RS62542B1 - 2-(2,4,5-supstituisani-anilino) pirimidinski derivati - Google Patents

2-(2,4,5-supstituisani-anilino) pirimidinski derivati

Info

Publication number
RS62542B1
RS62542B1 RS20211378A RSP20211378A RS62542B1 RS 62542 B1 RS62542 B1 RS 62542B1 RS 20211378 A RS20211378 A RS 20211378A RS P20211378 A RSP20211378 A RS P20211378A RS 62542 B1 RS62542 B1 RS 62542B1
Authority
RS
Serbia
Prior art keywords
compound
theta
ray powder
powder diffraction
polymorphic form
Prior art date
Application number
RS20211378A
Other languages
English (en)
Serbian (sr)
Inventor
Sam Butterworth
Richard Andrew Ward
Maurice Raymond Verschoyle Finlay
Vasantha Krishna Kadambar
Chandrasekhara Reddy Chintakuntla
Andiappan Murugan
Claudio Edmundo Chuaqui
Heather Marie Redfearn
Original Assignee
Astrazeneca Ab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46875901&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS62542(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of RS62542B1 publication Critical patent/RS62542B1/sr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Liquid Crystal Substances (AREA)
  • Luminescent Compositions (AREA)
  • Inks, Pencil-Leads, Or Crayons (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
RS20211378A 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati RS62542B1 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161512061P 2011-07-27 2011-07-27
US201261591363P 2012-01-27 2012-01-27
EP20157927.3A EP3686194B1 (en) 2011-07-27 2012-07-25 2-(2,4,5-substituted-anilino)pyrimidine compounds

Publications (1)

Publication Number Publication Date
RS62542B1 true RS62542B1 (sr) 2021-12-31

Family

ID=46875901

Family Applications (4)

Application Number Title Priority Date Filing Date
RS20200459A RS60190B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za lečenje raka
RS20160094A RS54653B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka
RS20211378A RS62542B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati
RS20171309A RS56679B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka

Family Applications Before (2)

Application Number Title Priority Date Filing Date
RS20200459A RS60190B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za lečenje raka
RS20160094A RS54653B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka

Family Applications After (1)

Application Number Title Priority Date Filing Date
RS20171309A RS56679B1 (sr) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka

Country Status (38)

Country Link
US (8) US8946235B2 (enExample)
EP (7) EP3686194B1 (enExample)
JP (3) JP5427321B2 (enExample)
KR (3) KR101410902B1 (enExample)
CN (7) CN103702990B (enExample)
AR (1) AR087336A1 (enExample)
AU (1) AU2012288626C1 (enExample)
BR (4) BR112014001768B1 (enExample)
CA (5) CA2882018C (enExample)
CL (1) CL2013003281A1 (enExample)
CO (1) CO6811863A2 (enExample)
CR (1) CR20130629A (enExample)
CY (4) CY1117431T1 (enExample)
DK (5) DK3009431T3 (enExample)
DO (1) DOP2013000263A (enExample)
EA (3) EA024421B1 (enExample)
EC (1) ECSP13013033A (enExample)
ES (5) ES2654177T3 (enExample)
GT (1) GT201300288A (enExample)
HR (4) HRP20160135T1 (enExample)
HU (4) HUE026429T2 (enExample)
IL (6) IL229199A (enExample)
LT (3) LT3009431T (enExample)
ME (3) ME02382B (enExample)
MX (3) MX2014000528A (enExample)
MY (2) MY194532A (enExample)
NI (1) NI201300134A (enExample)
PE (1) PE20141700A1 (enExample)
PH (2) PH12013502312A1 (enExample)
PL (5) PL3333161T3 (enExample)
PT (4) PT3686193T (enExample)
RS (4) RS60190B1 (enExample)
SG (5) SG194783A1 (enExample)
SI (4) SI3333161T1 (enExample)
SM (3) SMT202100652T1 (enExample)
TW (3) TWI583386B (enExample)
UY (1) UY34219A (enExample)
WO (1) WO2013014448A1 (enExample)

