of Spinosad against ticks, but for determining whether the use of Spinosad spray would be suitable for use on cattle specifically arriving at US ports of entry (Davey, Abstract)1. Davey explicitly indicates that the requirement for such a specific use case would be 100% efficacy in a single treatment. While Spinosad does not meet such a requirement, Davey indicates that a single treatment of Spinosad was capable achieving 85-90% control when used on b.microplus infested cattle (Davey page 50)2. This effectiveness is also recognized by Davey, as they suggest that Spinosad would be useful in eradicating tick infestations with repeated treatments over a longer period of time (Davey page 51)3. In other words, the findings of Davey as a whole, do not highlight the ineffectiveness of Spinosad on ticks, but the opposite; that Spinosad is indeed effective in eradicating tick infestations.
In view of the state of the art at the time of invention, Davey may actually, in part, support the predictability of fluralaner to eradicate tick infestations. Looking towards the prior art, Sparks (The management of diamondback moth and other crucifer pests, Nov. 2001, pages 37-44) indicates that Spinosad targets nicotinic acetylcholine receptors, but also alters function of GABA gated chloride channels (Sparks page 41)4. As fluralaner appears to be an inhibitor of GABA gated chloride channels, a person of ordinary skill in the art may have found it reasonable to use fluralaner against tick infestations. Expounding on this further, it appears that GABA gated chloride channels were a known target for parasiticides targeting both ticks and fleas, as evidenced by Connelly (ENVIRONMENTAL FATE OF FIPRONIL, December 2001), which teaches the use of fipronil to control both tick and flea infestations by blocking GABA gated chloride channels (pages 11-12)5.
With regards to element (2), Applicant with support from the Declaration of Dr. Kaminsky, contend that the in vitro testing of a compound may not necessarily be representative of its ability to act as a successful tick medicament, because the compound must be safely administered to a host animal in an amount which safely and sufficiently reaches a systemic concentration allowing it to be effective (Remarks pages 16-17). While Applicant is not explicitly incorrect in this assessment, this statement could be applicable to in vitro testing of any pharmaceutical compound for any biological purpose. Such risks and considerations are imbedded in the art. With regards to the testing carried out in the Lahm prior art, Examiner maintains that the testing is at least reasonably analogous to the treatment of an in vivo tick infestation. For reference, Lahm’s biological testing was carried out in vivo in mice having infestations of cat fleas (Lahm, col. 57-58, Tests A-C). Said subjects were dosed orally such that the circulating amount of the target compound (fluralaner) was sufficient to kill 50% of the fleas without toxic harm to the subjects. While Test D (Lahm, col. 58) was indeed an in vitro demonstration against cat fleas feeding on bovine blood, Lahm further demonstrated safe and effective administration to live animals alongside it.
For the reasons as iterated above, the rejections of the claims are hereby maintained. Reiterated rejections are provided below solely for the purpose of reference.
Reiterated rejections:
Claim 1 recites a method for controlling a tick infestation of an animal, wherein the method comprises systemically administering an effective amount of about 1 mg/kg to about 50 mg/kg of a isoxazoline, a salt of the isoxazoline, or a solvate of the isoxazoline to the animal; wherein the isoxazoline corresponds to the following formula:
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Lahm teaches antiparasitic compounds and methods of use in protecting animals from parasitic pests by administering said compounds orally or by injection (Abstract)6. One such compound taught by Lahm is the following compound 3 (Table A, column 56):
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As can be seen from the above structure and table, compound 3 of Lahm is identical to the formula of the instant claim. Lahm further indicates exemplary tests carried out with said compounds in order to evaluate effectiveness in protection against cat fleas. Of particular interest is Test C which indicates the subcutaneous dosing of mice with compound 3 at 10 mg/kg (column 57 lines 62-67, column 58 lines 21-26)7.
While Lahm does not explicitly teach the use of said compounds on a tick infestation, it would have been obvious for a person of ordinary skill in the art to apply the aforementioned dosing to a tick infestation because Lahm indicates use of the compound for treating infestations by a number of different invertebrates, including ticks.
