US2013225556A1PendingUtilityA1

Azetidine and cyclobutane derivatives as jak inhibitors

Assignee: INCYTE CORPPriority: Mar 11, 2008Filed: Mar 29, 2013Published: Aug 29, 2013
Est. expiryMar 11, 2028(~1.6 yrs left)· nominal 20-yr term from priority
A61P 37/08A61P 37/00A61P 37/02A61P 37/06A61P 9/04A61P 35/00A61P 5/14A61P 7/00A61P 41/00A61P 3/10A61P 9/00A61P 35/02A61P 25/00A61P 29/00A61P 13/12A61P 1/04A61P 17/06A61P 21/04A61P 17/02A61P 1/00A61P 19/02A61P 17/00B60Q 3/80Y10S362/802C07D 487/04Y10S362/80B60Q 3/76A61K 31/519C07D 403/14
56
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Claims

Abstract

The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.

Claims

exact text as granted — not AI-modified
1 - 130 . (canceled) 
     
     
         131 . {1-(cyclopropylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof. 
     
     
         132 . {1-(propylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof. 
     
     
         133 . {1-[(1-methyl-1H-pyrazol-3-yl)sulfonyl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof. 
     
     
         134 . 3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutanecarbonitrile, or a pharmaceutically acceptable salt thereof. 
     
     
         135 . {1-(ethylsulfonyl)-3-[3-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrrol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof. 
     
     
         136 . A composition comprising a compound of  claim 131 , or pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 
     
     
         137 . A method of treating an autoimmune disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 131 , or pharmaceutically acceptable salt thereof. 
     
     
         138 . A method of treating an inflammatory disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 131 , or pharmaceutically acceptable salt thereof. 
     
     
         139 . A composition comprising a compound of  claim 132 , or pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 
     
     
         140 . A method of treating an autoimmune disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 132 , or pharmaceutically acceptable salt thereof. 
     
     
         141 . A method of treating an inflammatory disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 132 , or pharmaceutically acceptable salt thereof. 
     
     
         142 . A composition comprising a compound of  claim 133 , or pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 
     
     
         143 . A method of treating an autoimmune disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 133 , or pharmaceutically acceptable salt thereof. 
     
     
         144 . A method of treating an inflammatory disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 133 , or pharmaceutically acceptable salt thereof. 
     
     
         145 . A composition comprising a compound of  claim 134 , or pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 
     
     
         146 . A method of treating an autoimmune disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 134 , or pharmaceutically acceptable salt thereof. 
     
     
         147 . A method of treating an inflammatory disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 134 , or pharmaceutically acceptable salt thereof. 
     
     
         148 . A composition comprising a compound of  claim 135 , or pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 
     
     
         149 . A method of treating an autoimmune disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 135 , or pharmaceutically acceptable salt thereof. 
     
     
         150 . A method of treating an inflammatory disease in a patient in need thereof, comprising administering to said patient an effective amount of a compound of  claim 135 , or pharmaceutically acceptable salt thereof.

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