CN100366614C - 具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物 - Google Patents

具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物 Download PDF

Info

Publication number
CN100366614C
CN100366614C CNB028017773A CN02801777A CN100366614C CN 100366614 C CN100366614 C CN 100366614C CN B028017773 A CNB028017773 A CN B028017773A CN 02801777 A CN02801777 A CN 02801777A CN 100366614 C CN100366614 C CN 100366614C
Authority
CN
China
Prior art keywords
phenyl
compound
chloro
disease
formula
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CNB028017773A
Other languages
English (en)
Chinese (zh)
Other versions
CN1486301A (zh
Inventor
J·H·M·兰格
C·G·克鲁斯
J·蒂普克
J·胡格多恩
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abbott Healthcare Products BV
Original Assignee
Solvay Pharmaceuticals BV
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8180044&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN100366614(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Solvay Pharmaceuticals BV filed Critical Solvay Pharmaceuticals BV
Publication of CN1486301A publication Critical patent/CN1486301A/zh
Application granted granted Critical
Publication of CN100366614C publication Critical patent/CN100366614C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D231/08Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB028017773A 2001-03-22 2002-03-18 具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物 Expired - Fee Related CN100366614C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01201062.5 2001-03-22
EP01201062 2001-03-22

Publications (2)

Publication Number Publication Date
CN1486301A CN1486301A (zh) 2004-03-31
CN100366614C true CN100366614C (zh) 2008-02-06

Family

ID=8180044

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028017773A Expired - Fee Related CN100366614C (zh) 2001-03-22 2002-03-18 具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物

Country Status (25)

Country Link
EP (1) EP1373216B1 (enExample)
JP (1) JP4373675B2 (enExample)
KR (1) KR100846614B1 (enExample)
CN (1) CN100366614C (enExample)
AR (1) AR033046A1 (enExample)
AT (1) ATE284872T1 (enExample)
AU (1) AU2002256690B2 (enExample)
BR (1) BR0205602A (enExample)
CA (1) CA2422708C (enExample)
CZ (1) CZ2003698A3 (enExample)
DE (1) DE60202270T2 (enExample)
ES (1) ES2229132T3 (enExample)
HU (1) HUP0303148A3 (enExample)
IL (1) IL153508A (enExample)
MX (1) MXPA03003534A (enExample)
NO (1) NO324953B1 (enExample)
NZ (1) NZ524633A (enExample)
PL (1) PL363751A1 (enExample)
PT (1) PT1373216E (enExample)
RU (1) RU2281941C2 (enExample)
SI (1) SI1373216T1 (enExample)
SK (1) SK287592B6 (enExample)
UA (1) UA74066C2 (enExample)
WO (1) WO2002076949A1 (enExample)
ZA (1) ZA200307322B (enExample)