Lahm expressly indicates that the disclosed compounds are effective against ectoparasites, which include stable flies, ticks, and fleas of both dogs and cats (column 49, lines 35-41)8. Without evidence of the contrary, a person of ordinary skill in the art would have found it obvious to apply Lahm’s 10 mg/kg dosing regimen for cat flea infestations to a mammal with a tick infestation because there would be a reasonable expectation that such a treatment would be effective in treating a tick infestation as both parasites are considered as ectoparasites targeted by compound 3.
Claim 33 further limits the method of claim 1 wherein the animal is a canine or feline and the isoxazoline is administered at a frequency of at least about every 2 months.
As discussed previously, Lahm obviates the method of claim 1 wherein a compound identical to the recited isoxazoline is applied to control a tick infestation. Lahm further makes mention of preferential dosing interval of once per month (page column 56 lines 19-26)9, as well as express desire for dosing to both canines and felines (column 59, claim 5)10.
Claim 34 further limits the method of claim 1 wherein the animal is a canine and the isoxazoline is administered at a dose of from about 10 to about 50 mg/kg.
As discussed previously, Lahm teaches a dosing amount of 10 mg/kg, as well as treatment of canines.
Claim 35 further limits the method of claim 1 wherein the mammal is a canine and the isoxazoline of Formula 11-1 is administered at a dose of from 10-30 mg/kg.
As discussed previously, Lahm teaches a dosing amount of 10 mg/kg of a compound identical to Formula 11-1, as well as treatment of canines.
Claim 36 further limits the method of claim 1 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, an American dog tick (Dermacentor variabilis) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10)11.
Claim 37 further limits the method of claim 1 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 38 further limits the method of claim 1 wherein the dose is administered at a frequency of from about once every month to about once every 3 months.
As discussed in the rejection of claim 33, Lahm indicates a preferred dosing interval of once per month, which meets the limitation of the instant claim.
Claim 46 recites a method for reducing, eradicating, or inhibiting a tick infestation in a canine, comprising: orally administering to the canine in need thereof a composition comprising a compound of Formula 11-1, a salt thereof, or a solvate of any of the foregoing and at least one excipient or carrier wherein the administering comprises orally administering the composition to provide the canine with a dose of 10 mg/kg to 50 mg/kg body weight of the compound, the salt thereof, or the solvate of any of the foregoing.
Lahm teaches antiparasitic compounds and methods of use in protecting animals from parasitic pests by administering said compounds orally or by injection (Abstract)12. One such compound taught by Lahm is the following compound 3 (Table A, column 56):
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As can be seen from the above structure and table, compound 3 of Lahm is identical to the formula of the instant claim. Lahm further indicates exemplary tests carried out with said compounds in order to evaluate effectiveness in protection against cat fleas. Of particular interest is Test A which indicates the oral dosing of mice with compound 3 at 10 mg/kg (column 57 lines 33-43)13 by administering a composition comprising compound 3 solubilized in propylene glycol/glycerol (60:40)..
While Lahm does not explicitly teach the use of said compounds on a tick infestation in a canine, it would have been obvious for a person of ordinary skill in the art to apply the aforementioned dosing to a tick infestation because Lahm indicates use of the compound for treating infestations by a number of different invertebrates, including ticks, and it would be further obvious to apply such a treatment to dogs, because Lahm further indicates dogs as target animals for their application of the compound.
Lahm expressly indicates that the disclosed compounds are effective against ectoparasites, which include stable flies, ticks, and fleas of both dogs and cats (column 49, lines 35-41)14. Furthermore, Lahm expressly indicates the intent to treat canines as a target animal using the disclosed compounds (column 58, lines 66-67)15.
Without evidence of the contrary, a person of ordinary skill in the art would have found it obvious to apply Lahm’s 10 mg/kg oral dosing regimen for cat flea infestations to a canine with a tick infestation because there would be a reasonable expectation that such a treatment would be effective in treating said tick infestation, as both parasites are considered as ectoparasites targeted by compound 3.
Claim 48 further limits the method of claim 46 wherein the method comprises administering the composition at a frequency in the range of once every month to once every 3 months.
Lahm teaches a preferential dosing interval of once per month (page column 56 lines 19-26).
Claim 49 further limits the method of claim 46 wherein the composition does not comprise and is not administered in the form of microspheres, granules, or implants.
Lahm’s Test A comprises the administration of an oral formulation which does not comprise or is not administered in the form of microspheres, granules, or implants.
Claim 50 further limits the method of claim 46 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, an American dog tick (Dermacentor variabilis) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 51 further limits the method of claim 46 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 54 recites a method for reducing, eradicating, or inhibiting a tick infestation in a canine, comprising: administering to the canine in need thereof a composition comprising a compound of Formula 11-1, a salt thereof, or a solvate of any of the foregoing and least one excipient or carrier wherein the administering comprises administering the composition to provide the canine with a dose of 1 mg/kg to 50 mg/kg body weight of the compound, the salt thereof, or the solvate of any of the foregoing.
Lahm teaches antiparasitic compounds and methods of use in protecting animals from parasitic pests by administering said compounds orally or by injection (Abstract)16. One such compound taught by Lahm is the following compound 3 (Table A, column 56):
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As can be seen from the above structure and table, compound 3 of Lahm is identical to the formula of the instant claim. Lahm further indicates exemplary tests carried out with said compounds in order to evaluate effectiveness in protection against cat fleas. Of particular interest is Test A which indicates the oral dosing of mice with compound 3 at 10 mg/kg (column 57 lines 33-43)17 by administering a composition comprising compound 3 solubilized in propylene glycol/glycerol (60:40)..
While Lahm does not explicitly teach the use of said compounds on a tick infestation in a canine, it would have been obvious for a person of ordinary skill in the art to apply the aforementioned dosing to a tick infestation because Lahm indicates use of the compound for treating infestations by a number of different invertebrates, including ticks, and it would be further obvious to apply such a treatment to dogs, because Lahm further indicates dogs as target animals for their application of the compound.
Lahm expressly indicates that the disclosed compounds are effective against ectoparasites, which include stable flies, ticks, and fleas of both dogs and cats (column 49, lines 35-41)18. Furthermore, Lahm expressly indicates the intent to treat canines as a target animal using the disclosed compounds (column 58, lines 66-67)19.
Without evidence of the contrary, a person of ordinary skill in the art would have found it obvious to apply Lahm’s 10 mg/kg oral dosing regimen for cat flea infestations to a canine with a tick infestation because there would be a reasonable expectation that such a treatment would be effective in treating said tick infestation, as both parasites are considered as ectoparasites targeted by compound 3.
Claim 56 further limits the method of claim 54 wherein the composition is administered in the range of once every 2 months to once every 3 months.
While Lahm does not explicitly teach a dosing regimen in the range of once every 2 months to once every 3 months, Lahm does make the suggestion of dosing in a range of about weekly to about once every 6 months (column 56, lines 19-26), indicating acceptable variation in dosing intervals. While the such a range does not outright obviate the limitation of the instant claim, the use of such a dosing regimen would still remain obvious to a person of ordinary skill in the art per the principle of routine optimization. Lahm obviates a method of treating tick infestations by administration of a composition comprising a compound of Formula 11-1, and at the same time makes the suggestion of multiple administration intervals of preferably one month, or weekly to every six months. A skilled artisan would have motivation to find the optimal dosing interval through experimentation and routine optimization. Such experimentation is supported by Lahm, wherein Lahm indicates that a desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the amount needed to achieve a particular result can be determined through experimentation (column 56, lines 4-13)20. See MPEP 2144.05(II):
“Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. "[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation." In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955) (Claimed process which was performed at a temperature between 40°C and 80°C and an acid concentration between 25% and 70% was held to be prima facie obvious over a reference process which differed from the claims only in that the reference process was performed at a temperature of 100°C and an acid concentration of 10%.); see also Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."); In re Hoeschele, 406 F.2d 1403, 160 USPQ 809 (CCPA 1969) (Claimed elastomeric polyurethanes which fell within the broad scope of the references were held to be unpatentable thereover because, among other reasons, there was no evidence of the criticality of the claimed ranges of molecular weight or molar proportions.). For more recent cases applying this principle, see Merck & Co. Inc. v. Biocraft Lab. Inc., 874 F.2d 804, 10 USPQ2d 1843 (Fed. Cir.), cert. denied, 493 U.S. 975 (1989); In re Kulling, 897 F.2d 1147, 14 USPQ2d 1056 (Fed. Cir. 1990); and In re Geisler, 116 F.3d 1465, 43 USPQ2d 1362 (Fed. Cir. 1997); Smith v. Nichols, 88 U.S. 112, 118-19 (1874) (a change in form, proportions, or degree "will not sustain a patent"); In re Williams, 36 F.2d 436, 438 (CCPA 1929) ("It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions."). See also KSR Int’l Co. v. Teleflex Inc., 550 U.S. 398, 416, 82 USPQ2d 1385, 1395 (2007) (identifying "the need for caution in granting a patent based on the combination of elements found in the prior art.").”
