RU2711077C9 - Соли ингибитора киназы рецептора эпидермального фактора роста - Google Patents

Соли ингибитора киназы рецептора эпидермального фактора роста Download PDF

Info

Publication number
RU2711077C9
RU2711077C9 RU2014136893A RU2014136893A RU2711077C9 RU 2711077 C9 RU2711077 C9 RU 2711077C9 RU 2014136893 A RU2014136893 A RU 2014136893A RU 2014136893 A RU2014136893 A RU 2014136893A RU 2711077 C9 RU2711077 C9 RU 2711077C9
Authority
RU
Russia
Prior art keywords
compound
acid
salt
peaks
compound according
Prior art date
Application number
RU2014136893A
Other languages
English (en)
Russian (ru)
Other versions
RU2014136893A (ru
RU2711077C2 (ru
Inventor
Мэй ЛАЙ
Стивен Ричард ВИТОВСКИ
Ричланд Вэйн ТЕСТЕР
Квангхо ЛИ
Original Assignee
Селджен Кар Ллс
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 Кар Ллс filed Critical Селджен Кар Ллс
Publication of RU2014136893A publication Critical patent/RU2014136893A/ru
Publication of RU2711077C2 publication Critical patent/RU2711077C2/ru
Application granted granted Critical
Publication of RU2711077C9 publication Critical patent/RU2711077C9/ru

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/05Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/25Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
    • C07C309/27Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton containing carboxyl groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35Naphthalene sulfonic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/06Oxalic acid
    • C07C55/07Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/02Saturated compounds containing hydroxy or O-metal groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (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)
  • Air-Conditioning For Vehicles (AREA)
  • Electric Connection Of Electric Components To Printed Circuits (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
RU2014136893A 2012-03-15 2013-03-13 Соли ингибитора киназы рецептора эпидермального фактора роста RU2711077C9 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261611400P 2012-03-15 2012-03-15
US61/611,400 2012-03-15
PCT/US2013/030996 WO2013138502A1 (en) 2012-03-15 2013-03-13 Salts of an epidermal growth factor receptor kinase inhibitor

Publications (3)

Publication Number Publication Date
RU2014136893A RU2014136893A (ru) 2016-05-10
RU2711077C2 RU2711077C2 (ru) 2020-01-15
RU2711077C9 true RU2711077C9 (ru) 2020-08-11

Family

ID=49161781

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2014136893A RU2711077C9 (ru) 2012-03-15 2013-03-13 Соли ингибитора киназы рецептора эпидермального фактора роста

Country Status (28)

Country Link
US (5) US9108927B2 (cg-RX-API-DMAC7.html)
EP (1) EP2825042B1 (cg-RX-API-DMAC7.html)
JP (2) JP6317320B2 (cg-RX-API-DMAC7.html)
KR (1) KR102090453B1 (cg-RX-API-DMAC7.html)
CN (2) CN109053595B (cg-RX-API-DMAC7.html)
AR (1) AR090357A1 (cg-RX-API-DMAC7.html)
AU (3) AU2013201519C1 (cg-RX-API-DMAC7.html)
BR (1) BR112014022790B1 (cg-RX-API-DMAC7.html)
CA (1) CA2866857C (cg-RX-API-DMAC7.html)
CY (1) CY1122176T1 (cg-RX-API-DMAC7.html)
DK (1) DK2825042T3 (cg-RX-API-DMAC7.html)
ES (1) ES2698298T3 (cg-RX-API-DMAC7.html)
HR (1) HRP20181784T1 (cg-RX-API-DMAC7.html)
IL (1) IL234426B (cg-RX-API-DMAC7.html)
LT (1) LT2825042T (cg-RX-API-DMAC7.html)
MX (1) MX356179B (cg-RX-API-DMAC7.html)
MY (1) MY185243A (cg-RX-API-DMAC7.html)
PH (1) PH12014502037B1 (cg-RX-API-DMAC7.html)
PL (1) PL2825042T3 (cg-RX-API-DMAC7.html)
PT (1) PT2825042T (cg-RX-API-DMAC7.html)
RS (1) RS57901B1 (cg-RX-API-DMAC7.html)
RU (1) RU2711077C9 (cg-RX-API-DMAC7.html)
SG (2) SG11201405692UA (cg-RX-API-DMAC7.html)
SI (1) SI2825042T1 (cg-RX-API-DMAC7.html)
SM (1) SMT201800571T1 (cg-RX-API-DMAC7.html)
TR (1) TR201816244T4 (cg-RX-API-DMAC7.html)
TW (1) TWI591060B (cg-RX-API-DMAC7.html)
WO (1) WO2013138502A1 (cg-RX-API-DMAC7.html)

