CN102918027A - Gpr119受体调节剂和对与所述受体有关的障碍的治疗 - Google Patents

Gpr119受体调节剂和对与所述受体有关的障碍的治疗 Download PDF

Info

Publication number
CN102918027A
CN102918027A CN2011800275776A CN201180027577A CN102918027A CN 102918027 A CN102918027 A CN 102918027A CN 2011800275776 A CN2011800275776 A CN 2011800275776A CN 201180027577 A CN201180027577 A CN 201180027577A CN 102918027 A CN102918027 A CN 102918027A
Authority
CN
China
Prior art keywords
alkyl
oxygen base
base
methyl
group
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.)
Pending
Application number
CN2011800275776A
Other languages
English (en)
Chinese (zh)
Inventor
R.M.琼斯
韩相敦
D.J.布扎德
J.莱曼
S.纳拉亚南
岳大伟
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.)
Arena Pharmaceuticals Inc
Original Assignee
Arena Pharmaceuticals Inc
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 Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Publication of CN102918027A publication Critical patent/CN102918027A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P3/08Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
CN2011800275776A 2010-04-06 2011-04-05 Gpr119受体调节剂和对与所述受体有关的障碍的治疗 Pending CN102918027A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US34186610P 2010-04-06 2010-04-06
US61/341,866 2010-04-06
US40186310P 2010-08-20 2010-08-20
US61/401,863 2010-08-20
PCT/US2011/031243 WO2011127051A1 (en) 2010-04-06 2011-04-05 Modulators of the gpr119 receptor and the treatment of disorders related thereto

Publications (1)

Publication Number Publication Date
CN102918027A true CN102918027A (zh) 2013-02-06

Family

ID=44151966

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800275776A Pending CN102918027A (zh) 2010-04-06 2011-04-05 Gpr119受体调节剂和对与所述受体有关的障碍的治疗

Country Status (9)

Country Link
US (1) US20130023494A1 (enExample)
EP (1) EP2556056A1 (enExample)
JP (1) JP2013523819A (enExample)
CN (1) CN102918027A (enExample)
AU (1) AU2011237775A1 (enExample)
BR (1) BR112012025592A2 (enExample)
CA (1) CA2795513A1 (enExample)
MX (1) MX2012011631A (enExample)
WO (1) WO2011127051A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102731492B (zh) * 2011-03-30 2016-06-29 江苏恒瑞医药股份有限公司 环己烷类衍生物、其制备方法及其在医药上的应用

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602004009295T2 (de) 2003-01-14 2008-07-03 Arena Pharmaceuticals, Inc., San Diego 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie
KR101526592B1 (ko) * 2009-09-17 2015-06-05 주식회사 엘지생활건강 피부주름 개선용 조성물
SG10201500639TA (en) 2010-01-27 2015-03-30 Arena Pharm Inc Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
EP2571864A1 (en) 2010-05-17 2013-03-27 Array Biopharma, Inc. Piperidinyl-substituted lactams as gpr119 modulators
FR2960875B1 (fr) * 2010-06-04 2012-12-28 Sanofi Aventis Derives de carbamates d'hexafluoroisopropyle, leur preparation et leur application en therapeutique
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) * 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EA031618B1 (ru) 2011-06-09 2019-01-31 Ризен Фармасьютикалз Са Соединения-модуляторы gpr-119
EP2760855B1 (en) 2011-09-30 2017-03-15 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes
WO2013055910A1 (en) * 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EP2771000B1 (en) * 2011-10-24 2016-05-04 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
DK2858986T3 (da) * 2012-06-12 2019-11-25 Chong Kun Dang Pharmaceutical Corp Piperidinderivater som gpr119-agonister
CA2878625A1 (en) 2012-07-11 2014-01-16 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014074700A1 (en) * 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Antagonists of gpr119 receptor and the treatment of disorders related thereto
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
NZ720304A (en) 2013-11-26 2017-08-25 Chong Kun Dang Pharmaceutical Corp Amide derivatives for gpr119 agonist
ES2995737T3 (en) 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
AR111199A1 (es) * 2017-03-31 2019-06-12 Takeda Pharmaceuticals Co Compuesto aromático agonista de gpr40
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
TW202325306A (zh) 2021-09-02 2023-07-01 美商天恩治療有限公司 改良免疫細胞之生長及功能的方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004067575A (ja) * 2002-08-06 2004-03-04 Yaizu Suisankagaku Industry Co Ltd 糖尿病治療薬効果促進剤
CN1212117C (zh) * 1995-06-20 2005-07-27 武田药品工业株式会社 用于治疗糖尿病的药物组合物
CN1823056A (zh) * 2003-07-11 2006-08-23 艾尼纳制药公司 作为新陈代谢调节剂的三取代芳基和杂芳基衍生物以及预防和治疗与其相关之病症
CN101657471A (zh) * 2006-12-06 2010-02-24 史密丝克莱恩比彻姆公司 二环化合物及其作为抗糖尿病药的用途
WO2010074271A1 (ja) * 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤

Family Cites Families (241)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD296075A5 (de) 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
DK0528858T3 (da) 1990-04-14 1997-07-28 Univ Tufts Med Inhibitorer af dipeptidyl-aminopeptidase type IV
EP1050540B1 (en) 1991-10-22 2006-12-27 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
MX9206628A (es) 1991-11-22 1993-05-01 Boehringer Ingelheim Pharma Ester de prolinaboronato y metodo para su preparacion.
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
JPH1081666A (ja) 1996-06-12 1998-03-31 Ishihara Sangyo Kaisha Ltd フタルイミド誘導体又はその塩、それらの製造方法及びそれらを含有する医薬組成物
AU4721897A (en) 1996-10-25 1998-05-22 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
JPH10182613A (ja) 1996-10-25 1998-07-07 Tanabe Seiyaku Co Ltd テトラヒドロイソキノリン誘導体
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
CN1163594C (zh) 1997-09-29 2004-08-25 尖端医疗有限公司 体外造血细胞的刺激
DE69839279T2 (de) 1997-11-18 2009-05-28 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Neue physiologisch aktive substanz sulphostin, herstellung und verwendung derselben
DE04029691T1 (de) 1998-02-02 2007-11-08 Trustees Of Tufts College, Medford Verwendung von Dipetidylpeptidasehemmer zur Regulierung des Glukosemetabolismus
AU770319C (en) 1998-05-04 2004-11-25 Point Therapeutics, Inc. Hematopoietic stimulation
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
JP2002517401A (ja) 1998-06-05 2002-06-18 ポイント セラピューティクス, インコーポレイテッド 環状ボロプロリン化合物
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
WO2000010549A1 (en) 1998-08-21 2000-03-02 Point Therapeutics, Inc. Regulation of substrate activity
WO2000020592A1 (en) 1998-10-07 2000-04-13 Medical College Of Georgia Research Institute, Inc. Glucose-dependent insulinotropic peptide for use as an osteotropic hormone
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
ES2308759T3 (es) 1998-11-20 2008-12-01 Arena Pharmaceuticals, Inc. Receptores acoplados a proteina g humanos huerfanos.
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
JP2000191616A (ja) 1998-12-24 2000-07-11 Senju Pharmaceut Co Ltd 新規ジペプチジルアルデヒド誘導体およびそれを含有する医薬
GB9906714D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for improving fertility
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
JP4121215B2 (ja) 1999-05-17 2008-07-23 財団法人微生物化学研究会 スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法
EP1187619A1 (en) 1999-05-25 2002-03-20 Point Therapeutics, Inc. Anti-tumor agents comprising boroproline compounds
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
AU1916401A (en) 1999-11-12 2001-06-06 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
ES2275654T5 (es) 2000-01-21 2012-06-07 Novartis Ag Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos
JP2003520849A (ja) 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivの阻害剤であるn−置換2−シアノピロールおよび−ピロリン
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
GB0014969D0 (en) 2000-06-19 2000-08-09 Smithkline Beecham Plc Novel method of treatment
AUPQ844600A0 (en) 2000-06-29 2000-07-27 Australian Loyalty Systems Pty Ltd Protecting against impluse expenditure
MXPA02012272A (es) 2000-07-04 2003-04-25 Novo Nordisk As Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv.
CA2418656C (en) 2000-08-10 2011-02-01 Mitsubishi Pharma Corporation Proline derivatives and use thereof as drugs
JP4329290B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 脂肪族含窒素五員環化合物
AU2001294196B2 (en) 2000-10-06 2005-11-17 Tanabe Seiyaku Co., Ltd. Nitrogenous five-membered ring compounds
JP2004035574A (ja) 2000-10-06 2004-02-05 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