Claim 57 further limits the method of claim 54 wherein the composition does not comprise and is not administered in the form of microspheres, granules, or implants.
Lahm does not teach the administration of a composition comprising a compound of Formula 11-1 and microspheres, granules, or implants.
Claim 58 further limits the method of claim 54 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, an American dog tick (Dermacentor variabilis) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 59 further limits the method of claim 54 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 60 recites a method for reducing, eradicating, or inhibiting a tick infestation in a feline, comprising: administering to the feline in need thereof a composition comprising a compound of Formula 11-1, a salt thereof, or a solvate of any of the foregoing and least one excipient or carrier wherein the administering comprises administering the composition to provide the feline with a dose of 10 mg/kg to 50 mg/kg of the compound, the salt thereof, or the solvate of any of the foregoing.
Lahm teaches antiparasitic compounds and methods of use in protecting animals from parasitic pests by administering said compounds orally or by injection (Abstract)21. One such compound taught by Lahm is the following compound 3 (Table A, column 56):
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As can be seen from the above structure and table, compound 3 of Lahm is identical to the formula of the instant claim. Lahm further indicates exemplary tests carried out with said compounds in order to evaluate effectiveness in protection against cat fleas. Of particular interest is Test A which indicates the oral dosing of mice with compound 3 at 10 mg/kg (column 57 lines 33-43)22 by administering a composition comprising compound 3 solubilized in propylene glycol/glycerol (60:40).
While Lahm does not explicitly teach the use of said compounds on a tick infestation in a feline, it would have been obvious for a person of ordinary skill in the art to apply the aforementioned dosing to a tick infestation because Lahm indicates use of the compound for treating infestations by a number of different invertebrates, including ticks, and it would be further obvious to apply such a treatment to a feline, because Lahm further indicates felines as target animals for their application of the compound.
Lahm expressly indicates that the disclosed compounds are effective against ectoparasites, which include stable flies, ticks, and fleas of both dogs and cats (column 49, lines 35-41)23. Furthermore, Lahm expressly indicates the intent to treat felines as a target animal using the disclosed compounds (column 59, lines 1-2)24.
Without evidence of the contrary, a person of ordinary skill in the art would have found it obvious to apply Lahm’s 10 mg/kg oral dosing regimen for cat flea infestations to a canine with a tick infestation because there would be a reasonable expectation that such a treatment would be effective in treating said tick infestation, as both parasites are considered as ectoparasites targeted by compound 3.
Claim 62 further limits the method of claim 60 wherein the method comprises administering the composition at a frequency in the range of once every 2 months to once every 3 months.
While Lahm does not explicitly teach a dosing regimen in the range of once every 2 months to once every 3 months, Lahm does make the suggestion of dosing in a range of about weekly to about once every 6 months (column 56, lines 19-26), indicating acceptable variation in dosing intervals. While the such a range does not outright obviate the limitation of the instant claim, the use of such a dosing regimen would still remain obvious to a person of ordinary skill in the art per the principle of routine optimization. Lahm obviates a method of treating tick infestations by administration of a composition comprising a compound of Formula 11-1, and at the same time makes the suggestion of multiple administration intervals of preferably one month, or weekly to every six months. A skilled artisan would have motivation to find the optimal dosing interval through experimentation and routine optimization. Such experimentation is supported by Lahm, wherein Lahm indicates that a desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the amount needed to achieve a particular result can be determined through experimentation (column 56, lines 4-13)25. See MPEP 2144.05(II).
