EA201391626A1 - Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака - Google Patents

Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака

Info

Publication number
EA201391626A1
EA201391626A1 EA201391626A EA201391626A EA201391626A1 EA 201391626 A1 EA201391626 A1 EA 201391626A1 EA 201391626 A EA201391626 A EA 201391626A EA 201391626 A EA201391626 A EA 201391626A EA 201391626 A1 EA201391626 A1 EA 201391626A1
Authority
EA
Eurasian Patent Office
Prior art keywords
egfr
compounds
cell proliferation
cancer types
inhibiting cell
Prior art date
Application number
EA201391626A
Other languages
English (en)
Inventor
Дэвид К. Далгарно
Вэй-Шэн Хуан
Уилльям К. Шекспир
Ихань Ван
Сяотянь Чжу
Original Assignee
Ариад Фармасьютикалз, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ариад Фармасьютикалз, Инк. filed Critical Ариад Фармасьютикалз, Инк.
Publication of EA201391626A1 publication Critical patent/EA201391626A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • A61K31/55—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Изобретение раскрывает соединения, фармацевтические композиции и способы для лечения пациентов с EGFR-стимулированным раком, включающие соединение формулы (I), где переменные имеют значения, определенные в настоящей заявке.
EA201391626A 2011-05-04 2012-05-04 Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака EA201391626A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161482433P 2011-05-04 2011-05-04
PCT/US2012/036683 WO2012151561A1 (en) 2011-05-04 2012-05-04 Compounds for inhibiting cell proliferation in egfr-driven cancers

Publications (1)

Publication Number Publication Date
EA201391626A1 true EA201391626A1 (ru) 2014-03-31

Family

ID=47108074

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391626A EA201391626A1 (ru) 2011-05-04 2012-05-04 Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака

Country Status (12)

Country Link
US (1) US9834518B2 (ru)
EP (1) EP2704572B1 (ru)
JP (1) JP5999177B2 (ru)
KR (1) KR101884010B1 (ru)
CN (1) CN103501612B (ru)
AU (1) AU2012250517B2 (ru)
BR (1) BR112013027734A2 (ru)
CA (1) CA2832504C (ru)
EA (1) EA201391626A1 (ru)
IL (1) IL228739B (ru)
MX (1) MX360404B (ru)
WO (1) WO2012151561A1 (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2649001C1 (ru) * 2014-02-25 2018-03-29 Шанхай Хайянь Фармасьютикал Текнолоджи Ко., Лтд. Производные 2,4-дизамещенного фенилен-1,5-диамина и их применения, фармацевтические композиции и фармацевтически приемлемые композиции, полученные из них

