CN103611161A - 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法 - Google Patents

用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法 Download PDF

Info

Publication number
CN103611161A
CN103611161A CN201310606771.0A CN201310606771A CN103611161A CN 103611161 A CN103611161 A CN 103611161A CN 201310606771 A CN201310606771 A CN 201310606771A CN 103611161 A CN103611161 A CN 103611161A
Authority
CN
China
Prior art keywords
group
pyrimidine
oxygen base
phenyl
methyl
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
CN201310606771.0A
Other languages
English (en)
Chinese (zh)
Inventor
楚志良
詹姆斯.N.伦纳德
侯赛因.A.阿尔-沙马
罗伯特.M.琼斯
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36570727&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN103611161(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Publication of CN103611161A publication Critical patent/CN103611161A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/76Human chorionic gonadotropin including luteinising hormone, follicle stimulating hormone, thyroid stimulating hormone or their receptors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/28Drugs 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
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P9/08Vasodilators for multiple indications
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/04Endocrine or metabolic disorders
    • G01N2800/042Disorders of carbohydrate metabolism, e.g. diabetes, glucose metabolism
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/28Neurological disorders
    • G01N2800/2814Dementia; Cognitive disorders
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/28Neurological disorders
    • G01N2800/2835Movement disorders, e.g. Parkinson, Huntington, Tourette
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/28Neurological disorders
    • G01N2800/2857Seizure disorders; Epilepsy
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/28Neurological disorders
    • G01N2800/2871Cerebrovascular disorders, e.g. stroke, cerebral infarct, cerebral haemorrhage, transient ischemic event

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Obesity (AREA)
  • Physics & Mathematics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Microbiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
CN201310606771.0A 2005-01-10 2006-01-09 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法 Pending CN103611161A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US64308605P 2005-01-10 2005-01-10
US60/643,086 2005-01-10
US68317205P 2005-05-19 2005-05-19
US60/683,172 2005-05-19
US72688005P 2005-10-14 2005-10-14
US60/726,880 2005-10-14

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNA2006800064168A Division CN101128192A (zh) 2005-01-10 2006-01-09 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法

Publications (1)

Publication Number Publication Date
CN103611161A true CN103611161A (zh) 2014-03-05

Family

ID=36570727

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201310606771.0A Pending CN103611161A (zh) 2005-01-10 2006-01-09 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法
CN2011100978256A Pending CN102218141A (zh) 2005-01-10 2006-01-09 治疗糖尿病和其相关病状以及治疗通过增加血液glp-1水平而改善的病状的组合疗法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2011100978256A Pending CN102218141A (zh) 2005-01-10 2006-01-09 治疗糖尿病和其相关病状以及治疗通过增加血液glp-1水平而改善的病状的组合疗法

Country Status (35)

Country Link
US (12) US20060154866A1 (enExample)
EP (9) EP2322152A1 (enExample)
JP (8) JP4118323B1 (enExample)
KR (5) KR101016890B1 (enExample)
CN (2) CN103611161A (enExample)
AR (1) AR052082A1 (enExample)
AT (2) ATE432693T1 (enExample)
AU (3) AU2006205164B2 (enExample)
BR (1) BRPI0606727A (enExample)
CA (2) CA2593427C (enExample)
CL (1) CL2010000565A1 (enExample)
CR (1) CR9220A (enExample)
CY (2) CY1109260T1 (enExample)
DE (2) DE602006006765D1 (enExample)
DK (2) DK1758565T4 (enExample)
DO (2) DOP2006000008A (enExample)
EA (1) EA011883B1 (enExample)
ES (2) ES2327268T5 (enExample)
GT (1) GT200600004A (enExample)
HN (1) HN2006000971A (enExample)
HR (2) HRP20090403T4 (enExample)
IL (1) IL184364A0 (enExample)
MX (1) MX2007008376A (enExample)
NI (1) NI200700174A (enExample)
NO (2) NO331089B1 (enExample)
NZ (4) NZ578504A (enExample)
PA (1) PA8659301A1 (enExample)
PE (2) PE20100398A1 (enExample)
PL (2) PL1758565T5 (enExample)
PT (2) PT1758565E (enExample)
RS (2) RS51127B (enExample)
SG (2) SG158876A1 (enExample)
SI (2) SI1808168T1 (enExample)
TW (1) TW200637534A (enExample)
WO (1) WO2006076231A2 (enExample)

