JP2011523646A - キナーゼ阻害剤としてのリン誘導体 - Google Patents

キナーゼ阻害剤としてのリン誘導体 Download PDF

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JP2011523646A
JP2011523646A JP2011510716A JP2011510716A JP2011523646A JP 2011523646 A JP2011523646 A JP 2011523646A JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011523646 A JP2011523646 A JP 2011523646A
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ring
compound
phenyl
compounds
general formula
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JP2011523646A5 (OSRAM
Inventor
ワン、イーハン
ホワン、ウェイ−シェン
リゥ、シュアンギン
シェークスピア、ウィリアム・シー
トーマス、アール・マシュー
チー、ジーウェイ
リー、フェン
チュー、シャオチァン
コールマン、アンナ
ダルガーノ、ディビッド・シー
ロメロ、ジャン・アントワネット・シー
ツォウ、ドン
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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
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    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/6533Six-membered rings
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    • A61K31/33Heterocyclic compounds
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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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
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    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
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    • C07F9/02Phosphorus compounds
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    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
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    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/65616Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
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    • C07F9/6568Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • C07F9/65685Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
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    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65846Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system

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  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
JP2011510716A 2008-05-21 2009-05-21 キナーゼ阻害剤としてのリン誘導体 Withdrawn JP2011523646A (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US12831708P 2008-05-21 2008-05-21
US61/128,317 2008-05-21
US13749008P 2008-07-31 2008-07-31
US61/137,490 2008-07-31
US18879608P 2008-08-13 2008-08-13
US61/188,796 2008-08-13
US19293808P 2008-09-23 2008-09-23
US19296408P 2008-09-23 2008-09-23
US61/192,938 2008-09-23
US61/192,964 2008-09-23
PCT/US2009/044918 WO2009143389A1 (en) 2008-05-21 2009-05-21 Phosphorous derivatives as kinase inhibitors

Related Child Applications (1)

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JP2015087857A Division JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体

Publications (2)

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JP2011523646A true JP2011523646A (ja) 2011-08-18
JP2011523646A5 JP2011523646A5 (OSRAM) 2012-07-05

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JP2011510716A Withdrawn JP2011523646A (ja) 2008-05-21 2009-05-21 キナーゼ阻害剤としてのリン誘導体
JP2015087857A Active JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体
JP2017091616A Active JP6271064B2 (ja) 2008-05-21 2017-05-02 キナーゼ阻害剤としてのリン誘導体
JP2017248633A Active JP6483233B2 (ja) 2008-05-21 2017-12-26 キナーゼ阻害剤としてのリン誘導体
JP2019023097A Active JP6690032B2 (ja) 2008-05-21 2019-02-13 キナーゼ阻害剤としてのリン誘導体
JP2020069505A Pending JP2020125308A (ja) 2008-05-21 2020-04-08 キナーゼ阻害剤としてのリン誘導体
JP2022079291A Pending JP2022116057A (ja) 2008-05-21 2022-05-13 キナーゼ阻害剤としてのリン誘導体
JP2024074178A Pending JP2024102203A (ja) 2008-05-21 2024-05-01 キナーゼ阻害剤としてのリン誘導体

Family Applications After (7)

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JP2015087857A Active JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体
JP2017091616A Active JP6271064B2 (ja) 2008-05-21 2017-05-02 キナーゼ阻害剤としてのリン誘導体
JP2017248633A Active JP6483233B2 (ja) 2008-05-21 2017-12-26 キナーゼ阻害剤としてのリン誘導体
JP2019023097A Active JP6690032B2 (ja) 2008-05-21 2019-02-13 キナーゼ阻害剤としてのリン誘導体
JP2020069505A Pending JP2020125308A (ja) 2008-05-21 2020-04-08 キナーゼ阻害剤としてのリン誘導体
JP2022079291A Pending JP2022116057A (ja) 2008-05-21 2022-05-13 キナーゼ阻害剤としてのリン誘導体
JP2024074178A Pending JP2024102203A (ja) 2008-05-21 2024-05-01 キナーゼ阻害剤としてのリン誘導体

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US (5) US9012462B2 (OSRAM)
EP (2) EP3210609A1 (OSRAM)
JP (8) JP2011523646A (OSRAM)
KR (3) KR101860057B1 (OSRAM)
CN (1) CN102105150B (OSRAM)
AU (1) AU2009248923B2 (OSRAM)
BR (1) BRPI0908637B8 (OSRAM)
CA (1) CA2723961C (OSRAM)
CY (2) CY1119534T1 (OSRAM)
DK (1) DK2300013T4 (OSRAM)
EA (1) EA029131B1 (OSRAM)
ES (1) ES2645689T5 (OSRAM)
FI (2) FI2300013T4 (OSRAM)
FR (1) FR19C1033I2 (OSRAM)
HR (1) HRP20171534T4 (OSRAM)
HU (2) HUE035029T2 (OSRAM)
IL (2) IL208716B (OSRAM)
LT (2) LT2300013T (OSRAM)
LU (1) LUC00120I2 (OSRAM)
MX (2) MX353308B (OSRAM)
NL (1) NL300990I2 (OSRAM)
NO (2) NO2300013T3 (OSRAM)
PL (1) PL2300013T5 (OSRAM)
PT (1) PT2300013T (OSRAM)
SI (1) SI2300013T2 (OSRAM)
WO (1) WO2009143389A1 (OSRAM)

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012528864A (ja) * 2009-06-01 2012-11-15 オーエスアイ・ファーマシューティカルズ,エルエルシー アミノピリミジン抗癌性化合物
JP2015163621A (ja) * 2008-05-21 2015-09-10 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 キナーゼ阻害剤としてのリン誘導体
JP2015535266A (ja) * 2012-11-06 2015-12-10 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2017516825A (ja) * 2014-05-30 2017-06-22 ベイジン・パール・バイオテクノロジー・リミテッド・ライアビリティ・カンパニー Alkキナーゼ阻害剤並びにその調製方法及び使用
JP2017518336A (ja) * 2014-06-17 2017-07-06 コリア リサーチ インスティチュート オブ ケミカル テクノロジーKorea Research Institute Of Chemical Technology ピリミジン‐2,4‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物
JP2017535538A (ja) * 2014-10-21 2017-11-30 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]ピリミジン−2,4−ジアミンの結晶形態
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
JP2018515514A (ja) * 2015-05-13 2018-06-14 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
JP2018536667A (ja) * 2015-11-27 2018-12-13 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. 重水素化されたBrigatinib誘導体、かかる誘導体を含む薬学的組成物、並びにそれらの使用
JP2019535673A (ja) * 2016-10-21 2019-12-12 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
JP2020503271A (ja) * 2016-11-30 2020-01-30 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 造血前駆体キナーゼ1(hpk1)阻害剤としてのアニリノピリミジンas
JP2021506937A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのアリールホスフィンオキシド
JP2021506942A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP2021506820A (ja) * 2017-12-13 2021-02-22 上海科技大学Shanghai Tech University Alkタンパク質分解剤及びそれらの癌療法における使用
JP2021521163A (ja) * 2018-04-09 2021-08-26 上海科技大学Shanghai Tech University 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
JP2022508055A (ja) * 2018-11-01 2022-01-19 サイロス ファーマシューティカルズ, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
JP2022518723A (ja) * 2019-01-18 2022-03-16 ボロノイ・カンパニー・リミテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
JP2023507319A (ja) * 2019-12-16 2023-02-22 コリア リサーチ インスティチュート オブ ケミカル テクノロジー 新規なピリミジン誘導体及びその用途
JP2023513333A (ja) * 2020-02-14 2023-03-30 貝達薬業股▲ふん▼有限公司 キノリニル基ホスフィンオキシド化合物、並びにその組成物及び使用
JP2023532151A (ja) * 2020-07-03 2023-07-26 成都地奥九泓製薬廠 アリールリン酸化物化合物およびその使用
JP2024502175A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのイソインドリノンアミノピリミジン化合物、その組成物及び使用
JP2024502174A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのチエニル及びシクロアルキルアミノピリミジン化合物、その組成物及び使用

