CA2450740C - Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes - Google Patents

Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes Download PDF

Info

Publication number
CA2450740C
CA2450740C CA002450740A CA2450740A CA2450740C CA 2450740 C CA2450740 C CA 2450740C CA 002450740 A CA002450740 A CA 002450740A CA 2450740 A CA2450740 A CA 2450740A CA 2450740 C CA2450740 C CA 2450740C
Authority
CA
Canada
Prior art keywords
compound
6alkyl
treatment
effective amount
substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
CA002450740A
Other languages
English (en)
French (fr)
Other versions
CA2450740A1 (en
Inventor
Scott D. Edmondson
Michael H. Fisher
Dooseop Kim
Malcolm Maccoss
Emma R. Parmee
Ann E. Weber
Jinyou Xu
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck and Co 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=23172273&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2450740(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of CA2450740A1 publication Critical patent/CA2450740A1/en
Application granted granted Critical
Publication of CA2450740C publication Critical patent/CA2450740C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K38/22Hormones
    • A61K38/28Insulins
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • 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
    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
CA002450740A 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes Expired - Lifetime CA2450740C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30347401P 2001-07-06 2001-07-06
US60/303,474 2001-07-06
PCT/US2002/021349 WO2003004498A1 (en) 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

Publications (2)

Publication Number Publication Date
CA2450740A1 CA2450740A1 (en) 2003-01-16
CA2450740C true CA2450740C (en) 2006-02-14

Family

ID=23172273

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002450740A Expired - Lifetime CA2450740C (en) 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

Country Status (45)

Country Link
US (9) US7125873B2 (enExample)
EP (4) EP2292232B1 (enExample)
JP (1) JP3762407B2 (enExample)
KR (1) KR100606871B1 (enExample)
CN (2) CN1861077A (enExample)
AR (1) AR036114A1 (enExample)
AT (2) ATE471148T1 (enExample)
AU (1) AU2002320303B2 (enExample)
BE (1) BE2007C047I2 (enExample)
BG (1) BG108493A (enExample)
BR (1) BRPI0210866B8 (enExample)
CA (1) CA2450740C (enExample)
CR (1) CR7235A (enExample)
CY (3) CY2007019I2 (enExample)
DE (4) DE60236767D1 (enExample)
DK (2) DK1625847T3 (enExample)
DO (1) DOP2002000438A (enExample)
EA (2) EA012701B1 (enExample)
EC (1) ECSP044935A (enExample)
ES (2) ES2344846T3 (enExample)
FR (2) FR07C0041I2 (enExample)
GE (2) GEP20053734B (enExample)
HR (1) HRP20031098B1 (enExample)
HU (2) HU225695B1 (enExample)
IL (3) IL159109A0 (enExample)
IS (2) IS2218B (enExample)
JO (1) JO2230B1 (enExample)
LT (1) LTC1412357I2 (enExample)
LU (2) LUC91360I2 (enExample)
MA (1) MA27053A1 (enExample)
ME (1) ME00439B (enExample)
MX (1) MXPA04000018A (enExample)
MY (1) MY127961A (enExample)
NL (2) NL300287I2 (enExample)
NO (4) NO321999B1 (enExample)
NZ (1) NZ529833A (enExample)
PE (1) PE20030654A1 (enExample)
PL (1) PL196278B6 (enExample)
PT (2) PT1412357E (enExample)
RS (1) RS50737B (enExample)
SI (1) SI1412357T1 (enExample)
TW (1) TWI226331B (enExample)
UA (1) UA74912C2 (enExample)
WO (1) WO2003004498A1 (enExample)
ZA (1) ZA200309294B (enExample)

Families Citing this family (439)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020006899A1 (en) * 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
US7544511B2 (en) * 1996-09-25 2009-06-09 Neuralstem Biopharmaceuticals Ltd. Stable neural stem cell line methods
US20030176357A1 (en) * 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
PT1140942E (pt) * 1998-12-31 2004-05-31 Conseils De Rec Appl Scient S Inibidores da prenil-transferase
ES2257555T3 (es) 2001-06-20 2006-08-01 MERCK & CO., INC. Inhibidores de dipeptidilpeptidasa para el tratamiento de la diabetes.
AU2002344820B2 (en) 2001-06-20 2006-12-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
ES2296979T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
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
US20050009739A1 (en) * 2002-02-14 2005-01-13 Wei Wang Formulation strategies in stabilizing peptides in organic solvents and in dried states
DE60316416T2 (de) 2002-03-25 2008-06-26 Merck & Co., Inc. Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
DE60330485D1 (de) * 2002-07-15 2010-01-21 Merck & Co Inc Zur behandlung von diabetes
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
EP1554280B1 (en) * 2002-10-07 2007-08-15 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
ATE390416T1 (de) * 2002-10-18 2008-04-15 Merck & Co Inc Heterozyklische beta-aminoverbindungen als inhibitoren des dipeptidylpeptidase zur behandlung bzw. prevention von diabetes
AU2003290577B2 (en) 2002-11-07 2008-12-11 Merck Sharp & Dohme Corp. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2006510630A (ja) * 2002-12-04 2006-03-30 メルク エンド カムパニー インコーポレーテッド 糖尿病を治療又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フェニルアラニン誘導体
EP1576134B1 (en) * 2002-12-09 2013-03-06 Judith Kelleher-Andersson Method for discovering neurogenic agents
US8293488B2 (en) 2002-12-09 2012-10-23 Neuralstem, Inc. Method for screening neurogenic agents
ATE404191T1 (de) * 2002-12-10 2008-08-15 Novartis Pharma Ag Kombinationen von einem dpp-iv inhibitor und einem ppar- alpha agonist
AU2003297219A1 (en) * 2002-12-20 2004-07-22 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
MXPA05007485A (es) 2003-01-14 2006-01-30 Arena Pharm Inc Derivados de arilo y heteroarilo 1,2,3-trisubstituidos como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con ello tales como diabetes e hiperglicemia.
AU2004206812A1 (en) * 2003-01-17 2004-08-05 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
CA2513684A1 (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
AR043443A1 (es) * 2003-03-07 2005-07-27 Merck & Co Inc Procedimiento de preparacion de tetrahidrotriazolopirazinas y productos intermedios
AR043505A1 (es) * 2003-03-18 2005-08-03 Merck & Co Inc Preparacion de beta-cetoamidas e intermediarios de reaccion
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
WO2004087053A2 (en) * 2003-03-25 2004-10-14 Syrrx, Inc. Dipeptidyl peptidase inhibitors
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
US7371871B2 (en) 2003-05-05 2008-05-13 Probiodrug Ag Inhibitors of glutaminyl cyclase
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
JP2006528693A (ja) * 2003-05-14 2006-12-21 メルク エンド カムパニー インコーポレーテッド 糖尿病を治療又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3−アミノ−4−フェニルブタン酸誘導体
EP1635832A2 (en) * 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
CA2526770A1 (en) * 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2004249163A1 (en) * 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
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
EP2287165A3 (en) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
JP2007520441A (ja) * 2003-07-25 2007-07-26 コンジュシェム,インコーポレイティド 持続性インスリン誘導体及びその方法
DE602004018503D1 (de) * 2003-07-31 2009-01-29 Merck & Co Inc Hexahydrodiazepinone als inhibitoren des dipeptidylpeptidase-iv zur behandlung bzw. prävention von diabetes
US7579357B2 (en) 2003-08-13 2009-08-25 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase 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
WO2005026148A1 (en) * 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1697342A2 (en) * 2003-09-08 2006-09-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7547693B2 (en) 2003-09-22 2009-06-16 Banyu Pharmaceutical Co. Ltd. Piperidine derivative
US20070021430A1 (en) * 2003-09-23 2007-01-25 Chen Alex M Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
EP1684786A4 (en) * 2003-10-24 2007-12-12 Merck & Co Inc IMPROVING THE MIRROR OF THE GROWTH HORMONE WITH A DIPEPTIDYL PEPTIDASE IV INHIBITOR AND A GROWTH HORMONE SECRETAGOG
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
EP1682120A4 (en) * 2003-11-04 2009-05-27 Merck & Co Inc CAPACITATED PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDAS IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
US7317109B2 (en) * 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7767828B2 (en) * 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7576121B2 (en) * 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
BRPI0416444B8 (pt) * 2003-11-12 2021-05-25 Chiesi Farm Spa composto de ácido borônico heterocíclico, composição farmacêutica, e, combinação farmacêutica compreendendo o mesmo
AU2004290897B2 (en) 2003-11-17 2009-02-26 Novartis Ag Use of dipeptidyl peptidase IV inhibitors
US20080227786A1 (en) * 2004-01-16 2008-09-18 Ferlita Russell R Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor
WO2005067976A2 (en) 2004-01-20 2005-07-28 Novartis Ag Direct compression formulation and process
KR101130433B1 (ko) * 2004-02-05 2012-03-27 교린 세이야꾸 가부시키 가이샤 비시클로에스테르 유도체
EP1713780B1 (en) 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
AU2005212073B2 (en) * 2004-02-18 2010-07-08 Kyorin Pharmaceutical Co., Ltd. Bicyclic amide derivatives
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
US7514571B2 (en) * 2004-02-27 2009-04-07 Kyorin Pharmaceutical Co., Ltd. Bicyclo derivative
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN102140090A (zh) * 2004-03-15 2011-08-03 武田药品工业株式会社 二肽基肽酶抑制剂
AU2005230864A1 (en) 2004-03-29 2005-10-20 Merck Sharp & Dohme Corp. Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
TW200602293A (en) * 2004-04-05 2006-01-16 Merck & Co Inc Process for the preparation of enantiomerically enriched beta amino acid derivatives
CN1950349A (zh) * 2004-05-04 2007-04-18 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的1,2,4-噁二唑衍生物
WO2005116029A1 (en) * 2004-05-18 2005-12-08 Merck & Co., Inc. Cyclohexylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1753730A1 (en) * 2004-06-04 2007-02-21 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN101014598B (zh) * 2004-06-21 2012-06-13 默沙东公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的氨基环己烷化合物
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1794120B1 (en) * 2004-07-23 2012-04-11 Nuada, LLC Peptidase inhibitors
TW200608967A (en) 2004-07-29 2006-03-16 Sankyo Co Pharmaceutical compositions containing with diabetic agent
CA2575736A1 (en) 2004-08-06 2006-02-16 Merck & Co., Inc. Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
US7625888B2 (en) 2004-08-23 2009-12-01 Merck & Co., Inc. Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
JP4854511B2 (ja) * 2004-08-26 2012-01-18 武田薬品工業株式会社 糖尿病治療剤
PE20060652A1 (es) 2004-08-27 2006-08-11 Novartis Ag Composiciones farmaceuticas de liberacion inmediata que comprenden granulos de fusion
EP1796671A4 (en) * 2004-09-15 2009-01-21 Merck & Co Inc AMORPHIC FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL-PEPTIDASE IV HEMMER
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
CN101031300A (zh) 2004-10-01 2007-09-05 默克公司 用于治疗或预防糖尿病的作为二肽基肽酶-ⅳ抑制剂的氨基哌啶化合物
WO2006040625A1 (en) * 2004-10-12 2006-04-20 Glenmark Pharmaceuticals S.A. Novel dipeptidyl peptidase iv inhibitors, pharmaceutical compositions containing them, and process for their preparation
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
IN2014CN03629A (enExample) * 2004-11-17 2015-09-04 Neuralstem Inc
JP2008524331A (ja) * 2004-12-21 2008-07-10 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤
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
US8017633B2 (en) 2005-03-08 2011-09-13 Nycomed Gmbh Roflumilast for the treatment of diabetes mellitus
TWI357902B (en) 2005-04-01 2012-02-11 Lg Life Science Ltd Dipeptidyl peptidase-iv inhibiting compounds, meth
JP2008540426A (ja) * 2005-05-02 2008-11-20 メルク エンド カムパニー インコーポレーテッド 糖尿病及び肥満の治療のためのジペプチジルペプチダーゼiv阻害薬及びカンナビノイドcb1受容体拮抗薬の組み合わせ
