Patent number: 6720325
Abstract: Compounds of the formula
or a pharmaceutically acceptable salt or isomer thereof, wherein:
Q, X and Z are CH or N;
R, R4—R7 and R13 are H or alkyl;
R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—;
R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—;
or R2 and R3 together are ═O, ═NOR10, ═N—NR11R12 or ═CH-alkyl;
R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, al
Type:
Grant
Filed:
March 27, 2002
Date of Patent:
April 13, 2004
Assignee:
Schering Corporation
Inventor:
Michael W. Miller
Patent number: 6689765
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, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV o
Type:
Grant
Filed:
January 30, 2002
Date of Patent:
February 10, 2004
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: 6602885
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 H, alkyl or alkenyl;
R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl;
R3 is optionally substituted phenyl, heteroaryl or naphthyl;
R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2;
R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and
R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
August 5, 2003
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, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
Patent number: 6391865
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:
May 1, 2000
Date of Patent:
May 21, 2002
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, Eric Gilbert, Marc A. Labroli
Patent number: 6387930
Abstract: The use of CCR5 antagonists of the formula
or a pharmaceutically acceptable salt thereof, wherein
X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—,
R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;
R1 is H, alkyl or alkenyl;
R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl;
R3 is optionally substituted phenyl, heteroaryl or naphthyl;
R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2;
R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and
R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.
Type:
Grant
Filed:
May 1, 2000
Date of Patent:
May 14, 2002
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, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
