WO2001062266A3 - Inhibition de la degenerescence des cellules beta - Google Patents

Inhibition de la degenerescence des cellules beta Download PDF

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Publication number
WO2001062266A3
WO2001062266A3 PCT/DK2001/000115 DK0100115W WO0162266A3 WO 2001062266 A3 WO2001062266 A3 WO 2001062266A3 DK 0100115 W DK0100115 W DK 0100115W WO 0162266 A3 WO0162266 A3 WO 0162266A3
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WO
WIPO (PCT)
Prior art keywords
diabetes
dpp
relates
inhibitors
treatment
Prior art date
Application number
PCT/DK2001/000115
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English (en)
Other versions
WO2001062266A2 (fr
Inventor
Richard David Carr
Original Assignee
Novo Nordisk As
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
Priority claimed from PCT/DK2001/000045 external-priority patent/WO2001055105A1/fr
Application filed by Novo Nordisk As filed Critical Novo Nordisk As
Priority to JP2001561331A priority Critical patent/JP2003523396A/ja
Priority to AU2001233622A priority patent/AU2001233622A1/en
Priority to EP01905634A priority patent/EP1259246A2/fr
Publication of WO2001062266A2 publication Critical patent/WO2001062266A2/fr
Publication of WO2001062266A3 publication Critical patent/WO2001062266A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/27—Growth hormone [GH], i.e. somatotropin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/2257—Prolactin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/25—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un procédé pour empêcher la dégénérescence des cellules bêta, par exemple, la nécrose ou l'apoptose des cellules bêta chez un sujet; le procédé consiste à administrer à l'individu un inhibiteur de DPP-IV. L'invention concerne en outre un procédé pour augmenter le nombre et/ou la taille des cellules bêta. Elle se rapporte également à un procédé pour freiner la progression de l'intolérance au glucose vers le diabète de type 2 ainsi qu'un procédé pour retarder la progression du diabète de type 2 non insulino-dépendant vers le diabète de type 2 insulino-dépendant.
PCT/DK2001/000115 2000-02-25 2001-02-20 Inhibition de la degenerescence des cellules beta WO2001062266A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2001561331A JP2003523396A (ja) 2000-02-25 2001-02-20 ベータ細胞変性の抑制
AU2001233622A AU2001233622A1 (en) 2000-02-25 2001-02-20 Inhibition of beta cell degeneration
EP01905634A EP1259246A2 (fr) 2000-02-25 2001-02-20 Inhibition de la degenerescence des cellules beta

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DKPA200000295 2000-02-25
DKPA200000295 2000-02-25
DKPA200000983 2000-06-23
DKPA200000983 2000-06-23
DKPCT/DK01/00045 2001-01-22
PCT/DK2001/000045 WO2001055105A1 (fr) 2000-01-24 2001-01-22 2-cyanopyroles et -pyrrolines a substitution n inhibant l'enzyme dpp-iv

Publications (2)

Publication Number Publication Date
WO2001062266A2 WO2001062266A2 (fr) 2001-08-30
WO2001062266A3 true WO2001062266A3 (fr) 2002-05-02

Family

ID=27222185

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2001/000115 WO2001062266A2 (fr) 2000-02-25 2001-02-20 Inhibition de la degenerescence des cellules beta

Country Status (4)

Country Link
EP (1) EP1259246A2 (fr)
JP (1) JP2003523396A (fr)
AU (1) AU2001233622A1 (fr)
WO (1) WO2001062266A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
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
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors

Families Citing this family (32)