JP4329291B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 含窒素五員環化合物
AUPR107800A0 (en) 2000-10-27 2000-11-23 University Of Sydney, The Peptide and nucleic acid molecule ii
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
AU2002218509A1 (en) 2000-12-01 2002-06-11 Yamanouchi Pharmaceutical Co..Ltd. Method of screening remedy for diabetes
JPWO2002051836A1 (ja) 2000-12-27 2004-04-22 協和醗酵工業株式会社 ジペプチジルペプチダーゼ−iv阻害剤
WO2002055088A1 (en) 2001-01-16 2002-07-18 Nippon Kayaku Kabushiki Kaisha Remedies for bone marrow suppression and infectious diseases and white blood cell count elevating agents
JP4213390B2 (ja) 2001-02-02 2009-01-21 武田薬品工業株式会社 縮合複素環化合物
SK10802003A3 (sk) 2001-02-02 2004-05-04 Takeda Chemical Industries, Ltd. Kondenzovaná heterocyklická zlúčenina, jej použitie a jej farmaceutický prípravok
MXPA03007349A (es) 2001-02-24 2003-12-04 Boehringer Ingelheim Pharma Derivados de xantina, su preparacion y su empleo como medicamentos.
JP2002265439A (ja) 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
CA2441092A1 (en) 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
FR2822826B1 (fr) 2001-03-28 2003-05-09 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB0109146D0 (en) 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE60224189T2 (de) 2001-06-20 2008-12-11 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
US7183290B2 (en) 2001-06-27 2007-02-27 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7196201B2 (en) 2001-06-27 2007-03-27 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
CA2419888A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
ES2296979T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
CA2418543A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag New dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
DE60225556D1 (de) 2001-07-03 2008-04-24 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
TWI246510B (en) 2001-09-14 2006-01-01 Mitsubishi Pharma Corp Thiazolidine derivatives and pharmaceutical uses thereof
WO2003024965A2 (en) 2001-09-19 2003-03-27 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
CA2464995A1 (en) 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
AU2002357767C1 (en) 2001-11-26 2009-03-19 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
JP2005511636A (ja) 2001-11-26 2005-04-28 トラスティーズ オブ タフツ カレッジ 自己免疫疾患の治療方法及びそれに関する試薬
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
EP1480999A2 (en) 2002-02-08 2004-12-01 Idun Pharmaceuticals (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
KR100608414B1 (ko) 2002-02-13 2006-08-02 에프. 호프만-라 로슈 아게 신규한 피리딘- 및 피리미딘-유도체
EP1476429B1 (en) 2002-02-13 2005-11-16 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
US6906074B2 (en) 2002-02-22 2005-06-14 Nippon Zoki Pharmaceutical Co., Ltd. 2-phenylpiperazine derivatives
DE60304911D1 (de) 2002-02-25 2006-06-08 Eisai Co Ltd Xanthin-Derivate als DPP-IV-Inhibitoren
JP2004043429A (ja) 2002-02-25 2004-02-12 Eisai Co Ltd 新規キサンチン誘導体およびdppiv阻害剤
DE60217186T2 (de) 2002-02-28 2007-09-27 Prosidion Ltd. Dpiv-inhibitoren auf glutaminbasis
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
DE60322857D1 (de) 2002-03-25 2008-09-25 Nippon Kayaku Kk Neues alpha-amino-n-(diaminophosphinyl)lactamderivat
EP1490335B1 (en) 2002-03-25 2007-09-19 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP4329382B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
JP4329381B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
RU2004132719A (ru) 2002-04-08 2005-08-27 Торрент Фармасьютикалз Лтд. (In) Тиазолидин-4-карбонитрилы и их аналоги, применение указанных соединений в качестве ингибиторов дипептидилпептидаз