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
ES2645689T3 (es) 2008-05-21 2017-12-07 Ariad Pharmaceuticals, Inc. Derivados de fósforo como inhibidores de quinasas
RU2536584C2 (ru) 2008-06-27 2014-12-27 Авила Терапьютикс, Инк. Гетероарильные соединения и их применение
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TW201100441A (en) * 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
US8563568B2 (en) 2010-08-10 2013-10-22 Celgene Avilomics Research, Inc. Besylate salt of a BTK inhibitor
CN103269704B (zh) 2010-11-01 2018-07-06 西建卡尔有限责任公司 杂环化合物和其用途
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
ES2665013T3 (es) 2010-11-10 2018-04-24 Celgene Car Llc Inhibidores de EGFR selectivos de mutante y usos de los mismos
JP6000273B2 (ja) 2010-11-29 2016-09-28 オーエスアイ・ファーマシューティカルズ，エルエルシー 大環状キナーゼ阻害剤
KR101884010B1 (ko) 2011-05-04 2018-07-31 어리어드 파마슈티칼스, 인코포레이티드 Egfr-유도된 암의 세포 증식을 억제하는 화합물
AU2012288626C1 (en) * 2011-07-27 2015-09-17 Astrazeneca Ab 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as EGFR modulators useful for treating cancer
EP2770830A4 (en) 2011-10-28 2015-05-27 Celgene Avilomics Res Inc METHODS OF TREATING A DISEASE OR DISEASE ASSOCIATED WITH TYROSINE KINASE BTK (BRUTON'S TYROSINE KINASE)
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
JP6353788B2 (ja) 2012-01-13 2018-07-04 エイシア バイオサイエンシーズ インコーポレイテッド 抗がん剤としての複素環式化合物およびその使用
RS57901B1 (sr) 2012-03-15 2019-01-31 Celgene Car Llc Soli inhibitora kinaze receptora epidermalnog faktora rasta
MX356753B (es) 2012-03-15 2018-06-12 Celgene Avilomics Res Inc Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico.
JP6469567B2 (ja) * 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EA201591051A1 (ru) 2013-02-08 2016-06-30 Селджен Авиломикс Рисерч, Инк. Ингибиторы erk и варианты их применения
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
DK3019496T3 (da) * 2013-07-11 2019-12-09 Acea Therapeutics Inc Pyrimidinderivater som kinaseinhibitorer
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
UA115388C2 (uk) * 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN105315285B (zh) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
CN105315259B (zh) * 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
ES2741785T3 (es) 2014-08-13 2020-02-12 Celgene Car Llc Formas y composiciones de un inhibidor de ERK
BR112017006713B1 (pt) 2014-10-11 2023-11-21 Shanghai Hansoh Biomedical Co., Ltd. Inibidores de egfr, seus usos e seu processo de preparação, e composição farmacêutica
CN111170998B (zh) * 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
MX2017007664A (es) 2014-12-11 2018-01-23 Beta Pharma Inc Derivados de 2-anilinopirimidina sustituida como moduladores de egfr.
WO2016187028A1 (en) * 2015-05-15 2016-11-24 Celgene Avilomics Research, Inc. Heteroaryl compounds, synthesis thereof, and intermediates thereto
CN106187915A (zh) * 2015-05-27 2016-12-07 上海翰森生物医药科技有限公司 具有alk与egfr双重活性的抑制剂及其制备方法和应用
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
CN106883213B (zh) * 2015-12-15 2021-04-20 合肥中科普瑞昇生物医药科技有限公司 一种egfr和alk激酶的双重抑制剂
WO2017111076A1 (ja) 2015-12-24 2017-06-29 協和発酵キリン株式会社 α、β不飽和アミド化合物
EA201892311A1 (ru) 2016-05-11 2019-06-28 Бета Фарма, Инк. Производные 2-анилинопиримидина в качестве терапевтических агентов для лечения рака мозга
CN106083736A (zh) * 2016-06-21 2016-11-09 郑州泰基鸿诺医药股份有限公司 一种嘧啶类化合物、egfr抑制剂及其应用
WO2018108064A1 (zh) * 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为***egfr激酶抑制剂的螺环芳基磷氧化合物
CA3059072A1 (en) 2017-04-07 2018-10-11 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
WO2019015655A1 (zh) * 2017-07-19 2019-01-24 正大天晴药业集团股份有限公司 作为egfr激酶抑制剂的芳基磷氧化合物
WO2019034153A1 (zh) * 2017-08-18 2019-02-21 北京韩美药品有限公司 一种化合物，其药物组合物及其用途及应用
CN111683662B (zh) * 2017-08-28 2024-04-02 陈志宏 取代嘧啶类化合物及其药物组合物和治疗方法
CN107522742B (zh) * 2017-10-20 2019-10-18 常州工程职业技术学院 一种Brigatinib关键中间体的均相“一锅法”制备方法
WO2019120121A1 (zh) * 2017-12-21 2019-06-27 深圳市塔吉瑞生物医药有限公司 用于抑制激酶活性的二苯氨基嘧啶类化合物
KR20190108080A (ko) * 2018-03-13 2019-09-23 보로노이바이오 주식회사 2,4,5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암 또는 염증질환의 예방 또는 치료용 약학적 조성물
EP3783005B1 (en) * 2018-04-20 2023-12-06 Guizhou Inochini Technology Co., Ltd Dimethylphosphine oxide compound
CN111718325A (zh) * 2019-03-22 2020-09-29 烟台药物研究所 一种2,4,5-取代嘧啶类化合物及其制备方法和应用
US20220227796A1 (en) * 2019-04-04 2022-07-21 Betta Pharmaceuticals Co., Ltd. Egfr inhibitors, compositions and methods there of
JP2022539208A (ja) 2019-07-03 2022-09-07 スミトモ ファーマ オンコロジー， インコーポレイテッド チロシンキナーゼ非受容体１（ｔｎｋ１）阻害剤およびその使用
CN112538072B (zh) * 2019-09-21 2024-02-06 齐鲁制药有限公司 氨基嘧啶类egfr抑制剂
WO2021073498A1 (zh) * 2019-10-17 2021-04-22 贝达药业股份有限公司 Egfr抑制剂、组合物及其制备方法
WO2021104441A1 (zh) * 2019-11-29 2021-06-03 江苏先声药业有限公司 作为egfr激酶抑制剂的多芳基化合物
CN114885607A (zh) * 2020-02-14 2022-08-09 贝达药业股份有限公司 喹啉基膦氧化合物及其组合物和用途
JP2023518609A (ja) * 2020-03-23 2023-05-02 チールー ファーマシューティカル カンパニー、リミテッド 新規アミノピリミジン系ｅｇｆｒ阻害剤
KR20230002721A (ko) * 2020-04-14 2023-01-05 치루 파머수티컬 컴퍼니 리미티드 Egfr 억제제로서의 삼환계 화합물
CN114728994B (zh) * 2020-07-03 2023-04-28 成都地奥九泓制药厂 芳基磷氧类化合物及其用途
EP4237418A1 (en) * 2020-10-30 2023-09-06 Blueprint Medicines Corporation Pyrimidine compounds, compositions, and medicinal applications thereof
WO2022199589A1 (zh) * 2021-03-23 2022-09-29 南京明德新药研发有限公司 嘧啶衍生物
KR20230054567A (ko) * 2021-10-15 2023-04-25 제이투에이치바이오텍 (주) Alk 및/또는 egfr 돌연변이 키나제 억제 효과를 나타내는 화합물 및 이의 의약 용도

