EA200200421A1 - АМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-a]-1,3,5-ТРИАЗИНЫ - Google Patents

АМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-a]-1,3,5-ТРИАЗИНЫ

Info

Publication number
EA200200421A1
EA200200421A1 EA200200421A EA200200421A EA200200421A1 EA 200200421 A1 EA200200421 A1 EA 200200421A1 EA 200200421 A EA200200421 A EA 200200421A EA 200200421 A EA200200421 A EA 200200421A EA 200200421 A1 EA200200421 A1 EA 200200421A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
pyrazolo
disorders
receptors
amynic
Prior art date
Application number
EA200200421A
Other languages
English (en)
Inventor
Джеймс В. Дэрроу
Стефан Де Ломбаер
Чарльз Блюм
Дженнифер Трэн
Марк Джанджордано
Дэвид Эндрю Гриффит
Филип Альберт Карпино
Original Assignee
Ньюроджен Корпорейшн
Пфайзер Инк.
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 Ньюроджен Корпорейшн, Пфайзер Инк. filed Critical Ньюроджен Корпорейшн
Publication of EA200200421A1 publication Critical patent/EA200200421A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/575—Hormones
    • G01N2333/5755—Neuropeptide Y
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70571—Assays involving receptors, cell surface antigens or cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Раскрыты соединения формулы (I), где R, R, R, R, R, Rи Х имеют указанные в описании значения. Данные соединения являются селективными модуляторами NPY1 рецепторов. Данные соединения полезны для лечения ряда заболеваний ЦНС, метаболических нарушений и периферических нарушений, особенно нарушений питания и гипертензии. Предложены также способы лечения таких нарушений, а также упакованные фармацевтические композиции. Соединения настоящего изобретения также полезны в качестве зондов для локализации NPY1 рецепторов и в качестве стандартов в анализах связывания NPY1 рецепторов. Предложены способы применения этих соединений для изучения локализации рецепторов.Отчет о международном поиске был опубликован 2001.10.18.
EA200200421A 1999-09-30 2000-09-29 АМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-a]-1,3,5-ТРИАЗИНЫ EA200200421A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15686899P 1999-09-30 1999-09-30
PCT/US2000/026885 WO2001023388A2 (en) 1999-09-30 2000-09-29 AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES

Publications (1)

Publication Number Publication Date
EA200200421A1 true EA200200421A1 (ru) 2002-10-31

Family

ID=22561433

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200421A EA200200421A1 (ru) 1999-09-30 2000-09-29 АМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-a]-1,3,5-ТРИАЗИНЫ

Country Status (21)

