Patent number: 7057049
Abstract: This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4, and Y5 are as defined in the specification.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
June 6, 2006
Assignee:
Pharmacia Corporation
Inventors:
Kimberley C. Allen, Dennis K. Anderson, John E. Baldus, Todd Boehlow, Jerry D. Clark, Dan R. Dukesherer, Albert D. Edney, Tom Fevig, Sastry Kunda, Jon P. Lawson, Patrick H. Lau, Lisa L. McDermott, Michael K. Mao, Jodi L. Moe, Partha Mudipalli, Win Naing, Shaun R. Selness, Christine B. Seymour, Tobin C. Schilke, Shekhar Viswanath, John K. Walker, Gopichand Yalamanchili
Patent number: 7030138
Abstract: A compound of a formula (1) and pharmacologically acceptable salts thereof: wherein R1 represents hydrogen, halogen, alkyl or hydroxyl; R2 represents hydrogen or halogen; R3 represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R4 and R5 represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R6 represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R7 and R8 represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.
Type:
Grant
Filed:
October 3, 2003
Date of Patent:
April 18, 2006
Assignee:
Sankyo Company, Limited
Inventors:
Koichi Fujimoto, Naoki Tanaka, Ikuko Shimada, Fumitoshi Asai
Patent number: 6924374
Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)R6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetra-hydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)2, and pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.
Type:
Grant
Filed:
December 22, 2000
Date of Patent:
August 2, 2005
Assignee:
A. Carlsson Research AB
Inventors:
Clas Sonesson, Ingela Marianne Svan, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
Patent number: 6875831
Abstract: The invention pertains to a compound of formula (I), (II) or (III) wherein R1 and R2 are independently of each other hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; A is a group capable of forming a stable free nitroxyl radical A*, which is bound via its oxygen atom to the carbon atom; Y is O, NR3 or CHR3—Xa, wherein Xa is O, S or NR3; R3 is hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; Q1 is an organic or inorganic radical, derived from a compound having at least one functional group being capable of reacting with a hydroxy group; Q2 is an organic radical derived from a mono or polyfunctional alcohol, mono or polyfunctional aminoalcohol, mono or polyfunctional amine
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
April 5, 2005
Assignee:
CIBA Specialty Chemicals Corp.
Inventors:
Andreas Kramer, Peter Nesvadba, Marie-Odile Zink, Wiebke Wunderlich