JP6068340B2 - Btk阻害剤のベシル酸塩 - Google Patents

Btk阻害剤のベシル酸塩 Download PDF

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JP6068340B2
JP6068340B2 JP2013524147A JP2013524147A JP6068340B2 JP 6068340 B2 JP6068340 B2 JP 6068340B2 JP 2013524147 A JP2013524147 A JP 2013524147A JP 2013524147 A JP2013524147 A JP 2013524147A JP 6068340 B2 JP6068340 B2 JP 6068340B2
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スティーブン リチャード ウィトウスキ,
スティーブン リチャード ウィトウスキ,
ウィリアム フレデリック ザ サード ウェストリン,
ウィリアム フレデリック ザ サード ウェストリン,
リッチランド ウェイン テスター,
リッチランド ウェイン テスター,
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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
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
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    • 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
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/02Immunomodulators
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    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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

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  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
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  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
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  • Endocrinology (AREA)
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  • Neurology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013524147A 2010-08-10 2011-08-08 Btk阻害剤のベシル酸塩 Expired - Fee Related JP6068340B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37234910P 2010-08-10 2010-08-10
US61/372,349 2010-08-10
PCT/US2011/046926 WO2012021444A1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor

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JP2013533314A JP2013533314A (ja) 2013-08-22
JP2013533314A5 JP2013533314A5 (https=) 2014-09-18
JP6068340B2 true JP6068340B2 (ja) 2017-01-25

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US (2) US8563568B2 (https=)
EP (2) EP2603081B1 (https=)
JP (1) JP6068340B2 (https=)
KR (1) KR20130099040A (https=)
CN (2) CN103096716B (https=)
AR (1) AR082600A1 (https=)
AU (1) AU2011289604C1 (https=)
BR (1) BR112013003388A2 (https=)
CA (1) CA2807051A1 (https=)
DK (1) DK2603081T3 (https=)
ES (1) ES2617763T3 (https=)
IL (1) IL224271A (https=)
MX (1) MX336875B (https=)
MY (1) MY160734A (https=)
NZ (1) NZ607845A (https=)
PH (1) PH12013500246A1 (https=)
PT (1) PT2603081T (https=)
RU (1) RU2013109393A (https=)
SG (1) SG187796A1 (https=)
TW (1) TWI533872B (https=)
WO (1) WO2012021444A1 (https=)
ZA (1) ZA201301802B (https=)