Families Citing this family (159)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI389893B (zh) 2007-07-06 2013-03-21 Astellas Pharma Inc 二(芳胺基)芳基化合物
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8846664B2 (en) 2008-11-12 2014-09-30 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
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
DK2428508T3 (en) 2009-05-08 2016-02-01 Astellas Pharma Inc Diamino heterocyclic carboxamide COMPOUND
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
RU2013109393A (ru) 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
BR112013008816A2 (pt) * 2010-10-14 2016-06-28 Ariad Pharma Inc método de tratamento de câncer direcionado ao egfr resistente à erlotinibe ou gefitinibe, ou uso de um sal farmacêuticamente aceito em um indivíduo
CA2815858C (en) 2010-11-01 2018-10-16 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
BR112013011600B1 (pt) 2010-11-10 2022-01-11 Genentech, Inc Derivados de pirazol aminopirimidina, seu uso e composição que os compreende
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
PL2646448T3 (pl) 2010-11-29 2017-12-29 OSI Pharmaceuticals, LLC Makrocykliczne inhibitory kinazy
CN114989139A (zh) * 2010-12-17 2022-09-02 诺华股份有限公司 制备嘧啶-2,4-二胺二盐酸盐的方法
WO2012110774A1 (en) 2011-02-17 2012-08-23 Cancer Therapeutics Crc Pty Limited Selective fak inhibitors
DK2675793T3 (en) 2011-02-17 2018-11-12 Cancer Therapeutics Crc Pty Ltd FAK INHIBITORS
CN103826641B (zh) * 2011-02-24 2018-09-07 江苏豪森药业集团有限公司 作为蛋白激酶抑制剂的含磷化合物
SG194086A1 (en) 2011-04-22 2013-11-29 Signal Pharm Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
EP2704572B1 (en) * 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CA2875025C (en) * 2011-05-31 2021-08-03 Newgen Therapeutics, Inc. Tricyclic inhibitors of poly(adp-ribose)polymerase
EP3409278B8 (en) 2011-07-21 2020-11-04 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
CA2853498A1 (en) 2011-10-28 2013-05-02 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
CN110194748A (zh) 2012-01-13 2019-09-03 艾森生物科学公司 杂环化合物及其作为抗癌药的用途
RU2711077C9 (ru) 2012-03-15 2020-08-11 Селджен Кар Ллс Соли ингибитора киназы рецептора эпидермального фактора роста
BR112014022789B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo
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
CN103420902A (zh) * 2012-05-18 2013-12-04 苏州爱斯鹏药物研发有限责任公司 一种2-氯-4-碘-5-甲基吡啶的制备方法
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
RU2509770C2 (ru) * 2012-06-22 2014-03-20 Общество с ограниченной ответственностью "Молекулярные Технологии" Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP2953457B1 (en) 2013-02-08 2020-04-08 Celgene CAR LLC Erk inhibitors and uses thereof
TW201522337A (zh) 2013-03-12 2015-06-16 Arqule Inc 經取代之三環吡唑並-嘧啶化合物類
US10202356B2 (en) * 2013-03-14 2019-02-12 Tolero Pharmaceuticals, Inc. JAK2 and ALK2 inhibitors and methods for their use
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CN103242341B (zh) * 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2,4取代嘧啶类化合物及其药物组合物与应用
CN104470921B (zh) * 2013-05-17 2017-05-03 上海恒瑞医药有限公司 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
AU2014287016B2 (en) 2013-07-11 2018-11-01 Acea Biosciences Inc. Pyrimidine derivatives as kinase inhibitors
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
EP3059227B1 (en) 2013-10-16 2019-06-26 FUJIFILM Corporation Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and flt3 inhibitor
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
KR101656382B1 (ko) 2014-02-28 2016-09-09 한국화학연구원 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물
WO2016004413A2 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
JP6619758B2 (ja) 2014-07-03 2019-12-11 ボード・オブ・リージエンツ,ザ・ユニバーシテイ・オブ・テキサス・システム 疾患を処置するためのgls1阻害薬
CN105330698B (zh) * 2014-07-04 2019-05-28 齐鲁制药有限公司 螺环芳基磷氧化物和硫化物
US10053477B2 (en) 2014-07-04 2018-08-21 Qilu Pharmaceutical Co., Ltd. Spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide
CN106459111B (zh) * 2014-08-07 2019-05-31 江苏豪森药业集团有限公司 一种抗癌化合物的晶型及其制备方法和用途
CN106661064B (zh) * 2014-08-07 2019-10-15 江苏豪森药业集团有限公司 一种抗癌化合物的新晶型及其制备方法和用途
CN105330697B (zh) * 2014-08-07 2019-05-28 江苏豪森药业集团有限公司 一种抗癌化合物的晶型及其制备方法和用途
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
BR112017003186A2 (pt) 2014-08-22 2017-11-28 Fujifilm Corp composição farmacêutica para tratamento de cancer positivo para mutação em flt3, inibidor de flt3 mutante e usos dos mesmos
KR101633722B1 (ko) 2014-10-08 2016-06-28 한국화학연구원 4-(1-퍼롤-3,4-디카르복시아미드)피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
SG11201704827UA (en) 2014-12-16 2017-07-28 Signal Pharm Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
WO2016100308A1 (en) 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-jun n-terminal kinase in skin
EP3250557B1 (en) 2015-01-29 2024-11-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN105985317B (zh) * 2015-02-12 2018-09-18 正大天晴药业集团股份有限公司 一种色瑞替尼的制备方法及其中间体
KR101772134B1 (ko) 2015-04-14 2017-08-29 한국화학연구원 N2-(2-메톡시페닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효 성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN106146468B (zh) * 2015-04-17 2020-12-01 杭州雷索药业有限公司 吡啶酮类蛋白激酶抑制剂
KR101653571B1 (ko) 2015-04-22 2016-09-05 한국화학연구원 4-(2-아미노-테트라하이드로나프탈렌닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN104892526A (zh) * 2015-06-17 2015-09-09 药源药物化学(上海)有限公司 一种2,5-二氯-n-(2-(异丙基磺酰基)苯基)嘧啶-4-胺的制备方法
ES2794868T3 (es) 2015-06-30 2020-11-19 Univ Texas Inhibidores de GLS1 para el tratamiento de enfermedades
CN106336398A (zh) * 2015-07-06 2017-01-18 杭州雷索药业有限公司 2‑饱和环基取代的苯胺类蛋白激酶抑制剂
JP6412471B2 (ja) 2015-07-15 2018-10-24 富士フイルム株式会社 含窒素複素環化合物の製造方法およびその中間体
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
CN107922287B (zh) 2015-07-24 2021-04-09 细胞基因公司 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体
CN105061506B (zh) * 2015-07-27 2017-08-29 苏州明锐医药科技有限公司 抗肿瘤药物ap26113的制备方法
CN106478700B (zh) * 2015-08-26 2020-12-29 杭州雷索药业有限公司 硼基取代的苯胺类蛋白激酶抑制剂
RU2018115334A (ru) 2015-10-09 2019-11-11 Ацея Терапьютикс, Инк. Фармацевтические соли, физические формы и композиции пирролопиримидиновых ингибиторов киназ, и способы их получения
CN106699810A (zh) * 2015-11-17 2017-05-24 清华大学 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用
RU2606951C1 (ru) * 2015-11-19 2017-01-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных N4-[2-(диметилфосфорил)фенил]-N2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов ALK и EGFR, предназначенных для лечения рака
CN108948082A (zh) * 2015-12-02 2018-12-07 深圳市塔吉瑞生物医药有限公司 一种二氨基嘧啶化合物及包含该化合物的组合物
CN105294759B (zh) * 2015-12-02 2018-01-19 苏州东南药业股份有限公司 一种抗肿瘤药物的制备方法
SG11201804664XA (en) 2015-12-22 2018-07-30 Univ Texas Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1h-1,2,3-triazole-4-carboxamide
CN109071512A (zh) * 2016-02-03 2018-12-21 重庆复创医药研究有限公司 作为激酶抑制剂的含磷化合物