Families Citing this family (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI231757B (en) 2001-09-21 2005-05-01 Solvay Pharm Bv 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity
CA2478183C (en) 2002-03-12 2010-02-16 Merck & Co. Inc. Substituted amides
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7247628B2 (en) 2002-12-12 2007-07-24 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
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
US7141669B2 (en) 2003-04-23 2006-11-28 Pfizer Inc. Cannabiniod receptor ligands and uses thereof
US7145012B2 (en) 2003-04-23 2006-12-05 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7268133B2 (en) 2003-04-23 2007-09-11 Pfizer, Inc. Patent Department Cannabinoid receptor ligands and uses thereof
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
AR045533A1 (es) * 2003-09-02 2005-11-02 Solvay Pharm Gmbh Uso de un compuesto antagonista de receptor de cb1, composicion farmaceutica y metodo de tratamiento y/o profilaxis de enfermedades relacionadas con dicho receptor de cb1
CA2551037A1 (en) 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. Novel piperidine derivative
TW200528102A (en) * 2003-10-24 2005-09-01 Solvay Pharm Gmbh Novel medical combination treatment of obesity involving 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
BRPI0415851A (pt) * 2003-10-24 2007-01-02 Solvay Pharm Gmbh utilizações médicas de compostos que apresentam atividade antagonìstica de cb1 e tratamento de combinação envolvendo os referidos compostos
WO2005049615A1 (en) * 2003-11-21 2005-06-02 Pfizer Products Inc. Pyrazolo`1,5-a!`1,3,5! triazin -4-one derivatives as cb1 receptor antagonists
JP4436369B2 (ja) 2004-01-28 2010-03-24 エフ.ホフマン−ラ ロシュ アーゲー スピロ−ベンゾジオキソール類およびそれらのcb1アンタゴニストとしての使用
ATE402697T1 (de) * 2004-01-30 2008-08-15 Solvay Pharm Bv 1,3,5-trisubstituierte 4,5-dihydro-1h-pyrazol- derivative mit cb1-antagonistischer aktivität
US7649002B2 (en) 2004-02-04 2010-01-19 Pfizer Inc (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists
JP2007530690A (ja) 2004-03-29 2007-11-01 メルク エンド カムパニー インコーポレーテッド 11−β−ヒドロキシステロイドデヒドロゲナーゼ−1の阻害剤としてのジアリールトリアゾール
WO2005097127A2 (en) 2004-04-02 2005-10-20 Merck & Co., Inc. Method of treating men with metabolic and anthropometric disorders
US20060025448A1 (en) 2004-07-22 2006-02-02 Cadila Healthcare Limited Hair growth stimulators
CN1993320A (zh) 2004-08-06 2007-07-04 默克公司 作为11-β-羟基类固醇脱氢酶-1的抑制剂的磺酰化合物
WO2006020959A2 (en) 2004-08-13 2006-02-23 Amgen Inc. Substituted benzofused heterocycles
RU2007119315A (ru) 2004-10-25 2008-11-27 Зольвай Фармасьютиклз Гмбх (De) Фармацевтические композиции, содержащие антагонисты каннабиноидного рецептора св1 и открыватели калиевых каналов, предназначенные для лечения сахарного диабета типа i, ожирения и связанных с ними состояний
CA2584806C (en) 2004-11-01 2014-06-17 Amylin Pharmaceuticals, Inc. Treatment of obesity and related disorders
US8394765B2 (en) 2004-11-01 2013-03-12 Amylin Pharmaceuticals Llc Methods of treating obesity with two different anti-obesity agents
CA2586068A1 (en) 2004-11-09 2006-05-18 F.Hoffmann-La Roche Ag Dibenzosuberone derivatives
WO2006060201A2 (en) * 2004-11-30 2006-06-08 Bayer Pharmaceuticals Corporation Pyrazole derivatives for the treatment of psychiatric disorders
WO2006060186A2 (en) * 2004-11-30 2006-06-08 Bayer Pharmaceuticals Corporation Pyrazole derivatives for the treatment of dementia and related disorders
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
ES2574014T3 (es) 2005-05-30 2016-06-14 Msd K.K. Derivado de piperidina novedoso
PL1902034T3 (pl) 2005-06-02 2011-09-30 Glenmark Pharmaceuticals Sa Nowe ligandy receptorów kanabinoidowych, kompozycja farmaceutyczna je zawierająca oraz proces ich wytwarzania
US7923465B2 (en) 2005-06-02 2011-04-12 Glenmark Pharmaceuticals S.A. Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
EP1757587A1 (en) * 2005-07-15 2007-02-28 Laboratorios Del Dr. Esteve, S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
AU2006277253A1 (en) 2005-08-10 2007-02-15 Msd K.K. Pyridone compound
EP2330125A3 (en) 2005-08-11 2012-12-12 Amylin Pharmaceuticals, Inc. Hybrid polypeptides with selectable properties
AU2006279680B2 (en) 2005-08-11 2012-12-06 Amylin Pharmaceuticals, Llc Hybrid polypeptides with selectable properties
WO2007024004A1 (ja) 2005-08-24 2007-03-01 Banyu Pharmaceutical Co., Ltd. フェニルピリドン誘導体
KR20080048502A (ko) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
WO2007049798A1 (ja) 2005-10-27 2007-05-03 Banyu Pharmaceutical Co., Ltd. 新規ベンゾオキサチイン誘導体
BRPI0618354B8 (pt) 2005-11-10 2021-05-25 Banyu Pharma Co Ltd composto e seu uso, composição farmacêutica, preventivo ou remédio
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
ES2402581T3 (es) 2006-02-23 2013-05-06 Pfizer Limited Piperidinoilpirrolidinas como agonistas del receptor de melanocortina tipo 4
US7763607B2 (en) 2006-04-27 2010-07-27 Solvay Pharmaceuticals Gmbh Pharmaceutical compositions comprising CBx cannabinoid receptor modulators and potassium channel modulators
JP2009534439A (ja) * 2006-04-27 2009-09-24 ゾルファイ ファーマスーティカルズ ゲゼルシャフト ミット ベシュレンクテル ハフツング Cbxカンナビノイド受容体モジュレータ及びカリウムチャンネルモジュレータを含む医薬組成物
AU2007283113A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use
EP2698157B1 (en) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20090247560A1 (en) 2006-09-28 2009-10-01 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
MX2009004314A (es) 2006-11-13 2009-05-05 Pfizer Prod Inc Diaril, dipiridinil y arilpiridinilderivados y usos de los mismos.
ATE547394T1 (de) 2006-12-01 2012-03-15 Bristol Myers Squibb Co N-((3-benzyl)-2,2-(bis-phenyl)-propan-1- aminderivate als cetp-hemmer für die behandlung von atherosklerose und herz-kreislauf- erkrankungen
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
