Title:
SUBSTITUTED IMIDAZOLES AS DUAL HISTAMINE H1 AND H3 AGONISTS OR ANTAGONISTS
Document Type and Number:
WIPO Patent Application WO2002044141
Kind Code:
A3
Abstract:
The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, nasal congestion, inflammatory and CNS-related diseases and others.
Inventors:
SHIH NENG-YANG
ASLANIAN ROBERT G
SOLOMON DANIEL M
ROSENBLUM STUART B
MUTAHI MWANGI WA
TOM WING C
MC CORMICK KEVIN D
PIWINSKI JOHN J
WOLIN RONALD
ASLANIAN ROBERT G
SOLOMON DANIEL M
ROSENBLUM STUART B
MUTAHI MWANGI WA
TOM WING C
MC CORMICK KEVIN D
PIWINSKI JOHN J
WOLIN RONALD
Application Number:
PCT/US2001/029062
Publication Date:
November 07, 2002
Filing Date:
September 18, 2001
Export Citation:
Assignee:
SCHERING CORP (US)
International Classes:
A61K31/454; A61K31/4545; A61K31/496; A61P1/00; A61P3/04; A61P9/00; A61P11/00; A61P25/00; A61P27/16; A61P29/00; A61P37/00; A61P37/08; A61P43/00; C07D213/38; C07D233/54; C07D401/06; C07D233/64; C07D401/12; C07D401/14; C07D403/06; (IPC1-7): C07D403/06; C07D401/14; C07D401/06; C07D401/12; A61P29/00; A61P37/00; A61K31/415; A61K31/44; C07D233/54; C07D213/38; C07D403/06
Domestic Patent References:
| WO2000023438A1 | 2000-04-27 |
Foreign References:
| US5182294A | 1993-01-26 | |||
| EP0289227A1 | 1988-11-02 | |||
| EP0468885A1 | 1992-01-29 | |||
| US5869479A | 1999-02-09 |
Other References:
CHEMICAL ABSTRACTS, vol. 121, no. 7, 1994, Columbus, Ohio, US; abstract no. 83338, GIZOR ET AL: "Process for production of new 4-methyl-2-imidazolinone derivatives for treatment of cerebrovascular diseases and hypoxia and pharmaceutical preparations containing them" XP002205148
HULS A ET AL: "Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 6, no. 16, 20 August 1996 (1996-08-20), pages 2013 - 2018, XP004135646, ISSN: 0960-894X
BUSCHAUER A: "IMIDAZOLYLALKYLGUANIDINE MIT DIARYL-PARTIALSTRUKTUREN IMIDAZOLYLALKYLGUANIDINES WITH DIARYL STRUCTURAL PARTS", SCIENTIA PHARMACEUTICA, OESTERREICHISCHE APOTHEKER VERLAGSGESELLSCHAFT,, AT, vol. 56, no. 2, 1988, pages 81 - 88, XP001062163, ISSN: 0036-8709
NISHIKAWA ET AL: "acrylamide derivatives as antiallergic agents III Synthesis and structure activity relationships of N-[4-(4-diphenylmethyl-1-piperazinyl)butyl]- and N-[4-(4-diphenylmethylene-1-piperidyl)butyl]-3-heteroarylacrylamides", CHEMICAL AND PHARMACEUTICAL BULLETIN, vol. 37, no. 3, 1989, JP, pages 684 - 687, XP001084111
WALCZYNSKI: "non-imidazole histamine H3 ligands. Part I. Synthesis of 2-(1-piperazinyl)-and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives as H3-antagonists with H1 blocking activities", IL FARMACO, vol. 54, 1999, NL, pages 684 - 694, XP002204857
HULS A ET AL: "Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 6, no. 16, 20 August 1996 (1996-08-20), pages 2013 - 2018, XP004135646, ISSN: 0960-894X
BUSCHAUER A: "IMIDAZOLYLALKYLGUANIDINE MIT DIARYL-PARTIALSTRUKTUREN IMIDAZOLYLALKYLGUANIDINES WITH DIARYL STRUCTURAL PARTS", SCIENTIA PHARMACEUTICA, OESTERREICHISCHE APOTHEKER VERLAGSGESELLSCHAFT,, AT, vol. 56, no. 2, 1988, pages 81 - 88, XP001062163, ISSN: 0036-8709
NISHIKAWA ET AL: "acrylamide derivatives as antiallergic agents III Synthesis and structure activity relationships of N-[4-(4-diphenylmethyl-1-piperazinyl)butyl]- and N-[4-(4-diphenylmethylene-1-piperidyl)butyl]-3-heteroarylacrylamides", CHEMICAL AND PHARMACEUTICAL BULLETIN, vol. 37, no. 3, 1989, JP, pages 684 - 687, XP001084111
WALCZYNSKI: "non-imidazole histamine H3 ligands. Part I. Synthesis of 2-(1-piperazinyl)-and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives as H3-antagonists with H1 blocking activities", IL FARMACO, vol. 54, 1999, NL, pages 684 - 694, XP002204857
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