US2018265509A1PendingUtilityA1
Tetrahydro-Pyrido-Pyrimidine Derivatives
Est. expiryJul 6, 2030(~3.9 yrs left)· nominal 20-yr term from priority
Inventors:Nigel Graham CookePaulo Fernandes Gomes Dos SantosNadege GraveleauChristina HebachKlemens HoegenauerGregory John HollingworthAlexander Baxter SmithNicolas SoldermannFrank StowasserRoss Sinclair StrangNicola TufilliAnette Von MattRomain WolfFrederic Zecri
A61P 7/04A61P 37/06A61P 37/08A61P 43/00A61P 35/02A61P 37/00A61P 35/00A61P 7/06A61P 9/00A61P 25/00A61P 25/28A61P 29/00A61P 3/00A61P 17/00A61P 21/04A61P 19/02A61P 17/02A61P 17/04A61P 11/02A61K 31/5377C07D 471/04A61K 31/519
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Claims
Abstract
wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
Claims
exact text as granted — not AI-modified1 . A salt form of 1-{(S)-3-[6-(6-Methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one, wherein the salt form comprises an anion selected from phosphate, chloride or hippurate.
2 . The salt form according to claim 1 , wherein the anion is phosphate.
3 . The salt according to claim 2 in anhydrous form.
4 . The salt form according to claim 3 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 11.6, 16.6, 20.7 and 23.3.
5 . The salt form according to claim 3 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 9.8, 11.6, 16.6, 19.5, 20.7 and 23.3.
6 . The salt form according to claim 1 , wherein the anion is chloride.
7 . The salt according to claim 6 in anhydrous form.
8 . The salt form according to claim 7 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 5.6, 11.3 and 23.1.
9 . The salt form according to claim 7 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 5.6, 11.3, 14.7, 19.4 and 23.1.
10 . The salt form according to claim 1 , wherein the anion is hippurate.
11 . The salt according to claim 10 , in anhydrous form.
12 . The salt form according to claim 11 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 5.2, 7.5, 23.2 and 24.2.
13 . The salt form according to claim 11 , characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 5.2, 7.5, 10.3, 10.9, 23.2 and 24.2.
14 . A pharmaceutical composition comprising a therapeutically effective amount of a salt form according to claim 1 , and one or more pharmaceutically acceptable carriers.
15 . A pharmaceutical combination comprising a therapeutically effective amount of a salt form according to claim 1 , and one or more therapeutically active agents.
16 . A method of modulating the activity of PI3Kδ isoform in a subject, the method comprising the step of administering to a subject a therapeutically effective amount of a salt form according to claim 1 .
17 . The method of claim 16 , wherein the anion of the salt form is phosphate.
18 . The method of claim 16 , wherein the anion of the salt form is chloride.
19 . The method of claim 16 , wherein the anion of the salt form is hippurate.Join the waitlist — get patent alerts
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