[go: up one dir, main page]

EA011086B9 - Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv - Google Patents

Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv

Info

Publication number
EA011086B9
EA011086B9 EA200601896A EA200601896A EA011086B9 EA 011086 B9 EA011086 B9 EA 011086B9 EA 200601896 A EA200601896 A EA 200601896A EA 200601896 A EA200601896 A EA 200601896A EA 011086 B9 EA011086 B9 EA 011086B9
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
dipeptidyl peptidase
proline derivatives
diabetic
prodrugs
Prior art date
Application number
EA200601896A
Other languages
English (en)
Other versions
EA200601896A1 (ru
EA011086B1 (ru
Inventor
Бернар Юлэн
Дэвид Уолтер Пиотровски
Original Assignee
Пфайзер Продактс Инк.
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=34966115&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA011086(B9) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200601896A1 publication Critical patent/EA200601896A1/ru
Publication of EA011086B1 publication Critical patent/EA011086B1/ru
Publication of EA011086B9 publication Critical patent/EA011086B9/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/12—Antiepileptics; Anticonvulsants for grand-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Anesthesiology (AREA)

Abstract

В настоящем изобретении представлены соединения формулы (I) и стереоизомеры, фармацевтически приемлемые соли соединений и стереоизомеров, где R, R, R, HET, n, Q, x, Y и Z такие, как представлено в описании; их композиции и их применение для лечения диабетических осложнений, включая диабетическую невропатию, диабетическую нефропатию, диабетическую микроангиопатию и подобные.
EA200601896A 2004-05-12 2005-04-29 Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv EA011086B9 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US57030004P 2004-05-12 2004-05-12
US66430505P 2005-03-21 2005-03-21
PCT/IB2005/001194 WO2005116014A1 (en) 2004-05-12 2005-04-29 Proline derivatives and their use as dipeptidyl peptidase iv inhibitors

Publications (3)

Publication Number Publication Date
EA200601896A1 EA200601896A1 (ru) 2007-02-27
EA011086B1 EA011086B1 (ru) 2008-12-30
EA011086B9 true EA011086B9 (ru) 2012-08-30

Family

ID=34966115

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200601896A EA011086B9 (ru) 2004-05-12 2005-04-29 Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv

Country Status (36)

Country Link
US (4) US7291618B2 (ru)
EP (2) EP2116541B1 (ru)
JP (1) JP4227660B2 (ru)
KR (1) KR100869616B1 (ru)
AP (1) AP2320A (ru)
AR (1) AR049894A1 (ru)
AT (1) ATE437870T1 (ru)
AU (1) AU2005247684B2 (ru)
BR (1) BRPI0510284A (ru)
CA (1) CA2566108C (ru)
CR (1) CR8744A (ru)
CY (1) CY1109322T1 (ru)
DE (1) DE602005015699D1 (ru)
DK (1) DK1753748T3 (ru)
EA (1) EA011086B9 (ru)
EC (1) ECSP066985A (ru)
ES (1) ES2327857T3 (ru)
GE (1) GEP20084421B (ru)
HR (1) HRP20090471T1 (ru)
IL (1) IL178339A (ru)
MA (1) MA28578B1 (ru)
MX (1) MXPA06013114A (ru)
MY (1) MY139805A (ru)
NL (1) NL1029015C2 (ru)
NO (1) NO20064400L (ru)
NZ (1) NZ550229A (ru)
PA (1) PA8632701A1 (ru)
PE (1) PE20060316A1 (ru)
PL (1) PL1753748T3 (ru)
PT (1) PT1753748E (ru)
RS (1) RS51106B (ru)
SI (1) SI1753748T1 (ru)
SV (1) SV2006002110A (ru)
TW (1) TWI347322B (ru)
UY (1) UY28892A1 (ru)
WO (1) WO2005116014A1 (ru)