Claim 63 further limits the method of claim 60 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, an American dog tick (Dermacentor variabilis) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 65 further limits the method of claim 60 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 66 recites a method for reducing, eradicating, or inhibiting a tick infestation in a feline, comprising: administering to the feline in need thereof a composition comprising a compound of Formula 11-1, a salt thereof, or a solvate of any of the foregoing, at least one anthelmintic, and at least one excipient or carrier wherein the administering comprises administering the composition to provide the feline with a dose of 10 mg/kg to 50 mg/kg body weight of the compound, the salt thereof, or the solvate of any of the foregoing.
Lahm teaches antiparasitic compounds and methods of use in protecting animals from parasitic pests by administering said compounds orally or by injection (Abstract)26. One such compound taught by Lahm is the following compound 3 (Table A, column 56):
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As can be seen from the above structure and table, compound 3 of Lahm is identical to the formula of the instant claim. Lahm further indicates exemplary tests carried out with said compounds in order to evaluate effectiveness in protection against cat fleas. Of particular interest is Test A which indicates the oral dosing of mice with compound 3 at 10 mg/kg (column 57 lines 33-43)27 by administering a composition comprising compound 3 solubilized in propylene glycol/glycerol (60:40).
Lahm does not explicitly teach the following:
Administration to a feline having a tick infestation
A composition comprising both a compound of Formula 11-1 together with an anthelmintic
However, it would be obvious for a person or ordinary skill in the art to apply Lahm’s method to a feline having a tick infestation because Lahm teaches that the compound of Formula 11-1 is effective for treating ticks infestation, and Lahm further indicates that felines are a target animal for the dosing of the disclosed compound. It would further be obvious to combine a compound of Formula 11-1 with an anthelmintic, because Lahm suggests the inclusion of an additional biologically active compound in the form of an anthelminthic.
Lahm expressly indicates that the disclosed compounds are effective against ectoparasites, which include stable flies, ticks, and fleas of both dogs and cats (column 49, lines 35-41)28. Furthermore, Lahm expressly indicates the intent to treat felines as a target animal using the disclosed compounds (column 59, lines 1-2)29.
Lahm further indicates the inclusion of anthelminthics as additionally active biologic compounds in formulations comprising a compound of Formula 11-1. More specifically, Lahm indicates the inclusion of avermectins such as ivermectin, moxidectin, and milbemycin, as well as praziquantel (column 51, lines 23-29)30. The inclusion of such compounds would be obvious to a person of ordinary skill in the art as there would be a reasonable expectation that they would provide a clear improvement by providing the antiparasitic formulation a broader spectrum effect in treating different types of parasites.
Claim 68 further limits the method of claim 66 wherein the method comprises administering the composition at a frequency in the range of once every 2 months to every 3 months.
While Lahm does not explicitly teach a dosing regimen in the range of once every 2 months to once every 3 months, Lahm does make the suggestion of dosing in a range of about weekly to about once every 6 months (column 56, lines 19-26), indicating acceptable variation in dosing intervals. While the such a range does not outright obviate the limitation of the instant claim, the use of such a dosing regimen would still remain obvious to a person of ordinary skill in the art per the principle of routine optimization. Lahm obviates a method of treating tick infestations by administration of a composition comprising a compound of Formula 11-1, and at the same time makes the suggestion of multiple administration intervals of preferably one month, or weekly to every six months. A skilled artisan would have motivation to find the optimal dosing interval through experimentation and routine optimization. Such experimentation is supported by Lahm, wherein Lahm indicates that a desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the amount needed to achieve a particular result can be determined through experimentation (column 56, lines 4-13)31. See MPEP 2144.05(II).
Claim 69 further limits the method of claim 66 wherein the composition does not comprise and is not administered in the form of microspheres, granules, or implants.
Lahm does not teach a method of the claim 66 wherein the composition comprises or is administered in the form of microspheres, granules, or implants.
Claim 70 further limits the method of claim 66 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, an American dog tick (Dermacentor variabilis) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 71 further limits the method of claim 60 wherein the tick infestation comprises at least one of a brown dog tick (Rhipicephalus sanguineus) infestation, a castor bean tick (Ixodes ricinus) infestation, an ornate cow tick (Dermacentor reticulates) infestation, a lone star tick (Amblyomma americanum) infestation, and a chicken tick (Ornithodoros moubata) infestation.