Family Cites Families (279)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1129563A (en) 1966-03-31 1968-10-09 Ici Ltd Phosphorus-containing pyrimidine derivatives and biologically active compositions containing them
EP0391451A1 (en) 1986-04-17 1990-10-10 Imperial Chemical Industries Plc Fungicides
US4966622A (en) 1988-04-12 1990-10-30 Ciba-Geigy Corporation N-phenyl-N-pyrimidin-2-ylureas
GB8828222D0 (en) 1988-12-02 1989-01-05 Ici Plc Reactive dyes
GB8903019D0 (en) 1989-02-10 1989-03-30 Ici Plc Fungicides
GB9016584D0 (en) 1990-07-27 1990-09-12 Ici Plc Fungicides
ATE167473T1 (de) 1990-08-20 1998-07-15 Eisai Co Ltd Sulfonamid-derivate
GB9220964D0 (en) 1991-11-15 1992-11-18 Ici Plc Anionic compounds
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
TW225528B (ru) 1992-04-03 1994-06-21 Ciba Geigy Ag
CA2148931A1 (en) 1993-10-01 1995-04-13 Jurg Zimmermann Pyrimidineamine derivatives and processes for the preparation thereof
AU692484B2 (en) 1993-10-12 1998-06-11 Du Pont Pharmaceuticals Company 1N-alkyl-N-arylpyrimidinamines and derivatives thereof
DE69630214T2 (de) 1995-03-10 2004-07-15 Berlex Laboratories, Inc., Richmond Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
US5728201A (en) 1995-09-14 1998-03-17 Canon Kabushiki Kaisha Ink, and ink-jet recording method and instruments using the same
GB9519197D0 (en) 1995-09-20 1995-11-22 Affinity Chromatography Ltd Novel affinity ligands and their use
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
GB9608771D0 (en) 1996-04-27 1996-07-03 Agrevo Uk Ltd Pyrimethanil salts
JP3106966B2 (ja) 1996-07-17 2000-11-06 富士ゼロックス株式会社 インクジェット記録用インク及びインクジェット記録方法
JPH1060338A (ja) 1996-08-21 1998-03-03 Fuji Xerox Co Ltd インクジェット記録用インク及びインクジェット記録方法
US6008234A (en) 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
CN1234798A (zh) 1996-09-12 1999-11-10 舍林股份公司 环状氨基酸和环状羟基羧酸衍生物取代的苄脒衍生物和它们用作抗凝剂的用途
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
US6573044B1 (en) 1997-08-07 2003-06-03 The Regents Of The University Of California Methods of using chemical libraries to search for new kinase inhibitors
JPH1160573A (ja) 1997-08-22 1999-03-02 Nippon Kayaku Co Ltd トリアジン誘導体及びテロメラーゼ阻害剤
US6432963B1 (en) 1997-12-15 2002-08-13 Yamanouchi Pharmaceutical Co., Ltd. Pyrimidine-5-carboxamide derivatives
US6562833B1 (en) 1998-06-10 2003-05-13 Basf Aktiengesellschaft Use of 2-(n-phenylamino)pyrimidines as fungicides, and novel 2-(n-phenylamino) pyrimidines
AU5648599A (en) 1998-09-11 2000-04-03 Kyorin Pharmaceutical Co. Ltd. Phosphonic ester derivatives and process for producing the same
AP1683A (en) 1998-11-10 2006-11-29 Janssen Pharmaceutica Nv HIV replication inhibiting pyrimidines.
EP1132387B1 (en) 1998-11-17 2005-09-28 Kumiai Chemical Industry Co., Ltd. Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultural/horticultural fungicides
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
CA2362401A1 (en) 1999-02-04 2000-08-10 Paul Fleming G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9910807D0 (en) 1999-05-10 1999-07-07 Prometic Biosciences Limited Novel detoxification agents and their use
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
ITMI992711A1 (it) 1999-12-27 2001-06-27 Novartis Ag Composti organici
AU3704101A (en) 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
US6525051B2 (en) 2000-03-27 2003-02-25 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
CA2407754C (en) 2000-05-08 2009-09-15 Janssen Pharmaceutica N.V. Prodrugs of hiv replication inhibiting pyrimidines
CA2406562C (en) 2000-05-08 2009-09-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
AU2001294511A1 (en) 2000-06-30 2002-01-08 The Regents Of The University Of California New strategy for leukemia therapy
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
GB0022438D0 (en) 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
JP4988140B2 (ja) 2000-12-05 2012-08-01 クラリアント ファイナンス （ビーブイアイ） リミティド 三原色染色法
IL156306A0 (en) 2000-12-21 2004-01-04 Glaxo Group Ltd Pyrimidineamines as angiogenesis modulators
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
DE60232510D1 (de) 2001-06-15 2009-07-16 Vertex Pharma 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US6960572B2 (en) 2001-06-21 2005-11-01 Ariad Pharmaceuticals, Inc. Indolinones and uses thereof
WO2003000186A2 (en) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
AU2002330003A1 (en) 2001-09-07 2003-03-24 Irm Llc Sensory neuron receptors
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
