US2017267678A1PendingUtilityA1

Tetrahydro-Pyrido-Pyrimidine Derivatives

61
Assignee: COOKE NIGEL GRAHAMPriority: Jul 6, 2010Filed: Jun 5, 2017Published: Sep 21, 2017
Est. expiryJul 6, 2030(~4 yrs left)· nominal 20-yr term from priority
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
61
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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-modified
1 - 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.

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