CN113105475B - 布鲁顿氏酪氨酸激酶的抑制剂及其使用方法 - Google Patents

布鲁顿氏酪氨酸激酶的抑制剂及其使用方法 Download PDF

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Publication number
CN113105475B
CN113105475B CN202110404344.9A CN202110404344A CN113105475B CN 113105475 B CN113105475 B CN 113105475B CN 202110404344 A CN202110404344 A CN 202110404344A CN 113105475 B CN113105475 B CN 113105475B
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China
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oxo
thia
dihydro
carboxamide
triazacenaphthylene
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Chinese (zh)
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CN113105475A (zh
Inventor
N.阿罗拉
G.M.巴卡尼
J.K.巴尔贝
S.D.本贝内克
C.P.德克胡特
J.P.爱德华兹
B.戈什
K.克罗伊特
M.S.蒂切诺尔
J.D.韦纳布莱
J.韦
J.J.M.韦纳
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/16—Peri-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202110404344.9A 2015-12-10 2016-12-09 布鲁顿氏酪氨酸激酶的抑制剂及其使用方法 Active CN113105475B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562265780P 2015-12-10 2015-12-10
US62/265780 2015-12-10
PCT/US2016/065964 WO2017100668A1 (en) 2015-12-10 2016-12-09 Inhibitors of bruton's tyrosine kinase and methods of their use
CN201680072147.9A CN109071563A (zh) 2015-12-10 2016-12-09 布鲁顿氏酪氨酸激酶的抑制剂及其使用方法

Related Parent Applications (1)

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CN113105475A CN113105475A (zh) 2021-07-13
CN113105475B true CN113105475B (zh) 2022-09-09

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CN201680072147.9A Pending CN109071563A (zh) 2015-12-10 2016-12-09 布鲁顿氏酪氨酸激酶的抑制剂及其使用方法

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US (3) US10689396B2 (enExample)
EP (1) EP3386992B1 (enExample)
JP (2) JP7110097B2 (enExample)
KR (1) KR20180094514A (enExample)
CN (2) CN113105475B (enExample)
AR (1) AR107041A1 (enExample)
AU (1) AU2016366546B2 (enExample)
BR (1) BR112018011525B1 (enExample)
CA (1) CA3007993C (enExample)
EA (1) EA038031B1 (enExample)
IL (1) IL259862B (enExample)
JO (1) JO3793B1 (enExample)
MX (1) MX386700B (enExample)
TW (1) TWI739779B (enExample)
UY (1) UY37016A (enExample)
WO (1) WO2017100668A1 (enExample)

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JP3003987B2 (ja) 1996-08-20 2000-01-31 篠▲崎▼ 晴彦 合成樹脂管内に施設されるケーブルの支持装置及びそのケーブル支持具を取付ける方法
JO3794B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون
JO3793B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv مثبطات تيروزين كاينيز بروتون وأساليب استخدامها
WO2018170220A1 (en) * 2017-03-15 2018-09-20 Janssen Sciences Ireland Uc Methods of selective aryl- and heteroaryl-nitrogen bond formation
CN110028525A (zh) * 2018-04-13 2019-07-19 太仓运通新材料科技有限公司 一种2-氟磷酰基乙酸三乙酯的合成方法
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
EP4218934B1 (en) * 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
CA3116141C (en) 2018-12-06 2023-09-05 Daiichi Sankyo Company, Limited Cycloalkane-1,3-diamine derivative
CN114401957B (zh) * 2019-09-04 2023-11-21 正大天晴药业集团股份有限公司 一种喹唑啉衍生物的制备方法及其结晶
CN111635368B (zh) * 2020-06-12 2021-06-29 东莞市东阳光仿制药研发有限公司 一种胺化合物的制备方法
MX2023014435A (es) 2021-06-04 2024-03-08 Janssen Pharmaceutica Nv Inhibidores de la tirosina quinasa de bruton y métodos de su uso.
MX2023015147A (es) * 2021-06-30 2024-04-01 Janssen Pharmaceutica Nv Inhibidores de la tirosina quinasa de bruton y métodos de su uso.
CN114478346A (zh) * 2021-12-31 2022-05-13 和鼎(南京)医药技术有限公司 一种制备乌帕替尼中间体的方法

