JP5111113B2 - Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン - Google Patents

Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン Download PDF

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JP5111113B2
JP5111113B2 JP2007545694A JP2007545694A JP5111113B2 JP 5111113 B2 JP5111113 B2 JP 5111113B2 JP 2007545694 A JP2007545694 A JP 2007545694A JP 2007545694 A JP2007545694 A JP 2007545694A JP 5111113 B2 JP5111113 B2 JP 5111113B2
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pharmaceutically acceptable
acceptable salt
alkyl
hydrogen
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JP2008523099A (ja
JP2008523099A5 (enExample
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ヨハン ディー． オスロブ，
チヤン チュ，
ケネス バー，
ジェニファー クロスロー，
ブライアン レイムンド，
ヒロコ タナカ，
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サネシス 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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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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JP2007545694A 2004-12-13 2005-12-12 Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン Expired - Fee Related JP5111113B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US63564404P 2004-12-13 2004-12-13
US60/635,644 2004-12-13
US63674004P 2004-12-16 2004-12-16
US60/636,740 2004-12-16
US11/301,311 US7767687B2 (en) 2004-12-13 2005-12-12 Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
PCT/US2005/044804 WO2006065703A1 (en) 2004-12-13 2005-12-12 Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
US11/301,311 2005-12-12

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JP2008523099A JP2008523099A (ja) 2008-07-03
JP2008523099A5 JP2008523099A5 (enExample) 2009-02-26
JP5111113B2 true JP5111113B2 (ja) 2012-12-26

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US (2) US7767687B2 (enExample)
EP (1) EP1828186A1 (enExample)
JP (1) JP5111113B2 (enExample)
AU (1) AU2005316668B2 (enExample)
CA (1) CA2590294A1 (enExample)
WO (1) WO2006065703A1 (enExample)