Families Citing this family (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03007349A (es) * 2001-02-24 2003-12-04 Boehringer Ingelheim Pharma Derivados de xantina, su preparacion y su empleo como medicamentos.
JP2005501058A (ja) 2001-07-31 2005-01-13 ザ ガバメント オブ ザ ユナイテッドステイツ オブ アメリカ アズ リプレゼンテッド バイ ザ セクレタリー デパートメント オブ ヘルス アンド ヒューマン サービシーズ ザ ナショナル インステ Glp−1、exendin−4、そのペプチド・アナログ及びその使用
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
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
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
EP2292620A3 (en) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prohylaxis and treatment of disorders related thereto
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
BRPI0516407A (pt) * 2004-12-24 2008-09-02 Prosidion Ltd agonistas de receptor acoplado à proteìna g (gpr116) e uso destes para o tratamento de obesidade e diabetes
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
MY148521A (en) * 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
WO2007027225A2 (en) 2005-04-27 2007-03-08 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of obesity and diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
KR20080027908A (ko) * 2005-06-30 2008-03-28 프로시디온 리미티드 Gpcr 효능제
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
US20070179123A1 (en) * 2005-11-08 2007-08-02 Chiang Peter K Methods and compositions for treating diseases associated with pathogenic proteins
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
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
MX2008014024A (es) 2006-05-04 2008-11-14 Boehringer Ingelheim Int Formas poliformas.
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
WO2008008887A2 (en) * 2006-07-13 2008-01-17 Smithkline Beecham Corporation Gpr119 agonists for treating metabolic disorders
EP2059516A1 (en) * 2006-08-30 2009-05-20 BIOVITRUM AB (publ) Pyridine compounds for treating gpr119 related disorders
CA2672059A1 (en) 2006-12-14 2008-06-26 Merck & Co., Inc. Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
SI2114933T1 (sl) * 2007-01-04 2012-01-31 Prosidion Ltd Windrush Court Piperidinski gpcr-agonisti
AR064735A1 (es) * 2007-01-04 2009-04-22 Prosidion Ltd Agonistas de gpcr y composicion farmaceutica en base al compuesto
AR064736A1 (es) * 2007-01-04 2009-04-22 Prosidion Ltd Agonistas de gpcr
WO2008141074A1 (en) * 2007-05-10 2008-11-20 Salk Institute For Biological Studies Identification of compounds that protect against amyloid diseases
AU2008279447A1 (en) 2007-07-19 2009-01-29 Metabolex, Inc. N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders
PE20090938A1 (es) 2007-08-16 2009-08-08 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
EP2197873B1 (en) 2007-09-20 2014-07-16 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2009117421A2 (en) * 2008-03-17 2009-09-24 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
DK2280704T3 (en) * 2008-03-31 2015-06-29 Cymabay Therapeutics Inc Oxymethylenarylforbindelser and uses thereof
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
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
EP2297117B1 (en) * 2008-05-19 2012-10-31 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
JP2011527332A (ja) * 2008-07-10 2011-10-27 プロシディオン・リミテッド ピペリジンgpcr作動薬
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
MX2011002558A (es) * 2008-09-10 2011-04-26 Boehringer Ingelheim Int Terapia de combinacion para el tratamiento de diabetes y estados relacionados.
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
KR101054911B1 (ko) 2008-10-17 2011-08-05 동아제약주식회사 디펩티딜펩티다아제-ⅳ의 활성을 저해하는 화합물 및 다른 항당뇨 또는 항비만 약물을 유효성분으로 함유하는 당뇨 또는 비만의 예방 및 치료용 약학적 조성물
CN101723947B (zh) * 2008-10-21 2012-05-30 山东轩竹医药科技有限公司 二肽酶-ⅳ抑制剂化合物
EP2382216A1 (en) 2008-12-23 2011-11-02 Boehringer Ingelheim International GmbH Salt forms of organic compound
WO2010074271A1 (ja) * 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
US20220387305A1 (en) * 2009-01-12 2022-12-08 Biokier, Inc. Composition and method for treatment of diabetes