Families Citing this family (23)

* 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
NZ710636A (en) 2010-11-01 2017-02-24 Celgene Avilomics Res Inc Heterocyclic compounds and uses thereof
JP6317319B2 (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固体形態
ES2698298T3 (es) 2012-03-15 2019-02-04 Celgene Car Llc Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico
PE20151274A1 (es) 2013-02-08 2015-09-12 Celgene Avilomics Res Inc Inhibidores de erk y sus usos
EP2994456A4 (en) * 2013-05-06 2017-01-04 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
NO2718543T3 (cg-RX-API-DMAC7.html) * 2014-02-04 2018-01-06
DK3179858T3 (da) 2014-08-13 2019-07-22 Celgene Car Llc Forme og sammensætninger af en ERK-inhibitor
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
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
WO2017016463A1 (zh) * 2015-07-24 2017-02-02 上海海雁医药科技有限公司 Egfr抑制剂及其药学上可接受的盐和多晶型物及其应用
CN105461640B (zh) * 2015-12-02 2017-11-21 芷威(上海)化学科技有限公司 一种酪氨酸激酶抑制剂的制备方法
CN105481779B (zh) * 2015-12-24 2019-01-25 南京华威医药科技集团有限公司 抗癌药物Rociletinib及其中间体制备
JP7303108B2 (ja) 2016-12-22 2023-07-04 インサイト・コーポレイション 免疫調節剤としての二環式複素芳香環化合物
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
TWI798334B (zh) 2018-01-31 2023-04-11 大陸商迪哲(江蘇)醫藥股份有限公司 Erbb/btk抑制劑
EP4212529B1 (en) 2018-03-30 2025-01-29 Incyte Corporation Heterocyclic compounds as immunomodulators
EP4520328A3 (en) 2018-05-11 2025-04-16 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2021030162A1 (en) * 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
CR20220190A (es) 2019-09-30 2022-06-15 Incyte Corp Compuestos de pirido [3,2-d] primidina como inmunomoduladores
EP4058461A1 (en) * 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
PE20231438A1 (es) 2020-11-06 2023-09-14 Incyte Corp Proceso para hacer un inhibidor de pd-1/pd-l1 y sales y formas cristalinas del mismo
AU2022324410A1 (en) * 2021-08-02 2024-01-18 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Novel pharmaceutical salts and polymorphic forms of an erbb and btk inhibitor

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
RU2013118648A (ru) * 2010-11-01 2014-12-10 Селджен Авиломикс Рисерч, Инк. Гетероциклические соединения и их применение

Family Cites Families (161)