Families Citing this family (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1757606T3 (da) * 2001-02-24 2009-09-07 Boehringer Ingelheim Pharma Anvendelse af xanthinderivater som l gemidler samt fremgangsm de til deres fremstilling
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
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
PL1753748T3 (pl) 2004-05-12 2010-01-29 Pfizer Prod Inc Pochodne proliny i ich zastosowanie jako inhibitorów peptydazy dipeptylowej IV
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
US7635698B2 (en) 2004-12-29 2009-12-22 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006073167A1 (ja) * 2005-01-07 2006-07-13 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
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
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
US7728146B2 (en) 2006-04-12 2010-06-01 Probiodrug Ag Enzyme inhibitors
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
JP5323684B2 (ja) 2006-05-04 2013-10-23 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 多形体
TW200815405A (en) * 2006-06-09 2008-04-01 Astrazeneca Ab Novel compounds
WO2007148185A2 (en) * 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
PE20090938A1 (es) * 2007-08-16 2009-08-08 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
CL2008002424A1 (es) * 2007-08-16 2009-09-11 Boehringer Ingelheim Int Composicion farmaceutica que comprende un compuesto derivado de pirazol-o-glucosido; y uso de la composicion farmaceutica para el tratamiento de la diabetes mellitus, tolerancia anormal a la glucosa e hiperglucemia, trastornos metabolicos, entre otras.
UA108596C2 (xx) 2007-11-09 2015-05-25 Інгібітори пептиддеформілази
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
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"
EP2326326B1 (en) * 2008-08-15 2019-10-09 Boehringer Ingelheim International GmbH Dpp-4 inhibitors for use for the treatment of wound healing in diabetic patients
JP2012502081A (ja) 2008-09-10 2012-01-26 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 糖尿病及び関連症状の治療のための組み合わせ治療
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
WO2010071819A1 (en) * 2008-12-19 2010-06-24 Schering Corporation Bicyclic heterocyclic derivatives and methods of use thereof
TWI508965B (zh) 2008-12-23 2015-11-21 Boehringer Ingelheim Int 有機化合物的鹽形式
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
AR075204A1 (es) 2009-01-29 2011-03-16 Boehringer Ingelheim Int Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
US20110046076A1 (en) 2009-02-13 2011-02-24 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
NZ594044A (en) 2009-02-13 2014-08-29 Boehringer Ingelheim Int Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG Heterocylcic derivatives as inhibitors of glutaminyl cyclase
KR20190071840A (ko) 2009-11-27 2019-06-24 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
EP2547339A1 (en) 2010-03-18 2013-01-23 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
KR101455917B1 (ko) 2010-03-19 2014-11-03 화이자 인코포레이티드 2,3-디히드로-1h-인덴-1-일-2,7-디아자스피로[3.5]노난 유도체 및 그렐린 수용체의 길항제 또는 역 작용제로서의 그 용도
US20130023494A1 (en) 2010-04-06 2013-01-24 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
MX366325B (es) 2010-05-05 2019-07-05 Boehringer Ingelheim Int Terapia de combinacion.
CA2803504C (en) 2010-06-24 2022-08-30 Boehringer Ingelheim International Gmbh A combination for diabetes therapy comprising linagliptin and a long-acting insulin
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
CN104774205A (zh) 2010-10-29 2015-07-15 辉瑞大药厂 N1/n2-内酰胺乙酰辅酶a羧化酶抑制剂
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
UY33937A (es) 2011-03-07 2012-09-28 Boehringer Ingelheim Int Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
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