EP2395983B1 (en) 2009-02-13 2020-04-08 Boehringer Ingelheim International GmbH Pharmaceutical composition comprisng a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof
EP2414348B1 (en) 2009-04-03 2013-11-20 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders
NZ596467A (en) * 2009-06-05 2014-01-31 Pfizer L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators
EA201200046A1 (ru) 2009-06-24 2012-08-30 Бёрингер Ингельхайм Интернациональ Гмбх Новые соединения, фармацевтическая композиция и связанные с ними способы
JP2012530758A (ja) 2009-06-24 2012-12-06 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化合物、医薬組成物及びそれに関する方法
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
NO2462246T3 (enExample) * 2009-09-28 2018-02-03
WO2011041154A1 (en) 2009-10-01 2011-04-07 Metabolex, Inc. Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts
CN102812011A (zh) 2009-11-16 2012-12-05 梅利科技公司 [1,5]-二氮杂环辛间四烯衍生物
EP3646859A1 (en) 2009-11-27 2020-05-06 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
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
US20120035103A1 (en) * 2010-01-29 2012-02-09 Pillion Dennis J Method for administration of insulin and pharmaceutical composition thereof
US20130109703A1 (en) * 2010-03-18 2013-05-02 Boehringer Ingelheim International Gmbh Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions
JP2013523819A (ja) 2010-04-06 2013-06-17 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 Gpr119レセプターのモジュレーターおよびそれに関連する障害の処置
AU2011249722B2 (en) 2010-05-05 2015-09-17 Boehringer Ingelheim International Gmbh Combination therapy
EP2585048B1 (en) 2010-06-23 2018-04-11 CymaBay Therapeutics, Inc. Compositions of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
CN106975074A (zh) 2010-06-24 2017-07-25 勃林格殷格翰国际有限公司 糖尿病治疗
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
AR085689A1 (es) 2011-03-07 2013-10-23 Boehringer Ingelheim Int Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, 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
PH12014500137A1 (en) 2011-07-15 2017-08-18 Boehringer Ingelheim Int Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013171167A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
CA2878625A1 (en) 2012-07-11 2014-01-16 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
CN103344773B (zh) * 2013-06-19 2015-04-15 天津美德太平洋科技有限公司 一种胰高血糖素样肽-1生物学活性检测试剂及检测方法和试剂盒
US10493042B2 (en) 2013-08-01 2019-12-03 University-Industry Cooperation Group Of Kyung Hee University Method for preventing or treating diabetes mellitus, and method for screening for diabetes mellitus therapeutic agent
WO2015016682A1 (ko) 2013-08-01 2015-02-05 경희대학교 산학협력단 당뇨병 예방 또는 치료용 약학적 조성물, 당뇨병 예방 또는 치료 방법, 및 당뇨병 치료제 스크리닝 방법
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
ES2995737T3 (en) 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MX386778B (es) 2015-03-09 2025-03-19 Intekrin Therapeutics Inc Métodos para el tratamiento de enfermedad de hígado graso no alcohólico y/o lipodistrofia.
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
WO2017211979A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
CA3032432A1 (en) 2016-08-03 2018-02-08 Charles A. Mcwherter Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
CA3058806A1 (en) 2017-04-03 2018-10-11 Coherus Biosciences Inc. Ppar.gamma. agonist for treatment of progressive supranuclear palsy
US20200129511A1 (en) 2017-06-19 2020-04-30 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of nafld and nash
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
CN112805002A (zh) 2018-09-12 2021-05-14 东亚St株式会社 用于预防或治疗非酒精性脂肪肝病的含有gpr119配体作为活性成分的药物组合物
EP3996704A4 (en) 2019-07-08 2023-07-12 Mankind Pharma Ltd MULTIPLE THERAPY INCLUDING GPR119 AGONISTS AND DPP-4 INHIBITORS
CN115243689A (zh) * 2020-03-11 2022-10-25 东亚St株式会社 用于预防或治疗糖尿病和与之相关的代谢疾病的药物组合物
US20250263402A1 (en) * 2020-10-12 2025-08-21 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Benzimidazolone glp-1 receptor agonist and use thereof
WO2024102952A1 (en) * 2022-11-10 2024-05-16 Acerand Therapeutics (Usa) Limited Sos1 inhibitors

