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1. WO2000043000 - PROTEASOME INHIBITORS

Publication Number WO/2000/043000
Publication Date 27.07.2000
International Application No. PCT/JP2000/000247
International Filing Date 20.01.2000
Chapter 2 Demand Filed 20.01.2000
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07C 229/46 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
46having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 237/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 271/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
22to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 327/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
327Thiocarboxylic acids
20Esters of monothiocarboxylic acids
22having carbon atoms of esterified thiocarboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 327/28 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
327Thiocarboxylic acids
20Esters of monothiocarboxylic acids
28having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07C 229/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
46having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 237/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 2601/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
02with a three-membered ring
C07C 271/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
22to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 327/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
327Thiocarboxylic acids
20Esters of monothiocarboxylic acids
22having carbon atoms of esterified thiocarboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
Applicants
  • KYOWA HAKKO KOGYO CO., LTD. [JP/JP]; 6-1, Ohtemachi 1-chome Chiyoda-ku Tokyo 100-8185, JP (AllExceptUS)
  • YAMAGUCHI, Hiroyuki [JP/JP]; JP (UsOnly)
  • ASAI, Akira [JP/JP]; JP (UsOnly)
  • MIZUKAMI, Tamio [JP/JP]; JP (UsOnly)
  • YAMASHITA, Yoshinori [JP/JP]; JP (UsOnly)
  • AKINAGA, Shiro [JP/JP]; JP (UsOnly)
  • IKEDA, Shun-ichi [JP/JP]; JP (UsOnly)
  • KANDA, Yutaka [JP/JP]; JP (UsOnly)
Inventors
  • YAMAGUCHI, Hiroyuki; JP
  • ASAI, Akira; JP
  • MIZUKAMI, Tamio; JP
  • YAMASHITA, Yoshinori; JP
  • AKINAGA, Shiro; JP
  • IKEDA, Shun-ichi; JP
  • KANDA, Yutaka; JP
Priority Data
11/1239120.01.1999JP
11/28853908.10.1999JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PROTEASOME INHIBITORS
(FR) INHIBITEURS DE PROTEASOME
Abstract
(EN)
Proteasome inhibitors containing as the active ingredient carboxylic acid derivatives represented by general formula (I) or pharmacologically acceptable salts thereof: wherein m and n are each independently an integer of 0 to 10; p is 0 or 1; R1 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, or the like; and R2 is hydrogen, COR13 or CH2OR3a, or alternatively R1 and R2 together represent formula (II), wherein X1 is a linkage, substituted or unsubstituted alkylene, substituted or unsubstituted cycloalkylene, or the like; X2 is oxygen, sulfur, or NR17; R3 is as defined for R3a; and R4 is hydroxyl, mercapto, substituted or unsubstituted alkoxy, or the like, or alternatively R3 and R4 together represent a linkage; and R5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or the like.
(FR)
La présente invention concerne des inhibiteurs de protéasome contenant comme principe actif des dérivés d'acide carboxylique représentés par la formule générale (I), ou des sels de ceux-ci acceptables sur le plan pharmaceutique. Dans cette formule, m et n représentent individuellement un nombre entier compris entre 0 et 10; p est égale à 0 ou 1; R1 représente hydrogène, alkyle substitué ou non, cycloalkyle substitué ou non, ou analogue; R2 représente hydrogène, COR13 ou CH2OR3a, ou éventuellement R1 et R2 représentent ensemble formule (II), où X1 représente une liaison, alkylène substitué ou non, ou analogue; X2 représente oxygène, soufre, ou NR17; R4 représente hydroxyle, mercapto, alcoxy substitué ou non, ou analogue, ou éventuellement R3 et R4 représentent ensemble une liaison; et R5 représente hydrogène, alkyle substitué ou non, alcényle substitué ou non, ou analogue.
Also published as
US09889519
Latest bibliographic data on file with the International Bureau