Patent number: 6562857
Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure
wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—;
n=1-5; p=1-4; q=1-4;
R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA;
RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R5 is hydrogen, alkyl, or substituted alkyl;
R6 is hydrogen, alkyl, substituted alkyl, or CORB,
RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino
Type:
Grant
Filed:
January 9, 2002
Date of Patent:
May 13, 2003
Assignee:
Wyeth
Inventors:
Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
Patent number: 6541503
Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by ca
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
April 1, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
Patent number: 6302837
Abstract: A compound selected from those of formula (I):
wherein:
X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description,
Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases,
T represents nitrogen, carbon, or CH,
A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description,
W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino,
U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms,
V1 represents arylene, heteroarylene,or heterocycloalkylene,
U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms,
V2 represents aryl, heteroaryl, or heterocycloalkyl,
Ra, Rb, Rc, which may be identical or different, each independently of the others r
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
October 16, 2001
Assignee:
Adir et Compagnie
Inventors:
Guillaume De Nanteuil, Christine Lila, Tony Verbeuren, Alain Rupin
Patent number: 6166064
Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are as defined in the description, R.sup.2 being an aromatic group, useful in the treatment and condition selected from the group consisting of the group meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzeimer's disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including human.
Type:
Grant
Filed:
July 16, 1999
Date of Patent:
December 26, 2000
Assignee:
Pfizer Inc
Inventors:
Mark Anthony Dombroski, James Frederick Eggler
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