JP6911019B2 (ja) 2016-05-17 2021-07-28 公益財団法人がん研究会 Egfr−tki耐性を獲得した肺癌の治療薬
CN106220608B (zh) * 2016-07-25 2018-11-27 安润医药科技(苏州)有限公司 二苯氨基嘧啶及三嗪化合物、其药用组合物及用途
CN107698603B (zh) * 2016-08-09 2022-04-08 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用
WO2018077187A1 (zh) * 2016-10-25 2018-05-03 苏州晶云药物科技有限公司 Ap26113的新晶型及其制备方法
WO2018108064A1 (zh) * 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物
KR102602558B1 (ko) * 2016-12-13 2023-11-14 브리스톨-마이어스 스큅 컴퍼니 Il-12, il-23 및/또는 ifn 알파 반응의 조정제로서의 포스핀 옥시드 알킬 아미드 치환된 헤테로아릴 화합물
WO2018165145A1 (en) 2017-03-08 2018-09-13 Ariad Pharmaceuticals, Inc. Pharmaceutical formulations comprising 5-chloro-n4-[2-(dimethylphosphoryl) phenyl]-n2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl} pyrimidine-2,4-diamine
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
JOP20190281A1 (ar) 2017-06-13 2019-12-02 Korea Res Inst Chemical Tech مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه
EP3697764B1 (en) 2017-10-18 2025-06-11 Board Of Regents, The University Of Texas System Gls-1 inhibitors for use in the treatment of cancer
WO2019112344A1 (ko) 2017-12-07 2019-06-13 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
KR101992621B1 (ko) 2017-12-07 2019-09-27 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
WO2019143730A1 (en) 2018-01-16 2019-07-25 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3740207A4 (en) 2018-01-16 2021-10-13 Syros Pharmaceuticals, Inc. CYCLINE-DEPENDENT KINASE 7 (CDK7) INHIBITORS
WO2019148789A1 (zh) * 2018-02-02 2019-08-08 苏州科睿思制药有限公司 布格替尼的晶型及其制备方法
CN109851638B (zh) * 2018-02-07 2022-05-31 深圳市塔吉瑞生物医药有限公司 取代的二氨基嘧啶化合物
EP3752132B1 (en) 2018-02-13 2021-12-08 Sandoz AG Pharmaceutical composition of brigatinib
EP3768275A1 (en) 2018-03-19 2021-01-27 ARIAD Pharmaceuticals, Inc. Methods of treating cancer in pediatric patients
CN110305161A (zh) * 2018-03-20 2019-10-08 暨南大学 2-氨基嘧啶类化合物及其应用
US20210113562A1 (en) 2018-04-13 2021-04-22 Sumitomo Dainippon Pharma Oncology, Inc. Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer
CN110467637B (zh) * 2018-05-09 2022-02-18 北京赛特明强医药科技有限公司 一种含有氧化膦类取代苯胺的双氨基氯代嘧啶类化合物、制备方法及其应用
CN110467638A (zh) * 2018-05-09 2019-11-19 北京赛特明强医药科技有限公司 一种含有间氯苯胺类取代基的双氨基氯代嘧啶类化合物、制备方法及其应用
WO2019223777A1 (zh) * 2018-05-24 2019-11-28 北京赛特明强医药科技有限公司 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用
CN110526941A (zh) * 2018-05-24 2019-12-03 北京赛特明强医药科技有限公司 一种含有间氯苯胺类取代基的吡咯并嘧啶类化合物、制备方法及其应用
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
CN109053693B (zh) * 2018-09-20 2021-02-05 顺毅股份有限公司 哒嗪胺类化合物的制备及其应用
WO2020080979A1 (en) * 2018-10-15 2020-04-23 Gero Discovery Limited Liability Company Pfkfb3 inhibitors and their uses
CN112771032B (zh) * 2018-10-29 2023-01-03 江苏先声药业有限公司 作为第四代egfr抑制剂的嘧啶吡唑类化合物
WO2020099483A1 (en) 2018-11-15 2020-05-22 Sandoz Ag Crystalline forms of brigatinib
CN113195000A (zh) 2018-12-21 2021-07-30 第一三共株式会社 抗体-药物缀合物和激酶抑制剂的组合
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
WO2020188467A1 (zh) * 2019-03-15 2020-09-24 杭州英创医药科技有限公司 作为激酶抑制剂的稠合三环化合物
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
CN111825719A (zh) * 2019-04-15 2020-10-27 北京赛特明强医药科技有限公司 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用
CN111848677B (zh) * 2019-04-29 2023-03-17 浙江同源康医药股份有限公司 一种alk激酶抑制剂化合物的晶型、制备方法及应用
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
CN112047978A (zh) * 2019-06-05 2020-12-08 北京赛思源生物医药技术有限公司 5-氯-n4-[2-(二甲基磷酰基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺新晶型
WO2021003417A1 (en) 2019-07-03 2021-01-07 Sumitomo Dainippon Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof
KR20220042159A (ko) 2019-08-01 2022-04-04 인테그랄 바이오사이언스 피브이티. 엘티디. 키나제 억제제로서의 헤테로사이클릭 화합물 및 이의 용도
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
CN110713497A (zh) * 2019-10-30 2020-01-21 成都海杰亚医药科技有限公司 一种Brigatinib的中间体2-氨基苯基二甲基氧化膦制备方法
KR102168179B1 (ko) 2019-10-31 2020-10-20 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 헤테로 고리 치환 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
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
JP2023507943A (ja) 2019-12-16 2023-02-28 オンコビクス・カンパニー・リミテッド 新規な重水素置換ピリミジン誘導体及びこれを含む薬剤学的組成物
WO2021125803A1 (ko) * 2019-12-16 2021-06-24 한국화학연구원 신규한 피리미딘 유도체 및 이의 용도
CN111138492B (zh) * 2020-01-06 2022-08-02 沈阳药科大学 Alk抑制剂布格替尼的制备方法
CN111620852B (zh) * 2020-01-19 2023-05-09 镇江植生源农业科技有限公司 一种5-氯-嘧啶-2,4-二胺类化合物及其制备方法和应用
US20230049130A1 (en) * 2020-01-19 2023-02-16 Crystal Pharmaceutical (Suzhou) Co., Ltd. Deucravacitinib crystal form, preparation method therefor and use thereof
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115443269A (zh) 2020-03-31 2022-12-06 施万生物制药研发Ip有限责任公司 经取代的嘧啶和使用方法
CN112225703B (zh) * 2020-09-28 2022-03-11 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
KR20220081631A (ko) 2020-12-09 2022-06-16 보로노이 주식회사 염증성 질환의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도
MX2023009685A (es) 2021-02-19 2023-10-30 Sudo Biosciences Ltd Inhibidores de tyk2 y sus usos.
WO2022175747A1 (en) 2021-02-19 2022-08-25 Sudo Biosciences Limited Tyk2 inhibitors and uses 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
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
EP4330251A4 (en) * 2021-04-30 2025-03-05 BeiGene Switzerland GmbH EGFR DEGRADING AGENTS AND METHODS OF USE THEREOF
WO2022253081A1 (zh) * 2021-06-03 2022-12-08 希格生科(深圳)有限公司 氧化膦衍生物及其制备方法和应用
CN117500813A (zh) * 2021-06-17 2024-02-02 微境生物医药科技(上海)有限公司 芳基氧膦类化合物
EP4393930A4 (en) * 2021-08-27 2025-07-16 Chengdu Diao Jiuhong Pharmaceutical Factory CRYSTALLINE FORMS, PREPARATION METHOD AND APPLICATION OF AN ARYL PHOSPHINE OXIDE COMPOUND
TW202333667A (zh) * 2021-12-13 2023-09-01 大陸商希格生科(深圳)有限公司 嘧啶或吡啶類衍生物及其醫藥用途
WO2023204822A1 (en) * 2022-04-22 2023-10-26 Vivace Therapeutics, Inc. Phenyl phosphine oxide compounds and methods of use thereof
CN115260234A (zh) * 2022-07-01 2022-11-01 江苏医药职业学院 一种2-氨基-4-氨基芳基磷氧基嘧啶化合物及其制备方法与应用
CN115154473A (zh) * 2022-08-04 2022-10-11 中国人民解放军陆军特色医学中心 布格替尼作为axl、c-met、st3gal4抑制剂的新应用
CN115448906B (zh) * 2022-09-26 2024-04-02 深圳大学 一种2-苯胺基嘧啶类衍生物及其制备方法与应用
CN120112538A (zh) 2022-10-13 2025-06-06 拜耳公司 Sos1抑制剂
TW202432145A (zh) * 2022-10-27 2024-08-16 大陸商勤浩醫藥(蘇州)有限公司 含磷化合物、藥物組合物及其應用
EP4611753A1 (en) 2022-10-31 2025-09-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
CN115785154B (zh) * 2022-12-01 2025-09-05 希格生科(深圳)有限公司 杂芳环化合物及其医药用途
CN116768885A (zh) * 2023-03-14 2023-09-19 浙江大学 N2-取代双环-2-氨基嘧啶类衍生物、其制备方法及医药用途
CN119019454A (zh) * 2023-05-23 2024-11-26 广州智睿医药科技有限公司 一种杂芳基衍生物的制备及用途
WO2024249831A2 (en) * 2023-06-02 2024-12-05 Unogen Biotech Ltd. Triple kinase inhibitors
US20240425484A1 (en) * 2023-06-02 2024-12-26 Atomwise Inc. Inhibitors of tyk2
TW202509078A (zh) 2023-07-07 2025-03-01 美商維里迪恩醫療股份有限公司 治療慢性甲狀腺眼病之方法
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma
CN119143806B (zh) * 2024-11-19 2025-03-11 四川大学华西医院 一种靶向egfr突变的二甲基氧膦取代的苯胺嘧啶衍生物、其制备方法、用途及其制成的药物

