Title:
PROTEASOME INHIBITORS
Document Type and Number:
WIPO Patent Application WO/2000/043000
Kind Code:
A1
Abstract:
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; R?1¿ is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, or the like; and R?2¿ is hydrogen, COR?13¿ or CH¿2?OR?3a¿, or alternatively R?1¿ and R?2¿ together represent formula (II), wherein X?1¿ is a linkage, substituted or unsubstituted alkylene, substituted or unsubstituted cycloalkylene, or the like; X?2¿ is oxygen, sulfur, or NR?17¿; R?3¿ is as defined for R?3a¿; and R?4¿ is hydroxyl, mercapto, substituted or unsubstituted alkoxy, or the like, or alternatively R?3¿ and R?4 ¿together represent a linkage; and R?5¿ is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or the like.
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Inventors:
YAMAGUCHI HIROYUKI (JP)
ASAI AKIRA (JP)
MIZUKAMI TAMIO (JP)
YAMASHITA YOSHINORI (JP)
AKINAGA SHIRO (JP)
IKEDA SHUN-ICHI (JP)
KANDA YUTAKA (JP)
ASAI AKIRA (JP)
MIZUKAMI TAMIO (JP)
YAMASHITA YOSHINORI (JP)
AKINAGA SHIRO (JP)
IKEDA SHUN-ICHI (JP)
KANDA YUTAKA (JP)
Application Number:
PCT/JP2000/000247
Publication Date:
July 27, 2000
Filing Date:
January 20, 2000
Export Citation:
Assignee:
KYOWA HAKKO KOGYO KK (JP)
YAMAGUCHI HIROYUKI (JP)
ASAI AKIRA (JP)
MIZUKAMI TAMIO (JP)
YAMASHITA YOSHINORI (JP)
AKINAGA SHIRO (JP)
IKEDA SHUN ICHI (JP)
KANDA YUTAKA (JP)
YAMAGUCHI HIROYUKI (JP)
ASAI AKIRA (JP)
MIZUKAMI TAMIO (JP)
YAMASHITA YOSHINORI (JP)
AKINAGA SHIRO (JP)
IKEDA SHUN ICHI (JP)
KANDA YUTAKA (JP)
International Classes:
A61P35/00; A61P43/00; C07C229/46; C07C237/22; C07C271/22; C07C327/22; C07C327/28; C07D305/12; C07K5/06; A61K38/00; (IPC1-7): A61K31/215; A61K31/27; A61K31/337; A61K31/497; A61K31/501; A61K31/506; A61P35/00; A61P43/00; C07C237/10; C07C271/22; C07C327/22; C07C327/28; C07D305/12; C07D405/12
Foreign References:
| JPH0421661A | 1992-01-24 | |||
| EP0768317A1 | 1997-04-16 |
Other References:
LOTFY D. ISMAIL ET AL.: "Isolation and Synthesis of an alpha-Malamic Acid Derivative from Justicia ghiesbreghtiana", JOURNAL OF NATURAL PRODUCTS, vol. 61, no. 9, 1998, pages 1174 - 1176, XP002926028
P. LORENZ ET AL.: "On the Reaction of (S)-Trifluoroacetoxysuccinic Anhydride with Amines to Produce Hydroxysuccinamic (Malamic) Acid Derivatives", JOURNAL FUER PRAKTISCHE CHEMIE CHEMIKER-ZEITUNG, vol. 340, no. 8, 1998, pages 733 - 737, XP002926029
M. BEAR ET AL.: "Synthesis and Polymerization of Benzyl (3R,4R)-3-Methylmalolactonate Via Enzymatic Preparation of the Chriral Precursor", CHIRALITY, vol. 10, no. 8, 1998, pages 727 - 733, XP002926030
M. HAAS ET AL.: "Effect of proteasome inhibitors on monocytic IkappaB-alpha and -beta depletion, NF-kappaB activation and cytokine production", JOURNAL OF LEUKOCYTE BIOLOGY, vol. 63, no. 3, 1998, pages 395 - 404, XP002926031
See also references of EP 1166781A4
P. LORENZ ET AL.: "On the Reaction of (S)-Trifluoroacetoxysuccinic Anhydride with Amines to Produce Hydroxysuccinamic (Malamic) Acid Derivatives", JOURNAL FUER PRAKTISCHE CHEMIE CHEMIKER-ZEITUNG, vol. 340, no. 8, 1998, pages 733 - 737, XP002926029
M. BEAR ET AL.: "Synthesis and Polymerization of Benzyl (3R,4R)-3-Methylmalolactonate Via Enzymatic Preparation of the Chriral Precursor", CHIRALITY, vol. 10, no. 8, 1998, pages 727 - 733, XP002926030
M. HAAS ET AL.: "Effect of proteasome inhibitors on monocytic IkappaB-alpha and -beta depletion, NF-kappaB activation and cytokine production", JOURNAL OF LEUKOCYTE BIOLOGY, vol. 63, no. 3, 1998, pages 395 - 404, XP002926031
See also references of EP 1166781A4
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