Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
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Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
Claim(s) 1, 6-11, 14-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Ren, US 9403820 and Ibrahim US 20180207100.
Ren teaches at page hydrochloric acid salt of Serabelisib (see claim1) and pharmaceutical composition (claim 9). How to make
Serabelisib, is known as INK-1117, MLN-1117, TAK-117 or ART-001 is a well-established, kinase inhibitor. Also see applicant admitted references with regards to pH dependence and oral syrups at page 2.
Claims of Ren corresponds to the inorganic salt limitations of base claim 1 (and that of dependent claims 6, 9, 16).
In column 23 line 52 onto column 24 lines 67 Ren teaches ionic surfactants that correspond to ‘hydrophilic polymer’ limitation of instant claim 1 ( and as specified in claims dependent 7, 10, 14, 17),
Claims 8, 9, 10, 15, 17 of the dependent claims relate to weight ratio of the active ingredient Serabelisib relative to the acid and hydrophilic polymer in the compositions.
At column 20 lines 4 to 67 Ren teaches the amount of active ingredient for the composition. According to Ren, the exact dosage will depend upon the route of administration, the form in which the polymorphs is administered, the subject to be treated, the body weight of the subject to be treated, and the preference and experience of the attending physician. Further, it has been held that where the general conditions of a claim are disclosed in the prior art, discovering the optimum or workable ranges involves only routine skill in the art. The 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).
The instant kinase inhibitor Serabelisib is a known BCS class II drug with low solubility and high permeability same as the kinase inhibitor palbociclib. Ibrahim teaches that the solubility of palbociclib depends on pH, see page 1, paragraph [0005] :
Palbociclib is a dibasic compound and has two basic groups with pKa's of approximately 7.3 (the secondary piperazine nitrogen) and 4.1 (the pyridine nitrogen). The solubility of palbociclib free base is pH dependent. Palbociclib is water soluble at low pH (2.1-4.5), while the solubility dramatically decreases as pH rises above 4.5. Palbociclib has poor water solubility (9 μg/mL) at pH 7.9. Concomitant administration of agents which increase gastric pH can alter the solubility and absorption of palbociclib free base formulations.
Though Ren teaches, HCl salt of Serabelisib, one of skill in the art would anticipate, given the low basicity of free base of Serabelisib which has weakly basic nitrogens, by decreasing the pH, increasing the amount of acid would increase the protonation of the nitrogens of Serabelisib, thereby increasing the solubility.
At page 7, [0093]-[0095], Ibrahim teaches how to make pharmaceutical compositions with palbociclib as ingredient and the instantly recited hydrophilic polymers (of instant claims) that has a pH-dependent dissolution profile and is capable of achieving excellent absorption efficiency regardless of the pH in the digestive tract. Also see claims 1-18 at page 18 of Ibrahim.
Each ingredients active (Ren), the acid and inactive hydrophilic polymer (Ibrahim) is known in the art; It would have been obvious to one of ordinary skill in the art at the time the claimed invention was made to combine the instant ingredients for their known benefit, that is the why and how ((Ibrahim) since each is well known in the art for their beneficial properties. Again, the invention is a selective combination of the inventions by the prior arts done in a manner obvious to one of ordinary skill in the art. Patent for the combination of known elements wherein their functions remain the same withdraws “what is already known into field of its monopoly and diminishes resources available to skilled men”. Sakraida v. Ag Pro, Inc.189 USPQ 449, 425 US 273, (1976).
Therefore nothing unobvious is seen in the claims.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to NIZAL S CHANDRAKUMAR whose telephone number is (571)272-6202. The examiner can normally be reached M-F 8-5 EST.
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/NIZAL S CHANDRAKUMAR/Primary Examiner, Art Unit 1625