CN103275083A (zh) * 2005-05-25 2013-09-04 默沙东公司 用于糖尿病治疗或者预防的作为二肽基肽酶-iv抑制剂的氨基环己烷
US7825139B2 (en) * 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
KR101397913B1 (ko) 2005-05-30 2014-05-26 엠에스디 가부시키가이샤 신규 피페리딘 유도체
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
JP4915833B2 (ja) * 2005-07-01 2012-04-11 雪印メグミルク株式会社 ジペプチジルペプチダーゼiv阻害剤
US8076514B2 (en) * 2005-07-20 2011-12-13 Eli Lilly And Company Phenyl compounds and their use in the treatment of Type II diabetes
EP1910317B1 (en) 2005-07-20 2013-07-03 Eli Lilly And Company 1-amino linked compounds
WO2007015767A1 (en) 2005-07-20 2007-02-08 Eli Lilly And Company Pyridine derivatives as dipeptedyl peptidase inhibitors
US20090221592A1 (en) * 2005-07-25 2009-09-03 Ellison Martha E Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor
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
JPWO2007018248A1 (ja) 2005-08-10 2009-02-19 萬有製薬株式会社 ピリドン化合物
JPWO2007024004A1 (ja) 2005-08-24 2009-03-05 萬有製薬株式会社 フェニルピリドン誘導体
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
JPWO2007029847A1 (ja) 2005-09-07 2009-03-19 萬有製薬株式会社 二環性芳香族置換ピリドン誘導体
CN102935081B (zh) * 2005-09-14 2015-03-04 武田药品工业株式会社 用于治疗糖尿病的二肽基肽酶抑制剂
EP1942898B2 (en) 2005-09-14 2014-05-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
CN101360723A (zh) * 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
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
TW200745080A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor
CA2624030A1 (en) 2005-09-29 2007-04-12 Tianying Jian Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
TW200738266A (en) * 2005-09-29 2007-10-16 Sankyo Co Pharmaceutical agent containing insulin resistance improving agent
JP2009513633A (ja) * 2005-10-25 2009-04-02 メルク エンド カムパニー インコーポレーテッド 糖尿病および高血圧を治療するためのジペプチジルペプチダーゼ−4インヒビターと降圧薬との組合せ
EP1944301A4 (en) 2005-10-27 2012-01-04 Msd Kk NEW BENZOXATHIIN DERIVATIVES
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
JP5165582B2 (ja) * 2005-12-16 2013-03-21 メルク・シャープ・エンド・ドーム・コーポレイション ジペプチジルペプチダーゼ−4インヒビターとメトホルミンとを組み合わせた医薬組成物
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
GB0526291D0 (en) * 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
KR20080081354A (ko) * 2005-12-28 2008-09-09 다케다 야쿠힌 고교 가부시키가이샤 당뇨병 치료제
US20090156465A1 (en) 2005-12-30 2009-06-18 Sattigeri Jitendra A Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors
BRPI0620844A2 (pt) * 2005-12-30 2011-11-29 Ranbaxy Lab Ltd compostos antagonistas dos receptores muscarìnicos, seus métodos de preparação, composições farmacêuticas compreendendo os mesmos, usos dos referidos compostos na preparação de medicamentos
JP5111398B2 (ja) * 2006-01-25 2013-01-09 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阻害剤としてのアミノシクロヘキサン類
EP1995237A4 (en) * 2006-03-08 2011-07-06 Kyorin Seiyaku Kk PROCESS FOR PREPARING AN AMINOACETYLPYRROLIDINCARBONITRILE DERIVATIVE AND PRODUCTION PRODUCT THEREOF
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US20100029941A1 (en) * 2006-03-28 2010-02-04 Takeda Pharmaceutical Company Limited Preparation of (r)-3-aminopiperidine dihydrochloride
CL2007001006A1 (es) 2006-04-11 2008-07-11 Novartis Ag Compuestos derivados de piperidina u 8-aza-biciclo[3.2.1]octano sustituidos; formulacion farmaceutica; producto; y uso para el tratamiento o prevencion de enfermedades tales como diabetes mellitus no insulino dependiente, artritis, obesidad, dislipid
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
EP2410330A3 (en) * 2006-04-11 2012-06-13 Arena Pharmaceuticals, Inc. Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
NZ600394A (en) 2006-05-04 2014-04-30 Boehringer Ingelheim Int Polymorphs of a dpp-iv enzyme inhibitor
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
KR20090047546A (ko) 2006-09-07 2009-05-12 니코메드 게엠베하 당뇨병을 위한 조합 치료
GEP20125701B (en) * 2006-09-13 2012-12-10 Takeda Pharmaceuticals Co Application of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
AU2007301126A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
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
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
KR20080071476A (ko) * 2007-01-30 2008-08-04 주식회사 엘지생명과학 신규한 디펩티딜 펩티데이즈 iv(dpp-iv) 저해제
DE602008003522D1 (de) 2007-02-01 2010-12-30 Takeda Pharmaceutical Feste zubereitung mit alogliptin und pioglitazon
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US20080064701A1 (en) * 2007-04-24 2008-03-13 Ramesh Sesha Anti-diabetic combinations
US20070172525A1 (en) * 2007-03-15 2007-07-26 Ramesh Sesha Anti-diabetic combinations
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
EP2145884B1 (en) 2007-04-02 2014-08-06 Msd K.K. Indoledione derivative
CN101652147B (zh) 2007-04-03 2013-07-24 田边三菱制药株式会社 二肽基肽酶iv抑制化合物和甜味剂的并用
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
US8338458B2 (en) 2007-05-07 2012-12-25 Merck Sharp & Dohme Corp. Method of treatment using fused aromatic compounds having anti-diabetic activity
WO2008141021A1 (en) * 2007-05-08 2008-11-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of tetrahydrotriazolopyrazine compounds and their use as dpp-iv inhibitors
US8034782B2 (en) 2008-07-16 2011-10-11 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
ES2559319T3 (es) 2007-06-04 2016-02-11 Synergy Pharmaceuticals Inc. Agonistas de guanilato cliclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
JP5508258B2 (ja) 2007-06-04 2014-05-28 ベン グリオン ユニバーシティ オブ ザ ネガフ リサーチ アンド ディベロップメント オーソリティ トリアリール化合物および前記化合物を含む組成物
CN101318922B (zh) * 2007-06-08 2010-11-10 上海阳帆医药科技有限公司 一类二肽基肽酶抑制剂、合成方法和用途
CL2008002427A1 (es) 2007-08-16 2009-09-11 Boehringer Ingelheim Int Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2.
ES2733348T3 (es) * 2007-08-17 2019-11-28 Boehringer Ingelheim Int Derivados de purina para uso en el tratamiento de enfermedades relacionadas con FAP
CN101397300B (zh) * 2007-09-04 2011-04-27 山东轩竹医药科技有限公司 二肽酶-ⅳ抑制剂衍生物
US20090076013A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched sitagliptin
CN101417999A (zh) * 2007-10-25 2009-04-29 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
WO2009084024A2 (en) * 2007-11-02 2009-07-09 Glenmark Generics Limited A process for the preparation of r-sit agliptin and its pharmaceutically acceptable salts thereof
US20090192326A1 (en) * 2007-11-13 2009-07-30 Nurit Perlman Preparation of sitagliptin intermediate
WO2009085990A2 (en) 2007-12-20 2009-07-09 Dr. Reddy's Laboratories Limited Processes for the preparation of sitagliptin and pharmaceutically acceptable salts thereof
JP5358585B2 (ja) * 2007-12-21 2013-12-04 エルジー ライフ サイエンス リミテッド ジペプチジルペプチダーゼ−iv阻害化合物、同化合物を製造する方法、及び活性剤として同化合物を含む医薬組成物
CN101468988A (zh) * 2007-12-26 2009-07-01 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
CL2008003653A1 (es) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
CL2009000135A1 (es) 2008-01-24 2009-10-09 M/S Panacea Biotec Ltd Compuestos derivados de 1,4-benzodiazepinas sustituidas, inhibidores de dipeptidilpeptidasa iv (dpp-iv); composicion farmaceutica; procedimiento de preparacion; y su uso en el tratamiento de enfermedades tales como diabetes tipo 2, cataratas, glaucoma, hipertrofia prostatica benigna, cancer, entre otras; compuestos intermediarios.
US20100330177A1 (en) * 2008-02-05 2010-12-30 Merck Sharp & Dohme Corp. Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-iv inhibitor
JP2011513408A (ja) * 2008-03-04 2011-04-28 メルク・シャープ・エンド・ドーム・コーポレイション メトホルミン及びジペプチジルペプチダーゼ−iv阻害剤の併用医薬組成物
EP2264026A4 (en) 2008-03-06 2012-03-28 Msd Kk ALKYLAMINOPYRIDINDERIVATE
US8551524B2 (en) * 2008-03-14 2013-10-08 Iycus, Llc Anti-diabetic combinations
US20090247532A1 (en) * 2008-03-28 2009-10-01 Mae De Ltd. Crystalline polymorph of sitagliptin phosphate and its preparation
EP2272841A1 (en) 2008-03-28 2011-01-12 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor
AR071175A1 (es) 2008-04-03 2010-06-02 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante
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
US20090264476A1 (en) * 2008-04-18 2009-10-22 Mckelvey Craig CB-1 receptor modulator formulations
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
US8003672B2 (en) * 2008-04-21 2011-08-23 Merck Sharp & Dohme Corp. CB-1 receptor modulator formulations
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
EP2328910B1 (en) 2008-06-04 2014-08-06 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2009154132A1 (ja) 2008-06-19 2009-12-23 萬有製薬株式会社 スピロジアミン-ジアリールケトオキシム誘導体
