Title:
【発明の名称】PDEIV阻害性の2―シアノイミノイミダゾール誘導体
Document Type and Number:
Japanese Patent JP3068208
Kind Code:
B2
Abstract:
PCT No. PCT/EP97/05322 Sec. 371 Date Mar. 19, 1999 Sec. 102(e) Date Mar. 19, 1999 PCT Filed Sep. 24, 1997 PCT Pub. No. WO98/14432 PCT Pub. Date Apr. 9, 1998The present invention concerns 2-cyanoiminoimidazole derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy; R4 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyloxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R4 is -O-R7 or -NH-R8; R5 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R6 is a hydrogen or C1-4alkyl; or R4 and R6, or R4 and R5 taken together may form a bivalent radical; -A-B- is -CR10=CR11- or -CHR10-CHR11-; L is hydrogen; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidinyl; substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.
Inventors:
Freine, Eddie Jean-Edgard
Fernandez-Gadea, Francisco Javier
Andres-Jill, Jose Ignacio
Fernandez-Gadea, Francisco Javier
Andres-Jill, Jose Ignacio
Application Number:
JP51621598A
Publication Date:
July 24, 2000
Filing Date:
September 24, 1997
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
A61K31/00; A61K31/415; A61K31/4164; A61K31/4168; A61P11/00; C07D233/44; A61P11/06; A61P29/00; A61P37/00; A61P37/08; C07D233/48; C07D233/88; C07D405/12; (IPC1-7): C07D233/44; A61K31/4164; A61P11/06; A61P37/08; C07D233/88
Attorney, Agent or Firm:
Heiyoshi Odashima (1 person outside)