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WO2004089471A3 - Utilisation pharmaceutique de pyrazolo[1,5-a]pyrimidines substituees - Google Patents

Utilisation pharmaceutique de pyrazolo[1,5-a]pyrimidines substituees Download PDF

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Publication number
WO2004089471A3
WO2004089471A3 PCT/DK2004/000253 DK2004000253W WO2004089471A3 WO 2004089471 A3 WO2004089471 A3 WO 2004089471A3 DK 2004000253 W DK2004000253 W DK 2004000253W WO 2004089471 A3 WO2004089471 A3 WO 2004089471A3
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WO
WIPO (PCT)
Prior art keywords
pyrimidines
pharmaceutical use
11βhsd1
activity
compounds
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.)
Ceased
Application number
PCT/DK2004/000253
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English (en)
Other versions
WO2004089471A2 (fr
Inventor
Henrik Sune Andersen
Gita Camilla Tejlgaard Kampen
Inge Thoeger Christensen
John Patrick Mogensen
Annette Rosendal Larsen
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Novo Nordisk AS
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Novo Nordisk AS
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Filing date
Publication date
Application filed by Novo Nordisk AS filed Critical Novo Nordisk AS
Priority to JP2006504356A priority Critical patent/JP2006522749A/ja
Priority to EP04725889A priority patent/EP1615697A2/fr
Publication of WO2004089471A2 publication Critical patent/WO2004089471A2/fr
Publication of WO2004089471A3 publication Critical patent/WO2004089471A3/fr
Priority to US11/254,118 priority patent/US20070270408A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

L'invention concerne l'utilisation de pyrazolo[1,5-a]pyrimidines substituées dans la modulation de l'activité de la 11β-hydroxystéroïde déshydrogénase de type 1 (11βHSD1), ainsi que l'utilisation desdits composés sous forme de compositions pharmaceutiques. L'invention concerne également une nouvelle catégorie de pyrazolo[1,5-a]pyrimidines substituées, leur utilisation dans le traitement thérapeutique, des compositions pharmaceutiques contenant lesdits composés, ainsi que leur utilisation dans la fabrication de médicaments. Les composés selon l'invention sont des modulateurs, plus particulièrement des inhibiteurs de l'activité de la 11βHSD1, et sont utiles dans le traitement, la prévention et/ou la prophylaxie de divers troubles médicaux pour lesquels une concentration intracellulaire réduite du glucocorticoïde est souhaitable.
PCT/DK2004/000253 2003-04-11 2004-04-06 Utilisation pharmaceutique de pyrazolo[1,5-a]pyrimidines substituees Ceased WO2004089471A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2006504356A JP2006522749A (ja) 2003-04-11 2004-04-06 置換ピラゾロ［１，５−ａ］ピリミジンの薬学的使用
EP04725889A EP1615697A2 (fr) 2003-04-11 2004-04-06 Utilisation pharmaceutique de pyrazolo 1,5-a]pyrimidines substituees
US11/254,118 US20070270408A1 (en) 2003-04-11 2005-10-11 Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DKPA200300569 2003-04-11
DKPA200300569 2003-04-11
US46745303P 2003-05-02 2003-05-02
US60/467,453 2003-05-02

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/254,118 Continuation US20070270408A1 (en) 2003-04-11 2005-10-11 Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines

Publications (2)

Publication Number Publication Date
WO2004089471A2 WO2004089471A2 (fr) 2004-10-21
WO2004089471A3 true WO2004089471A3 (fr) 2004-12-23

Family

ID=33160909

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2004/000253 Ceased WO2004089471A2 (fr) 2003-04-11 2004-04-06 Utilisation pharmaceutique de pyrazolo[1,5-a]pyrimidines substituees

Country Status (3)

Country Link
EP (1) EP1615697A2 (fr)
JP (1) JP2006522749A (fr)
WO (1) WO2004089471A2 (fr)

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US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
US8927549B2 (en) 2008-11-21 2015-01-06 High Point Pharmaceuticals, Llc Adamantyl benzamide derivatives
US9346815B2 (en) 2014-05-23 2016-05-24 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US9394285B2 (en) 2013-03-15 2016-07-19 Pfizer Inc. Indole and indazole compounds that activate AMPK
US10307426B2 (en) 2017-05-22 2019-06-04 Genentech, Inc. Therapeutic compounds and compositions, and methods of use thereof

