DE602004032446D1 - 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel - Google Patents

2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel

Info

Publication number
DE602004032446D1
DE602004032446D1 DE602004032446T DE602004032446T DE602004032446D1 DE 602004032446 D1 DE602004032446 D1 DE 602004032446D1 DE 602004032446 T DE602004032446 T DE 602004032446T DE 602004032446 T DE602004032446 T DE 602004032446T DE 602004032446 D1 DE602004032446 D1 DE 602004032446D1
Authority
DE
Germany
Prior art keywords
compounds
pyrimidindiamin
antiproliferative agents
compositions
methods
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
DE602004032446T
Other languages
English (en)
Inventor
Ankush Argade
Rajinder Singh
Hui Li
David Carroll
Susan Catalano
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rigel Pharmaceuticals Inc
Original Assignee
Rigel Pharmaceuticals Inc
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 Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of DE602004032446D1 publication Critical patent/DE602004032446D1/de
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—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 ortho- or peri-condensed with 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
DE602004032446T 2003-08-07 2004-08-06 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel Active DE602004032446D1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US49400803P 2003-08-07 2003-08-07
US57253404P 2004-05-18 2004-05-18
PCT/US2004/025409 WO2005013996A2 (en) 2003-08-07 2004-08-06 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents

Publications (1)

Publication Number Publication Date
DE602004032446D1 true DE602004032446D1 (de) 2011-06-09

Family

ID=34138795

Family Applications (1)

Application Number Title Priority Date Filing Date
DE602004032446T Active DE602004032446D1 (de) 2003-08-07 2004-08-06 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel

Country Status (9)

Country Link
US (6) US20050113398A1 (de)
EP (1) EP1663242B1 (de)
JP (1) JP4741491B2 (de)
AT (1) ATE506953T1 (de)
DE (1) DE602004032446D1 (de)
DK (1) DK1663242T3 (de)
ES (1) ES2365223T3 (de)
SI (1) SI1663242T1 (de)
WO (1) WO2005013996A2 (de)

