MX2013006768A - Moduladores de receptor de glucagon. - Google Patents

Moduladores de receptor de glucagon.

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Publication number
MX2013006768A
MX2013006768A MX2013006768A MX2013006768A MX2013006768A MX 2013006768 A MX2013006768 A MX 2013006768A MX 2013006768 A MX2013006768 A MX 2013006768A MX 2013006768 A MX2013006768 A MX 2013006768A MX 2013006768 A MX2013006768 A MX 2013006768A
Authority
MX
Mexico
Prior art keywords
formula
receptor modulators
glucagon receptor
compounds
glucagon
Prior art date
Application number
MX2013006768A
Other languages
English (en)
Inventor
Kevin James Filipski
Jeffrey Allen Pfefferkorn
Gary Erik Aspnes
Mary Theresa Didiuk
Angel Guzman-Perez
Benjamin Dawson Stevens
Meihua Mike Tu
Original Assignee
Pfizer
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Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of MX2013006768A publication Critical patent/MX2013006768A/es

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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/82—Amides; Imides in position 3
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    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
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    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems

Abstract

La presente invención proporciona un compuesto de Fórmula (I) (Ver Formula) o una sal farmacéuticamente aceptable del mismo en la que R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 y B4 son como se definen en el presente documento. Se ha descubierto que los compuestos de Fórmula I actúan como antagonistas o agonistas inversos del glucagón. En consecuencia, los compuestos de Fórmula I y las composiciones farmacéuticas de los mismos son útiles para el tratamiento de enfermedades, trastornos o afecciones mediadas por el glucagón.
MX2013006768A 2010-12-23 2011-12-09 Moduladores de receptor de glucagon. MX2013006768A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201061426600P 2010-12-23 2010-12-23
US201161562008P 2011-11-21 2011-11-21
PCT/IB2011/055588 WO2012085745A1 (en) 2010-12-23 2011-12-09 Glucagon receptor modulators

Publications (1)

Publication Number Publication Date
MX2013006768A true MX2013006768A (es) 2013-07-22

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MX2013006768A MX2013006768A (es) 2010-12-23 2011-12-09 Moduladores de receptor de glucagon.

Country Status (17)

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US (4) US8809342B2 (es)
EP (1) EP2655331A1 (es)
JP (1) JP5694561B2 (es)
KR (1) KR101506829B1 (es)
CN (1) CN103261165B (es)
AR (1) AR084579A1 (es)
AU (1) AU2011346670B2 (es)
BR (1) BR112013016033A2 (es)
CA (1) CA2822017C (es)
MX (1) MX2013006768A (es)
NZ (1) NZ611529A (es)
RU (1) RU2013127611A (es)
SG (1) SG191040A1 (es)
TW (1) TWI429630B (es)
UY (1) UY33824A (es)
WO (1) WO2012085745A1 (es)
ZA (1) ZA201303950B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR081626A1 (es) * 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
NZ611529A (en) * 2010-12-23 2015-06-26 Pfizer Glucagon receptor modulators
WO2013147026A1 (ja) 2012-03-29 2013-10-03 武田薬品工業株式会社 芳香環化合物
WO2014172191A1 (en) 2013-04-15 2014-10-23 E. I. Du Pont De Nemours And Company Fungicidal carboxamides
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
US20230131180A1 (en) * 2020-03-06 2023-04-27 Alphala Co., Ltd. Processes for producing amide compounds, and their crystalline and salt form