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
JP5657174B2 (ja) 2011-04-22 2015-01-21 ファイザー・インク アセチルＣｏＡカルボキシラーゼ阻害剤として使用するためのピラゾロスピロケトン誘導体
US20140051714A1 (en) 2011-04-22 2014-02-20 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
CA2841757A1 (en) 2011-07-15 2013-01-24 Etzer Darout Gpr 119 modulators
KR101985384B1 (ko) 2011-07-15 2019-06-03 베링거 인겔하임 인터내셔날 게엠베하 치환된 퀴나졸린, 이의 제조 및 약제학적 조성물에서의 이의 용도
BR112014000288A2 (pt) 2011-07-22 2017-01-10 Pfizer moduladores do receptor de glucagon de quinolinila
EP2751116B1 (en) 2011-08-31 2016-10-12 Pfizer Inc Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
BR112014011254A2 (pt) 2011-11-11 2017-05-16 Pfizer 2-tiopirimidinonas
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
SG11201405477XA (en) 2012-04-06 2014-11-27 Pfizer Diacylglycerol acyltransferase 2 inhibitors
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
WO2013164730A1 (en) 2012-05-04 2013-11-07 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.
JP6218811B2 (ja) 2012-05-14 2017-10-25 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 Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体
EP2849755A1 (en) 2012-05-14 2015-03-25 Boehringer Ingelheim International GmbH A xanthine derivative as dpp -4 inhibitor for use in the treatment of 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
CA2882389A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
WO2014091352A1 (en) 2012-12-11 2014-06-19 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
EP2935282A1 (en) 2012-12-19 2015-10-28 Pfizer Inc. CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS
JP2016507551A (ja) 2013-02-13 2016-03-10 ファイザー・インク ヘテロアリール置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2015019238A1 (en) * 2013-08-06 2015-02-12 Ranbaxy Laboratories Limited Process for the preparation of n-protected (5s)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-one
ES2665153T3 (es) 2013-10-09 2018-04-24 Pfizer Inc. Antagonistas del receptor EP3 de prostaglandina
ES2950384T3 (es) 2014-02-28 2023-10-09 Boehringer Ingelheim Int Uso médico de un inhibidor de DPP-4
TR201809388T4 (tr) 2014-03-17 2018-07-23 Pfizer Metabolik ve ilişkili hastalıkların tedavisinde kullanılmaya yönelik diasilgliserol asiltransferaz 2 inhibitörleri.
HUE044180T2 (hu) 2014-04-04 2019-10-28 Pfizer Biciklusos kondenzált heteroaril- vagy aril-vegyületek és ezek alkalmazása IRAK4 inhibitorokként
PE20170327A1 (es) 2014-04-10 2017-04-21 Pfizer 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS
WO2016092413A1 (en) 2014-12-10 2016-06-16 Pfizer Inc. Indole and indazole compounds that activate ampk
JP2017538769A (ja) 2014-12-22 2017-12-28 ファイザー・インク プロスタグランジンｅｐ３受容体の拮抗薬
BR112017022340A2 (pt) 2015-05-05 2018-07-10 Pfizer 2-tiopirimidinonas
JP2018516254A (ja) 2015-05-29 2018-06-21 ファイザー・インク バニン１酵素の阻害薬としての新規なヘテロ環化合物
UA125334C2 (uk) 2015-06-17 2022-02-23 Пфайзер Інк. Трициклічні сполуки та їх застосування як інгібіторів фосфодіестерази
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
JP2018527337A (ja) 2015-08-13 2018-09-20 ファイザー・インク 二環式縮合ヘテロアリールまたはアリール化合物
JP6804524B2 (ja) 2015-08-27 2020-12-23 ファイザー・インク Ｉｒａｋ４モジュレーターとしての二環式縮合ヘテロアリールまたはアリール化合物
WO2017037567A1 (en) 2015-09-03 2017-03-09 Pfizer Inc. Regulators of frataxin
EP3353182A1 (en) 2015-09-24 2018-08-01 Pfizer Inc Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
EP3353174A1 (en) 2015-09-24 2018-08-01 Pfizer Inc N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl]amides useful as bace inhibitors
EP3353183A1 (en) 2015-09-24 2018-08-01 Pfizer Inc N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides
CU24540B1 (es) 2015-12-29 2021-08-06 Pfizer 3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasa
BR112018072401A2 (pt) 2016-06-10 2019-02-19 Boehringer Ingelheim International Gmbh combinações de linagliptina e metformina
