CA2487636A1 - Amides cycliques fluores utilises comme inhibiteurs de la dipeptidyl peptidase iv - Google Patents

Amides cycliques fluores utilises comme inhibiteurs de la dipeptidyl peptidase iv Download PDF

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Publication number
CA2487636A1
CA2487636A1 CA002487636A CA2487636A CA2487636A1 CA 2487636 A1 CA2487636 A1 CA 2487636A1 CA 002487636 A CA002487636 A CA 002487636A CA 2487636 A CA2487636 A CA 2487636A CA 2487636 A1 CA2487636 A1 CA 2487636A1
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compound
amino
hydrochloride
syndrome
methyl
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CA002487636A
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Janice Catherine Parker
Bernard Hulin
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Pfizer Products Inc
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/08Heterocyclic 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
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    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/38Halogen atoms or nitro radicals

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

L'invention de nouveaux inhibiteurs thérapeutiquement actifs et sélectifs de l'enzyme dipeptidyl peptidase-IV (DPP-IV), des compositions pharmaceutiques comprenant les composés et l'utilisation de ces composés pour traiter des maladies associées à des protéines soumises à un traitement par la DPP-IV, telles que le diabète sucré de type 2, l'hyperglycémie, la tolérance au glucose altérée, un syndrome métabolique (syndrome X ou syndrome de résistance à l'insuline), la glycosurie, l'acidose métabolique, la cataracte, la neuropathie diabétique, la néphropathie diabétique, la rétinopathie diabétique, la cardiomyopathie diabétique, le diabète de type 1, l'obésité, les états exacerbés par l'obésité, l'hypertension, l'hyperlipidémie, l'athérosclérose, l'ostéoporose, l'ostéopénie, la fragilité, la perte osseuse, les fractures osseuses, le syndrome coronaire aiguë, l'infertilité due au syndrome polycystique ovarien, le syndrome de l'intestin court, l'anxiété, la dépression, l'insomnie, la fatigue chronique, l'épilepsie, les troubles de l'alimentation, les douleurs chroniques, l'addiction à l'alcool, les maladies associées à la motilité intestinale, les ulcères, le syndrome de l'intestin irritable, le syndrome de l'intestin inflammatoire; et pour prévenir l'évolution d'une maladie dans le diabète de type 2. L'invention concerne également une méthode permettant d'identifier un agent sécrétagogue de l'insuline dans le diabète.
CA002487636A 2002-06-04 2003-05-23 Amides cycliques fluores utilises comme inhibiteurs de la dipeptidyl peptidase iv Abandoned CA2487636A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US38615702P 2002-06-04 2002-06-04
US60/386,157 2002-06-04
PCT/IB2003/002257 WO2003101958A2 (fr) 2002-06-04 2003-05-23 Amides cycliques fluores utilises comme inhibiteurs de la dipeptidyl peptidase iv

Publications (1)

Publication Number Publication Date
CA2487636A1 true CA2487636A1 (fr) 2003-12-11

Family

ID=29712235

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002487636A Abandoned CA2487636A1 (fr) 2002-06-04 2003-05-23 Amides cycliques fluores utilises comme inhibiteurs de la dipeptidyl peptidase iv

Country Status (7)

