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WO2002013798A3 - Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors - Google Patents

Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors Download PDF

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Publication number
WO2002013798A3
WO2002013798A3 PCT/IB2001/001428 IB0101428W WO0213798A3 WO 2002013798 A3 WO2002013798 A3 WO 2002013798A3 IB 0101428 W IB0101428 W IB 0101428W WO 0213798 A3 WO0213798 A3 WO 0213798A3
Authority
WO
WIPO (PCT)
Prior art keywords
insulin resistance
resistance syndrome
treatment
cgmp pde5
selective cgmp
Prior art date
Application number
PCT/IB2001/001428
Other languages
French (fr)
Other versions
WO2002013798A2 (en
Inventor
David Albert Fryburg
Earl Michael Gibbs
Nandan Parmanand Koppiker
Original Assignee
Pfizer Ltd
David Albert Fryburg
Earl Michael Gibbs
Nandan Parmanand Koppiker
Pfizer
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 GB0030649A external-priority patent/GB0030649D0/en
Priority claimed from GB0106468A external-priority patent/GB0106468D0/en
Priority claimed from GB0106465A external-priority patent/GB0106465D0/en
Priority claimed from GB0117134A external-priority patent/GB0117134D0/en
Priority to KR10-2003-7001961A priority Critical patent/KR20030023747A/en
Priority to JP2002518944A priority patent/JP2004506009A/en
Application filed by Pfizer Ltd, David Albert Fryburg, Earl Michael Gibbs, Nandan Parmanand Koppiker, Pfizer filed Critical Pfizer Ltd
Priority to IL15415801A priority patent/IL154158A0/en
Priority to AU2001276607A priority patent/AU2001276607A1/en
Priority to CA002419033A priority patent/CA2419033A1/en
Priority to HU0300725A priority patent/HUP0300725A3/en
Priority to EP01954266A priority patent/EP1307183A2/en
Publication of WO2002013798A2 publication Critical patent/WO2002013798A2/en
Publication of WO2002013798A3 publication Critical patent/WO2002013798A3/en

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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
    • A61K38/28—Insulins
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • 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
    • A61P5/48—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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Zoology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Use of a selective cGMP PDE5 inhibitor or a pharmaceutical composition thereof in the preparation of a medicament for the curative, palliative or prophylactic treatment of the insulin resistance syndrome wherein the insulin resistance syndrome means the concomitant existence in a subject of two or more of: dyslipidemia; hypertension; type 2 diabetes mellitus, impaired glucose tolerance (IGT) or a family history of diabetes; hyperuricaemia and/or gout; a pro-coagulant state; atherosclerosis; or truncal obesity wherein said use can occur alone or in combination with other agents to treat the insulin resistance syndrome or individual aspects of the insulin resistance syndrome.
PCT/IB2001/001428 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors WO2002013798A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
EP01954266A EP1307183A2 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors
HU0300725A HUP0300725A3 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors
CA002419033A CA2419033A1 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors
AU2001276607A AU2001276607A1 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective CGMP PDE5 inhibitors
JP2002518944A JP2004506009A (en) 2000-08-11 2001-08-06 Treatment of insulin resistance syndrome
KR10-2003-7001961A KR20030023747A (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome
IL15415801A IL154158A0 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
US22492800P 2000-08-11 2000-08-11
US60/224,928 2000-08-11
GB0030649.8 2000-12-15
GB0030649A GB0030649D0 (en) 2000-12-15 2000-12-15 Treatment of the insulin resistance syndrome
US26608301P 2001-02-02 2001-02-02
US60/266,083 2001-02-02
GB0106465A GB0106465D0 (en) 2001-03-15 2001-03-15 Treatment of the insulin resistance syndrome
GB0106465.8 2001-03-15
GB0106468.2 2001-03-15
GB0106468A GB0106468D0 (en) 2001-03-15 2001-03-15 Treatment of diabetes mellitus
GB0117134A GB0117134D0 (en) 2001-07-13 2001-07-13 Treatment of the insulin resistance syndrome
GB0117134.7 2001-07-13

Publications (2)

Publication Number Publication Date
WO2002013798A2 WO2002013798A2 (en) 2002-02-21
WO2002013798A3 true WO2002013798A3 (en) 2003-01-23

Family

ID=27546614

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2001/001428 WO2002013798A2 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors

Country Status (9)