WO2010000469A2 (en) 2008-07-03 2010-01-07 Ratiopharm Gmbh Crystalline salts of sitagliptin
EP2324027B1 (en) * 2008-07-29 2016-02-24 Medichem, S.A. New crystalline salt forms of a 5,6,7,8-tetrahydro-1,2,4- triazolo[4,3-a]pyrazine derivative
US20110124674A1 (en) 2008-07-30 2011-05-26 Hiroyuki Kishino 5/5-or 5/6-membered condensed ring cycloalkylamine derivative
KR20190016601A (ko) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
CA2732984A1 (en) * 2008-08-07 2010-02-11 Kyorin Pharmaceutical Co., Ltd. Process for production of bicyclo[2.2.2]octylamine derivative
US20110152342A1 (en) * 2008-08-14 2011-06-23 Hiroshi Uchida Stabilized pharmaceutical composition
CA2735562C (en) 2008-08-15 2017-10-17 Boehringer Ingelheim International Gmbh Dpp-4 inhibitors for wound healing
WO2010032264A2 (en) * 2008-08-27 2010-03-25 Cadila Healthcare Limited Improved process for preparation of (2r)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin- 7(8h)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine & new impurities in preparation thereof
MX2011002558A (es) 2008-09-10 2011-04-26 Boehringer Ingelheim Int Terapia de combinacion para el tratamiento de diabetes y estados relacionados.
WO2010039789A1 (en) 2008-10-03 2010-04-08 Schering Corporation Spiro-imidazolone derivatives as glucagon receptor antagonists
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
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
KR101320245B1 (ko) 2008-10-30 2013-10-30 머크 샤프 앤드 돔 코포레이션 이소니코틴아미드 오렉신 수용체 길항제
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
US8759539B2 (en) 2008-11-17 2014-06-24 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
CA2745037C (en) 2008-12-23 2020-06-23 Boehringer Ingelheim International Gmbh Salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8(3-(r)-amino-piperidin-1-yl)-xanthine
WO2010078440A1 (en) * 2008-12-31 2010-07-08 Chiral Quest, Inc. Process and intermediates for the preparation of n-acylated-4-aryl beta-amino acid derivatives
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
WO2010079433A2 (en) * 2009-01-07 2010-07-15 Glenmark Pharmaceuticals, S.A. Pharmaceutical composition that includes a dipeptidyl peptidase-iv inhibitor
KR101750420B1 (ko) 2009-01-09 2017-06-26 오키드 파마 리미티드 디펩티딜 펩티다제 iv 억제제
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
EP2218721A1 (en) 2009-02-11 2010-08-18 LEK Pharmaceuticals d.d. Novel salts of sitagliptin
AU2010212867B2 (en) 2009-02-13 2013-05-16 Boehringer Ingelheim International Gmbh Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a further antidiabetic agent and uses thereof
CN117547538A (zh) 2009-02-13 2024-02-13 勃林格殷格翰国际有限公司 包含dpp-4抑制剂(利格列汀)任选地组合其它抗糖尿病药的抗糖尿病药物
EP2223923A1 (en) 2009-02-25 2010-09-01 Esteve Química, S.A. Process for the preparation of a chiral beta aminoacid derivative and intermediates thereof
CN101824036A (zh) * 2009-03-05 2010-09-08 上海恒瑞医药有限公司 四氢咪唑并[1,5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用
NZ608028A (en) 2009-03-30 2014-09-26 Dong A Pharm Co Ltd Improved method for preparing dipeptidyl peptidase-iv inhibitor and intermediate
BRPI1014070B8 (pt) 2009-03-30 2021-05-25 Dong A Pharm Co Ltd processos para a produção de inibidor de dipeptidil peptidase-iv e intermediário
CN101849944A (zh) * 2009-03-31 2010-10-06 江苏恒瑞医药股份有限公司 治疗2型糖尿病的药物组合物
WO2010122578A2 (en) * 2009-04-20 2010-10-28 Msn Laboratories Limited Process for the preparation of sitagliptin and its intermediates
CA2759077C (en) * 2009-05-11 2016-02-16 Generics [Uk] Limited Sitagliptin synthesis
CN101899047B (zh) * 2009-05-26 2016-01-20 盛世泰科生物医药技术(苏州)有限公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的β-氨基四氢吡嗪、四氢嘧啶和四氢吡啶
CN101899048B (zh) * 2009-05-27 2013-04-17 上海恒瑞医药有限公司 (R)-7-[3-氨基-4-(2,4,5-三氟-苯基)-丁酰]-3-三氟甲基-5,6,7,8-四氢-咪唑并[1,5-a]吡嗪-1-羧酸甲酯的盐
US8470773B2 (en) 2009-06-12 2013-06-25 Merck Sharp & Dohme Corp. Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
IT1395596B1 (it) 2009-06-30 2012-10-16 Dipharma Francis Srl Procedimento per la preparazione di sitagliptin
AR077463A1 (es) * 2009-07-09 2011-08-31 Irm Llc Derivados de imidazo[1, 2 - a]pirazina y su uso en medicamentos para el tratamiento de enfermedades parasitarias
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
US20120189611A1 (en) 2009-08-03 2012-07-26 Kaneka Corporation Dipeptidyl peptidase-4 inhibitor
EP2464228B1 (en) 2009-08-13 2017-12-06 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
CN102471344B (zh) * 2009-08-13 2016-01-20 桑多斯股份公司 7-[(3r)-3-氨基-1-氧代-4-(2,4,5-三氟苯基)丁基]-5,6,7,8-四氢-3-(三氟甲基)-1,2,4-三唑并[4,3-a]吡嗪的结晶化合物
BR112012004335A8 (pt) 2009-09-02 2016-06-21 Merck Sharp & Dohme Composto, composição farmacêutica, e, uso do composto.
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
EP2295083A1 (de) 2009-09-15 2011-03-16 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit den Wirkstoffen Metformin und Sitagliptin oder Vildagliptin
CN102030683B (zh) * 2009-09-27 2013-07-31 浙江九洲药业股份有限公司 西他列汀中间体及其制备方法和用途
EP2308847B1 (en) 2009-10-09 2014-04-02 EMC microcollections GmbH Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases
EP2501685A1 (en) 2009-11-16 2012-09-26 Mellitech [1,5]-diazocin derivatives
CN102753161A (zh) 2009-11-27 2012-10-24 贝林格尔.英格海姆国际有限公司 基因型糖尿病患者利用dpp-iv抑制剂例如利拉利汀的治疗
EP2521721B1 (en) 2009-12-30 2014-10-01 Shanghai Fochon Pharmaceutical Co. Ltd 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors
KR101156587B1 (ko) 2010-02-19 2012-06-20 한미사이언스 주식회사 시타글립틴의 제조방법 및 이에 사용되는 아민염 중간체
WO2011103256A1 (en) 2010-02-22 2011-08-25 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
ES2481823T3 (es) 2010-03-10 2014-07-31 Probiodrug Ag Inhibidores heterocíclicos de glutaminil ciclasa (QC, EC 2.3.2.5)
CZ303113B6 (cs) 2010-03-16 2012-04-11 Zentiva, K.S. Zpusob prípravy sitagliptinu
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
US8183373B2 (en) 2010-03-31 2012-05-22 Teva Pharmaceutical Industries Ltd. Solid state forms of sitagliptin salts
EP2769978A1 (en) * 2010-04-05 2014-08-27 Cadila Pharmaceuticals Limited saxagliptin derivatives
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
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP2566843B1 (en) * 2010-04-28 2017-03-29 Sun Pharmaceutical Industries Limited Process for the preparation of chiral beta amino carboxamide derivatives
CN107961377B (zh) 2010-05-05 2022-11-22 勃林格殷格翰国际有限公司 组合疗法
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
CN102260265B (zh) 2010-05-24 2015-09-02 上海阳帆医药科技有限公司 六氢吡咯[3,4-b]吡咯衍生物、其制备方法及其用途
US8765668B2 (en) * 2010-06-04 2014-07-01 Lek Pharmaceuticals D.D. Methods of synthesis of β-aminobutyryl substituted compounds
EP2392575A1 (en) 2010-06-04 2011-12-07 LEK Pharmaceuticals d.d. A novel synthetic approach to ß-aminobutyryl substituted compounds
EP2397141A1 (en) 2010-06-16 2011-12-21 LEK Pharmaceuticals d.d. Process for the synthesis of beta-amino acids and derivatives thereof
MX2012014247A (es) 2010-06-24 2013-01-18 Boehringer Ingelheim Int Terapia para la diabetes.
EP2407469A1 (en) 2010-07-13 2012-01-18 Chemo Ibérica, S.A. Salt of sitagliptin
JP6077996B2 (ja) 2010-07-28 2017-02-08 ニューラルステム, インコーポレイテッド 神経変性性疾患および/または障害を処置および/または逆転させるための方法
EP2423178A1 (en) 2010-07-28 2012-02-29 Chemo Ibérica, S.A. Process for the production of sitagliptin
EP2418196A1 (en) * 2010-07-29 2012-02-15 IMTM GmbH Dual alanyl-aminopeptidase and dipeptidyl-peptidase IV inhibitors
WO2012024183A1 (en) 2010-08-18 2012-02-23 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US20130158265A1 (en) 2010-08-27 2013-06-20 Dhananjay Govind Sathe Sitagliptin, salts and polymorphs thereof
WO2012035549A2 (en) 2010-09-13 2012-03-22 Panacea Biotec Ltd An improved process for the synthesis of beta amino acid derivatives
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP3323818A1 (en) 2010-09-22 2018-05-23 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN103228658A (zh) 2010-10-08 2013-07-31 卡迪拉保健有限公司 用于通过酶促转化制备西他列汀的中间体的方法
WO2012049566A1 (en) 2010-10-14 2012-04-19 Japan Tobacco Inc. Combination therapy for use in treating diabetes
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
CN102485718B (zh) 2010-12-03 2014-03-26 浙江海翔药业股份有限公司 西他列汀的中间体及其制备方法
EP2648517B1 (en) 2010-12-06 2015-08-05 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
WO2012076973A2 (en) 2010-12-09 2012-06-14 Aurobindo Pharma Limited Novel salts of dipeptidyl peptidase iv inhibitor
TWI494313B (zh) * 2010-12-29 2015-08-01 Jiangsu Hengrui Medicine Co 治療包括人類之哺乳動物中第2型糖尿病的醫藥組成物