Families Citing this family (222)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2300013T5 (pl) 2008-05-21 2025-04-28 Takeda Pharmaceutical Company Limited Pochodne fosforu jako inhibitor kinazy
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
KR101769999B1 (ko) 2008-09-18 2017-08-21 노오쓰웨스턴 유니버시티 Ｎｍｄａ 수용체 조절제 및 그의 용도
CN102498115B (zh) 2009-08-20 2016-12-07 卡鲁斯治疗有限公司 作为磷酸肌醇3-激酶抑制剂的三环杂环化合物
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2654177T3 (es) 2011-07-27 2018-02-12 Astrazeneca Ab Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
SI2951183T1 (sl) 2013-01-29 2019-07-31 Aptinyx Inc. Spiro-laktam NMDA receptorski modulatorji in njihove uporabe
WO2014120784A1 (en) * 2013-01-29 2014-08-07 Naurex, Inc. Spiro-lactam nmda receptor modulators and uses thereof
EP2968291B1 (en) 2013-03-15 2025-04-16 Pharmacosmos Holding A/S Hspc-sparing treatments for rb-positive abnormal cellular proliferation
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP3052494B1 (en) * 2013-06-28 2018-12-26 H. Hoffnabb-La Roche Ag Azaindazole compounds as inhibitors of t790m containing egfr mutants
CN104292142B (zh) * 2013-07-17 2019-05-14 天津大地康和医药技术有限公司 一种n-芳基杂环丁烷脱芳基方法
US20170050936A1 (en) 2013-08-23 2017-02-23 Neupharma, Inc. Certain chemical entities, compositions, and methods
HUE044683T2 (hu) * 2013-10-21 2019-11-28 Merck Patent Gmbh Heteroaril vegyületek mint BTK inhibitorok és alkalmazásuk
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
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
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
AU2015242407B2 (en) * 2014-04-04 2017-11-09 Astrazeneca Ab Combination of EGFR inhibitor and MEK inhibitor for use in the treatment of NRAS mutated cancer
CA2946538A1 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
US20170166598A1 (en) * 2014-05-13 2017-06-15 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN111892579B (zh) * 2014-06-12 2023-07-25 上海艾力斯医药科技股份有限公司 一类激酶抑制剂
BR112016029662B1 (pt) * 2014-06-19 2023-10-24 Takeda Pharmaceutical Company Limited COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO
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
CN105315259B (zh) * 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
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
CN113121575A (zh) * 2014-08-25 2021-07-16 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
CN104356040A (zh) * 2014-09-17 2015-02-18 爱斯特（成都）生物制药有限公司 一种1-二苯甲基-3-羟基氮杂环丁烷盐酸盐的制备方法
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
CN105524068B (zh) 2014-09-30 2017-11-24 上海海雁医药科技有限公司 氮杂双环衍生物、其制法与医药上的用途
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
SI3205650T1 (sl) * 2014-10-11 2021-10-29 Shanghai Hansoh Biomedical Co Ltd Zaviralec EGFR-ja in priprava ter uporaba le-tega
HRP20250213T1 (hr) * 2014-10-13 2025-04-25 Yuhan Corporation Spojevi i pripravci za modulaciju aktivnosti egfr mutantne kinaze
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
JP6769962B2 (ja) * 2014-12-03 2020-10-14 オークランド ユニサービシーズ リミティド 癌治療のためのキナーゼ阻害剤プロドラッグ
SG11201704685TA (en) * 2014-12-11 2017-07-28 Beta Pharma Inc Substituted 2-anilinopyrimidine derivatives as egfr modulators