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20040242611A1 (en) * 2001-06-21 2004-12-02 Metcalf Chester A. Novel phenylamino-pyrimidines and uses thereof
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
JP2006524487A (ja) * 2002-04-26 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド 抗hiv治療化合物を同定するための方法および組成物
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
JP2007502260A (ja) * 2003-08-15 2007-02-08 ノバルティス アクチエンゲゼルシャフト 新生物疾患、炎症および免疫障害の処置に有用な2,4−ピリミジンジアミン
JP2007537234A (ja) * 2004-05-14 2007-12-20 ファイザー・プロダクツ・インク 異常な細胞増殖を処置するためのピリミジン誘導体

Family Cites Families (276)

* 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
US4736866A (en) 1984-06-22 1988-04-12 President And Fellows Of Harvard College Transgenic non-human mammals
EP0242081B1 (en) 1986-04-17 1994-04-27 Zeneca Limited 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
US5175383A (en) 1989-02-17 1992-12-29 President And Fellows Of Harvard College Animal model for benign prostatic disease
GB9016584D0 (en) 1990-07-27 1990-09-12 Ici Plc Fungicides
ATE167473T1 (de) 1990-08-20 1998-07-15 Eisai Co Ltd Sulfonamid-derivate
EP0542420A1 (en) 1991-11-15 1993-05-19 Zeneca Limited Anionic xanthene derivatives and their use in inks
TW225528B (OSRAM) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
AU693475B2 (en) 1993-10-01 1998-07-02 Novartis Ag Pyrimidineamine derivatives and processes for the preparation thereof
NZ274978A (en) 1993-10-12 1998-04-27 Du Pont Merck Pharma 1n-alkyl-n-aryl pyrimidinamine derivatives and pharmaceutical compositions thereof
CA2214685C (en) 1995-03-10 2008-05-20 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
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
WO1997020822A1 (en) 1995-12-01 1997-06-12 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
DK0929547T3 (da) 1996-09-12 2003-03-10 Schering Ag Benzamidinderivater substitueret af cykliske aminosyrederivater eller cykliske hydroxysyrederivater og deres anvendelse som antikoagulantia
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
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
WO1999031073A1 (en) 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
DE59905472D1 (de) 1998-06-10 2003-06-12 Basf Ag Verwendung von 2-(n-phenylamino)pyrimidinen als fungizide sowie neue 2-(n-phenylamino)pyrimidine
AU5648599A (en) 1998-09-11 2000-04-03 Kyorin Pharmaceutical Co. Ltd. Phosphonic ester derivatives and process for producing the same
AU762523C (en) 1998-11-10 2004-02-12 Janssen Pharmaceutica N.V. HIV replication inhibiting pyrimidines
SK286264B6 (sk) 1998-11-17 2008-06-06 Kumiai Chemical Industry Co., Ltd. Derivát pyrimidinylbenzimidazolu alebo triazinylbenzimidazolu, medziprodukty na jeho prípravu a poľnohospodársky/záhradnícky fungicíd s jeho obsahom
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
WO2000046203A2 (en) 1999-02-04 2000-08-10 Millennium Pharmaceuticals, Inc. 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
CA2386218A1 (en) 1999-10-07 2001-04-12 Amgen Inc. Triazine kinase inhibitors
ITMI992711A1 (it) 1999-12-27 2001-06-27 Novartis Ag Composti organici
US20030004174A9 (en) * 2000-02-17 2003-01-02 Armistead David M. 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
JP5230050B2 (ja) 2000-05-08 2013-07-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Hiv複製阻害剤
EP1282607B1 (en) 2000-05-08 2015-11-11 Janssen Pharmaceutica NV Prodrugs of hiv replication inhibiting pyrimidines
WO2002000024A1 (en) 2000-06-30 2002-01-03 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
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
BR0115909B1 (pt) 2000-12-05 2013-09-03 processo de tingimento tricromático
ATE430742T1 (de) 2000-12-21 2009-05-15 Smithkline Beecham Corp Pyrimidinamine als angiogenesemodulatoren
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
ATE317850T1 (de) 2001-05-30 2006-03-15 Novartis Pharma Gmbh 2-((n-(2-amino-3-(heteroaryl- oder - aryl)propionyl)aminoacyl)amino)- alkylboronsäurederivate
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
EP1408980A4 (en) 2001-06-21 2004-10-20 Ariad Pharma Inc NEW QUINAZOLINES AND THEIR USE
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
CA2463563A1 (en) 2001-10-12 2003-04-17 Irm Llc Kinase inhibitor scaffolds and methods for their preparation
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
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
EA007298B1 (ru) 2001-11-01 2006-08-25 Янссен Фармацевтика Н.В. Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)
IL162838A0 (en) 2002-01-04 2005-11-20 Univ Rockefeller Compositions and methods for prevention and treatment peptide-of amyloid- related disorders
KR100956195B1 (ko) 2002-02-01 2010-05-06 어리어드 파마슈티칼스, 인코포레이티드 인 함유 화합물 및 이의 용도
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
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
WO2003095448A1 (en) 2002-05-06 2003-11-20 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
EP1511473B8 (en) 2002-05-27 2013-07-24 Novartis AG Bis-aromatic alkanols
GB0217431D0 (en) 2002-07-27 2002-09-04 Astrazeneca Ab Novel compounds
ATE451104T1 (de) 2002-07-29 2009-12-15 Rigel Pharmaceuticals Inc Verfahren zur behandlung oder pruvention von autoimmunkrankheiten mit 2,4-pyrimidindiamin- verbindungen
ES2295685T3 (es) 2002-08-24 2008-04-16 Astrazeneca Ab Derivados de pirimidina como moduladores de la actividad del receptor de quimioquinas.
EP1562911B1 (en) 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
CN1747941A (zh) 2003-02-07 2006-03-15 詹森药业有限公司 抑制hiv的1,2,4-三嗪
US7256206B2 (en) 2003-02-11 2007-08-14 Irm Llc Bicyclic compounds and compositions
EP1597251B1 (en) 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimidine compounds
CL2004000306A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa.
WO2004078682A2 (en) 2003-03-05 2004-09-16 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
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