US6949644B2 (en) 2001-10-12 2005-09-27 Irm Llc Methods for the synthesis of substituted purines
US20060009642A1 (en) 2001-10-12 2006-01-12 Irm Llc, A Delaware Limited Liability Company Methods for the synthesis of substituted purines
JP2005512972A (ja) 2001-10-12 2005-05-12 アイアールエム エルエルシー キナーゼ阻害剤足場およびそれらの調製方法
US6770652B2 (en) * 2001-10-18 2004-08-03 Duquesne University Of The Holy Ghost Multiple acting anti-angiogenic and cytotoxic compounds and methods for using the same
EP1448556A1 (en) 2001-11-01 2004-08-25 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
EP1469810A4 (en) 2002-01-04 2009-01-14 Univ Rockefeller COMPOSITIONS AND METHODS FOR THE PREVENTION AND TREATMENT OF DISEASES RELATED TO AMYLOID-BETA PEPTIDE
EP1479693A4 (en) 2002-02-05 2005-07-27 Japan Science & Tech Agency EGF / EGFR COMPLEX
US7459455B2 (en) 2002-02-08 2008-12-02 Smithkline Beecham Corporation Pyrimidine compounds
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
JP2005523922A (ja) 2002-04-26 2005-08-11 ギリアード サイエンシーズ， インコーポレイテッド 非ヌクレオシド逆転写酵素阻害剤
US20050239054A1 (en) 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
US7019017B2 (en) 2002-05-14 2006-03-28 Baylor College Of Medicine Small molecule inhibitors of HER2 expression
CA2486853A1 (en) 2002-05-27 2003-12-04 Novartis Ag Bis-aromatic alkanols
GB0217431D0 (en) 2002-07-27 2002-09-04 Astrazeneca Ab Novel compounds
DK1534286T3 (da) 2002-07-29 2010-04-26 Rigel Pharmaceuticals Inc Fremgangsmåder til behandling eller forebyggelse af autoimmune sygdomme med 2,4-pyrimidindiamin-forbindelser
ES2295685T3 (es) 2002-08-24 2008-04-16 Astrazeneca Ab Derivados de pirimidina como moduladores de la actividad del receptor de quimioquinas.
AU2003286876A1 (en) 2002-11-01 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
AU2004210697B2 (en) 2003-02-11 2007-10-18 Irm Llc Novel bicyclic compounds and compositions
CL2004000303A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
WO2004074244A2 (en) 2003-02-20 2004-09-02 Smithkline Beecham Corporation Pyrimidine compounds
US7151096B2 (en) 2003-03-05 2006-12-19 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US7253166B2 (en) 2003-04-22 2007-08-07 Irm Llc 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
WO2004098520A2 (en) 2003-05-01 2004-11-18 Irm Llc Compounds and compositions as protein kinase inhibitors
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
WO2005011597A2 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
CN1849318B (zh) 2003-07-30 2011-10-12 里格尔药品股份有限公司 用2,4-嘧啶二胺化合物预防和治疗自体免疫疾病的方法
ES2365223T3 (es) 2003-08-07 2011-09-26 Rigel Pharmaceuticals, Inc. Compuestos 2,4-pirimidindiamínicos y usos como agentes antiproliferativos.
CA2535620A1 (en) 2003-08-15 2005-02-24 Irm Llc 6-substituted anilino purines as rtk inhibitors
SG145749A1 (en) 2003-08-15 2008-09-29 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
US7338957B2 (en) 2003-08-28 2008-03-04 Irm Llc Compounds and compositions as protein kinase inhibitors
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
CN100412066C (zh) 2003-09-30 2008-08-20 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
WO2005030151A2 (en) 2003-10-02 2005-04-07 Irm Llc Compounds and compositions as protein kinase inhibitors
MXPA06003996A (es) 2003-10-08 2006-07-05 Irm Llc Compuestos y composiciones como inhibidores de la proteina cinasa.
DE10349587A1 (de) 2003-10-24 2005-05-25 Merck Patent Gmbh Benzimidazolylderivate
CA2543294A1 (en) 2003-10-24 2005-05-26 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
JP2007514775A (ja) 2003-12-19 2007-06-07 ライジェル ファーマシューティカルズ， インコーポレイテッド １−（２，４−ピリミジンジアミノ）−２−シクロペンタンカルボキサイミド合成中間体の立体異性体および立体異性体混合物
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
US7432377B2 (en) 2004-01-16 2008-10-07 Wyeth Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof
CA2553785C (en) 2004-02-14 2011-02-08 Irm Llc Compounds and compositions as protein kinase inhibitors
CA2566531A1 (en) 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
CA2567662C (en) 2004-06-10 2012-11-27 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2005258266A1 (en) 2004-06-23 2006-01-05 Irm Llc Compounds and compositions as protein kinase inhibitors
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
WO2006038594A1 (ja) 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. Ｎ型カルシウムチャネル阻害薬
EP1799652A1 (en) 2004-10-13 2007-06-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
GT200500321A (es) 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