Families Citing this family (151)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
DK1534286T3 (da) 2002-07-29 2010-04-26 Rigel Pharmaceuticals Inc Fremgangsmåder til behandling eller forebyggelse af autoimmune sygdomme med 2,4-pyrimidindiamin-forbindelser
CA2533377C (en) * 2003-07-30 2012-11-27 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
WO2005013996A2 (en) * 2003-08-07 2005-02-17 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
BR122019017579B8 (pt) * 2003-08-15 2021-07-27 Novartis Ag 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica
CN100584832C (zh) * 2003-09-18 2010-01-27 诺瓦提斯公司 可用于治疗增殖性病症的2,4-二(苯基氨基)嘧啶类
US7754714B2 (en) * 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
GB2420559B (en) * 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
DK1814878T3 (da) * 2004-11-24 2012-05-07 Rigel Pharmaceuticals Inc Spiro-2, 4-pyrimidindiamin-forbindelser og anvendelser deraf
EP2161275A1 (de) 2005-01-19 2010-03-10 Rigel Pharmaceuticals, Inc. Prodrugs aus 2,4-Pyrimidindiamin-Verbindungen und ihre Verwendungen
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
AU2006241825A1 (en) 2005-04-28 2006-11-09 Mitsubishi Tanabe Pharma Corporation Cyanopyridine derivative and use thereof as medicine
CA2604551A1 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
DE102005027274A1 (de) * 2005-06-08 2006-12-14 Schering Ag Inhibitoren der löslichen Adenylatzyklase
US7417066B2 (en) 2005-06-08 2008-08-26 Schering Ag Inhibitors of soluble adenylate cyclase
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
RU2485106C2 (ru) 2005-06-08 2013-06-20 Райджел Фамэсьютикэлз, Инк. Соединения, проявляющие активность в отношении jak-киназы (варианты), способ лечения заболеваний, опосредованных jak-киназой, способ ингибирования активности jak-киназы (варианты), фармацевтическая композиция на основе указанных соединений
WO2006135915A2 (en) 2005-06-13 2006-12-21 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
DE602005000514T2 (de) * 2005-06-17 2007-10-25 Magneti Marelli Powertrain S.P.A. Brennstoffeinspritzventil
EP1904479A2 (de) * 2005-07-11 2008-04-02 Sanofi-Aventis Neue 2,4-dianilinopyrimidinderivate, ihre herstellung, ihre verwendung als medikamente, pharmazeutische zusammensetzungen und insbesondere als ikk-inhibitoren
FR2888239B1 (fr) * 2005-07-11 2008-05-09 Sanofi Aventis Sa Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
ATE517874T1 (de) 2005-10-21 2011-08-15 Exelixis Inc Pyrimidinone als modulatoren von caseinkinase ii (ck2)
CA2642211C (en) 2006-02-17 2012-01-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
PE20120006A1 (es) * 2006-05-15 2012-02-02 Boehringer Ingelheim Int Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
CA2653777A1 (en) 2006-06-15 2007-12-21 Boehringer Ingelheim International Gmbh 2-anilino-4-(heterocyclic)amino-pyrimidines
CN101506176A (zh) 2006-06-15 2009-08-12 贝林格尔.英格海姆国际有限公司 2-苯胺基-4-氨基亚烷基氨基嘧啶
WO2008024724A1 (en) 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
WO2008051547A1 (en) 2006-10-23 2008-05-02 Cephalon, Inc. Fused bicyclic derivatives of 2,4-diaminopyrimidine as alk and c-met inhibitors
US20090048214A1 (en) * 2006-11-15 2009-02-19 Rigel Pharmaceuticals, Inc Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds
RS53588B1 (en) 2006-12-08 2015-02-27 Irm Llc COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
CA2670645A1 (en) * 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
WO2008077810A2 (en) 2006-12-22 2008-07-03 F. Hoffmann-La Roche Ag Spiro-piperidine derivatives
US20100144706A1 (en) * 2006-12-22 2010-06-10 Boehringer Ingelheim International Gmbh Compounds
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
WO2008118823A2 (en) * 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP2134684B1 (de) 2007-04-16 2017-08-02 AbbVie Inc. 7-substituierte indole als mcl-1-hemmer
US20090012045A1 (en) * 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of Treating Cell Proliferative Disorders
AU2008275918B2 (en) 2007-07-17 2014-01-30 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as PKC inhibitors
JP5306373B2 (ja) 2008-01-11 2013-10-02 エフ．ホフマン−ラ ロシュ アーゲー アミロイドβのモジュレーター
AU2009216851B2 (en) 2008-02-22 2013-11-07 F. Hoffmann-La Roche Ag Modulators for amyloid beta
US20100155402A1 (en) * 2008-02-27 2010-06-24 Pwp Industries, Inc. Display and storage container
EA018282B1 (ru) * 2008-04-07 2013-06-28 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
AU2009248923B2 (en) 2008-05-21 2015-01-29 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MX2010014568A (es) * 2008-06-25 2011-03-29 Irm Llc Derivados de pirmidina como inhibidores de cinasa.
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR20110025224A (ko) 2008-06-27 2011-03-09 아빌라 테라퓨틱스, 인크. 헤테로아릴 화합물 및 이의 용도
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2013202496B2 (en) * 2008-06-27 2016-08-04 Celgene Car Llc Heteroaryl compounds and uses thereof
