Patent number: 6911448
Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ?C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof.
Type:
Grant
Filed:
May 10, 2001
Date of Patent:
June 28, 2005
Assignee:
Solvay Pharmaceuticals B.V.
Inventors:
Roelof W. Feenstra, Johannes A. M. van der Heijden, Cornelis G. Kruse, Stephen K. Long, Gustaaf J. M. van Scharrenburg
Publication number: 20040110741
Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
Type:
Application
Filed:
September 19, 2002
Publication date:
June 10, 2004
Inventors:
Arija A. Bergmanis, Michael Clare, Joyce Z. Crich, Lifeng Geng, Timothy J. Hagen, Gunnar J. Hanson, Stephen Houdek, He Huang, Donna M. Iula, Francis J. Koszyk, Shuyuan Liao, Scott B. Mohler, Maria Nguyen, Richard A. Partis, Michael A. Stealey, Michael B. Tollefson, Richard M. Weier, Xiangdong Xu, Dominique Bonafoux, Theresa R. Fletcher, Bruce C. Hamper, Patrick J. Lennon, Subo Liao, Suzanne Metz, David S. Oburn, Thomas J. Owen, Angela M. Scates, Michael L. Vazquez, Serge G. Wolfson
Publication number: 20040092524
Abstract: The invention concerns compounds corresponding to general formula (I), wherein, in particular: W represents hydrogen, COR6, CSR6, SO2R6, CO(CH2)nR6, (CH2)nR7; X represents CH or N; Y represents (CH2)n, CO, CH2CO, CH═CHCO, CH2CH2CO; Z represents a heterocycle. When Z=pyridine, then Y is other than CO. R1 represents hydrogen, C1-C6 alkyl, halogen OCH3, CF3; R2 and R3, identical or different, represent hydrogen, C1-C6 alkyl; R4 represents a) hydrogen, b) C1-C6 alkyl, c) an aryl, d) a heterocycle; R5 represents hydrogen, COR7R8, SO2R7, CO(CH2)nSR7, CO(CH2)nOR7, CONR7R8, CO(CH2)mCOR7; R6 represents a) a phenyl or a naphthyl, b) a C1-C6 alkyl, a cycloalkyl, c) a heterocycle, d) NR7R8; R7 and R8, identical or different, represent a) hydrogen, C1-C15 alkyl, b) a heterocycle, c) an aryl; n represents 0 to 10; m represents 2 to 10; provided that when Z represents a quinozaline or benzimidazole group, then R5 is other than CH2Ph or methyl and n is other than zero.
Type:
Application
Filed:
November 12, 2003
Publication date:
May 13, 2004
Inventors:
Michel Perez, Marie Lamothe, Anna Kruczynski, Bridget Hill
Patent number: 6646123
Abstract: The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1).
[In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
Type:
Grant
Filed:
April 22, 2002
Date of Patent:
November 11, 2003
Assignee:
Daiichi Pharmaceutical Co., Ltd.
Inventors:
Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama