专利号:US-7968752-B2 优先权日:2003-06-16 标 题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-10793551-B2 优先权日:2017-10-19 标 题:Benzimidazole-indole inhibitors of Mnk1 and Mnk2 发明人:ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; XIANG ALAN X 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , Y 1 , Y 2 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 and R 13 are as defined in the specification. The inventive Formula I and Formula II compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:US-7645754-B2 优先权日:2001-12-20 标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use 发明人:CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO 权利人:OSI PHARM INC 摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
专利号:WO-2008035086-A2 优先权日:2006-09-22 标题:Synthesis of leukotriene compounds
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