AU2017269335B2 - EGFR inhibitor compounds - Google Patents

EGFR inhibitor compounds Download PDF

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Publication number
AU2017269335B2
AU2017269335B2 AU2017269335A AU2017269335A AU2017269335B2 AU 2017269335 B2 AU2017269335 B2 AU 2017269335B2 AU 2017269335 A AU2017269335 A AU 2017269335A AU 2017269335 A AU2017269335 A AU 2017269335A AU 2017269335 B2 AU2017269335 B2 AU 2017269335B2
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AU
Australia
Prior art keywords
compound
optionally substituted
cancer
alkyl
egfr
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AU2017269335A
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AU2017269335A1 (en
Inventor
Sunny Abraham
Kevin Duane Bunker
Chad Daniel Hopkins
Peter Qinhua HUANG
Joseph Robert Pinchman
Deborah Helen Slee
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Recurium IP Holdings LLC
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Recurium IP Holdings LLC
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Publication of AU2017269335A1 publication Critical patent/AU2017269335A1/en
Assigned to RECURIUM IP HOLDINGS, LLC reassignment RECURIUM IP HOLDINGS, LLC Amend patent request/document other than specification (104) Assignors: Zeno Royalties & Milestones, LLC
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Publication of AU2017269335B2 publication Critical patent/AU2017269335B2/en
Priority to AU2021240162A priority Critical patent/AU2021240162A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C13/00—Cyclic hydrocarbons containing rings other than, or in addition to, six-membered aromatic rings
    • C07C13/28—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof
    • C07C13/32—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings
    • C07C13/36—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with a bicyclo ring system containing five carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/38—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/38—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing five carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2017269335A 2016-05-26 2017-05-24 EGFR inhibitor compounds Active AU2017269335B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2021240162A AU2021240162A1 (en) 2016-05-26 2021-09-29 EGFR inhibitor compounds

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662342141P 2016-05-26 2016-05-26
US62/342,141 2016-05-26
PCT/US2017/034163 WO2017205459A1 (en) 2016-05-26 2017-05-24 Egfr inhibitor compounds

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2021240162A Division AU2021240162A1 (en) 2016-05-26 2021-09-29 EGFR inhibitor compounds

Publications (2)

Publication Number Publication Date
AU2017269335A1 AU2017269335A1 (en) 2018-12-13
AU2017269335B2 true AU2017269335B2 (en) 2021-07-01

Family

ID=60411884

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2017269335A Active AU2017269335B2 (en) 2016-05-26 2017-05-24 EGFR inhibitor compounds
AU2021240162A Abandoned AU2021240162A1 (en) 2016-05-26 2021-09-29 EGFR inhibitor compounds

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2021240162A Abandoned AU2021240162A1 (en) 2016-05-26 2021-09-29 EGFR inhibitor compounds

Country Status (16)