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2526933T3 (en) 2006-09-22 2015-05-18 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
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
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
CA2730930C (en) 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス, インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
CA3007787C (en) 2010-06-03 2020-03-10 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (btk)
MX336875B (es) * 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
EP2635284B1 (en) 2010-11-01 2019-12-18 Celgene CAR LLC Heterocyclic compounds and uses thereof
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
CA2866852C (en) * 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
BR112014022790B1 (pt) * 2012-03-15 2022-04-19 Celgene Car Llc Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2013173518A1 (en) 2012-05-16 2013-11-21 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
KR20210033067A (ko) 2012-06-04 2021-03-25 파마싸이클릭스 엘엘씨 브루톤 타이로신 키나아제 저해제의 결정 형태
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
WO2014039452A1 (en) * 2012-09-04 2014-03-13 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
SI2892900T1 (en) 2012-09-10 2018-01-31 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
EA201590855A1 (ru) 2012-11-15 2015-11-30 Фармасайкликс, Инк. Соединения пирролопиримидина как ингибиторы киназ
WO2014081709A2 (en) * 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
WO2014081714A2 (en) * 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US20140142128A1 (en) * 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
WO2014081712A2 (en) * 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US9126950B2 (en) 2012-12-21 2015-09-08 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.
US20160030426A1 (en) * 2013-03-14 2016-02-04 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2014155300A2 (en) * 2013-03-28 2014-10-02 Aurigene Discovery Technologies Limited Substitued pyrimidine amine derivatives as tak-1 inhibitors
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CA2909579A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
CA2902686C (en) 2013-04-25 2017-01-24 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
EP2991651A1 (en) * 2013-05-03 2016-03-09 Celgene Corporation Methods for treating cancer using combination therapy
EP2994456A4 (en) * 2013-05-06 2017-01-04 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法
US9415050B2 (en) 2013-08-12 2016-08-16 Pharmacyclics Llc Methods for the treatment of HER2 amplified cancer
US20150064172A1 (en) * 2013-08-27 2015-03-05 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
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
CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
CN103694241A (zh) 2013-11-27 2014-04-02 苏州晶云药物科技有限公司 Pci-32765的新晶型a及其制备方法
CN105979948A (zh) 2013-12-05 2016-09-28 安塞塔制药公司 Pi3k抑制剂和btk抑制剂的治疗组合
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN112353806A (zh) * 2014-02-21 2021-02-12 普林斯匹亚生物制药公司 Btk抑制剂的盐和固体形式
WO2015134805A1 (en) * 2014-03-07 2015-09-11 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
WO2015185998A2 (en) 2014-04-11 2015-12-10 Acerta Pharma B.V. Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase
US9937171B2 (en) 2014-04-11 2018-04-10 Acerta Pharma B.V. Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
AU2015296215A1 (en) 2014-08-01 2017-03-23 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
TW201618783A (zh) 2014-08-07 2016-06-01 艾森塔製藥公司 以布魯頓(Bruton)氏酪胺酸激酶(BTK)佔據和BTK再合成速率為基礎之治療癌症、免疫和自體免疫疾病及發炎性疾病之方法
KR20170033358A (ko) 2014-08-07 2017-03-24 파마싸이클릭스 엘엘씨 브루톤 티로신 키나아제 저해제의 신규한 제제
TW201618774A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 使用btk抑制劑透過調變腫瘤微環境來治療實體腫瘤及其他疾病之方法
TW201618775A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Btk抑制劑、pi3k抑制劑、jak-2抑制劑、pd-1抑制劑及/或pd-l1抑制劑之治療組合物
PL3179991T3 (pl) 2014-08-11 2022-02-14 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2
AR101504A1 (es) 2014-08-11 2016-12-21 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
WO2016087994A1 (en) 2014-12-05 2016-06-09 Acerta Pharma B.V. Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment
SG11201704808VA (en) 2014-12-18 2017-07-28 Principia Biopharma Inc Treatment of pemphigus
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibitor
WO2016210165A1 (en) 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2017033113A1 (en) 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
WO2017046746A1 (en) 2015-09-15 2017-03-23 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor and a gitr binding molecule, a 4-1bb agonist, or an ox40 agonist
EP3747472B1 (en) 2015-09-15 2024-04-03 Acerta Pharma B.V. Therapeutic combinations of a cd19 inhibitor and a btk inhibitor
DK3402503T3 (da) 2016-01-13 2020-12-21 Acerta Pharma Bv Terapeutiske kombinationer af et antifolat og en btk-hæmmer
CN115054586B (zh) 2016-06-29 2024-08-02 普林斯匹亚生物制药公司 改性的释放制剂
US10864203B2 (en) 2016-07-05 2020-12-15 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
WO2018033853A2 (en) 2016-08-16 2018-02-22 Beigene, Ltd. Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
WO2018033135A1 (en) 2016-08-19 2018-02-22 Beigene, Ltd. Use of a combination comprising a btk inhibitor for treating cancers
IL292938A (en) 2016-09-19 2022-07-01 Mei Pharma Inc Combined treatment
CA3045339A1 (en) 2016-12-03 2018-06-07 Juno Therapeutics, Inc. Methods and compositions for use of therapeutic t cells in combination with kinase inhibitors
US20190376971A1 (en) 2017-01-19 2019-12-12 Acerta Pharma B.V. Compositions and Methods for the Assessment of Drug Target Occupancy for Bruton's Tyrosine Kinase
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
TWI787284B (zh) 2017-06-22 2022-12-21 美商西建公司 以b型肝炎病毒感染表徵之肝細胞癌之治療
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
KR20210038877A (ko) 2018-07-25 2021-04-08 노파르티스 아게 Nlrp3 인플라마좀 억제제
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
US20220249491A1 (en) 2019-06-10 2022-08-11 Beigene Switzerland Gmbh Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
US20210106584A1 (en) 2019-10-14 2021-04-15 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US11814390B2 (en) 2020-01-22 2023-11-14 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
JP7545570B2 (ja) 2020-08-14 2024-09-04 ノバルティス アーゲー ヘテロアリール置換スピロピペリジニル誘導体及びその薬学的使用
WO2022161484A1 (en) * 2021-01-30 2022-08-04 Beigene, Ltd. Methods of treating chronic active antibody-mediated rejection using btk inhibitors
EP4313023A1 (en) 2021-04-02 2024-02-07 Biogen MA Inc. Combination treatment methods of multiple sclerosis
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3

