RU2673077C2 - Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста - Google Patents

Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста Download PDF

Info

Publication number
RU2673077C2
RU2673077C2 RU2014136896A RU2014136896A RU2673077C2 RU 2673077 C2 RU2673077 C2 RU 2673077C2 RU 2014136896 A RU2014136896 A RU 2014136896A RU 2014136896 A RU2014136896 A RU 2014136896A RU 2673077 C2 RU2673077 C2 RU 2673077C2
Authority
RU
Russia
Prior art keywords
compound
peaks
crystalline form
diffraction pattern
ray powder
Prior art date
Application number
RU2014136896A
Other languages
English (en)
Russian (ru)
Other versions
RU2014136896A (ru
Inventor
Мэй ЛАЙ
Original Assignee
Селджен Авиломикс Рисерч, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Селджен Авиломикс Рисерч, Инк. filed Critical Селджен Авиломикс Рисерч, Инк.
Publication of RU2014136896A publication Critical patent/RU2014136896A/ru
Application granted granted Critical
Publication of RU2673077C2 publication Critical patent/RU2673077C2/ru

Links

Images

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
RU2014136896A 2012-03-15 2013-03-13 Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста RU2673077C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261611376P 2012-03-15 2012-03-15
US61/611,376 2012-03-15
PCT/US2013/030982 WO2013138495A1 (en) 2012-03-15 2013-03-13 Solid forms of an epidermal growth factor receptor kinase inhibitor

Publications (2)

Publication Number Publication Date
RU2014136896A RU2014136896A (ru) 2016-05-10
RU2673077C2 true RU2673077C2 (ru) 2018-11-22

Family

ID=49161778

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2014136896A RU2673077C2 (ru) 2012-03-15 2013-03-13 Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста

Country Status (17)

Country Link
US (5) US9056839B2 (enExample)
EP (1) EP2825041B1 (enExample)
JP (2) JP6317319B2 (enExample)
KR (1) KR102081042B1 (enExample)
CN (2) CN104302178B (enExample)
AU (2) AU2016203338A1 (enExample)
BR (1) BR112014022789B1 (enExample)
CA (1) CA2866852C (enExample)
ES (1) ES2880109T3 (enExample)
IL (1) IL234425B (enExample)
IN (1) IN2014DN07401A (enExample)
MX (1) MX356753B (enExample)
MY (1) MY169233A (enExample)
RU (1) RU2673077C2 (enExample)
SG (2) SG11201405691WA (enExample)
WO (1) WO2013138495A1 (enExample)
ZA (1) ZA201407441B (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
BR112013010564B1 (pt) 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
JP6317320B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
CN105188371A (zh) 2013-02-08 2015-12-23 西建阿维拉米斯研究公司 Erk抑制剂及其用途
EP2994456A4 (en) * 2013-05-06 2017-01-04 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
BR112016006775A2 (pt) 2013-10-02 2017-08-01 3M Innovative Properties Co pilha de filmes ópticos e artigo
JP6453864B2 (ja) 2013-10-02 2019-01-16 スリーエム イノベイティブ プロパティズ カンパニー ポリアクリレート感圧性プライマーと、ポリアクリレート成分を含む接着剤と、を含む物品
NO2718543T3 (enExample) * 2014-02-04 2018-01-06
WO2016025561A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Forms and compositions of an erk inhibitor
WO2016029002A2 (en) * 2014-08-22 2016-02-25 Clovis Oncology, Inc. Growth factor receptor inhibitors
UA120108C2 (uk) 2014-12-12 2019-10-10 Мерк Патент Гмбх Комбінація похідної 6-оксо-1,6-дигідропіридазину, що має протиракову активність, з інгібітором рефр
WO2016101912A1 (zh) * 2014-12-25 2016-06-30 苏州晶云药物科技有限公司 一种表皮生长因子受体激酶抑制剂的盐的晶型及其制备方法
CN104961688A (zh) * 2014-12-25 2015-10-07 苏州晶云药物科技有限公司 一种表皮生长因子受体激酶抑制剂的磷酸盐及其制备方法
CN107614503B (zh) * 2015-04-29 2020-03-10 广东众生药业股份有限公司 稠环或三环芳基嘧啶化合物用作激酶抑制剂
CN106146406A (zh) * 2016-02-23 2016-11-23 深圳市塔吉瑞生物医药有限公司 一种取代的二氨基嘧啶类化合物及包含该化合物的组合物及其用途
CN107663207B (zh) * 2016-07-27 2021-07-30 南京圣和药业股份有限公司 一种egfr激酶抑制剂的甲磺酸盐结晶及制备方法
CN107663208B (zh) * 2016-07-27 2021-10-15 南京圣和药业股份有限公司 一种新型egfr激酶抑制剂的药用盐及其制备方法与用途
CN107955019B (zh) * 2016-10-17 2021-09-14 广东众生药业股份有限公司 一种egfr抑制剂的盐型、晶型及其制备方法
CN108299419B (zh) * 2017-01-11 2022-04-26 南京圣和药业股份有限公司 一种新型egfr激酶抑制剂的几种新晶型及其制备方法
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
US12523663B2 (en) 2019-06-04 2026-01-13 Inserm (Institut National De La Santé Et De La Rescherche Médicale) Use of CD9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6908906B2 (en) * 2001-02-09 2005-06-21 Sankyo Company, Limited Crystalline forms of pyrimidine nucleoside derivative
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
WO2012021444A1 (en) * 2010-08-10 2012-02-16 Avila Therapeutics, Inc. Besylate salt of a btk inhibitor
US8975249B2 (en) * 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof

Family Cites Families (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1062357A (en) * 1965-03-23 1967-03-22 Pfizer & Co C Quinazolone derivatives
US4337341A (en) * 1976-11-02 1982-06-29 Eli Lilly And Company 4a-Aryl-octahydro-1H-2-pyrindines
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
EP0813525B9 (en) 1995-03-10 2004-02-04 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
AU5438299A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
ID28376A (id) 1998-11-10 2001-05-17 Janssen Pharmaceutica Nv Pirimidina yang menghambat replikasi hiv
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
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
EP1150955A2 (en) 1999-02-04 2001-11-07 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU5835400A (en) 1999-06-29 2001-01-31 Egis Gyogyszergyar Rt. Novel piperazinylalkylthiopyrimidine derivatives, pharmaceutical compositions containing the same, and process for the preparation of the active substance
CA2396693A1 (en) 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
KR20030024659A (ko) 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
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
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
JP3748536B2 (ja) * 2001-02-09 2006-02-22 三共株式会社 ピリミジンヌクレオシド誘導体の結晶
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
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
IL161662A0 (en) 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
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
WO2003081210A2 (en) 2002-03-21 2003-10-02 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
US20040002395A1 (en) 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
EP1597237B1 (en) 2003-02-07 2016-07-27 Janssen Pharmaceutica NV Pyrimidine derivatives for the prevention of HIV infection
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
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
DK1663242T3 (da) 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
ATE542801T1 (de) 2003-08-15 2012-02-15 Novartis Ag Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
AU2004272288B2 (en) 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
ES2389203T3 (es) 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Inhibidores de quinasa selectivos
CN1930128A (zh) 2004-01-16 2007-03-14 惠氏公司 受体酪氨酸激酶抑制剂的喹啉中间体及其合成
US7378448B2 (en) 2004-03-15 2008-05-27 Eli Lilly And Company Diphenylether amide derivatives as opioid receptor antagonists
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
JP4812763B2 (ja) 2004-05-18 2011-11-09 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 シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
AU2005250484B2 (en) 2004-06-04 2011-08-11 Genentech, Inc. EGFR mutations
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
EP1805142A4 (en) 2004-09-23 2009-06-10 Reddy Us Therapeutics Inc PYRIDINE-BASED COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING SAME
ATE520672T1 (de) 2004-09-30 2011-09-15 Tibotec Pharm Ltd Hiv-hemmende 5-carbo- oder heterozyklisch substituierte pyrimidine
US7799915B2 (en) 2004-10-13 2010-09-21 Wyeth Llc Anilino-pyrimidine analogs
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
AU2006204724A1 (en) 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2006086777A2 (en) 2005-02-11 2006-08-17 Memorial Sloan Kettering Cancer Center Methods and compositions for detecting a drug resistant egfr mutant
WO2006101977A2 (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
JP2008540436A (ja) 2005-05-03 2008-11-20 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 Ｊａｋキナーゼインヒビターおよびそれらの使用
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006128172A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2626789A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrimidinones as casein kinase ii (ck2) modulators
WO2007053452A1 (en) 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CA2626479A1 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
JP2009520038A (ja) 2005-12-19 2009-05-21 ジェネンテック・インコーポレーテッド ピリミジンキナーゼインヒビター
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
EA200870217A1 (ru) 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
KR101411695B1 (ko) 2006-02-17 2014-07-03 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2353725T3 (es) 2006-03-30 2011-03-04 Tibotec Pharmaceuticals Pirimidinas sustituidas con 5-(hidroximetileno y aminometileno) que inhiben el vih.
AU2007233737B2 (en) 2006-03-30 2012-11-29 Janssen Sciences Ireland Uc HIV inhibiting 5-amido substituted pyrimidines
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
AU2007269540B2 (en) 2006-07-05 2013-06-27 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
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
DK2089369T3 (da) 2006-10-19 2011-05-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008064274A1 (en) 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
JP5208123B2 (ja) 2006-12-08 2013-06-12 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
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
US8318736B2 (en) 2006-12-29 2012-11-27 Janssen R&D Ireland HIV inhibiting 5,6-substituted pyrimidines
US9006243B2 (en) 2006-12-29 2015-04-14 Janssen R&D Ireland HIV inhibiting 6-substituted pyrimidines
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
JP4221470B2 (ja) 2007-02-01 2009-02-12 トヨタ自動車株式会社 電動車両制御装置及び電動車両制御方法
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
CA2681250A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
US20100105674A1 (en) 2007-03-20 2010-04-29 Deanda Jr Felix Chemical Compounds
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US8242271B2 (en) 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
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
BRPI0815979A2 (pt) 2007-08-28 2017-06-13 Irm Llc compostos e composições com inibidores de quinase, bem como uso dos mesmos
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
JP5600063B2 (ja) 2007-10-19 2014-10-01 セルジーン アビロミクス 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
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
RU2490015C2 (ru) 2008-02-22 2013-08-20 Райджел Фармасьютикалз, Инк. Применение 2,4-пиримидиндиаминов для лечения атеросклероза
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
US8205348B2 (en) 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
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.
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
CA2722326A1 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
JP2011523646A (ja) 2008-05-21 2011-08-18 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
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
WO2010077740A2 (en) 2008-12-09 2010-07-08 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2748758C (en) 2009-01-15 2017-06-13 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
US20120270237A9 (en) 2009-04-03 2012-10-25 Cellzone AG Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
MX2011011875A (es) 2009-05-08 2011-12-08 Astellas Pharma Inc Compuesto de carboxamida heterociclica diamino.
WO2010146132A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
WO2012061415A1 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
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 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CN102558149A (zh) 2010-12-29 2012-07-11 中国医学科学院药物研究所 嘧啶衍生物、及其制法和药物组合物与用途
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
DK2710007T3 (da) 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
JP6317320B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
SG11201503459SA (en) 2012-11-02 2015-06-29 Pharmacyclics Inc Tec family kinase inhibitor adjuvant therapy