WO2016105525A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
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
CN104788427B (zh) * 2015-02-05 2017-05-31 上海泓博智源医药股份有限公司 3‑(2‑嘧啶氨基)苯基丙烯酰胺类化合物及其应用
CN107613769A (zh) 2015-02-17 2018-01-19 润新生物公司 某些化学实体、组合物和方法
TWI687420B (zh) * 2015-04-29 2020-03-11 大陸商南京聖和藥業股份有限公司 稠環或三環芳基嘧啶化合物用作激酶抑制劑
JP6457697B2 (ja) 2015-04-29 2019-01-23 カントン チョンション ファーマシューティカル カンパニー，リミティド キナーゼ阻害剤としての縮合環式または三環式アリールピリミジン化合物
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
WO2016183278A1 (en) * 2015-05-13 2016-11-17 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
EP3294299A1 (en) 2015-05-15 2018-03-21 Novartis AG Methods for treating egfr mutant cancers
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
KR102666414B1 (ko) 2015-07-16 2024-05-17 치아타이 티안큉 파마수티컬 그룹 주식회사 아닐린 피리미딘 유도체 및 그의 용도
WO2017015363A1 (en) * 2015-07-20 2017-01-26 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
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
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
GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
GB201514760D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds and method of use
GB201514751D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
CN106117185B (zh) 2015-08-31 2017-11-07 广州必贝特医药技术有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用
KR102051609B1 (ko) * 2015-08-31 2019-12-03 우시 상량 바이오테크놀로지 씨오., 엘티디. 2-아릴아미노피리딘, 피리미딘 또는 트리아진 유도체 및 그 제조방법과 사용
CN110483485A (zh) * 2015-09-02 2019-11-22 益方生物科技（上海）有限公司 嘧啶类化合物、其制备方法和医药用途
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
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
CN106749267B (zh) * 2015-11-23 2020-08-21 南京圣和药业股份有限公司 新的表皮生长因子受体抑制剂及其应用
CN106810553B (zh) * 2015-11-30 2020-03-17 江苏正大丰海制药有限公司 3-(4,5-取代氨基嘧啶)苯基衍生物及其应用
US10829495B2 (en) 2015-12-03 2020-11-10 Zhejiang Jianfeng-Yien Biotechnology Co., Ltd. Thieno-pyrimidine derivatives and uses thereof
EP3383877B1 (en) * 2015-12-03 2021-09-15 Zhejiang Jianfeng-Yien Biotechnology Co., Ltd. Heterocycle compounds and uses thereof
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
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
JP2019501222A (ja) 2016-01-07 2019-01-17 シーエス ファーマテック リミテッド Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬
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
CN108610331A (zh) * 2016-01-22 2018-10-02 焦玉奇 2-(2,4,5-取代苯胺)嘧啶衍生物
CN106995437A (zh) * 2016-01-22 2017-08-01 齐鲁制药有限公司 取代吲哚或吲唑嘧啶衍生物及其制备方法和用途
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
CN107043368B (zh) * 2016-02-05 2020-07-31 齐鲁制药有限公司 芳胺嘧啶化合物及其盐的结晶
CN107043369A (zh) * 2016-02-06 2017-08-15 焦玉奇 2‑(2,4,5‑取代苯胺)嘧啶衍生物
CN107098887B (zh) * 2016-02-22 2019-08-09 复旦大学 嘧啶类化合物
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
CN105646467B (zh) * 2016-02-25 2018-07-20 黄燕鸽 一种抗癌化合物奥美替尼及其合成方法
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
CN107163027B (zh) 2016-03-07 2019-11-05 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物甲磺酸盐的结晶形式及其制备和应用
CN107163026B (zh) * 2016-03-07 2019-07-02 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物的盐及其制备方法和应用
