ME02887B - 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka - Google Patents

2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka

Info

Publication number
ME02887B
ME02887B MEP-2017-290A MEP2017290A ME02887B ME 02887 B ME02887 B ME 02887B ME P2017290 A MEP2017290 A ME P2017290A ME 02887 B ME02887 B ME 02887B
Authority
ME
Montenegro
Prior art keywords
compound
pharmaceutically acceptable
cancer
acceptable salt
amino
Prior art date
Application number
MEP-2017-290A
Other languages
German (de)
English (en)
French (fr)
Inventor
Vasantha Krishna Kadambar
Sam Butterworth
Maurice Raymond Verschoyle Finlay
Richard Andrew Ward
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=ME02887(B) "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 ME02887B publication Critical patent/ME02887B/me

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
    • 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
    • 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
    • A61K31/435—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
    • C07D403/14—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
    • 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

Landscapes

  • 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)
  • Luminescent Compositions (AREA)
  • Inks, Pencil-Leads, Or Crayons (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Liquid Crystal Substances (AREA)

Claims (12)

1. Jedinjenje naznačeno time što je izabrano od N-(2-[2-dimetilaminoetil-metilamino]-5-{[4-(1H-indol-3-il)pirimidin-2-il]amino}-4-metoksifenil)-prop-2-enamida: i N-(4-metoksi-5-{[4-(1-metilindol-3-il)pirimidin-2-il]amino}-2-[metil-(2-metilaminoetil)amino]fenil)prop-2-enamida: ili njihova farmaceutski prihvatljiva so.
2. Jedinjenje prema zahtevu 1 naznačeno time što je N-(2-[2-dimetilaminoetil-metilamino]-5-{[4-(1H-indol-3-il)pirimidin-2-il]amino}-4-metoksifenil)-prop-2-enamid
3. Jedinjenje kako je zatraženo u zahtevu 1, naznačeno time što je N-(4-metoksi-5-{[4-(1-metilindol-3-il)pirimidin-2-il]amino}}-2-[metil-(2-metilaminoetil)amino]fenil)prop-2-enamid.
4. Farmaceutska kompozicija, naznačena time, što sadrži jedinjenje ili neku njegovu farmaceutski prihvatljivu so kao šta se zahteva u bilo kojem od zahteva od 1 do 3 zajedno sa nekim farmaceutski prihvatljivim razređivačem ili nosiocem.
5. Jedinjenje ili neka njegova farmaceutski prihvatljiva so kao šta se zahteva u bilo kojem od zahteva od 1 do 3, naznačeno time, što se upotrebljava kao lek.
6. Jedinjenje ili neka njegova farmaceutski prihvatljiva so kao šta se zahteva u bilo kojem od zahteva od 1 do 3, naznačeno time, što se koristi u tretmanu raka.
7. Jedinjenje ili neka njegova farmaceutski prihvatljiva so prema zahtevu 6, naznačeno time, što karcinom je nesitnoćelijski karcinom pluća.
8. Jedinjenje ili neka njegova farmaceutski prihvatljiva so kao šta se zahteva u bilo kojem od zahteva od 1 do 3, naznačeno time, što se upotrebljava u tretmanu bolesti koje su posredovane mutantom L858R EGFR i/ili mutantom T790M EGFR i/ili mutantom koji aktiviše deleciju Egzona 19.
9. Farmaceutski proizvod koji sadrži jedinjenje ili neku njegovu farmaceutski prihvatljiva so, kao šta se zahteva u bilo kojem od zahteva od 1 do 3, i dodatnu anti-tumorsku supstanciju, naznačen time, što se koristi za objedinjeni tretman raka.
10. Farmaceutski produkt kao šta se zahteva u zahtevu 9, naznačen time, što pomenuti rak je nesitnoćelijski karcinom pluća.
11. Jedinjenje ili neka njegova farmaceutski prihvatljiva so, kao šta se zahteva u bilo kojem od zahteva od 1 do 3, i neka dodatna anti-tumorska supstancija, naznačeno time, što se upotrebljava u objedinjenom tretmanu raka.
12. Jedinjenje ili neka njegova farmaceutski prihvatljiva so, kao šta se zahteva u bilo kojem od zahteva od 1 do 3, i neka dodatna anti-tumorska supstancija, naznačeno time, što se upotrebljava u objedinjenom tretmanu nesitnoćelijskog karcinoma pluća.
MEP-2017-290A 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka ME02887B (me)