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6908906B2 (en) * 2001-02-09 2005-06-21 Sankyo Company, Limited Crystalline forms of pyrimidine nucleoside derivative
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
RU2536584C2 (ru) * 2008-06-27 2014-12-27 Авила Терапьютикс, Инк. Гетероарильные соединения и их применение
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
WO2012021444A1 (en) * 2010-08-10 2012-02-16 Avila Therapeutics, Inc. Besylate salt of a btk inhibitor
RU2013109393A (ru) * 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
US8975249B2 (en) * 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
OGISO H; ET AL Crystal structure of the complex of human epidermal growth factor and receptor extracellular domains CELL, 20020920 CELL PRESS, USVol:110, Nr:6, Page(s): 775 - 787. *
RU 2013118648A1, приоритет 31.11.2011, опубл.10.12.2014 & *
RU2013109393 (A), 20.09.2014. *

Also Published As

Publication number Publication date
US20220062280A1 (en) 2022-03-03
HK1205431A1 (en) 2015-12-18
CN108658873A (zh) 2018-10-16
US9056839B2 (en) 2015-06-16
CN104302178B (zh) 2018-07-13
EP2825041B1 (en) 2021-04-21
IN2014DN07401A (enExample) 2015-04-24
WO2013138495A1 (en) 2013-09-19
AU2018201897A1 (en) 2018-04-12
AU2013201520A1 (en) 2013-10-03
US10946016B2 (en) 2021-03-16
MX2014010849A (es) 2014-12-10
CN108658873B (zh) 2021-09-14
US20160022677A1 (en) 2016-01-28
AU2013201520B2 (en) 2016-02-25
US20190151313A1 (en) 2019-05-23
RU2014136896A (ru) 2016-05-10
JP2018024713A (ja) 2018-02-15
SG10201700804XA (en) 2017-03-30
CA2866852A1 (en) 2013-09-19
US20130267530A1 (en) 2013-10-10
BR112014022789A2 (pt) 2021-05-25
KR20140145157A (ko) 2014-12-22
IL234425B (en) 2019-03-31
BR112014022789B1 (pt) 2022-04-19
US10004741B2 (en) 2018-06-26
ES2880109T3 (es) 2021-11-23
SG11201405691WA (en) 2014-10-30
ZA201407441B (en) 2022-05-25
MX356753B (es) 2018-06-12
JP6317319B2 (ja) 2018-04-25
KR102081042B1 (ko) 2020-02-26
AU2016203338A1 (en) 2016-06-16
EP2825041A4 (en) 2015-08-26
CA2866852C (en) 2020-12-29
CN104302178A (zh) 2015-01-21
AU2018201897B2 (en) 2019-10-31
MY169233A (en) 2019-03-19
US20170281623A1 (en) 2017-10-05
US9539255B2 (en) 2017-01-10
JP2015514060A (ja) 2015-05-18
EP2825041A1 (en) 2015-01-21

Similar Documents

Publication Publication Date Title
US10946016B2 (en) Solid forms of an epidermal growth factor receptor kinase inhibitor
RU2711077C2 (ru) Соли ингибитора киназы рецептора эпидермального фактора роста
US20160074399A1 (en) Salts of an Epidermal Growth Factor Receptor Kinase Inhibitor
HK1205431B (en) Solid forms of an epidermal growth factor receptor kinase inhibitor

Legal Events

Date Code Title Description
PC43 Official registration of the transfer of the exclusive right without contract for inventions

Effective date: 20190902