Country Link
EP (1) EP1307183A2 (en)
JP (1) JP2004506009A (en)
KR (1) KR20030023747A (en)
CN (1) CN1446084A (en)
AU (1) AU2001276607A1 (en)
CA (1) CA2419033A1 (en)
HU (1) HUP0300725A3 (en)
IL (1) IL154158A0 (en)
WO (1) WO2002013798A2 (en)

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BR0206847A (en) * 2001-02-02 2004-02-25 Pfizer Diabetes Mellitus Treatment
JP4142356B2 (en) 2001-07-05 2008-09-03 オイクロ ヨーロピアン コントラクト リサーチ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディト ゲゼルシャフト PP2C substrate
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US20030114469A1 (en) * 2001-09-27 2003-06-19 Cohen David Saul Combinations
US7019010B2 (en) 2001-09-27 2006-03-28 Novertis Ag Combinations
PL370599A1 (en) 2001-11-02 2005-05-30 Pfizer Products Inc. Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors
US20030181461A1 (en) * 2002-01-25 2003-09-25 Lautt Wilfred Wayne Use of phosphodiesterase antagonists to treat insulin resistance
JP2005519927A (en) * 2002-02-07 2005-07-07 ファイザー・インク Use of a PDE5 inhibitor such as sildenafil in the treatment of polycystic ovary syndrome
JP2004018524A (en) * 2002-06-13 2004-01-22 Eucro European Contract Research Gmbh & Co Kg Method for treating arteriosclerosis
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JP2006520777A (en) * 2003-03-17 2006-09-14 ファイザー・プロダクツ・インク Treatment of type 1 diabetes with PDE5 inhibitors
UA80871C2 (en) * 2003-04-29 2007-11-12 Pfizer Ltd 5,7-diaminopyrazolo[4,3-d]pyrimidines useful in the treatment of hypertension
MXPA05011643A (en) 2003-04-29 2005-12-15 Pfizer Ltd 5,7-diaminopyrazolo`4,3-d!pyrimidines useful in the treatment of hypertension.
CA2537230A1 (en) 2003-09-05 2005-03-17 Altana Pharma Ag Use of pde4 inhibitors for the treatment of diabetes mellitus
US7572799B2 (en) 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
WO2005097799A1 (en) 2004-04-07 2005-10-20 Pfizer Limited Pyrazolo`4,3-d! pyrimidines
CA2599376C (en) 2005-03-08 2014-05-13 Nycomed Gmbh Roflumilast for the treatment of diabetes mellitus
EP1909793A2 (en) * 2005-07-15 2008-04-16 Proxomed Medizintechnik GmbH Use of phosphodiesterase type 5 inhibitors for the prevention and treatment of diseases or health disorders and dispensing system for said inhibitors
US20100179131A1 (en) 2006-09-07 2010-07-15 Nycomed Gmbh Combination treatment for diabetes mellitus
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AT512084A1 (en) 2011-10-20 2013-05-15 Univ Wien Tech DIAZABICYCLO AND DIAZASPIRO ALKAN DERIVATIVES AS PHOSPHODIESTERASE-5 INHIBITORS
US20130315891A1 (en) 2012-05-25 2013-11-28 Matthew Charles Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
PT2854841T (en) 2012-06-04 2017-05-15 Diamedica Inc Human tissue kallikrein 1 glycosylation isoforms
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EP2803362B1 (en) * 2013-05-14 2017-07-26 SciMar Ltd. Hepatic insulin sensitizing substance and test meal for insulin sensitization
KR20160094956A (en) 2013-11-05 2016-08-10 벤-구리온 유니버시티 오브 더 네게브 리서치 앤드 디벨럽먼트 어쏘러티 Compounds for the treatment of diabetes and disease complications arising from same
WO2018165551A1 (en) 2017-03-09 2018-09-13 Diamedica Inc. Dosage forms of tissue kallikrein 1
MX2017016930A (en) * 2017-12-19 2019-06-20 Malesil Research & Tech Llc Method of treatment of diabetic foot ulcers.
KR102068299B1 (en) * 2018-12-21 2020-01-20 한국기초과학지원연구원 A pharmaceutical composition for prevention or treatment of metabolic disease comprising CYP4A inhibitor

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CN1446084A (en) 2003-10-01
EP1307183A2 (en) 2003-05-07
KR20030023747A (en) 2003-03-19
HUP0300725A2 (en) 2003-11-28
JP2004506009A (en) 2004-02-26
CA2419033A1 (en) 2002-02-21
AU2001276607A1 (en) 2002-02-25
IL154158A0 (en) 2003-07-31
HUP0300725A3 (en) 2005-11-28
WO2002013798A2 (en) 2002-02-21

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