WO2000059886A3 - Benzimidazole abd imidazolophyridine derivaties, their preparation and their use as selective modulators of bradykinin b2 (=bk-2) receptors - Google Patents

Benzimidazole abd imidazolophyridine derivaties, their preparation and their use as selective modulators of bradykinin b2 (=bk-2) receptors Download PDF

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Publication number
WO2000059886A3
WO2000059886A3 PCT/US2000/008568 US0008568W WO0059886A3 WO 2000059886 A3 WO2000059886 A3 WO 2000059886A3 US 0008568 W US0008568 W US 0008568W WO 0059886 A3 WO0059886 A3 WO 0059886A3
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Prior art keywords
alkyl
alkylamino
mono
bradykinin
receptors
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PCT/US2000/008568
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French (fr)
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WO2000059886A2 (en
Inventor
Robert W Desimone
Alan Hutchison
Kenneth Shaw
George D Maynard
John M Peterson
Richard Lew
Harry L Brielmann
Original Assignee
Neurogen Corp
Robert W Desimone
Alan Hutchison
Kenneth Shaw
George D Maynard
John M Peterson
Richard Lew
Harry L Brielmann
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by Neurogen Corp, Robert W Desimone, Alan Hutchison, Kenneth Shaw, George D Maynard, John M Peterson, Richard Lew, Harry L Brielmann filed Critical Neurogen Corp
Priority to AU40553/00A priority Critical patent/AU4055300A/en
Priority to EP00919946A priority patent/EP1165518A2/en
Priority to CA002369544A priority patent/CA2369544A1/en
Priority to JP2000609398A priority patent/JP2002541145A/en
Publication of WO2000059886A2 publication Critical patent/WO2000059886A2/en
Publication of WO2000059886A3 publication Critical patent/WO2000059886A3/en

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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

Disclosed are compounds of formula (I) or pharmaceutically acceptable salts thereof wherein: R1 is not 3-fluorobenzyl and represents (C2-C6) alkenyl, aryl (C1-C6)alkyl or heteroaryl (C1-C6)alkyl, OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R2 represents hydrogen, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, amino (C1-C6)alkyl, mono- or di(C1-C6)alkylamino (C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R3 represents (C1-C6)alkyl; R4 represents halogen or trifluoromethyl; R5 and R6 represent hydrogen, trifluoromethyl, triluoromethoxy, cyano, (C1-C6)alkyl, halogen, (C1-C6)alkylamino(C1-C6)alkyl, mono or di(C1-C6)alkylamino(C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or together form a 5 or 6 membered aromatic ring which is optionally substituted. X represents a bond or CH2 which is optionally mono- or disubstituted with a (C1-C6)alkyl or (C1-C6)alkoxy; and A, B, C and D are the same or different and represent CRp or N with the proviso that not more than two of A,B, C and D represent N; which compounds are selective modulators of Bradykinin B2 receptors.
PCT/US2000/008568 1999-04-02 2000-03-31 Benzimidazole abd imidazolophyridine derivaties, their preparation and their use as selective modulators of bradykinin b2 (=bk-2) receptors WO2000059886A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU40553/00A AU4055300A (en) 1999-04-02 2000-03-31 Aryl and heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of Bradykinin B2 receptors
EP00919946A EP1165518A2 (en) 1999-04-02 2000-03-31 Benzimidazole and imidazolopyridine derivatives, their preparation and their use as selective modulators of bradykinin b2 (= bk-2) receptors
CA002369544A CA2369544A1 (en) 1999-04-02 2000-03-31 Aryl and heteroaryl fused aminoalkyl-imidazole derivatives:selective modulators of bradykinin b2 receptors
JP2000609398A JP2002541145A (en) 1999-04-02 2000-03-31 Aryl and heteroaryl fused aminoalkyl-imidazole derivatives: Bradykinin B2 receptor selective modulators

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US28532799A 1999-04-02 1999-04-02
US12750599P 1999-04-02 1999-04-02
US09/285,327 1999-04-02
US60/127,505 1999-04-02

Publications (2)