Country Link
US (1) US6476038B1 (ru)
EP (1) EP1218381B1 (ru)
JP (2) JP2003510326A (ru)
KR (1) KR20020047201A (ru)
CN (1) CN1377355A (ru)
AT (1) ATE347553T1 (ru)
AU (1) AU7737900A (ru)
BG (1) BG106507A (ru)
CA (1) CA2379633C (ru)
CZ (1) CZ20021089A3 (ru)
DE (1) DE60032249T2 (ru)
EA (1) EA200200421A1 (ru)
ES (1) ES2277855T3 (ru)
HU (1) HUP0203131A3 (ru)
IL (1) IL148904A0 (ru)
NO (1) NO20021357L (ru)
OA (1) OA12049A (ru)
PL (1) PL354982A1 (ru)
WO (1) WO2001023388A2 (ru)
YU (1) YU23602A (ru)
ZA (1) ZA200202517B (ru)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6472528B1 (en) * 1999-08-10 2002-10-29 Neurocrine Biosciences, Inc. Synthesis of substituted pyrazolopyrimidines
EA200200422A1 (ru) * 1999-09-30 2002-10-31 Ньюроджен Корпорейшн НЕКОТОРЫЕ АЛКИЛЕНДИАМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-а]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-а]-1,3,5-ТРИАЗИНЫ
ES2245772T3 (es) 2002-03-07 2006-01-16 Smithkline Beecham Corporation Derivados de pirazolopirimidina y pirazolotriazina y composiciones farmaceuticas que los contienen.
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
FR2842809A1 (fr) * 2002-07-26 2004-01-30 Greenpharma Sas NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
PL377847A1 (pl) 2003-01-14 2006-02-20 Arena Pharmaceuticals Inc. 1,2,3-Tripodstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu oraz profilaktyka i leczenie związanych z nim zaburzeń takich jak cukrzyca i hiperglikemia
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7329658B2 (en) * 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
US7176210B2 (en) * 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
EA010023B1 (ru) 2003-07-14 2008-06-30 Арена Фармасьютикалз, Инк. Конденсированные арильные и гетероарильные производные в качестве модуляторов метаболизма и для профилактики и лечения расстройств, связанных с нарушением метаболизма
US7547693B2 (en) 2003-09-22 2009-06-16 Banyu Pharmaceutical Co. Ltd. Piperidine derivative
US7153961B2 (en) 2003-11-25 2006-12-26 Bristol-Myers Squibb Pharma Co. Salt and crystalline form thereof of a corticotropin releasing factor receptor antagonist
US7208596B2 (en) 2003-11-25 2007-04-24 Bristol-Myers Squibb Pharma Company Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof
CA2550948A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
US20070293511A1 (en) * 2003-12-22 2007-12-20 Sb Pharmco Puerto Rico Inc. And Neurocrine Biosciences, Inc., A Corporation Crf Receptor Antagonists and Methods
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
GB0519957D0 (en) * 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
EP2286840A3 (en) 2004-11-01 2013-09-04 Amylin Pharmaceuticals, LLC Treatment of obesity and related diseases
ATE433454T1 (de) * 2004-12-21 2009-06-15 Schering Corp Pyrazoloä1,5-aüpyrimidine als antagonisten des adenosin-a2a-rezeptors
US20090286723A1 (en) 2005-02-11 2009-11-19 Amylin Pharmaceuticals, Inc. Hybrid Polypeptides with Selectable Properties
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
US8138206B2 (en) 2005-05-30 2012-03-20 Msd. K.K. Piperidine derivative
EP2380589A3 (en) 2005-06-23 2012-09-12 Statens Serum Institut Improved tuberculosis vaccines
WO2007018248A1 (ja) 2005-08-10 2007-02-15 Banyu Pharmaceutical Co., Ltd. ピリドン化合物
BRPI0614649A2 (pt) 2005-08-11 2011-04-12 Amylin Pharmaceuticals Inc polipeptìdeos hìbridos com propriedades selecionáveis
WO2007024004A1 (ja) 2005-08-24 2007-03-01 Banyu Pharmaceutical Co., Ltd. フェニルピリドン誘導体
JPWO2007029847A1 (ja) 2005-09-07 2009-03-19 萬有製薬株式会社 二環性芳香族置換ピリドン誘導体
KR20080048502A (ko) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
WO2007048027A2 (en) 2005-10-21 2007-04-26 Novartis Ag Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent
US8163770B2 (en) 2005-10-27 2012-04-24 Msd. K. K. Benzoxathiin derivative
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
RS51545B (en) 2006-09-20 2011-06-30 Eli Lilly And Company THIAZOL PIRAZOLOPIRAMIDINS AS ANTAGONISTS OF CRF1 RECEPTORS
EA016056B1 (ru) * 2006-09-20 2012-01-30 Эли Лилли Энд Компани Тиофенпиразолопиримидиновые соединения
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
AU2007301126A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