Country Link
US (3) US10513509B2 (https=)
EP (1) EP3464275B1 (https=)
JP (1) JP7030066B2 (https=)
KR (2) KR20220130249A (https=)
CN (2) CN112624954A (https=)
AR (1) AR110038A1 (https=)
AU (2) AU2017269335B2 (https=)
CA (1) CA3023176A1 (https=)
ES (1) ES2979136T3 (https=)
IL (2) IL263081B (https=)
MX (2) MX383920B (https=)
RU (1) RU2751341C2 (https=)
SG (2) SG11201809751XA (https=)
TW (1) TWI752033B (https=)
WO (1) WO2017205459A1 (https=)
ZA (1) ZA201807399B (https=)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX383920B (es) * 2016-05-26 2025-03-14 Recurium Ip Holdings Llc Compuestos inhibidores de egfr.
CN108864079B (zh) * 2017-05-15 2021-04-09 深圳福沃药业有限公司 一种三嗪化合物及其药学上可接受的盐
IL272875B2 (en) 2017-09-11 2023-10-01 Recurium Ip Holdings Llc Continuous flow processes for the preparation of bicyclic compounds
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
CN110041302B (zh) * 2019-03-01 2021-11-30 南方医科大学 2-氨基-4-取代吡啶衍生物及其合成方法和应用
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
US20220340547A1 (en) * 2019-05-22 2022-10-27 Shanghi Hansoh Biosoh Biomedical Co., Ltd. Indole derivative-containing inhibitor, preparation method therefor and application thereof
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
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
US20230234941A1 (en) * 2020-06-23 2023-07-27 Shenzhen Forward Pharmaceuticals Co., Limited. Salts of Compound and Pharmaceutical Compositions Containing the Same
US20240226101A1 (en) * 2021-04-30 2024-07-11 Suzhou Puhe BioPharma Co., Ltd. Pyrimidinylaminobenzenes for lung cancer treatment
CA3226006A1 (en) * 2021-07-13 2023-01-19 Korea Research Institute Of Chemical Technology Novel pyrimidine-2,4-diamine derivatives, preparation method therefor, and pharmaceutical composition containing same as active ingredient for prevention or treatment of cancer
EP4403541B1 (en) * 2021-09-13 2026-02-04 FUJIFILM Corporation Method for producing halogenobicyclo[1.1.1]pentane
AU2023347153A1 (en) * 2022-09-19 2025-05-01 Advenchen Pharmaceuticals, LLC Novel pyrimidine compound as kinase inhibitors with biological activities on egfr mutants
WO2024094064A1 (en) * 2022-11-02 2024-05-10 Suzhou Puhe Biopharma Co., Ltd Pyrimidinylaminobenzenes for treating lung cancer with distant metastasis
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015195228A1 (en) * 2014-06-19 2015-12-23 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1051350A (en) 1910-02-02 1913-01-21 Thomas Nogier Apparatus for the sterilization of liquids.
DE4124942A1 (de) 1991-07-27 1993-01-28 Thomae Gmbh Dr K 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
WO1995009847A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag Pyrimidineamine derivatives and processes for the preparation thereof
TW440563B (en) 1996-05-23 2001-06-16 Hoffmann La Roche Aryl pyrimidine derivatives and a pharmaceutical composition thereof
ATE337312T1 (de) 2001-07-03 2006-09-15 Vertex Pharma Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
US7396940B2 (en) 2003-10-23 2008-07-08 Hoffmann-La Roche Inc. Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid
JP2008502687A (ja) 2004-06-14 2008-01-31 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
WO2006026754A2 (en) 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
WO2006096564A1 (en) 2005-03-04 2006-09-14 Merck & Co., Inc. Fused aromatic compounds having anti-diabetic activity
