Global patent index - EP 1091960 A1

EP 1091960 A1 2001-04-18 - BIFUNCTIONAL ANTAGONISTS OF CYTOKINE-SENSITIVE PROTEIN KINASE ACTIVATION CASCADES AND METHODS FOR USE AS ANTI-INFLAMMATORY AGENTS

Title (en)

BIFUNCTIONAL ANTAGONISTS OF CYTOKINE-SENSITIVE PROTEIN KINASE ACTIVATION CASCADES AND METHODS FOR USE AS ANTI-INFLAMMATORY AGENTS

Title (de)

AKTIVIERUNGSKASKADEN-BIFUNKTIONELLE ANTAGONISTEN VON CYTOKIN-EMPFINDLICHEN PROTEIN-KINASEN UND VERFAHREN ZUR VERWENDUNG ALS ENTZÜNDUNGSHEMMENDE MITTEL

Title (fr)

ANTAGONISTES BIFONCTIONNELS DES CASCADES D'ACTIVATION DES KINASES SENSIBLES AUX CYTOKINES ET TECHNIQUE PERMETTANT DE LES UTILISER COMME ANTI-INFLAMMATOIRES

Publication

EP 1091960 A1 (EN)

Application

EP 99931893 A

Priority

  • US 9914320 W
  • US 10702698 A

Abstract (en)

[origin: WO0000491A1] Bifunctional activation cascade antagonist compounds inhibit inflammatory responses associated with TNF- alpha and fibroblast proliferation in vivo and in vitro by blocking activation of both the c-Jun and p38 kinases. The compounds of the invention possess greater than additive activity as compared to the individual constituents of each compound. One such constituent blocks activation of c-Jun kinase while the other blocks activation of p38 kinase, in a non-overlapping manner. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Methods for the use of the novel compounds as anti-imflammatory agents are also described. The methods are expected to be of use in reducing or protecting a vertebrate host against inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression.

IPC 1-7 (main, further and additional classification)

C07D 475/02; A61K 31/505; A61K 31/52; C07D 217/24; C07D 239/96; C07D 401/14; C07D 473/04; C07D 513/04

IPC 8 full level (invention and additional information)

A61K 31/505 (2006.01); A61K 31/52 (2006.01); C07D 217/24 (2006.01); C07D 239/96 (2006.01); C07D 401/14 (2006.01); C07D 473/04 (2006.01); C07D 475/02 (2006.01); C07D 513/04 (2006.01)

CPC (invention and additional information)

C07D 401/14 (2013.01); A61K 31/505 (2013.01); A61K 31/52 (2013.01); C07D 217/24 (2013.01); C07D 239/96 (2013.01); C07D 473/04 (2013.01); C07D 475/02 (2013.01); C07D 513/04 (2013.01)

Combination set (CPC)

  1. A61K 31/505 + A61K 2300/00
  2. A61K 31/52 + A61K 2300/00

Citation (search report)

See references of WO 0000491A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

WO 0000491 A1 20000106; AU 4830799 A 20000117; CA 2335595 A1 20000106; EP 1091960 A1 20010418

INPADOC legal status

2002-05-29 [18D] DEEMED TO BE WITHDRAWN

- Ref Legal Event Code: 18D

- Effective date: 20011119

2001-08-22 [17Q] FIRST EXAMINATION REPORT

- Ref Legal Event Code: 17Q

- Effective date: 20010706

2001-04-18 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 20010123

2001-04-18 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE