BR9916965A - Compostos antagonistas de receptores não peptìdicos de glp-1, seus derivados, composto útil derivado dos mesmos, composição farmacêutica, método para regular a secreção de insulina em mamìferos, método de inibição da atividade de glp-1, método de inibição da ligação de glp-1 ao receptor de glp-1 e método de inibição da ativação do receptor de glp-1 - Google Patents

Compostos antagonistas de receptores não peptìdicos de glp-1, seus derivados, composto útil derivado dos mesmos, composição farmacêutica, método para regular a secreção de insulina em mamìferos, método de inibição da atividade de glp-1, método de inibição da ligação de glp-1 ao receptor de glp-1 e método de inibição da ativação do receptor de glp-1

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Publication number
BR9916965A
BR9916965A BR9916965-7A BR9916965A BR9916965A BR 9916965 A BR9916965 A BR 9916965A BR 9916965 A BR9916965 A BR 9916965A BR 9916965 A BR9916965 A BR 9916965A
Authority
BR
Brazil
Prior art keywords
glp
receptor
inhibiting
peptide
binding
Prior art date
Application number
BR9916965-7A
Other languages
English (en)
Inventor
Larry Kenneth Truesdale
Richard A Bychowski
Javier Gonzalez
Atsuo Kuki
Ranjan Jagath Rajapakse
Min Teng
Dan Kiel
Daljit S Dhanoa
Yufeng Hong
Tso-Sheng Chou
Anthony L Ling
Michael David Johnson
Vlad Edward Gregor
Original Assignee
Agouron Pharma
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.)
Filing date
Publication date
Application filed by Agouron Pharma filed Critical Agouron Pharma
Publication of BR9916965A publication Critical patent/BR9916965A/pt

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems

Abstract

"COMPOSTOS ANTAGONISTAS DE RECEPTORES NãO PEPTìDICOS DE GLP-1, SEUS DERIVADOS, COMPOSTO úTIL DERIVADO DOS MESMOS, COMPOSIçãO FARMACêUTICA, MéTODO PARA REGULAR A SECREçãO DE INSULINA EM MAMìFEROS, MéTODO DE INIBIçãO DA ATIVIDADE DE GLP-1, MéTODO DE INIBIçãO DA LIGAçãO DE GLP-1 AO RECEPTOR DE GLP-1 E MéTODO DE INIBIçãO DA ATIVAçãO DO RECEPTOR DE GLP-1". Compostos não peptídicos que agem como antagonistas do hormónio intestinal peptídio 1 do tipo glucagon (GLP-1) que possuem preferencialmente 9H-<225>-carbolina. Os compostos apresentam propriedades físicas, químicas e biológicas vantajosas e inibem a ligação do peptídio GLP1 ao receptor de GLP-1 e/ou impedem a ativação do receptor pelo GLP-1 ligado. A invenção também refere-se a um método de inibição da ligação de GLP-1 ao receptor de GLP-1 e a um método de inibição da ativação do receptor de GLP-1. Também são descritos os compostos intermediários úteis para a formação de antagonistas de receptor de GLP-1 não peptídicos.
BR9916965-7A 1998-12-10 1999-12-08 Compostos antagonistas de receptores não peptìdicos de glp-1, seus derivados, composto útil derivado dos mesmos, composição farmacêutica, método para regular a secreção de insulina em mamìferos, método de inibição da atividade de glp-1, método de inibição da ligação de glp-1 ao receptor de glp-1 e método de inibição da ativação do receptor de glp-1 BR9916965A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11173698P 1998-12-10 1998-12-10
PCT/US1999/029065 WO2000033839A1 (en) 1998-12-10 1999-12-08 Non-peptide antagonists of glp-1 receptor and methods of use

Publications (1)

Publication Number Publication Date
BR9916965A true BR9916965A (pt) 2001-11-06

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR9916965-7A BR9916965A (pt) 1998-12-10 1999-12-08 Compostos antagonistas de receptores não peptìdicos de glp-1, seus derivados, composto útil derivado dos mesmos, composição farmacêutica, método para regular a secreção de insulina em mamìferos, método de inibição da atividade de glp-1, método de inibição da ligação de glp-1 ao receptor de glp-1 e método de inibição da ativação do receptor de glp-1