US10906888B2 (en) 2016-07-14 2021-02-02 Pfizer Inc. Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
WO2019133445A1 (en) 2017-12-28 2019-07-04 Inception Ibd, Inc. Aminothiazoles as inhibitors of vanin-1
CN112955147A (zh) 2018-08-31 2021-06-11 辉瑞公司 用于治疗nash/nafld和相关疾病的组合
WO2020102575A1 (en) 2018-11-16 2020-05-22 Inception Ibd, Inc. Heterocyclic aminothiazoles and uses thereof
WO2020234726A1 (en) 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases
TW202115086A (zh) 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑
WO2020261144A1 (en) 2019-06-28 2020-12-30 Pfizer Inc. 5-(thiophen-2-yl)-1h-tetrazole derivatives as bckdk inhibitors useful for treating various diseases
TWI771766B (zh) 2019-10-04 2022-07-21 美商輝瑞股份有限公司 二醯基甘油醯基轉移酶２ 抑制劑
JP2022058085A (ja) 2020-02-24 2022-04-11 ファイザー・インク ジアシルグリセロールアシルトランスフェラーゼ２阻害剤とアセチル－ＣｏＡカルボキシラーゼ阻害剤との組合せ
HRP20241177T1 (hr) 2020-06-09 2024-11-22 Pfizer Inc. Spiro-spojevi kao antagonisti melanokortinskog receptora 4 i njihova upotreba
WO2023026180A1 (en) 2021-08-26 2023-03-02 Pfizer Inc. Amorphous form of (s)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-n-(tetrahydrofuran-3- yl)pyrimidine-5-carboxamide
EP4441037A1 (en) 2021-12-01 2024-10-09 Pfizer Inc. 3-phenyl-1-benzothiophene-2-carboxylic acid derivatives as branched-chain alpha keto acid dehydrogenase kinase inhibitors for the treatment of diabetes, kidney diseases, nash and heart failure
US20250129048A1 (en) 2021-12-06 2025-04-24 Pfizer Inc. Melanocortin 4 receptor antagonists and uses thereof
WO2024075051A1 (en) 2022-10-07 2024-04-11 Pfizer Inc. Hsd17b13 inhibitors and/or degraders
AU2023364628A1 (en) 2022-10-18 2025-04-03 Pfizer Inc. Patatin-like phospholipase domain-containing protein 3 (pnpla3) modifiers
WO2024118524A1 (en) 2022-11-28 2024-06-06 Cerevel Therapeutics, Llc Azaindole compounds and their use as phosphodiesterase inhibitors
CN120731201A (zh) 2022-12-16 2025-09-30 辉瑞公司 含3-氟-4-羟基苯甲酰胺的抑制剂和/或降解剂及其用途
KR20250172881A (ko) 2023-04-14 2025-12-09 화이자 인코포레이티드 글루코스-의존성 인슐린 분비 촉진 폴리펩티드 수용체 길항제 및 이의 용도
WO2025099566A1 (en) 2023-11-08 2025-05-15 Pfizer Inc. A crystalline form of 6-fluoro-3-(2,4,5-trifluoro-3-methoxyphenyl)-1-benzothiophene-2-carboxylic acid
WO2025163561A1 (en) 2024-02-01 2025-08-07 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2025224599A1 (en) 2024-04-22 2025-10-30 Pfizer Inc. Pyrrolidine-based glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000250A1 (en) * 2001-06-25 2003-01-03 Ferring Bv 3-fluoro-pyrrolidines as antidiabetic agents
EP1308439A1 (en) * 2000-08-10 2003-05-07 Welfide Corporation Proline derivatives and use thereof as drugs
WO2005019168A2 (en) * 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3170059B2 (ja) 1992-08-25 2001-05-28 誠 大塚 リン酸カルシウム系薬物徐放体及びその製造方法
US6090786A (en) 1994-06-10 2000-07-18 Fondatech Benelux N.V. Serine proteases, their activity and their synthetic inhibitors
GB9903119D0 (en) 1999-02-11 1999-04-07 Merck Sharp & Dohme Therapeutic agents
US6960249B2 (en) 1999-07-14 2005-11-01 Calcitec, Inc. Tetracalcium phosphate (TTCP) having calcium phosphate whisker on surface
US7169373B2 (en) 1999-07-14 2007-01-30 Calcitec, Inc. Tetracalcium phosphate (TTCP) having calcium phosphate whisker on surface and process for preparing the same
US6840995B2 (en) 1999-07-14 2005-01-11 Calcitec, Inc. Process for producing fast-setting, bioresorbable calcium phosphate cements
US7094282B2 (en) 2000-07-13 2006-08-22 Calcitec, Inc. Calcium phosphate cement, use and preparation thereof
US7270705B2 (en) 1999-07-14 2007-09-18 Jiin-Huey Chern Lin Method of increasing working time of tetracalcium phosphate cement paste
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