MXPA06001098A (es) 2003-07-29 2006-04-24 Irm Llc Compuestos y composiciones utiles como inhibidores de proteina cinasa.
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
EP1663242B1 (en) 2003-08-07 2011-04-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
MXPA06001758A (es) 2003-08-15 2006-08-11 Irm Llc Anilino purinas sustituidas en la posicion 6 utiles como inhibidores de rtk.
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
JP2007505858A (ja) 2003-09-18 2007-03-15 ノバルティス アクチエンゲゼルシャフト 増殖性障害の処置に有用な2,4−ジ(フェニルアミノ)ピリミジン
US7189729B2 (en) 2003-09-30 2007-03-13 Irm Llc Methods and compositions as protein kinase inhibitors
CN100455579C (zh) 2003-10-02 2009-01-28 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CA2542105C (en) 2003-10-08 2011-08-02 Irm Llc Compounds and compositions as protein kinase inhibitors
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
CA2545384A1 (en) 2003-11-10 2005-05-26 Merck Sharp & Dohme Limited Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
EP1690148B1 (de) 2003-12-01 2008-03-05 TUCHENHAGEN GmbH Verfahren zur zeitnahen überwachung, erfassung und übermittlung von prozessdaten
ATE497949T1 (de) 2003-12-03 2011-02-15 Ym Biosciences Australia Pty Tubulininhibitoren
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
AU2005206541A1 (en) 2004-01-16 2005-08-04 Wyeth Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
EP1713806B1 (en) 2004-02-14 2013-05-08 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
TW200610762A (en) 2004-06-10 2006-04-01 Irm Llc Compounds and compositions as protein kinase inhibitors
RU2007102226A (ru) 2004-06-23 2008-07-27 Айрм Ллк (Bm) Соединения и композиции в качестве ингибиторов протеинкиназы
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
ES2442857T3 (es) 2004-08-10 2014-02-13 Janssen Pharmaceutica Nv Derivados de 1,2,4-triazin-6-ona inhibidores de VIH
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
AU2005295788A1 (en) 2004-10-13 2006-04-27 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
ATE430747T1 (de) 2004-12-21 2009-05-15 Smithkline Beecham Corp 2-pyrimidinyl-pyrazolopyridin-erbb- kinaseinhibitoren
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
US20090105250A1 (en) 2005-01-26 2009-04-23 Irm Llc Compounds and compositions as protein kinase inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
AU2006227790B2 (en) 2005-03-15 2009-09-10 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2006227628A1 (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
EP1891066B1 (en) 2005-05-13 2010-12-22 Irm, Llc Compounds and compositions as protein kinase inhibitors
CN101218241B (zh) 2005-05-16 2011-02-16 Irm责任有限公司 用作蛋白激酶抑制剂的吡咯并吡啶衍生物
WO2006123165A2 (en) 2005-05-19 2006-11-23 Astex Therapeutics Limited Pyrimidine derivatives as hsp90 inhibitors
WO2006128172A2 (en) 2005-05-26 2006-11-30 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
US7491732B2 (en) 2005-06-08 2009-02-17 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
MX2007016066A (es) 2005-07-01 2008-03-10 Irm Llc Derivados de bencimidazol sustituidos por pirimidina como inhibidores de cinasa de proteina.
NZ566021A (en) 2005-07-26 2011-03-31 Vertex Pharma Benzimidazoles useful as inhibitors of protein kinases
AU2006275849A1 (en) 2005-08-02 2007-02-08 Irm Llc 5-substituted thiazol-2-yl amino compounds and compositions as protein kinase inhibitors
CA2617359A1 (en) 2005-08-09 2007-02-22 Irm Llc Compounds and compositions as protein kinase inhibitors
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
EP1948659A1 (en) 2005-10-13 2008-07-30 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
JP5376950B2 (ja) 2005-10-21 2013-12-25 エクセリクシス, インク. カゼインキナーゼii(ck2)モジュレーターとしてのピリミジオン類
PT1940844E (pt) 2005-10-28 2010-01-06 Scripps Research Inst Compostos e composições como inibidores de proteína-quinase
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
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
WO2007056151A2 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhbitors
EP1971606B1 (en) 2005-12-05 2013-04-24 GlaxoSmithKline LLC 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
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
KR20080110998A (ko) 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Jak­2 조절자로서 4­아릴­2­아미노­피리미딘 또는 4­아릴­2­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
BRPI0707666A2 (pt) 2006-02-06 2011-05-10 Irm Llc compostos e composiÇÕes como inibidores de proteÍna cinase
TW200804364A (en) 2006-02-22 2008-01-16 Boehringer Ingelheim Int New compounds
US20070208164A1 (en) 2006-02-27 2007-09-06 Wyeth Methods of synthesizing radiolabeled 3-cyano[14C]quinolines
BRPI0709690B8 (pt) 2006-03-30 2021-05-25 Janssen R & D Ireland 5-amido pirimidinas substituídas e composição farmacêutica que as compreende
ATE482953T1 (de) 2006-03-30 2010-10-15 Tibotec Pharm Ltd Hiv-inhibierende 5-(hydroxymethylen- und aminomethylen) substituierte pyrimidine
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
JP2009537520A (ja) 2006-05-15 2009-10-29 アイアールエム・リミテッド・ライアビリティ・カンパニー Fgf受容体キナーゼ阻害剤のための組成物および方法
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
CA2656290A1 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
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
WO2008049123A2 (en) 2006-10-19 2008-04-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases
CN105693730A (zh) 2006-10-19 2016-06-22 西格诺药品有限公司 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途
AU2007309427B2 (en) 2006-10-23 2013-02-28 Cephalon, Inc. Fused bicyclic derivatives of 2,4-diaminopyrimidine as ALK and c-Met inhibitors
WO2008057280A1 (en) 2006-10-27 2008-05-15 Amgen Inc. Multi-cyclic compounds and methods of use
JP5180967B2 (ja) 2006-11-03 2013-04-10 ブリストル−マイヤーズ スクイブ カンパニー ピロロトリアジンキナーゼ阻害剤
KR101149295B1 (ko) 2006-12-08 2012-07-05 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물
