发明名称 Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors.
摘要 Therapeutically active compositions of matter are described which are useful for treating or preventing diseases and conditions comprising inflammatory diseases including joint inflammation, Crohn's disease, and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said components of its overall chemical structure. Included are compounds of Formula (IA) or (IB): wherein R2a and R2b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R2a and R2b must be independently selected as hydrogen, wherein said substituents comprise moieties including the following:
申请公布号 ZA9810042(B) 申请公布日期 2000.05.03
申请号 ZA19980010042 申请日期 1998.11.03
申请人 PFIZER PRODUCTS INC. 发明人 ANTHONY MARFAT
分类号 A61K31/416;A61K31/496;A61K31/497;A61K31/517;A61K31/52;A61K31/525;A61K31/5377;A61K31/541;A61P1/04;A61P3/10;A61P7/06;A61P9/02;A61P11/00;A61P11/04;A61P11/06;A61P13/12;A61P17/00;A61P17/02;A61P17/06;A61P19/02;A61P27/16;A61P29/00;A61P31/04;A61P35/02;A61P37/06;A61P37/08;C07D231/56 主分类号 A61K31/416
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