US2017267678A1PendingUtilityA1
Tetrahydro-Pyrido-Pyrimidine Derivatives
Est. expiryJul 6, 2030(~4 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 35/00A61P 37/00A61P 37/08A61P 7/04A61P 43/00A61P 37/06A61P 7/06A61P 35/02A61P 9/00A61P 25/00A61P 29/00A61P 3/00A61P 25/28A61P 11/02A61P 19/02A61P 17/00A61P 21/04A61P 17/04A61P 17/02C07D 471/04A61K 31/5377A61K 31/519
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Claims
Abstract
The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R 1 , R 2 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 - 20 . (canceled)
21 : 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 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.
22 : The method of claim 21 , wherein said modulating the activity of PI3Kδ isoform in the subject treats Sjögren's syndrome in the subject.
23 : The method of claim 23 , wherein the anion is phosphate.
24 : The method of claim 23 , wherein the salt is in anhydrous form.
25 : The method of claim 24 , wherein the salt is 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.
26 : The method of claim 24 , wherein the salt is 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.
27 : The method of claim 22 , wherein the anion is chloride.
28 : The method of claim 27 , wherein the salt is in anhydrous form.
29 : The method of claim 28 , wherein the salt is characterized by an X-Ray powder diffraction pattern comprising the following peaks given at degrees 2-Theta: 5.6, 11.3 and 23.1.
30 : The method of claim 28 , wherein the salt is 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.
31 : The method of claim 22 , wherein the anion is hippurate.
32 : The method of claim 31 , wherein the salt is in anhydrous form.
33 : The method of claim 32 , wherein the salt is 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.
34 : The method of claim 32 , wherein the salt is 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.Cited by (0)
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