MX2010014565A (es) 2008-07-01 2011-03-04 Genentech Inc Isoindolona y metodos de uso.
US8841462B2 (en) 2008-07-01 2014-09-23 Robert A. Heald Bicyclic heterocycles as MEK kinase inhibitors
EP2161259A1 (de) 2008-09-03 2010-03-10 Bayer CropScience AG 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide
CN102177151A (zh) 2008-10-09 2011-09-07 弗·哈夫曼-拉罗切有限公司 β-淀粉样蛋白的调节剂
WO2010052199A1 (en) 2008-11-10 2010-05-14 F. Hoffmann-La Roche Ag Heterocyclic gamma secretase modulators
KR101741168B1 (ko) 2008-12-22 2017-05-29 밀레니엄 파머슈티컬스 인코퍼레이티드 오로라 키나아제 억제제 및 항­ｃｄ 항체의 병용
US8278299B2 (en) 2008-12-30 2012-10-02 Rigel Pharmaceuticals, Inc. Pyrimidinediamine kinase inhibitors
EP2387402A4 (de) * 2009-01-14 2014-11-12 Rigel Pharmaceuticals Inc Verfahren zur behandlung von entzündungserkrankungen mit 2,4-pyrimidindiaminverbindungen
CA2749195C (en) * 2009-01-15 2017-03-07 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
CA2749837C (en) 2009-01-21 2017-07-11 Rigel Pharmaceuticals, Inc. Derivatives of n2-(3-pyridil or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases
US20110071158A1 (en) * 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
EP2440559B1 (de) 2009-05-05 2018-01-10 Dana-Farber Cancer Institute, Inc. Egfr-hemmer und verfahren zur krankheitsbehandlung damit
RU2557982C2 (ru) * 2009-07-28 2015-07-27 Райджел Фармасьютикалз, Инк. Композиции и способы ингибирования пути jak
KR101726444B1 (ko) 2009-08-31 2017-04-12 스미또모 가가꾸 가부시키가이샤 수지, 레지스트 조성물 및 레지스트 패턴의 제조 방법
JP5681723B2 (ja) * 2009-11-20 2015-03-11 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 ２，４−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用
US20110130415A1 (en) 2009-12-01 2011-06-02 Rajinder Singh Protein kinase c inhibitors and uses thereof
US8486096B2 (en) * 2010-02-11 2013-07-16 Ethicon Endo-Surgery, Inc. Dual purpose surgical instrument for cutting and coagulating tissue
US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
US8618095B2 (en) 2010-04-13 2013-12-31 Rigel Pharmaceuticals, Inc. 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
JP5607241B2 (ja) 2010-05-21 2014-10-15 ケミリア・エービー 新規ピリミジン誘導体
EP2395001A1 (de) * 2010-05-21 2011-12-14 Chemilia AB Neue Pyrimidinderivate
EP3075730B1 (de) 2010-06-04 2018-10-24 Genentech, Inc. Aminopyrimidinderivate als lrrk2-modulatoren
EP2595982B1 (de) * 2010-07-21 2018-06-13 Rigel Pharmaceuticals, Inc. Proteinkinase-c-hemmer und ihre verwendung
US9063414B2 (en) 2010-07-28 2015-06-23 Sumitomo Chemical Company, Limited Photoresist composition
WO2012021444A1 (en) * 2010-08-10 2012-02-16 Avila Therapeutics, Inc. Besylate salt of a btk inhibitor
KR101776320B1 (ko) 2010-08-30 2017-09-07 스미또모 가가꾸 가부시키가이샤 레지스트 조성물 및 레지스트 패턴의 제조 방법
NZ609957A (en) 2010-11-01 2015-08-28 Celgene Avilomics Res Inc Heterocyclic compounds and uses thereof
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
EP2637502B1 (de) 2010-11-10 2018-01-10 Celgene CAR LLC Mutanten-selektive egfr-hemmer und verwendungen davon
AU2011328139A1 (en) 2010-11-10 2013-04-04 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as LRRK2 modulators
EP2489663A1 (de) 2011-02-16 2012-08-22 Almirall, S.A. Verbindungen als Syk-Kinasehemmer
JP5947053B2 (ja) 2011-02-25 2016-07-06 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5947051B2 (ja) 2011-02-25 2016-07-06 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP6034025B2 (ja) 2011-02-25 2016-11-30 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5829941B2 (ja) 2011-02-25 2015-12-09 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5829939B2 (ja) 2011-02-25 2015-12-09 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5898521B2 (ja) 2011-02-25 2016-04-06 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5898520B2 (ja) 2011-02-25 2016-04-06 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP6034026B2 (ja) 2011-02-25 2016-11-30 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5829940B2 (ja) 2011-02-25 2015-12-09 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
BR112013024378A2 (pt) 2011-03-24 2016-12-13 Chemilia Ab novos derivados de pirimidina
US9249124B2 (en) 2011-03-30 2016-02-02 H. Lee Moffitt Cancer Center And Research Institute, Inc. Aurora kinase inhibitors and methods of making and using thereof
KR101884010B1 (ko) 2011-05-04 2018-07-31 어리어드 파마슈티칼스, 인코포레이티드 Egfr-유도된 암의 세포 증식을 억제하는 화합물
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
AU2012253886A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as Syk inhibitors
RU2013154412A (ru) 2011-05-10 2015-06-20 Мерк Шарп И Доум Корп. Аминопиримидины в качестве ингибиторов syc
JP6013799B2 (ja) 2011-07-19 2016-10-25 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5886696B2 (ja) 2011-07-19 2016-03-16 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP5912912B2 (ja) 2011-07-19 2016-04-27 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP6189020B2 (ja) 2011-07-19 2017-08-30 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