CN107188888A (zh) * 2016-03-15 2017-09-22 罗欣生物科技（上海）有限公司 一种制备甲磺酸迈瑞替尼的方法
JP7007287B2 (ja) * 2016-03-22 2022-01-24 ジエンス ハンセン ファーマセウティカル グループ カンパニー リミテッド Ｅｇｆｒ阻害薬フリー塩基または酸性塩の多結晶形、その製造方法、および応用
KR20190006991A (ko) * 2016-05-11 2019-01-21 베타 파마, 인크. 뇌암의 치료를 위한 치료제로서의 2-아닐리노피리미딘 유도체
WO2017201285A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
WO2017201283A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
EP3464275B1 (en) 2016-05-26 2024-05-08 Recurium IP Holdings, LLC Egfr inhibitor compounds
AU2017285448B2 (en) * 2016-06-17 2021-02-04 Beta Pharma, Inc. Pharmaceutical salts of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof
CN107522690B (zh) * 2016-06-20 2022-08-05 海南先声药业有限公司 一种Osimertinib的制备方法
CN107540661A (zh) * 2016-06-24 2018-01-05 正大天晴药业集团股份有限公司 作为egfr抑制剂的苯胺嘧啶化合物的结晶
CN107663207B (zh) * 2016-07-27 2021-07-30 南京圣和药业股份有限公司 一种egfr激酶抑制剂的甲磺酸盐结晶及制备方法
CN107663208B (zh) * 2016-07-27 2021-10-15 南京圣和药业股份有限公司 一种新型egfr激酶抑制剂的药用盐及其制备方法与用途
WO2018026763A1 (en) 2016-08-01 2018-02-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
MX383650B (es) 2016-08-01 2025-03-14 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos.
JP7032378B2 (ja) 2016-08-01 2022-03-08 アプティニックス インコーポレイテッド スピロ－ラクタムｎｍｄａ受容体修飾因子及びその使用
SG11201900554YA (en) 2016-08-01 2019-02-27 Aptinyx Inc Spiro-lactam nmda modulators and methods of using same
AU2017306158B2 (en) 2016-08-01 2021-10-14 Aptinyx Inc. Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
WO2018035061A1 (en) 2016-08-15 2018-02-22 Neupharma, Inc. Certain chemical entities, compositions, and methods
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
US10654851B2 (en) * 2016-09-19 2020-05-19 Nanjing Chuangte Pharmaceutical Technology Co., Ltd. Deuterated 3-(4,5-substituted aminopyrimidine)phenyl derivatives and use thereof
CN107955019B (zh) * 2016-10-17 2021-09-14 广东众生药业股份有限公司 一种egfr抑制剂的盐型、晶型及其制备方法
WO2018073839A1 (en) 2016-10-18 2018-04-26 Mylan Laboratories Limited Amorphous osimertinib mesylate, processes for its preparation and solid amorphous dispersions thereof
EP3528798A4 (en) * 2016-10-19 2020-10-21 United States Government as Represented by The Department of Veterans Affairs COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
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
CN108299419B (zh) * 2017-01-11 2022-04-26 南京圣和药业股份有限公司 一种新型egfr激酶抑制剂的几种新晶型及其制备方法
PL3514153T3 (pl) 2017-01-26 2022-01-17 Hanmi Pharm. Co., Ltd. Związek pirymidynowy i jego zastosowanie farmaceutyczne
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
EP3585389A4 (en) * 2017-02-22 2020-12-23 G1 Therapeutics, Inc. EGFR-CAUSED CANCER TREATMENT WITH LESS SIDE EFFECTS
TWI796326B (zh) 2017-03-24 2023-03-21 日商第一三共股份有限公司 含有ａｘｌ抑制劑與ｅｇｆｒ酪胺酸激酶抑制藥的醫藥品及其用途
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
CN108503627A (zh) * 2017-04-19 2018-09-07 郑州泰基鸿诺医药股份有限公司 用作egfr抑制剂的2,4-二取代苯-1,5-二胺衍生物及其应用
AR111469A1 (es) * 2017-04-21 2019-07-17 Yuhan Corp Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma
CN106967050A (zh) * 2017-05-11 2017-07-21 北京工业大学 一种azd9291的制备方法
CN108929311B (zh) * 2017-05-22 2020-07-28 焦玉奇 2-(2,4,5-取代苯胺)嘧啶衍生物
CN108558835B (zh) 2017-05-24 2024-08-16 浙江同源康医药股份有限公司 一种氘代azd9291的晶型、制备方法及用途