Family Cites Families (286)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US751426A (en) * 1904-02-02 Safety hair-pin
US747699A (en) * 1903-09-05 1903-12-22 Achilles C Gough Universal sanding-machine.
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4704362A (en) * 1977-11-08 1987-11-03 Genentech, Inc. Recombinant cloning vehicle microbial polypeptide expression
US4265874A (en) * 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
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
US5462856A (en) 1990-07-19 1995-10-31 Bunsen Rush Laboratories, Inc. Methods for identifying chemicals that act as agonists or antagonists for receptors and other proteins involved in signal transduction via pathways that utilize G-proteins
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.
US6100042A (en) * 1993-03-31 2000-08-08 Cadus Pharmaceutical Corporation Yeast cells engineered to produce pheromone system protein surrogates, and uses therefor
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
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
AU4721897A (en) 1996-10-25 1998-05-22 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
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
US6183974B1 (en) * 1997-07-31 2001-02-06 The General Hospital Corporation Screening assays for G protein coupled receptor agonists and antagonists
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
US5922576A (en) * 1998-02-27 1999-07-13 The John Hopkins University Simplified system for generating recombinant adenoviruses
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
DE19828114A1 (de) * 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler 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
US20030125539A1 (en) * 1999-02-22 2003-07-03 Synaptic Pharmaceutical Corporation DNA encoding SNORF25 receptor
US6221660B1 (en) * 1999-02-22 2001-04-24 Synaptic Pharmaceutical Corporation DNA encoding SNORF25 receptor
AU3960400A (en) * 1999-03-05 2000-09-28 Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
GB9906714D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for improving fertility
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
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
US6653064B1 (en) * 1999-09-23 2003-11-25 Boehringer Ingelheim International Gmbh Method for identifying compounds useful in the therapy of bone disorders
GB9923177D0 (en) 1999-09-30 1999-12-01 Pfizer Ltd Novel polypeptide
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
US6608038B2 (en) * 2000-03-15 2003-08-19 Novartis Ag Methods and compositions for treatment of diabetes and related conditions via gene therapy
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
EP1287133B1 (en) 2000-05-18 2006-12-13 Bayer HealthCare AG Regulation of human dopamine-like g protein-coupled receptor
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
WO2001096597A2 (en) * 2000-06-13 2001-12-20 Glaxo Group Limited High throughput screening of compounds for biological activity
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
GB0014969D0 (en) 2000-06-19 2000-08-09 Smithkline Beecham Plc Novel method of treatment
MXPA02012272A (es) 2000-07-04 2003-04-25 Novo Nordisk As Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv.
AU7705601A (en) * 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
CA2418656C (en) * 2000-08-10 2011-02-01 Mitsubishi Pharma Corporation Proline derivatives and use thereof as drugs
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
AU2001294196B2 (en) 2000-10-06 2005-11-17 Tanabe Seiyaku Co., Ltd. Nitrogenous five-membered ring compounds
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
JP2004035574A (ja) 2000-10-06 2004-02-05 Tanabe Seiyaku Co Ltd 脂肪族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
WO2002042461A2 (en) 2000-11-27 2002-05-30 Arena Pharmaceuticals, Inc. Endogenous and non-endogenous versions of human g protein-coupled receptors
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
US6397767B1 (en) * 2001-02-01 2002-06-04 Case Corporation Knife applicator for applying liquid fertilizer in the ground
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
WO2002080860A2 (en) * 2001-03-27 2002-10-17 The Regents Of The University Of California Methods, compounds, and compositions for reducing body fat and modulating fatty acid metabolism
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
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
DE60224189T2 (de) 2001-06-20 2008-12-11 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
US7368421B2 (en) * 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
US7183290B2 (en) 2001-06-27 2007-02-27 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US20030130199A1 (en) * 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
CA2419888A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
CA2418543A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag New dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
US7196201B2 (en) 2001-06-27 2007-03-27 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
ES2296979T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
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
US6844316B2 (en) * 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
WO2003026661A1 (fr) * 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
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
RU2353625C2 (ru) * 2001-10-18 2009-04-27 Бристол-Маерс Сквибб Компани Миметики человеческого глюканоподобного пептида-1 и их применение в лечении диабета и родственных состояний
US7238671B2 (en) * 2001-10-18 2007-07-03 Bristol-Myers Squibb Company Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
GB0125446D0 (en) * 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
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
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
AU2002357767C1 (en) 2001-11-26 2009-03-19 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
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
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
DE60304911D1 (de) * 2002-02-25 2006-06-08 Eisai Co Ltd Xanthin-Derivate als DPP-IV-Inhibitoren
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
JP4329381B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
JP4329382B2 (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
WO2003101449A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
AU2003232405A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
CA2485641C (en) 2002-06-06 2010-12-14 Eisai Co., Ltd. Novel condensed imidazole derivatives
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
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
DE10236667B4 (de) * 2002-08-09 2007-06-06 J. Eberspächer GmbH & Co. KG Abgasanlage für den Verbrennungsmotor eines Kraftfahrzeugs
US20050101542A1 (en) * 2002-08-20 2005-05-12 Regents Of The University Of California Combination therapy for controlling appetites
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
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
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
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, 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
UA78104C2 (en) 2002-08-29 2007-02-15 Taisho Pharmaceutical Co Ltd Benzenesulfonate salts of 4-fluoro-2-cyanopyrrolidine derivatives
WO2004024184A1 (ja) * 2002-09-11 2004-03-25 Takeda Pharmaceutical Company Limited 徐放性製剤
WO2004024943A1 (ja) * 2002-09-11 2004-03-25 Yamanouchi Pharmaceutical Co., Ltd. インスリン含量増加剤スクリーニング方法
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
AR041470A1 (es) * 2002-10-17 2005-05-18 Upjohn Co Compuestos de pirrolo (1,2 - b) piridazina y sus usos
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
UY28103A1 (es) 2002-12-03 2004-06-30 Boehringer Ingelheim Pharma Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos
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
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
US6982164B2 (en) * 2003-01-10 2006-01-03 Mgp Ingredients, Inc. Unhydrolyzed jojoba protein products having high simmondsin concentration
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
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
DK1595866T3 (en) 2003-01-31 2016-08-22 Sanwa Kagaku Kenkyusho Co Cyanopyrrolidines suitable for the treatment of inter alia metabolism syndrome
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
JP2004269469A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
JP2004269468A (ja) * 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
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
WO2004098591A2 (en) * 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
US7083933B1 (en) * 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
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
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1627870A1 (en) 2003-05-15 2006-02-22 Taisho Pharmaceutical Co., Ltd Cyanofluoropyrrolidine derivative
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
US20070099884A1 (en) 2003-06-06 2007-05-03 Erondu Ngozi E Combination therapy for the treatment of diabetes
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
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
EP2292620A3 (en) * 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prohylaxis and treatment of disorders related thereto
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
US7008957B2 (en) * 2003-07-25 2006-03-07 Sanofi-Aventis Deutschland Gmbh Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
US7094800B2 (en) * 2003-07-25 2006-08-22 Sanofi-Aventis Deutschland Gmbh Cyanopyrrolidides, 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
PE20050249A1 (es) 2003-07-25 2005-06-01 Aventis Pharma Gmbh Nuevas cianopirrolididas y procedimiento para su preparacion como medicamentos
WO2005011581A2 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
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
HU227684B1 (en) 2003-08-29 2011-11-28 Sanofi Aventis Adamantane and azabicyclo-octane and nonane derivatives and their use as dpp-iv inhibitors