JP2003300977A (ja) 2002-04-10 2003-10-21 Sumitomo Pharmaceut Co Ltd キサンチン誘導体
JP2004026820A (ja) 2002-05-09 2004-01-29 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼiv阻害剤
AU2003235913A1 (en) 2002-05-09 2003-11-11 Taisho Pharmaceutical Co., Ltd. Cyanopyrrolidine derivatives
JP2003327532A (ja) 2002-05-10 2003-11-19 Takeda Chem Ind Ltd ペプチダーゼ阻害剤
GB0212412D0 (en) 2002-05-29 2002-07-10 Novartis Ag Combination of organic compounds
PT1513519E (pt) 2002-06-03 2009-05-06 Novartis Ag Uso de cianopirrolidinas substituídas e preparações de combinações que as contêm para tratar hiperlipidemia e doenças associadas
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
AU2003232405A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
WO2003101449A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
CA2485641C (en) 2002-06-06 2010-12-14 Eisai Co., Ltd. Novel condensed imidazole derivatives
EP1549336B1 (en) 2002-06-14 2011-01-05 Amylin Pharmaceuticals, Inc. Prevention and/or treatment of ulcerative colitis using pyy or pyy[3-36]
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
JP2004026678A (ja) 2002-06-24 2004-01-29 Microbial Chem Res Found 2型糖尿病治療剤
IL166156A0 (en) 2002-07-09 2006-01-15 Point Therapeutics Inc Boroproline compound combination therapy
AU2003248259A1 (en) 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
DE10231370B4 (de) 2002-07-11 2006-04-06 Sanofi-Aventis Deutschland Gmbh Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
TW200401635A (en) 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
TW200404060A (en) 2002-08-08 2004-03-16 Takeda Chemical Industries Ltd Fused heterocyclic compounds
JP4542757B2 (ja) 2002-08-08 2010-09-15 武田薬品工業株式会社 縮合複素環化合物
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
DK1532149T3 (da) 2002-08-21 2010-05-10 Boehringer Ingelheim Pharma 8-[3-amino-piperiden-1-yl]-xanthiner, fremstilling deraf og anvendelse deraf som lægemiddel
DE10238243A1 (de) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
UA78104C2 (en) 2002-08-29 2007-02-15 Taisho Pharmaceutical Co Ltd Benzenesulfonate salts of 4-fluoro-2-cyanopyrrolidine derivatives
JP4712387B2 (ja) 2002-09-19 2011-06-29 アボット・ラボラトリーズ ジペプチジルペプチダーゼ−iv(dpp−iv)阻害薬としての医薬組成物
DE60315687T2 (de) 2002-10-07 2008-06-05 Merck & Co., Inc. Antidiabetische heterocyclische beta-aminoverbindungen als inhibitoren von dipeptidylpeptidase
AU2003269850A1 (en) 2002-10-08 2004-05-04 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
PL216527B1 (pl) 2002-10-18 2014-04-30 Merck & Co Inc Związki ß-aminoheterocykliczne i kompozycja farmaceutyczna
US6995180B2 (en) 2002-10-23 2006-02-07 Bristol Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase IV and methods
WO2004041795A1 (en) 2002-10-30 2004-05-21 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
WO2004048379A1 (ja) 2002-11-01 2004-06-10 Sumitomo Pharmaceuticals Co., Ltd. キサンチン化合物
EP1562925B1 (en) 2002-11-07 2007-01-03 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004046106A1 (en) 2002-11-18 2004-06-03 Pfizer Products Inc. Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides
DE10256264A1 (de) 2002-12-03 2004-06-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
UY28103A1 (es) 2002-12-03 2004-06-30 Boehringer Ingelheim Pharma Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
CN100348189C (zh) 2002-12-10 2007-11-14 诺瓦提斯公司 DPP-IV抑制剂与PPAR-α化合物的组合
WO2004058266A1 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE602004009295T2 (de) 2003-01-14 2008-07-03 Arena Pharmaceuticals, Inc., San Diego 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie
US7265128B2 (en) 2003-01-17 2007-09-04 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2004244412A (ja) 2003-01-20 2004-09-02 Kotobuki Seiyaku Kk 4位に置換基を有する2−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤
DK1595866T3 (en) 2003-01-31 2016-08-22 Sanwa Kagaku Kenkyusho Co Cyanopyrrolidines suitable for the treatment of inter alia metabolism syndrome
AU2004210149A1 (en) 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
JP2006518763A (ja) 2003-02-24 2006-08-17 アリーナ ファーマシューティカルズ, インコーポレイテッド グルコース代謝のモジュレーターとしてのフェニル−およびピリジルピペリジン誘導体
AU2003207881A1 (en) 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
ES2363941T3 (es) 2003-03-14 2011-08-19 Astellas Pharma Inc. Derivados de c-glucósido para el tratamiento de diabetes.
AR043515A1 (es) 2003-03-19 2005-08-03 Merck & Co Inc Procedimiento para preparar derivados quirales beta aminoacidos mediante hidrogenacion asimetrica
WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
WO2004087650A2 (en) 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
WO2004092128A1 (en) 2003-04-10 2004-10-28 Smithkline Beecham Corporation Anhydrous crystalline forms of (2s, 4s)-1-{(2r)-2-amino-3-‘4-methoxybenzyl)sulfonyl!-3-methylbutanoyl}-4-fluoropyrrolindine-2-carbonitrile
JPWO2004096806A1 (ja) 2003-04-30 2006-07-13 大日本住友製薬株式会社 縮合イミダゾール誘導体
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
CN1787823A (zh) 2003-05-14 2006-06-14 麦克公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的3-氨基-4-苯基丁酸衍生物
EP1631680A2 (en) 2003-05-21 2006-03-08 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4)
EP1631679A2 (en) 2003-05-21 2006-03-08 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CN1798556A (zh) 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
US20070099884A1 (en) 2003-06-06 2007-05-03 Erondu Ngozi E Combination therapy for the treatment of diabetes
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
JP4579239B2 (ja) 2003-06-17 2010-11-10 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療または予防するためのジペプチジルペプチダーゼ阻害剤としてのシクロヘキシルグリシン誘導体
DE10327439A1 (de) 2003-06-18 2005-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2004251829B2 (en) 2003-06-20 2009-12-17 F. Hoffmann-La Roche Ag Hexahydropyridoisoqinolines as DPP-IV inhibitors
DK1638970T3 (da) 2003-06-20 2011-01-03 Hoffmann La Roche Pyrid (2, 1-A)-isoquinolinderivater som DPP-IV-inhibitorer
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
JP2005023038A (ja) 2003-07-04 2005-01-27 Taisho Pharmaceut Co Ltd 慢性腎疾患治療薬
AR045047A1 (es) * 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
CN1852893A (zh) 2003-07-21 2006-10-25 史密丝克莱恩比彻姆公司 (2S,4S)-4-氟-1-[4-氟-β-(4-氟苯基)-L-苯基丙氨酰基]-2-吡咯烷甲腈对甲苯磺酸盐及其无水晶体形式
PE20050249A1 (es) 2003-07-25 2005-06-01 Aventis Pharma Gmbh Nuevas cianopirrolididas y procedimiento para su preparacion como medicamentos
US7008957B2 (en) 2003-07-25 2006-03-07 Sanofi-Aventis Deutschland Gmbh Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
DE10333935A1 (de) 2003-07-25 2005-02-24 Aventis Pharma Deutschland Gmbh Neue bicyclische Cyanoheterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7094800B2 (en) 2003-07-25 2006-08-22 Sanofi-Aventis Deutschland Gmbh Cyanopyrrolidides, process for their preparation and their use as medicaments
WO2005011581A2 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
ES2649737T5 (es) 2003-08-01 2021-07-07 Mitsubishi Tanabe Pharma Corp Compuestos novedosos que tienen actividad inhibidora frente a transportador de glucosa dependiente de sodio
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
WO2005019168A2 (en) 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors
JP2007504230A (ja) 2003-09-02 2007-03-01 メルク エンド カムパニー インコーポレーテッド ジペプチジルペプチダーゼ−iv阻害剤のリン酸塩の新規結晶性形態
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