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WO2004089416A2 (fr) * 2003-04-11 2004-10-21 Novo Nordisk A/S Polytherapie utilisant un inhibiteur de type 1 de la 11beta-hydroxysteroide deshydrogenase et un agent hypotenseur dans le traitement du syndrome metabolique et des troubles et maladies associes
WO2004089415A2 (fr) * 2003-04-11 2004-10-21 Novo Nordisk A/S Therapie combinatoire utilisant un inhibiteur de 11$g(b)-hydroxysteroide deshydrogenase de type 1 et agoniste du recepteur de glucocorticoides pour minimiser les effets secondaires associes a la therapie a base d'agoniste du recepteur de glucocorticoides
US20100222316A1 (en) 2004-04-29 2010-09-02 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
US8415354B2 (en) 2004-04-29 2013-04-09 Abbott Laboratories Methods of use of inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
US7880001B2 (en) 2004-04-29 2011-02-01 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
US8198331B2 (en) 2005-01-05 2012-06-12 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
CA2594116A1 (fr) 2005-01-05 2006-07-13 Abbott Laboratories Inhibiteurs de l'enzyme 11-beta-hydroxysteroide dehydrogenase de type 1
KR101496206B1 (ko) 2005-01-05 2015-02-27 애브비 인코포레이티드 11-베타-하이드록시스테로이드 데하이드로게나제 타입 1 효소의 억제제로서의 아다만틸 유도체
US20090192198A1 (en) 2005-01-05 2009-07-30 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
WO2006106052A1 (fr) 2005-04-05 2006-10-12 F. Hoffmann-La Roche Ag 1h-pyrazole 4-carboxylamides, preparation et utilisation de ceux-ci comme 11-beta-hydroxysteroide deshydrogenase
EP2527337A1 (fr) * 2005-04-14 2012-11-28 Bristol-Myers Squibb Company Inhibiteurs de la 11-bêta hydroxystéroïde déshydrogénase de type I
US7622492B2 (en) 2005-08-31 2009-11-24 Hoffmann-La Roche Inc. Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase
CA2627307A1 (fr) * 2005-11-01 2007-05-10 Transtech Pharma, Inc. Utilisation pharmaceutique d'amides substitues
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KR101081293B1 (ko) 2006-01-18 2011-11-08 에프. 호프만-라 로슈 아게 11 베타-에이치에스디1 억제제로서 티아졸
WO2007092435A2 (fr) 2006-02-07 2007-08-16 Wyeth Inhibiteurs 11-beta hsd1
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
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US20090215778A1 (en) * 2007-04-27 2009-08-27 Panacos Pharmaceuticals, Inc. Alpha-substituted Arylmethyl Piperazine Pyrazolo [1,5-alpha]Pyrimidine Amide Derivatives
EP2025674A1 (fr) 2007-08-15 2009-02-18 sanofi-aventis Tetrahydronaphthaline substituée, son procédé de fabrication et son utilisation en tant que médicament
JP5736098B2 (ja) 2007-08-21 2015-06-17 アッヴィ・インコーポレイテッド 中枢神経系障害を治療するための医薬組成物
EP2085398A1 (fr) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, leur procédé de préparation et leur utilisation en tant que médicament
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EP2683703B1 (fr) 2011-03-08 2015-05-27 Sanofi Nouveaux dérivés phényl-oxathiazine substitués, procédé pour leur préparation, agent pharmaceutique contenant ces composés et leur utilisation
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KR102727682B1 (ko) * 2023-01-20 2024-11-07 주식회사 이노보테라퓨틱스 신규한 헤테로사이클릭 화합물

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DATABASE CHEMCATS CHEMICAL ABSTRACTS SERVICE COLUMBUS, OHIO, US; April 2003 (2003-04-01), XP002292075 *
DATABASE CHEMCATS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 2002, XP002292071 *
DATABASE CHEMCATS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; April 2003 (2003-04-01), XP002292072 *
DATABASE CHEMCATS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; April 2003 (2003-04-01), XP002292073 *
DATABASE CHEMCATS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; April 2003 (2003-04-01), XP002292074 *
DATABASE WPI Section Ch Week 200412, Derwent World Patents Index; Class B02, AN 2004-112780, XP002292087 *

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US8927549B2 (en) 2008-11-21 2015-01-06 High Point Pharmaceuticals, Llc Adamantyl benzamide derivatives
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9394285B2 (en) 2013-03-15 2016-07-19 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9346815B2 (en) 2014-05-23 2016-05-24 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US9604984B2 (en) 2014-05-23 2017-03-28 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US10307426B2 (en) 2017-05-22 2019-06-04 Genentech, Inc. Therapeutic compounds and compositions, and methods of use thereof

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WO2004089471A2 (fr) 2004-10-21
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