WO2009106980A3 - Indazole derivatives - Google Patents

Indazole derivatives 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
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/IB2009/000409
Other languages
French (fr)
Other versions
WO2009106980A2 (en
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
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 Corp Belgium
Pfizer Corp SRL
Original Assignee
Pfizer Corp Belgium
Pfizer Corp SRL
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 Corp Belgium, Pfizer Corp SRL filed Critical Pfizer Corp Belgium
Publication of WO2009106980A2 publication Critical patent/WO2009106980A2/en
Publication of WO2009106980A3 publication Critical patent/WO2009106980A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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

This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of Formula (I): wherein R1, R2 and R3 are as defined in this specification.
PCT/IB2009/000409 2008-02-29 2009-02-26 Indazole derivatives Ceased WO2009106980A2 (en)

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 (en) 2009-09-03
WO2009106980A3 true WO2009106980A3 (en) 2009-10-29

Family

ID=40676297

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2009/000409 Ceased WO2009106980A2 (en) 2008-02-29 2009-02-26 Indazole derivatives

Country Status (1)

Country Link
WO (1) WO2009106980A2 (en)

Families Citing this family (33)

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US7741350B1 (en) 2009-01-28 2010-06-22 Cara Therapeutics, Inc. Bicyclic pyrazolo-heterocycles
JP6062633B2 (en) 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 Bicyclic pyrazoloheterocycles
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)
WO2012093101A1 (en) * 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
US9487483B2 (en) 2012-06-28 2016-11-08 Novartis Ag Complement pathway modulators and uses thereof
JP6154897B2 (en) 2012-06-28 2017-06-28 ノバルティス アーゲー Pyrrolidine derivatives and their use as complement pathway regulators
EP2867226B1 (en) 2012-06-28 2018-11-14 Novartis AG Complement pathway modulators and uses thereof
WO2014002053A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
ES2647124T3 (en) 2012-06-28 2017-12-19 Novartis Ag Pyrrolidine derivatives and their use as modulators of the complement pathway
JP6238980B2 (en) 2012-07-12 2017-11-29 ノバルティス アーゲー Complement pathway modulators and uses thereof
IL239682B (en) 2013-01-08 2018-10-31 Kalvista Pharmaceuticals Ltd Benzylamine and 2-(aminomethyl)pyridine derivatives
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
TWI636047B (en) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 Heterocyclic derivatives
EP2998743B1 (en) * 2014-09-19 2018-02-21 Randox Laboratories Ltd Detection of indazole synthetic cannabinoids
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
WO2017034872A1 (en) * 2015-08-25 2017-03-02 Janssen Pharmaceutica Nv Indazole derivatives useful as cb-1 inverse agonists
US20190016680A1 (en) 2016-01-14 2019-01-17 Beth Israel Deaconess Medical Center, Inc. Mast-cell modulators and uses thereof
CN105709226A (en) * 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 Applications of CB2R (cannabinoid receptor 2) agonist in preparing medicines for treating hypertensive cerebral hemorrhage
TWI854164B (en) 2016-02-01 2024-09-01 美商百歐克斯製藥公司 Benzopyrazole compounds and analogues thereof
RS60600B1 (en) 2016-05-31 2020-08-31 Kalvista Pharmaceuticals Ltd Pyrazole derivatives as plasma kallikrein inhibitors
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
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
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
IL274557B2 (en) 2017-11-29 2024-09-01 Kalvista Pharmaceuticals Ltd Dosage forms containing a plasma kallikrein inhibitor
WO2020059660A1 (en) * 2018-09-20 2020-03-26 日清食品ホールディングス株式会社 Compound having enac activation potency
JP7330828B2 (en) * 2018-09-20 2023-08-22 日清食品ホールディングス株式会社 Compound having ENaC activating ability
CN114206852A (en) 2019-08-09 2022-03-18 卡尔维斯塔制药有限公司 Plasma kallikrein inhibitors
EP4097088A4 (en) * 2020-01-30 2024-01-24 Research Triangle Institute INDAZOL DERIVATIVES AS PARTIAL CANNABANOID RECEPTOR AGONISTS
CN116438162A (en) * 2020-09-17 2023-07-14 伊赛恩特制药公司 Modulators of MAS-associated G protein receptor X4 and related products and methods
WO2022192562A1 (en) * 2021-03-10 2022-09-15 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
CN117986183A (en) * 2022-10-28 2024-05-07 浙江友宁生物医药科技有限公司 GPR139 receptor agonist, preparation method and application thereof
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Citations (9)

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WO1996033713A1 (en) * 1995-03-16 1996-10-31 Eli Lilly And Company Indazolecarboxamides
WO2001058869A2 (en) * 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
WO2004014864A1 (en) * 2002-08-10 2004-02-19 Astex Technology Limited 1h-indazole-3-carboxamide compounds as cyclin dependent kinases (cdk) inhibitors
WO2004031158A1 (en) * 2002-10-02 2004-04-15 Sanofi-Aventis Indazolecarboxamide derivatives, preparation and use thereof as cdk1, cdk2 and cdk4 inhibitors
WO2005037839A1 (en) * 2003-10-14 2005-04-28 Entomed Norcantharidin derivative compounds, method for the production thereof, compositions containing said compounds and the use thereof
WO2005092890A2 (en) * 2004-03-25 2005-10-06 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof
WO2005099703A1 (en) * 2004-03-16 2005-10-27 Sanofi-Aventis Use of indazolecarboxamide derivatives for the preparation of a medicament that is intended for the treatment and prevention of paludism
EP2020232A1 (en) * 2007-08-03 2009-02-04 Zeltia, S.A. N-(1-thiazolyl)-amide derivatives for the treatment of obesity, diabetes and cardiovascular diseases

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1301882A (en) * 1969-04-01 1973-01-04
WO1996033713A1 (en) * 1995-03-16 1996-10-31 Eli Lilly And Company Indazolecarboxamides
WO2001058869A2 (en) * 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
WO2004014864A1 (en) * 2002-08-10 2004-02-19 Astex Technology Limited 1h-indazole-3-carboxamide compounds as cyclin dependent kinases (cdk) inhibitors
WO2004031158A1 (en) * 2002-10-02 2004-04-15 Sanofi-Aventis Indazolecarboxamide derivatives, preparation and use thereof as cdk1, cdk2 and cdk4 inhibitors
WO2005037839A1 (en) * 2003-10-14 2005-04-28 Entomed Norcantharidin derivative compounds, method for the production thereof, compositions containing said compounds and the use thereof
WO2005099703A1 (en) * 2004-03-16 2005-10-27 Sanofi-Aventis Use of indazolecarboxamide derivatives for the preparation of a medicament that is intended for the treatment and prevention of paludism
WO2005092890A2 (en) * 2004-03-25 2005-10-06 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof
EP2020232A1 (en) * 2007-08-03 2009-02-04 Zeltia, S.A. N-(1-thiazolyl)-amide derivatives for the treatment of obesity, diabetes and cardiovascular diseases

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