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5320825A (en) 1991-05-01 1994-06-14 Trustees Of The University Of Pennsylvania Serotonin reuptake inhibitors for S.P.E.C.T. imaging
WO1994014427A2 (en) 1992-12-23 1994-07-07 Zymogenetics, Inc. Use of skyrin and analogues for the treatment of diabetes mellitus and process for their preparation
PT617001E (pt) 1993-03-19 2000-06-30 Merck & Co Inc Derivados do acido fenoxifenilacetico
GB9408185D0 (en) 1994-04-25 1994-06-15 Fujisawa Pharmaceutical Co New benzamide derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
DE4426346A1 (de) 1994-07-25 1996-02-01 Basf Ag Herbizide Pyrazinderivate
GB2292149A (en) 1994-08-09 1996-02-14 Ferring Res Ltd Peptide inhibitors of pro-interleukin-1beta converting enzyme
AU3642795A (en) 1994-09-27 1996-04-19 Merck & Co., Inc. Endothelin receptor antagonists for the treatment of emesis
US5837719A (en) 1995-08-10 1998-11-17 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
EP0859771A4 (en) 1995-10-31 2000-03-15 Merck & Co Inc SUBSTITUTED PYRIDYL PYRROLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHOD OF USE
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
US5776954A (en) 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
US5880139A (en) 1996-11-20 1999-03-09 Merck & Co., Inc. Triaryl substituted imidazoles as glucagon antagonists
EP0959886A4 (en) 1996-11-20 2001-05-02 Merck & Co Inc TRIARYL SUBSTITUTED IMIDAZOLES AS GLUCAGON ANTAGONISTS
TW520362B (en) 1996-12-05 2003-02-11 Amgen Inc Substituted pyrimidine compounds and pharmaceutical composition comprising same
NZ335992A (en) 1996-12-05 2001-09-28 Amgen Inc Substituted pyrimidinone and pyridone compounds and methods of use
IL130124A0 (en) 1996-12-11 2000-06-01 Basf Ag Ketobenzamides as calpain inhibitors
JPH10259176A (ja) 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
BR9810378A (pt) 1997-07-01 2000-08-29 Novo Nordisk As Composto,uso do mesmo, composição farmacêutica, e, processos de tratar a diabete do tipo i ou do tipo ii, de tratar a hiperglicemia, e de diminuir a glicose do sangue em um mamìfero
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
IL136711A0 (en) 1997-12-19 2001-06-14 Amgen Inc Substituted pyridine and pyridazine compounds and their pharmaceutical use
RU2278860C2 (ru) 1999-04-28 2006-06-27 Санофи-Авентис Дойчланд Гмбх Производные триарил-содержащих кислот в качестве лигандов рецепторов ппар
RU2267484C2 (ru) 1999-04-28 2006-01-10 Авентис Фарма Дойчланд Гмбх Производные диариловой кислоты и фармацевтическая композиция на их основе
EP1183229B1 (en) 1999-05-17 2005-10-26 Novo Nordisk A/S Glucagon antagonists/inverse agonists
MXPA02012273A (es) 2000-06-23 2003-04-25 Novo Nordisk As Antagonistas/agonistas inversos de glucagon.
US20030203946A1 (en) 2000-11-17 2003-10-30 Carsten Behrens Glucagon antagonists/inverse agonists
JP2004513936A (ja) 2000-11-17 2004-05-13 ノボ　ノルディスク　アクティーゼルスカブ グルカゴンアンタゴニスト／逆アゴニスト
EP1383501B1 (en) 2001-02-28 2007-04-04 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
EP1453541A1 (en) 2001-12-03 2004-09-08 Novo Nordisk A/S Use of a glucokinase activator in combination with a glucagon antagonist for treating type 2 diabetes