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
EP15192658.1A EP3009431B1 (en) 2011-07-27 2012-07-25 2-(2,4,5-substituted-anilino)pyrimidine derivatives as egfr modulators useful for treating cancer

Publications (1)

Publication Number Publication Date
ME02887B true ME02887B (me) 2018-04-20

Family

ID=46875901

Family Applications (3)

Application Number Title Priority Date Filing Date
MEP-2020-87A ME03785B (me) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino)pirimidinski derivati kao egfr modulatori korisni za liječenje raka
MEP-2016-34A ME02382B (me) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) piramidisnki derivati kao egfr modulatori korisni za tretman raka
MEP-2017-290A ME02887B (me) 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
MEP-2020-87A ME03785B (me) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino)pirimidinski derivati kao egfr modulatori korisni za liječenje raka
MEP-2016-34A ME02382B (me) 2011-07-27 2012-07-25 2-(2,4,5-supstituisani-anilino) piramidisnki derivati kao egfr modulatori korisni za tretman raka

Country Status (38)

Country Link
US (8) US8946235B2 (me)
EP (7) EP2736895B1 (me)
JP (3) JP5427321B2 (me)
KR (3) KR101410902B1 (me)
CN (7) CN104109161B (me)
AR (1) AR087336A1 (me)
AU (1) AU2012288626C1 (me)
BR (4) BR122014026114B1 (me)
CA (5) CA2843109C (me)
CL (1) CL2013003281A1 (me)
CO (1) CO6811863A2 (me)
CR (1) CR20130629A (me)
CY (4) CY1117431T1 (me)
DK (5) DK2736895T3 (me)
DO (1) DOP2013000263A (me)
EA (3) EA029488B1 (me)
EC (1) ECSP13013033A (me)
ES (5) ES2654177T3 (me)
GT (1) GT201300288A (me)
HR (4) HRP20160135T1 (me)
HU (4) HUE049060T2 (me)
IL (6) IL229199A (me)
LT (3) LT3686194T (me)
ME (3) ME03785B (me)
MX (3) MX2014000528A (me)
MY (2) MY161925A (me)
NI (1) NI201300134A (me)
PE (1) PE20141700A1 (me)
PH (2) PH12013502312A1 (me)
PL (5) PL3686193T3 (me)
PT (4) PT3686193T (me)
RS (4) RS54653B1 (me)
SG (5) SG10201910984XA (me)
SI (4) SI3686194T1 (me)
SM (3) SMT202100652T1 (me)
TW (3) TWI583386B (me)
UY (1) UY34219A (me)
WO (1) WO2013014448A1 (me)

Families Citing this family (227)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MX2010012703A (es) 2008-05-21 2010-12-21 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
KR101769999B1 (ko) 2008-09-18 2017-08-21 노오쓰웨스턴 유니버시티 Ｎｍｄａ 수용체 조절제 및 그의 용도
JP5746172B2 (ja) 2009-08-20 2015-07-08 カルス セラピューティクス リミテッド ホスホイノシチド３−キナーゼ阻害剤としての三環式複素環化合物
BR112013027734A2 (pt) 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
EP2736895B1 (en) 2011-07-27 2016-01-06 Astrazeneca AB 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
BR112015018087B1 (pt) 2013-01-29 2022-09-20 Aptinyx Inc Compostos moduladores de receptor n-metil-d-aspartato (nmda) de espiro-lactama, composição farmacêutica e uso dos mesmos
JP6531042B2 (ja) * 2013-01-29 2019-06-12 アプティニックス インコーポレイテッド スピロラクタム系ｎｍｄａ受容体モジュレーターおよびその使用
US9527857B2 (en) 2013-03-15 2016-12-27 GI Therapeutics, Inc. 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
WO2014210354A1 (en) * 2013-06-28 2014-12-31 Genentech, Inc. 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
NZ718190A (en) 2013-08-23 2017-10-27 Neupharma Inc Substituted quinazolines for inhibiting kinase activity
RU2019131017A (ru) * 2013-10-21 2019-11-25 Мерк Патент Гмбх Соединения гетероарила в качестве ингибиторов btk и их применение
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
WO2015150826A1 (en) * 2014-04-04 2015-10-08 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
CN106687457B (zh) * 2014-05-13 2020-01-10 阿里亚德医药股份有限公司 用于激酶抑制的杂芳基化合物
CN106660993B (zh) * 2014-06-12 2020-09-11 上海复尚慧创医药研究有限公司 一类激酶抑制剂
PE20170268A1 (es) 2014-06-19 2017-04-21 Ariad Pharma Inc Compuestos de heteroarilo para la inhibicion de cinasa
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
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
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
RU2702631C2 (ru) 2014-10-11 2019-10-09 Шанхай Хэнсох Биомедикал Ко., Лтд. Ингибитор egfr и его получение и применение
MX2017003181A (es) 2014-10-13 2017-07-20 Yuhan Corp Compuestos y composiciones para modular actividades de quinasa de mutante de receptor del factor de crecimiento epidermico.
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
EP3226869A4 (en) * 2014-12-03 2018-07-18 Auckland UniServices, Ltd. Kinase inhibitor prodrug for the treatment of cancer
US10590111B2 (en) * 2014-12-11 2020-03-17 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as EGFR modulators
US10266517B2 (en) 2014-12-23 2019-04-23 Dana-Farber Cancer Institute, Inc. Pyrimidines as EGFR inhibitors and methods of treating disorders
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
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
EP3270694A4 (en) 2015-02-17 2018-09-05 Neupharma, Inc. Certain chemical entities, compositions, and methods
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
TWI685494B (zh) * 2015-04-29 2020-02-21 大陸商廣東眾生藥業股份有限公司 稠環或三環芳基嘧啶化合物用作激酶抑制劑
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
EP3294712A4 (en) * 2015-05-13 2018-11-07 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
JP6970081B2 (ja) * 2015-07-16 2021-11-24 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 アニリンピリミジン誘導体及びその使用
AU2016296877B2 (en) 2015-07-20 2020-09-17 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as EGFR inhibitors and methods of treating disorders
US10561646B2 (en) 2015-07-24 2020-02-18 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. EGFR inhibitor and pharmaceutically acceptable salt and polymorph thereof, and use thereof
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
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
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
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
US10377747B2 (en) 2015-08-31 2019-08-13 Wuxi Shuangliang Biotechnology Co., Ltd. 2-arylamino pyridine, pyrimidine or triazine derivatives, preparation method and use thereof
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
TW201718583A (zh) * 2015-11-23 2017-06-01 Nanjing Sanhome Pharmaceutical Co Ltd 新的表皮生長因子受體抑制劑及其應用
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
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
US10829495B2 (en) 2015-12-03 2020-11-10 Zhejiang Jianfeng-Yien Biotechnology Co., Ltd. Thieno-pyrimidine derivatives 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