Family Cites Families (165)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4032637A (en) * 1972-09-26 1977-06-28 Sandoz Ltd. Method of promoting sleep
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
DE69630214T2 (de) 1995-03-10 2004-07-15 Berlex Laboratories, Inc., Richmond Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
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
ATE342892T1 (de) 1998-08-29 2006-11-15 Astrazeneca Ab Pyrimidine verbindungen
SK287270B6 (sk) 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Derivát pyrimidínu
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
AU2871900A (en) 1999-02-04 2000-08-25 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
DE60004671T2 (de) * 1999-06-29 2004-07-29 EGIS Gyógyszergyár Rt. Neue piperazinylalkylthiopyrimidine derivate, diese enthaltende pharmazeutische zusammenstellungen und verfahren zu deren herstellung
EP1246823A1 (en) 1999-12-28 2002-10-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
AU3704101A (en) 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
GB0004887D0 (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
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AU782948B2 (en) 2000-05-08 2005-09-15 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University 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
HUP0402106A3 (en) 2001-11-01 2009-07-28 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors, process for their preparation and pharmaceutical compositions containing them
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
AU2003209077A1 (en) 2002-02-08 2003-09-02 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
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
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
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
BRPI0407329A (pt) 2003-02-07 2006-01-10 Janssen Pharmaceutica Nv Derivados de pirimidina para a prevenção de infecção de hiv
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
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
PT1660458E (pt) 2003-08-15 2012-04-27 Novartis Ag 2,4-pirimidinodiaminas úteis no tratamento de doenças neoplásicas, desordens inflamatórias e do sistema imunitário
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 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
DK1704145T3 (da) 2004-01-12 2012-09-24 Ym Biosciences Australia Pty Selektive kinaseinhibitorer
GT200500008A (es) 2004-01-16 2005-08-16 Intermediarios de quinolina como inhibidores de receptores de tirosina quinasas y la sintesis de los mismos
CA2557794A1 (en) 2004-03-15 2005-10-06 Eli Lilly And Company 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
US7754714B2 (en) 2004-05-18 2010-07-13 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
CA2581454A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
ES2371924T3 (es) 2004-09-30 2012-01-11 Tibotec Pharmaceuticals Pirimidinas 5-carbo o heterociclo- sustituidas que inhiben el hiv.
JP2008515986A (ja) 2004-10-13 2008-05-15 ワイス N−ベンゼンスルホニル置換アニリノ−ピリミジン類似物
US20060088471A1 (en) 2004-10-20 2006-04-27 Proteolix, Inc. Compounds for enzyme inhibition
TW200628463A (en) 2004-11-10 2006-08-16 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
SI1814878T1 (sl) 2004-11-24 2012-06-29 Rigel Pharmaceuticals Inc Spojine spiro-2,4-pirimidindiamina in njihova uporaba
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
AU2006204724A1 (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
EP2505591A1 (en) 2005-02-11 2012-10-03 Memorial Sloan-Kettering Cancer Center Methods and compositions for detecting a drug resistant EGFR mutant
JP2008533166A (ja) 2005-03-16 2008-08-21 ターゲジェン インコーポレーティッド ピリミジン化合物および使用法
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
EP1883302A4 (en) 2005-05-03 2009-05-20 Rigel Pharmaceuticals Inc JAK KINASE HEMMER AND ITS USE
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8372851B2 (en) 2005-10-21 2013-02-12 Exelixis, Inc. Pyrazolo pyrimidines as casein kinase II (CK2) modulators
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
JP2009514876A (ja) 2005-11-03 2009-04-09 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のための化合物および組成物
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US20080318989A1 (en) 2005-12-19 2008-12-25 Burdick Daniel J Pyrimidine Kinase Inhibitors
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
