JP5871896B2 - Ｂ−ｒａｆキナーゼインヒビター - Google Patents

Ｂ−ｒａｆキナーゼインヒビター Download PDF

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JP5871896B2
JP5871896B2 JP2013500523A JP2013500523A JP5871896B2 JP 5871896 B2 JP5871896 B2 JP 5871896B2 JP 2013500523 A JP2013500523 A JP 2013500523A JP 2013500523 A JP2013500523 A JP 2013500523A JP 5871896 B2 JP5871896 B2 JP 5871896B2
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alkyl
methyl
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mmol
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JP2013523614A5 (enExample
JP2013523614A (ja
Inventor
シュテフェン シュトイラー
シュテフェン シュトイラー
ペーター エトマイヤー
ペーター エトマイヤー
アンドレアス マントウリディス
アンドレアス マントウリディス
Original Assignee
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • 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
    • C07D487/10—Spiro-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
    • A61K31/435—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
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
JP2013500523A 2010-03-26 2011-03-25 Ｂ−ｒａｆキナーゼインヒビター Active JP5871896B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10158041.3 2010-03-26
EP10158041 2010-03-26
PCT/EP2011/054611 WO2011117381A1 (en) 2010-03-26 2011-03-25 B-raf kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2013523614A JP2013523614A (ja) 2013-06-17
JP2013523614A5 JP2013523614A5 (enExample) 2014-05-15
JP5871896B2 true JP5871896B2 (ja) 2016-03-01

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JP2013500523A Active JP5871896B2 (ja) 2010-03-26 2011-03-25 Ｂ−ｒａｆキナーゼインヒビター

Country Status (4)

Country Link
US (1) US9290507B2 (enExample)
EP (1) EP2552905B1 (enExample)
JP (1) JP5871896B2 (enExample)
WO (1) WO2011117381A1 (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0712795A2 (pt) 2006-07-07 2012-09-04 Boehringer Ingelheim Int derivados de heteroarila substituìdos com fenila e uso dos mesmos como agentes antitumorais
PE20090837A1 (es) * 2007-07-02 2009-07-24 Boehringer Ingelheim Int Nuevos compuestos quimicos
TW201014860A (en) 2008-09-08 2010-04-16 Boehringer Ingelheim Int New chemical compounds
EA201100564A1 (ru) 2008-09-29 2011-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Антипролиферативные соединения
US8569316B2 (en) 2009-02-17 2013-10-29 Boehringer Ingelheim International Gmbh Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
JP5871896B2 (ja) 2010-03-26 2016-03-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂ−ｒａｆキナーゼインヒビター
WO2011117382A1 (en) 2010-03-26 2011-09-29 Boehringer Ingelheim International Gmbh Pyridyltriazoles
US8546443B2 (en) 2010-12-21 2013-10-01 Boehringer Ingelheim International Gmbh Benzylic oxindole pyrimidines
US8710055B2 (en) 2010-12-21 2014-04-29 Boehringer Ingelheim International Gmbh Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
US8889684B2 (en) 2011-02-02 2014-11-18 Boehringer Ingelheim International Gmbh Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
MX363708B (es) 2013-10-14 2019-03-29 Eisai R&D Man Co Ltd Compuestos de quinolina selectivamente sustituidos.
SG10201704327RA (en) 2013-10-14 2017-06-29 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
WO2015171833A1 (en) * 2014-05-06 2015-11-12 The Regents Of The University Of California Wound healing using braf inhibitors
WO2017100593A1 (en) 2015-12-09 2017-06-15 Luc Therapeutics Thienopyrimidinone nmda receptor modulators and uses thereof
DK3386591T3 (da) 2015-12-09 2020-09-28 Cadent Therapeutics Inc Heteroaromatic nmda receptor modulators and uses thereof
US11274107B2 (en) 2016-12-22 2022-03-15 Cadent Therapeutics, Inc. NMDA receptor modulators and uses thereof
EP3579872A1 (en) 2017-02-10 2019-12-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
CA3086765A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
HUE062566T2 (hu) 2018-08-03 2023-11-28 Novartis Ag Heteroaromás NMDA receptor modulátorok és alkalmazásaik
RS64618B1 (sr) * 2019-02-12 2023-10-31 Lutris Pharma Ltd Upotreba lokalnih kompozicija braf inhibitorа za lečenje radijacijskog dermatitisa
CN111606887B (zh) 2019-02-26 2023-03-17 安徽中科拓苒药物科学研究有限公司 一种新型激酶抑制剂
WO2021035788A1 (zh) * 2019-08-29 2021-03-04 中国科学院合肥物质科学研究院 吡唑衍生物及其用途
CN116057045A (zh) 2020-06-05 2023-05-02 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂
WO2022188792A1 (zh) * 2021-03-12 2022-09-15 四川科伦博泰生物医药股份有限公司 具有蛋白激酶抑制活性的杂环化合物、包含其的药物组合物及其制备方法和用途