JP4070951B2 (ja) 2000-12-07 2008-04-02 ペンタックス株式会社 多孔質リン酸カルシウム系セラミックス焼結体の製造方法
WO2002076450A1 (en) 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE60222667T2 (de) 2001-06-27 2008-07-17 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidylpeptidaseinhibitoren
US7183290B2 (en) 2001-06-27 2007-02-27 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US6616742B2 (en) 2001-08-30 2003-09-09 Cana Lab Corporation Process for preparing a paste from calcium phosphate cement
CN100341862C (zh) 2001-09-14 2007-10-10 三菱制药株式会社 噻唑烷衍生物及其医药用途
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
US7045105B2 (en) 2001-12-21 2006-05-16 Lagow Richard J Calcium phosphate bone replacement materials and methods of use thereof
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6955716B2 (en) 2002-03-01 2005-10-18 American Dental Association Foundation Self-hardening calcium phosphate materials with high resistance to fracture, controlled strength histories and tailored macropore formation rates
US20040137032A1 (en) 2002-03-15 2004-07-15 Wang Francis W. Combinations of calcium phosphates, bone growth factors, and pore-forming additives as osteoconductive and osteoinductive composite bone grafts
WO2003095425A1 (en) 2002-05-09 2003-11-20 Taisho Pharmaceutical Co.,Ltd. Cyanopyrrolidine derivatives
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
US20030216777A1 (en) 2002-05-16 2003-11-20 Yin-Chun Tien Method of enhancing healing of interfacial gap between bone and tendon or ligament
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
CA2487636A1 (en) 2002-06-04 2003-12-11 Janice Catherine Parker Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
AU2003248259A1 (en) 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
ES2242916T3 (es) 2002-07-11 2005-11-16 Biomet Deutschland Gmbh Metodos de preparacion de segmentos y granulos de fosfato de calcio poroso mediante procesamiento con gelatina.
TW200404796A (en) 2002-08-19 2004-04-01 Ono Pharmaceutical Co Nitrogen-containing compound
ATE350374T1 (de) 2002-11-07 2007-01-15 Merck & Co Inc Phenylalaninderivate als hemmer der dipeptidyl peptidase zur behandlung oder prävention von diabetes
MXPA05005260A (es) 2002-11-18 2005-07-25 Pfizer Prod Inc Amidas ciclicas fluoradas que inhiben la dipeptidil peptidasa iv.
JP2005170792A (ja) * 2002-11-22 2005-06-30 Mitsubishi Pharma Corp Ｌ−プロリン誘導体およびその医薬としての用途。
WO2004050022A2 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
US20040180091A1 (en) 2003-03-13 2004-09-16 Chang-Yi Lin Carbonated hydroxyapatite-based microspherical composites for biomedical uses
US7306610B2 (en) 2003-03-21 2007-12-11 Cana Lab Corporation Method and device for forming a hardened cement in a bone cavity
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
ATE463492T1 (de) 2003-06-06 2010-04-15 Merck Sharp & Dohme Kondensierte indole als dipeptidyl-peptidase- hemmer zur behandlung oder prävention von diabetes
EP1638950A4 (en) 2003-06-17 2010-06-30 Merck Sharp & Dohme CYCLOHEXYLGLYCIN DERIVATIVES AS DIPEPTIDYLPEPTIDASEINHIBITORS FOR THE TREATMENT OF BZW. PREVENTION OF DIABETES
EP1654226B1 (en) 2003-07-21 2008-10-22 SmithKline Beecham Corporation (2s,4s)-4-fluoro-1- 4-fluoro-beta-(4-fluorophenyl)-l-phenylalanyl -2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
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)
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
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
JP2005139107A (ja) 2003-11-05 2005-06-02 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼｉｖ阻害剤
WO2005046440A2 (en) 2003-11-07 2005-05-26 Calcitec, Inc. Spinal fusion procedure using an injectable bone substitute
PL1753748T3 (pl) 2004-05-12 2010-01-29 Pfizer Prod Inc Pochodne proliny i ich zastosowanie jako inhibitorów peptydazy dipeptylowej IV