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
US20100267707A1 (en) 2006-06-22 2010-10-21 Merck Sharp & Dohme Corp. Tyrosine Kinase Inhibitors
WO2008024978A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
AU2008248186B2 (en) 2007-05-07 2014-02-06 Merck Sharp & Dohme Corp. Method of treatment using fused aromatic compounds having anti-diabetic activity
JP2010031249A (ja) 2008-06-23 2010-02-12 Sumitomo Chemical Co Ltd 組成物及び該組成物を用いてなる発光素子
NZ603525A (en) * 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
GB0815369D0 (en) 2008-08-22 2008-10-01 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
DE102008052943A1 (de) * 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
US8846673B2 (en) 2009-08-11 2014-09-30 Bristol-Myers Squibb Company Azaindazoles as kinase inhibitors and use thereof
JP2013504325A (ja) 2009-09-09 2013-02-07 アビラ セラピューティクス， インコーポレイテッド Ｐｉ３キナーゼインヒビターおよびその使用
KR101116234B1 (ko) 2009-10-29 2014-03-06 (주)퓨쳐켐 (3-플루오로-2-히드록시)프로필 작용기가 도입된 아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
ES2552462T3 (es) 2010-10-14 2015-11-30 Jw Pharmaceutical Corporation Nuevo compuesto de un mimético de giro inverso y un procedimiento de producción y uso del mismo
MX2013010513A (es) 2011-03-16 2013-10-07 Hoffmann La Roche Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos.
CN103608014A (zh) 2011-03-24 2014-02-26 罗楹 激酶抑制剂在治疗和预防炎症疾病中的用途
EP4119551A1 (en) * 2011-07-27 2023-01-18 Astrazeneca AB 2-(2,4,5-substituted-anilino)pyrimidine compounds
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
CN103508961B (zh) 2012-06-26 2015-07-22 中美冠科生物技术（太仓）有限公司 抗肿瘤药物
US9738610B2 (en) 2012-09-24 2017-08-22 Whitehead Institute For Biomedical Research Indazole derivatives and uses thereof
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
MX361088B (es) 2012-11-21 2018-11-26 Janssen Biotech Inc Anticuerpos del receptor del factor de crecimiento epidérmico aislado/del receptor del factor de crecimiento de hepatocitos (egfr/c-met) biespecíficos.
US9695228B2 (en) 2012-11-21 2017-07-04 Janssen Biotech, Inc. EGFR and c-Met fibronectin type III domain binding molecules
BR112015027114B1 (pt) 2013-04-29 2021-12-21 Chong Kun Dang Pharmaceutical Corp Compostos inibidores seletivos de histona desacetilase e seu uso
US20180057603A1 (en) 2013-08-09 2018-03-01 The Trustees Of The University Of Pennsylvania Combination of IFN-gamma with Anti-ERBB Antibody for the Treatment of Cancers
EA034866B1 (ru) 2013-08-30 2020-03-31 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Замещенные пиримидиновые ингибиторы bmi-1
WO2015035410A1 (en) 2013-09-09 2015-03-12 Triact Therapeutic, Inc. Cancer therapy
CA2925057A1 (en) 2013-10-01 2015-04-09 Simon T. BARRY Methods of treating and diagnosing alpha-v-beta-6 overexpressing cancer
GB201400034D0 (en) 2014-01-02 2014-02-19 Astrazeneca Ab Pharmaceutical Compositions comprising AZD9291
CN104761544B (zh) 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
WO2015112705A2 (en) 2014-01-24 2015-07-30 Clovis Oncology, Inc. Therapeutic combinations for treating cancer
WO2015127234A1 (en) 2014-02-20 2015-08-27 Board Of Regents, The University Of Texas System Use of ibrutinib to treat egfr mutant cancer
CN104860941B (zh) * 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
CN104876914B (zh) 2014-02-28 2017-04-19 山东轩竹医药科技有限公司 嘧啶衍生物类间变性淋巴瘤激酶抑制剂
TW201622744A (zh) 2014-03-04 2016-07-01 美國禮來大藥廠 癌症之組合療法