EP1659123A1 (en) 2003-08-29 2006-05-24 Dainippon Sumitomo Pharma Co., Ltd. Bicyclic pyrazole derivative
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
ATE534404T1 (de) 2003-10-03 2011-12-15 Takeda Pharmaceutical Dipeptidylpeptidase-iv-inhibitoren zur behandlung von diabetes-patienten mit sekundärversagen durch sulfonylharnstoffe
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
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
DE10355304A1 (de) * 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
US7217711B2 (en) * 2003-12-17 2007-05-15 Boehringer Ingelheim International Gmbh Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions
DE10360835A1 (de) 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
CN1898235A (zh) * 2003-12-24 2007-01-17 普罗西迪恩有限公司 作为gpcr受体激动剂的杂环衍生物
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
US7501426B2 (en) * 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
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
DE102004009039A1 (de) * 2004-02-23 2005-09-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel
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
ATE415397T1 (de) * 2004-06-04 2008-12-15 Arena Pharm Inc Substituierte aryl- und heteroarylderivate als modulatoren des stoffwechsels und für die prophylaxe und behandlung von damit in zusammenhang stehenden erkrankungen
US20060024313A1 (en) * 2004-07-06 2006-02-02 Xin Chen Agents that disrupt dimer formation in DPP-IV family of prolyl dipeptidases
WO2006019965A2 (en) * 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
DE102004037554A1 (de) 2004-08-03 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituierte 8-Aminoalkylthio-xanthine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE102004038268A1 (de) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituierte, bizyklische 8-Pyrrolidino-xanthine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US20060046978A1 (en) * 2004-08-31 2006-03-02 Morphochem Ag Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
DE102004043944A1 (de) 2004-09-11 2006-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(3-Amino-piperidin-1-yl)-7-(but-2-inyl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE102004044221A1 (de) * 2004-09-14 2006-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
WO2006041797A2 (en) * 2004-10-07 2006-04-20 Merck & Co., Inc. Acyclic hydrazides as cannabinoid receptor modulators
CA2581298A1 (en) * 2004-10-25 2006-05-04 Novartis Ag Combination of dpp-iv inhibitor, ppar antidiabetic and metformin
US7411093B2 (en) * 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
EP1828192B1 (en) * 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
MX2007007483A (es) 2004-12-24 2007-07-20 Dainippon Sumitomo Pharma Co Derivados de pirroles biciclicos.
US7589088B2 (en) * 2004-12-29 2009-09-15 Bristol-Myers Squibb Company Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
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
MY148521A (en) * 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
US20070032420A1 (en) * 2005-02-09 2007-02-08 Entelos, Inc. Treating diabetes with glucagon-like peptide-1 secretagogues
WO2007027225A2 (en) * 2005-04-27 2007-03-08 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of obesity and diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
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
JP2008545010A (ja) * 2005-06-30 2008-12-11 プロシディオン・リミテッド Gタンパク質共役受容体アゴニスト
US20090325924A1 (en) * 2005-06-30 2009-12-31 Stuart Edward GPCR Agonists
WO2007003961A2 (en) * 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
US7708191B2 (en) * 2005-07-28 2010-05-04 Edwin Vega Telebanking apparatus for transferring money or cash value between two parties in the same country or across national borders, for paying bills and browsing the internet
JP4827483B2 (ja) * 2005-10-04 2011-11-30 キヤノン株式会社 核酸試料処理装置
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
WO2008008887A2 (en) * 2006-07-13 2008-01-17 Smithkline Beecham Corporation Gpr119 agonists for treating metabolic disorders
EP2059516A1 (en) * 2006-08-30 2009-05-20 BIOVITRUM AB (publ) Pyridine compounds for treating gpr119 related disorders
WO2008070692A2 (en) * 2006-12-06 2008-06-12 Smithkline Beecham Corporation Bicyclic compounds and use as antidiabetics
CA2672059A1 (en) * 2006-12-14 2008-06-26 Merck & Co., Inc. Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment
DK2280704T3 (en) * 2008-03-31 2015-06-29 Cymabay Therapeutics Inc Oxymethylenarylforbindelser and uses thereof
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
WO2009150144A1 (en) * 2008-06-10 2009-12-17 Inovacia Ab New gpr119modulators
MX2011002558A (es) * 2008-09-10 2011-04-26 Boehringer Ingelheim Int Terapia de combinacion para el tratamiento de diabetes y estados relacionados.
WO2010074271A1 (ja) * 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤
US20140193463A1 (en) * 2013-01-04 2014-07-10 China Medical University Peptide for inhibiting dipeptidyl-peptidase iv