WO2008120653A1 (ja) 2007-04-02 2008-10-09 Banyu Pharmaceutical Co., Ltd. インドールジオン誘導体
CN101318931B (zh) * 2007-06-04 2010-05-19 上海阳帆医药科技有限公司 二芳基取代吡唑衍生物、其制备方法和用途
CN103601792B (zh) 2007-06-04 2016-06-29 协同医药品公司 有效用于胃肠功能紊乱、炎症、癌症和其他疾病治疗的鸟苷酸环化酶激动剂
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
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
GB2456183A (en) * 2008-01-04 2009-07-08 Gw Pharma Ltd Anti-psychotic composition comprising cannabinoids and anti-psychotic medicament
WO2009110510A1 (ja) 2008-03-06 2009-09-11 萬有製薬株式会社 アルキルアミノピリジン誘導体
CA2717384A1 (en) 2008-03-28 2009-10-01 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
AU2009256157B2 (en) 2008-06-04 2014-12-18 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US20110071129A1 (en) 2008-06-19 2011-03-24 Makoto Ando Spirodiamine-diaryl ketoxime derivative
UY31968A (es) 2008-07-09 2010-01-29 Sanofi Aventis Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
JPWO2010013595A1 (ja) 2008-07-30 2012-01-12 Msd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
WO2010015972A1 (en) 2008-08-06 2010-02-11 Pfizer Limited Diazepine and diazocane compounds as mc4 agonists
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
EP2358200A4 (en) 2008-11-17 2012-05-16 Merck Sharp & Dohme SUBSTITUTED BICYCLIC AMINES FOR THE TREATMENT OF DIABETES
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
EP2379562A1 (en) 2008-12-16 2011-10-26 Schering Corporation Bicyclic pyranone derivatives as nicotinic acid receptor agonists
US20110245209A1 (en) 2008-12-16 2011-10-06 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
WO2010079241A1 (es) 2009-01-12 2010-07-15 Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion Uso de antagonistas y/o agonistas inversos de los receptores cb1 para la preparación de medicamentos que incrementen la excitabilidad de las motoneuronas
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011508A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
BR112012003973A2 (pt) 2009-08-26 2015-09-08 Sanofi Sa hidratos de fluoroglicosídeo heteroaromático cristalinos, produtos farmacêuticos compreendendo estes compostos e seu uso
WO2011058193A1 (en) 2009-11-16 2011-05-19 Mellitech [1,5]-diazocin derivatives
CN102791701B (zh) 2009-12-30 2014-02-12 深圳信立泰药业股份有限公司 作为二肽基肽酶iv(dpp-iv)抑制剂的3-(3-氨基哌啶-1-基)-5-氧代-1,2,4-三嗪衍生物
AR079935A1 (es) 2010-01-29 2012-02-29 Abbott Healthcare Products Bv Sintesis de derivados de pirazolin carboxamidina sustituida
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2011137024A1 (en) 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
US9365539B2 (en) 2010-05-11 2016-06-14 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
WO2011156246A1 (en) 2010-06-11 2011-12-15 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
SG192941A1 (en) 2011-02-25 2013-09-30 Merck Sharp & Dohme Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
US8710050B2 (en) 2011-03-08 2014-04-29 Sanofi Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120050A1 (de) 2011-03-08 2012-09-13 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683705B1 (de) 2011-03-08 2015-04-22 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8809325B2 (en) 2011-03-08 2014-08-19 Sanofi Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8895547B2 (en) 2011-03-08 2014-11-25 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683701B1 (de) 2011-03-08 2014-12-24 Sanofi Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
US8680131B2 (en) 2012-07-25 2014-03-25 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating disease conditions, including metabolic disorders and cancers
KR20150036245A (ko) 2012-08-02 2015-04-07 머크 샤프 앤드 돔 코포레이션 항당뇨병 트리시클릭 화합물
US11155521B2 (en) 2012-11-13 2021-10-26 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
IN2015DN03733A (enExample) 2012-11-13 2015-09-18 Us Health
MX2015010935A (es) 2013-02-22 2015-10-29 Merck Sharp & Dohme Compuestos biciclicos antidiabeticos.
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
EP4424697A3 (en) 2013-06-05 2024-12-25 Bausch Health Ireland Limited 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
AU2015255765A1 (en) 2014-05-09 2016-11-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Pyrazole derivatives and their use as cannabinoid receptor mediators
JP6769963B2 (ja) 2014-08-29 2020-10-14 ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ α−アミノ−β−カルボキシムコン酸セミアルデヒド脱炭酸酵素の阻害剤
WO2017151802A1 (en) * 2016-03-04 2017-09-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
AU2017342083A1 (en) 2016-10-14 2019-04-11 Tes Pharma S.R.L. Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
CA3119509A1 (en) 2018-11-20 2020-05-28 Tes Pharma S.R.L Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxxylase
WO2020167701A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. Pyrrolidine orexin receptor agonists
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
PE20231384A1 (es) 2020-08-18 2023-09-12 Merck Sharp And Dohme Llc Agonistas de bicicloheptano pirrolidina de los receptores de orexina
EP4341246A1 (en) * 2021-05-17 2024-03-27 The United States of America, as represented by The Secretary, Department of Health and Human Services A facile and odor-free approach to convert sulfonyl urea derivatives to chalcogenide sulfonyl urea derivatives
JP2025512995A (ja) * 2022-04-07 2025-04-22 コーバス ファーマシューティカルズ インコーポレーテッド カンナビノイド受容体1アンタゴニスト/インバースアゴニスト及びその使用
WO2025103493A1 (zh) * 2023-11-16 2025-05-22 西藏海思科制药有限公司 一种大麻素受体1拮抗剂及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4070365A (en) * 1974-07-12 1978-01-24 U.S. Philips Corporation Pyrazoline compounds
EP0173323A1 (de) * 1984-08-30 1986-03-05 Bayer Ag Amidinoazole
US5624941A (en) * 1992-06-23 1997-04-29 Sanofi Pyrazole derivatives, method of preparing them and pharmaceutical compositions in which they are present

