CA2931189C - Inhibitors of bruton's tyrosine kinase - Google Patents

Inhibitors of bruton's tyrosine kinase Download PDF

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Publication number
CA2931189C
CA2931189C CA2931189A CA2931189A CA2931189C CA 2931189 C CA2931189 C CA 2931189C CA 2931189 A CA2931189 A CA 2931189A CA 2931189 A CA2931189 A CA 2931189A CA 2931189 C CA2931189 C CA 2931189C
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CA
Canada
Prior art keywords
phenoxy
amino
carbonyl
pyrazol
methyl
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.)
Active
Application number
CA2931189A
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English (en)
French (fr)
Other versions
CA2931189A1 (en
Inventor
Francisco Javier Lopez-Tapia
Norman Kong
Sung-Sau So
Yan Lou
Romyr Dominique
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.)
F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CA2931189A1 publication Critical patent/CA2931189A1/en
Application granted granted Critical
Publication of CA2931189C publication Critical patent/CA2931189C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4155—1,2-Diazoles non condensed and containing further 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 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
    • C07D413/14—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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2931189A 2013-12-13 2014-12-10 Inhibitors of bruton's tyrosine kinase Active CA2931189C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361915582P 2013-12-13 2013-12-13
US61/915,582 2013-12-13
PCT/EP2014/077124 WO2015086642A1 (en) 2013-12-13 2014-12-10 Inhibitors of bruton's tyrosine kinase

Publications (2)

Publication Number Publication Date
CA2931189A1 CA2931189A1 (en) 2015-06-18
CA2931189C true CA2931189C (en) 2017-09-26

Family

ID=52016584

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2931189A Active CA2931189C (en) 2013-12-13 2014-12-10 Inhibitors of bruton's tyrosine kinase

Country Status (10)

Country Link
US (1) US9556150B2 (https=)
EP (1) EP3080099B1 (https=)
JP (1) JP6219523B2 (https=)
KR (1) KR101768402B1 (https=)
CN (1) CN105793252B (https=)
CA (1) CA2931189C (https=)
MX (1) MX374758B (https=)
RU (1) RU2648236C2 (https=)
TW (1) TW201534600A (https=)
WO (1) WO2015086642A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112016013540B1 (pt) 2013-12-13 2021-03-02 F. Hoffmann-La Roche Ag inibidores de tirosina quinase de bruton
US10391081B2 (en) 2013-12-27 2019-08-27 Chugai Seiyaku Kabushiki Kaisha FGFR gatekeeper mutant gene and drug targeting same
EP3312172B1 (en) 2015-06-17 2020-05-06 Chugai Seiyaku Kabushiki Kaisha Aminopyrazole derivatives useful as src kinase inhibitors
PL3954690T3 (pl) 2015-07-02 2023-08-14 Acerta Pharma B.V. Postacie stałe i formulacje (s)-4-(8-amino-3-(1-(but-2-ynoilo)pirolidyn-2-ylo)imidazo[1,5-a]-pirazyn-1-ylo)-n-(pirydyn-2-ylo)benzamidu
WO2018152434A1 (en) * 2017-02-17 2018-08-23 The Regents Of The University Of California Systems and methods for making assignments in isotope-labelled proteins using nuclear magnetic resonance data
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2025175249A1 (en) 2024-02-14 2025-08-21 Olema Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof

Family Cites Families (22)

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US5527819A (en) 1991-09-06 1996-06-18 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
FR2772763B1 (fr) 1997-12-24 2004-01-23 Sod Conseils Rech Applic Nouveaux analogues tetracycliques de camptothecines, leurs procedes de preparation, leur application comme medicaments et les compositions pharmaceutiques les contenant
US6316466B1 (en) * 1998-05-05 2001-11-13 Syntex (U.S.A.) Llc Pyrazole derivatives P-38 MAP kinase inhibitors
US20030236288A1 (en) 2002-02-28 2003-12-25 Karl Schoenafinger Use of substituted 3-phenyl-5-alkoxy-3H-(1,3,4)-oxadizol-2-ones for inhibiting pancreatic lipase
UA79804C2 (en) 2002-07-03 2007-07-25 Janssen Pharmaceutica Nv Cck-1 receptor modulators
EA011609B1 (ru) 2003-06-24 2009-04-28 Юнироял Кемикал Компани, Инк. Фунгицидные феноксифенилгидразиновые производные
PT1732892E (pt) 2004-03-26 2008-12-22 Hoffmann La Roche Tetra-hidrocarbazóis e os seus derivados
UA86283C2 (uk) 2005-01-07 2009-04-10 Пфайзер Продактс Инк. Гетероароматичні сполуки хіноліну і їх застосування як інгібіторів pde10
EP2308839B1 (en) 2005-04-20 2017-03-01 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
FR2892416B1 (fr) 2005-10-20 2008-06-27 Sanofi Aventis Sa Derives de 6-heteroarylpyridoindolone, leur preparation et leur application en therapeutique
EP1960382A1 (en) 2005-11-03 2008-08-27 ChemBridge Research Laboratories, Inc. Heterocyclic compounds as tyrosine kinase modulators
JP2009516702A (ja) 2005-11-18 2009-04-23 スミスクライン・ビーチャム・コーポレイション 化合物
US8115005B2 (en) 2006-08-04 2012-02-14 Decode Genetics Ehf. Pyrazolylphenyl and pyrrolylphenyl inhibitors of LTA4H for treating inflammation
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
MX2009010696A (es) 2007-04-06 2009-10-20 Novartis Ag Derivados de 2,6-naftiridina como moduladores de cinasa de proteina.
CN104447716A (zh) 2007-05-09 2015-03-25 沃泰克斯药物股份有限公司 Cftr调节剂
US8026257B2 (en) 2007-07-11 2011-09-27 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
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JP5620417B2 (ja) 2011-02-07 2014-11-05 中外製薬株式会社 アミノピラゾール誘導体を含む医薬

Also Published As

Publication number Publication date
JP6219523B2 (ja) 2017-10-25
EP3080099A1 (en) 2016-10-19
MX2016006744A (es) 2016-09-08
KR20160097353A (ko) 2016-08-17
EP3080099B1 (en) 2018-04-11
KR101768402B1 (ko) 2017-08-14
MX374758B (es) 2025-03-06
JP2016540022A (ja) 2016-12-22
CN105793252B (zh) 2018-01-30
WO2015086642A1 (en) 2015-06-18
US9556150B2 (en) 2017-01-31
US20160311801A1 (en) 2016-10-27
CA2931189A1 (en) 2015-06-18
CN105793252A (zh) 2016-07-20
RU2648236C2 (ru) 2018-03-23
TW201534600A (zh) 2015-09-16

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