Publication number: 20080188485
Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.
Type:
Application
Filed:
March 26, 2008
Publication date:
August 7, 2008
Inventors:
Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
Patent number: 7384944
Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.
Type:
Grant
Filed:
September 23, 2003
Date of Patent:
June 10, 2008
Assignee:
Schering Corporation
Inventors:
Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
Patent number: 7041666
Abstract: Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(?CH2)CH3, —C?C—CH3, —CH?C(CH3)2, or —CH?CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
May 9, 2006
Assignee:
Schering Corporation
Inventors:
Julius J. Matasi, John P. Caldwell, Deen Tulshian, Lisa S. Silverman, Bernard R. Neustadt
Patent number: 6897216
Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of form
Type:
Grant
Filed:
May 30, 2003
Date of Patent:
May 24, 2005
Assignee:
Schering Corporation
Inventors:
Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil