ECSP045482A - Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia - Google Patents

Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia

Info

Publication number
ECSP045482A
ECSP045482A EC2004005482A ECSP045482A ECSP045482A EC SP045482 A ECSP045482 A EC SP045482A EC 2004005482 A EC2004005482 A EC 2004005482A EC SP045482 A ECSP045482 A EC SP045482A EC SP045482 A ECSP045482 A EC SP045482A
Authority
EC
Ecuador
Prior art keywords
diabetes
obesity
treatment
inhibitors
dislipidemia
Prior art date
Application number
EC2004005482A
Other languages
English (en)
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 filed Critical
Publication of ECSP045482A publication Critical patent/ECSP045482A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

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

Abstract

Los compuestos que tengan Formula I, incluyendo sales farmacéuticamente aceptables, hidratos y solvatos del mismo: son inhibidores selectivos de la enzima 11ß-HSD1. Los compuestos son útiles para el tratamiento de la diabetes, tal como la diabetes no insulina dependiente (DMNID), hiperglicemia, obesidad, resistencia a la insulina, dislipidemia, hiperlipidemia, hipertensión, Síndrome X, y otros síntomas asociados con DMNID.
EC2004005482A 2002-06-10 2004-12-09 Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia ECSP045482A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38738502P 2002-06-10 2002-06-10

Publications (1)

Publication Number Publication Date
ECSP045482A true ECSP045482A (es) 2005-01-28

Family

ID=29736306

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2004005482A ECSP045482A (es) 2002-06-10 2004-12-09 Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia

Country Status (29)

Country Link
US (2) US6730690B2 (es)
EP (1) EP1532122B1 (es)
JP (1) JP4405384B2 (es)
KR (1) KR20050008805A (es)
CN (2) CN1312137C (es)
AR (1) AR040241A1 (es)
AT (1) ATE537155T1 (es)
AU (2) AU2003251410B2 (es)
BR (1) BR0311137A (es)
CA (1) CA2488592C (es)
EC (1) ECSP045482A (es)
ES (1) ES2377200T3 (es)
HK (1) HK1081946A1 (es)
HR (1) HRP20041180A2 (es)
IL (1) IL165257A0 (es)
IS (1) IS7519A (es)
JO (1) JO2315B1 (es)
MA (1) MA27317A1 (es)
MX (1) MXPA04012381A (es)
MY (1) MY134664A (es)
NO (1) NO20050102L (es)
NZ (1) NZ536188A (es)
PE (1) PE20040726A1 (es)
PL (1) PL373372A1 (es)
RU (1) RU2319703C2 (es)
TW (1) TWI324153B (es)
UA (1) UA81417C2 (es)
WO (2) WO2003104207A2 (es)
ZA (1) ZA200408772B (es)

Families Citing this family (161)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030148987A1 (en) * 2001-12-21 2003-08-07 Morris David J. Selective 11beta-HSD inhibitors and methods of use thereof
US20060148725A1 (en) * 2001-12-21 2006-07-06 The Miriam Hospital Selective 11beta HSD inhibitors and methods of use thereof
US7329683B2 (en) 2002-02-01 2008-02-12 Merck & Co., Inc. 11-β-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
JO2397B1 (en) * 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
US8293751B2 (en) 2003-01-14 2012-10-23 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2004097002A2 (en) * 2003-04-29 2004-11-11 The Miriam Hospital SELECTIVE TESTICULAR 11β-HSD INHIBITORS AND METHODS OF USE THEREOF
US20070099884A1 (en) * 2003-06-06 2007-05-03 Erondu Ngozi E Combination therapy for the treatment of diabetes
GB0315111D0 (en) 2003-06-27 2003-07-30 Cancer Rec Tech Ltd Substituted 5-membered ring compounds and their use
JP2007533625A (ja) 2003-09-22 2007-11-22 バイオネットワークス ゲゼルシャフト ミット ベシュレンクテル ハフツング 炎症性及び/又は免疫媒介性の骨量減少の予防及び治療
WO2005044192A2 (en) 2003-10-28 2005-05-19 Amgen Inc. Triazole compounds and uses related thereto
WO2005060694A2 (en) * 2003-12-18 2005-07-07 Agy Therapeutics, Inc. Treatment of neurologic disorders with inhibitors of 11beta-hsd1
US7745630B2 (en) 2003-12-22 2010-06-29 Justin Stephen Bryans Triazolyl piperidine arginine vasopressin receptor modulators
CA2553345C (en) * 2004-01-26 2011-11-15 Merck & Co., Inc. Novel crystalline forms of an inhibitor of 11-beta-hydroxysteroid dehydrogenase type 1
US7354938B2 (en) 2004-03-23 2008-04-08 Amgen Inc. Pyrazole compounds and uses related thereto
AU2005230864A1 (en) 2004-03-29 2005-10-20 Merck Sharp & Dohme Corp. Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
US20050261302A1 (en) * 2004-04-29 2005-11-24 Hoff Ethan D Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their therapeutic application
PL1747198T3 (pl) * 2004-05-07 2008-11-28 Janssen Pharmaceutica Nv Pochodne adamantylopirolidyn-2-onu jako inhibitory 11ß-dehydrogenazy hydroksysteroidowej
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
EP1747199B1 (en) 2004-05-07 2014-09-17 Janssen Pharmaceutica NV Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
WO2005121132A1 (ja) * 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗hcv作用を有する縮合ヘテロ環化合物
US20060025445A1 (en) * 2004-08-02 2006-02-02 Xiang Jason S 11-Beta HSD1 inhibitors
GB0418877D0 (en) * 2004-08-24 2004-09-29 Univ Edinburgh Heart
DE602005017159D1 (de) 2004-08-30 2009-11-26 Janssen Pharmaceutica Nv Oxysteroid-dehydrogenase-inhibitoren
CA2576839C (en) 2004-08-30 2013-07-02 Janssen Pharmaceutica N.V. N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
AU2005279209B2 (en) 2004-08-30 2011-03-24 Janssen Pharmaceutica N.V. Tricyclic lactam derivatives as 11-BETA hydroxysteroid dehydrogenase inhibitors
US7776897B2 (en) 2004-09-16 2010-08-17 Astellas Pharma Inc. Triazole derivative or salt thereof
JP5140577B2 (ja) 2005-03-31 2013-02-06 タケダ カリフォルニア インコーポレイテッド ヒドロキシステロイドデヒドロゲナーゼ阻害剤
PL1928840T3 (pl) 2005-04-05 2012-01-31 Hoffmann La Roche 1H-pirazolo-4-karboksyamidy, ich wytwarzanie i ich zastosowanie jako inhibitory dehydrogenazy 11-beta-hydroksysteroidowej
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
WO2006132197A1 (ja) * 2005-06-07 2006-12-14 Shionogi & Co., Ltd. I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7579360B2 (en) * 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
US7622492B2 (en) 2005-08-31 2009-11-24 Hoffmann-La Roche Inc. Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase
GEP20135838B (en) 2005-09-14 2013-06-10 Takeda Pharmaceutical Dipeptidyl peptidase inhibitors usage at diabetes treatment
CA2622642C (en) 2005-09-16 2013-12-31 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
RU2302066C1 (ru) * 2005-09-22 2007-06-27 Научный центр волоконной оптики при Институте общей физики им. А.М. Прохорова Российской академии наук Волоконный световод для оптического усиления излучения на длине волны в диапазоне 1000-1700 нм, способы его изготовления и волоконный лазер
RU2008116844A (ru) 2005-09-29 2009-11-10 Мерк энд Ко., Инк. (US) Ацилированные производные спиропиперидина как модуляторы рецептора меланокортина-4
WO2007058346A1 (ja) * 2005-11-21 2007-05-24 Shionogi & Co., Ltd. I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物
US7998959B2 (en) 2006-01-12 2011-08-16 Incyte Corporation Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
AU2007207055B2 (en) 2006-01-18 2011-06-02 F. Hoffmann-La Roche Ag Thiazoles as 11 beta-HSD1 inhibitors
WO2007088895A1 (ja) * 2006-01-31 2007-08-09 Mochida Pharmaceutical Co., Ltd. 3-アリールアミノ-1,2,4-トリアゾール誘導体
US7834178B2 (en) 2006-03-01 2010-11-16 Bristol-Myers Squibb Company Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors
US20090082367A1 (en) 2006-03-16 2009-03-26 Astellas Pharma Inc. Triazole derivative or a salt thereof
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
WO2008017381A1 (de) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituierte imidazolidin-2,4-dione, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und ihre verwendung
PT2054049E (pt) 2006-08-24 2016-06-02 Univ Tennessee Res Found Acilanilidas substituídas e métodos de utilização das mesmas
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
EP2698157B1 (en) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
UY30820A1 (es) * 2006-12-21 2008-07-03 Centocor Inc Uso de agonistas del receptor de glp-1 de accion prolongada para mejorar la sensibilidad a la insulina y los perfiles lipidicos
DE102007005045B4 (de) 2007-01-26 2008-12-18 Sanofi-Aventis Phenothiazin Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US8106086B2 (en) 2007-04-02 2012-01-31 Msd K.K. Indoledione derivative
ES2535317T3 (es) 2007-05-18 2015-05-08 Shionogi & Co., Ltd. Derivado heterocíclico que contiene nitrógeno que tiene actividad inhibidora de la 11 beta-hidroxiesteroide deshidrogenasa de tipo 1
JP5223864B2 (ja) 2007-06-27 2013-06-26 大正製薬株式会社 11β−HSD1阻害活性を有する化合物
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8119658B2 (en) * 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
WO2009126861A2 (en) * 2008-04-11 2009-10-15 Bristol-Myers Squibb Company Triazolopyridine compounds useful as dgat1 inhibitors
WO2009126624A1 (en) * 2008-04-11 2009-10-15 Bristol-Myers Squibb Company Triazolo compounds useful as dgat1 inhibitors
TWI465439B (zh) 2008-07-03 2014-12-21 Astellas Pharma Inc 三氮唑衍生物或其鹽
US8470841B2 (en) 2008-07-09 2013-06-25 Sanofi Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
WO2010051236A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Isonicotinamide orexin receptor antagonists
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
AU2009314200B2 (en) 2008-11-17 2011-11-17 Merck Sharp & Dohme Corp. 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
CN102395567A (zh) * 2009-02-12 2012-03-28 埃克塞利希斯股份有限公司 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物
ES2350077B1 (es) 2009-06-04 2011-11-04 Laboratorios Salvat, S.A. Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1.
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011019538A1 (en) 2009-08-13 2011-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
CA2771278A1 (en) 2009-08-26 2011-03-03 Sanofi Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
WO2011028455A1 (en) 2009-09-02 2011-03-10 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US20120269830A1 (en) 2009-12-07 2012-10-25 Lawrence Horowitz Conjugates with improved pharmacokinetic properties
EP2509960A1 (en) * 2009-12-11 2012-10-17 Exelixis, Inc. Tgr5 agonists
US8853212B2 (en) 2010-02-22 2014-10-07 Merck Sharp & Dohme Corp Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8980929B2 (en) 2010-05-21 2015-03-17 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
US8742110B2 (en) 2010-08-18 2014-06-03 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
UA112418C2 (uk) 2010-09-07 2016-09-12 Астеллас Фарма Інк. Терапевтичний болезаспокійливий засіб
