EA029210B1 - Гетероароматические соединения в качестве ингибиторов btk - Google Patents

Гетероароматические соединения в качестве ингибиторов btk Download PDF

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Publication number
EA029210B1
EA029210B1 EA201500207A EA201500207A EA029210B1 EA 029210 B1 EA029210 B1 EA 029210B1 EA 201500207 A EA201500207 A EA 201500207A EA 201500207 A EA201500207 A EA 201500207A EA 029210 B1 EA029210 B1 EA 029210B1
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Eurasian Patent Office
Prior art keywords
compound
mmol
pharmaceutically acceptable
compound according
group
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EA201500207A
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English (en)
Russian (ru)
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EA201500207A1 (ru
Inventor
Йёрг Мартин Бентцин
Анджела Кей Берри
Тодд Босанак
Майкл Джейсон БЕРК
Даррен Тодд Дисалво
Джошуа Кортни Хоран
Шуан Лян
Кан Мао
Ван Мао
Ю Шэнь
Фариба Солимензадех
Рени М. Зинделл
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Бёрингер Ингельхайм Интернациональ Гмбх
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Application filed by Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201500207A1 publication Critical patent/EA201500207A1/ru
Publication of EA029210B1 publication Critical patent/EA029210B1/ru

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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • 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
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
EA201500207A 2012-08-10 2013-08-08 Гетероароматические соединения в качестве ингибиторов btk EA029210B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261681684P 2012-08-10 2012-08-10
PCT/US2013/054096 WO2014025976A1 (en) 2012-08-10 2013-08-08 Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors

Publications (2)

Publication Number Publication Date
EA201500207A1 EA201500207A1 (ru) 2015-08-31
EA029210B1 true EA029210B1 (ru) 2018-02-28

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EA201500207A EA029210B1 (ru) 2012-08-10 2013-08-08 Гетероароматические соединения в качестве ингибиторов btk

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US (5) US20140045813A1 (cg-RX-API-DMAC7.html)
EP (1) EP2882741B1 (cg-RX-API-DMAC7.html)
JP (1) JP6348492B2 (cg-RX-API-DMAC7.html)
KR (1) KR20150040292A (cg-RX-API-DMAC7.html)
CN (1) CN104603124B (cg-RX-API-DMAC7.html)
AP (1) AP2015008203A0 (cg-RX-API-DMAC7.html)
AU (1) AU2013299557B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015002590A2 (cg-RX-API-DMAC7.html)
CA (1) CA2881519A1 (cg-RX-API-DMAC7.html)
CL (1) CL2015000256A1 (cg-RX-API-DMAC7.html)
EA (1) EA029210B1 (cg-RX-API-DMAC7.html)
EC (1) ECSP15008851A (cg-RX-API-DMAC7.html)
GE (1) GEP201706748B (cg-RX-API-DMAC7.html)
IL (1) IL236495A0 (cg-RX-API-DMAC7.html)
IN (1) IN2015DN00524A (cg-RX-API-DMAC7.html)
MA (1) MA37830B1 (cg-RX-API-DMAC7.html)
MX (1) MX2015001802A (cg-RX-API-DMAC7.html)
NZ (1) NZ703607A (cg-RX-API-DMAC7.html)
PE (1) PE20150756A1 (cg-RX-API-DMAC7.html)
PH (1) PH12015500294A1 (cg-RX-API-DMAC7.html)
SA (1) SA515360007B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201500499TA (cg-RX-API-DMAC7.html)
TN (1) TN2015000029A1 (cg-RX-API-DMAC7.html)
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US20140045813A1 (en) 2012-08-10 2014-02-13 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
WO2014068527A1 (en) * 2012-11-02 2014-05-08 Pfizer Inc. Bruton's tyrosine kinase inhibitors
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
EP2970163B1 (en) * 2013-03-14 2018-02-28 Boehringer Ingelheim International GmbH 5-thiazolecarboxamide dervatives and their use as btk inhibitors
EP2970300B1 (en) 2013-03-15 2018-05-16 Boehringer Ingelheim International GmbH Heteroaromatic compounds as btk inhibitors
KR102311329B1 (ko) * 2013-03-15 2021-10-14 얀센 파마슈티카 엔.브이. 약제를 제조하기 위한 방법 및 중간체
WO2015048662A2 (en) * 2013-09-30 2015-04-02 X-Rx Discovery, Inc. Substituted nicotinimide inhibitors of btk and their preparation and use in the treatment of cancer, inflammation and autoimmune disease
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
EP3099674B1 (en) * 2014-01-29 2018-10-24 Boehringer Ingelheim International Gmbh Pyrazole compounds as btk inhibitors
WO2015185998A2 (en) * 2014-04-11 2015-12-10 Acerta Pharma B.V. Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase
CN105085474B (zh) * 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN105884747B (zh) * 2014-08-28 2021-01-05 首药控股(北京)有限公司 一种制备布鲁顿酪氨酸激酶(btk)激酶抑制剂的制备方法
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
CA3005268C (en) 2015-12-16 2024-04-30 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
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