EP1463715A1 (en) 2001-12-03 2004-10-06 Novo Nordisk A/S Novel glucagon antagonists
WO2003051357A1 (en) 2001-12-19 2003-06-26 Novo Nordisk A/S Glucagon receptor antagonists/inverse agonists
WO2003053938A1 (en) 2001-12-20 2003-07-03 Novo Nordisk A/S Benzimidazols and indols as glucagon receptor antagonists/inverse agonisten
CZ2004747A3 (cs) 2001-12-21 2004-11-10 Novo Nordisk A/S Deriváty amidů jako GK aktivátory
EP1489077A4 (en) 2002-02-01 2006-06-21 Dainippon Sumitomo Pharma Co 2- FURANCARA ACID HYDRATES AND PHARMACEUTICAL COMPOSITION CONTAINING THEM
WO2003080545A2 (en) 2002-03-20 2003-10-02 Metabolex, Inc. Substituted phenylacetic acids
AU2003226927A1 (en) 2002-04-09 2003-10-27 7Tm Pharma A/S Novel carboxamide compounds for use in mch receptor related disorders
WO2004002480A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
MXPA05000130A (es) 2002-06-27 2005-02-17 Novo Nordisk As Derivados de aril-carbonilo como agentes terapeuticos.
CA2498399A1 (en) 2002-09-12 2004-03-25 Merck & Co., Inc. Method of treating diabetes and related conditions
US7196106B2 (en) 2002-11-05 2007-03-27 Merck & Co., Inc Cyanothiophene derivatives, compositions containing such compounds and methods of use
US20040097557A1 (en) 2002-11-13 2004-05-20 Duffy Joseph L. Cyanothiophene derivatives, compositions containing such compounds and methods of use
CA2508581A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Spirocyclic ureas, compositions containing such compounds and methods of use
WO2004056763A2 (en) 2002-12-20 2004-07-08 Novo Nordisk A/S Novel glucagon antagonists
US20040209928A1 (en) 2002-12-30 2004-10-21 Ravi Kurukulasuriya Glucagon receptor antagonists/inverse agonists
DE10300398A1 (de) 2003-01-09 2004-07-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von substituierten 2-Phenylbenzimidazolen als Arzneimittel
US7151114B2 (en) 2003-01-09 2006-12-19 Boehringer Ingelheim International Gmbh Use of substituted 2-phenylbenzimidazoles as medicaments
WO2004063147A1 (en) 2003-01-10 2004-07-29 Novo Nordisk A/S Salts and solvates of glucagon antagonists
ATE490244T1 (de) 2003-01-27 2010-12-15 Merck Sharp & Dohme Substituierte pyrazole, zusammensetzungen,die solche verbindungen enthalten, und anwendungsverfahren
BRPI0409447A (pt) 2003-04-14 2006-04-18 Inst For Pharm Discovery Inc ácidos fenilalcanóicos substituìdos
US7138529B2 (en) 2003-04-16 2006-11-21 Hoffmann-La Roche Inc. Substituted 3-cyanothiophene acetamides as glucagon receptor antagonists
KR20060006954A (ko) 2003-04-30 2006-01-20 디 인스티튜트스 포 파마슈티컬 디스커버리, 엘엘씨 단백질 티로신 포스파타제-１ｂ 억제제로서의 페닐 치환된카르복실산
JP2006528687A (ja) 2003-05-09 2006-12-21 メルク　エンド　カムパニー　インコーポレーテッド ベンズイミダゾール、こうした化合物を含有する組成物および使用方法
US7355049B2 (en) 2003-06-24 2008-04-08 Hoffmann-La Roche Inc. Biaryloxymethylarenecarboxylic acids as glycogen synthase activator
JP4412098B2 (ja) 2003-07-31 2010-02-10 Ｊｆｅスチール株式会社 溶接熱影響部靭性に優れた低降伏比高強度鋼板及びその製造方法
WO2005014534A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2005058845A2 (en) 2003-12-19 2005-06-30 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
EP1699453A4 (en) 2003-12-19 2009-07-01 Merck & Co Inc CYCLIC GUANIDINES, COMPOSITIONS AND METHOD OF ADMINISTRATION CONTAINING SUCH COMPOUNDS