CN104892585B (zh) 2014-03-06 2018-07-03 山东轩竹医药科技有限公司 嘧啶衍生物类间变性淋巴瘤激酶抑制剂
HUE055747T2 (hu) 2014-04-04 2021-12-28 Astrazeneca Ab EGFR-gátló és MEK-gátló kombinációja NRAS-mutált rák kezelésében történõ alkalmazásra
CN110229142A (zh) 2014-04-04 2019-09-13 希洛斯医药品股份有限公司 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂
WO2015175965A1 (en) 2014-05-15 2015-11-19 The Research Foundation For Suny Compositions targeting the interaction domain between p27kip1 and brk and methods of use thereof
WO2015188777A1 (en) 2014-06-12 2015-12-17 Shanghai Fochon Pharmaceutical Co Ltd Certain protein kinase inhibitors
SMT202000265T1 (it) 2014-07-11 2020-07-08 Genmab As Anticorpi che legano axl
CN105254615B (zh) 2014-07-11 2017-02-22 杭州华东医药集团新药研究院有限公司 苯胺嘧啶衍生物及其在制备抗恶性肿瘤药物中的用途
CN105315285B (zh) 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
WO2016024185A1 (en) * 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
CN104140418B (zh) 2014-08-15 2016-08-24 常州润诺生物科技有限公司 2-(2，4，5-取代苯胺)嘧啶衍生物及其用途
WO2016023822A1 (en) 2014-08-15 2016-02-18 Boehringer Ingelheim International Gmbh Afatinib pharmaceutical kit for cancer treatment
CN106458969A (zh) 2014-08-25 2017-02-22 四川海思科制药有限公司 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途
JPWO2016032003A1 (ja) 2014-08-30 2017-07-13 国立大学法人金沢大学 肺癌患者用治療剤及び肺癌患者治療の有効性の予測検査方法
WO2016038609A1 (en) 2014-09-08 2016-03-17 Yeda Research And Development Co. Ltd. Anti-her3 antibodies and uses of same
EP3191523B1 (en) 2014-09-08 2019-08-07 Yeda Research and Development Co., Ltd. Compositions and methods for treating cancer resistant to a tyrosine kinase inhibitor (tki)
EP3191128A4 (en) 2014-09-11 2018-03-14 Celldex Therapeutics, Inc. Uses of anti-her3 antibodies for treating cancer
CA2962476C (en) 2014-09-26 2023-09-26 Hi-Stem Ggmbh Novel methods for sub-typing and treating cancer
CN105461695B (zh) 2014-09-29 2018-03-27 齐鲁制药有限公司 嘧啶或三嗪衍生物及其制备方法和用途
CN105237515B (zh) 2014-10-10 2018-06-05 益方生物科技（上海）有限公司 氘代嘧啶类化合物、其制备方法、药物组合物和用途
WO2016054987A1 (zh) * 2014-10-11 2016-04-14 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
HUE054848T2 (hu) 2014-10-13 2021-09-28 Yuhan Corp Vegyületek és készítmények EGFR mutáns kináz aktivitás módosítására
WO2016058544A1 (en) 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN105085489B (zh) 2014-11-05 2019-03-01 益方生物科技（上海）有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
WO2016090174A1 (en) 2014-12-03 2016-06-09 Auckland Uniservices, Ltd. Kinase inhibitor prodrug for the treatment of cancer
JP6709786B2 (ja) 2014-12-11 2020-06-17 ベータ ファーマ，インコーポレイテッド Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体
US20180193274A1 (en) 2014-12-24 2018-07-12 Principia Biopharma Inc. Compositions for ileo-jejunal drug delivery
US20180271853A1 (en) 2015-01-09 2018-09-27 Metastat, Inc. Method of Use for Inhibitors of Epidermal Growth Factor Receptor Variant III
WO2016112302A1 (en) 2015-01-09 2016-07-14 Metastat, Inc. Method of predicting sensitivity of tumor cell growth to combination therapy of fgfr inhibitor
EP3255042B1 (en) 2015-02-04 2020-12-30 Beyondbio Inc. Heterocyclic compound and pharmaceutical composition comprising same
CN104961731A (zh) 2015-02-05 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抑制剂的磷酸盐、其晶型及制备方法
CN107250108B (zh) 2015-02-05 2020-11-27 特尔诺沃有限公司 用于治疗癌症的irs/stat3双重调节剂与抗癌剂的组合
CN105985323A (zh) 2015-02-15 2016-10-05 宁波文达医药科技有限公司 新型表皮生长因子受体抑制剂及其应用