JP6013797B2 (ja) 2011-07-19 2016-10-25 住友化学株式会社 レジスト組成物及びレジストパターンの製造方法
MX339685B (es) 2011-07-28 2016-06-06 Rigel Pharmaceuticals Inc Formulaciones de (trimetoxifenilamino) pirimidinilo nuevas.
BR112014003997A2 (pt) 2011-08-25 2017-03-21 Hoffmann La Roche composto, método para inibição da atividade de pak1 em uma célula e paciente, método para o tratamento ou melhoria da gravidade do câncer ou de um distúrbio hiperproliferativo em um paciente, utilização do composto e composição
WO2013052394A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763975B1 (de) 2011-10-05 2016-04-06 Merck Sharp & Dohme Corp. 3-pyridyl-carboxamidhaltige milztyrosinkinase-(syk)-hemmer
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
US8815877B2 (en) 2011-12-22 2014-08-26 Genentech, Inc. Serine/threonine kinase inhibitors
KR102081042B1 (ko) 2012-03-15 2020-02-26 셀젠 카르 엘엘씨 상피 성장 인자 수용체 키나제 억제제의 고체 형태
LT2825042T (lt) 2012-03-15 2018-12-10 Celgene Car Llc Epidermio augimo faktoriaus receptoriaus kinazės slopiklio druskos
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
US9242984B2 (en) 2012-06-20 2016-01-26 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as Syk inhibitors
US9487504B2 (en) 2012-06-20 2016-11-08 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863915B1 (de) 2012-06-22 2017-12-06 Merck Sharp & Dohme Corp. Substituierte diazin- und triazin-milz-tyrosinkinase-hemmer
WO2013192098A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
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
US9353066B2 (en) 2012-08-20 2016-05-31 Merck Sharp & Dohme Corp. Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
US9624210B2 (en) 2012-12-12 2017-04-18 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase (Syk) inhibitors
US9598405B2 (en) 2012-12-21 2017-03-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
MX2015009952A (es) 2013-02-08 2015-10-05 Celgene Avilomics Res Inc Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos.
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP2988744A4 (de) 2013-04-26 2016-11-02 Merck Sharp & Dohme Thiazolsubstituierte aminoheteroaryle als milztyrosinkinasehemmer
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine 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
JP6525474B2 (ja) 2013-12-06 2019-06-05 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Ｍｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． オーロラキナーゼ阻害剤と抗ｃｄ３０抗体の併用
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9670196B2 (en) 2013-12-20 2017-06-06 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
CN105017159B (zh) * 2014-04-28 2019-05-17 四川大学 5-氟-2,4-二取代氨基嘧啶衍生物及其制备方法和用途
US10106507B2 (en) 2014-08-03 2018-10-23 H. Lee Moffitt Cancer Center and Research Insitute, Inc. Potent dual BRD4-kinase inhibitors as cancer therapeutics
TW201613892A (en) 2014-08-13 2016-04-16 Celgene Avilomics Res Inc Forms and compositions of an ERK inhibitor
WO2016029002A2 (en) * 2014-08-22 2016-02-25 Clovis Oncology, Inc. Growth factor receptor inhibitors
WO2017066428A1 (en) 2015-10-13 2017-04-20 H. Lee Moffitt Cancer Center & Research Institute, Inc. Brd4-kinase inhibitors as cancer therapeutics
US11203576B2 (en) * 2016-03-11 2021-12-21 H. Lee Moffitt Cancer Center And Research Institute, Inc. Aurora kinase and Janus kinase inhibitors for prevention of graft versus host disease
MA47233A (fr) * 2016-12-19 2019-10-23 Epizyme Inc Composés hétérocycliques substitués par une amine utilisés comme inhibiteurs de l'ehmt2 et leurs méthodes d'utilisation
CN110520412A (zh) * 2017-02-15 2019-11-29 南洋理工大学 用于治疗结核病的化合物
EP3612181A4 (de) 2017-04-21 2021-01-06 Epizyme, Inc. Kombinationstherapien mit ehmt2-inhibitoren
EP3710006A4 (de) * 2017-11-19 2021-09-01 Sunshine Lake Pharma Co., Ltd. Substituierte heteroarylverbindungen und verfahren zur verwendung
US11874276B2 (en) 2018-04-05 2024-01-16 Dana-Farber Cancer Institute, Inc. STING levels as a biomarker for cancer immunotherapy
SG11202112171XA (en) 2019-05-10 2021-12-30 Deciphera Pharmaceuticals Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
PL3966207T3 (pl) 2019-05-10 2024-03-04 Deciphera Pharmaceuticals, Llc Fenyloaminopirymidynoamidowe inhibitory autofagii i sposoby ich zastosowania
JP2022536540A (ja) 2019-06-17 2022-08-17 デシフェラ・ファーマシューティカルズ，エルエルシー アミノピリミジンアミドオートファジー阻害剤およびその使用方法
WO2021003417A1 (en) 2019-07-03 2021-01-07 Sumitomo Dainippon Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
CN115304551A (zh) * 2022-07-25 2022-11-08 南通大学 2-((4-吗啉苯基)氨基)嘧啶氨基酸衍生物及其制备方法与应用
CN115304550A (zh) * 2022-07-25 2022-11-08 南通大学 哌嗪苯基氨基取代的嘧啶氨基酸衍生物及制备方法与应用
CN115232076A (zh) * 2022-07-25 2022-10-25 南通大学 苯氨基取代的嘧啶氨基酸衍生物及其制备方法与应用