US11759441B2 (en) 2011-01-07 2023-09-19 Anji Pharmaceuticals Inc. Biguanide compositions and methods of treating metabolic disorders
US11974971B2 (en) 2011-01-07 2024-05-07 Anji Pharmaceuticals Inc. Compositions and methods for treating metabolic disorders
US8796338B2 (en) 2011-01-07 2014-08-05 Elcelyx Therapeutics, Inc Biguanide compositions and methods of treating metabolic disorders
US9572784B2 (en) 2011-01-07 2017-02-21 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
HRP20201731T1 (hr) * 2011-01-07 2020-12-25 Anji Pharma (Us) Llc Terapije na bazi liganda kemozensoričkog receptora
US9480663B2 (en) 2011-01-07 2016-11-01 Elcelyx Therapeutics, Inc. Biguanide compositions and methods of treating metabolic disorders
US9211263B2 (en) 2012-01-06 2015-12-15 Elcelyx Therapeutics, Inc. Compositions and methods of treating metabolic disorders
KR101290029B1 (ko) 2011-01-20 2013-07-30 에스티팜 주식회사 시타글립틴의 중간체 제조방법
ES2569248T3 (es) 2011-01-31 2016-05-09 Cadila Healthcare Limited Tratamiento para la lipodistrofia
EP3243385B1 (en) 2011-02-25 2021-01-13 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
CN103764672A (zh) 2011-03-01 2014-04-30 辛纳吉制药公司 制备鸟苷酸环化酶c激动剂的方法
EP2681220B1 (en) * 2011-03-03 2015-08-19 Cadila Healthcare Limited Novel crystalline form of a dpp-iv inhibitor
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
SI2691083T1 (sl) 2011-03-29 2017-12-29 Krka, D.D., Novo Mesto Farmacevtski sestavek sitagliptina
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
AU2012240122B2 (en) 2011-04-08 2016-08-25 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
KR101369584B1 (ko) 2011-04-19 2014-03-06 일양약품주식회사 페닐-이속사졸 유도체 및 그의 제조방법
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
CN102757431B (zh) * 2011-04-24 2016-03-30 浙江华海药业股份有限公司 一种合成西他列汀的新方法
ITMI20110765A1 (it) 2011-05-05 2012-11-06 Chemo Iberica Sa Processo per la produzione di sitagliptina
US8524936B2 (en) 2011-05-18 2013-09-03 Milan Soukup Manufacturing process for sitagliptin from L-aspartic acid
US9359385B2 (en) * 2011-05-27 2016-06-07 Lek Pharmaceuticals D.D. Preparation of sitagliptin intermediates
EP2527320A1 (en) 2011-05-27 2012-11-28 LEK Pharmaceuticals d.d. Preparation of Sitagliptin Intermediates
US20140088124A1 (en) 2011-06-02 2014-03-27 Robert J. DeVita Imidazole derivatives
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR086675A1 (es) * 2011-06-14 2014-01-15 Merck Sharp & Dohme Composiciones farmaceuticas de combinaciones de inhibidores de la dipeptidil peptidasa-4 con simvastatina
CA2838079A1 (en) 2011-06-16 2012-12-20 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
US20150025080A1 (en) 2011-06-29 2015-01-22 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
EP2726075A4 (en) 2011-06-29 2014-11-19 Merck Sharp & Dohme NEW CRYSTALLINE FORMS OF A DIPEPTIDYL-PEPTIDASE IV HEMMER
WO2013001457A1 (en) 2011-06-30 2013-01-03 Ranbaxy Laboratories Limited Novel salts of sitagliptin
WO2013006526A2 (en) 2011-07-05 2013-01-10 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
PL2731947T3 (pl) 2011-07-15 2019-07-31 Boehringer Ingelheim International Gmbh Podstawiona dimeryczna pochodna chinazoliny, sposób jej wytwarzania i jej zastosowanie w kompozycjach farmaceutycznych do leczenia cukrzycy typu I i II
EA024688B1 (ru) * 2011-07-27 2016-10-31 ФАРМА ДжРС, Д.О.О. Способ получения ситаглиптина и его фармацевтически приемлемых солей
EA201490556A1 (ru) 2011-09-07 2014-08-29 Сановел Илач Санайи Ве Тиджарет Аноним Ширкети Составы ингибитора дпп-4
US9422266B2 (en) 2011-09-30 2016-08-23 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2578208B1 (en) 2011-10-06 2014-05-21 Sanovel Ilac Sanayi ve Ticaret A.S. DPP-IV inhibitor solid dosage formulations
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EP2766369A4 (en) * 2011-10-14 2015-07-01 Laurus Labs Private Ltd NOVEL SALT OF SITAGLIPTIN, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION THEREOF
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
EP2771000B1 (en) 2011-10-24 2016-05-04 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
CN102603749B (zh) * 2011-10-27 2017-02-08 浙江华海药业股份有限公司 一种西他列汀中间体的合成方法
WO2013065066A1 (en) 2011-11-02 2013-05-10 Cadila Healthcare Limited Processes for preparing 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,41-triazolo[43-a]pyrazin-7(8h)-yl]-l-(2,4,5- trifluorophenyl)butan-2-amine
WO2013068328A1 (en) 2011-11-07 2013-05-16 Intervet International B.V. Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors
WO2013068439A1 (en) 2011-11-09 2013-05-16 Intervet International B.V. 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors
JP6101279B2 (ja) 2011-11-15 2017-03-22 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Gpr119アゴニストとして有用な置換シクロプロピル化合物
US20140350023A1 (en) 2011-12-08 2014-11-27 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
AU2013207329B2 (en) 2012-01-06 2017-10-26 Anji Pharmaceuticals Inc. Compositions and methods for treating metabolic disorders
KR20230095124A (ko) 2012-01-06 2023-06-28 앤지 파마 유에스 엘엘씨 바이구아나이드 조성물 및 대사 장애를 치료하는 방법
EP2615080A1 (en) 2012-01-12 2013-07-17 LEK Pharmaceuticals d.d. Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
ES2421956B1 (es) 2012-03-02 2014-09-29 Moehs Ibérica S.L. Nueva forma cristalina de sulfato de sitagliptina
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013155600A1 (en) 2012-04-16 2013-10-24 Kaneq Pharma Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors
TWI469785B (zh) 2012-04-25 2015-01-21 Inovobiologic Inc 用於治療代謝性疾病之膳食纖維組成物
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
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
EP2674432A1 (en) 2012-06-14 2013-12-18 LEK Pharmaceuticals d.d. New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds
EP2874622A4 (en) 2012-07-23 2015-12-30 Merck Sharp & Dohme TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS
EP2874626A4 (en) 2012-07-23 2016-03-23 Merck Sharp & Dohme TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS
RU2015106909A (ru) 2012-08-02 2016-09-27 Мерк Шарп И Доум Корп. Антидиабетические трициклические соединения
JP2015525793A (ja) 2012-08-08 2015-09-07 シプラ・リミテッド シタグリプチン及び中間体化合物の調製方法
CN102898387B (zh) * 2012-09-26 2015-01-07 浙江工业大学 管道化连续生产n-[(2z)-哌嗪-2-亚基]-2,2,2-三氟乙酰肼的方法
TWI500613B (zh) 2012-10-17 2015-09-21 Cadila Healthcare Ltd 新穎之雜環化合物
CN103788070B (zh) * 2012-10-26 2017-10-20 南京华威医药科技开发有限公司 Dpp‑4抑制剂类多聚物
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
CZ306115B6 (cs) * 2012-12-04 2016-08-10 Zentiva, K.S. Způsob přípravy derivátů kyseliny 3-amino-4-(2,4,5-trifluorfenyl)-butanové
CN103319487B (zh) * 2013-01-10 2015-04-01 药源药物化学(上海)有限公司 西格列汀的制备方法及其中间体
EP2769712A1 (en) 2013-02-21 2014-08-27 Siegfried International AG Pharmaceutical formulation comprising DPP-IV inhibitor agglomerates and DPP-IV inhibitor particles
KR20150118158A (ko) 2013-02-22 2015-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병 비시클릭 화합물
CN105669682B (zh) * 2013-02-22 2019-08-30 成都先导药物开发股份有限公司 一种dpp-iv抑制剂的中间体
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
AU2014235215A1 (en) 2013-03-15 2015-10-01 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
IN2013MU00916A (enExample) 2013-03-20 2015-06-26 Cadila Healthcare Ltd
JP6246895B2 (ja) 2013-04-22 2017-12-13 カディラ・ヘルスケア・リミテッド 非アルコール性脂肪性肝疾患(nafld)のための新規組成物
MX2015016403A (es) 2013-05-30 2016-04-11 Cadila Healthcare Ltd Proceso para la preparacion de pirroles que tienen actividad hipolipidemica e hipocolesterolemica.
BR112015030326A2 (pt) 2013-06-05 2017-08-29 Synergy Pharmaceuticals Inc Agonistas ultrapuros de guanilato ciclase c, método de fabricar e usar os mesmos
WO2015001568A2 (en) * 2013-07-01 2015-01-08 Laurus Labs Private Limited Sitagliptin lipoate salt, process for the preparation and pharmaceutical composition thereof
TW201513857A (zh) 2013-07-05 2015-04-16 Cadila Healthcare Ltd 協同性組成物
IN2013MU02470A (enExample) 2013-07-25 2015-06-26 Cadila Healthcare Ltd
IN2013MU02905A (enExample) 2013-09-06 2015-07-03 Cadila Healthcare Ltd
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US10517892B2 (en) 2013-10-22 2019-12-31 Medtronic Minimed, Inc. Methods and systems for inhibiting foreign-body responses in diabetic patients
CZ2013842A3 (cs) 2013-11-01 2015-05-13 Zentiva, K.S. Stabilní polymorf soli (2R)-4-oxo-4-[3-(trifluorometyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorofenyl)butan-2-aminu s kyselinou L-vinnou
CN106061940A (zh) 2013-11-05 2016-10-26 本古里安大学内盖夫研究发展局 治疗糖尿病和由其引发的并发疾病的化合物