CN107176954B (zh) * 2017-06-02 2019-01-11 无锡双良生物科技有限公司 一种egfr抑制剂的药用盐及其晶型、制备方法和应用
KR102388312B1 (ko) * 2017-06-13 2022-04-19 베이징 아다메이들 바이오테크놀로지 리미티드 라이어빌리티 컴퍼니 아미노피리미딘 화합물, 이의 제조방법 및 용도
TW201904577A (zh) 2017-06-16 2019-02-01 美商貝達醫藥公司 N-(2-(2-二甲胺基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)胺基)苯基)丙烯醯胺及其鹽之醫藥調配物
WO2019001425A1 (zh) * 2017-06-27 2019-01-03 浙江同源康医药股份有限公司 一种氘代奥斯替尼衍生物及其应用
CN107095873A (zh) * 2017-06-28 2017-08-29 卢凯华 具有低耐药性的抗肺癌靶向药物组合物
CN107216313B (zh) * 2017-06-29 2019-11-19 山东四环药业股份有限公司 一种抗肿瘤药物azd9291的制备方法
WO2019010619A1 (zh) * 2017-07-10 2019-01-17 焦玉奇 2-(2,4,5-取代苯胺)嘧啶衍生物
DK3658552T3 (da) 2017-07-28 2023-11-20 Yuhan Corp Fremgangsmåde til fremstilling af n-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamid ved reaktion af den tilsvarende amin med et 3-halogen-propionylchlorid
PT3658547T (pt) * 2017-07-28 2023-10-20 Yuhan Corp Processo de preparação de n -(5 -(4 -(4 -formil -3- fenil- 1h -pirazol- 1 -il)pirimidin -2- ilamino) -4 -metoxi 2- morfolinofenil) acrilamida
CN107266426A (zh) * 2017-08-15 2017-10-20 南通因诺威医药科技有限公司 2‑氨烃基嘧啶类化合物及其制备方法和用途
JP7135068B2 (ja) 2017-08-21 2022-09-12 イーライ リリー アンド カンパニー Ｅｇｆｒ阻害剤と抗ヒトｖｅｇｆｒ－２抗体との組み合わせ
CN109485638B (zh) * 2017-09-12 2020-07-17 新发药业有限公司 一种奥希替尼中间体的制备方法
CN107915725B (zh) * 2017-10-20 2023-06-27 复旦大学 Azd9291的药用盐及其制备方法
SG11202004384YA (en) * 2017-11-17 2020-06-29 Univ Illinois Cancer therapy by degrading dual mek signaling
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
WO2019152696A1 (en) * 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
CN112204031B (zh) 2018-01-31 2024-05-24 元羿生物科技(香港)有限公司 螺-内酰胺nmda受体调节剂及其用途
EP3749310B1 (en) * 2018-02-08 2025-11-26 Neupharma, Inc. Certain chemical entities, compositions, and methods
AU2019219304A1 (en) * 2018-02-12 2020-09-24 Astrazeneca Ab Osimertinib for use in the treatment of non-small cell lung cancer
WO2019164945A1 (en) * 2018-02-20 2019-08-29 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of egfr inhibitors and methods of use thereof
WO2019164949A1 (en) * 2018-02-20 2019-08-29 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of egfr inhibitors and methods of use thereof
CN108250187B (zh) * 2018-03-01 2021-01-05 中国科学院上海药物研究所 吲哚-1-碳酸酯类化合物、其制备方法和应用
CN108191861B (zh) * 2018-03-01 2020-10-02 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-反式-2,4-戊二烯酰胺
WO2019175093A1 (en) 2018-03-12 2019-09-19 Astrazeneca Ab Method for treating lung cancer
CN108218839A (zh) * 2018-03-20 2018-06-29 上药康丽（常州）药业有限公司 一种抗肿瘤药物azd9291的制备方法
CN109666024A (zh) * 2018-03-20 2019-04-23 兰州大学 2-氧嘧啶类化合物及其制备方法和用途
CN108484579A (zh) * 2018-03-28 2018-09-04 黑龙江鑫创生物科技开发有限公司 一种微通道反应器合成奥希替尼中间体的方法
CN108530450B (zh) * 2018-05-03 2021-03-30 赖建智 具有egfr抑制活性的化合物、制备方法及其在疾病治疗中的应用
WO2019222093A1 (en) 2018-05-14 2019-11-21 Ariad Pharmaceuticals, Inc. Pharmaceutical salts of pyrimidine derivatives and method of treating disorders
US11639344B2 (en) 2018-05-15 2023-05-02 InventisBio Co., Ltd. EGFR inhibitors
CN110606842B (zh) * 2018-06-15 2021-06-01 上海艾力斯医药科技股份有限公司 吡啶胺基嘧啶衍生物的制备方法及其中间体
CN110698461B (zh) * 2018-07-09 2024-04-05 上海翰森生物医药科技有限公司 第三代egfr抑制剂的制备方法