EP1828185B1 (en) 2004-12-21 2009-05-06 SmithKline Beecham Corporation 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
JP5208516B2 (ja) 2004-12-30 2013-06-12 エグゼリクシス， インコーポレイテッド キナーゼモジュレーターとしてのピリミジン誘導体および使用方法
CN101115761B (zh) 2005-01-19 2012-07-18 里格尔药品股份有限公司 2,4-嘧啶二胺化合物的前药及其应用
RU2368602C2 (ru) 2005-01-26 2009-09-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
RU2383545C2 (ru) 2005-03-15 2010-03-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
CA2600531A1 (en) 2005-03-16 2006-09-28 Targegen, Inc. Pyrimidine compounds and methods of use
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
AU2006247757B2 (en) 2005-05-13 2009-08-27 Irm, Llc Compounds and compositions as protein kinase inhibitors
PT1896470E (pt) 2005-05-16 2010-08-26 Scripps Research Inst Derivados de pirrolopiridina como inibidores de proteína-quinase
US20090215777A1 (en) 2005-05-19 2009-08-27 Astex Therapeutics Ltd. Pyrimidine Derivatives As HSP90 Inhibitors
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7491732B2 (en) 2005-06-08 2009-02-17 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
ATE527253T1 (de) 2005-07-01 2011-10-15 Irm Llc Pyrimidin-substituierte benzimidazolderivate als proteinkinasehemmer
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
WO2007006926A2 (fr) 2005-07-11 2007-01-18 Sanofi-Aventis Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
NZ566021A (en) 2005-07-26 2011-03-31 Vertex Pharma Benzimidazoles useful as inhibitors of protein kinases
US20080227783A1 (en) 2005-08-02 2008-09-18 Irm Llc 5-Substituted Thiazol-2-Yl Amino Compounds and Compositions as Protein Kinase Inhibitors
BRPI0614804A2 (pt) 2005-08-09 2011-04-12 Irm Llc compostos e composições como inibidores de proteìna cinase
JP5321061B2 (ja) 2005-08-11 2013-10-23 アリアド・ファーマシューティカルズ・インコーポレイテッド 不飽和複素環誘導体
EP1919924A2 (en) 2005-08-16 2008-05-14 Irm, Llc Compounds and compositions as protein kinase inhibitors
US7973060B2 (en) 2005-10-13 2011-07-05 Crystalgenomics, Inc. Fab I inhibitor and process for preparing same
WO2007042299A1 (en) 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
US8101625B2 (en) 2005-10-21 2012-01-24 Exelixis, Inc. Pyrimidinones as Casein Kinase II (CK2) modulators
US8592433B2 (en) 2005-10-28 2013-11-26 Advait Nagle Compounds and compositions as protein kinase inhibitors
NZ592990A (en) 2005-11-01 2013-01-25 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
AU2006311910A1 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors
PL1948180T3 (pl) 2005-11-11 2013-09-30 Boehringer Ingelheim Int Terapia skojarzona raka polegająca na podawaniu inhibitorów EGFR/HER2
CN101326182B (zh) 2005-12-05 2011-09-28 史密丝克莱恩比彻姆公司 2-嘧啶基吡唑并吡啶ErbB激酶抑制剂
US20080318989A1 (en) 2005-12-19 2008-12-25 Burdick Daniel J Pyrimidine Kinase Inhibitors
DE102005062742A1 (de) 2005-12-22 2007-06-28 Bayer Schering Pharma Ag Sulfoximin substituierte Pyrimidine, Verfahren zu deren Herstellung und ihre Verwendung als Arzneimittel
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
CA2640398A1 (en) 2006-01-30 2007-08-09 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them
CA2637225A1 (en) 2006-02-06 2007-08-16 Irm Llc Compounds and compositions as protein kinase inhibitors
US7569561B2 (en) 2006-02-22 2009-08-04 Boehringer Ingelheim International Gmbh 2,4-diaminopyrimidines useful for treating cell proliferation diseases
US20070208164A1 (en) 2006-02-27 2007-09-06 Wyeth Methods of synthesizing radiolabeled 3-cyano[14C]quinolines
CA2645958C (en) 2006-03-30 2014-11-04 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-amido substituted pyrimidines
CN101410394B (zh) 2006-03-30 2012-02-08 泰博特克药品有限公司 抑制人免疫缺陷病毒的5-(羟基亚甲基和氨基亚甲基)取代的嘧啶
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
US7601716B2 (en) 2006-05-01 2009-10-13 Cephalon, Inc. Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
CA2650611A1 (en) 2006-05-15 2007-11-29 Irm Llc Compositions and methods for fgf receptor kinases inhibitors
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR and ABL kinase modulators
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
JP2009544592A (ja) 2006-07-21 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｊａｋキナーゼ阻害剤としての２，４−ジ（アリールアミノ）−ピリミジン−５−カルボキサミド化合物
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
US8314234B2 (en) 2006-09-25 2012-11-20 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
CA2598893C (en) 2006-10-11 2012-04-10 Astellas Pharma Inc. Eml4-alk fusion gene