CN103626775B (zh) * 2013-12-02 2015-05-20 南京华威医药科技开发有限公司 具有二嗪结构的dpp-4抑制剂
WO2015089809A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
WO2015114657A2 (en) 2014-01-21 2015-08-06 Cadila Healthcare Limited Amorphous form of sitagliptin free base
EP3097101B1 (en) 2014-01-24 2020-12-23 Merck Sharp & Dohme Corp. Isoquinoline derivatives as mgat2 inhibitors
IN2014MU00651A (enExample) 2014-02-25 2015-10-23 Cadila Healthcare Ltd
WO2015128453A1 (en) 2014-02-28 2015-09-03 Boehringer Ingelheim International Gmbh Medical use of a dpp-4 inhibitor
WO2015145333A1 (en) 2014-03-26 2015-10-01 Sun Pharmaceutical Industries Limited Process for the preparation of sitagliptin and its intermediate
AU2015247921B2 (en) * 2014-04-17 2019-07-11 Merck Sharp & Dohme Llc Sitagliptin tannate complex
WO2015162506A1 (en) 2014-04-21 2015-10-29 Suven Life Sciences Limited Process for the preparation of sitagliptin and novel intermediates
WO2015170340A2 (en) * 2014-05-06 2015-11-12 Laurus Labs Private Limited Novel polymorphs of sitagliptin hydrochloride, processes for its preparation and pharmaceutical composition thereof
WO2015176267A1 (en) 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2016014324A1 (en) 2014-07-21 2016-01-28 Merck Sharp & Dohme Corp. Process for preparing chiral dipeptidyl peptidase-iv inhibitors
US10968193B2 (en) 2014-08-08 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
US10100042B2 (en) 2014-08-08 2018-10-16 Merck Sharp & Dohme Corp. [5,6]—fused bicyclic antidiabetic compounds
CN104140430B (zh) * 2014-08-08 2016-07-13 广东东阳光药业有限公司 一种异构体的消旋方法
WO2016022448A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
WO2016046679A1 (en) * 2014-09-28 2016-03-31 Mohan M Alapati Compositions and methods for the treatment of diabetes and pre-diabetes
WO2016064737A1 (en) 2014-10-20 2016-04-28 Neuralstem, Inc. Stable neural stem cells comprising an exogenous polynucleotide coding for a growth factor and methods of use thereof
WO2016112075A1 (en) 2015-01-06 2016-07-14 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
WO2016110750A1 (en) 2015-01-08 2016-07-14 Lee Pharma Limited Novel process for the preparation of dipeptidyl peptidase-4 (dpp-4) enzyme inhibitor
CZ27898U1 (cs) 2015-01-13 2015-03-02 Zentiva, K.S. Krystalická modifikace 2 L-vínanu (3R)-3-amino-1-[3-(trifluormethyl)-6,8-dihydro-5H-[1,2,4,]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorfenyl)butan-1-onu
CZ27930U1 (cs) 2015-01-13 2015-03-10 Zentiva, K.S. Krystalická modifikace 3 L-vínanu (3R)-3-amino-1-[3-(trifluormethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorfenyl)butan-1-onu
HK1249847A1 (zh) 2015-03-09 2018-11-16 Intekrin Therapeutics, Inc. 用於治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
US9447015B1 (en) * 2015-04-15 2016-09-20 Valent Biosciences Corporation (S)-2′-vinyl-abscisic acid derivatives
KR101772898B1 (ko) 2015-06-11 2017-08-31 동방에프티엘(주) 시타글립틴의 개선된 제조방법
KR101709127B1 (ko) 2015-06-16 2017-02-22 경동제약 주식회사 Dpp-iv 억제제의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 dpp-iv 억제제의 제조방법
KR102603199B1 (ko) 2015-06-22 2023-11-16 아레나 파마슈티칼스, 인크. S1p1 수용체-관련 장애에서의 사용을 위한 (r)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[b]인돌-3-일)아세트산 (화합물 1)의 결정성 l-아르기닌 염
CN105017260B (zh) * 2015-07-30 2017-04-19 新发药业有限公司 一种西他列汀中间体三唑并吡嗪衍生物的制备方法
US11000521B2 (en) 2015-08-03 2021-05-11 Institut Pasteur Dipeptidylpeptidase 4 inhibition enhances lymphocyte trafficking, improving both naturally occurring tumor immunity and immunotherapy
MX2018002916A (es) * 2015-09-09 2018-09-12 C Lau Warren Metodos, composiciones y usos de nuevos inhibidores de fyn quinasa.
KR20170036288A (ko) 2015-09-24 2017-04-03 주식회사 종근당 시타글립틴의 신규염 및 이의 제조방법
US10385017B2 (en) 2015-10-14 2019-08-20 Cadila Healthcare Limited Pyrrole compound, compositions and process for preparation thereof
ES2638266T3 (es) * 2015-10-22 2017-10-19 F.I.S.- Fabbrica Italiana Sintetici S.P.A. Procedimiento mejorado para la preparación de triazol y una de sus sales
WO2017095725A1 (en) 2015-11-30 2017-06-08 Merck Sharp & Dohme Corp. Aryl sulfonamides as blt1 antagonists
EP3383868B1 (en) 2015-11-30 2022-10-05 Merck Sharp & Dohme LLC Aryl sulfonamides as blt1 antagonists
KR102405278B1 (ko) 2016-04-22 2022-06-07 악셀레론 파마 인코포레이티드 Alk7 결합 단백질 및 이들의 용도
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
CA3022202A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
US10414774B2 (en) 2016-08-15 2019-09-17 Merck Sharp & Dohme Corp. Compound useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolc disease
WO2018034917A1 (en) 2016-08-15 2018-02-22 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
CN106124667B (zh) * 2016-08-29 2018-07-31 上海应用技术学院 一种分离测定西格列汀有关物质的方法
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
MX2016016260A (es) 2016-12-08 2018-06-07 Alparis Sa De Cv Nuevas formas solidas de sitagliptina.
JP6840853B2 (ja) 2016-12-09 2021-03-10 カディラ・ヘルスケア・リミテッド 原発性胆汁性胆管炎の治療
WO2018107415A1 (en) 2016-12-15 2018-06-21 Merck Sharp & Dohme Corp. Hydroxy isoxazole compounds useful as gpr120 agonists
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
US11197949B2 (en) 2017-01-19 2021-12-14 Medtronic Minimed, Inc. Medication infusion components and systems
US10047094B1 (en) 2017-02-10 2018-08-14 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Process for the preparation of triazole and salt thereof
MA47504A (fr) 2017-02-16 2019-12-25 Arena Pharm Inc Composés et méthodes de traitement de l'angiocholite biliaire primitive
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
BR112019020485A2 (pt) 2017-04-03 2020-05-12 Coherus Biosciences, Inc. Agonista ppary para tratamento de paralisia supranuclear progressiva
JP7377717B2 (ja) 2017-04-24 2023-11-10 ノバルティス アーゲー 2-アミノ-l-(2-(4-フルオロフェニル)-3-(4-フルオロフェニルアミノ)-8,8-ジメチル-5,6-ジヒドロイミダゾ[1,2-a]ピラジン-7(8h)-イル)エタノン及びそれらの組み合わせの治療レジメン
US11096890B2 (en) 2017-09-29 2021-08-24 Merck Sharp & Dohme Corp. Chewable dosage forms containing sitagliptin and metformin
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
KR20190060235A (ko) 2017-11-24 2019-06-03 제일약품주식회사 시타글립틴 캄실산염의 제조방법
TR201722603A2 (tr) 2017-12-28 2019-07-22 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Metformi̇n ve si̇tagli̇pti̇n i̇çeren sicak eri̇tme ekstrüzyonu i̇le gerçekleşti̇ri̇len tablet formülasyonlari
CN108586346B (zh) 2018-05-10 2019-10-01 北京富盛嘉华医药科技有限公司 一种生物催化合成西他列汀及其中间体的方法
CN112601516A (zh) 2018-06-06 2021-04-02 艾尼纳制药公司 治疗与s1p1受体相关的病况的方法
US12331018B2 (en) 2019-02-13 2025-06-17 Merck Sharp & Dohme Llc Pyrrolidine orexin receptor agonists
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
US12281109B2 (en) 2019-04-04 2025-04-22 Merck Sharp & Dohme Llc Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
EP4010314B1 (en) 2019-08-08 2024-02-28 Merck Sharp & Dohme LLC Heteroaryl pyrrolidine and piperidine orexin receptor agonists
EP4045048A4 (en) 2019-10-14 2023-05-24 Santa Farma Ilaç Sanayi A.S. ORAL FORMULATIONS COMPRISING SITAGLIPTIN HCI MONOHYDRATE WITH ENHANCED PHARMACEUTICAL CHARACTERISTICS
KR20210057603A (ko) 2019-11-12 2021-05-21 제이투에이치바이오텍 (주) 시타글립틴의 제조방법
US20230365533A1 (en) 2020-08-18 2023-11-16 Merck Sharp & Dohme Llc Bicycloheptane pyrrolidine orexin receptor agonists
US20230331732A1 (en) * 2020-09-10 2023-10-19 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
KR102589305B1 (ko) 2021-04-22 2023-10-16 주식회사 메디켐코리아 시타글립틴 인산염의 개선된 제조방법
CN113979896A (zh) * 2021-11-18 2022-01-28 浙江永太手心医药科技有限公司 一种西格列汀杂质i及其制备方法
WO2023139276A1 (en) 2022-01-24 2023-07-27 Zaklady Farmaceutyczne Polpharma S.A. Process for preparing crystalline sitagliptin hydrochloride monohydrate
EP4604931A1 (en) 2022-10-21 2025-08-27 Merck Sharp & Dohme LLC Compositions of a dipeptidyl peptidase-iv inhibitor and an antioxidant
EP4630568A1 (en) 2022-12-09 2025-10-15 KRKA, D.D., Novo Mesto Process for the preparation of sitagliptin
CN116064457B (zh) 2022-12-16 2025-08-19 浙江工业大学 一种ω-转氨酶突变体及其应用
EP4431087A1 (en) 2023-03-14 2024-09-18 Sanovel Ilac Sanayi Ve Ticaret A.S. A film coated tablet of sitagliptin or a pharmaceutically acceptable salt thereof
JP2025076633A (ja) 2023-11-02 2025-05-16 沢井製薬株式会社 シタグリプチン製剤及びその保管方法
EP4563143A1 (en) 2023-11-30 2025-06-04 Sanovel Ilac Sanayi ve Ticaret A.S. A bilayer tablet formulation of metformin and sitagliptin comprising antioxidant
EP4566593A1 (en) 2023-11-30 2025-06-11 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi A tablet comprising an extended-release formulation for metformin and immediate release formulation comprising sitagliptin

