Recall back in January, the patent made headlines when Eli Lilly won in court with an opinion that Teva was liable for induced infringement of the patent’s methods of administering pemetrexed.
Teva Liable for Induced Infringement of Eli Lilly’s Methods of Administering Pemetrexed (ALIMTA®)
September 21, 2017
MYLAN LABORATORIES LIMITED, (Petitioner)
v.
AVENTIS PHARMA S.A. (Patent Owner)
The PTAB ordered that Sanofi’s (Aventis Pharma S.A.) patent claims to uses of Cabazitaxel have been proved to be unpatentable by a preponderance of the evidence.
4α-acetoxy-2α-benzoyloxy-5β, 20-epoxy-lβ-hydroxy-7β, 10β-dimethoxy-9-oxo-ll-taxen-13α-yl(2R,3S)-3tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate.
Improved synthesis should help chemists to invent new salvinorin A analogs to sidestep its psychoactive effects while preserving its analgesic effects. Salvinorin A, a hallucinogen produced by the plant Salvia divinorum, is promising for treating itch and pain by activating the kappa-opioid receptor while avoiding the mu-opioid receptor, which has been associated with opioid abuse.
So far Scripps has a few patents and applications directed to other classes of Kappa Opioid ligands.
US9,682,966 Kappa Opioid Ligands
US9,345,703 Kappa Opioid Receptor Effectors and Uses Thereof
US2016/0257685 Kappa Opioid Receptor Effectors and Uses Thereof
US2015/0210673 Kappa Opioid Ligands
Probably a few new patent applications are in the works. I haven’t seen any patent publications yet.
Salvinorin A & 20-Norsalvinorin
Mylan and other generic manufacturers petitioned the Patent Trial and Appeal Board (PTAB) to institute an inter partes review of AstraZeneca’s patent claiming compositions including saxagliptin. AstraZeneca markets saxagliptin as Onglyza® and Kombiglyze® XR for diabetes.
The PTAB’s Administrative Patent Judges (APJ) decided that the petitioners did not show with preponderance of the evidence that the claims of Reissue RE44,186 of U.S. Patent No. 6,395,767 would have been obvious to a skilled artisan. Particularly, saxagliptin was not obvious over “compound 25.”
Saxagliptin Structure
Structure of “Compound-25”
Experienced medicinal chemists (Persons of Ordinary Skill in the Art [PHOSITA]) knew saxagliptin bound to DP 4. But they did not have detailed knowledge of DP 4’s active site for guidance in designing inhibitors because DP 4’s crystalline structure was unknown. At the time of invention, knowledge of DP 4’s binding requirements came from structure-activity relationship (“SAR”) studies.
Petitioners cited a publication by Ashworth containing Compound-25, which they argued would have been selected as a lead compound. (Ashworth et al., 2-“Cyanopyrrolidides as Potent, Stable Inhibitors of Dipeptidyl Peptidase IV,” 6(10) Bioorganic &Med. Chem. Lett., 1163–66 (1996)).
The PTAB reasoned that a medicinal chemist would not have selected compound 25 as a lead compound because, among other reasons, (i) Compound 25 was only one of several other similar compounds (ii) Compound 25 only had in vitro data obtained using non-physiological conditions, (ii) there were two much more advanced compounds in clinical trials (i.e., NVP-DPP728 & P32/98) and (iii) Ashworth’s subsequent publication focused on different series of compounds.
Clinical Compounds NVP-DPP728 & P32/98
The PTAB’s analysis could have ended there. But even accepting Petitioners’ assertion that a skilled artisan would have chosen compound 25 as a lead compound, the PTAB determined that the Petitioners didn’t demonstrate that a skilled artisan would have had reason to modify compound 25 with a reasonable expectation of success to arrive at the claimed saxagliptin.
http://www.patentdocs.org/2017/09/mylan-pharm-v-astrazeneca-ab-ptab-2017.html
PerkinElmer Informatics, Inc. patented a “Draw-ahead feature for chemical structure drawing applications.”
Albeit usefull at times, I often turn off the type-ahead / Quick-Type feature on my iPhone to prevent embarasing errors. I would likely turn off a draw-ahead feature just in case too.
August 18, 2017
August 15, 2017
* Numbers include RCE reworks that substantially reduce the delay of organic chemistry patent applications.
† Report last updated on June 30, 2017.
See also: PatentlyO Post