KR101954370B1 (ko) 2018-07-25 2019-03-05 한미약품 주식회사 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
WO2020072774A1 (en) 2018-10-05 2020-04-09 The Board Of Trustees Of The University Of Illinois Combination therapy for the treatment of uveal melanoma
CN109134435B (zh) * 2018-10-29 2023-01-03 湖南大学 一种奥希替尼azd9291的合成方法
CN111233774B (zh) * 2018-11-28 2023-04-14 鲁南制药集团股份有限公司 一种胺基嘧啶类化合物
CN113195000A (zh) 2018-12-21 2021-07-30 第一三共株式会社 抗体-药物缀合物和激酶抑制剂的组合
CN113227073B (zh) * 2019-01-05 2022-09-16 山东轩竹医药科技有限公司 Egfr酪氨酸激酶的选择性抑制剂的盐及其晶型
CN111410651B (zh) * 2019-01-05 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂的盐及其晶型
BR112021016522A2 (pt) 2019-02-22 2021-10-26 Hanmi Pharm. Co., Ltd. Composição farmacêutica para o tratamento da leucemia mieloide aguda
CN113773304B (zh) * 2019-02-25 2023-03-10 江苏豪森药业集团有限公司 抗耐药抗肿瘤egfr抑制剂的制备方法
CN111606889B (zh) * 2019-02-25 2023-03-07 上海翰森生物医药科技有限公司 4-(1-环丙基-1h-吲哚-3-基)-n-苯基嘧啶-2-胺衍生物的制备方法
CN109928956B (zh) * 2019-02-27 2020-10-13 杭州偶联医药科技有限公司 一种靶向泛素化降解egfr蛋白的化合物及其药物组合物和应用
WO2020192302A1 (zh) * 2019-03-27 2020-10-01 广州必贝特医药技术有限公司 含嘧啶的三取代咪唑类化合物及其应用
CN111747950B (zh) 2019-03-29 2024-01-23 深圳福沃药业有限公司 用于治疗癌症的嘧啶衍生物
MX2021011810A (es) 2019-03-29 2021-10-26 Astrazeneca Ab Osimertinib para su uso en el tratamiento de cancer de pulmon de celulas no peque?as.
WO2020206603A1 (zh) * 2019-04-09 2020-10-15 河南真实生物科技有限公司 2-(2，4，5-取代苯氨基)嘧啶衍生物及其晶形b
CN109942550A (zh) * 2019-04-15 2019-06-28 广州医科大学附属第一医院（广州呼吸中心） 11c标记的egfr正电子示踪剂及其制备方法和应用
WO2020222188A1 (en) 2019-05-01 2020-11-05 Clexio Biosciences Ltd. Methods of treating pruritus
US20220296595A1 (en) 2019-05-05 2022-09-22 Qilu Regor Therapeutics Inc. Cdk inhibitors
US20220340547A1 (en) * 2019-05-22 2022-10-27 Shanghi Hansoh Biosoh Biomedical Co., Ltd. Indole derivative-containing inhibitor, preparation method therefor and application thereof
MX2021015724A (es) 2019-06-27 2022-05-16 Hanmi Pharm Ind Co Ltd Composición farmacéutica para el tratamiento de la leucemia mieloide aguda, que contiene inhibidores de flt3 y agentes quimioterapéuticos.
CN110283162B (zh) * 2019-07-09 2022-04-05 辽宁大学 一种表皮生长因子受体抑制剂及其应用
CN110483486B (zh) * 2019-09-17 2024-01-26 鲁南制药集团股份有限公司 一种奥西替尼酮咯酸盐晶型及其制备方法
US12012413B2 (en) 2019-11-11 2024-06-18 Tenacia Biotechnology (Hong Kong) Co., Limited Methods of treating painful diabetic peripheral neuropathy
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
WO2021111462A1 (en) * 2019-12-02 2021-06-10 Natco Pharma Limited An improved process for the preparation of osimertinib mesylate
EP4076667A1 (en) 2019-12-20 2022-10-26 Erasca, Inc. Tricyclic pyridones and pyrimidones
AU2021211871A1 (en) 2020-01-20 2022-09-08 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
IL272441B (en) * 2020-02-03 2021-08-31 Ottek Ltd System and method for driving an endoscope
CN113372332B (zh) * 2020-03-10 2023-09-12 鲁南制药集团股份有限公司 一种奥希替尼新晶型
CN113372331B (zh) * 2020-03-10 2023-09-12 鲁南制药集团股份有限公司 一种奥希替尼一水合物新晶型
CN111303123B (zh) * 2020-03-31 2021-08-31 南京雷正医药科技有限公司 2-(2,4,5-取代苯胺基)嘧啶化合物及其应用
CN111285852A (zh) * 2020-04-02 2020-06-16 广州博济医药生物技术股份有限公司 氘代奥希替尼药用盐的晶型及其制备方法
CN111303124A (zh) * 2020-04-08 2020-06-19 北京赛思源生物医药技术有限公司 一种甲磺酸奥希替尼的新晶体