Country Status (14)

Country Link
US (1) US6469021B1 (pt)
EP (1) EP1137413B1 (pt)
JP (1) JP2002531501A (pt)
KR (1) KR20010089563A (pt)
AT (1) ATE288268T1 (pt)
AU (1) AU758968B2 (pt)
BR (1) BR9916965A (pt)
CA (1) CA2350887A1 (pt)
DE (1) DE69923587T2 (pt)
ES (1) ES2233089T3 (pt)
NZ (1) NZ511698A (pt)
PT (1) PT1137413E (pt)
WO (1) WO2000033839A1 (pt)
ZA (1) ZA200104128B (pt)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1292324A2 (en) 2000-05-05 2003-03-19 Novo Nordisk A/S Critical illness neuropathy
WO2002045712A1 (en) * 2000-12-04 2002-06-13 Biovitrum Ab Novel method and use
US20030199445A1 (en) 2002-02-07 2003-10-23 Knudsen Lotte Bjerre Use of GLP-1 compound for treatment of critically ill patients
WO2003066084A1 (en) * 2002-02-07 2003-08-14 Novo Nordisk A/S Use of glp-1 compound for treatment of critically ill patients
CN1308311C (zh) * 2002-02-13 2007-04-04 霍夫曼-拉罗奇有限公司 新型吡啶－和喹啉－衍生物
CN100503607C (zh) 2003-06-02 2009-06-24 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物类化合物及其应用
EP3456340B1 (en) * 2007-01-08 2022-02-16 The Trustees of the University of Pennsylvania Glp-1 receptor antagonist for use in the treatment of congenital hyperinsulinism
EP2194980A4 (en) * 2007-09-20 2012-01-18 D2E Llc PYRIDO FLUORINE DERIVATIVES [4,3-B] HYDROGENATED INDOLES HAVING NEUROPROTECTIVE AND COGNITIVE PROPERTIES, PREPARATION METHOD AND USE
WO2009067233A1 (en) * 2007-11-20 2009-05-28 Millennium Pharmaceuticals, Inc. Beta carbolines and uses thereof
LT3297653T (lt) 2015-05-22 2022-01-10 The Board Of Trustees Of The Leland Stanford Junior University Postbariatrinės hipoglikemijos gydymas glp-1 antagonistais
US10653753B2 (en) 2016-03-04 2020-05-19 Eiger Biopharmaceuticals, Inc. Treatment of hyperinsulinemic hypoglycemia with exendin-4 derivatives
BR112019010236A2 (pt) 2016-11-21 2019-08-20 Eiger Biopharmaceuticals Inc formulações tamponadas de exendina (9-39)
CN111362937B (zh) * 2020-03-06 2021-06-22 贵州医科大学 N-芳基-β-卡波林类衍生物及其用途
BR112022026385A2 (pt) * 2020-07-23 2023-01-31 Merck Patent Gmbh Heterociclos tricíclicos
CA3195925A1 (en) * 2020-10-30 2022-05-05 Robin Elaine DUNCAN Modulation of glucagon-like peptide 1 and uses thereof

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Publication number Priority date Publication date Assignee Title
WO1996034865A1 (en) 1995-05-05 1996-11-07 Novo Nordisk A/S Novel heterocyclic chemistry

Also Published As

Publication number Publication date
DE69923587D1 (de) 2005-03-10
US6469021B1 (en) 2002-10-22
NZ511698A (en) 2003-09-26
AU1751800A (en) 2000-06-26
EP1137413A2 (en) 2001-10-04
ES2233089T3 (es) 2005-06-01
CA2350887A1 (en) 2000-06-15
PT1137413E (pt) 2005-05-31
JP2002531501A (ja) 2002-09-24
DE69923587T2 (de) 2005-06-23
EP1137413A4 (en) 2002-06-26
WO2000033839B1 (en) 2000-09-28
WO2000033839A1 (en) 2000-06-15
ZA200104128B (en) 2002-05-21
ATE288268T1 (de) 2005-02-15
AU758968B2 (en) 2003-04-03
EP1137413B1 (en) 2005-02-02
KR20010089563A (ko) 2001-10-06

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