Publication Number Publication Date
WO2000059886A2 WO2000059886A2 (en) 2000-10-12
WO2000059886A3 true WO2000059886A3 (en) 2001-09-13

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PCT/US2000/008568 WO2000059886A2 (en) 1999-04-02 2000-03-31 Benzimidazole abd imidazolophyridine derivaties, their preparation and their use as selective modulators of bradykinin b2 (=bk-2) receptors

Country Status (5)

Country Link
EP (1) EP1165518A2 (en)
JP (1) JP2002541145A (en)
AU (1) AU4055300A (en)
CA (1) CA2369544A1 (en)
WO (1) WO2000059886A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001229580A1 (en) 2000-01-18 2001-08-14 Nuerogen Corporation Substituted imidazoles as selective modulators of bradykinin b2 receptors
CA2425185A1 (en) * 2000-10-06 2002-04-11 Stephane De Lombaert Benzimidazole and indole derivatives as crf receptor modulators
PA8535601A1 (en) 2000-12-21 2002-11-28 Pfizer BENZIMIDAZOL AND PIRIDILIMIDAZOL DERIVATIVES AS LIGANDOS FOR GABAA
US6903126B2 (en) 2001-07-09 2005-06-07 Schering Ag 1-Aryl-2-N-, S- or O-substituted benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
DE10135050A1 (en) * 2001-07-09 2003-02-06 Schering Ag 1-Ary1-2-N-, S- or O-substituted benzimidazole derivatives, their use for the preparation of medicaments and pharmaceutical preparations containing them
EP1465888A2 (en) 2002-01-10 2004-10-13 Neurogen Corporation Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues
CN1902181A (en) 2003-10-28 2007-01-24 沃泰克斯药物股份有限公司 Benzimidazoles useful as modulators of ion channels
TW201031665A (en) 2009-02-04 2010-09-01 Gruenenthal Gmbh Substituted indole-compound
AR118983A1 (en) * 2019-05-23 2021-11-17 Pharvaris Gmbh CYCLIC BRADYKININ RECEPTOR ANTAGONISTS

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996000730A1 (en) * 1994-06-29 1996-01-11 Smithkline Beecham Corporation Vitronectin receptor antagonists
WO1997011069A1 (en) * 1995-09-18 1997-03-27 Fujisawa Pharmaceutical Co., Ltd. Heterocyclic compounds as bradykinin antagonists
WO2000059905A1 (en) * 1999-04-02 2000-10-12 Neurogen Corporation ARYL AND HETEROARYL FUSED AMINOALKYL-IMIDAZOLE DERIVATIVES: SELECTIVE MODULATORS OF GABAa RECEPTORS
WO2000059887A1 (en) * 1999-04-02 2000-10-12 Neurogen Corporation Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996000730A1 (en) * 1994-06-29 1996-01-11 Smithkline Beecham Corporation Vitronectin receptor antagonists
WO1997011069A1 (en) * 1995-09-18 1997-03-27 Fujisawa Pharmaceutical Co., Ltd. Heterocyclic compounds as bradykinin antagonists
WO2000059905A1 (en) * 1999-04-02 2000-10-12 Neurogen Corporation ARYL AND HETEROARYL FUSED AMINOALKYL-IMIDAZOLE DERIVATIVES: SELECTIVE MODULATORS OF GABAa RECEPTORS
WO2000059887A1 (en) * 1999-04-02 2000-10-12 Neurogen Corporation Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
AHLUWALIA A. & PERRETTI M.: "B1 receptors as a new inflammatory target. Could this B the 1?", TRENDS IN PHARMACOLOGICAL SCIENCES, GB, ELSEVIER TRENDS JOURNAL, CAMBRIDGE, vol. 20, no. 3, March 1999 (1999-03-01), pages 100 - 104, XP004162861, ISSN: 0165-6147 *

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JP2002541145A (en) 2002-12-03
CA2369544A1 (en) 2000-10-12
EP1165518A2 (en) 2002-01-02
AU4055300A (en) 2000-10-23
WO2000059886A2 (en) 2000-10-12

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