CN105793252B - 布鲁顿氏酪氨酸激酶抑制剂 - Google Patents

布鲁顿氏酪氨酸激酶抑制剂 Download PDF

Info

Publication number
CN105793252B
CN105793252B CN201480066841.0A CN201480066841A CN105793252B CN 105793252 B CN105793252 B CN 105793252B CN 201480066841 A CN201480066841 A CN 201480066841A CN 105793252 B CN105793252 B CN 105793252B
Authority
CN
China
Prior art keywords
carbonyl
phenoxy
amino
phenyl
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.)
Expired - Fee Related
Application number
CN201480066841.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN105793252A (zh
Inventor
F·J·洛佩斯-塔比亚
N·孔
S-S·索
Y·楼
R·多米尼克
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
Chugai Pharmaceutical Co Ltd
Original Assignee
F Hoffmann La Roche AG
Chugai Pharmaceutical Co Ltd
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 F Hoffmann La Roche AG, Chugai Pharmaceutical Co Ltd filed Critical F Hoffmann La Roche AG
Publication of CN105793252A publication Critical patent/CN105793252A/zh
Application granted granted Critical
Publication of CN105793252B publication Critical patent/CN105793252B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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)
  • 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)
CN201480066841.0A 2013-12-13 2014-12-10 布鲁顿氏酪氨酸激酶抑制剂 Expired - Fee Related CN105793252B (zh)

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
CN105793252A CN105793252A (zh) 2016-07-20
CN105793252B true CN105793252B (zh) 2018-01-30

Family

ID=52016584

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480066841.0A Expired - Fee Related CN105793252B (zh) 2013-12-13 2014-12-10 布鲁顿氏酪氨酸激酶抑制剂

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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2471786A1 (en) * 2009-08-07 2012-07-04 Chugai Seiyaku Kabushiki Kaisha Aminopyrazole derivative

Family Cites Families (21)

* 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
CN103709148B (zh) * 2008-06-24 2015-10-21 霍夫曼-拉罗奇有限公司 取代的吡啶-2-酮和哒嗪-3-酮
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2471786A1 (en) * 2009-08-07 2012-07-04 Chugai Seiyaku Kabushiki Kaisha Aminopyrazole derivative

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Bruton’s Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies;Yan Lou et al.;《Journal of Medicinal Chemistry》;20120306;第55卷(第10期);第4539-4550页 *
Discovery of S-[5-Amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]-methanone (RO3201195), an Orally Bioavailable and Highly Selective Inhibitor of p38 Map Kinase;David M. Goldstein et al.;《Journal of Medicinal Chemistry》;20060209;第49卷(第5期);第1562-1575页 *

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
KR101768402B1 (ko) 2017-08-14
KR20160097353A (ko) 2016-08-17
RU2648236C2 (ru) 2018-03-23
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
CN104812746B (zh) 布鲁顿氏酪氨酸激酶抑制剂
CN105793252B (zh) 布鲁顿氏酪氨酸激酶抑制剂
TW201300374A (zh) 布魯頓氏酪氨酸激酶（ｂｒｕｔｏｎ’ｓ ｔｙｒｏｓｉｎｅ ｋｉｎａｓｅ）之抑制劑
US10640491B2 (en) Inhibitors of bruton's tyrosine kinase
CN105143215B (zh) 布鲁顿氏酪氨酸激酶抑制剂
CN105722834B (zh) 酪氨酸蛋白激酶抑制剂
HK1226070A1 (en) Inhibitors of bruton’s tyrosine kinase
HK1226735B (en) Inhibitors of bruton’s tyrosine kinase
HK1226735A1 (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

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1226735

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1226735

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20180130

CF01 Termination of patent right due to non-payment of annual fee