CA2419033A1 - 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
CA2419033A1
CA2419033A1 CA002419033A CA2419033A CA2419033A1 CA 2419033 A1 CA2419033 A1 CA 2419033A1 CA 002419033 A CA002419033 A CA 002419033A CA 2419033 A CA2419033 A CA 2419033A CA 2419033 A1 CA2419033 A1 CA 2419033A1
Authority
CA
Canada
Prior art keywords
ethyl
dihydro
pyrazolo
pyrimidin
sildenafil
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002419033A
Other languages
English (en)
French (fr)
Inventor
Earl Michael Gibbs
David Albert Fryburg
Nandan Parmanand Koppiker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Ltd
Original Assignee
Individual
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 GB0106465A external-priority patent/GB0106465D0/en
Priority claimed from GB0106468A external-priority patent/GB0106468D0/en
Priority claimed from GB0117134A external-priority patent/GB0117134D0/en
Application filed by Individual filed Critical Individual
Publication of CA2419033A1 publication Critical patent/CA2419033A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
CA002419033A 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors Abandoned CA2419033A1 (en)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US22492800P 2000-08-11 2000-08-11
US60/224,928 2000-08-11
GB0030649A GB0030649D0 (en) 2000-12-15 2000-12-15 Treatment of the insulin resistance syndrome
GB0030649.8 2000-12-15
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
GB0106468A GB0106468D0 (en) 2001-03-15 2001-03-15 Treatment of diabetes mellitus
GB0106468.2 2001-03-15
GB0117134A GB0117134D0 (en) 2001-07-13 2001-07-13 Treatment of the insulin resistance syndrome
GB0117134.7 2001-07-13
PCT/IB2001/001428 WO2002013798A2 (en) 2000-08-11 2001-08-06 Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors

Publications (1)

Publication Number Publication Date
CA2419033A1 true CA2419033A1 (en) 2002-02-21

Family

ID=27546614

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002419033A Abandoned CA2419033A1 (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 (ko)
JP (1) JP2004506009A (ko)
KR (1) KR20030023747A (ko)
CN (1) CN1446084A (ko)
AU (1) AU2001276607A1 (ko)
CA (1) CA2419033A1 (ko)
HU (1) HUP0300725A3 (ko)
IL (1) IL154158A0 (ko)
WO (1) WO2002013798A2 (ko)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2436576A1 (en) * 2001-02-02 2002-08-08 Pfizer Inc. Treatment of diabetes mellitus using vardenafil
US6933127B2 (en) 2001-07-05 2005-08-23 Eucro European Contract Research Gmbh & Co. Kg Substrate for PP2C
DE10135815A1 (de) * 2001-07-23 2003-02-06 Bayer Ag Verwendung von 2-Alkoxyphenyl-substituierten Imidazotriazinonen
US7019010B2 (en) 2001-09-27 2006-03-28 Novertis Ag Combinations
US20030114469A1 (en) * 2001-09-27 2003-06-19 Cohen David Saul Combinations
IL161155A0 (en) * 2001-11-02 2004-08-31 Pfizer Prod 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
AU2003205926A1 (en) * 2002-02-07 2003-09-02 Pfizer Limited Use of pde5 inhibitors such as sildenafil in the treatment of polycystic ovary syndrome
JP2004018524A (ja) * 2002-06-13 2004-01-22 Eucro European Contract Research Gmbh & Co Kg 動脈硬化症を処置するための方法
GB0214784D0 (en) * 2002-06-26 2002-08-07 Pfizer Ltd Novel combination
WO2004082667A1 (en) * 2003-03-17 2004-09-30 Pfizer Products Inc. Treatment of type 1 diabetes with pde5 inhibitors
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
CN100439371C (zh) * 2003-04-29 2008-12-03 辉瑞大药厂 可用于治疗高血压的5,7-二氨基吡唑并[4,3-d]嘧啶
JP2007504201A (ja) 2003-09-05 2007-03-01 アルタナ　ファルマ　アクチエンゲゼルシャフト 真性糖尿病の治療のためのｐｄｅ４阻害剤の使用
US7572799B2 (en) 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
US7569572B2 (en) 2004-04-07 2009-08-04 Pfizer Inc Pyrazolo[4,3-D]pyrimidines
WO2006094933A1 (en) 2005-03-08 2006-09-14 Nycomed Gmbh Roflumilast for the treatment of diabetes mellitus
EP1909793A2 (de) * 2005-07-15 2008-04-16 Proxomed Medizintechnik GmbH Verwendung von phosphodiesterase typ 5-hemmern für die prävention und behandlung von erkrankungen oder gesundheitsstörungen, sowie abgabesysteme für dieselben
MEP8509A (en) 2006-09-07 2011-12-20 Combination treatment for diabetes mellitus
MX2009013354A (es) 2007-06-04 2010-07-06 Univ Ben Gurion Compuestos de triarilo y composiciones que los contienen.
AT512084A1 (de) 2011-10-20 2013-05-15 Univ Wien Tech Diazabicyclo- und diazaspiro-alkanderivate als phosphodiesterase-5 inhibitoren
WO2013173923A1 (en) 2012-05-25 2013-11-28 Diamedica, Inc. Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
CA2880085C (en) 2012-06-04 2021-09-07 Diamedica Inc. Human tissue kallikrein 1 glycosylation isoforms
CN108452311A (zh) * 2012-11-13 2018-08-28 纽斯尔特科学公司 用于增强能量代谢的组合物和方法
US9840547B2 (en) 2013-05-14 2017-12-12 Scimar Ltd. Hepatic insulin sensitizing substance and test meal for insulin sensitization
WO2015068156A1 (en) 2013-11-05 2015-05-14 Ben-Gurion University Of The Negev Research And Development Authority Compounds for the treatment of diabetes and disease complications arising from same
CN110446501A (zh) 2017-03-09 2019-11-12 代阿麦迪卡股份有限公司 组织激肽释放酶1的剂型
MX2017016930A (es) * 2017-12-19 2019-06-20 Malesil Research & Tech Llc Uso del maleato de sildenafil en el tratamiento de ulceras de pie diabetico.