Country Link
EP (1) EP1513808A2 (fr)
JP (1) JP2005533771A (fr)
AU (1) AU2003232405A1 (fr)
BR (1) BR0311608A (fr)
CA (1) CA2487636A1 (fr)
MX (1) MXPA04011958A (fr)
WO (1) WO2003101958A2 (fr)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200508439B (en) 2003-05-05 2007-03-28 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
AP2320A (en) 2004-05-12 2011-11-07 Pfizer Procucts Inc Proline derivatives and their use as dipeptidyl peptidase IV inhibitors.
JPWO2006057152A1 (ja) * 2004-11-08 2008-06-05 小野薬品工業株式会社 タンパク質分解酵素阻害化合物からなる糖尿病治療剤
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
DE602006017997D1 (de) * 2005-04-26 2010-12-16 Mitsubishi Tanabe Pharma Corp Prophylaktisches/therapeutisches mittel für abweichungen im fettstoffwechsel
US20070060530A1 (en) 2005-09-14 2007-03-15 Christopher Ronald J Administration of dipeptidyl peptidase inhibitors
CN102675221A (zh) 2005-09-16 2012-09-19 武田药品工业株式会社 用于制备嘧啶二酮衍生物的方法中的中间体
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
WO2007112347A1 (fr) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Inhibiteurs de la dipeptidyl peptidase
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
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
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
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
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
ES2533484T3 (es) 2007-04-18 2015-04-10 Probiodrug Ag Derivados de tiourea como inhibidores de la glutaminil ciclasa
EP2146210A1 (fr) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Procédés d'utilisation du récepteur couplé aux protéines A G pour identifier les secrétagogues de peptide YY (PYY) et composés utiles dans le traitement d'états modulés par PYY
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
DK2475428T3 (en) 2009-09-11 2015-09-28 Probiodrug Ag Heterocyclic derivatives as glutaminylcyklaseinhibitorer
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
BR112012022478B1 (pt) 2010-03-10 2021-09-21 Probiodrug Ag Inibidores heterocíclicos de glutaminil ciclase (qc, ec 2.3.2.5), seu processo de preparação, e composição farmacêutica
EP2556056A1 (fr) 2010-04-06 2013-02-13 Arena Pharmaceuticals, Inc. Modulateurs du récepteur de gpr119 et traitement de troubles associés
EP2560953B1 (fr) 2010-04-21 2016-01-06 Probiodrug AG Inhibiteurs de glutaminyl cyclase
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
DK2686313T3 (en) 2011-03-16 2016-05-02 Probiodrug Ag Benzimidazole derivatives as inhibitors of glutaminyl cyclase
WO2012135570A1 (fr) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulateurs du récepteur gpr119 et traitement de troubles qui lui sont associés
WO2012145361A1 (fr) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulateurs du récepteur gpr119 et traitement de troubles liés à celui-ci
WO2012145604A1 (fr) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulateurs du récepteur gpr119 et traitement de troubles liés à celui-ci
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (fr) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulateurs du récepteur gpr119 et traitement de troubles associés à celui-ci
WO2013055910A1 (fr) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulateurs du récepteur gpr119 et traitement de troubles associés
WO2014074668A1 (fr) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulateurs de gpr119 et traitement de troubles associés à ceux-ci
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
EA201791982A1 (ru) 2015-03-09 2020-02-17 Интекрин Терапьютикс, Инк. Способы лечения неалкогольной жировой болезни печени и/или липодистрофии
MX2019011867A (es) 2017-04-03 2020-01-09 Coherus Biosciences Inc Agonista de ppary para el tratamiento de la paralisis supranuclear progresiva.
GB201714745D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
GB201714734D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
GB201714736D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
GB201714740D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
CN107892663B (zh) * 2017-12-04 2019-08-13 武汉药明康德新药开发有限公司 一种3,3,4,4-四氟吡咯烷的合成方法
GB201903832D0 (en) * 2019-03-20 2019-05-01 Atrogi Ab New compounds and methods

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US6090786A (en) * 1994-06-10 2000-07-18 Fondatech Benelux N.V. Serine proteases, their activity and their synthetic inhibitors
TWI243162B (en) * 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives

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Publication number Publication date
JP2005533771A (ja) 2005-11-10
AU2003232405A8 (en) 2003-12-19
WO2003101958A2 (fr) 2003-12-11
EP1513808A2 (fr) 2005-03-16
MXPA04011958A (es) 2005-03-31
WO2003101958A3 (fr) 2004-04-22
BR0311608A (pt) 2005-02-22
AU2003232405A1 (en) 2003-12-19

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