Abstract: 4-Substituted-3-substituted-amino-cyclobutyl-3-ene-1,2-diones having the Formula (I):
wherein R1, R2, R3, R4, R5, A and W are as defined in the specification which compounds relaxes smooth muscles.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
October 15, 2002
Assignee:
American Home Products
Inventors:
John A. Butera, Joseph R. Lennox, Douglas J. Jenkins
Abstract: 4-Substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones having the Formula (I):
wherein R1, R2, R3, R4, R5, A and W are as defined in the specification which compounds relaxes smooth muscles.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
October 8, 2002
Assignee:
American Home Products
Inventors:
John A. Butera, Joseph R. Lennox, Douglas J. Jenkins
Abstract: The invention is a method of treating, inhibiting or controlling a ras-associated disease by inhibiting farnesyl-protein transferase(FPTase) enzyme, treating ras oncogene-dependent tumors, which include cancers of pancreas, breast, lung, colon, epidermis, prostate, bladder, thyroid, myelodysplastic tumors and myeloid leukemia; controlling metastasis, suppressing angiogenesis, inducing apoptosis, and in treating Ras-associated proliferative diseases other than cancer, such as restenosis, neuro-fibromatosis, endometriosis, and psoriasis, in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound of Formula I:
or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, Q, a, and b are defined in the specification.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
June 11, 2002
Assignee:
American Cyanamid Company
Inventors:
Semiramis Ayral-Kaloustian, Douglas Bruce Kitchen, Andrei Shavnya
Abstract: Compounds of the Formulae (I) and (II):
wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
May 21, 2002
Assignee:
American Home Products Corporation
Inventors:
Schuyler A. Antane, John A. Butera, Joseph R. Lennox
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: 4-Substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones having the Formula (I):
wherein R1, R2, R3, R4, R5, A and W are as defined in the specification which compounds relaxes smooth muscles.
Type:
Grant
Filed:
November 15, 2000
Date of Patent:
April 23, 2002
Assignee:
American Home Products Corporation
Inventors:
John A. Butera, Joseph R. Lennox, Douglas J. Jenkins
Abstract: The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects of chemotherapeutic drugs.
Type:
Grant
Filed:
May 27, 1999
Date of Patent:
April 16, 2002
Assignee:
American Cyanamid Company
Inventors:
Sridhar Krishna Rabindran, Haiyin He, Lee Martin Greenberger
Abstract: Compounds of the Formulae (I) and (II):
wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.
Type:
Grant
Filed:
December 3, 1999
Date of Patent:
September 11, 2001
Assignee:
American Home Products Corporation
Inventors:
Schuyler A. Antane, John A. Butera, Joseph R. Lennox
Abstract: This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, antihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sup.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.7 and R.sup.8 are independently OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl, phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13, --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.sup.
Abstract: The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.
Type:
Grant
Filed:
June 28, 1999
Date of Patent:
February 8, 2000
Assignee:
American Cyanamid Company
Inventors:
Mark E. Salvati, Nancy H. Eudy, William A. Hallett, Dennis William Powell
Abstract: This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, andihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sup.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl; R.sup.7 and R.sup.8 are independently hydrogen OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl, phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13, --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.
Abstract: This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, antihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.7 and R.sup.8 are independently OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13 --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.sup.12 OCOOR.