Also Published As

Publication number Publication date
US8198232B2 (en) 2012-06-12
SG189762A1 (en) 2013-05-31
HRP20090403T1 (hr) 2009-08-31
SI1758565T1 (sl) 2009-10-31
US20100298333A1 (en) 2010-11-25
NZ556219A (en) 2010-09-30
EP1997484A3 (en) 2009-02-11
DK1808168T3 (da) 2009-10-05
US20100286153A1 (en) 2010-11-11
DK1758565T4 (da) 2013-02-04
JP2008526235A (ja) 2008-07-24
US7803754B2 (en) 2010-09-28
AU2009202900B8 (en) 2010-06-03
CA2654733A1 (en) 2006-07-20
US20100286168A1 (en) 2010-11-11
KR20070095400A (ko) 2007-09-28
NZ578502A (en) 2011-01-28
JP2008220374A (ja) 2008-09-25
NZ578504A (en) 2011-02-25
WO2006076231A8 (en) 2006-09-21
DOP2006000008A (es) 2006-08-31
KR101016890B1 (ko) 2011-02-22
US20100137293A1 (en) 2010-06-03
US20060154866A1 (en) 2006-07-13
EP2322157A1 (en) 2011-05-18
WO2006076231A2 (en) 2006-07-20
WO2006076231A3 (en) 2007-01-18
PE20061116A1 (es) 2006-10-12
EP1808168A1 (en) 2007-07-18
PT1758565E (pt) 2009-08-19
JP4807887B2 (ja) 2011-11-02
US20100286172A1 (en) 2010-11-11
EP2322151A2 (en) 2011-05-18
US20100285494A1 (en) 2010-11-11
HRP20090446T1 (hr) 2009-09-30
ATE432693T1 (de) 2009-06-15
EP1758565B1 (en) 2009-05-13
JP4237243B2 (ja) 2009-03-11
DK1758565T3 (da) 2009-09-07
CL2010000565A1 (es) 2010-10-15
EA011883B1 (ru) 2009-06-30
RS51127B (sr) 2010-10-31
RS51174B (sr) 2010-10-31
EP2322156A1 (en) 2011-05-18
MX2007008376A (es) 2008-01-11
JP2008220375A (ja) 2008-09-25
EP1808168B1 (en) 2009-06-03
US20100285495A1 (en) 2010-11-11
KR20130140226A (ko) 2013-12-23
GT200600004A (es) 2006-09-11
EP2322151A3 (en) 2012-01-18
KR20120139849A (ko) 2012-12-27
TW200637534A (en) 2006-11-01
AR052082A1 (es) 2007-02-28
US20070072803A1 (en) 2007-03-29
CY1109260T1 (el) 2014-07-02
CR9220A (es) 2009-07-31
JP2008195733A (ja) 2008-08-28
PL1808168T3 (pl) 2009-11-30
JP2008110964A (ja) 2008-05-15
NO20101746L (no) 2007-09-27
JP4912349B2 (ja) 2012-04-11
US8003597B2 (en) 2011-08-23
HK1100353A1 (en) 2007-09-21
NO331089B1 (no) 2011-10-03
CY1109321T1 (el) 2014-07-02
NI200700174A (es) 2008-05-09
JP4221444B2 (ja) 2009-02-12
AU2009202900B2 (en) 2010-02-11
EP1997484A2 (en) 2008-12-03
ES2327872T3 (es) 2009-11-04