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
CN113801101A (zh) * 2020-06-15 2021-12-17 鲁南制药集团股份有限公司 Azd9291-2-酮戊二酸盐及其制备方法
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
CN113929663B (zh) * 2020-06-29 2025-06-17 鲁南制药集团股份有限公司 Azd9291-2-吲哚甲酸盐及其制备方法
CN113929664A (zh) * 2020-07-13 2022-01-14 鲁南制药集团股份有限公司 Azd9291-3,5-吡啶二羧酸盐及其制备方法
CN113968845A (zh) * 2020-07-24 2022-01-25 鲁南制药集团股份有限公司 Azd9291-没食子酸盐及其制备方法
US20230321098A1 (en) 2020-08-25 2023-10-12 Loxo Oncology, Inc. Osimertinib and selpercatinib combinations for the treatment of egfr- and ret-associated cancers
IL301524A (en) 2020-09-23 2023-05-01 Erasca Inc Tricyclic pyridones and pyrimidones
CN112430231B (zh) * 2020-11-06 2022-09-30 德州德药制药有限公司 一种azd9291的工业化制备方法
CN112358468B (zh) * 2020-11-10 2022-03-22 德州德药制药有限公司 一种工业化合成azd9291的方法
TW202222795A (zh) * 2020-11-19 2022-06-16 大陸商上海翰森生物醫藥科技有限公司 一種含吲哚類衍生物的鹽、晶型及其製備方法和應用
US11780824B2 (en) 2020-12-16 2023-10-10 Scinopharm Taiwan, Ltd. Process for preparing osimertinib or a salt thereof
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
TW202317126A (zh) 2021-06-15 2023-05-01 美商建南德克公司 Ｅｇｆｒ抑制劑和ｐｅｒｋ活化劑組合療法
CN113387935B (zh) * 2021-07-23 2022-06-10 苏州雅深智慧科技有限公司 抑制三突变表皮生长因子受体酪氨酸激酶的化合物及用途
WO2023011505A1 (zh) * 2021-08-06 2023-02-09 上海和誉生物医药科技有限公司 嘧啶或吡啶衍生物及其制备方法和在药学上的应用
JP2024530782A (ja) * 2021-09-02 2024-08-23 シントン・ビー．ブイ． オシメルチニブの製造方法
CN113683612B (zh) * 2021-09-07 2022-06-17 山东铂源药业股份有限公司 一种帕布昔利布的制备方法
JP7702205B2 (ja) * 2021-09-15 2025-07-03 株式会社東芝 新規アミン化合物、酸性ガス吸収剤、酸性ガスの除去方法及び酸性ガス除去
CN116099006A (zh) * 2021-11-10 2023-05-12 上海交通大学医学院附属新华医院 奥西替尼及其药学上可接受的盐在制备急性髓细胞白血病药物中的应用
CN114014847B (zh) * 2021-12-08 2023-11-03 滨州医学院 一种含苯并噻吩嘧啶衍生物及其制备方法和在制备抗肿瘤药物中的应用
CN114380806B (zh) * 2022-03-24 2022-06-10 中国药科大学 2-氨基-4-吲哚基嘧啶类化合物及其制备方法与应用
CA3255389A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Combination with an AKT Inhibitor for the Treatment of Cancer
AR128999A1 (es) 2022-04-07 2024-07-03 Astrazeneca Ab Proceso mejorado para la fabricación de osimertinib
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209084A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
CA3250910A1 (en) * 2022-05-03 2023-11-09 Deutsches Zentrum Für Neurodegenerative Erkrankungen E. V. TAU PROTEIN INHIBITORS
MA71241A (fr) 2022-06-27 2025-04-30 Astrazeneca Ab Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer
WO2024003241A1 (en) 2022-06-30 2024-01-04 Astrazeneca Ab Treatment for immuno-oncology resistant subjects with an anti pd-l1 antibody an antisense targeted to stat3 and an inhibitor of ctla-4
WO2024008929A1 (en) 2022-07-08 2024-01-11 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors in combination with hgf-receptor inhibitors for the treatment of cancer
CN115650974B (zh) * 2022-08-04 2024-06-18 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-顺式戊二烯酰胺衍生物及应用
CN119894871A (zh) * 2022-09-19 2025-04-25 南京爱德程医药科技有限公司 作为对egfr突变体具有生物活性的激酶抑制剂的新型嘧啶化合物
CN116655601B (zh) * 2023-06-05 2025-08-29 河南应用技术职业学院 一种奥希替尼的合成方法
WO2025124936A1 (en) 2023-12-15 2025-06-19 Synthon B.V. A process for making osimertinib
WO2025245045A1 (en) 2024-05-21 2025-11-27 The Regents Of The University Of California Methods of treating lung cancer