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WO2006118749A1 (en) * 2005-05-04 2006-11-09 Janssen Pharmaceutica, N.V. Thia-tetraazaacenaphthylene kinase inhibitors
WO2007092879A2 (en) * 2006-02-08 2007-08-16 Janssen Pharmaceutica, N.V. Substituted thiatriazaacenaphthylene-6-carbonitrile kinase inhibitors
WO2010056875A1 (en) * 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
WO2015089337A1 (en) * 2013-12-11 2015-06-18 Biogen Idec Ma Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology

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DE3112415A1 (de) 1981-03-28 1982-10-07 Dynamit Nobel Ag, 5210 Troisdorf Verfahren zur chlorierung von cyclischen amiden und cyclischen vinylogen amiden
US5430150A (en) 1992-12-16 1995-07-04 American Cyanamid Company Retroviral protease inhibitors
US5300478A (en) 1993-01-28 1994-04-05 Zeneca Limited Substituted fused pyrazolo compounds
AU2005284796A1 (en) 2004-09-15 2006-03-23 Janssen Pharmaceutica, N.V. Thiazolopyridine kinase inhibitors
US7605154B2 (en) 2005-08-08 2009-10-20 Janssen Pharmaceutica N.V. Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
WO2011133609A2 (en) 2010-04-19 2011-10-27 The Translational Genomics Research Institute Methods and kits to predict therapeutic outcome of btk inhibitors
FR2978441A1 (fr) 2011-07-25 2013-02-01 Diverchim Nouveaux analogues de ceramides, leurs procedes de preparation et leurs applications dans les compositions pharmaceutiques et cosmetiques
EP2970291B1 (en) 2013-03-15 2022-05-11 Janssen Pharmaceutica, N.V. Processes and intermediates for preparing a medicament
JO3794B1 (ar) * 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون
JO3793B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv مثبطات تيروزين كاينيز بروتون وأساليب استخدامها
WO2018103058A1 (en) 2016-12-09 2018-06-14 Janssen Pharmaceutica Nv Inhibitors of bruton's tyrosine kinase and methods of their use
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Patent Citations (4)

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WO2006118749A1 (en) * 2005-05-04 2006-11-09 Janssen Pharmaceutica, N.V. Thia-tetraazaacenaphthylene kinase inhibitors
WO2007092879A2 (en) * 2006-02-08 2007-08-16 Janssen Pharmaceutica, N.V. Substituted thiatriazaacenaphthylene-6-carbonitrile kinase inhibitors
WO2010056875A1 (en) * 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
WO2015089337A1 (en) * 2013-12-11 2015-06-18 Biogen Idec Ma Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology

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Publication number Publication date
EA038031B1 (ru) 2021-06-25
IL259862B (en) 2022-04-01
UY37016A (es) 2017-06-30
JP7471348B2 (ja) 2024-04-19
JP2022141851A (ja) 2022-09-29
MX2018007084A (es) 2018-11-09
CN113105475A (zh) 2021-07-13
TW201734020A (zh) 2017-10-01
US10689396B2 (en) 2020-06-23
WO2017100668A1 (en) 2017-06-15
KR20180094514A (ko) 2018-08-23
US20190284204A1 (en) 2019-09-19
BR112018011525A2 (pt) 2018-11-21
AR107041A1 (es) 2018-03-14
US20170283431A1 (en) 2017-10-05
US20190284203A1 (en) 2019-09-19
JP7110097B2 (ja) 2022-08-01
TWI739779B (zh) 2021-09-21
IL259862A (en) 2018-07-31
JO3793B1 (ar) 2021-01-31
AU2016366546A1 (en) 2018-05-31
JP2018536684A (ja) 2018-12-13
US10822348B2 (en) 2020-11-03
CN109071563A (zh) 2018-12-21
BR112018011525B1 (pt) 2023-10-24
EP3386992A1 (en) 2018-10-17
MX386700B (es) 2025-03-19
EP3386992B1 (en) 2019-11-27
EA201891379A1 (ru) 2018-12-28
CA3007993C (en) 2024-01-16
US10800792B2 (en) 2020-10-13
CA3007993A1 (en) 2017-06-15
AU2016366546B2 (en) 2021-08-12

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