Lahm indicates that their disclosed compounds are effective for tick infestations, including at least Rhipicephalus sanguineus (brown dog tick) (column 50, lines 4-10).
Claim 72 further limits the method of claim 66 wherein the at least one anthelmintic comprises a macrocyclic lactone parasiticide.
Lahm teaches the inclusion of macrocyclic lactones as additional actives.
Claim 73 further limits the method of claim 72 wherein the macrocyclic lactone parasiticide is selected from ivermectin, moxidectin, and milbemycin.
Lahm teaches moxidectin as an additional active.
Claim 74 further limits the method of claim 72 wherein the macrocyclic lactone parasiticide is moxidectin.
Lahm teaches moxidectin as an additional active.
Claim 75 further limits the method of claim 66 wherein the at least one anthelmintic comprises praziquantel.
Lahm teaches praziquantel as an additional active.
Claim 76 further limits the method of claim 46 wherein the composition is a unit dosage form.
Lahm teaches an embodiment wherein their disclosed compositions may be in the form of a chewable treat or edible tablet (specification col. 55, lines 4-9)32. An edible tablet would be considered a unit dosage form.
Claim 77 further limits the method of claim 46 wherein the composition is solid.
Lahm teaches an embodiment wherein their disclosed compositions may be in the form of a chewable treat or edible tablet (specification col. 55, lines 4-9). Such dosage forms would be considered to be solids.
Claim 78 further limits the method of claim 46 wherein the composition is in a chewable dosage form.
Lahm teaches an embodiment wherein their disclosed compositions may be in the form of a chewable treat (specification col. 55, lines 4-9).
Claim 79 further limits the method of claim 46 wherein the method further comprises administering the chewable dosage form with food.
As iterated in the rejection of claim 78, Lahm teaches their compositions as chewable dosage forms. Lahm further indicates that their compounds and composition may be administered with food depending on the contemplated end use (specification Col. 46, lines 4-9)33.
Conclusion
Claims 1, 33-38, 45-46, 48-51, 54, 56-60, 62-66, and 68-79 remain rejected.
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/ERIC TRAN/Examiner, Art Unit 1629
/JEFFREY S LUNDGREN/Supervisory Patent Examiner, Art Unit 1629
1 “Thus, the use of spinosad at US ports-of-entry would be unacceptable because of the critical necessity of achieving 100% control with a single treatment to prevent the reintroduction of ticks.“
2 “Results of the study demonstrated that a single whole-body spray treatment with spinosad at concentrations of 0.05 and 0.15%AIappliedtocattle infested with all parasitic life stages of B. microplus would provide ≈85–90% control.”
3 “Since the results of this study indicated that spinosad had an activity level that is similar to permethrin, as previously discussed, it can be assumed that if spinosad was used in repeated (systematic) treatments of cattle in an infested premises there would be a high likelihood of eradicating the ticks on the premises. In addition, since results of this study showed that 0.15% AI spinosad provided 2-weeks of total residual control, it might be possible that intervals between treatments could be extended to 21 or perhaps even 28 days, thus reducing the costs of gathering and treating animals.”
4 “Spinosad (a mixture of spinosyns A and D, Figure 1) represents a new class of fermentation derived tetracyclic macrolides (Kirst et al. 1992, Sparks et al. 1999). The spinosyns, which act via the insect nervous system, are especially active against a variety of lepidopterous pests (DeAmicis et al. 1997, Sparks et al.1999) and possess very favourable mammalian toxicity and environmental profiles (Sparks et al. 1999, Crouse & Sparks 1998, Table 1). The mode of action appears to involve alteration of nicotinic receptor function as well as the function of GABA gated chloride channels (Salgado et al. 1997, Watson 2001).”
5 “Fipronil (5-amino-1-[2,6-dichloro-4-(trifluromethyl)phenyl]-4-[(trifluromethyl)sulfinyl] 1H-pyrazole), a phenylpyrazole insecticide, exhibits neurotoxic activity by blocking the GABA- regulated chloride channels of neurons. It is useful for the control of roaches, ants, termites, fleas and ticks. It is often formulated as insect bait, sprays for pets, and as a granular turf product to control mole crickets. Fipronil affects target species by blocking the chloride channels of neurons; therefore the resting membrane potential cannot be re-established, the result is excessive neuronal activity. At sufficient doses fipronil causes paralysis and insect death.”
6 “Disclosed is a method for protecting an animal from a parasitic invertebrate pest comprising treating an animal orally or by injection with a pesticidally effective amount of a compound of Formula: (I)…”
7 “For evaluating control of the cat flea (Ctenocephalides felis), a CD-I® mouse (about 30 g, male, obtained from Charles River Laboratories, Wilmington, MA) was subcutaneously dosed with a test compound in an amount of 1 0 mg/kg solubilized in propylene glycol/glycerol formal (60:40). Two hours after oral administration of the test compound, approximately 8 to 16 adult fleas were applied to each mouse. The fleas were then evaluated for mortality 48 hours after flea application to the mouse. Of the compounds tested, the following compounds resulted in at least 20% mortality: I, 2 and 3. The following compounds resulted in at least 50% mortality: I and 3.”
8 “In particular, the compounds of Formula I are especially effective against ectoparasites including Stomoxys calcitrans (stable fly); ticks such as Ixodes spp., Boophilus spp., Rhipicephalus spp., Amblyomma spp., Dermacentor spp., Hyalomma spp. and Haemaphysalis spp.; and fleas such as Ctenocephalides felis (cat flea) and Ctenocephalides canis (dog flea).”
9 “Suitable intervals for the administration of compounds of the present invention to animals range from about daily to about yearly. Of note are administration intervals ranging 20 from about weekly to about once every 6 months. Of particular note are monthly administration intervals (i.e. administering the compound to the animal once every month).”
10 “5. The method according to claim 1, wherein the mammal
is a cat or dog.”
11 “Ticks include, e.g., soft-bodied ticks including Argasidae spp. for example Argas spp. and Ornithodoros spp.; hardbodied ticks including Ixodidae spp., for example Rhipicephalus sanguineus, Dermacentor variabilis, Dermacentor andersoni, Amblyomma americanum, Ixodes scapularis and other Rhipicephalus spp. (including the former Boophilus genera).”
12 “Disclosed is a method for protecting an animal from a parasitic invertebrate pest comprising treating an animal orally or by injection with a pesticidally effective amount of a compound of Formula: (I)…”
13 “For evaluating control of the cat flea (Ctenocephalides felis), a CD-1® mouse (about 30 g, male, obtained from Charles River Laboratories, Wilmington, Mass.) was orally dosed with a test compound in an amount of 10 mg/kg solubilized in propylene glycol/glycerol formal (60:40). Two hours after oral administration of the test compound, approximately 8 to 16 adult fleas were applied to each mouse. The fleas were then evaluated for mortality 48 hours after flea application to the mouse.”
14 “In particular, the compounds of Formula I are especially effective against ectoparasites including Stomoxys calcitrans (stable fly); ticks such as Ixodes spp., Boophilus spp., Rhipicephalus spp., Amblyomma spp., Dermacentor spp., Hyalomma spp. and Haemaphysalis spp.; and fleas such as Ctenocephalides felis (cat flea) and Ctenocephalides canis (dog flea).”
15 “The method according to claim 1, wherein the mammal is a canine.”
16 “Disclosed is a method for protecting an animal from a parasitic invertebrate pest comprising treating an animal orally or by injection with a pesticidally effective amount of a compound of Formula: (I)…”
17 “For evaluating control of the cat flea (Ctenocephalides felis), a CD-1® mouse (about 30 g, male, obtained from Charles River Laboratories, Wilmington, Mass.) was orally dosed with a test compound in an amount of 10 mg/kg solubilized in propylene glycol/glycerol formal (60:40). Two hours after oral administration of the test compound, approximately 8 to 16 adult fleas were applied to each mouse. The fleas were then evaluated for mortality 48 hours after flea application to the mouse.”