RS53588B1 (sr) 2006-12-08 2015-02-27 Irm Llc Jedinjenja i kompozicije kao inhibitori protein kinaza
CA2670645A1 (en) 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
US20100298557A1 (en) 2006-12-28 2010-11-25 Taisho Pharmaceutical Co., Ltd Pyrazolopyrimidine compound
KR20090094073A (ko) 2006-12-29 2009-09-03 티보텍 파마슈티칼즈 리미티드 Hiv를 억제하는 6-치환된 피리미딘
CN101573342A (zh) 2006-12-29 2009-11-04 泰博特克药品有限公司 抑制hiv的5,6-取代的嘧啶类化合物
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
KR20090112732A (ko) * 2007-01-26 2009-10-28 아이알엠 엘엘씨 플라스모듐 관련 질환의 치료를 위한 키나제 억제제로서의 퓨린 화합물 및 조성물
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
AU2008210266B2 (en) 2007-01-31 2013-09-05 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
TW200834459A (en) 2007-02-05 2008-08-16 Huper Lab Co Ltd Video object segmentation method applied for rainy situations
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
CN101677554A (zh) 2007-03-20 2010-03-24 史密丝克莱恩比彻姆公司 化合物
CN101686675A (zh) 2007-03-20 2010-03-31 史密丝克莱恩比彻姆公司 化合物
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
BRPI0809974A2 (pt) 2007-03-30 2014-10-07 Sanofi Aventis Compostos de pirimidina hidrazida como inibidores de pgds
CA2689989A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
KR20100035635A (ko) 2007-06-21 2010-04-05 아이알엠 엘엘씨 단백질 키나제 억제제 및 그의 사용 방법
TWI389893B (zh) 2007-07-06 2013-03-21 Astellas Pharma Inc 二(芳胺基)芳基化合物
WO2009012421A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
CN101827848B (zh) 2007-08-08 2012-11-07 葛兰素史密丝克莱恩有限责任公司 作为IGF-1R抑制剂用于治疗癌症的2-[(2-{苯基氨基}-1H-吡咯并[2,3-d]嘧啶-4-基)氨基]苯甲酰胺衍生物
CA2696824A1 (en) 2007-08-28 2009-03-12 Irm Llc Compounds and compositions as kinase inhibitors
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
CA2702674C (en) 2007-10-19 2016-05-03 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
KR20100130583A (ko) 2007-11-28 2010-12-13 다나-파버 캔서 인스티튜트 인크. Bcr-abl의 소 분자 미리스테이트 억제제 및 이의 사용 방법
EP2231620A1 (en) 2007-12-03 2010-09-29 Boehringer Ingelheim International GmbH Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
CN104557861A (zh) 2007-12-21 2015-04-29 阿维拉制药公司 Hcv蛋白酶抑制剂和其用途
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
EP2237666A4 (en) 2007-12-21 2012-05-16 Avila Therapeutics Inc HCV PROTEASE INHIBITORS AND USES THEREOF
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
US20110021524A1 (en) 2008-01-14 2011-01-27 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
WO2009109605A1 (en) 2008-03-05 2009-09-11 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
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited 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.
JP5214799B2 (ja) 2008-04-07 2013-06-19 アイアールエム・リミテッド・ライアビリティ・カンパニー キナーゼ阻害剤としての化合物および組成物
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
US20110071197A1 (en) 2008-04-16 2011-03-24 Peter Nilsson Bis-aryl compounds for use as medicaments
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20130225527A1 (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
PL2300013T5 (pl) * 2008-05-21 2025-04-28 Takeda Pharmaceutical Company Limited Pochodne fosforu jako inhibitor kinazy
US20130225528A1 (en) 2008-05-21 2013-08-29 Ariad Pharmaceuticals, Inc. Phosphorus Derivatives as Kinase Inhibitors
CN102089278A (zh) 2008-06-11 2011-06-08 Irm责任有限公司 用于治疗疟疾的化合物和组合物
CN102203074A (zh) 2008-06-20 2011-09-28 麦它波莱克斯股份有限公司 芳基gpr119激动剂及其用途
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8735579B2 (en) 2008-09-02 2014-05-27 Boehringer Ingelheim International Gmbh Benzamides, production thereof, and use thereof as medicaments
US20110230478A1 (en) 2008-09-03 2011-09-22 Bayer ScienceCrop AG 4-Alkyl-substituted diaminopyrimidines
CN102405284B (zh) 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
US8394818B2 (en) 2008-10-17 2013-03-12 Dana-Farber Cancer Institute, Inc. 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
US8846664B2 (en) 2008-11-12 2014-09-30 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
US8809343B2 (en) 2008-12-26 2014-08-19 Fudan University Pyrimidine derivative, preparation method and use thereof
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
DK2881402T3 (en) 2009-02-12 2017-08-28 Cell Signaling Technology Inc Mutant ROS expression in human liver cancer
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
WO2010112210A1 (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
US20120142667A1 (en) 2009-06-10 2012-06-07 Nigel Ramsden Pyrimidine derivatives as zap-70 inhibitors
CA2763720A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
CA2771190C (en) 2009-08-17 2020-01-21 Memorial Sloan-Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
JP2013504325A (ja) 2009-09-09 2013-02-07 アビラ セラピューティクス, インコーポレイテッド Pi3キナーゼインヒビターおよびその使用
EP2478361A4 (en) 2009-09-16 2014-05-21 Celgene Avilomics Res Inc CONJUGATES AND INHIBITORS OF PROTEIN KINASE
JP2013505927A (ja) 2009-09-25 2013-02-21 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法
CA2778615C (en) 2009-10-26 2019-04-23 Signal Pharmaceuticals, Llc Methods of synthesis and purification of heteroaryl compounds
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
US9334269B2 (en) 2010-02-17 2016-05-10 Amgen Inc. Carboxamides as inhibitors of voltage-gated sodium channels
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
RU2013109393A (ru) 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
BR112013008816A2 (pt) 2010-10-14 2016-06-28 Ariad Pharma Inc método de tratamento de câncer direcionado ao egfr resistente à erlotinibe ou gefitinibe, ou uso de um sal farmacêuticamente aceito em um indivíduo
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2815858C (en) 2010-11-01 2018-10-16 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2654177T3 (es) 2011-07-27 2018-02-12 Astrazeneca Ab Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer
PE20141228A1 (es) 2011-09-22 2014-10-01 Pfizer Derivados de pirrolopirimidina y purina
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