CN102218141A (zh) 2011-10-19
US7803753B2 (en) 2010-09-28
PL1758565T5 (pl) 2013-03-29
HN2006000971A (es) 2011-12-27
EA200701469A1 (ru) 2008-02-28
US8022034B2 (en) 2011-09-20
JP4787804B2 (ja) 2011-10-05
IL184364A0 (en) 2007-10-31
AU2006205164B2 (en) 2011-09-08
AU2009202900A1 (en) 2009-08-06
CA2593427C (en) 2011-11-29
KR20100072085A (ko) 2010-06-29
SG158876A1 (en) 2010-02-26
NO20073816L (no) 2007-09-27
JP4118323B1 (ja) 2008-07-16
PT1808168E (pt) 2009-08-25
BRPI0606727A (pt) 2008-03-11
EP1758565A2 (en) 2007-03-07
KR20100129328A (ko) 2010-12-08
PL1758565T3 (pl) 2009-10-30
EP1758565B2 (en) 2012-11-14
JP2008239623A (ja) 2008-10-09
US8030270B2 (en) 2011-10-04
PA8659301A1 (es) 2008-12-18
DE602006007093D1 (de) 2009-07-16
HK1096537A1 (en) 2007-06-01
CA2654733C (en) 2011-09-06
JP2011184458A (ja) 2011-09-22
EP2116235A1 (en) 2009-11-11
US20100286111A1 (en) 2010-11-11
NZ587368A (en) 2011-01-28
CA2593427A1 (en) 2006-07-20
US20100291589A1 (en) 2010-11-18
US20070072804A1 (en) 2007-03-29
DOP2011000040A (es) 2011-09-30
JP2012017330A (ja) 2012-01-26
PE20100398A1 (es) 2010-06-07
EP2322152A1 (en) 2011-05-18
HRP20090403T4 (hr) 2012-12-31
ES2327268T9 (es) 2013-11-12
EP2322150A2 (en) 2011-05-18
AU2009202898B2 (en) 2010-02-18
AU2006205164A1 (en) 2006-07-20
ATE431139T1 (de) 2009-05-15
ES2327268T3 (es) 2009-10-27
AU2009202898A1 (en) 2009-08-06
DE602006006765D1 (de) 2009-06-25
ES2327268T5 (es) 2013-03-21
EP2322150A3 (en) 2011-11-16
SI1808168T1 (sl) 2009-10-31

Similar Documents

Publication Publication Date Title
CN103611161A (zh) 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法
CN101332303A (zh) 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法
HK1157234A (en) Composition for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
HK1120227A (en) Method of identifying glp-1 secretagogues
HK1157232A (en) Method of identifying glp-1 secretagogues
HK1157230A (en) Sustained release formulation comprising a gpr119 agonist and a dpp-iv inhibitor
HK1136510A (en) Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level

Legal Events

Date Code Title Description
PB01 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: 20140305