WO2003022871A3 - Nouveaux inhibiteurs de dipeptidylpeptidase i - Google Patents

Nouveaux inhibiteurs de dipeptidylpeptidase i Download PDF

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Publication number
WO2003022871A3
WO2003022871A3 PCT/EP2002/010020 EP0210020W WO03022871A3 WO 2003022871 A3 WO2003022871 A3 WO 2003022871A3 EP 0210020 W EP0210020 W EP 0210020W WO 03022871 A3 WO03022871 A3 WO 03022871A3
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WO
WIPO (PCT)
Prior art keywords
unbranched
branched
chain
heteroaryl
amino acid
Prior art date
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PCT/EP2002/010020
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English (en)
Other versions
WO2003022871A2 (fr
Inventor
Hans-Ulrich Demuth
Ulrich Heiser
Andre Niestroj
Original Assignee
Probiodrug Ag
Hans-Ulrich Demuth
Ulrich Heiser
Andre Niestroj
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Probiodrug Ag, Hans-Ulrich Demuth, Ulrich Heiser, Andre Niestroj filed Critical Probiodrug Ag
Priority to EP02779316A priority Critical patent/EP1423410A2/fr
Priority to JP2003526944A priority patent/JP2005511505A/ja
Priority to AU2002342657A priority patent/AU2002342657A1/en
Publication of WO2003022871A2 publication Critical patent/WO2003022871A2/fr
Publication of WO2003022871A3 publication Critical patent/WO2003022871A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne de nouveaux composés qui agissent en tant qu'inhibiteurs spécifiques de la cystéine protéase dipeptidylpeptidase I (DP I), lesquels sont représentés par la formule générale (I), ainsi que des sels pharmaceutiquement acceptables de ceux-ci. Dans cette formule générale (I), R représente un résidu d'acyle comprenant un uréthanne et un peptide, ou une chaîne alkyle C1-C9 ramifiée ou non ramifiée, une chaîne alcényle C2-C9 ramifiée ou non ramifiée, une chaîne alcynyle C2-C9 ramifiée ou non ramifiée, un cycloalkyle C3-C9, un carbocycle C4-C9, un aryle C5-C14, un hétéroaryle C3-C9, un hétérocycle C3-C9, tous les résidus susmentionnnés pouvant être éventuellement substitués, ou représente H, AS représentant un acide aminé ou un peptide mimétique de celui-ci. Cet acide aminé possède une liaison peptidique avec R, et R' représente une chaîne alkyle C1-C9 ramifiée ou non ramifiée, une chaîne alcényle C2-C9 ramifiée ou non ramifiée, une chaîne alcynyle C2-C9 ramifiée ou non ramifiée, un cycloalkyle C3-C9, un cycloalcényle C4-C9, un hétérocycloalkyle C2-C9, un hétérocycloalcényle C3-C9, un aryle C5-C14, un hétéroaryle C3-C9, un hétérocycle C3-C9, le résidu hétérocylcoalkyle, hétérocycloalcényle, hétéroaryle, hétérocylcique pouvant posséder jusqu'à 6 hétéroatomes sur le cycle, un acide aminé ou un peptide mimétique de celui-ci, touts les résidus susmentionnés pouvant être éventuellement substitués, ou représente H.
PCT/EP2002/010020 2001-09-06 2002-09-06 Nouveaux inhibiteurs de dipeptidylpeptidase i WO2003022871A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP02779316A EP1423410A2 (fr) 2001-09-06 2002-09-06 Inhibiteurs de dipeptidylpeptidase i renfermant un group hydroxylamino c-terminal
JP2003526944A JP2005511505A (ja) 2001-09-06 2002-09-06 ジペプチジルペプチダーゼｉの新規な阻害剤
AU2002342657A AU2002342657A1 (en) 2001-09-06 2002-09-06 Peptides having a c- terminal hydroxylamino group as inhibitors of dipeptidyl peptidase i

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10143840.0 2001-09-06
DE10143840A DE10143840A1 (de) 2001-09-06 2001-09-06 Neue Inhibitoren der Dipeptidylpeptidase I