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1308439A1 (en) * 2000-08-10 2003-05-07 Welfide Corporation Proline derivatives and use thereof as drugs
WO2003000250A1 (en) * 2001-06-25 2003-01-03 Ferring Bv 3-fluoro-pyrrolidines as antidiabetic agents
WO2005019168A2 (en) * 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors

Also Published As

Publication number Publication date
US20070161664A1 (en) 2007-07-12
TWI347322B (en) 2011-08-21
EP2116541B1 (en) 2015-02-25
US20060079498A1 (en) 2006-04-13
NL1029015A1 (nl) 2005-11-15
PL1753748T3 (pl) 2010-01-29
US20070099897A1 (en) 2007-05-03
JP2007537231A (ja) 2007-12-20
EP2116541A1 (en) 2009-11-11
KR20070009699A (ko) 2007-01-18
JP4227660B2 (ja) 2009-02-18
TW200536578A (en) 2005-11-16
EP1753748A1 (en) 2007-02-21
AU2005247684B2 (en) 2008-10-23
AP2320A (en) 2011-11-07
EA200601896A1 (ru) 2007-02-27
MXPA06013114A (es) 2007-02-28
DE602005015699D1 (de) 2009-09-10
US20050256310A1 (en) 2005-11-17
CR8744A (es) 2006-11-30
RS51106B (sr) 2010-10-31
EP1753748B1 (en) 2009-07-29
AR049894A1 (es) 2006-09-13
PA8632701A1 (es) 2006-06-02
HRP20090471T1 (hr) 2009-10-31
SV2006002110A (es) 2006-05-25
CY1109322T1 (el) 2014-07-02
NZ550229A (en) 2009-07-31
SI1753748T1 (sl) 2009-12-31
IL178339A (en) 2013-08-29
GEP20084421B (en) 2008-07-10
DK1753748T3 (da) 2009-10-05
AP2006003770A0 (en) 2006-10-31
MY139805A (en) 2009-10-30
CA2566108A1 (en) 2005-12-08
ECSP066985A (es) 2006-12-29
ATE437870T1 (de) 2009-08-15
BRPI0510284A (pt) 2007-10-30
ES2327857T3 (es) 2009-11-04
US7465732B2 (en) 2008-12-16
US7291618B2 (en) 2007-11-06
AU2005247684A1 (en) 2005-12-08
HK1106767A1 (en) 2008-03-20
PE20060316A1 (es) 2006-05-08
IL178339A0 (en) 2007-02-11
PT1753748E (pt) 2009-08-28
NO20064400L (no) 2006-10-25
NL1029015C2 (nl) 2006-05-16
UY28892A1 (es) 2005-12-30
KR100869616B1 (ko) 2008-11-21
WO2005116014A1 (en) 2005-12-08
CA2566108C (en) 2010-04-06
EA011086B1 (ru) 2008-12-30
MA28578B1 (fr) 2007-05-02

Similar Documents

Publication Publication Date Title
EA011086B9 (ru) Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv
TW200745067A (en) Novel compounds
GEP20094679B (en) Dipeptidyl peptidase inhibitors
GEP20125456B (en) Azetidines as mek inhibitors for the treatment of proliferative diseases
TW200612947A (en) Organic compounds
TW200634018A (en) Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and uses
TW200745084A (en) Novel compounds
UA89040C2 (ru) Замещенные глюкопиранозилом бензольные производные, лекарственное средство, которое содержит эти соединения
GEP20125564B (en) Pyrimidine derivatives as kinase inhibitors
TW200942527A (en) Pyridazine derivatives as factor XIa inhibitors
UA84878C2 (ru) Производные 2-пиридона как ингибиторы нейтрофилов эластазы, фармацевтическая композиция на их основе, способ их получения
MX2009004441A (es) Derivados de indazol utiles como inhibidores de las isoformas de higado.
TW200616978A (en) Quinazolinone derivatives as parp inhibitors
MX2008005398A (es) Derivados de 4-(3-amino-pirazol)-pirimidina para uso como inhibidores de tirosina cinasa en el tratamiento de cancer.
MX2009003157A (es) Pirazoliltienopiridinas terapeuticas.
SG154433A1 (en) Phthalazine derivatives as parp inhibitors
TW200611898A (en) Organic compounds
UA103181C2 (ru) Соединения, которые ингибируют дипептидилпептидазу-iv и фармацевтическая композиция, которая содержит их как активный агент
PT2383271E (pt) Aminoquinolonas como inibidores de gsk-3
TW200745004A (en) Novel compounds, their preparation and use
MX2012006805A (es) Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa.
GEP20146063B (en) Solid pharmaceutical composition
MX2011011764A (es) Compuestos de carboxamida y su uso como inhibidores de calpaina.
MX2010006108A (es) Inhibidores de estearoil-coa-desaturasa.
UA96759C2 (en) 2-ARYLINDOLE DERIVATIVES AS mPGES-I INHIBITORS

Legal Events

Date Code Title Description
TH4A Publication of the corrected specification to eurasian patent
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM TJ TM

QB4A Registration of a licence in a contracting state
ND4A Extension of term of a eurasian patent
QB4A Registration of a licence in a contracting state