JP5513118B2 (ja) 2006-10-19 2014-06-04 シグナル ファーマシューティカルズ，エルエルシー ヘテロアリール化合物、その組成物、及びプロテインキナーゼ阻害剤としてのそれらの使用
ATE497496T1 (de) 2006-10-19 2011-02-15 Rigel Pharmaceuticals Inc 2,4-pyridimediamon-derivate als hemmer von jak- kinasen zur behandlung von autoimmunerkrankungen
TWI432427B (zh) 2006-10-23 2014-04-01 Cephalon Inc 作為ＡＬＫ及ｃ-ＭＥＴ抑制劑之２，４-二胺基嘧啶之融合雙環衍生物
US8236823B2 (en) 2006-10-27 2012-08-07 Amgen Inc. Multi-cyclic compounds and methods of use
US8039479B2 (en) 2006-12-08 2011-10-18 Irm Llc Compounds and compositions as protein kinase inhibitors
BRPI0720264B1 (pt) 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
CN101563327A (zh) 2006-12-19 2009-10-21 健泰科生物技术公司 嘧啶类激酶抑制剂
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
KR20090103897A (ko) 2006-12-28 2009-10-01 다이쇼 세이야꾸 가부시끼가이샤 피라졸로피리미딘 화합물
CN106045965A (zh) 2006-12-29 2016-10-26 爱尔兰詹森科学公司 抑制hiv的5,6‑取代的嘧啶类化合物
JP5185283B2 (ja) 2006-12-29 2013-04-17 テイボテク・フアーマシユーチカルズ Ｈｉｖ阻害６−置換ピリミジン
FR2911138B1 (fr) 2007-01-05 2009-02-20 Sanofi Aventis Sa Nouveaux derives de n, n'-2,4-dianilinopyrimidines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
AR065015A1 (es) 2007-01-26 2009-05-13 Smithkline Beecham Corp Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
MX2009007944A (es) 2007-01-26 2009-08-07 Irm Llc Compuestos y composiciones de purina como inhibidores de quinasa para el tratamiento de enfermedades relacionadas con plasmodium.
ES2702362T3 (es) 2007-01-31 2019-02-28 Ym Biosciences Australia Pty Compuestos a base de tiopirimidina y usos de los mismos
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
MX2009010047A (es) 2007-03-20 2009-12-04 Smithkline Beecham Corp Compuestos quimicos.
AU2008229147A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
SG179437A1 (en) 2007-03-30 2012-04-27 Sanofi Aventis Pyrimidine hydrazide compounds as pgds inhibitors
WO2008151183A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
ES2417148T3 (es) 2007-06-08 2013-08-06 Genentech, Inc. Marcadores de expresión génica de la resistencia tumoral al tratamiento con inhibidor de HER2
US20110053932A1 (en) 2007-06-21 2011-03-03 Irm Llc Protein Kinase Inhibitors and Methods for Using Thereof
TWI389893B (zh) 2007-07-06 2013-03-21 Astellas Pharma Inc 二（芳胺基）芳基化合物
KR20100049068A (ko) 2007-07-17 2010-05-11 리겔 파마슈티칼스, 인크. Ｐｋｃ 억제제로서의 시클릭 아민 치환된 피리미딘디아민
US7981903B2 (en) 2007-08-08 2011-07-19 Glaxosmithkline Llc 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer
WO2009032694A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
AU2008296545B2 (en) 2007-08-28 2011-09-29 Irm Llc 2 -biphenylamino-4 -aminopyrimidine derivatives as kinase inhibitors
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2707046A1 (en) 2007-11-28 2009-06-11 Nathanael S. Gray Small molecule myristate inhibitors of bcr-abl and methods of use
CA2707653A1 (en) 2007-12-03 2009-06-11 Boehringer Ingelheim International Gmbh Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
US20110028405A1 (en) 2007-12-20 2011-02-03 Richard John Harrison Sulfamides as zap-70 inhibitors
KR20150117305A (ko) 2007-12-21 2015-10-19 셀진 아빌로믹스 리서치, 인코포레이티드 Ｈｃｖ 프로테아제 억제제 및 이의 용도
NZ586232A (en) 2007-12-21 2012-12-21 Avila Therapeutics Inc HCV protease inhibitors comprising a functionalised proline derivative
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
EP2229217A1 (en) 2008-01-14 2010-09-22 Irm Llc Compositions and methods for treating cancers
WO2009102446A2 (en) 2008-02-12 2009-08-20 The Brigham And Women's Hospital, Inc. Fish assay for eml4 and alk fusion in lung cancer
EP2599499A1 (en) 2008-03-05 2013-06-05 Novartis AG Use of pyrimidine derivatives for the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
KR20110002080A (ko) 2008-04-07 2011-01-06 아이알엠 엘엘씨 키나제 억제제로서의 화합물 및 조성물
JP5298187B2 (ja) 2008-04-07 2013-09-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
JP2011520785A (ja) 2008-04-16 2011-07-21 バイオリポックス エービー 薬剤としての使用のためのビスアリール化合物
CA2723185A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20130225528A1 (en) 2008-05-21 2013-08-29 Ariad Pharmaceuticals, Inc. Phosphorus Derivatives as Kinase Inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US20130225527A1 (en) 2008-05-21 2013-08-29 Ariad Pharmaceuticals, Inc. Phosphorus Derivatives as Kinase Inhibitors
ES2645689T3 (es) 2008-05-21 2017-12-07 Ariad Pharmaceuticals, Inc. Derivados de fósforo como inhibidores de quinasas
JP2011524365A (ja) 2008-06-11 2011-09-01 アイアールエム・リミテッド・ライアビリティ・カンパニー マラリアの処置に有用な化合物および組成物
US20110294836A1 (en) 2008-06-20 2011-12-01 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