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
GB9324803D0 (en) * 1993-12-03 1994-01-19 Ferring Bv Enzyme inhibitors
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5705483A (en) * 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
DE19616486C5 (de) * 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO1999001423A1 (en) 1997-07-01 1999-01-14 Novo Nordisk A/S Glucagon antagonists/inverse agonists
AU9651198A (en) 1997-11-11 1999-05-31 Ono Pharmaceutical Co. Ltd. Fused pyrazine compounds
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
DE19828114A1 (de) * 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
FR2780974B1 (fr) 1998-07-08 2001-09-28 Sod Conseils Rech Applic Utilisation de derives d'imidazopyrazines pour preparer un medicament destine a traiter les pathologies qui resultent de la formation de la proteine g heterotrimetrique
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
AU3033500A (en) 1999-01-15 2000-08-01 Agouron Pharmaceuticals, Inc. Non-peptide glp-1 agonists
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
AU3441400A (en) 1999-03-29 2000-10-16 Uutech Limited Peptide
WO2000059887A1 (en) 1999-04-02 2000-10-12 Neurogen Corporation Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics
BR0010651A (pt) 1999-05-17 2002-03-19 Novo Nordisk As Composto, uso de um composto, composição farmacêutica, e, método para o tratamento e/ou prevenção de distúrbios ou de doenças mediadas por uma ação antagonìstica de glucagon
ES2307534T3 (es) 1999-09-28 2008-12-01 Bayer Corporation Agonistas de receptores 3 (r3) del peptido activador de la adenilato ciclasa hipofisiaria (pacap) y sus metodos de uso farmacologicos.
EP1228061A4 (en) 1999-11-12 2004-12-15 Guilford Pharm Inc DIPEPTIDYL PEPTIDASE IV INHIBITORS; METHODS OF MANUFACTURE AND USE OF SAID INHIBITORS
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
AU2001268958B2 (en) 2000-07-04 2006-03-09 Novo Nordisk A/S Heterocyclic compounds, which 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
DE60316416T2 (de) * 2002-03-25 2008-06-26 Merck & Co., Inc. Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes
EP1554280B1 (en) * 2002-10-07 2007-08-15 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
CA2513684A1 (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