18 “In particular, the compounds of Formula I are especially effective against ectoparasites including Stomoxys calcitrans (stable fly); ticks such as Ixodes spp., Boophilus spp., Rhipicephalus spp., Amblyomma spp., Dermacentor spp., Hyalomma spp. and Haemaphysalis spp.; and fleas such as Ctenocephalides felis (cat flea) and Ctenocephalides canis (dog flea).”
19 “The method according to claim 1, wherein the mammal is a canine.”
20 “One skilled in the art will appreciate that the pesticidally effective dose can vary for the various compounds and compositions useful for the method of the present invention, the desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the like, and the amount needed to achieve a particular result can be determined through simple experimentation.”
21 “Disclosed is a method for protecting an animal from a parasitic invertebrate pest comprising treating an animal orally or by injection with a pesticidally effective amount of a compound of Formula: (I)…”
22 “For evaluating control of the cat flea (Ctenocephalides felis), a CD-1® mouse (about 30 g, male, obtained from Charles River Laboratories, Wilmington, Mass.) was orally dosed with a test compound in an amount of 10 mg/kg solubilized in propylene glycol/glycerol formal (60:40). Two hours after oral administration of the test compound, approximately 8 to 16 adult fleas were applied to each mouse. The fleas were then evaluated for mortality 48 hours after flea application to the mouse.”
23 “In particular, the compounds of Formula I are especially effective against ectoparasites including Stomoxys calcitrans (stable fly); ticks such as Ixodes spp., Boophilus spp., Rhipicephalus spp., Amblyomma spp., Dermacentor spp., Hyalomma spp. and Haemaphysalis spp.; and fleas such as Ctenocephalides felis (cat flea) and Ctenocephalides canis (dog flea).”
24 “The method according to claim 1, wherein the mammal is a feline.”
25 “One skilled in the art will appreciate that the pesticidally effective dose can vary for the various compounds and compositions useful for the method of the present invention, the desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the like, and the amount needed to achieve a particular result can be determined through simple experimentation.”
26 “Disclosed is a method for protecting an animal from a parasitic invertebrate pest comprising treating an animal orally or by injection with a pesticidally effective amount of a compound of Formula: (I)…”
27 “For evaluating control of the cat flea (Ctenocephalides felis), a CD-1® mouse (about 30 g, male, obtained from Charles River Laboratories, Wilmington, Mass.) was orally dosed with a test compound in an amount of 10 mg/kg solubilized in propylene glycol/glycerol formal (60:40). Two hours after oral administration of the test compound, approximately 8 to 16 adult fleas were applied to each mouse. The fleas were then evaluated for mortality 48 hours after flea application to the mouse.”
28 “In particular, the compounds of Formula I are especially effective against ectoparasites including Stomoxys calcitrans (stable fly); ticks such as Ixodes spp., Boophilus spp., Rhipicephalus spp., Amblyomma spp., Dermacentor spp., Hyalomma spp. and Haemaphysalis spp.; and fleas such as Ctenocephalides felis (cat flea) and Ctenocephalides canis (dog flea).”
29 “The method according to claim 1, wherein the mammal is a feline.”
30 “Of note are additional biologically active compounds or agents selected from art-known anthelmintics, such as, for example, avermectins (e.g., ivermectin, moxidectin, milbemycin), benzimidazoles (e.g., albendazole, triclabendazole), salicylanilides (e.g., closantel, oxyclozanide), substituted phenols (e.g., nitroxynil), pyrimidines (e.g., pyrantel), imidazothiazoles (e.g., levamisole) and praziquantel.”
31 “One skilled in the art will appreciate that the pesticidally effective dose can vary for the various compounds and compositions useful for the method of the present invention, the desired pesticidal effect and duration, the target parasitic invertebrate pest species, the animal to be protected, the mode of application and the like, and the amount needed to achieve a particular result can be determined through simple experimentation.”
32 “A preferred embodiment is a composition of the present method formulated into a chewable and/or edible product (e.g., a chewable treat or edible tablet). Such a product would ideally have a taste, texture and/or aroma favored by the animal to be protected so as to facilitate oral administration of the compound of Formula 1.”
33 “The compounds of Formula 1 can be applied without other adjuvants, but most often application will be of a formulation comprising one or more active ingredients with suitable carriers, diluents, and surfactants and possibly in combination with a food depending on the contemplated end use.”
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