EP3399968B8 (en) 2016-01-07 2021-12-01 Xuanzhu Biopharmaceutical Co., Ltd. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
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
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
CN108610331A (zh) * 2016-01-22 2018-10-02 焦玉奇 2-(2,4,5-取代苯胺)嘧啶衍生物
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
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
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
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
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
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
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
RU2733412C2 (ru) * 2016-03-22 2020-10-01 Цзянсу Хансох Фармасьютикал Груп Ко., Лтд. Поликристаллическая форма свободного основания или соли присоединения кислоты ингибитора egfr, способ её получения и применение
US11052086B2 (en) * 2016-05-11 2021-07-06 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
WO2017201285A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
PE20190174A1 (es) 2016-05-19 2019-02-01 Aptinyx Inc Moduladores del receptor espiro-lactama n-metil-d-aspartato y usos de los mismos
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
EP3471730B1 (en) 2016-06-17 2021-10-20 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
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
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
CN109661398B (zh) 2016-08-01 2022-07-05 阿普廷伊克斯股份有限公司 螺-内酰胺和二-螺-内酰胺nmda受体调节剂及其用途
AU2017306152A1 (en) 2016-08-01 2019-01-31 Aptinyx Inc. Spiro-lactam NMDA receptor modulators and uses thereof
SG11201900554YA (en) 2016-08-01 2019-02-27 Aptinyx Inc Spiro-lactam nmda modulators and methods of using same
BR112019001921A2 (pt) 2016-08-01 2019-05-14 Aptinyx Inc. moduladores do receptor nmda de espiro-lactama e seus usos
US10918637B2 (en) 2016-08-01 2021-02-16 Aptinyx Inc. Spiro-lactam NMDA receptor modulators and uses thereof
AU2017312561B2 (en) 2016-08-15 2022-06-30 Neupharma, Inc. Certain chemical entities, compositions, and methods
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
CN106366072B (zh) * 2016-08-19 2018-12-07 上海工程技术大学 一种azd9291的制备方法
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
CA3037097C (en) * 2016-09-19 2021-06-29 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
AU2017345574A1 (en) * 2016-10-19 2019-05-23 United States Government As Represented By The Department Of Veterans Affairs Compositions and methods for treating 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
KR101954369B1 (ko) 2017-01-26 2019-03-05 한미약품 주식회사 피리미딘 화합물 및 그의 의약 용도
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
CN110325191A (zh) * 2017-02-22 2019-10-11 G1治疗公司 以较少的副作用治疗egfr-驱动的癌症
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
US10882845B2 (en) 2017-05-24 2021-01-05 TYK Medicines Inc. Crystal form of deuterated AZD9291, preparation method therefor, and use thereof
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
TWI808977B (zh) * 2017-06-13 2023-07-21 大陸商北京浦潤奧生物科技有限責任公司 胺基嘧啶類化合物及其製備方法和用途
MX2019015177A (es) * 2017-06-16 2020-02-07 Beta Pharma Inc Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas.
CN108467385A (zh) * 2017-06-27 2018-08-31 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
CN111295381A (zh) 2017-07-28 2020-06-16 株式会社柳韩洋行 可用于合成抗蛋白激酶的选择性抑制剂的中间体及其制备方法
MX393995B (es) * 2017-07-28 2025-03-24 Yuhan Corp Proceso mejorado para preparar derivados de aminopirimidina
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
US11471457B2 (en) 2017-08-21 2022-10-18 Eli Lilly And Company Method of treating epithelial growth factor receptor (EGFR) T790M-positive non-small cell lung cancer by administering a combination of a VEGFR-2 antibody and osimertinib
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
MX2020004991A (es) * 2017-11-17 2022-02-10 Univ Illinois Terapia oncológica mediante la degradación de la señalización dual de mek.
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
US11578072B2 (en) 2018-01-31 2023-02-14 Aptinyx Inc. Spiro-lactam NMDA receptor modulators and uses thereof
WO2019152696A1 (en) * 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
KR20200143361A (ko) * 2018-02-08 2020-12-23 뉴파마, 인크. 특정 화학 물질, 조성물, 및 방법