Publications (2)

Publication Number Publication Date
WO2003022871A2 WO2003022871A2 (fr) 2003-03-20
WO2003022871A3 true WO2003022871A3 (fr) 2003-11-13

Family

ID=7698010

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/010020 WO2003022871A2 (fr) 2001-09-06 2002-09-06 Nouveaux inhibiteurs de dipeptidylpeptidase i

Country Status (5)

Country Link
EP (1) EP1423410A2 (fr)
JP (1) JP2005511505A (fr)
AU (1) AU2002342657A1 (fr)
DE (1) DE10143840A1 (fr)
WO (1) WO2003022871A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues

Families Citing this family (34)

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Publication number Priority date Publication date Assignee Title
US20040242566A1 (en) 2003-03-25 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
ATE399763T1 (de) 2003-05-30 2008-07-15 Prozymex As Proteasehemmer
CN1867560A (zh) 2003-08-13 2006-11-22 武田药品工株式会社 4－嘧啶酮衍生物及其作为肽基肽酶抑制剂的用途
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
EP1699777B1 (fr) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Inhibiteurs de la dipeptidylpeptidase
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN102127053A (zh) 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
US20070286854A1 (en) * 2004-04-28 2007-12-13 Bayer Healthcare Ag Diagnostics And Therapeutics For Diseases Associated With Dipeptidyl-Peptidase 1 (Dpp1)
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006019965A2 (fr) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Inhibiteurs de la dipeptidyl peptidase
EP2805953B1 (fr) 2004-12-21 2016-03-09 Takeda Pharmaceutical Company Limited Inhibiteurs de peptidase dipeptidyl
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
ME02005B (fr) 2005-09-14 2012-08-31 Takeda Pharmaceuticals Co Inhibiteurs de la dipeptidyl peptidase permettant de traiter le diabete
CA2622642C (fr) 2005-09-16 2013-12-31 Takeda Pharmaceutical Company Limited Inhibiteurs de dipeptidylpeptidase
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
ES2354390T3 (es) 2006-04-11 2011-03-14 Arena Pharmaceuticals, Inc. Procedimientos de uso del receptor gpr119 para identificar compuestos útiles para aumentar la masa ósea en un individuo.
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
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
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
CN102918027A (zh) 2010-04-06 2013-02-06 艾尼纳制药公司 Gpr119受体调节剂和对与所述受体有关的障碍的治疗
AU2011305525B2 (en) 2010-09-22 2016-08-18 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145361A1 (fr) 2011-04-19 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
US20140051714A1 (en) 2011-04-22 2014-02-20 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
JP2018507914A (ja) 2015-03-09 2018-03-22 インテクリン・セラピューティクス・インコーポレイテッド 非アルコール性脂肪肝疾患および／またはリポジストロフィーの処置のための方法
JP2020515639A (ja) 2017-04-03 2020-05-28 コヒラス・バイオサイエンシズ・インコーポレイテッド 進行性核上性麻痺の処置のためのＰＰＡＲγアゴニスト
CN113292465B (zh) * 2021-06-17 2022-11-08 贵州医科大学 一种半胱氨酸衍生物及其合成方法、应用

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Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO1998022494A2 (fr) * 1996-11-22 1998-05-28 Elan Pharmaceuticals, Inc. METHODES ET COMPOSES DESTINES A INHIBER LA LIBERATION ET/OU LA SYNTHESE DU PEPTIDE β-AMYLOIDE
EP0995756A2 (fr) * 1998-07-31 2000-04-26 Probiodrug Gesellschaft für Arzneimittelforschung mbH Inhibiteurs orientés a méchanisme du peptidase dipeptidique I

Non-Patent Citations (6)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues

Also Published As

Publication number Publication date
WO2003022871A2 (fr) 2003-03-20
JP2005511505A (ja) 2005-04-28
AU2002342657A1 (en) 2003-03-24
EP1423410A2 (fr) 2004-06-02
DE10143840A1 (de) 2003-03-27

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