EA010888B1 (ru) 2004-05-25 2008-12-30 Пфайзер Продактс, Инк. Тетраазабензо[е]азуленовые производные и их аналоги
US7989457B2 (en) * 2004-05-28 2011-08-02 Eli Lilly And Company Glucagon receptor antagonists, preparation and therapeutic uses
AU2005252183B2 (en) 2004-06-04 2008-07-17 Merck Sharp & Dohme Corp. Pyrazole derivatives, compositions containing such compounds and methods of use
ES2337596T3 (es) * 2004-06-14 2010-04-27 Eli Lilly And Company Antagonistas del receptor de glucacion, preparacion y usos terapeuticaos.
EP1765335B1 (en) 2004-07-07 2009-11-25 Merck & Co., Inc. Pyrazole amide derivatives, compositions containing such compounds and methods of use
DE602005021494D1 (de) 2004-07-22 2010-07-08 Merck Sharp & Dohme Substituierte pyrazole, derartige verbindungen enthaltende zusammensetzungen und verfahren zu ihrer verwendung
DE102004051188A1 (de) 2004-10-21 2006-04-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Cyanothiophene, deren Herstellung und deren Verwendung als Arzneimittel
US7524870B2 (en) 2004-12-03 2009-04-28 Hoffmann-La Roche Inc. Biaryloxymethylarenecarboxylic acids as glycogen synthase activators
US20060122236A1 (en) * 2004-12-06 2006-06-08 Wood Michael R Substituted biaryl-carboxylate derivatives
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
SI1856090T1 (sl) 2005-02-11 2010-02-26 Lilly Co Eli Substituirani derivati tiofena kot antagonisti glukagonskega receptorja, priprava in terapevtske uporabe
CN101146762A (zh) 2005-03-21 2008-03-19 默克公司 取代的芳基和杂芳基衍生物
EP1868985A4 (en) 2005-03-30 2010-05-05 Merck Sharp & Dohme GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS COMPRISING SUCH COMPOUNDS, AND METHODS OF USE
US7709658B2 (en) 2005-07-26 2010-05-04 Merck Sharp & Dohme Corp. Process for synthesizing a substituted pyrazole
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
WO2007040446A1 (en) 2005-10-06 2007-04-12 Probi Ab Use of lactobacillus for treatment of autoimmune diseases
TW200745031A (en) 2005-10-13 2007-12-16 Merck & Co Inc Acyl indoles, compositions containing such compounds and methods of use
AR056574A1 (es) 2005-10-19 2007-10-10 Merck & Co Inc Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso
WO2007059195A1 (en) 2005-11-14 2007-05-24 University Of Southern California Integrin-binding small molecules
WO2007123581A1 (en) * 2005-11-17 2007-11-01 Eli Lilly And Company Glucagon receptor antagonists, preparation and therapeutic uses
PL1951661T3 (pl) * 2005-11-17 2012-12-31 Lilly Co Eli Antagoniści receptora glukagonu, wytwarzanie i terapeutyczne zastosowania
DE602006015509D1 (de) 2005-11-18 2010-08-26 Lilly Co Eli Glucagonrezeptorantagonisten, deren herstellung und therapeutische verwendung
CN101312723B (zh) * 2005-11-22 2012-01-11 伊莱利利公司 胰高血糖素受体拮抗剂、制备和治疗用途
SI1957484T1 (sl) 2005-11-23 2010-07-30 Lilly Co Eli Antagonisti glukagonskega receptorja, priprava in terapevtske uporabe
EP1963258A4 (en) 2005-12-19 2011-06-29 Methylgene Inc HISTONE DEACETYLASE INHIBITORS FOR INCREASING THE ACTIVITY OF ANTIFUNGAL AGENTS
TW200806611A (en) 2006-02-09 2008-02-01 Daiichi Seiyaku Co Novel amidopropionic acid derivatives and medicine containing the same
WO2007111864A2 (en) 2006-03-23 2007-10-04 Merck & Co., Inc. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