EP3265562A4 (en) 2015-03-05 2018-12-19 TrovaGene, Inc. Early assessment of mechanism of action and efficacy of anti-cancer therapies using molecular markers in bodily fluids
CN106138061B (zh) 2015-04-03 2019-06-04 中国人民解放军第三军医大学第三附属医院 预防或减弱肺纤维化的复合物及其制剂和用途
CN106138020A (zh) 2015-04-03 2016-11-23 中国人民解放军第三军医大学第三附属医院 双胍类药物在制备预防或减弱肺纤维化的药物中的应用
WO2016164217A1 (en) 2015-04-09 2016-10-13 Clovis Oncology, Inc. Therapeutic combinations for treating cancer
CN104844580B (zh) 2015-04-17 2017-10-20 中国药科大学 嘧啶类化合物、其制备方法及医药用途
RU2017136709A (ru) 2015-04-23 2019-05-23 Медиммьюн Лимитед Комбинированное лечение немелкоклеточного рака легкого с выявленной мутацией в egfr
CN104817541B (zh) 2015-05-11 2017-06-16 苏州东南药业股份有限公司 一种抗肿瘤药物的合成方法
CN108012529A (zh) 2015-05-15 2018-05-08 诺华股份有限公司 治疗egfr突变的癌症的方法
DK3297438T3 (da) 2015-05-21 2022-01-17 Chemocentryx Inc Ccr2-modulatorer
WO2016191471A1 (en) 2015-05-27 2016-12-01 Metastat, Inc. Method of use for inhibitors of epidermal growth factor receptor variants ii, iii and vi
CA2988131A1 (en) 2015-06-03 2016-12-08 National Yang-Ming University Therapeutic methods and compositions for treating non-small cell lung cancer
US20160355503A1 (en) 2015-06-04 2016-12-08 Cleave Biosciences, Inc. NITROGEN HEXACYCLE COMPOUNDS AS INHIBITORS OF p97 COMPLEX
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CN104910049B (zh) 2015-06-16 2016-06-29 苏州明锐医药科技有限公司 Azd9291中间体及其制备方法
PL3319993T3 (pl) 2015-07-10 2020-07-27 Genmab A/S Specyficzne wobec AXL koniugaty przeciwciało-lek do leczenia raka
JP7539760B2 (ja) 2015-07-17 2024-08-26 パシレックス・ファーマシューティカルズ・インコーポレイテッド Ｎｍｔ２の後成的なサイレンシング
WO2017015363A1 (en) 2015-07-20 2017-01-26 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
TW201716439A (zh) 2015-07-20 2017-05-16 美國禮來大藥廠 Ｈｅｒ３抗體
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
CN107531678B (zh) 2015-07-24 2020-12-22 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
CN105001208A (zh) 2015-08-06 2015-10-28 南京雷科星生物技术有限公司 一种表皮生长因子受体egfr抑制剂及其制备方法与用途
US10980765B2 (en) 2015-08-14 2021-04-20 Board Of Supervisors Of Louisiana State University Isothiocyanatostilbenes as a novel method and product for treating cancer
CN105153122B (zh) 2015-08-27 2018-07-20 上海圣考医药科技有限公司 [(吲哚-3-基)嘧啶-2-基]氨基苯基丙-2-烯酰胺衍生物及盐、制备方法、应用
CN106478605A (zh) 2015-09-02 2017-03-08 上海页岩科技有限公司 嘧啶类化合物、其制备方法和医药用途
CN105126125A (zh) 2015-09-12 2015-12-09 复旦大学 一种氧化锌-钆-药物复合纳米粒子及其制备方法和应用
JP6767491B2 (ja) 2015-09-25 2020-10-14 ディザル（ジァンスー）ファーマシューティカル・カンパニー・リミテッド Ｊａｋを阻害するための化合物及び方法
US10308658B2 (en) 2015-10-19 2019-06-04 Sunshine Lake Pharma Co., Ltd. Salt of EGFR inhibitor, crystalline form and uses thereof
US20170115275A1 (en) 2015-10-23 2017-04-27 Arizona Board Of Regents On Behalf Of Arizona State University Engineered substrates for high-throughput generation of 3d models of tumor dormancy, relapse and micrometastases for phenotype specific drug discovery and development
WO2017075367A1 (en) 2015-10-28 2017-05-04 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
CN106674202A (zh) 2015-11-05 2017-05-17 惠州信立泰药业有限公司 化合物a的二甲磺酸盐及其晶型和含有该盐的药物组合物
CN106699736A (zh) 2015-11-17 2017-05-24 惠州信立泰药业有限公司 化合物A甲磺酸盐的晶型γ和含有该晶型的药物组合物
CN105461729B (zh) 2015-11-18 2017-12-05 乳源瑶族自治县大众药品贸易有限公司 一种egfr抑制剂的盐、晶型及其用途
CN105294717B (zh) 2015-11-18 2017-12-22 乳源瑶族自治县大众药品贸易有限公司 一种egfr抑制剂的盐、晶型及其用途