* 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
US4032637A (en) 1972-09-26 1977-06-28 Sandoz Ltd. Method of promoting sleep
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
US5453510A (en) 1990-07-13 1995-09-26 Burroughs Wellcome Co. Neuromuscular blocking agents
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
AU707323B2 (en) 1995-03-10 1999-07-08 Berlex Laboratories, Inc. Benzamidine derivatives 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
EP1054004B1 (en) 1997-12-15 2008-07-16 Astellas Pharma Inc. Novel pyrimidine-5-carboxamide derivatives
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
WO2000012485A1 (en) 1998-08-29 2000-03-09 Astrazeneca Ab Pyrimidine compounds
HU230394B1 (hu) 1998-11-10 2016-04-28 Janssen Pharmaceutica N.V. HIV-vírus szaporodását gátló pirimidin-származékok
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
CA2362401A1 (en) 1999-02-04 2000-08-10 Paul Fleming 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
PT1194415E (pt) 1999-06-29 2004-01-30 Egyt Gyogyszervegyeszeti Gyar Novos derivados da piperazinil-alquil-tiopirimidina composicoes farmaceuticas que os contem e um processo de preparacao da substancia activa
DE60043397D1 (de) 1999-12-28 2010-01-07 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
EP1257546A1 (en) 2000-02-17 2002-11-20 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2407754C (en) 2000-05-08 2009-09-15 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
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
AU2002363176B2 (en) 2001-11-01 2008-09-25 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3Beta inhibitors (GSK3 inhibitors)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
JP2005522438A (ja) 2002-02-08 2005-07-28 スミスクライン ビーチャム コーポレーション ピリミジン化合物
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
ES2445208T3 (es) 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias
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
CN102151270A (zh) 2003-02-07 2011-08-17 詹森药业有限公司 预防hiv感染的嘧啶衍生物
WO2004074244A2 (en) 2003-02-20 2004-09-02 Smithkline Beecham Corporation Pyrimidine compounds
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
PT1656372E (pt) 2003-07-30 2013-06-27 Rigel Pharmaceuticals Inc Métodos para o tratamento ou prevenção de doenças autoimunes com compostos de 2,4-pirimidinadiamina
DK1663242T3 (da) 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
BRPI0413616B8 (pt) 2003-08-15 2021-05-25 Irm Llc 2,4-pirimidinadiaminas, seus usos, e composição farmacêutica
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
WO2005063722A1 (en) 2003-12-19 2005-07-14 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
JP5283336B2 (ja) 2004-01-12 2013-09-04 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド 選択的キナーゼ阻害剤
UA85698C2 (ru) 2004-01-16 2009-02-25 Уайет Хинолиновые промежуточные соединения для синтеза ингибиторов рецепторной тирозинкиназы и способ их получения
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
WO2005118544A2 (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
EP3042964A1 (en) 2004-06-04 2016-07-13 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
AU2005286592A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
MX2007003798A (es) 2004-09-30 2007-04-23 Tibotec Pharm Ltd Pirimidinas 5-sustituidas con carbociclos o heterociclos inhibidoras del vih.
RU2007114080A (ru) 2004-10-13 2008-11-27 Вайет (Us) N-бензилсульфонил-замещенные аналоги анилинопиримидина
EP1805208A2 (en) 2004-10-20 2007-07-11 Proteolix, Inc. Labeled compounds for proteasome inhibition
US7919487B2 (en) 2004-11-10 2011-04-05 Synta Pharmaceuticals Corporation Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
JP5095409B2 (ja) 2004-11-24 2012-12-12 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 スピロ2,4−ピリミジンジアミン化合物およびその使用
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
WO2006076706A1 (en) 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
AU2006206458B2 (en) 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
CA2597673C (en) 2005-02-11 2014-07-08 Harold Varmus Methods and compositions for detecting a drug resistant egfr mutant
MX2007011500A (es) 2005-03-16 2007-11-21 Targegen Inc Compuestos pirimidina y metodos de uso.
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
US20060270694A1 (en) 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
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
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
NZ563454A (en) 2005-06-08 2011-03-31 Rigel Pharmaceuticals Inc 2,4-diaminopyrimidine derivatives 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
ATE517874T1 (de) 2005-10-21 2011-08-15 Exelixis Inc Pyrimidinone als modulatoren von caseinkinase ii (ck2)
