Publication number: 20160194330
Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
Type:
Application
Filed:
December 20, 2013
Publication date:
July 7, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Michael Berlin, Pauline Ting, Gang Zhou, Tao Yu, Christopher Boyce, Joseph Michael Kelly, Jayaram R. Tagat, Junying Zheng, Xianhai Huang, Wei Zhou, Jae-Hun Kim, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Rajan Anand, Qiaolin Deng
Publication number: 20070167435
Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(?O)—, —C(?NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combinat
Type:
Application
Filed:
December 19, 2006
Publication date:
July 19, 2007
Inventors:
Mwangi Mutahi, Robert Aslanian, Michael Berlin, Christopher Boyce, Manuel de Lera Ruiz, Kevin McCormick, Daniel Solomon, Henry Vaccaro, Junying Zheng, Purakkattle Biju, Younong Yu, Wei Zhou, Xiaohong Zhu
Publication number: 20070142394
Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(?O)—, —C(?NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(?O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(?NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination
Type:
Application
Filed:
December 19, 2006
Publication date:
June 21, 2007
Inventors:
Daniel Solomon, Robert Aslanian, Michael Berlin, Manuel de Lera Ruiz, Kevin McCormick, Mwangi Mutahi, Wing Tom
Publication number: 20070015807
Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(?O)—, —C(?S)—, —(CH2)q—, —C(?NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other age
Type:
Application
Filed:
June 19, 2006
Publication date:
January 18, 2007
Inventors:
Robert Aslanian, Michael Berlin, Christopher Boyce, Jianhua Chao, Manuel de Lera Ruiz, Pietro Mangiaracina, Kevin McCormick, Mwangi Mutahi, Stuart Rosenblum, Neng-Yang Shih, Daniel Solomon, Wing Tom, Henry Vaccaro, Junying Zheng, Xiaohong Zhu
Publication number: 20070010513
Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(?O)—, —C(?S)—, —(CH2)q—, —C(?NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R1 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.
Type:
Application
Filed:
June 19, 2006
Publication date:
January 11, 2007
Inventors:
Robert Aslanian, Michael Berlin, Ying Huang, Kevin McCormick, Mwangi Mutahi, Neng-Yang Shih, Pauline Ting, Wing Tom, Junying Zheng