Patent number: 6506758
Abstract: A compound of formula (I):
or a salt thereof, or a solvate thereof, wherein:
A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group;
Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group;
R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and
R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carbox
Type:
Grant
Filed:
October 11, 2001
Date of Patent:
January 14, 2003
Assignees:
SmithKline Beecham Laboratoires Pharmceutiques, SmithKline Beecham SpA
Inventors:
Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler, Pietro A T Novella
Patent number: 6469029
Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I:
or pharmaceutically acceptable salts thereof; wherein
Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino;
X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and
R1 R2 and R3 are independently hydrogen or C1-3 alkyl.
Type:
Grant
Filed:
September 13, 2000
Date of Patent:
October 22, 2002
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
Patent number: 6436957
Abstract: Compounds of the formula
where W is
n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or -Q-R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR9, —CO2R9, —CONR9R10, —OR9, —SO2NR9R10, or —S(O)qR9; R8 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkyl-aryl; q i
Type:
Grant
Filed:
October 23, 2000
Date of Patent:
August 20, 2002
Assignee:
Pfizer Inc.
Inventors:
John Eugene Macor, Martin James Wythes
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