MA51823A (fr) 2018-02-12 2021-05-19 Astrazeneca Ab Osimertinib destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules
EP3755330A4 (en) * 2018-02-20 2021-11-24 Dana-Farber Cancer Institute, Inc. PHARMACEUTICAL COMBINATIONS OF EGFR INHIBITORS AND THEIR METHODS OF USE
JP2021514011A (ja) * 2018-02-20 2021-06-03 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒ阻害剤の組合せ医薬製剤およびその使用法
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
KR20200144579A (ko) 2018-05-14 2020-12-29 어리어드 파마슈티칼스, 인코포레이티드 피리미딘 유도체의 약학 염 및 장애의 치료 방법
CN112119074A (zh) * 2018-05-15 2020-12-22 益方生物科技（上海）有限公司 Egfr抑制剂
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
US12090153B2 (en) 2018-10-05 2024-09-17 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
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
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
PH12021551985A1 (en) 2019-02-22 2022-08-22 Hanmi Pharmaceutical Co Ltd Pharmaceutical composition comprising flt3 inhibitor and hypomethylating agent for treating acute myeloid leukemia
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
CN113645976A (zh) 2019-03-29 2021-11-12 阿斯利康(瑞典)有限公司 用于治疗非小细胞肺癌的奧希替尼
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
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
JP7534795B2 (ja) 2019-05-01 2024-08-15 クレキシオ バイオサイエンシーズ エルティーディー． そう痒症を治療する方法
WO2020224568A1 (en) 2019-05-05 2020-11-12 Qilu Regor Therapeutics Inc. Cdk inhibitors
CA3138648A1 (en) * 2019-05-22 2020-11-26 Shanghai Hansoh Biomedical Co., Ltd. Indole derivative-containing inhibitor, preparation method therefor and application thereof
KR20210002015A (ko) 2019-06-27 2021-01-06 한미약품 주식회사 Flt3 저해제 및 화학치료제를 포함하는 급성 골수성 백혈병 치료용 약학적 조성물
GB201909468D0 (en) 2019-07-01 2019-08-14 Karus Therapeutics Ltd Compounds for treating cancer
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
AU2020408562A1 (en) 2019-12-20 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
CA3166980A1 (en) 2020-01-20 2021-07-29 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
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
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
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
WO2022046867A1 (en) 2020-08-25 2022-03-03 Loxo Oncology, Inc. Osimertinib and selpercatinib combinations for the treatment of egfr- and ret-associated cancers
US12162893B2 (en) 2020-09-23 2024-12-10 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
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
JP2024523861A (ja) 2021-06-15 2024-07-02 ジェネンテック， インコーポレイテッド がんを処置するための併用療法におけるｅｇｆｒ阻害剤およびｐｅｒｋ活性化剤、ならびにこれらの使用
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
CN117440945A (zh) * 2021-08-06 2024-01-23 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
AU2022340897A1 (en) * 2021-09-02 2024-03-14 Synthon B.V. A process for making osimertinib
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
CN119278041A (zh) 2022-03-31 2025-01-07 阿斯利康(瑞典)有限公司 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂
AR128999A1 (es) 2022-04-07 2024-07-03 Astrazeneca Ab Proceso mejorado para la fabricación de osimertinib
AU2023262556A1 (en) 2022-04-28 2024-12-05 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20250275968A1 (en) * 2022-05-03 2025-09-04 Deutsches Zentrum Für Neurodegenerative Erkrankungen E.V. Inhibitors of tau proteins
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
JP2025522965A (ja) 2022-07-08 2025-07-17 アストラゼネカ・アクチエボラーグ 癌の治療のためのｈｇｆ受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤
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
IL319661A (en) * 2022-09-19 2025-05-01 Advenchen Pharmaceuticals Llc A novel pyrimidine compound as kinase inhibitors with biological activities on EGFR mutations
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
WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib
WO2025245045A1 (en) 2024-05-21 2025-11-27 The Regents Of The University Of California Methods of treating lung cancer
WO2026009146A1 (en) 2024-07-01 2026-01-08 Hetero Labs Limited Benzimidazole compounds as egfr inhibitors
WO2026047630A1 (en) 2024-08-31 2026-03-05 Hetero Labs Limited Heterocyclic compounds as egfr inhibitors
WO2026053183A1 (en) 2024-09-09 2026-03-12 Hetero Labs Limited Benzothiazole and benzoxazole compounds as egfr inhibitors

