Title:
【発明の名称】ホスホジエステラーゼ阻害剤としての三置換フェニル誘導体およびそれらの製造方法
Document Type and Number:
Japanese Patent JPH08505158
Kind Code:
A
Abstract:
Compounds of general formula (1) are described wherein Y is a halogen atom or a group -OR1, where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R7)-, where R7 is a hydrogen atom or an alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 and R4, which may be the same or different, is each a hydrogen atom or an alkyl, -CO2R8 (where R8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), -CONR9R10 (where R9 and R10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), -CSNR9R10, -CN, -CH2CN group; Z is -(CH2)n- (where n is zero or an integer 1, 2 or 3; R5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R6 is a hydrogen atom or a hydroxyl group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
Inventors:
Valero, Graham John
Cole, Valerie Anne
Alexander Ricky Peter
Cole, Valerie Anne
Alexander Ricky Peter
Application Number:
JP51974894A
Publication Date:
June 04, 1996
Filing Date:
March 09, 1994
Export Citation:
Assignee:
Celtec Therapeutics Limited
International Classes:
A01N43/40; A01N43/48; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/4418; A61K31/495; A61K31/505; A61P11/08; A61P29/00; A61P43/00; C07C41/20; C07C43/235; C07C43/247; C07C59/72; C07C67/303; C07C67/343; C07C69/734; C07C69/736; C07C209/10; C07C209/68; C07C211/52; C07C237/08; C07C253/30; C07C255/32; C07C255/37; C07C319/20; C07C323/09; C07C323/20; C07D239/26; C07C323/62; C07C327/38; C07D213/30; C07D213/34; C07D213/56; C07D213/57; C07D213/61; C07D213/73; C07D237/08; C07D241/12; (IPC1-7): C07C43/235; A61K31/44; A61K31/495; A61K31/505; C07C41/20; C07C43/247; C07C59/72; C07C67/303; C07C67/343; C07C69/734; C07C69/736; C07C209/10; C07C209/68; C07C211/52; C07C237/08; C07C253/30; C07C255/32; C07C255/37; C07C319/20; C07C323/09; C07C323/20; C07C323/62; C07C327/38; C07D213/30; C07D213/34; C07D213/56; C07D213/57; C07D213/61; C07D239/26; C07D241/12
Attorney, Agent or Firm:
Keiichi Ota