WO2009106980A3 - Dérivés d'indazole - Google Patents

Dérivés d'indazole Download PDF

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Publication number
WO2009106980A3
WO2009106980A3 PCT/IB2009/000409 IB2009000409W WO2009106980A3 WO 2009106980 A3 WO2009106980 A3 WO 2009106980A3 IB 2009000409 W IB2009000409 W IB 2009000409W WO 2009106980 A3 WO2009106980 A3 WO 2009106980A3
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
indazole derivatives
mammal
compounds
human
Prior art date
Application number
PCT/IB2009/000409
Other languages
English (en)
Other versions
WO2009106980A2 (fr
Inventor
Ingrid Price Buchler
Michael Joseph Hayes
Shridhar Gajanan Hegde
Susan Landis Hockerman
Darin Eugene Jones
Steven Wade Kortum
Joseph Gerace Rico
Ruth Elizabeth Tenbrink
Kun Ken Wu
Original Assignee
Pfizer Inc.
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 Pfizer Inc. filed Critical Pfizer Inc.
Publication of WO2009106980A2 publication Critical patent/WO2009106980A2/fr
Publication of WO2009106980A3 publication Critical patent/WO2009106980A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne des composés, des compositions pharmaceutiques et des méthodes de traitement d'une pathologie induite par l'activité du récepteur CB1 chez un mammifère, notamment chez l'homme. Ces méthodes consistent à administrer à un mammifère nécessitant un tel traitement une quantité thérapeutiquement efficace du composé de formule (I), dans laquelle R1, R2 et R3 sont tels que définis dans la description.
PCT/IB2009/000409 2008-02-29 2009-02-26 Dérivés d'indazole WO2009106980A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3266708P 2008-02-29 2008-02-29
US61/032,667 2008-02-29

Publications (2)

Publication Number Publication Date
WO2009106980A2 WO2009106980A2 (fr) 2009-09-03
WO2009106980A3 true WO2009106980A3 (fr) 2009-10-29

Family

ID=40676297

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2009/000409 WO2009106980A2 (fr) 2008-02-29 2009-02-26 Dérivés d'indazole

Country Status (1)

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WO (1) WO2009106980A2 (fr)

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JP6062633B2 (ja) 2009-01-28 2017-01-18 カラ セラピューティクス インコーポレイテッド 二環式ピラゾロ複素環類
US7741350B1 (en) 2009-01-28 2010-06-22 Cara Therapeutics, Inc. Bicyclic pyrazolo-heterocycles
AU2014259534B2 (en) * 2011-01-04 2016-05-19 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (AMD)
MX347391B (es) * 2011-01-04 2017-04-25 Novartis Ag Compuestos de indol o análogos de los mismos útiles para el tratamiento de degeneración macular relacionada con la edad (amd).
EP2867227B1 (fr) 2012-06-28 2018-11-21 Novartis AG Modulateurs de la voie du complément et utilisations de ceux-ci
WO2014002052A1 (fr) 2012-06-28 2014-01-03 Novartis Ag Dérivés pyrrolidine et leur utilisation en tant que modulateurs de la voie du complément
JP6155332B2 (ja) 2012-06-28 2017-06-28 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
CN104603126B (zh) 2012-06-28 2017-05-31 诺华股份有限公司 吡咯烷衍生物及其作为补体途径调节剂的用途
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
JP6238980B2 (ja) 2012-07-12 2017-11-29 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
PH12015501492A1 (en) 2013-01-08 2015-09-28 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
EP2998743B1 (fr) * 2014-09-19 2018-02-21 Randox Laboratories Ltd Detection des cannabinoides synthetiques d'indazole
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
WO2017034872A1 (fr) * 2015-08-25 2017-03-02 Janssen Pharmaceutica Nv Dérivés d'indazole à utiliser en tant qu'agonistes inverses de cb-1
EP3402780A1 (fr) 2016-01-14 2018-11-21 Beth Israel Deaconess Medical Center, Inc. Modulateurs de mastocytes et leurs utilisations
CN105709226A (zh) * 2016-01-20 2016-06-29 中国人民解放军第三军医大学第一附属医院 Ii型***素受体激动剂在制备治疗高血压脑出血药物中的应用
TW202222786A (zh) 2016-02-01 2022-06-16 美商百歐克斯製藥公司 苯并吡唑化合物及其類似物
JP6884801B2 (ja) 2016-05-31 2021-06-09 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
IL274557B1 (en) 2017-11-29 2024-05-01 Kalvista Pharmaceuticals Ltd Dosage forms containing a plasma kallikrein inhibitor
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
JP7330828B2 (ja) * 2018-09-20 2023-08-22 日清食品ホールディングス株式会社 ＥＮａＣ活性化能を有する化合物
WO2020059660A1 (fr) * 2018-09-20 2020-03-26 日清食品ホールディングス株式会社 Composé ayant une puissance d'activation d'enac
WO2021028645A1 (fr) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Inhibiteurs de la kallicréine plasmatique
AU2021213804A1 (en) * 2020-01-30 2022-08-18 Research Triangle Institute Indazole derivatives as cannabinoid receptor partial agonists
WO2022192562A1 (fr) * 2021-03-10 2022-09-15 Vincere Biosciences, Inc. Inhibiteurs d'usp30 et leurs utilisations
CN117986183A (zh) * 2022-10-28 2024-05-07 浙江友宁生物医药科技有限公司 一种gpr139受体激动剂、其制备方法及其应用