KR20080110998A (ko) 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Jak­2 조절자로서 4­아릴­2­아미노­피리미딘 또는 4­아릴­2­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
US7659280B2 (en) 2006-02-17 2010-02-09 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
CN101405283B (zh) 2006-03-30 2014-06-18 泰博特克药品有限公司 Hiv抑制性5-酰氨基取代的嘧啶类化合物
ES2353725T3 (es) 2006-03-30 2011-03-04 Tibotec Pharmaceuticals Pirimidinas sustituidas con 5-(hidroximetileno y aminometileno) que inhiben el vih.
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
WO2007136790A2 (en) 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
EP2043651A2 (en) 2006-07-05 2009-04-08 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
DK2526933T3 (en) 2006-09-22 2015-05-18 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
JP5161233B2 (ja) 2006-10-19 2013-03-13 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 自己免疫疾患の処置のためのjakキナーゼの阻害剤としての2,4−ピリミジンアミン誘導体
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
ATE540041T1 (de) 2006-11-21 2012-01-15 Rigel Pharmaceuticals Inc Prodrug-salze von 2,4-pyrimidindiaminverbindungen und anwendungen davon
EA017405B9 (ru) 2006-12-08 2014-05-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
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
AU2007341227C1 (en) 2006-12-29 2013-08-29 Janssen Sciences Ireland Uc HIV inhibiting 6-substituted pyrimidines
AU2007341228B2 (en) 2006-12-29 2013-04-18 Janssen Sciences Ireland Uc HIV inhibiting 5,6-substituted pyrimidines
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
PT2114900T (pt) 2007-01-31 2019-01-17 Ym Biosciences Australia Pty Compostos à base de tiopirimidina e as suas utilizações
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
EA200901133A1 (ru) 2007-03-20 2010-04-30 Смитклайн Бичем Корпорейшн Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
EP2136635A4 (en) 2007-03-20 2011-07-27 Glaxosmithkline Llc 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
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
TWI433677B (zh) 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
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
EA017252B1 (ru) 2007-08-28 2012-11-30 Айрм Ллк Производные 2-бифениламино-4-аминопиримидина в качестве ингибиторов киназ
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
AU2008296479A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
MX2010009159A (es) 2008-02-22 2010-09-14 Rigel Pharmaceuticals Inc Uso de 2,4-pirimidindiaminas para el tratamiento de aterosclerosis.
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
SG165655A1 (en) 2008-04-16 2010-11-29 Portola Pharm Inc 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
ES2597441T3 (es) 2008-04-16 2017-01-18 Portola Pharmaceuticals, Inc. 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de las syk o JAK quinasas
EP2274288A2 (en) 2008-04-24 2011-01-19 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
CA2730930C (en) 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
US20110245156A1 (en) 2008-12-09 2011-10-06 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2965031C (en) 2009-01-15 2018-12-04 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
CA2757671A1 (en) 2009-04-03 2010-10-07 Cellzome Ag Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
US9908884B2 (en) 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
LT3009428T (lt) 2009-05-08 2018-04-10 Astellas Pharma Inc. Diamino heterociklinis karboksamido junginys
CA2763720A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7718662B1 (en) * 2009-10-12 2010-05-18 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
CA3007787C (en) 2010-06-03 2020-03-10 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (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
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
EP2635284B1 (en) 2010-11-01 2019-12-18 Celgene CAR LLC Heterocyclic compounds and uses thereof
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. 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
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2770550T3 (es) 2011-05-17 2020-07-02 Univ California Inhibidores de quinasa
MX391121B (es) 2011-10-19 2025-03-19 Pharmacyclics Llc Uso de inhibidores de la tirosina cinasa de bruton (btk).
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
TW201427664A (zh) 2012-11-02 2014-07-16 Pharmacyclics Inc Tec家族激酶抑制劑佐劑療法
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法

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