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY29439A1 (es) * 2005-03-25 2006-10-02 Glaxo Group Ltd Nuevos compuestos
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
PT1940839E (pt) 2005-10-07 2013-10-10 Exelixis Inc Inibidores de piridopirimidinona pi3k alfa
HRP20130902T1 (hr) 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
WO2007067444A1 (en) 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
CA2663401C (en) 2006-09-15 2011-07-12 Pfizer Products Inc. Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
ES2627352T3 (es) 2006-10-19 2017-07-27 Signal Pharmaceuticals, Llc Compuestos heteroarilo, sus composiciones y su uso como inhibidores de proteínas quinasas
TW200835497A (en) * 2007-01-11 2008-09-01 Astrazeneca Ab Chemical compounds 636
JP2010517989A (ja) 2007-02-01 2010-05-27 アストラゼネカ アクチボラグ Ｈｓｐ９０阻害剤としての５，６，７，８−テトラヒドロプテリジン誘導体
JP5238172B2 (ja) * 2007-03-22 2013-07-17 公益財団法人相模中央化学研究所 パーフルオロアルキル基を有する含窒素六員環化合物およびその製造方法
CL2008001933A1 (es) * 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
EP2167497A2 (en) * 2007-06-29 2010-03-31 Sunesis Pharmaceuticals, Inc. Heterocyclic compounds useful as raf kinase inhibitors
AU2009289649B2 (en) 2008-09-03 2016-05-05 Biomarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
TW201018685A (en) 2008-09-30 2010-05-16 Exelixis Inc Pyridopyrimidinone inhibitors of PI3Kα and mTOR
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
JP2012514044A (ja) * 2008-12-30 2012-06-21 ミレニアム ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なヘテロアリール化合物
BR112012011328A2 (pt) * 2009-10-23 2016-11-22 Lilly Co Eli inibidores de akt
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
BR112012019459A2 (pt) 2010-02-03 2017-10-17 Signal Pharm Llc identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase.
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
WO2012118782A1 (en) 2011-02-28 2012-09-07 Repligen Corporation Histone deacetylase inhibitors
JP2014528410A (ja) * 2011-09-30 2014-10-27 キネタ・インコーポレイテツド 抗ウイルス化合物
CN103998036B (zh) 2011-10-19 2017-05-31 西格诺药品有限公司 利用tor激酶抑制剂治疗癌症
BR112014013332B1 (pt) 2011-12-02 2022-09-06 Signal Pharmaceuticals, Llc Composições farmacêuticas de 7-(6-(2-hidroxi-propan-2-il)piridin-3-il)-1-((trans)-4- metoxicicloexil)-3,4-diidropirazino [2,3-b]pirazin-2(1h)-ona, uma forma sólida dessa e métodos de seu uso
DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
CN104271159B (zh) 2012-02-24 2017-11-28 西格诺药品有限公司 利用tor激酶抑制剂联合治疗来治疗非小细胞肺癌的方法
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
SG11201505446WA (en) 2013-01-16 2015-08-28 Signal Pharm Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
RU2665554C2 (ru) 2013-03-15 2018-08-31 Байомарин Фармасьютикал Инк. Ингибиторы hdac
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
JP6382946B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
WO2014172425A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
AU2014267360B2 (en) 2013-05-14 2018-07-05 Active Biotech Ab N-(heteroaryl)-sulfonamide derivatives useful as S100-inhibitors
CN107474051B (zh) 2013-05-29 2020-10-30 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
WO2015000715A1 (en) 2013-07-02 2015-01-08 Syngenta Participations Ag Pesticidally active bi- or tricyclic heterocycles with sulfur containing substituents
PL3089971T3 (pl) 2014-01-01 2021-01-25 Medivation Technologies Llc Związki i sposoby ich zastosowania
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
WO2015160880A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
BR112017002598B1 (pt) 2014-08-12 2022-03-03 Syngenta Participations Ag Derivados heterocíclicos ativos do ponto de vista pesticida com substituintes contendo enxofre
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
BR112017012232B1 (pt) 2014-12-11 2021-08-17 Syngenta Participations Ag Derivados tetraciclicos ativos em termos pesticidas com substituintes contendo enxofre
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
UY36548A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2779532T3 (es) 2015-04-08 2020-08-18 Bayer Cropscience Ag Derivados de imidazo[1,2a]piridin-2-ilo como pesticidas y sus productos intermedios
AU2016248376B2 (en) 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
JP6689297B2 (ja) 2015-07-23 2020-04-28 武田薬品工業株式会社 複素環化合物
AR105607A1 (es) 2015-08-07 2017-10-18 Bayer Cropscience Ag Derivados heterocíclicos condensados sustituidos por 2-(het)arilo como pesticidas
CN108430986B (zh) 2015-10-26 2021-08-31 拜耳作物科学股份公司 作为有害生物控制剂的稠合双环杂环衍生物
BR112018010347A2 (pt) 2015-11-23 2018-12-04 Syngenta Participations Ag derivados heterocíclicos ativos em termos pesticidas com substituintes contendo enxofre e ciclopropila
WO2017093180A1 (de) 2015-12-01 2017-06-08 Bayer Cropscience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
JP6175519B2 (ja) * 2016-01-04 2017-08-09 ベイジーン リミテッド Ｒａｆキナーゼ阻害剤としての縮合三環式化合物
WO2017144341A1 (de) 2016-02-23 2017-08-31 Bayer Cropscience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
WO2017174414A1 (de) 2016-04-05 2017-10-12 Bayer Cropscience Aktiengesellschaft Naphthalin-derivate als schädlingsbekämpfungsmittel
EP3241830A1 (de) 2016-05-04 2017-11-08 Bayer CropScience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
US10561145B2 (en) 2016-07-19 2020-02-18 Bayer Cropscience Aktiengesellschaft Fused bicyclic heterocycle derivatives as pesticides
AU2017314083B2 (en) 2016-08-15 2020-12-10 Bayer Aktiengesellschaft Condensed bicyclic heterocycle derivatives as pest control agents
CN109819653A (zh) 2016-08-16 2019-05-28 拜耳作物科学股份公司 制备2-(3,6-二卤代吡啶-2-基)-3H-咪唑[4,5-c]吡啶衍生物的方法以及通过3H-咪唑[4,5-c]吡啶衍生物与有机金属锌胺碱的反应得到的相关化合物
CN109963860A (zh) 2016-09-19 2019-07-02 拜耳作物科学股份公司 吡唑并[1,5-a]吡啶衍生物及其作为农药的用途
WO2018065292A1 (de) 2016-10-06 2018-04-12 Bayer Cropscience Aktiengesellschaft 2-(het)aryl-substituierte kondensierte bicyclische heterocyclen-derivate als schädlings-bekämpfungsmittel
CN117624038A (zh) 2016-12-01 2024-03-01 先正达参股股份有限公司 具有含硫取代基的杀有害生物活性杂环衍生物
US20200077658A1 (en) 2016-12-16 2020-03-12 Basf Se Pesticidal Compounds
WO2018138050A1 (de) 2017-01-26 2018-08-02 Bayer Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
TW201833107A (zh) 2017-02-06 2018-09-16 德商拜耳廠股份有限公司 作為殺蟲劑之經２－（雜）芳基取代的稠合雜環衍生物
AU2018257372B2 (en) 2017-04-24 2022-06-02 Bayer Aktiengesellschaft Condensed bicyclic heterocyclic-compound derivatives as pest control agents
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
EP3305786A3 (de) 2018-01-22 2018-07-25 Bayer CropScience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
CN111741958A (zh) 2018-02-21 2020-10-02 拜耳公司 作为害虫防治剂的稠合双环杂环衍生物
BR112020020081A2 (pt) 2018-04-20 2021-01-05 Bayer Aktiengesellschaft Derivados de heterocicleno como agentes de controle de pragas
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
EP3636645A1 (de) 2018-10-11 2020-04-15 Bayer Aktiengesellschaft Verfahren zur herstellung schwefel-substituierter pyridinderivate
PH12021552065A1 (en) 2019-02-26 2022-05-23 Bayer Ag Condensed bicyclic heterocyclic derivatives as pest control agents
CN113710669A (zh) 2019-02-26 2021-11-26 拜耳公司 作为农药的稠合双环杂环衍生物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
AR119140A1 (es) 2019-06-13 2021-11-24 Pi Industries Ltd Compuestos heterocíclicos fusionados y su uso como agentes de control de plagas
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN113912608B (zh) * 2020-07-10 2023-07-14 江苏恒瑞医药股份有限公司 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2025177310A1 (en) 2024-02-23 2025-08-28 Pi Industries Ltd. Fused heterocyclic compounds and its uses thereof
WO2025177312A1 (en) 2024-02-23 2025-08-28 Pi Industries Ltd. Fused heterocyclic compounds and its uses thereof

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
US5525711A (en) * 1994-05-18 1996-06-11 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Pteridine nucleotide analogs as fluorescent DNA probes
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
US6875769B2 (en) 1996-05-23 2005-04-05 Pfizer Inc. Substituted6,6-hetero-bicyclicderivatives
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
ES2301194T3 (es) * 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
SI1028950T1 (en) 1997-10-28 2003-08-31 Warner-Lambert Company Llc 7-substituted quinazolin-2,4-diones useful as antibacterial agents
WO1999051613A1 (en) 1998-04-03 1999-10-14 Medivir Ab Prodrugs of phosphorous-containing pharmaceuticals
DE69939168D1 (de) 1998-05-26 2008-09-04 Warner Lambert Co Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung
US20040044012A1 (en) 1998-05-26 2004-03-04 Dobrusin Ellen Myra Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation
JP2003509425A (ja) * 1999-09-15 2003-03-11 ワーナー−ランバート・カンパニー キナーゼ阻害剤としてのプテリジノン
SK10772002A3 (sk) 2000-01-27 2004-01-08 Warner-Lambert Company Pyridopyrimidinónové deriváty na liečbu neurodegeneratívnych ochorení
GB2359551A (en) * 2000-02-23 2001-08-29 Astrazeneca Uk Ltd Pharmaceutically active pyrimidine derivatives
AR030053A1 (es) * 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
EP1267876A1 (en) 2000-03-23 2003-01-02 Merck & Co., Inc. Thrombin inhibitors
DE10050661A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Substituierte 3,4-Dihydro-pyrimido[1,2-a]pyrimidine und 3,4-Dihydro-pyrazino[1,2-a]pyrimidine
AU2002246855B2 (en) * 2000-10-23 2005-12-22 Smithkline Beecham Corporation Novel compounds
WO2002076954A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
US6511867B2 (en) 2001-06-30 2003-01-28 Ovonyx, Inc. Utilizing atomic layer deposition for programmable device
ATE466581T1 (de) * 2001-12-07 2010-05-15 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
CN1665808A (zh) * 2002-05-06 2005-09-07 沃泰克斯药物股份有限公司 噻二唑或噁二唑及其作为jak蛋白激酶抑制剂的用途
US7384937B2 (en) 2002-11-06 2008-06-10 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
CA2533626A1 (en) 2003-07-22 2005-02-03 Janssen Pharmaceutica, N.V. Quinolinone derivatives as inhibitors of c-fms kinase
CA2683820A1 (en) * 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of p13k-alpha for the treatment of cancer

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