Citations (9)

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GB1301882A (fr) * 1969-04-01 1973-01-04
WO1996033713A1 (fr) * 1995-03-16 1996-10-31 Eli Lilly And Company Indazolecarboxamides
WO2001058869A2 (fr) * 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Modulateurs de recepteurs aux cannabinoides, leurs procedes de preparation et utilisations de modulateurs de recepteurs aux cannabinoides pour le traitement de maladies respiratoires et non respiratoires
WO2004014864A1 (fr) * 2002-08-10 2004-02-19 Astex Technology Limited Composes 1h-indazole-3-carboxamide utilises en tant qu'inhibiteurs de kinases cycline-dependantes (cdk)
WO2004031158A1 (fr) * 2002-10-02 2004-04-15 Sanofi-Aventis Derives d'indazolecarboxamides, leur preparation et leur utilisation comme inhibiteurs des cdk1, cdk2 et cdk4
WO2005037839A1 (fr) * 2003-10-14 2005-04-28 Entomed Composes derives de norcantharidine, leurs procedes de preparation, les compositions les contenant et leurs utilisations.
WO2005092890A2 (fr) * 2004-03-25 2005-10-06 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, et leur preparation et leurs utilisations
WO2005099703A1 (fr) * 2004-03-16 2005-10-27 Sanofi-Aventis Utilisation de derives d'indazolecarboxamides pour la preparation d'un medicament destine au traitement et a la prevention du paludisme
EP2020232A1 (fr) * 2007-08-03 2009-02-04 Zeltia, S.A. Dérives de N-(1-thiazolyl)-amide pour traiter l'obésité, le diabète et des maladies cardiovasculaires

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1301882A (fr) * 1969-04-01 1973-01-04
WO1996033713A1 (fr) * 1995-03-16 1996-10-31 Eli Lilly And Company Indazolecarboxamides
WO2001058869A2 (fr) * 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Modulateurs de recepteurs aux cannabinoides, leurs procedes de preparation et utilisations de modulateurs de recepteurs aux cannabinoides pour le traitement de maladies respiratoires et non respiratoires
WO2004014864A1 (fr) * 2002-08-10 2004-02-19 Astex Technology Limited Composes 1h-indazole-3-carboxamide utilises en tant qu'inhibiteurs de kinases cycline-dependantes (cdk)
WO2004031158A1 (fr) * 2002-10-02 2004-04-15 Sanofi-Aventis Derives d'indazolecarboxamides, leur preparation et leur utilisation comme inhibiteurs des cdk1, cdk2 et cdk4
WO2005037839A1 (fr) * 2003-10-14 2005-04-28 Entomed Composes derives de norcantharidine, leurs procedes de preparation, les compositions les contenant et leurs utilisations.
WO2005099703A1 (fr) * 2004-03-16 2005-10-27 Sanofi-Aventis Utilisation de derives d'indazolecarboxamides pour la preparation d'un medicament destine au traitement et a la prevention du paludisme
WO2005092890A2 (fr) * 2004-03-25 2005-10-06 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, et leur preparation et leurs utilisations
EP2020232A1 (fr) * 2007-08-03 2009-02-04 Zeltia, S.A. Dérives de N-(1-thiazolyl)-amide pour traiter l'obésité, le diabète et des maladies cardiovasculaires

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