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4738851A (en) 1985-09-27 1988-04-19 University Of Iowa Research Foundation, Inc. Controlled release ophthalmic gel formulation
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US4882150A (en) 1988-06-03 1989-11-21 Kaufman Herbert E Drug delivery system
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
US5521222A (en) 1989-09-28 1996-05-28 Alcon Laboratories, Inc. Topical ophthalmic pharmaceutical vehicles
CA2031376A1 (en) 1989-12-04 1991-06-05 Bahram Farhadieh Single layer transdermal drug administration system
US5077033A (en) 1990-08-07 1991-12-31 Mediventures Inc. Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
CA2123809A1 (en) 1991-12-18 1993-06-24 Debra L. Wilfong Multilayered barrier structures
ATE132381T1 (de) 1992-01-29 1996-01-15 Voelkl Franz Ski Ballspielschläger, insbesondere tennisschläger
IL114193A (en) 1994-06-20 2000-02-29 Teva Pharma Ophthalmic pharmaceutical compositions based on sodium alginate
ES2094688B1 (es) 1994-08-08 1997-08-01 Cusi Lab Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion.
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
IT1283911B1 (it) 1996-02-05 1998-05-07 Farmigea Spa Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo
US5800807A (en) 1997-01-29 1998-09-01 Bausch & Lomb Incorporated Ophthalmic compositions including glycerin and propylene glycol
ES2308821T3 (es) * 1997-12-15 2008-12-01 Astellas Pharma Inc. Nuevos derivados de pirimidin-5-carboxamida.
US6261547B1 (en) 1998-04-07 2001-07-17 Alcon Manufacturing, Ltd. Gelling ophthalmic compositions containing xanthan gum
US6197934B1 (en) 1998-05-22 2001-03-06 Collagenesis, Inc. Compound delivery using rapidly dissolving collagen film
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
DE122010000038I1 (de) * 2000-12-21 2011-01-27 Glaxosmithkline Llc Pyrimidinamine als angiogenesemodulatoren
KR100874791B1 (ko) * 2001-05-29 2008-12-18 바이엘 쉐링 파마 악티엔게젤샤프트 Ｃｄｋ-억제 피리미딘, 그의 제조방법 및 약제로서의 용도
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
WO2003026665A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003040141A1 (en) * 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
AU2002367172A1 (en) * 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
DK1534286T3 (da) * 2002-07-29 2010-04-26 Rigel Pharmaceuticals Inc Fremgangsmåder til behandling eller forebyggelse af autoimmune sygdomme med 2,4-pyrimidindiamin-forbindelser
WO2004065378A1 (en) * 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
EP1597251B1 (de) * 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimiidinverbindungen
GB0305929D0 (en) * 2003-03-14 2003-04-23 Novartis Ag Organic compounds
CA2533377C (en) * 2003-07-30 2012-11-27 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
WO2005013996A2 (en) * 2003-08-07 2005-02-17 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
US7754714B2 (en) * 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
US20060051406A1 (en) * 2004-07-23 2006-03-09 Manjeet Parmar Formulation of insoluble small molecule therapeutics in lipid-based carriers
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
US20090048214A1 (en) * 2006-11-15 2009-02-19 Rigel Pharmaceuticals, Inc Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds
CA2749837C (en) * 2009-01-21 2017-07-11 Rigel Pharmaceuticals, Inc. Derivatives of n2-(3-pyridil or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases
US20110130415A1 (en) * 2009-12-01 2011-06-02 Rajinder Singh Protein kinase c inhibitors and uses thereof

Also Published As

Publication number Publication date
US8809341B2 (en) 2014-08-19
US20080009484A1 (en) 2008-01-10
DK1663242T3 (da) 2011-08-01
ATE506953T1 (de) 2011-05-15
EP1663242A2 (de) 2006-06-07
US20050113398A1 (en) 2005-05-26
US20150011002A1 (en) 2015-01-08
WO2005013996A3 (en) 2005-06-09
US20080027045A1 (en) 2008-01-31
US20110190271A1 (en) 2011-08-04
JP2007501793A (ja) 2007-02-01
WO2005013996A2 (en) 2005-02-17
US20080021020A1 (en) 2008-01-24
JP4741491B2 (ja) 2011-08-03
SI1663242T1 (sl) 2011-09-30
US9598432B2 (en) 2017-03-21
ES2365223T3 (es) 2011-09-26
US7884111B2 (en) 2011-02-08
EP1663242B1 (de) 2011-04-27

Similar Documents

Publication Publication Date Title
ATE506953T1 (de) 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
CY1112743T1 (el) Στερεοϊσομερως εμπλουτισμενες ενωσεις 3-αμινοκαρβονυλ δικυκλοεπτενο πυριμιδινοδιαμινης και οι χρησεις τους
CY1119512T1 (el) Αντισωματα του υποδοχεα 1 της ιντερφερονης αλφα και οι χρησεις αυτων
WO2005118544A3 (en) Cycloalkyl substituted pyrimidinediamine compounds and their uses
DE60231439D1 (de) Mitotische kinesinhemmer
NO20034056D0 (no) Proliferative sykdommer
CY1111050T1 (el) Φωσφονικα, μονοφωσφοναμιδικα, διφωσφοναμιδικα για την αγωγη των ιϊκων παθησεων
TW200700422A (en) Compounds for inhibiting ksp kinesin activity
RS20050708A (en) Aminoheteroaryl compounds as protein kinase inhibitors
DE60329756D1 (de) Mitotische kinesin-hemmer
PT1200412E (pt) Agentes anti-proliferativos de imidazole
TW200700066A (en) Compounds for inhibiting ksp kinesin activity
ATE515262T1 (de) Verwendung von parthenolid-derivaten als antileukämische und zytotoxische mittel
ATE302203T1 (de) Pyrazolopyrimidin- und pyrazolotriazinderivate und diese enthaltende pharmazeutische zubereitungen
ATE447955T1 (de) Piperazinon-verbindungen als antitumorale und krebsbekämpfende mittel
UA80474C2 (en) Aminoheteroaryl compounds as inhibitors of protein kinase
HK1074840A1 (en) Novel dithiolopyrrolones with therapeutic activity
DE60304360D1 (de) N-aryl-2-oxazolidinone und deren derivate
DE60326348D1 (de) Makrozyclen zur behandlung von krebserkrankungen
ATE387913T1 (de) Xenogene oligo- oder/und polyribonukleotide als mittel zur behandlung von malignen tumoren
DE602004019899D1 (de) Zusammensetzungen und verwendung von peptiden und deren derivate als hemmer der oxidativen schädigung der haut
DE60305520D1 (de) 2" oxo-voruscharin und derivaten