EA027561B1 - Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона - Google Patents

Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона Download PDF

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Publication number
EA027561B1
EA027561B1 EA201490859A EA201490859A EA027561B1 EA 027561 B1 EA027561 B1 EA 027561B1 EA 201490859 A EA201490859 A EA 201490859A EA 201490859 A EA201490859 A EA 201490859A EA 027561 B1 EA027561 B1 EA 027561B1
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Eurasian Patent Office
Prior art keywords
methyl
oxo
mmol
fluoro
pyridin
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EA201490859A
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English (en)
Russian (ru)
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EA201490859A1 (ru
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Джеймс Джон Кроуфорд
Венди Б. Янг
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Ф.Хоффманн-Ля Рош Аг
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Publication of EA201490859A1 publication Critical patent/EA201490859A1/ru
Publication of EA027561B1 publication Critical patent/EA027561B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
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    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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    • 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
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    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/50Pyridazines; Hydrogenated pyridazines
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    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • C07D471/12Heterocyclic 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 three hetero rings
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  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
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  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201490859A 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона EA027561B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555395P 2011-11-03 2011-11-03
PCT/US2012/063198 WO2013067277A1 (en) 2011-11-03 2012-11-02 Alkylated piperazine compounds as inhibitors of btk activity

Publications (2)

Publication Number Publication Date
EA201490859A1 EA201490859A1 (ru) 2014-09-30
EA027561B1 true EA027561B1 (ru) 2017-08-31

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EA201490859A EA027561B1 (ru) 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона

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Country Link
US (3) US8729072B2 (enExample)
EP (1) EP2773639B1 (enExample)
JP (2) JP5976828B2 (enExample)
KR (1) KR101716011B1 (enExample)
CN (1) CN104024255B (enExample)
AR (1) AR088642A1 (enExample)
AU (1) AU2012332368A1 (enExample)
BR (1) BR112014010439A2 (enExample)
CA (1) CA2853970A1 (enExample)
CL (1) CL2014001158A1 (enExample)
CO (1) CO6950475A2 (enExample)
CR (1) CR20140187A (enExample)
EA (1) EA027561B1 (enExample)
IL (1) IL232280A0 (enExample)
IN (1) IN2014CN03265A (enExample)
MA (1) MA35725B1 (enExample)
MX (1) MX2014005289A (enExample)
PE (1) PE20141686A1 (enExample)
PH (1) PH12014500966A1 (enExample)
SG (1) SG11201401993RA (enExample)
TW (1) TW201326171A (enExample)
WO (1) WO2013067277A1 (enExample)
ZA (1) ZA201403158B (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013021374A2 (en) 2011-08-05 2013-02-14 Mitraltech Ltd. Techniques for percutaneous mitral valve replacement and sealing
SG11201401993RA (en) * 2011-11-03 2014-05-29 Hoffmann La Roche Alkylated piperazine compounds as inhibitors of btk activity
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
CN110698481B (zh) 2013-07-03 2023-02-28 豪夫迈·罗氏有限公司 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物
KR101813830B1 (ko) 2013-12-05 2017-12-29 에프. 호프만-라 로슈 아게 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물
US9908872B2 (en) 2013-12-13 2018-03-06 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
AU2014361798B2 (en) 2013-12-13 2020-06-11 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015151006A1 (en) 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
WO2015154064A2 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2015170266A1 (en) 2014-05-07 2015-11-12 Lupin Limited Substituted pyrimidine compounds as btk inhibitors
CN111303159A (zh) * 2014-10-02 2020-06-19 豪夫迈·罗氏有限公司 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物
EP3715346B1 (en) 2014-10-22 2024-01-03 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
EP3212645B1 (en) 2014-10-27 2018-11-28 F.Hoffmann-La Roche Ag Process for making tricyclic lactam compounds
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
CU24509B1 (es) * 2015-03-10 2021-05-12 Aurigene Discovery Tech Ltd Compuestos de 1,2,4-oxadiazol y tiadiazol como inmunomoduladores
US10246461B2 (en) 2016-02-29 2019-04-02 Genentech, Inc. Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
MA46995A (fr) 2016-12-03 2019-10-09 Acerta Pharma Bv Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase
IL284690B (en) * 2016-12-15 2022-07-01 Hoffmann La Roche Process for preparing btk inhibitors
CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治宫颈炎的活性化合物
EP3930717A1 (en) 2019-02-25 2022-01-05 Guangzhou Lupeng Pharmaceutical Company Ltd. Inhibitor of btk and mutants thereof
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
US20220363689A1 (en) 2019-10-05 2022-11-17 Newave Pharmaceutical Inc. Inhibitor of btk and mutants thereof
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202140488A (zh) 2020-02-20 2021-11-01 大陸商和記黃埔醫藥(上海)有限公司 雜芳基雜環化合物及其用途
US20230158031A1 (en) * 2020-04-22 2023-05-25 Principia Biopharma Inc. Treatment of Acute Respiratory Distress Syndrome and Other Disorders Involving Cytokine Storm Using BTK Inhibitors
WO2021254483A1 (zh) * 2020-06-18 2021-12-23 上海华汇拓医药科技有限公司 布鲁顿酪氨酸激酶抑制剂及其制备方法
CN116568687B (zh) 2020-09-21 2025-09-02 和记黄埔医药(上海)有限公司 杂芳基杂环化合物及其用途
US20230382900A1 (en) 2020-10-30 2023-11-30 Newave Pharmaceutical Inc. Inhibitors of btk
WO2022133184A1 (en) 2020-12-20 2022-06-23 Newave Pharmaceutical Inc. Btk degrader
CN118613470B (zh) * 2022-01-28 2025-08-15 和记黄埔医药(上海)有限公司 7,8-二氢-2h-环戊二烯并吡咯并吡嗪酮化合物的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010122038A1 (en) * 2009-04-24 2010-10-28 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
WO2011140488A1 (en) * 2010-05-07 2011-11-10 Gilead Connecticut, Inc. Pyridone and aza-pyridone compounds and methods of use
WO2012031004A1 (en) * 2010-09-01 2012-03-08 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
US8828902B2 (en) 2001-07-12 2014-09-09 Reaxa Limited Microencapsulated catalyst methods of preparation and method of use thereof
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
WO2006053121A2 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
CA2601628C (en) 2005-03-10 2014-05-13 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
EP1934174B1 (en) 2005-10-07 2011-04-06 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
AR063946A1 (es) 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
US8426441B2 (en) 2007-12-14 2013-04-23 Roche Palo Alto Llc Inhibitors of bruton's tyrosine kinase
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
WO2009137596A1 (en) 2008-05-06 2009-11-12 Cgi Pharmaceuticals, Inc. Substituted amides, method of making, and use as btk inhibitors
NZ601700A (en) 2008-06-24 2013-02-22 Hoffmann La Roche 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives as inhibitors of Bruton's Tyrosine Kinase (Btk)
PL2300459T3 (pl) 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy
EP2307413B1 (en) 2008-07-15 2015-09-09 F. Hoffmann-La Roche AG Novel phenyl-imidazopyridines and pyridazines
WO2010056875A1 (en) 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
US8299077B2 (en) * 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
EP2424368B1 (en) * 2009-04-29 2014-12-31 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
TWI711610B (zh) * 2009-09-04 2020-12-01 美商百健Ma公司 布魯頓氏酪胺酸激酶抑制劑
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
KR101864908B1 (ko) 2010-09-01 2018-06-05 질레드 코네티컷 인코포레이티드 피리다지논, 그의 제조 방법 및 사용 방법
AU2012257802A1 (en) 2011-05-17 2013-10-31 F. Hoffmann-La Roche Ag Inhibitors of Bruton's tyrosine kinase
PE20140865A1 (es) 2011-08-17 2014-07-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
SG11201401993RA (en) * 2011-11-03 2014-05-29 Hoffmann La Roche Alkylated piperazine compounds as inhibitors of btk activity
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010122038A1 (en) * 2009-04-24 2010-10-28 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
WO2011140488A1 (en) * 2010-05-07 2011-11-10 Gilead Connecticut, Inc. Pyridone and aza-pyridone compounds and methods of use
WO2012031004A1 (en) * 2010-09-01 2012-03-08 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof

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