RU2536584C2 (ru) 2008-06-27 2014-12-27 Авила Терапьютикс, Инк. Гетероарильные соединения и их применение
EA201100423A1 (ru) 2008-09-02 2011-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Новые бензамиды, их получение и их применение в качестве лекарственных средств
JP2012501983A (ja) 2008-09-03 2012-01-26 バイエル・クロップサイエンス・アーゲー ４−アルキル−置換ジアミノピリミジン類
CN105574346A (zh) 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
WO2010044885A2 (en) 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
CA2744563A1 (en) 2008-12-12 2010-06-17 Ariad Pharmaceuticals, Inc. Azaindole derivatives as kinase inhibitors
WO2010072155A1 (zh) 2008-12-26 2010-07-01 复旦大学 一种嘧啶类衍生物及其制备方法和用途
WO2010080712A2 (en) 2009-01-06 2010-07-15 Dana Farber Cancer Institute Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
PL2881402T3 (pl) 2009-02-12 2017-10-31 Cell Signaling Technology Inc Ekspresja zmutowanej ROS w ludzkim raku wątroby
TW201035088A (en) 2009-02-27 2010-10-01 Supergen Inc Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors
US20110071158A1 (en) 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
CA2757671A1 (en) 2009-04-03 2010-10-07 Cellzome Ag Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
US8410126B2 (en) 2009-05-29 2013-04-02 Boehringer Ingelheim International Gmbh Pyrimidine inhibitors of PKTK2
CA2763717A1 (en) 2009-06-10 2010-12-16 Cellzome Limited Pyrimidine derivatives as zap-70 inhibitors
WO2010146132A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
ES2608670T3 (es) 2009-08-17 2017-04-12 Memorial Sloan-Kettering Cancer Center Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos
AU2010292198A1 (en) 2009-09-09 2012-04-05 Celgene Avilomics Research, Inc. PI3 kinase inhibitors and uses thereof
IN2012DN02534A (ru) 2009-09-16 2015-08-28 Avila Therapeutics Inc
KR20120094920A (ko) 2009-09-25 2012-08-27 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피리미딘 유도체의 제조 방법
BR112012009751A2 (pt) 2009-10-26 2020-09-24 Signal Pharmaceuticals, Llc métodos de síntese e purificação de heteroarila
US20110207736A1 (en) 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
BR112012015721A2 (pt) 2009-12-30 2017-09-26 Avila Therapeutics Inc modificação covalente de proteínas dirigida por ligante
CA2789711C (en) 2010-02-17 2014-08-05 Amgen Inc. Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain
US8383793B2 (en) 2010-04-15 2013-02-26 St. Jude Children's Research Hospital Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US8497265B2 (en) 2010-05-13 2013-07-30 Amgen Inc. Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors
LT2585470T (lt) * 2010-06-23 2017-04-10 Hanmi Science Co., Ltd. Nauji kondensuoti pirimidino dariniai tirozino kinazės aktyvumo slopinimui
IT1401326B1 (it) 2010-07-29 2013-07-18 Parlux S P A Dispositivo silenziatore per asciugacapelli.
US8563568B2 (en) 2010-08-10 2013-10-22 Celgene Avilomics Research, Inc. Besylate salt of a BTK inhibitor
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
CN103153064B (zh) * 2010-10-14 2015-04-22 阿里亚德医药股份有限公司 抑制egfr导致的癌症中细胞增殖的方法
CN103269704B (zh) 2010-11-01 2018-07-06 西建卡尔有限责任公司 杂环化合物和其用途
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
ES2665013T3 (es) 2010-11-10 2018-04-24 Celgene Car Llc Inhibidores de EGFR selectivos de mutante y usos de los mismos
KR101884010B1 (ko) 2011-05-04 2018-07-31 어리어드 파마슈티칼스, 인코포레이티드 Egfr-유도된 암의 세포 증식을 억제하는 화합물
AU2012288626C1 (en) 2011-07-27 2015-09-17 Astrazeneca Ab 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as EGFR modulators useful for treating cancer
CA2847540C (en) 2011-09-22 2016-05-17 Pfizer Inc. Pyrrolopyrimidine and purine derivatives
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
JP6468611B2 (ja) 2014-05-13 2019-02-13 アリアド ファーマシューティカルズ， インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
CA2949793C (en) 2014-06-19 2024-02-27 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
EP3209647B1 (en) 2014-10-21 2020-06-03 ARIAD Pharmaceuticals, Inc. Crystalline forms of 5-chloro-n4-[-2-(dimethylphosphoryl) phenyl]-n2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl]pyrimidine-2,4-diamine
JP6863901B2 (ja) 2015-05-13 2021-04-28 アリアド ファーマシューティカルズ， インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2649001C1 (ru) * 2014-02-25 2018-03-29 Шанхай Хайянь Фармасьютикал Текнолоджи Ко., Лтд. Производные 2,4-дизамещенного фенилен-1,5-диамина и их применения, фармацевтические композиции и фармацевтически приемлемые композиции, полученные из них