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU507066B1 (en) 1977-09-06 1980-01-31 Sumitomo Chemical Company, Limited 2-Substituted-5-Hydroxy-1h-Imidazole 4-Carbozamide Derivatives
JPH03174153A (ja) 1989-09-20 1991-07-29 Fuji Photo Film Co Ltd カラー画像形成方法
CA2212061A1 (en) 1995-02-02 1996-08-08 Laramie Mary Gaster Indole derivatives as 5-ht receptor antagonist
AU6526896A (en) 1995-07-22 1997-02-18 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
JP2003529536A (ja) 1999-02-09 2003-10-07 ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド Ｃ１ｓ介在疾患および状態の処置法、およびそれのための化合物および組成物
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
US6531478B2 (en) 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
WO2003037274A2 (en) 2001-11-01 2003-05-08 Icagen, Inc. Pyrazole-amides and-sulfonamides
US20040010027A1 (en) 2001-12-17 2004-01-15 Pharmacia & Upjohn Spa Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them
JP2005162612A (ja) 2002-01-09 2005-06-23 Ajinomoto Co Inc アシルスルホンアミド誘導体
US7166628B2 (en) 2002-11-27 2007-01-23 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
CN102060806A (zh) 2003-09-11 2011-05-18 iTherX药品公司 细胞因子抑制剂
EP1663953A1 (en) 2003-09-24 2006-06-07 Methylgene, Inc. Inhibitors of histone deacetylase
WO2005040152A1 (en) 2003-10-20 2005-05-06 E.I. Dupont De Nemours And Company Heteroyclylphenyl-and heterocyclylpyridyl-substituted azolecarboxamides as herbicides
US7511042B2 (en) 2003-12-03 2009-03-31 Boehringer Ingelheim Pharmaceuticals, Inc. Triazole compounds
SI1725544T1 (sl) 2004-03-09 2009-10-31 Boehringer Ingelheim Pharma 3-(4-heterociklil-1,2,3-triazol-1-il)-N-aril-benzamidi kot inhibitorji proizvodnje citokinov za zdravljenje kroničnih vnetnih bolezni
US7485657B2 (en) 2004-05-12 2009-02-03 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
EP1819341A4 (en) 2004-11-10 2011-06-29 Synta Pharmaceuticals Corp IL-12 MODULATORY CONNECTIONS
US7531560B2 (en) 2004-11-10 2009-05-12 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
JP2007076376A (ja) 2005-09-09 2007-03-29 Yanmar Co Ltd トラクタ
WO2007056016A2 (en) 2005-11-02 2007-05-18 Kemia, Inc. Bisamide cytokine inhibitors
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
JP2009536618A (ja) 2006-04-18 2009-10-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ４−及び５−イミダゾリル環を含むサイトカイン阻害化合物の製造方法及びその中間体
RU2009103999A (ru) 2006-07-07 2010-08-20 Шеринг Корпорейшн (US) 3,4-дизамещенные циклобутен-1,2-дионы как лиганды схс-хемокиновых рецепторов
US8030487B2 (en) 2006-07-07 2011-10-04 Targegen, Inc. 2-amino—5-substituted pyrimidine inhibitors
PT2041138E (pt) 2006-07-07 2014-10-07 Bristol Myers Squibb Co Inibidores de pirrolotriazina quinase
BRPI0712795A2 (pt) * 2006-07-07 2012-09-04 Boehringer Ingelheim Int derivados de heteroarila substituìdos com fenila e uso dos mesmos como agentes antitumorais
PE20080906A1 (es) 2006-08-17 2008-07-05 Kemia Inc Derivados heteroarilo como inhibidores de citocina
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
WO2008089034A2 (en) 2007-01-11 2008-07-24 Kemia, Inc. Cytokine inhibitors
EP2176249A2 (en) 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
PE20090837A1 (es) 2007-07-02 2009-07-24 Boehringer Ingelheim Int Nuevos compuestos quimicos
JP5385382B2 (ja) 2008-07-24 2014-01-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ プロテインキナーゼ阻害剤としての３，４−ジアリールピラゾール
TW201014860A (en) 2008-09-08 2010-04-16 Boehringer Ingelheim Int New chemical compounds
EA201100564A1 (ru) 2008-09-29 2011-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Антипролиферативные соединения
US8569316B2 (en) 2009-02-17 2013-10-29 Boehringer Ingelheim International Gmbh Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
JP5871896B2 (ja) 2010-03-26 2016-03-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂ−ｒａｆキナーゼインヒビター
WO2011117382A1 (en) 2010-03-26 2011-09-29 Boehringer Ingelheim International Gmbh Pyridyltriazoles
US8710055B2 (en) 2010-12-21 2014-04-29 Boehringer Ingelheim International Gmbh Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
US20130023531A1 (en) 2011-01-27 2013-01-24 Boehringer Ingelheim International Gmbh Pyrimido[5,4-d]pyrimidylamino phenyl sulfonamides as serine/threonine kinase inhibitors
US8889684B2 (en) 2011-02-02 2014-11-18 Boehringer Ingelheim International Gmbh Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors

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