ES2393885T7 (es) 2007-06-04 2014-01-30 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
MX2009013336A (es) * 2007-06-07 2010-01-20 Schering Corp Sintesis de 3-aminopirazoles sustituidos.
JPWO2009110510A1 (ja) 2008-03-06 2011-07-14 Ｍｓｄ株式会社 アルキルアミノピリジン誘導体
CN101981025A (zh) 2008-03-28 2011-02-23 万有制药株式会社 具有黑色素浓缩激素受体拮抗作用的二芳基甲基酰胺衍生物
ES2522968T3 (es) 2008-06-04 2014-11-19 Synergy Pharmaceuticals Inc. Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
AU2009261248A1 (en) 2008-06-19 2009-12-23 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
US20100015171A1 (en) 2008-07-15 2010-01-21 Statens Serum Institute Vaccines comprising tb 10.4
AU2009270833B2 (en) 2008-07-16 2015-02-19 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
WO2010013595A1 (ja) 2008-07-30 2010-02-04 萬有製薬株式会社 ５員－５員又は５員－６員縮環シクロアルキルアミン誘導体
MX2011004258A (es) 2008-10-22 2011-06-01 Merck Sharp & Dohme Derivados de bencimidazol ciclicos novedosos utiles como agentes anti-diabeticos.
BRPI0919876A8 (pt) 2008-10-30 2016-02-10 Merck Sharp & Dohme Composto, composição farmacêutica, uso de um composto, e, método para intensificar a qualidade do sono, para tratar insônia, e para tratar ou controlar obesidade em um paciente mamífero que necessita do mesmo.
CA2741672A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US20110243940A1 (en) 2008-12-16 2011-10-06 Schering Corporation Bicyclic pyranone derivatives and methods of use thereof
EP2379547A1 (en) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
KR101668514B1 (ko) 2011-02-25 2016-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
JP2015525782A (ja) 2012-08-02 2015-09-07 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 抗糖尿病性三環式化合物
CA2889919C (en) * 2012-11-16 2021-08-17 University Health Network Pyrazolopyrimidine compounds
RU2015140066A (ru) 2013-02-22 2017-03-30 Мерк Шарп И Доум Корп. Противодиабетические бициклические соединения
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
JP2016514671A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼのアゴニストおよびその使用
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
US10011637B2 (en) 2013-06-05 2018-07-03 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase C, method of making and using same
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX2017002610A (es) 2014-08-29 2017-10-11 Tes Pharma S R L INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA.
AU2016205361C1 (en) 2015-01-06 2021-04-08 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
SI3310760T1 (sl) 2015-06-22 2023-02-28 Arena Pharmaceuticals, Inc. Kristalinična L-argininska sol (R)-2-(7-(4-ciklopentil-3-(trifluorometil)benziloksi)-1,2,3,4- tetrahidrociklo-penta(b)indol-3-il)ocetne kisline za uporabo pri motnjah, povezanih z receptorjem S1P1
EP3507290A1 (en) 2016-08-31 2019-07-10 Agios Pharmaceuticals, Inc. Inhibitors of cellular metabolic processes
US20180134667A1 (en) 2016-10-14 2018-05-17 TES Pharma S.r.I. Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
KR20190116416A (ko) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법
KR20200140351A (ko) * 2018-04-10 2020-12-15 바이엘 악티엔게젤샤프트 2,6-디알킬페닐아세트산을 제조하는 방법
CN112996790B (zh) 2018-10-30 2023-11-03 克洛诺斯生物公司 用于调节cdk9活性的化合物、组合物和方法
MX2021005904A (es) 2018-11-20 2021-09-08 Tes Pharma S R L Inhibidores de la ácido alfa-amino-beta-carboximucónico semialdehído descarboxilasa.
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2021026047A1 (en) 2019-08-08 2021-02-11 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
AU2021324839B2 (en) 2020-08-12 2024-02-29 Spruce Biosciences, Inc. Methods and compositions for treating polycystic ovary syndrome
US20230365533A1 (en) 2020-08-18 2023-11-16 Merck Sharp & Dohme Llc Bicycloheptane pyrrolidine orexin receptor agonists
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof
CN115304607B (zh) * 2022-07-06 2023-06-27 华南农业大学 吡唑并嘧啶衍生物的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU747708B2 (en) * 1996-07-24 2002-05-23 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
JP3711238B2 (ja) * 1997-08-05 2005-11-02 ファイザー・プロダクツ・インク 神経ペプチドＹ受容体アンタゴニストとしての４−アミノピロ−ル（３，２−ｄ）ピリミジン
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases

Also Published As

Publication number Publication date
OA12049A (en) 2006-05-02
NO20021357D0 (no) 2002-03-19
JP2003510326A (ja) 2003-03-18
US6476038B1 (en) 2002-11-05
JP2007077144A (ja) 2007-03-29
CN1377355A (zh) 2002-10-30
CA2379633A1 (en) 2001-04-05
HUP0203131A3 (en) 2004-06-28
CZ20021089A3 (cs) 2002-11-13
EP1218381B1 (en) 2006-12-06
WO2001023388A2 (en) 2001-04-05
CA2379633C (en) 2006-06-20
DE60032249T2 (de) 2007-07-19
BG106507A (en) 2002-12-29
NO20021357L (no) 2002-05-23
EP1218381A2 (en) 2002-07-03
ZA200202517B (en) 2003-05-28
WO2001023388A3 (en) 2001-10-18
HUP0203131A2 (hu) 2003-01-28
AU7737900A (en) 2001-04-30
YU23602A (sh) 2004-09-03
PL354982A1 (en) 2004-03-22
IL148904A0 (en) 2002-09-12
ATE347553T1 (de) 2006-12-15
KR20020047201A (ko) 2002-06-21
ES2277855T3 (es) 2007-08-01
DE60032249D1 (de) 2007-01-18

Similar Documents

Publication Publication Date Title
EA200200421A1 (ru) АМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-a]-1,3,5-ТРИАЗИНЫ
EA200200422A1 (ru) НЕКОТОРЫЕ АЛКИЛЕНДИАМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-а]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-а]-1,3,5-ТРИАЗИНЫ
EA200000592A1 (ru) Азаполициклические соединения, конденсированные с арилом
EA200600294A1 (ru) [1,8] нафтиридин-2-оны и родственные соединения для лечения шизофрении
EA200200716A1 (ru) Арилконденсированные азаполициклические соединения
EA200000274A2 (ru) Способы получения и промежуточные соединения для получения противораковых соединений
EA200300381A1 (ru) Нуклеиновые кислоты и полипептиды нового рецептора
EA199900559A1 (ru) Замещенные, азотсодержащие гетероциклы в качестве ингибиторов протеинкиназы p38
TR199902942T2 (xx) Nikotinik ACh Resept�rlerinde kolinerjik ligandlar olarak 8-Azabisiklo(3.2.1)okt-ene ve okstan t�revleri.
NO308601B1 (no) Tricykliske benzazepiner og farmasøytisk preparat inneholdende disse
YU40701A (sh) Piperidini kao modulatori ccr5
ME00513B (me) Azabicikloalkani kao modulatori ccr5
IS1904B (is) Hliðstæðar aðferðir við framleiðslu á nýjum (R)-5-karbamóýl-8-flúor-3-N,N-tvíútskiptum-amínó-3,4-díhýdró-2H-1-bensópýrönum
NO20022185D0 (no) Bisykliske og trisykliske heteroaromatiske forbindelser
EA199800116A1 (ru) Пирролопиримидины и фармацевтические композиции, включающие эти соединения
EA200500169A1 (ru) Замещенные производные 1,3-дифенилпроп-2-ен-1-она, получение и применение
EA200100203A1 (ru) Производные 4,4-биарилпиперидина с активностью в отношении опиоидных рецепторов
BG66085B1 (bg) Фенилаланинови производни
EA200100524A1 (ru) Амиды антраниловой кислоты и их применение в качестве лекарственных средств
EA200100001A1 (ru) Замещенные индолиноны, их получение и применение в качестве лекарственных средств
DE69804743T2 (de) Pyrazolo[4,3-d]pyrimidin-Derivate und diese enthaltende pharmazeutische Zubereitungen
EA200600209A1 (ru) ПРОИЗВОДНЫЕ ПИРРОЛО[3,4-c]ПИРАЗОЛА, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ КАК ИНГИБИТОРЫ КИНАЗЫ
EA199900632A1 (ru) 2-амино-6-(2-замещенные-4-фенокси)-замещенные-пиридины
EA200000996A1 (ru) Конденсированные с арилом азаполициклические соединения
ATE269865T1 (de) Pyrazolo(3,4-g)chinoxaline als pdgf-rezeptor protein tyrosin-kinase inhibitoren