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
JP4471404B2 (ja) 1996-02-13 2010-06-02 アストラゼネカ ユーケイ リミテッド Ｖｅｇｆインヒビターとしてのキナゾリン誘導体
ATE211134T1 (de) 1996-03-05 2002-01-15 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
DK1553097T3 (da) 1999-02-10 2010-12-13 Astrazeneca Ab Quinazolinderivat som angiogeneseinhibitor og mellemprodukter dertil
NZ522074A (en) 2000-05-31 2004-06-25 Astrazeneca Ab Indole derivatives with vascular damaging activity
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
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
CA2410562A1 (en) 2000-07-07 2002-01-31 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
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
WO2006068826A2 (en) * 2004-12-21 2006-06-29 Smithkline Beecham Corporation 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
ZA200706804B (en) 2005-02-03 2008-10-29 Gen Hospital Corp Method for treating gefitinib resistant cancer
TW200734327A (en) 2005-11-03 2007-09-16 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
US7807673B2 (en) * 2005-12-05 2010-10-05 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
EP2040546A4 (en) 2006-06-22 2009-12-23 Merck & Co Inc tyrosine kinase inhibitor
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
EP2214486A4 (en) 2007-10-19 2011-03-09 Avila Therapeutics Inc HETEROARYL COMPOUNDS AND ITS USES
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-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
SG10201510696RA (en) * 2008-06-27 2016-01-28 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
MY156789A (en) 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
WO2010042337A1 (en) 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. 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
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
IN2012DN02534A (me) 2009-09-16 2015-08-28 Avila Therapeutics Inc
CA2778265A1 (en) * 2009-11-02 2011-05-05 Abbott Laboratories Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
MX342164B (es) 2010-06-23 2016-09-19 Hanmi Science Co Ltd Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa.
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
BR112013027734A2 (pt) * 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
EP2736895B1 (en) 2011-07-27 2016-01-06 Astrazeneca AB 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer

