CN109310671B - 布鲁顿酪氨酸激酶抑制剂 - Google Patents

布鲁顿酪氨酸激酶抑制剂 Download PDF

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Publication number
CN109310671B
CN109310671B CN201780007631.8A CN201780007631A CN109310671B CN 109310671 B CN109310671 B CN 109310671B CN 201780007631 A CN201780007631 A CN 201780007631A CN 109310671 B CN109310671 B CN 109310671B
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Prior art keywords
pyrazolo
pyridin
phenyl
prop
fluoro
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Chinese (zh)
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CN109310671A (zh
Inventor
廖希斌
李佳
吕志俭
周宇波
高安慧
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Zibo Biopolar Changsheng Pharmaceutical Co ltd
Shanghai Institute of Materia Medica of CAS
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Zibo Biopolar Changsheng Pharmaceutical Co ltd
Shanghai Institute of Materia Medica of CAS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
CN201780007631.8A 2016-01-21 2017-01-17 布鲁顿酪氨酸激酶抑制剂 Active CN109310671B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662281252P 2016-01-21 2016-01-21
US62/281,252 2016-01-21
PCT/US2017/013815 WO2017127371A1 (en) 2016-01-21 2017-01-17 Bruton's tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
CN109310671A CN109310671A (zh) 2019-02-05
CN109310671B true CN109310671B (zh) 2021-08-06

Family

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Country Status (12)

Country Link
US (1) US10662187B2 (https=)
EP (1) EP3405192B1 (https=)
JP (1) JP6950897B2 (https=)
KR (1) KR102699906B1 (https=)
CN (1) CN109310671B (https=)
AU (1) AU2017208998B2 (https=)
CA (1) CA3009669C (https=)
EA (1) EA201891626A1 (https=)
IL (1) IL260691B (https=)
MX (1) MX384833B (https=)
WO (1) WO2017127371A1 (https=)
ZA (1) ZA201805439B (https=)

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US10793566B2 (en) * 2016-01-21 2020-10-06 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
KR102416971B1 (ko) 2016-03-11 2022-07-04 엔젤 파마슈티칼 컴퍼니, 리미티드 브루톤형 티로신 키나제를 조절하기 위한 화합물 및 방법
JOP20190113A1 (ar) * 2016-11-18 2019-05-15 Biocad Joint Stock Co مثبطات بروتون تيروزين كيناز
CN107915584A (zh) * 2017-12-16 2018-04-17 江苏长青农化股份有限公司 氟磺胺草醚中间体2‑氯‑4‑三氟甲基苯酚的合成方法
CN108276254A (zh) * 2018-03-26 2018-07-13 江苏长青农化南通有限公司 一种合成2-氯-4-三氟甲基苯酚的方法
CN113365631B (zh) 2019-01-18 2024-08-30 杭州邦顺制药有限公司 布鲁顿酪氨酸激酶抑制剂
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2021038540A1 (en) 2019-08-31 2021-03-04 Sun Pharma Advanced Research Company Limited Cycloalkylidene carboxylic acids and derivatives as btk inhibitors
HUE065965T2 (hu) * 2019-09-26 2024-06-28 Jumbo Drug Bank Co Ltd 4-fluor-1H-pyrazolo[3,4-C]piridin-származékok mint szelektív bruton-tirozinkináz (BTK) inhibitorok a B-sejtes limfóma és autoimmun betegségek kezelésére
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113493439B (zh) * 2020-03-20 2022-10-14 深圳市塔吉瑞生物医药有限公司 取代的丙烯酰胺衍生物及其组合物及用途
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CN117377675A (zh) * 2021-06-01 2024-01-09 正大天晴药业集团股份有限公司 含有并环或螺环的布鲁顿酪氨酸激酶降解剂
CN120058798A (zh) * 2023-11-30 2025-05-30 武汉人福创新药物研发中心有限公司 含双环的tead抑制剂
WO2025202889A1 (en) * 2024-03-28 2025-10-02 Array Biopharma Inc. Her2 mutation inhibitors

Citations (8)

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EP0254241A1 (en) * 1986-07-22 1988-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Pyrazolopyridine compounds, their preparation and use
JPH01190681A (ja) * 1988-01-22 1989-07-31 Yoshitomi Pharmaceut Ind Ltd ピラゾロピリジン化合物
EP0641564A1 (en) * 1992-05-21 1995-03-08 Yoshitomi Pharmaceutical Industries, Ltd. Optically active condensed pyrazole compound for use in treating thrombocytopenia and erythropenia
WO2010031791A1 (en) * 2008-09-16 2010-03-25 Biovitrum Ab (Publ) New compounds ii
US8377946B1 (en) * 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
US8673925B1 (en) * 2013-04-09 2014-03-18 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2014199171A1 (en) * 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors

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JPH0648941A (ja) * 1992-06-02 1994-02-22 Yoshitomi Pharmaceut Ind Ltd 赤血球減少症治療剤
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US8729107B2 (en) 2002-12-06 2014-05-20 Purdue Research Foundation Pyridines for treating injured mammalian nerve tissue
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BRPI0622054B8 (pt) 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
EP2487159A1 (en) * 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
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WO2014026329A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0254241A1 (en) * 1986-07-22 1988-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Pyrazolopyridine compounds, their preparation and use
JPH01190681A (ja) * 1988-01-22 1989-07-31 Yoshitomi Pharmaceut Ind Ltd ピラゾロピリジン化合物
EP0641564A1 (en) * 1992-05-21 1995-03-08 Yoshitomi Pharmaceutical Industries, Ltd. Optically active condensed pyrazole compound for use in treating thrombocytopenia and erythropenia
WO2010031791A1 (en) * 2008-09-16 2010-03-25 Biovitrum Ab (Publ) New compounds ii
US8377946B1 (en) * 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
US8673925B1 (en) * 2013-04-09 2014-03-18 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2014199171A1 (en) * 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors

Also Published As

Publication number Publication date
KR102699906B1 (ko) 2024-08-29
ZA201805439B (en) 2019-11-27
JP6950897B2 (ja) 2021-10-13
US20190062328A1 (en) 2019-02-28
MX384833B (es) 2025-03-14
AU2017208998A1 (en) 2018-08-09
AU2017208998B2 (en) 2021-07-15
KR20180135885A (ko) 2018-12-21
NZ744554A (en) 2025-03-28
WO2017127371A1 (en) 2017-07-27
JP2019502763A (ja) 2019-01-31
BR112018014705A2 (pt) 2018-12-11
IL260691A (https=) 2018-09-20
EP3405192C0 (en) 2024-12-11
MX2018008815A (es) 2019-03-28
CN109310671A (zh) 2019-02-05
EP3405192A1 (en) 2018-11-28
EP3405192B1 (en) 2024-12-11
US10662187B2 (en) 2020-05-26
CA3009669C (en) 2023-08-08
CA3009669A1 (en) 2017-07-27
EA201891626A1 (ru) 2019-04-30
EP3405192A4 (en) 2019-07-03
IL260691B (en) 2022-07-01

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