EP1697342A2 (en) 2003-09-08 2006-09-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AR046330A1 (es) 2003-09-09 2005-12-07 Japan Tobacco Inc Inhibidor de dipeptidilpeptidasa iv
EP1667524A4 (en) 2003-09-23 2009-01-14 Merck & Co Inc NEW CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYLPEPTIDASE IV INHIBITOR
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
ATE534404T1 (de) 2003-10-03 2011-12-15 Takeda Pharmaceutical Dipeptidylpeptidase-iv-inhibitoren zur behandlung von diabetes-patienten mit sekundärversagen durch sulfonylharnstoffe
DE10348022A1 (de) 2003-10-15 2005-05-25 Imtm Gmbh Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348044A1 (de) 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
TW200519105A (en) 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
TW200523252A (en) 2003-10-31 2005-07-16 Takeda Pharmaceutical Pyridine compounds
JP2007510651A (ja) 2003-11-04 2007-04-26 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−iv阻害剤としての縮合フェニルアラニン誘導体
AR046778A1 (es) 2003-11-12 2005-12-21 Phenomix Corp Compuestos heterociclicos de acido boronico. metodos de obtencion y composiciones farmaceuticas.
KR20140089408A (ko) 2003-11-17 2014-07-14 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
DE10360835A1 (de) 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
CA2554493C (en) 2004-02-05 2012-06-26 Kyorin Pharmaceutical Co., Ltd. Bicycloester derivative
AU2005215136A1 (en) 2004-02-20 2005-09-01 Novartis Ag DPP-IV inhibitors for treating neurodegeneration and cognitive disorders
BRPI0507972A (pt) 2004-02-23 2007-07-24 Tufts College composto ,composição farmacêutica , uso de um composto, método para inibição da atividade proteolìtica de uma enzima de clivagem pós prolina e composição farmacêutica embalada
US20090209491A1 (en) 2004-02-23 2009-08-20 Trustees Of Tufts College Lactams as conformationally constrained peptidomimetic inhibitors
EP1729774A4 (en) 2004-03-09 2009-05-06 Nat Health Research Institutes PYRROLIDINE CONNECTIONS
EA013427B1 (ru) 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
CN103030617A (zh) 2004-03-16 2013-04-10 贝林格尔.英格海姆国际有限公司 吡喃葡萄糖基取代的苯基衍生物、含该化合物的药物、其用途及其制造方法
HRP20090471T1 (hr) 2004-05-12 2009-10-31 Pfizer Products Inc. Derivati prolina i njihova upotreba kao inhibitori dipeptidil-peptidaze iv
DE102004038270A1 (de) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituierte, bizyklische 8-Amino-xanthine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
AP2007003973A0 (en) 2004-10-12 2007-07-30 Glenmark Pharmaceuticals Sa Novel dideptidyl peptidase IV inhibitors, pharmaceutical compositions containing them, and proces for their preparation
MX2007007483A (es) 2004-12-24 2007-07-20 Dainippon Sumitomo Pharma Co Derivados de pirroles biciclicos.
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
TW200637869A (en) 2005-01-28 2006-11-01 Chugai Pharmaceutical Co Ltd The spiroketal derivatives and the use as therapeutical agent for diabetes of the same
EA013119B1 (ru) 2005-02-18 2010-02-26 Мицубиси Танабе Фарма Корпорейшн Соль производного пролина, ее сольват и способ ее получения
AU2006226447B2 (en) 2005-03-22 2009-07-16 F. Hoffmann-La Roche Ag New salt and polymorphs of a DPP-IV inhibitor
JP4568361B2 (ja) 2005-04-22 2010-10-27 アラントス・ファーマシューティカルズ・ホールディング・インコーポレーテッド ジペプチジルペプチダーゼ−iv阻害剤
CA2611446A1 (en) 2005-06-09 2006-12-14 Banyu Pharmaceutical Co., Ltd. Npy y2 agonist for use as therapeutic agent for disease accompanied by diarrhea
ITBG20050040A1 (it) 2005-07-29 2007-01-30 Trasmetal Spa Cabina di verniciatura per impianti di verniciatura di manufatti.