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20040242611A1 (en) * 2001-06-21 2004-12-02 Metcalf Chester A. Novel phenylamino-pyrimidines and uses thereof
JP2006524487A (ja) * 2002-04-26 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド 抗hiv治療化合物を同定するための方法および組成物
JP2007502260A (ja) * 2003-08-15 2007-02-08 ノバルティス アクチエンゲゼルシャフト 新生物疾患、炎症および免疫障害の処置に有用な2,4−ピリミジンジアミン
JP2007537234A (ja) * 2004-05-14 2007-12-20 ファイザー・プロダクツ・インク 異常な細胞増殖を処置するためのピリミジン誘導体
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
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

Cited By (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015163621A (ja) * 2008-05-21 2015-09-10 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 キナーゼ阻害剤としてのリン誘導体
JP2017186345A (ja) * 2008-05-21 2017-10-12 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 キナーゼ阻害剤としてのリン誘導体
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JP2018119003A (ja) * 2012-11-06 2018-08-02 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2015535266A (ja) * 2012-11-06 2015-12-10 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2017516825A (ja) * 2014-05-30 2017-06-22 ベイジン・パール・バイオテクノロジー・リミテッド・ライアビリティ・カンパニー Alkキナーゼ阻害剤並びにその調製方法及び使用
JP2017518336A (ja) * 2014-06-17 2017-07-06 コリア リサーチ インスティチュート オブ ケミカル テクノロジーKorea Research Institute Of Chemical Technology ピリミジン‐2,4‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物
JP2017535538A (ja) * 2014-10-21 2017-11-30 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]ピリミジン−2,4−ジアミンの結晶形態
JP2020063276A (ja) * 2014-10-21 2020-04-23 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]フェニル}ピリミジン−2,4−ジアミンの結晶形態
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
JP2018515514A (ja) * 2015-05-13 2018-06-14 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
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JP2020503271A (ja) * 2016-11-30 2020-01-30 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 造血前駆体キナーゼ1(hpk1)阻害剤としてのアニリノピリミジンas
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US11771709B2 (en) 2017-12-13 2023-10-03 Shanghaitech University ALK protein degradation agent and anti-tumor application thereof
JP2021506820A (ja) * 2017-12-13 2021-02-22 上海科技大学Shanghai Tech University Alkタンパク質分解剤及びそれらの癌療法における使用
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JP2021506937A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのアリールホスフィンオキシド
US11254696B2 (en) 2017-12-21 2022-02-22 Shenzhen Targetrx, Inc. Dianilinopyrimidine compound for inhibiting kinase activity
JP7043098B2 (ja) 2017-12-21 2022-03-29 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP2021506942A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP7085242B2 (ja) 2017-12-21 2022-06-16 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのアリールホスフィンオキシド
JP2021521163A (ja) * 2018-04-09 2021-08-26 上海科技大学Shanghai Tech University 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
JP7367908B2 (ja) 2018-04-09 2023-10-24 上海科技大学 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
US12226424B2 (en) 2018-04-09 2025-02-18 Shanghaitech University Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates
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US12240869B2 (en) 2018-11-01 2025-03-04 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
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