US2019218217A1PendingUtilityA1

Tetrahydro-Pyrido-Pyrimidine Derivatives as PI3Kdelta inhibitors

Assignee: NOVARTIS AGPriority: Jul 6, 2010Filed: Mar 28, 2019Published: Jul 18, 2019
Est. expiryJul 6, 2030(~3.9 yrs left)· nominal 20-yr term from priority
A61P 35/00A61P 7/04A61P 37/00A61P 43/00A61P 37/06A61P 7/06A61P 37/08A61P 9/00A61P 35/02A61P 25/28A61P 29/00A61P 25/00A61P 3/00A61P 17/00A61P 17/02A61P 19/02A61P 11/02A61P 17/04A61P 21/04A61K 31/519C07D 471/04A61K 31/5377
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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-modified
1 . 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.

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