Also Published As

Publication number Publication date
AU2012288626A1 (en) 2013-05-02
CN105175396A (zh) 2015-12-23
CA2881987C (en) 2017-04-25
DK2736895T3 (da) 2016-02-29
JP2013544273A (ja) 2013-12-12
SG10201402860QA (en) 2014-08-28
CY1125405T1 (el) 2023-03-24
HK1192554A1 (en) 2014-08-22
TWI583386B (zh) 2017-05-21
ES2654177T3 (es) 2018-02-12
CY1120072T1 (el) 2018-12-12
IL242285A0 (en) 2015-11-30
DK3333161T3 (da) 2020-05-18
IL242279A (en) 2016-07-31
MX2020013020A (es) 2022-06-14
EP2736895B1 (en) 2016-01-06
EP3333161A1 (en) 2018-06-13
IL242278A0 (en) 2015-11-30
BR122014026150A2 (pt) 2019-05-28
EA201391491A1 (ru) 2014-08-29
CY1123210T1 (el) 2021-10-29
JP5537704B2 (ja) 2014-07-02
CN105175396B (zh) 2018-01-16
KR20140062181A (ko) 2014-05-22
DOP2013000263A (es) 2014-01-31
AU2012288626C1 (en) 2015-09-17
RS60190B1 (sr) 2020-06-30
EA201792394A2 (ru) 2018-03-30
BR112014001768B1 (pt) 2019-02-05
SG10201910986QA (en) 2020-01-30
US20210130318A1 (en) 2021-05-06
DK3009431T3 (en) 2018-01-08
US8946235B2 (en) 2015-02-03
KR20140030089A (ko) 2014-03-11
KR101410902B1 (ko) 2014-06-20
CA2881987A1 (en) 2013-01-31
US20190092746A1 (en) 2019-03-28
PL3686194T3 (pl) 2022-01-17
TWI465445B (zh) 2014-12-21
HK1256370A1 (en) 2019-09-20
RS56679B1 (sr) 2018-03-30
KR101691268B1 (ko) 2016-12-29
SG10201910984XA (en) 2020-01-30
MY194532A (en) 2022-11-30
CA2881991C (en) 2016-10-25
BR122014026114B1 (pt) 2021-01-12
BR112014001768A2 (pt) 2017-02-14
EA029488B1 (ru) 2018-04-30
SG10201402857QA (en) 2014-08-28
IL242286A0 (en) 2015-11-30
JP2014139226A (ja) 2014-07-31
CN105254616A (zh) 2016-01-20
US20240425476A1 (en) 2024-12-26
ECSP13013033A (es) 2014-01-31
PL3009431T3 (pl) 2018-02-28
IL242285A (en) 2016-07-31
EP3686193B1 (en) 2022-03-02
CN103702990B (zh) 2015-09-09
EP2736895A1 (en) 2014-06-04
AR087336A1 (es) 2014-03-19
SMT201600070B (it) 2016-04-29
BR122014026094A2 (pt) 2019-08-20
US10858336B2 (en) 2020-12-08
CA2882018C (en) 2017-04-25
CA2881993A1 (en) 2013-01-31
SI3333161T1 (sl) 2020-07-31
DK3686194T3 (da) 2021-11-22
WO2013014448A1 (en) 2013-01-31
HUE037645T2 (hu) 2018-09-28
CN104109161B (zh) 2016-08-17
US20190389834A1 (en) 2019-12-26
ES2914854T3 (es) 2022-06-17
HUE056365T2 (hu) 2022-02-28
IL242279A0 (en) 2015-11-30
SI3009431T1 (en) 2018-01-31
SMT202100652T1 (it) 2022-01-10
PL3686193T3 (pl) 2022-06-13
PL3333161T3 (pl) 2020-08-24
PT3686193T (pt) 2022-05-20
EA033733B1 (ru) 2019-11-20
CR20130629A (es) 2014-03-12
EA024421B1 (ru) 2016-09-30
JP2014094930A (ja) 2014-05-22
GT201300288A (es) 2017-10-09
CA2843109A1 (en) 2013-01-31
CN105254616B (zh) 2017-10-17
SG194783A1 (en) 2013-12-30
CN105198862B (zh) 2018-01-23
ES2791308T3 (es) 2020-11-03
CN105198862A (zh) 2015-12-30
LT3009431T (lt) 2018-01-10
CA2882018A1 (en) 2013-01-31
PH12013502312A1 (en) 2016-07-13
CY1117431T1 (el) 2017-04-26
CN105348266A (zh) 2016-02-24
IL242284A0 (en) 2015-11-30
KR20140047741A (ko) 2014-04-22
PH12015501326B1 (en) 2015-09-14
HRP20200624T1 (hr) 2020-07-10
HRP20160135T1 (hr) 2016-03-11
EP4119551A1 (en) 2023-01-18
EA201690328A1 (ru) 2016-11-30
HRP20171957T1 (hr) 2018-02-09
EP3686193A1 (en) 2020-07-29
TWI555743B (zh) 2016-11-01
CA2881991A1 (en) 2013-01-31
BR122014026094B1 (pt) 2020-10-13
US20240182441A1 (en) 2024-06-06
PL2736895T3 (pl) 2016-05-31
AU2012288626A8 (en) 2013-09-26
US11524951B2 (en) 2022-12-13
JP5977779B2 (ja) 2016-08-24
EP4086246A1 (en) 2022-11-09
PT3009431T (pt) 2017-12-26
IL242286A (en) 2016-07-31
CL2013003281A1 (es) 2014-07-25
PH12015501326A1 (en) 2015-09-14
HK1221216A1 (en) 2017-05-26
US20150119379A1 (en) 2015-04-30
LT3333161T (lt) 2020-05-11
ME02382B (me) 2016-06-20
US10017493B2 (en) 2018-07-10
NI201300134A (es) 2014-02-12
HK1192549A1 (zh) 2014-08-22
AU2012288626B2 (en) 2015-05-07
EP3009431A1 (en) 2016-04-20
NZ617393A (en) 2014-11-28
TW201443040A (zh) 2014-11-16
CO6811863A2 (es) 2013-12-16
PT3686194T (pt) 2021-11-11
JP5427321B2 (ja) 2014-02-26
ME03785B (me) 2021-04-20
EP3686194B1 (en) 2021-09-15
IL229199A0 (en) 2014-01-30
MX377900B (es) 2025-03-10
CN104109151B (zh) 2017-04-12
US20130053409A1 (en) 2013-02-28
BR122014026150B1 (pt) 2020-10-13
US20180162832A1 (en) 2018-06-14
LT3686194T (lt) 2021-11-25
HRP20211682T1 (hr) 2022-03-04
ES2564671T3 (es) 2016-03-28
SI2736895T1 (sl) 2016-03-31
MX2014000528A (es) 2014-05-01
MY161925A (en) 2017-05-15
CN105348266B (zh) 2018-04-10
ES2900230T3 (es) 2022-03-16
TW201319057A (zh) 2013-05-16
PT3333161T (pt) 2020-05-18
KR101422619B1 (ko) 2014-07-24
CA2881993C (en) 2017-05-09
PE20141700A1 (es) 2014-11-20
SMT202000208T1 (it) 2020-05-08
IL242284A (en) 2016-07-31
SI3686194T1 (sl) 2022-01-31
EP3333161B1 (en) 2020-02-19
RS62542B1 (sr) 2021-12-31
HUE026429T2 (en) 2016-05-30
CA2843109C (en) 2015-06-16
UY34219A (es) 2013-02-28
EP3686194A1 (en) 2020-07-29
IL242278A (en) 2016-12-29
TW201700099A (zh) 2017-01-01
CN103702990A (zh) 2014-04-02
DK3686193T3 (da) 2022-05-30
EP3009431B1 (en) 2017-10-25
RS54653B1 (sr) 2016-08-31
IL229199A (en) 2015-11-30
EA201792394A3 (ru) 2018-07-31
HUE049060T2 (hu) 2020-08-28
US9732058B2 (en) 2017-08-15
CN104109151A (zh) 2014-10-22
CN104109161A (zh) 2014-10-22
BR122014026114A2 (pt) 2019-08-20

