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1. WO1996002549 - SUBSTITUTED THIAZOLO[3,2-$g(a)]AZEPINE DERIVATIVE

Publication Number WO/1996/002549
Publication Date 01.02.1996
International Application No. PCT/JP1995/001139
International Filing Date 07.06.1995
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07D 513/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07K 5/078 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
078the first amino acid being heterocyclic, e.g. Pro, His, Trp
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07D 513/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07K 5/06139
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06139with the first amino acid being heterocyclic
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of products other than chlorine, adipic acid, caprolactam, or chlorodifluoromethane, e.g. bulk or fine chemicals or pharmaceuticals
55Synthetic design, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • EISAI CO., LTD. [JP/JP]; 6-10, Koishikawa 4-chome Bunkyo-ku Tokyo 112-88, JP (AllExceptUS)
  • OINUMA, Hitoshi [JP/JP]; JP (UsOnly)
  • SUDA, Shinji [JP/JP]; JP (UsOnly)
  • YONEDA, Naoki [JP/JP]; JP (UsOnly)
  • KOTAKE, Makoto [JP/JP]; JP (UsOnly)
  • MIZUNO, Masanori [JP/JP]; JP (UsOnly)
  • MATSUSHIMA, Tomohiro [JP/JP]; JP (UsOnly)
  • FUKUDA, Yoshio [JP/JP]; JP (UsOnly)
  • SAITO, Mamoru [JP/JP]; JP (UsOnly)
  • MATSUOKA, Toshiyuki [JP/JP]; JP (UsOnly)
  • ADACHI, Hideyuki [JP/JP]; JP (UsOnly)
  • NAMIKI, Masayuki [JP/JP]; JP (UsOnly)
  • SUDO, Takeshi [JP/JP]; JP (UsOnly)
  • MIYAKE, Kazutoshi [JP/JP]; JP (UsOnly)
  • OKITA, Makoto [JP/JP]; JP (UsOnly)
Inventors
  • OINUMA, Hitoshi; JP
  • SUDA, Shinji; JP
  • YONEDA, Naoki; JP
  • KOTAKE, Makoto; JP
  • MIZUNO, Masanori; JP
  • MATSUSHIMA, Tomohiro; JP
  • FUKUDA, Yoshio; JP
  • SAITO, Mamoru; JP
  • MATSUOKA, Toshiyuki; JP
  • ADACHI, Hideyuki; JP
  • NAMIKI, Masayuki; JP
  • SUDO, Takeshi; JP
  • MIYAKE, Kazutoshi; JP
  • OKITA, Makoto; JP
Agents
  • FURUYA, Kaoru ; Nihonbashi TM Building 1-8-11, Nihonbashi-Horidomecho Chuo-ku Tokyo 103, JP
Priority Data
6/16548118.07.1994JP
6/19918024.08.1994JP
6/30646809.12.1994JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) SUBSTITUTED THIAZOLO[3,2-$g(a)]AZEPINE DERIVATIVE
(FR) DERIVE DE THIAZOLO[3,2-$g(a)]AZEPINE A SUBSTITUTION
Abstract
(EN)
A substituted thiazolo[3,2-$g(a)]azepine derivative represented by general formula (I) and having the effect of inhibiting an agiotensin I-converting enzyme and an atrial natriuretic peptide hydrolase, wherein R1 represents hydrogen or a thiol-protective group; R2 represents hydrogen, lower alkyl, optionally substituted aryl, optionally substituted heteroaryl, lower alkoxy or lower alkylthio; R3, R4 and R5 represent each independently hydrogen, lower alkyl, lower alkoxy, lower alkylthio, etc., provided the case where all of R3, R4 and R5 are hydrogen atoms at the same time is excepted; R6 and R7 represent each independently hydrogen or lower alkyl; R8 represents hydrogen or a carboxyl-protective group; and m and n represent each independently 0, 1 or 2.
(FR)
L'invention se rapporte à un dérivé de thiazolo[3,2-$g(a)]azépine à substitution représenté par la formule (I) et ayant pour effet d'inhiber une enzyme convertissant l'angiotensine I et une hydrolase auriculaire de peptide natriurétique. Dans cette formule, R1 représente hydrogène ou un groupe protecteur de thiol; R2 représente hydrogène, alkyle inférieur, aryle éventuellemnt substitué, hétéroaryle éventuellement substitué, alcoxy inférieur ou alkylthio inférieur; R3, R4 et R5 représentent chacun, indépendamment, hydrogène, alkyle inférieur, alcoxy inférieur, alkylthio inférieur, etc., à l'exception du cas où les R3, R4 et R5 sont tous en même temps des atomes d'hydrogène; R6 et R7 représentene chacun, indépendamment, hydrogène ou alkyle inférieur; R8 représente hydrogène ou un groupe protecteur de carboxyle, et m et n représentent chacun indépendamment 0, 1 ou 2.
Also published as
FI20011154
FI961199
NO19961051
NZ287557
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