公开(公告)号：US20050215553A1

公开(公告)日：2005-09-29

申请号：US11009249

申请日：2004-12-10

Applicant: Neerja Bhatnagar ,  Pierre Broto ,  Jean-Francois Gourvest ,  Jacques Mauger

Inventor： Neerja Bhatnagar ,  Pierre Broto ,  Jean-Francois Gourvest ,  Jacques Mauger

IPC: A61K31/50 ,  A61K31/501 ,  A61K31/5377 ,  A61P1/02 ,  A61P3/14 ,  A61P9/00 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/02 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  C07B61/00 ,  C07D237/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07K5/06 ,  G01N33/53

CPC classification number: C07K5/06026 ,  C07B2200/11 ,  C07D237/04 ,  C40B40/00

Abstract: The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of the compounds of formula (I), pharmaceutical compositions, and methods for the preparation of combinatorial libraries and the compounds of formula (I) are also disclosed and claimed.

Abstract translation: 本发明公开并要求具有式（I）的六氢哒嗪-3-羧酸酰肼和腙作为蛋白酶和激酶的抑制剂，以及使用所述式（I）化合物预防或治疗某些心血管，中枢神经系统的方法 ，炎症和骨疾病以及传染病和某些癌症。 还公开并要求保护式（I）化合物的组合文库，药物组合物和制备组合文库和式（I）化合物的方法。

公开(公告)号：US07279480B2

公开(公告)日：2007-10-09

申请号：US11009249

申请日：2004-12-10

Applicant: Neerja Bhatnagar ,  Pierre Broto ,  Jean-Francois Gourvest ,  Jacques Mauger

Inventor： Neerja Bhatnagar ,  Pierre Broto ,  Jean-Francois Gourvest ,  Jacques Mauger

IPC: C07D237/04 ,  A61K31/501 ,  A61K31/50

CPC classification number: C07K5/06026 ,  C07B2200/11 ,  C07D237/04 ,  C40B40/00

Abstract: The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of the compounds of formula (I), pharmaceutical compositions, and methods for the preparation of combinatorial libraries and the compounds of formula (I) are also disclosed and claimed.

Abstract translation: 本发明公开并要求具有式（I）的六氢哒嗪-3-羧酸酰肼和腙作为蛋白酶和激酶的抑制剂，以及使用所述式（I）化合物预防或治疗某些心血管，中枢神经系统的方法 ，炎症和骨疾病以及传染病和某些癌症。 还公开并要求保护式（I）化合物的组合文库，药物组合物和制备组合文库和式（I）化合物的方法。

公开(公告)号：US5476840A

公开(公告)日：1995-12-19

申请号：US133020

申请日：1993-12-03

Applicant: Pierre Broto ,  Giles Hamon ,  Eve Mahe ,  Dung Le-Nguyen

Inventor： Pierre Broto ,  Giles Hamon ,  Eve Mahe ,  Dung Le-Nguyen

IPC: A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  C07K1/04 ,  C07K1/113 ,  C07K7/06 ,  C07K14/575 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

CPC classification number: C07K14/57536

Abstract: New peptidic derivatives having the general formula (I): X.sub.1 X.sub.2 X.sub.3 Ile X.sub.5 X.sub.6 wherein X.sub.1 is hydrogen, a rest of histidin, of acetyl-histidin or of D-histidin, X.sub.2 is a rest of alanin, of leucin, of tryptophan, of phenylalanin as well as their homologs in D series, X.sub.3 is a rest of alanin as well as its D series homolog, X.sub.5 is a rest of isoleucin, of alanin, of valin, of norleucin, of leucin and of aspanic acid as well as their D series homologs, X.sub.6 is a rest of tryptophan, of leucin, of isoleucin, of norleucin and their D series homologs, method for the preparation and application of such new derivatives as medicaments.

Abstract translation: PCT No.PCT / FR93 / 00145 Sec。 371日期1993年12月3日第 102（e）日期1993年12月3日PCT提交1993年2月11日PCT公布。 公开号WO93 / 16104 日期：1993年8月19日。具有通式（I）的新型肽衍生物：X1 X2 X3 Ile X5 X6其中X1为氢，其余组氨酸为乙酰基 - 组氨酸或D-组氨酸，X2为其余的丙氨酸 ，亮氨酸，色氨酸，苯丙氨酸以及它们在D系列中的同系物，X3是其余的丙氨酸及其D系列同系物，X5是其余的异亮氨酸，丙氨酸，缬氨酸，正亮氨酸，亮氨酸 以及它们的D系列同系物，X6是其余的色氨酸，亮氨酸，异亮氨酸，正亮氨酸及其D系列同系物，制备和应用这些新衍生物作为药物的方法。