RU2603960C1 (ru) 2015-11-19 2016-12-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетат n1,n2-дизамещенного n4-[4-(1-метил-1н-индол-3-ил)-пиримидин-2-ил]-5-метоксибензол-1,2,4-триамина в качестве модулятора egfr для лечения рака
RU2606949C9 (ru) 2015-11-19 2018-03-14 ЗАО "Р-Фарм" Замещенные N-{ 3-[4-(1-метил-1Н-индол-3-ил)пиримидин-2-иламино]-4-метоксифенил} -амиды в качестве модуляторов EGFR, предназначенные для лечения рака
CN105348267A (zh) 2015-12-01 2016-02-24 中山奕安泰医药科技有限公司 合成azd9291中间体的方法
JP6978003B2 (ja) 2015-12-03 2021-12-08 チョーチアン チアンフェン−イエン バイオテクノロジー カンパニー リミテッド 複素環式化合物およびその使用
JP6978002B2 (ja) 2015-12-03 2021-12-08 チョーチアン チアンフェン−イエン バイオテクノロジー カンパニー リミテッド チエノ−ピリミジン誘導体およびその使用
MA43416A (fr) 2015-12-11 2018-10-17 Regeneron Pharma Méthodes pour ralentir ou empêcher la croissance de tumeurs résistantes au blocage de l'egfr et/ou d'erbb3
TWI623316B (zh) 2015-12-22 2018-05-11 Taiho Pharmaceutical Co Ltd Antitumor effect enhancer derived from pyrrolopyrimidine compound
CN105601620A (zh) 2015-12-25 2016-05-25 北京康立生医药技术开发有限公司 一种甲磺酸迈瑞替尼的制备方法
CA3009850C (en) 2015-12-27 2020-05-26 NeuForm Pharmaceuticals, Inc. Deuterated compounds for treating cancer and related diseases and conditions, and compositions and methods thereof
CN106928150B (zh) 2015-12-31 2020-07-31 恩瑞生物医药科技（上海）有限公司 丙烯酰胺苯胺衍生物及其药学上的应用
TWI726968B (zh) 2016-01-07 2021-05-11 開曼群島商Ｃｓ醫藥技術公司 Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
EP3400218A4 (en) 2016-01-08 2019-09-18 Euclises Pharmaceuticals, Inc. COMBINATION OF A CHROME CONNECTION AND A SECOND ACTIVE SUBSTANCE
EP4218739A3 (en) 2016-01-08 2023-08-09 The Regents of The University of California Mesoporous silica nanoparticles with lipid bilayer coating for cargo delivery
CN105646454B (zh) 2016-01-19 2018-05-08 浙江大学 含异羟肟酸片段的2-芳胺基嘧啶类衍生物及制备和应用
TWI745345B (zh) 2016-02-01 2021-11-11 瑞典商阿斯特捷利康公司 製備奧希替尼（osimertinib，azd9291）或其鹽及「azd9291苯胺」或其鹽的改良方法
WO2017136342A1 (en) 2016-02-02 2017-08-10 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Fulvestrant for inducing immune-mediated cytotoxic lysis of cancer cells
CN108601781B (zh) 2016-02-04 2019-11-22 广州必贝特医药技术有限公司 作为检测点激酶1(chk1)抑制剂的3,5-二取代吡唑及其制备及应用
WO2017136774A1 (en) 2016-02-04 2017-08-10 Stem Cell Theranostics, Inc. Pharmaceutical compositions and methods for countering chemotherapy induced cardiotoxicity
CN105585557B (zh) 2016-02-25 2018-06-22 清华大学 用于靶向治疗癌症的egfr抑制剂及其制备方法与应用
CN105777716B (zh) 2016-02-25 2018-04-10 清华大学 一种用于靶向治疗癌症的egfr抑制剂及其制备方法与应用
MX383920B (es) * 2016-05-26 2025-03-14 Recurium Ip Holdings Llc Compuestos inhibidores de egfr.
CN105886648A (zh) 2016-06-06 2016-08-24 武汉海吉力生物科技有限公司 用于检测egfr基因t790m突变的试剂盒
CN106366072B (zh) 2016-08-19 2018-12-07 上海工程技术大学 一种azd9291的制备方法
CN106366022B (zh) 2016-08-19 2018-03-13 上海工程技术大学 一种用于制备azd9291的中间体及其制备方法和应用
CN106397407B (zh) 2016-08-31 2018-09-04 浙江科聚化工有限公司 抗肿瘤药物azd9291衍生物的制备方法
CN106432231B (zh) 2016-09-09 2018-06-12 无锡佰翱得生物科学有限公司 Azd9291的药用盐、及其晶型和制备方法
CN106565522A (zh) 2016-09-29 2017-04-19 福格森（武汉）生物科技股份有限公司 一种由氟代芳香化合物制备烷氧基芳香化合物的方法
CN106496196B (zh) 2016-10-20 2019-07-02 南京雷科星生物技术有限公司 一种喹唑啉、吡啶并嘧啶或则双并嘧啶衍生物表皮生长因子抑制剂及其制备方法与用途
CN106543060B (zh) 2016-10-31 2018-11-06 湖南欧亚药业有限公司 一种奥斯替尼甲磺酸盐的制备方法
CN106668866A (zh) 2017-02-13 2017-05-17 江苏省中医药研究院 一种抗非小细胞肺癌的药物组合物及其应用
CN106883216B (zh) 2017-04-06 2020-03-13 张家港威胜生物医药有限公司 一种奥希替尼的制备方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015195228A1 (en) * 2014-06-19 2015-12-23 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition

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