Similar Documents

Publication Publication Date Title
ME02887B (me) 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EA201790246A1 (ru) Гетероциклические карбоновые кислоты в качестве активаторов растворимой гуанилатциклазы
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
NZ630124A (en) Estrogen receptor modulators and uses thereof
JO3108B1 (ar) بيرروليدينونات أروماتية مخلطة مندمجة كمثبطات syk
EA201691151A1 (ru) Соединения для лечения пациентов с ros1-мутантными раковыми клетками
EA201690035A1 (ru) Новые циклические производные азабензимидазола, используемые в качестве антидиабетических агентов
EA201400358A1 (ru) Замещенные n-[1-циано-2-(фенил)этил]-2-азабицикло[2.2.1]гептан-3-карбоксамидные ингибиторы катепсина с
EA201492125A1 (ru) НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2
EA201591908A1 (ru) Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
EA201490016A1 (ru) Комбинация панобиностата и руксолитинаба при лечении рака, такого как миелопролиферативное новообразование
PE20130405A1 (es) Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
EA201592200A1 (ru) Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201692465A1 (ru) Кристаллические соли (s)-6-((1-ацетилпиперидин-4-ил)амино)-n-(3-(3,4-дигидроизохинолин-2(1h)-ил)-2-гидроксипропил)пиримидин-4-карбоксамида
EA201400553A1 (ru) Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида
PE20090876A1 (es) Nuevos derivados de 6-aril/heteroalquiloxi benzotiazol y bencimidazol, su procedimiento de preparacion, su aplicacion como medicamentos, composiciones farmaceuticas y nueva utilizacion principalmente como inhibidores de cmet
MD20160105A2 (ro) 2-Amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il-1,3-tiazol-4-il amide
PH12012502280A1 (en) Urea derivatives and their therapeutic use in the treatment of, inter alia, diseases of the respiratory tract
EA201300436A8 (ru) Совместные кристаллы и соли ингибиторов ccr3
NZ630099A (en) Phenicol antibacterials
EA201892415A1 (ru) Полиморфная форма n-{6-(2-гидроксипропан-2-ил)-2-[2-(метилсульфонил)этил]-2н-индазол-5-ил}-6-(трифторметил)пиридин-2-карбоксамида
EA201590205A1 (ru) N-алкил 2-(дизамещенные)алкиниладенозин-5-уронамиды в качестве а-агонистов