Title:
酵素阻害剤
Document Type and Number:
Japanese Patent JP5732408
Kind Code:
B2
Abstract:
Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C═O)—, —S(═O)2—, —C(C═O)O—, —C(C═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O)2NR— wherein R′ is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(C═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
Inventors:
Donald, Alastair, David, Graham
Moffat, David, Festas, Charles
Bellfield, Andrew, James
North, Carl, Leslie
Jones, Stuart, Andrew, Wayne
Moffat, David, Festas, Charles
Bellfield, Andrew, James
North, Carl, Leslie
Jones, Stuart, Andrew, Wayne
Application Number:
JP2011551519A
Publication Date:
June 10, 2015
Filing Date:
February 25, 2010
Export Citation:
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
International Classes:
C07C259/06; A61K31/16; A61K31/44; A61P1/02; A61P1/04; A61P1/16; A61P1/18; A61P3/00; A61P3/10; A61P5/10; A61P5/14; A61P7/00; A61P7/06; A61P9/00; A61P9/10; A61P11/00; A61P11/02; A61P11/06; A61P13/10; A61P13/12; A61P17/00; A61P17/04; A61P17/06; A61P19/00; A61P19/02; A61P21/04; A61P25/00; A61P25/14; A61P25/28; A61P27/02; A61P27/16; A61P29/00; A61P31/00; A61P31/04; A61P35/00; A61P35/02; A61P37/00; A61P37/06; A61P43/00; C07D213/56
Domestic Patent References:
| JP2004509105A | ||||
| JP2004511462A | ||||
| JP2004509941A | ||||
| JP2007519619A | ||||
| JP2011513289A |
Foreign References:
| WO2008040934A1 |
Attorney, Agent or Firm:
Shintaro Nogawa