JP2009537525A (ja) 2006-05-16 2009-10-29 メルク エンド カムパニー インコーポレーテッド グルカゴン受容体アンタゴニスト化合物、このような化合物を含む組成物及び使用方法
TW200821284A (en) 2006-10-03 2008-05-16 Merck & Co Inc Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
ES2720430T3 (es) 2007-02-09 2019-07-22 Metabasis Therapeutics Inc Antagonistas novedosos del receptor de glucagón
JP2009040702A (ja) 2007-08-07 2009-02-26 Daiichi Sankyo Co Ltd 新規アミドプロピオン酸誘導体を含有する医薬組成物
WO2009035558A1 (en) 2007-09-12 2009-03-19 Merck & Co., Inc. Process for the production of a crystalline glucagon receptor antagonist compound
US8309580B2 (en) * 2007-11-01 2012-11-13 Takeda Pharmaceutical Company Limited Heterocyclic compound
DK2231701T3 (da) 2007-12-11 2012-05-21 Cadila Healthcare Ltd Peptidomimetika med glucagon-antagonistiske og GLP-1-antagonistiske aktiviteter
KR101616140B1 (ko) 2008-03-05 2016-04-27 다케다 야쿠힌 고교 가부시키가이샤 복소환 화합물
US7727983B2 (en) 2008-03-07 2010-06-01 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
EP2291358B1 (en) 2008-05-16 2018-03-28 Merck Sharp & Dohme Corp. Glucagon receptor antagonists, compositions, and methods for their use
WO2010019828A1 (en) * 2008-08-13 2010-02-18 Metabasis Therapeutics, Inc. Glucagon receptor antagonists
WO2010019830A1 (en) 2008-08-13 2010-02-18 Metabasis Therapeutics, Inc. Glucagon antagonists
US8436015B2 (en) 2008-09-15 2013-05-07 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
EP2350020B1 (en) 2008-10-03 2014-08-13 Merck Sharp & Dohme Corp. Spiro-imidazolone derivatives as glucagon receptor antagonists
US8445538B2 (en) 2008-12-19 2013-05-21 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds
WO2010080971A1 (en) 2009-01-12 2010-07-15 Merck Sharp & Dohme Corp. Crystalline polymorphic forms of an antidiabetic compound
US20110281795A1 (en) 2009-01-28 2011-11-17 Songnian Lin Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
WO2010098948A1 (en) 2009-02-13 2010-09-02 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds, compositions containin such compounds and methods of use
US8318667B2 (en) 2009-02-25 2012-11-27 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
WO2010131669A1 (ja) 2009-05-14 2010-11-18 大日本住友製薬株式会社 ３－（４－アミノフェニル）－２－フランカルボン酸誘導体およびその薬学的に許容される塩
WO2010144664A1 (en) 2009-06-12 2010-12-16 Schering Corporation Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
JP2012188352A (ja) 2009-07-13 2012-10-04 Dainippon Sumitomo Pharma Co Ltd ３−（４−置換アルキル−フェニル）−２−フランカルボン酸誘導体およびその薬学的に許容される塩
WO2011027849A1 (ja) 2009-09-04 2011-03-10 武田薬品工業株式会社 複素環化合物
WO2011037815A1 (en) 2009-09-22 2011-03-31 Schering Corporation Novel pyrrolidines as glucagon receptor antagonists, compositions, and methods for their use
WO2011119559A1 (en) 2010-03-25 2011-09-29 Schering Corporation Novel spiro imidazolones as glucagon receptor antagonists, compositions, and methods for their use
WO2011119541A1 (en) 2010-03-26 2011-09-29 Schering Corporation Novel spiro imidazolone derivatives as glucagon receptor antagonists, compositions, and methods for their use
CN102206172B (zh) 2010-03-30 2015-02-25 中国医学科学院医药生物技术研究所 一组取代双芳基化合物及其制备方法和抗病毒应用
NZ611529A (en) * 2010-12-23 2015-06-26 Pfizer Glucagon receptor modulators

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