CA2617327A1 (en) 2005-08-04 2007-02-15 Novartis Ag Salts of vildagliptin
NZ565461A (en) 2005-08-30 2011-08-26 Abbott Lab Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200745079A (en) 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co 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 and methods of use therefor
JP2009520742A (ja) 2005-12-21 2009-05-28 エフ.ホフマン−ラ ロシュ アーゲー Dpp−iv阻害剤の新規な塩および多形
AU2007238805B2 (en) 2006-04-11 2012-04-05 Arena Pharmaceuticals, Inc. Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
MX2008014024A (es) 2006-05-04 2008-11-14 Boehringer Ingelheim Int Formas poliformas.
WO2007148185A2 (en) 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
CL2007002499A1 (es) 2006-08-30 2008-03-14 Phenomix Corp Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes.
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
US7846945B2 (en) 2007-03-08 2010-12-07 Lexicon Pharmaceuticals, Inc. Piperdine-based inhibitors of sodium glucose co-transporter 2 and methods of their use
JPWO2008114857A1 (ja) 2007-03-22 2010-07-08 杏林製薬株式会社 アミノアセチルピロリジンカルボニトリル誘導体の製造方法
WO2008128832A1 (en) * 2007-04-18 2008-10-30 Nicox S.A. Nitroderivatives of non-peptidic renin inhibitors for the treatment of cardiovascular, renal and chronic liver disease, inflammations and metabolic syndrome
TW200938200A (en) 2007-12-28 2009-09-16 Dainippon Sumitomo Pharma Co Methyl-substituted piperidine derivative
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1212117C (zh) * 1995-06-20 2005-07-27 武田药品工业株式会社 用于治疗糖尿病的药物组合物
JP2004067575A (ja) * 2002-08-06 2004-03-04 Yaizu Suisankagaku Industry Co Ltd 糖尿病治療薬効果促進剤
CN1823056A (zh) * 2003-07-11 2006-08-23 艾尼纳制药公司 作为新陈代谢调节剂的三取代芳基和杂芳基衍生物以及预防和治疗与其相关之病症
CN101657471A (zh) * 2006-12-06 2010-02-24 史密丝克莱恩比彻姆公司 二环化合物及其作为抗糖尿病药的用途
WO2010074271A1 (ja) * 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BRIGITTE L. KIEFFER,等: "The 6opioid receptor: Isolation of a cDNA by expression cloning and pharmacological characterization", 《PROC. NATL. ACAD. SCI.》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102731492B (zh) * 2011-03-30 2016-06-29 江苏恒瑞医药股份有限公司 环己烷类衍生物、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
CA2795513A1 (en) 2011-10-13
AU2011237775A1 (en) 2012-11-22
EP2556056A1 (en) 2013-02-13
MX2012011631A (es) 2013-01-18
BR112012025592A2 (pt) 2019-09-24
WO2011127051A1 (en) 2011-10-13
JP2013523819A (ja) 2013-06-17
US20130023494A1 (en) 2013-01-24

Similar Documents

Publication Publication Date Title
CN102918027A (zh) Gpr119受体调节剂和对与所述受体有关的障碍的治疗
TWI839416B (zh) Glp-1r促效劑及其用途
US20210340133A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN104812748B (zh) 二氢吡唑gpr40调节剂
WO2022219495A1 (en) 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
CN104918935B (zh) 二氢吡唑gpr40调节剂
US20140051714A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2013055910A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140066369A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2011005929A1 (en) Piperidine derivative and its use for the treatment of diabets and obesity
WO2012170702A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140038889A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140018371A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2014074668A1 (en) Modulators of gpr119 and the treatment of disorders related thereto
CN118715220A (zh) 2-((4-((s)-2-(4-氯-2-氟苯基)-2-甲基苯并[d][1,3]二氧戊环-4-基)哌啶-1-基)甲基)-1-(((s)-氧杂环丁烷-2-基)甲基)-1h-咪唑衍生物作为glp1受体激活剂用于治疗肥胖症
US20240182456A1 (en) 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
EA040124B1 (ru) Модуляторы рецептора gpr119 и лечение связанных с ним нарушений

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130206