RU2648236C2 - Ингибиторы тирозинкиназы брутона - Google Patents

Ингибиторы тирозинкиназы брутона Download PDF

Info

Publication number
RU2648236C2
RU2648236C2 RU2016126176A RU2016126176A RU2648236C2 RU 2648236 C2 RU2648236 C2 RU 2648236C2 RU 2016126176 A RU2016126176 A RU 2016126176A RU 2016126176 A RU2016126176 A RU 2016126176A RU 2648236 C2 RU2648236 C2 RU 2648236C2
Authority
RU
Russia
Prior art keywords
carbonyl
phenoxy
amino
pyrazol
phenyl
Prior art date
Application number
RU2016126176A
Other languages
English (en)
Russian (ru)
Inventor
Франсиско Хавьер Лопез-Тапиа
Норман КОН
Сун-Сау СО
Ян Лоу
Ромир ДОМИНИК
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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 Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Application granted granted Critical
Publication of RU2648236C2 publication Critical patent/RU2648236C2/ru

Links

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
    • 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
    • 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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (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)
RU2016126176A 2013-12-13 2014-12-10 Ингибиторы тирозинкиназы брутона RU2648236C2 (ru)

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 (1)

Publication Number Publication Date
RU2648236C2 true RU2648236C2 (ru) 2018-03-23

Family

ID=52016584

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2016126176A RU2648236C2 (ru) 2013-12-13 2014-12-10 Ингибиторы тирозинкиназы брутона

Country Status (10)

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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2929747C (en) * 2013-12-13 2018-01-23 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
JP6514645B2 (ja) 2013-12-27 2019-05-15 中外製薬株式会社 Ｆｇｆｒゲートキーパー変異遺伝子およびそれを標的とする医薬
US10479780B2 (en) 2015-06-17 2019-11-19 Chugai Seiyaku Kabushiki Kaisha Aminopyrazole derivatives
HRP20211511T1 (hr) 2015-07-02 2021-12-24 Acerta Pharma B.V. Čvrsti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2011101774A (ru) * 2008-06-24 2012-07-27 Ф.Хоффманн-Ля Рош Аг (Ch) Новые замещенные пиридин-2-оны и пиридазин-3-оны
RU2012108164A (ru) * 2009-08-07 2013-09-20 Чугаи Сеияку Кабушики Каиша Производное аминопиразола

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2005092856A1 (en) 2004-03-26 2005-10-06 F. Hoffmann-La Roche Ag Tetrahydrocarbazoles and derivatives
AP2362A (en) 2005-01-07 2012-02-08 Pfizer Prod Inc Heteroaromatic quinoline compounds and their use as PDE10 inhibitors.
WO2006112549A1 (ja) 2005-04-20 2006-10-26 Takeda Pharmaceutical Company Limited 縮合複素環化合物
FR2892416B1 (fr) 2005-10-20 2008-06-27 Sanofi Aventis Sa Derives de 6-heteroarylpyridoindolone, leur preparation et leur application en therapeutique
EP2298770A1 (en) 2005-11-03 2011-03-23 ChemBridge Corporation Heterocyclic compounds as TrkA 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
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
WO2008122614A1 (en) 2007-04-06 2008-10-16 Novartis Ag 2, 6-naphthyridine derivatives as protein kinase modulators
CA2686838C (en) 2007-05-09 2017-03-14 Vertex Pharmaceuticals Incorporated Modulators of cftr
US8026257B2 (en) 2007-07-11 2011-09-27 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
TW200920369A (en) 2007-10-26 2009-05-16 Amira Pharmaceuticals Inc 5-lipoxygenase activating protein (flap) inhibitor
WO2012078859A2 (en) 2010-12-09 2012-06-14 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Protein kinase d inhibitors
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2011101774A (ru) * 2008-06-24 2012-07-27 Ф.Хоффманн-Ля Рош Аг (Ch) Новые замещенные пиридин-2-оны и пиридазин-3-оны
RU2012108164A (ru) * 2009-08-07 2013-09-20 Чугаи Сеияку Кабушики Каиша Производное аминопиразола

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
YAN LOU et al. "Bruton's Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies", JOURNAL OF MEDICINAL CHEMISTRY, 2012, vol. 55, no. 10, pages 4539 - 4550. *

Also Published As

Publication number Publication date
CA2931189C (en) 2017-09-26
US9556150B2 (en) 2017-01-31
JP2016540022A (ja) 2016-12-22
US20160311801A1 (en) 2016-10-27
CA2931189A1 (en) 2015-06-18
CN105793252B (zh) 2018-01-30
KR101768402B1 (ko) 2017-08-14
KR20160097353A (ko) 2016-08-17
MX2016006744A (es) 2016-09-08
EP3080099A1 (en) 2016-10-19
JP6219523B2 (ja) 2017-10-25
CN105793252A (zh) 2016-07-20
TW201534600A (zh) 2015-09-16
WO2015086642A1 (en) 2015-06-18
MX374758B (es) 2025-03-06
EP3080099B1 (en) 2018-04-11

Similar Documents

Publication Publication Date Title
US9458105B2 (en) Inhibitors of Bruton's tyrosine kinase
RU2648236C2 (ru) Ингибиторы тирозинкиназы брутона
US10640491B2 (en) Inhibitors of bruton's tyrosine kinase
HK1217695A1 (zh) 布鲁顿氏酪氨酸激酶抑制剂
TWI540130B (zh) 布魯頓氏（ｂｒｕｔｏｎ'ｓ）酪胺酸激酶抑制劑
CA2893637A1 (en) Thiazole derivatives as inhibitors of bruton's tyrosine kinase
HK1226070A1 (en) Inhibitors of bruton’s tyrosine kinase
HK1226735A1 (en) Inhibitors of bruton’s tyrosine kinase
HK1226735B (en) Inhibitors of bruton’s tyrosine kinase
HK1226734A1 (en) Inhibitors of bruton’s tyrosine kinase
HK1226734B (en) Inhibitors of bruton’s tyrosine kinase
HK1212689B (en) Inhibitors of bruton's tyrosine kinase
HK1212975B (en) Thiazole derivatives as inhibitors of bruton's tyrosine kinase