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
GB9013750D0 (en) * 1990-06-20 1990-08-08 Pfizer Ltd Therapeutic agents
GB9511220D0 (en) * 1995-06-02 1995-07-26 Glaxo Group Ltd Solid dispersions
US6166219A (en) * 1995-12-28 2000-12-26 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
WO1998049166A1 (en) * 1997-04-25 1998-11-05 Pfizer Limited PYRAZOLOPYRIMIDINONES WHICH INHIBIT TYPE 5 CYCLIC GUANOSINE 3',5'-MONOPHOSPHATE PHOSPHODIESTERASE (cGMP PDE5) FOR THE TREATMENT OF SEXUAL DYSFUNCTION
RU2199532C2 (ru) * 1997-06-27 2003-02-27 Фудзисава Фармасьютикал Ко., Лтд. Сульфонамидное соединение
WO1999051574A1 (fr) * 1998-04-06 1999-10-14 Fujisawa Pharmaceutical Co., Ltd. Derives d'indole
KR20010086593A (ko) * 1998-12-04 2001-09-13 후지야마 아키라 술폰아미드 화합물 및 그의 의약 용도
ID30182A (id) * 1999-03-22 2001-11-08 Bristol Myers Squibb Co PENGHAMBAT-PENGHAMBAT PIRIDOPIRIDAZINA LEBURAN DARI cGMP FOSFODIESTERASE
DE19944161A1 (de) * 1999-09-15 2001-03-22 Bayer Ag Neue Kombination zur Behandlung von sexueller Dysfunktion
EP1088824B1 (en) * 1999-09-30 2004-01-07 Pfizer Products Inc. Bicyclic pyrrolyl amides as glycogen phosphorylase inhibitors
CA2323008C (en) * 1999-10-11 2005-07-12 Pfizer Inc. Pharmaceutically active compounds
CA2406947A1 (en) * 2000-04-19 2001-10-25 Johns Hopkins University Methods for prevention and treatment of gastrointestinal disorders

Also Published As

Publication number Publication date
HUP0300725A2 (hu) 2003-11-28
HUP0300725A3 (en) 2005-11-28
WO2002013798A2 (en) 2002-02-21
KR20030023747A (ko) 2003-03-19
EP1307183A2 (en) 2003-05-07
AU2001276607A1 (en) 2002-02-25
IL154158A0 (en) 2003-07-31
WO2002013798A3 (en) 2003-01-23
JP2004506009A (ja) 2004-02-26
CN1446084A (zh) 2003-10-01

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued