公开(公告)号：WO1995012589A1

公开(公告)日：1995-05-11

申请号：PCT/US1994012062

申请日：1994-10-21

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  RATAJCZYK, James, D. ,  CHEMBURKAR, San jay, R. ,  KU, Yi-Yin ,  PATEL, Ramesh, R. ,  BUSSE, Juliette, K. ,  DICKMAN, Daniel, A. ,  PATEL, Hemantkumar, H. ,  SAWICK, David, P.

IPC: C07D333/20

CPC classification number: C07D333/20 ,  C07D307/52

Abstract: A process for preparing a compound of structure (I), where A is oxygen and sulfur and R is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R is alkyl of one to four carbon atoms, comprising coupling a compound of formula (II), where X is bromine or iodine, with an N-hydroxyurea compound of formula (III), in the presence of a palladium catalyst. The compounds of formula (I) are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

Abstract translation: 制备式（I）化合物的方法，其中A是氧和硫，R 1选自氢，卤素，1至6个碳原子的烷基，1至6个碳原子的烷氧基， 和三氟甲基，R 2是1-4个碳原子的烷基，包括式（II）化合物（其中X是溴或碘）与式（III）的N-羟基脲化合物在式 钯催化剂。 式（I）化合物是5-脂氧合酶的抑制剂，因此可用作治疗过敏性和炎性疾病病症的治疗剂。

公开(公告)号：EP0667855B1

公开(公告)日：1999-03-24

申请号：EP94902209.9

申请日：1993-11-05

Applicant: ABBOTT LABORATORIES

Inventor： BASHA, Anwer ,  BHATIA, Pramila ,  BROOKS, Dee, W. ,  CRAIG, Richard, A. ,  RATAJCZYK, James, D. ,  STEWART, Andrew, O.

IPC: C07C275/20 ,  A61K31/17 ,  C07C275/64 ,  C07D307/52

CPC classification number: C07D405/06 ,  C07C275/64 ,  C07D213/61 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D409/06

Abstract: The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.

公开(公告)号：EP0726897A1

公开(公告)日：1996-08-21

申请号：EP94931426.0

申请日：1994-10-21

Applicant: Abbott Laboratories

Inventor： RATAJCZYK, James, D. ,  CHEMBURKAR, San jay, R. ,  KU, Yi-Yin ,  PATEL, Ramesh, R. ,  BUSSE, Juliette, K. ,  DICKMAN, Daniel, A. ,  PATEL, Hemantkumar, H. ,  SAWICK, David, P.

IPC: A61K31 ,  A61P29 ,  A61P37 ,  A61P43 ,  B01J27 ,  B01J31 ,  C07D307 ,  C07D333

CPC classification number: C07D333/20 ,  C07D307/52

Abstract: A process for preparing a compound of structure (I), where A is oxygen and sulfur and R1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula (II), where X is bromine or iodine, with an N-hydroxyurea compound of formula (III), in the presence of a palladium catalyst. The compounds of formula (I) are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

公开(公告)号：EP0667855A1

公开(公告)日：1995-08-23

申请号：EP94902209.0

申请日：1993-11-05

Applicant: ABBOTT LABORATORIES

Inventor： BASHA, Anwer ,  BHATIA, Pramila ,  BROOKS, Dee, W. ,  CRAIG, Richard, A. ,  RATAJCZYK, James, D. ,  STEWART, Andrew, O.

IPC: A61K31 ,  A61P9 ,  A61P11 ,  A61P17 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P37 ,  A61P43 ,  C07C273 ,  C07C275 ,  C07D213 ,  C07D277 ,  C07D307 ,  C07D333 ,  C07D405 ,  C07D409 ,  C07D417

CPC classification number: C07D405/06 ,  C07C275/64 ,  C07D213/61 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D409/06

Abstract: The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.