MX391408B (es) 2005-11-01 2025-03-21 Impact Biomedicines Inc Inhibidores de biaril meta-pirimidina de cinasas.
CN101300234A (zh) 2005-11-03 2008-11-05 Irm责任有限公司 蛋白激酶抑制剂
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
JP2009525337A (ja) 2006-01-30 2009-07-09 エクセリクシス, インク. Jak−2調節因子としての4−アリール−2−アミノ−ピリミジン類又は4−アリール−2−アミノアルキル−ピリミジン類と使用方法
SI1984357T1 (sl) 2006-02-17 2014-02-28 Rigel Pharmaceuticals, Inc. Spojine 2,4-pirimidindiamina za zdravljenje ali preventivo avtoimunih bolezni
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8933089B2 (en) 2006-03-30 2015-01-13 Janssen R & D Ireland HIV inhibiting 5-amido substituted pyrimidines
CA2645959C (en) 2006-03-30 2016-05-17 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
CA2650035C (en) 2006-04-27 2015-02-03 Intezyne Technologies, Inc. Poly (ethylene glycol) containing chemically disparate endgroups
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
EP2046759A1 (en) 2006-07-21 2009-04-15 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
NZ601278A (en) 2006-09-22 2013-09-27 Pharmacyclics Inc 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
EP2078026B1 (en) 2006-11-21 2012-01-04 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
MX2009006081A (es) 2006-12-08 2009-06-17 Irmc Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
CN101563327A (zh) 2006-12-19 2009-10-21 健泰科生物技术公司 嘧啶类激酶抑制剂
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
BRPI0720858B8 (pt) 2006-12-29 2021-05-25 Janssen R & D Ireland pirimidinas 6-substituídas inibidoras de hiv e composição farmacêutica que as compreende
JP5283633B2 (ja) 2006-12-29 2013-09-04 テイボテク・フアーマシユーチカルズ Hiv阻害性5,6−置換ピリミジン
TW200902010A (en) 2007-01-26 2009-01-16 Smithkline Beecham Corp Anthranilamide inhibitors of aurora kinase
US8846704B2 (en) 2007-01-31 2014-09-30 YM Biosciences Austraila 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
AU2008229147A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
US20100113445A1 (en) 2007-03-20 2010-05-06 Smithkline Beecham Corporation Chemical Compounds
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) 2007-03-26 2010-11-16 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
WO2008151183A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
AU2008275918B2 (en) 2007-07-17 2014-01-30 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as PKC inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US8440681B2 (en) 2007-08-28 2013-05-14 Irm Llc 2-biphenylamino-4-aminopyrimidine derivatives as kinase inhibitors
WO2009029682A1 (en) 2007-08-28 2009-03-05 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
US7982036B2 (en) 2007-10-19 2011-07-19 Avila Therapeutics, Inc. 4,6-disubstitued pyrimidines useful as kinase inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US20110028405A1 (en) 2007-12-20 2011-02-03 Richard John Harrison Sulfamides as zap-70 inhibitors
AU2009215430B2 (en) 2008-02-22 2015-02-12 Rigel Pharmaceuticals, Inc. Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
WO2009112490A1 (en) 2008-03-11 2009-09-17 Cellzome Limited 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
US8871753B2 (en) 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
MX2011000661A (es) 2008-07-16 2011-05-25 Pharmacyclics Inc Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos.
CN102203070A (zh) 2008-09-03 2011-09-28 拜尔农作物科学股份公司 烷氧基-和烷硫基-取代的苯胺基嘧啶类化合物
WO2010077740A2 (en) 2008-12-09 2010-07-08 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
EP2387586B1 (en) 2009-01-15 2014-12-17 F. Hoffmann-La Roche AG Antibodies against human epo receptor
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
RS57045B1 (sr) 2009-05-08 2018-05-31 Astellas Pharma Inc Jedinjenje diamino heterocikličnog karboksamida
EP2443095A1 (en) 2009-06-18 2012-04-25 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
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
EP2575818A4 (en) 2010-06-03 2013-11-06 Pharmacyclics Inc USE OF BRUTON TYROSINE KINASE INHIBITORS (BTK)
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012061415A1 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
JP5957003B2 (ja) 2010-11-10 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 変異体選択的egfr阻害剤およびその使用
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
MX355728B (es) 2011-05-17 2018-04-27 Univ California Inhibidores de cinasas.
JP6317319B2 (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固体形態
ES2698298T3 (es) 2012-03-15 2019-02-04 Celgene Car Llc Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico
MX2015005633A (es) 2012-11-02 2016-02-03 Pharmacyclics Inc Terapia adyuvante con inhibidores de quinasa de la familia tec.
EP2994456A4 (en) 2013-05-06 2017-01-04 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor

Patent Citations (8)

* 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
RU2013118648A (ru) * 2010-11-01 2014-12-10 Селджен Авиломикс Рисерч, Инк. Гетероциклические соединения и их применение
US8975249B2 (en) * 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof

Non-Patent Citations (2)

* 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, CELL PRESS, US, 2002,Vol:110, Nr:6, Page(s):775-787. *
RU 2013118648 A1, приоритет 31.11.2011, опубл.10.12.2014 & US 8975249 B2. *

Also Published As

Publication number Publication date
TW201341372A (zh) 2013-10-16
CA2866857C (en) 2021-03-09
US20210017137A1 (en) 2021-01-21
US10005738B2 (en) 2018-06-26
LT2825042T (lt) 2018-12-10
AU2016203343A1 (en) 2016-06-16
US20130267531A1 (en) 2013-10-10
AU2013201519A1 (en) 2013-10-03
HK1205430A1 (en) 2015-12-18
TWI591060B (zh) 2017-07-11
RU2014136893A (ru) 2016-05-10
CN104284584B (zh) 2019-06-04
DK2825042T3 (en) 2018-11-26
EP2825042B1 (en) 2018-08-01
BR112014022790B1 (pt) 2022-04-19
PH12014502037B1 (en) 2019-07-17
PH12014502037A1 (en) 2014-11-24
CA2866857A1 (en) 2013-09-19
CN109053595A (zh) 2018-12-21
CY1122176T1 (el) 2020-07-31
WO2013138502A1 (en) 2013-09-19
TR201816244T4 (tr) 2018-11-21
MX2014010848A (es) 2014-12-10
KR102090453B1 (ko) 2020-03-19
AR090357A1 (es) 2014-11-05
US9540335B2 (en) 2017-01-10
JP6317320B2 (ja) 2018-04-25
RU2711077C2 (ru) 2020-01-15
JP2018024708A (ja) 2018-02-15
JP2015510890A (ja) 2015-04-13
IL234426B (en) 2018-07-31
US20170217904A1 (en) 2017-08-03
HRP20181784T1 (hr) 2018-12-28
US20190152925A1 (en) 2019-05-23
AU2018201896B2 (en) 2019-10-31
PT2825042T (pt) 2018-11-16
EP2825042A4 (en) 2015-09-23
SG10201700799WA (en) 2017-02-27
CN104284584A (zh) 2015-01-14
RS57901B1 (sr) 2019-01-31
US10570099B2 (en) 2020-02-25
SG11201405692UA (en) 2014-10-30
SMT201800571T1 (it) 2019-01-11
AU2013201519C1 (en) 2016-06-23
US9108927B2 (en) 2015-08-18
AU2013201519B2 (en) 2016-02-25
SI2825042T1 (sl) 2019-01-31
CN109053595B (zh) 2022-04-01
PL2825042T3 (pl) 2019-02-28
ES2698298T3 (es) 2019-02-04
BR112014022790A2 (cg-RX-API-DMAC7.html) 2017-06-20
KR20140138941A (ko) 2014-12-04
MY185243A (en) 2021-04-30
US11292772B2 (en) 2022-04-05
MX356179B (es) 2018-05-17
JP6676602B2 (ja) 2020-04-08
EP2825042A1 (en) 2015-01-21
US20150344441A1 (en) 2015-12-03
AU2018201896A1 (en) 2018-04-12

Similar Documents

Publication Publication Date Title
RU2711077C9 (ru) Соли ингибитора киназы рецептора эпидермального фактора роста
RU2673077C2 (ru) Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста
US20160074399A1 (en) Salts of an Epidermal Growth Factor Receptor Kinase Inhibitor
HK1205430B (en) Salts of an epidermal growth factor receptor kinase inhibitor

Legal Events

Date Code Title Description
HZ9A Changing address for correspondence with an applicant
TH4A Reissue of patent specification