Also Published As

Publication number Publication date
EP1625847B1 (en) 2010-06-16
CR7235A (es) 2006-05-31
JP2004536115A (ja) 2004-12-02
IS2964B (is) 2017-02-15
US20150359793A1 (en) 2015-12-17
ES2344846T3 (es) 2010-09-08
NL300357I2 (nl) 2009-01-05
MXPA04000018A (es) 2004-05-21
FR07C0041I2 (fr) 2016-09-30
EP1412357B1 (en) 2006-03-22
HRP20031098A2 (en) 2004-06-30
US20130217695A1 (en) 2013-08-22
DE60210093T2 (de) 2006-11-23
CY2008014I2 (el) 2009-11-04
CY2007019I1 (el) 2009-11-04
NO2007010I1 (no) 2007-09-17
TWI226331B (en) 2005-01-11
BG108493A (en) 2005-04-30
PE20030654A1 (es) 2003-07-29
EA006845B1 (ru) 2006-04-28
RS50737B (sr) 2010-08-31
NL300357I1 (nl) 2008-10-01
BRPI0210866B1 (pt) 2016-07-05
ME00439B (me) 2011-12-20
PT1625847E (pt) 2010-08-20
EA200501805A1 (ru) 2006-06-30
FR07C0041I1 (enExample) 2007-10-19
DK1412357T3 (da) 2006-07-17
LUC91360I2 (enExample) 2020-06-12
DE60210093D1 (de) 2006-05-11
CN1290848C (zh) 2006-12-20
MA27053A1 (fr) 2004-12-20
EP1412357A1 (en) 2004-04-28
CY2008014I1 (el) 2009-11-04
IS8617A (is) 2007-03-06
US20030100563A1 (en) 2003-05-29
JP3762407B2 (ja) 2006-04-05
HUP0401104A3 (en) 2006-02-28
EP1625847A1 (en) 2006-02-15
IS2218B (is) 2007-03-15
HUP0401104A2 (hu) 2004-09-28
GEP20063734B (en) 2006-01-10
CN1524082A (zh) 2004-08-25
PL196278B6 (pl) 2023-02-13
US7125873B2 (en) 2006-10-24
EP2292232B1 (en) 2014-08-20
NO2020007I1 (no) 2020-03-19
CN1861077A (zh) 2006-11-15
LTC1412357I2 (lt) 2021-01-11
SI1412357T1 (sl) 2006-06-30
YU100603A (sh) 2006-05-25
ES2259713T3 (es) 2006-10-16
HK1068882A1 (en) 2005-05-06
US20200206221A1 (en) 2020-07-02
US6699871B2 (en) 2004-03-02
UA74912C2 (en) 2006-02-15
US20060270679A1 (en) 2006-11-30
GEP20053734B (en) 2006-01-10
ATE471148T1 (de) 2010-07-15
NL300287I2 (nl) 2009-04-01
NO2008013I1 (no) 2008-09-08
WO2003004498A1 (en) 2003-01-16
DE122008000046I1 (de) 2009-02-05
HRP20031098B1 (en) 2012-03-31
US8440668B2 (en) 2013-05-14
IL178307A (en) 2010-04-15
ATE321048T1 (de) 2006-04-15
HUS0700005I1 (hu) 2022-01-28
PT1412357E (pt) 2006-07-31
BR0210866A (pt) 2004-06-29
BE2007C047I2 (enExample) 2021-06-04
NZ529833A (en) 2005-01-28
PL196278B1 (pl) 2007-12-31
AU2002320303B2 (en) 2004-10-14
HU225695B1 (hu) 2007-06-28
KR100606871B1 (ko) 2006-08-01
DOP2002000438A (es) 2003-01-31
LU91470I2 (fr) 2008-10-20
LUC91360I1 (enExample) 2020-04-23
AR036114A1 (es) 2004-08-11
IS7062A (is) 2003-11-28
CY2007019I2 (el) 2017-07-12
EP2292232A1 (en) 2011-03-09
FR08C0033I1 (enExample) 2008-09-26
US8168637B2 (en) 2012-05-01
LTPA2007006I1 (lt) 2020-04-27
US20040167133A1 (en) 2004-08-26
EP2226324A1 (en) 2010-09-08
EA200400153A1 (ru) 2004-06-24
CA2450740A1 (en) 2003-01-16
US20170348309A1 (en) 2017-12-07
CY1110784T1 (el) 2015-06-10
MY127961A (en) 2007-01-31
DE122007000056I1 (de) 2007-12-13
US20110190308A1 (en) 2011-08-04
NO2008013I2 (no) 2011-01-24
DK1625847T3 (da) 2010-10-18
IL159109A0 (en) 2004-05-12
FR08C0033I2 (fr) 2010-12-31
JO2230B1 (en) 2004-10-07
PL367279A1 (en) 2005-02-21
NL300287I1 (nl) 2007-10-01
KR20040010842A (ko) 2004-01-31
IL159109A (en) 2007-06-03
BRPI0210866B8 (pt) 2021-05-25
ZA200309294B (en) 2004-07-22
ECSP044935A (es) 2004-02-26
NO20040021L (no) 2004-01-05
NO321999B1 (no) 2006-07-31
EA012701B1 (ru) 2009-12-30
NO2007010I2 (no) 2009-12-14
US20100130504A1 (en) 2010-05-27
DE60236767D1 (de) 2010-07-29

Similar Documents

Publication Publication Date Title
CA2450740C (en) Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1490335B1 (en) Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1554256B1 (en) Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
AU2002320303A1 (en) Beta-amino tetrahydroimidazo (1, 2-A) pyrazines and tetrahydrotrioazolo (4, 3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
HK1148939A (en) Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines for use in the treatment of diabetes type ii
HK1143135A (en) Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines for use in the treatment of diabetes type ii

Legal Events

Date Code Title Description
EEER Examination request
MKEX Expiry

Effective date: 20220705