Also Published As

Publication number Publication date
MX2013012895A (es) 2014-02-17
WO2012151561A1 (en) 2012-11-08
IL228739A0 (en) 2013-12-31
EP2704572A1 (en) 2014-03-12
BR112013027734A2 (pt) 2017-08-08
US20120316135A1 (en) 2012-12-13
CN103501612A (zh) 2014-01-08
AU2012250517A1 (en) 2013-05-02
JP2014514348A (ja) 2014-06-19
US9834518B2 (en) 2017-12-05
CA2832504C (en) 2019-10-01
EP2704572A4 (en) 2014-11-05
JP5999177B2 (ja) 2016-09-28
EP2704572B1 (en) 2015-12-30
IL228739B (en) 2018-10-31
CN103501612B (zh) 2017-03-29
AU2012250517B2 (en) 2016-05-19
KR101884010B1 (ko) 2018-07-31
KR20140028057A (ko) 2014-03-07
MX360404B (es) 2018-10-31
CA2832504A1 (en) 2012-11-08

Similar Documents

Publication Publication Date Title
EA201391626A1 (ru) Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
PH12017502141A1 (en) Compounds and their methods of use
GEP201706624B (en) Triazolopyrazine as brd4 inhibitors and usage thereof for cancer treatment
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
MA34064B1 (fr) Compose heterocyclique
MX2015012427A (es) Compuestos de morfolinona de acido heteroarilo como inhibidores mdm2 para el tratamiento de cancer.
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201200323A1 (ru) Соединения и композиции, как ингибиторы протеинкиназы
MX352975B (es) Piridina y derivados de pirazina.
NZ700612A (en) Methods and compositions for treating ewings sarcoma family of tumors
EA201692114A1 (ru) Замещенные дигидроизохинолиноновые соединения
EA201170832A1 (ru) Пуриновые соединения
MX2014012477A (es) Inhibidores pirrolopirazona de tanquirasa.
EA201300610A1 (ru) Хиназолинкарбоксамидазетидины
EA201490688A1 (ru) 2-тиопиримидиноны
EA201490846A1 (ru) Новые производные арилхинолина
MX2013012977A (es) Derivados de tiazol.
EP2670763A1 (en) Certain chemical entities, compositions, and methods
EA201200046A1 (ru) Новые соединения, фармацевтическая композиция и связанные с ними способы
EA201591024A1 (ru) Димерные соединения
EA201400339A1 (ru) Новые имидазоламины в качестве модуляторов киназной активности
EA201201676A1 (ru) Гетероарильные соединения и композиции в качестве ингибиторов протеинкиназы
EA201200247A1 (ru) Новые азагетероциклические соединения
EA201691177A1 (ru) Ингибиторы серин/треонинкиназ
MX2014003376A (es) Derivados de acido benzoico como inhibidores eif4e.