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2713225B1 (fr) * 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
WO2001070700A1 (en) * 2000-03-23 2001-09-27 Solvay Pharmaceuticals B.V. 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
AR034160A1 (es) * 2000-09-30 2004-02-04 Gruenenthal Gmbh Sulfonilguanidinas, medicamentos que contienen estos compuestos y el uso de sulfonilguanidinas

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4070365A (en) * 1974-07-12 1978-01-24 U.S. Philips Corporation Pyrazoline compounds
EP0173323A1 (de) * 1984-08-30 1986-03-05 Bayer Ag Amidinoazole
US5624941A (en) * 1992-06-23 1997-04-29 Sanofi Pyrazole derivatives, method of preparing them and pharmaceutical compositions in which they are present

Also Published As

Publication number Publication date
DE60202270D1 (de) 2005-01-20
ATE284872T1 (de) 2005-01-15
UA74066C2 (en) 2005-10-17
JP2004518763A (ja) 2004-06-24
HK1061852A1 (zh) 2004-10-08
ZA200307322B (en) 2004-12-20
IL153508A (en) 2008-07-08
AR033046A1 (es) 2003-12-03
MXPA03003534A (es) 2005-01-25
RU2281941C2 (ru) 2006-08-20
KR20030082890A (ko) 2003-10-23
CA2422708C (en) 2010-10-26
PT1373216E (pt) 2005-05-31
ES2229132T3 (es) 2005-04-16
IL153508A0 (en) 2003-07-06
HUP0303148A2 (hu) 2004-01-28
SI1373216T1 (en) 2005-06-30
JP4373675B2 (ja) 2009-11-25
AU2002256690B2 (en) 2006-05-18
HUP0303148A3 (en) 2009-08-28
EP1373216A1 (en) 2004-01-02
DE60202270T2 (de) 2005-05-19
KR100846614B1 (ko) 2008-07-16
NO324953B1 (no) 2008-01-14
SK3082003A3 (en) 2003-10-07
PL363751A1 (en) 2004-11-29
EP1373216B1 (en) 2004-12-15
NO20032892L (no) 2003-11-18
CA2422708A1 (en) 2002-10-03
CN1486301A (zh) 2004-03-31
NO20032892D0 (no) 2003-06-23
CZ2003698A3 (cs) 2003-06-18
NZ524633A (en) 2005-02-25
WO2002076949A1 (en) 2002-10-03
SK287592B6 (sk) 2011-03-04
BR0205602A (pt) 2003-07-08

Similar Documents

Publication Publication Date Title
CN100366614C (zh) 具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物
AU2002256690A1 (en) 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
US6476060B2 (en) 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
AU2002333852B2 (en) Novel 4,5-dihydro-1H-pyrazole derivativeshaving CB1-antagonistic activity
AU2001242501A1 (en) 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
KR20040035845A (ko) 효력있는 cb1-길항 작용을 가지는4,5-디하이드로-1h-피라졸 유도체
AU2002333852A1 (en) Novel 4,5-dihydro-1H-pyrazole derivativeshaving CB1-antagonistic activity
TWI227712B (en) 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
ZA200207303B (en) 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity.

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1061852

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1061852

Country of ref document: HK

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20080206

Termination date: 20120318