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DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19926233C1 (de) 1999-06-10 2000-10-19 Probiodrug Ges Fuer Arzneim Verfahren zur Herstellung von Thiazolidin
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
KR20080067009A (ko) 2000-03-31 2008-07-17 프로시디온 리미티드 디펩티딜 펩티다제 ⅳ 효소 활성 억제제를 포함하는약제학적 조성물
US7132104B1 (en) 2000-10-27 2006-11-07 Probiodrug Ag Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders
US6890905B2 (en) 2001-04-02 2005-05-10 Prosidion Limited Methods for improving islet signaling in diabetes mellitus and for its prevention
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
JP4357293B2 (ja) 2001-06-27 2009-11-04 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
WO2003002531A2 (fr) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines inhibitrices de la dipeptidyl peptidase
DE60223920T2 (de) 2001-06-27 2008-11-13 Smithkline Beecham Corp. Pyrrolidine als dipeptidyl-peptidase-inhibitoren
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
WO2003057144A2 (fr) * 2001-12-26 2003-07-17 Guilford Pharmaceuticals Changement d'inhibiteurs de la dipeptidyl peptidase iv
ES2278944T3 (es) 2002-02-28 2007-08-16 Prosidion Ltd. Inhibidores de dpiv basados en glutaminilo.
JPWO2004007446A1 (ja) * 2002-07-10 2005-11-10 アステラス製薬株式会社 新規なアゼチジン誘導体又はその塩
US20060039974A1 (en) 2002-09-11 2006-02-23 Takeda Pharmaceutical Company Limited Sustained release preparation
DE10314610A1 (de) 2003-04-01 2004-11-04 Aventis Pharma Deutschland Gmbh Neues Diphenylazetidinon mit verbesserten physiologischen Eigenschaften, Verfahren zu dessen Herstellung, diese Verbindungen enthaltende Arzneimittel und dessen Verwendung
DE202004021723U1 (de) 2003-05-05 2010-07-15 Probiodrug Ag Medizinische Verwendung von Hemmern von Glutaminyl- und Glutamatcyclasen
MXPA05013734A (es) 2003-06-20 2006-03-08 Hoffmann La Roche Hexahidropiroisoquinolinas como inhibidores de dpp-iv.
SI1638970T1 (sl) 2003-06-20 2011-03-31 Hoffmann La Roche Derivati pirid (2, 1-a)-izokinolina kot inhibitorji dpp-iv
JP5707014B2 (ja) 2003-10-15 2015-04-22 プロビオドルグ エージー グルタミニル、及びグルタミン酸シクラーゼのエフェクターの使用
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
JP4854511B2 (ja) * 2004-08-26 2012-01-18 武田薬品工業株式会社 糖尿病治療剤
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
WO2007112347A1 (fr) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Inhibiteurs de la dipeptidyl peptidase
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
ATE550319T1 (de) 2007-03-22 2012-04-15 Kyorin Seiyaku Kk Verfahren zur herstellung eines aminoacetylpyrrolidincarbonitrilderivats
DE102007054497B3 (de) 2007-11-13 2009-07-23 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993010127A1 (fr) * 1991-11-22 1993-05-27 Boehringer Ingelheim Pharmaceuticals, Inc. Procede de production d'un ester de prolineboronate
WO1995015309A1 (fr) * 1993-12-03 1995-06-08 Ferring B.V. Inhibiteurs de la dp-iv-serine protease
WO1995029691A1 (fr) * 1994-04-28 1995-11-09 Georgia Tech Research Corporation Derives de la proline phosphonate
WO1997040832A1 (fr) * 1996-04-25 1997-11-06 Probiodrug Gesellschaft für Arzneimittelforschung mbH Utilisation d'effecteurs de la dipeptidyl peptidase iv pour abaisser la teneur en glucose dans le sang chez les mammiferes
WO1998019998A2 (fr) * 1996-11-07 1998-05-14 Novartis Ag 2-cyanopyrrolidines a substitution n
WO1999038501A2 (fr) * 1998-02-02 1999-08-05 Trustees Of Tufts College Procede de regulation du metabolisme du glucose et reactifs afferents
DE29909210U1 (de) * 1998-05-28 1999-09-09 Probiodrug Ges Fuer Arzneim Neue Effektoren von Dipeptidylpeptidase IV
WO1999046272A1 (fr) * 1998-03-09 1999-09-16 Fondatech Benelux N.V. Modulateurs de la serine peptidase
WO1999067278A1 (fr) * 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Promedicaments d'inhibiteurs de la dipeptidylpeptidase iv
WO1999067279A1 (fr) * 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Composes d'inhibiteurs instables de la dipeptidylpeptidase iv

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993010127A1 (fr) * 1991-11-22 1993-05-27 Boehringer Ingelheim Pharmaceuticals, Inc. Procede de production d'un ester de prolineboronate
WO1995015309A1 (fr) * 1993-12-03 1995-06-08 Ferring B.V. Inhibiteurs de la dp-iv-serine protease
WO1995029691A1 (fr) * 1994-04-28 1995-11-09 Georgia Tech Research Corporation Derives de la proline phosphonate
WO1997040832A1 (fr) * 1996-04-25 1997-11-06 Probiodrug Gesellschaft für Arzneimittelforschung mbH Utilisation d'effecteurs de la dipeptidyl peptidase iv pour abaisser la teneur en glucose dans le sang chez les mammiferes
WO1998019998A2 (fr) * 1996-11-07 1998-05-14 Novartis Ag 2-cyanopyrrolidines a substitution n
WO1999038501A2 (fr) * 1998-02-02 1999-08-05 Trustees Of Tufts College Procede de regulation du metabolisme du glucose et reactifs afferents
WO1999046272A1 (fr) * 1998-03-09 1999-09-16 Fondatech Benelux N.V. Modulateurs de la serine peptidase
DE29909210U1 (de) * 1998-05-28 1999-09-09 Probiodrug Ges Fuer Arzneim Neue Effektoren von Dipeptidylpeptidase IV
DE29909208U1 (de) * 1998-05-28 1999-09-09 Probiodrug Ges Fuer Arzneim Neue Effektoren von Dipeptidylpeptidase IV
DE29909211U1 (de) * 1998-05-28 1999-09-23 Probiodrug Ges Fuer Arzneim Neue Effektoren von Dipeptidylpeptidase IV
WO1999067278A1 (fr) * 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Promedicaments d'inhibiteurs de la dipeptidylpeptidase iv
WO1999067279A1 (fr) * 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Composes d'inhibiteurs instables de la dipeptidylpeptidase iv

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
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
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors

Also Published As

Publication number Publication date
WO2001062266A2 (fr) 2001-08-30
JP2003523396A (ja) 2003-08-05
AU2001233622A1 (en) 2001-09-03
EP1259246A2 (fr) 2002-11-27

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