AU2011305525B2 (en) 2010-09-22 2016-08-18 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683704B1 (de) 2011-03-08 2014-12-17 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8901114B2 (en) 2011-03-08 2014-12-02 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
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
WO2012120054A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683703B1 (de) 2011-03-08 2015-05-27 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683702B1 (de) 2011-03-08 2014-12-24 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende 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
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
AU2012240122B2 (en) 2011-04-08 2016-08-25 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
ES2617215T3 (es) * 2011-04-19 2017-06-15 Daiichi Sankyo Company, Limited Derivado de tetrahirotiazepina
US20140088124A1 (en) 2011-06-02 2014-03-27 Robert J. DeVita Imidazole derivatives
JP2014517036A (ja) 2011-06-16 2014-07-17 メルク・シャープ・アンド・ドーム・コーポレーション 置換シクロプロピル化合物、そのような化合物を含有する組成物および治療方法
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9422266B2 (en) 2011-09-30 2016-08-23 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
WO2013062838A1 (en) 2011-10-24 2013-05-02 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
WO2013068328A1 (en) 2011-11-07 2013-05-16 Intervet International B.V. Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors
WO2013068439A1 (en) 2011-11-09 2013-05-16 Intervet International B.V. 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors
WO2013074388A1 (en) 2011-11-15 2013-05-23 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as gpr119 agonists
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
IN2014DN09640A (es) 2012-04-16 2015-07-31 Kaneq Pharma Inc
US10987334B2 (en) 2012-07-13 2021-04-27 University Of Tennessee Research Foundation Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs)
US10314807B2 (en) 2012-07-13 2019-06-11 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US9969683B2 (en) 2012-07-13 2018-05-15 Gtx, Inc. Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS)
US9622992B2 (en) 2012-07-13 2017-04-18 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US9744149B2 (en) 2012-07-13 2017-08-29 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
PT2872482T (pt) 2012-07-13 2020-09-22 Oncternal Therapeutics Inc Método de tratamento de cancro de mama com modulador seletivo do recetor de andrógeno (sarm)
EP2874622A4 (en) 2012-07-23 2015-12-30 Merck Sharp & Dohme TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS
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
EP2931734B1 (en) 2012-12-17 2020-12-02 Merck Sharp & Dohme Corp. Novel glucokinase activator compounds, compositions containing such compounds, and methods of treatment
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2015089809A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
EP3097101B1 (en) 2014-01-24 2020-12-23 Merck Sharp & Dohme Corp. Isoquinoline derivatives as mgat2 inhibitors
WO2015176267A1 (en) 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CA2950357A1 (en) 2014-06-12 2015-12-17 Universite De Lille 2 Droit Et Sante Imidazol- or 1,2,4-triazol-derivatives and their use
EP3177282B1 (en) 2014-08-08 2021-10-06 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP3177287B1 (en) 2014-08-08 2022-02-23 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP3177285B1 (en) 2014-08-08 2020-09-23 Merck Sharp & Dohme Corp. [5,6]-fused bicyclic antidiabetic compounds
EA201790914A1 (ru) 2014-10-24 2017-08-31 Мерк Шарп И Доум Корп. Коагонисты рецепторов глюкагона и glp-1
EP3701969A1 (en) 2014-10-31 2020-09-02 NGM Biopharmaceuticals, Inc. Compositions and methods of use for treating metabolic disorders
TW201625635A (zh) 2014-11-21 2016-07-16 默沙東藥廠 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物
WO2016112075A1 (en) 2015-01-06 2016-07-14 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
EP3303342B1 (en) 2015-05-27 2021-03-17 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
EP3310782B1 (en) 2015-05-28 2021-12-01 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
BR112017027656B1 (pt) 2015-06-22 2023-12-05 Arena Pharmaceuticals, Inc. Hábito cristalino de placa livre de sal de l-arginina de ácido (r)-2-(7-(4- ciclopentil-3-(trifluorometil)benzilóxi)- 1,2,3,4-tetra-hidrociclo-penta[b]indol-3- il)acético, composição farmacêutica que o compreende, seus usos e método de preparação do mesmo
EP3359191A4 (en) 2015-10-05 2019-05-29 Merck Sharp & Dohme Corp. ANTIBODY-PEPTIDE CONJUGATES HAVING AGONIST ACTIVITY AT GLUCAGON AND PEPTIDE-1 RECEPTORS SIMILAR TO GLUCAGON
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
EP3235813A1 (en) 2016-04-19 2017-10-25 Cidqo 2012, S.L. Aza-tetra-cyclo derivatives
WO2017197555A1 (en) 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
US10414774B2 (en) 2016-08-15 2019-09-17 Merck Sharp & Dohme Corp. Compound useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolc disease
WO2018034917A1 (en) 2016-08-15 2018-02-22 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
EP3515891B1 (en) 2016-09-20 2023-03-08 Merck Sharp & Dohme LLC Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as pcsk9 allosteric binders
WO2018093698A1 (en) 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. Indole derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
WO2018107415A1 (en) 2016-12-15 2018-06-21 Merck Sharp & Dohme Corp. Hydroxy isoxazole compounds useful as gpr120 agonists
AU2018220521A1 (en) 2017-02-16 2019-09-05 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
JOP20190150A1 (ar) 2018-06-21 2019-12-21 Merck Sharp & Dohme مركبات مناهضة لـ pcsk9
TW202045476A (zh) 2019-02-13 2020-12-16 美商默沙東藥廠 5-烷基吡咯啶食慾素受體促效劑
WO2020205688A1 (en) 2019-04-04 2020-10-08 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
EP4010314B1 (en) 2019-08-08 2024-02-28 Merck Sharp & Dohme LLC Heteroaryl pyrrolidine and piperidine orexin receptor agonists
WO2021041770A1 (en) 2019-08-30 2021-03-04 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds
EP3842060A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled lactam co-agonists of the glucagon and glp-1 receptors
EP3842061A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled triazole co-agonists of the glucagon and glp-1 receptors
EP3842449A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled olefin co-agonists of the glucagon and glp-1 receptors
US11787810B2 (en) 2020-05-18 2023-10-17 Merck Sharp & Dohme Llc Diacylglyceride O-acyltransferase 2 inhibitors
BR112023002957A2 (pt) 2020-08-18 2023-04-04 Merck Sharp & Dohme Llc Composto, composição farmacêutica, e, métodos para tratar narcolepsia e para tratar hipersonia em um sujeito mamífero
KR102445638B1 (ko) 2020-09-03 2022-09-20 충남대학교산학협력단 11 알파 하이드록시프로게스테론을 포함하는 당뇨병 예방 또는 치료용 조성물
AU2021356589A1 (en) 2020-10-08 2023-05-25 Merck Sharp & Dohme Llc Preparation of benzimidazolone derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors
KR20240050369A (ko) 2021-08-19 2024-04-18 머크 샤프 앤드 돔 엘엘씨 Pcsk9 활성과 관련된 상태를 치료하기 위한 화합물
CN116003279B (zh) * 2022-06-13 2024-05-28 苏州大学 一种绿色的n-甲基酰胺化合物的制备方法
TW202404574A (zh) 2022-06-15 2024-02-01 美商默沙東有限責任公司 用於捕捉介白素-1 β之環狀肽
WO2024118858A1 (en) 2022-12-02 2024-06-06 Merck Sharp & Dohme Llc Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0100860A3 (en) 1997-12-11 2003-03-28 Janssen Pharmaceutica Nv Retinoic acid mimetic anilides, process for their preparation and pharmaceutical compositions containing them
US20030073850A1 (en) 1998-08-07 2003-04-17 Altenbach Robert J. 4-Imidazole derivatives of benzyl and restricted benzyl sulfonamides, sulfamides, ureas, carbamates, and amides and their use
US6503935B1 (en) 1998-08-07 2003-01-07 Abbott Laboratories Imidazoles and related compounds as α1A agonists
SE0001899D0 (sv) * 2000-05-22 2000-05-22 Pharmacia & Upjohn Ab New compounds
JPWO2003004497A1 (ja) 2001-07-05 2004-10-28 住友製薬株式会社 新規複素環化合物
JO2397B1 (en) * 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors

Also Published As

Publication number Publication date
JO2315B1 (en) 2005-09-12
WO2003104207A2 (en) 2003-12-18
WO2003104207A3 (en) 2004-03-25
WO2003104208A1 (en) 2003-12-18
HK1081946A1 (en) 2006-05-26
AU2003251410A1 (en) 2003-12-22
CN1312137C (zh) 2007-04-25
RU2319703C2 (ru) 2008-03-20
CN1990474A (zh) 2007-07-04
AU2003243420A1 (en) 2003-12-22
ES2377200T3 (es) 2012-03-23
MA27317A1 (fr) 2005-05-02
AU2003243420A8 (en) 2003-12-22
PL373372A1 (en) 2005-08-22
TW200410947A (en) 2004-07-01
RU2004139063A (ru) 2005-06-27
NO20050102L (no) 2005-02-10
JP4405384B2 (ja) 2010-01-27
US20040048912A1 (en) 2004-03-11
BR0311137A (pt) 2005-02-22
MXPA04012381A (es) 2005-04-19
TWI324153B (en) 2010-05-01
US6730690B2 (en) 2004-05-04
ZA200408772B (en) 2005-11-18
IL165257A0 (en) 2005-12-18
ATE537155T1 (de) 2011-12-15
JP2005532357A (ja) 2005-10-27
US20040106664A1 (en) 2004-06-03
EP1532122B1 (en) 2011-12-14
KR20050008805A (ko) 2005-01-21
MY134664A (en) 2007-12-31
NZ536188A (en) 2006-11-30
CA2488592C (en) 2010-08-10
PE20040726A1 (es) 2004-10-23
EP1532122A1 (en) 2005-05-25
US7179802B2 (en) 2007-02-20
CA2488592A1 (en) 2003-12-18
HRP20041180A2 (en) 2005-08-31
UA81417C2 (en) 2008-01-10
IS7519A (is) 2004-10-29
AU2003251410B2 (en) 2009-05-21
AR040241A1 (es) 2005-03-23
CN1659151A (zh) 2005-08-24

Similar Documents

Publication Publication Date Title
ECSP045482A (es) Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia
ECSP055860A (es) Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
NI200800069A (es) Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide-deshidrogenasa-1
EP1797034A4 (en) SULFONYL COMPOUNDS AS AN INHIBITORS OF 11-BETA-HYDROXYSTEROIDDEHYDROGENASE-1
CR8402A (es) Indazol-o-glucosidos sustitutos
DK2035379T3 (da) Inhibitorer af 11-beta-hydroxysteroiddehydrogenase 1
DE60301491D1 (en) Acc-hemmer
MX2008013484A (es) Derivados de lactamas de ciclohexilpirazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1.
CA2534221A1 (en) Pyrazole carboxamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
MX2007005408A (es) Compuestos de aminoquinazolinas.
NO20044866L (no) Pyrazolo-pyrimidin-anilin-forbindelser anvendelige som kinase-inhibitorer
PL2021337T3 (pl) Inhibitory dehydrogenazy 11-beta-hydroksysteroidowej typu 1
UY29246A1 (es) Nuevos compuestos
CY1107945T1 (el) Διφαινυλκαρβοξαμιδια υποκατεστημενα με ν-αρυλ πιπεριδινη ως αναστολεις της εκκρισης της απολιποπρωτεϊνης β
NO20044534L (no) Substituerte fenylacetamider og deres anvendelse som glukokinaseaktivatorer
HK1162469A1 (en) Dgat inhibitor dgat
EA200870472A1 (ru) Ингибиторы 11-бета-гидроксистероид-дегидрогеназы типа 1
IL194879A0 (en) Pieridinyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
IL187005A0 (en) Diacylglycerol acyltransferase inhibitors
AR064955A1 (es) Composicion y metodo para estabilizar ingredientes sensibles
BRPI0417469A (pt) bifenil carboxamidas substituìdas com n-aril piperidina
DOP2003000658A (es) Inhibidores de la 11-beta-hydroxiesteroide deshidrogenasa 1 para la elaboracion de tratamiento de la diabetes, obesidad y dislipidemia
DOP2003000795A (es) Derivados de triazol como inhibidores de ii-beta- hidroxiesteroide deshidrogenasa-1
DE602004019698D1 (de) Morpholinderivate als inhibitoren der wiederaufnahme von norepinephrin
TNSN08095A1 (en) Association of 3 receptor agonist and monoamine reuptake inhibitors, pharmaceutical composition containing same and therapeutic use thereof