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
CA2242425C (en) 1996-02-13 2006-07-18 Zeneca Limited Quinazoline derivatives as vegf inhibitors
DE69709319T2 (de) 1996-03-05 2002-08-14 Astrazeneca Ab, Soedertaelje 4-anilinochinazolin derivate
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
EE05345B1 (et) 1999-02-10 2010-10-15 Astrazeneca Ab Kinasoliini derivaadid angiogeneesi inhibiitoritena
CN1431999A (zh) 2000-05-31 2003-07-23 阿斯特拉曾尼卡有限公司 具有血管损伤活性的吲哚衍生物
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
RU2003103603A (ru) 2000-07-07 2004-08-20 Энджиоджен Фармасьютикалз Лимитед (Gb) Производные колхинола в качестве ингибиторов ангиогенеза
JP2004502766A (ja) 2000-07-07 2004-01-29 アンギオジェン・ファーマシューティカルズ・リミテッド 血管損傷剤としてのコルヒノール誘導体
US6881737B2 (en) * 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
ATE430747T1 (de) * 2004-12-21 2009-05-15 Smithkline Beecham Corp 2-pyrimidinyl-pyrazolopyridin-erbb- kinaseinhibitoren
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
DK1848414T3 (da) 2005-02-03 2011-07-25 Gen Hospital Corp Fremgangsmåde til behandling af gefitinib-resistent cancer
JP5249770B2 (ja) 2005-11-03 2013-07-31 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリジン
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
EP1971606B1 (en) * 2005-12-05 2013-04-24 GlaxoSmithKline LLC 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
JP2009541318A (ja) 2006-06-22 2009-11-26 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害剤
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2702674C (en) 2007-10-19 2016-05-03 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
TWI458721B (zh) * 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
CN102405284B (zh) 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
US20110183975A1 (en) 2008-10-07 2011-07-28 Yasuhiro Goto Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
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
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
EP2478361A4 (en) 2009-09-16 2014-05-21 Celgene Avilomics Res Inc CONJUGATES AND INHIBITORS OF PROTEIN KINASE
JP2013509412A (ja) * 2009-11-02 2013-03-14 アボット・ラボラトリーズ 多標的キナーゼ阻害における新規な足場としてのイミダゾピリジン類
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
LT2585470T (lt) 2010-06-23 2017-04-10 Hanmi Science Co., Ltd. Nauji kondensuoti pirimidino dariniai tirozino kinazės aktyvumo slopinimui
TW201219383A (en) 2010-08-02 2012-05-16 Astrazeneca Ab Chemical compounds
EP2704572B1 (en) * 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2654177T3 (es) 2011-07-27 2018-02-12 Astrazeneca Ab Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer

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