Title:
5-LIPOXYGENASE INHIBITORS
Document Type and Number:
WIPO Patent Application WO/1996/011912
Kind Code:
A1
Abstract:
Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein Ar?1� is a heterocyclic moiety which is selected from the group consisting of imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl, benzimidazolyl, which is bonded to X?1� through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C�1-4? alkyl, C�1-4? alkoxy, C�1-4? alkylthio, C�1-4? halo-substituted alkyl, C�1-4? halo-substituted alkoxy, C�1-4? alkylamino and di(C�1-4?) alkylamino; X?1� is a direct bond or C�1-4? alkylene; Ar?2� is phenylene optionally substituted with halo, hydroxy, cyano, amino, C�1-4? alkyl, C�1-4? alkoxy, C�1-4? alkylthio, C�1-4? halo-substituted alkyl and C�1-4? halo-substituted alkoxy; X?2� is -A-X- or -X-A- wherein A is a direct bond or C�1-4? alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar?3� is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C�1-4? alkyl, C�1-4? alkoxy, C�1-4? alkylthio, C�1-4? halo-substituted alkyl, C�1-4? halo-substituted alkoxy, C�1-4? alkylamino and di(C�1-4?) alkylamino; R?1� and R?2� are each C�1-4? alkyl, or together they form a group of formula -D?1�-Z-D?2�- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D?1� and D?2� are C�1-4? alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D?1� and D?2� may be substituted by C�1-3? alkyl; and Y is CONR?3�R?4�, CN, COOR?3�, COR?3� or CSNR?3�R?4�, wherein R?3� and R?4� are each H or C�1-4? alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
Inventors:
Stevens, Rodney W. (Seishiro-cho Handa-shi, Aichi-ken 475, JP)
Mano, Takashi (Seishiro-cho Handa-shi, Aichi-ken 475, JP)
Nakao, Kazunari (Maeda Fujie Higashiura-ch, Chita-gun Aichi-ken 470-21, JP)
Okumura, Yoshiyuki (Shinchi Chita-shi, Aichi-ken 478, JP)
Mano, Takashi (Seishiro-cho Handa-shi, Aichi-ken 475, JP)
Nakao, Kazunari (Maeda Fujie Higashiura-ch, Chita-gun Aichi-ken 470-21, JP)
Okumura, Yoshiyuki (Shinchi Chita-shi, Aichi-ken 478, JP)
Application Number:
PCT/JP1994/001747
Publication Date:
April 25, 1996
Filing Date:
October 18, 1994
Export Citation:
Assignee:
PFIZER PHARMACEUTICALS INC. (1-1 Nishi-shinjuku 2-chom, Shinjuku-ku Tokyo 163-04, JP)
International Classes:
(IPC1-7): C07D233/60; C07D405/12; A61K31/415
Attorney, Agent or Firm:
Kobayashi, Hiroshi (Shinjuku Mitsui Building 1-1, Nishi-shinjuku 2-chom, Shinjuku-ku Tokyo 163-04, JP)
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