HRP20171957T1 - Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka - Google Patents

Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka Download PDF

Info

Publication number
HRP20171957T1
HRP20171957T1 HRP20171957TT HRP20171957T HRP20171957T1 HR P20171957 T1 HRP20171957 T1 HR P20171957T1 HR P20171957T T HRP20171957T T HR P20171957TT HR P20171957 T HRP20171957 T HR P20171957T HR P20171957 T1 HRP20171957 T1 HR P20171957T1
Authority
HR
Croatia
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
cancer
amino
Prior art date
Application number
HRP20171957TT
Other languages
English (en)
Inventor
Sam Butterworth
Maurice Raymond Verschoyle Finlay
Richard Andrew Ward
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=HRP20171957(T1) "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 HRP20171957T1 publication Critical patent/HRP20171957T1/hr

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
    • 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
    • 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

Claims (12)

1. Spoj naznačen time da je odabran od N-(2-[2-dimetilaminoetil-metilamino]-5-{[4-(1H-indol-3-il)pirimidin-2-il]amino}-4-metoksifenil)-prop-2-enamida: [image] i N-(4-metoksi-5-{[4-(1-metilindol-3-il)pirimidin-2-il]amino}-2-[metil-(2-metilaminoetil)amino]fenil)prop-2-enamida: [image] ili njihova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1 naznačen time da je N-(2-[2-dimetilaminoetil-metilamino]-5-{[4-(1H-indol-3-il)pirimidin-2-il]amino}-4-metoksifenil)-prop-2-enamid
3. Spoj kako je zatraženo u zahtjevu 1, naznačen time da je N-(4-metoksi-5-{[4-(1-metilindol-3-il)pirimidin-2-il]amino}}-2-[metil-(2-metilaminoetil)amino]fenil)prop-2-enamid.
4. Farmaceutski pripravak naznačen time da sadrži spoj ili njegovu farmaceutski prihvatljivu sol kako je zatraženo u bilo kojem od zahtjeva 1 do 3, u kombinaciji s farmaceutski prihvatljivim sredstvom za otapanje ili nosačem.
5. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, naznačen time da je za uporabu kao lijek.
6. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, naznačen time da je za uporabu za liječenje raka.
7. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u zahtjevu 6, naznačen time da rak je rak pluća ne-malih stanica.
8. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, naznačen time da je za uporabu za liječenje bolesti posredovane putem L858R EGFR mutanta i/ili T790M EGFR mutanta i/ili Exon19 mutant koji aktivira brisanje.
9. Farmaceutski proizvod naznačen time da sadrži spoj ili njegovu farmaceutski prihvatljivu sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, te dodatno protu-tumorsko sredstvo za zajedničko liječenje raka.
10. Farmaceutski proizvod prema zahtjevu 9, naznačen time da rak je rak pluća ne-malih stanica.
11. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, te dodatno protu-tumorsko sredstvo naznačen time da je za uporabu za zajedničko liječenje raka.
12. Spoj ili njegova farmaceutski prihvatljiva sol, kako je zatraženo u bilo kojem od zahtjeva 1 do 3, te dodatno protu-tumorsko sredstvo naznačen time da je za uporabu za zajedničko liječenje raka pluća ne-malih stanica.
HRP20171957TT 2011-07-27 2017-12-18 Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka HRP20171957T1 (hr)

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
HRP20171957T1 true HRP20171957T1 (hr) 2018-02-09

Family

ID=46875901

Family Applications (4)

Application Number Title Priority Date Filing Date
HRP20211682TT HRP20211682T1 (hr) 2011-07-27 2012-07-25 2-(2,4,5-supstituirani-anilino) pirimidinski spojevi
HRP20160135TT HRP20160135T1 (hr) 2011-07-27 2016-02-05 Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za lijeäśenje raka
HRP20171957TT HRP20171957T1 (hr) 2011-07-27 2017-12-18 Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka
HRP20200624TT HRP20200624T1 (hr) 2011-07-27 2020-04-20 Derivati 2-(2,4,5-supstituiranog-anilino)pirimidina kao modulatori egfr korisni za liječenje raka

Family Applications Before (2)

Application Number Title Priority Date Filing Date
HRP20211682TT HRP20211682T1 (hr) 2011-07-27 2012-07-25 2-(2,4,5-supstituirani-anilino) pirimidinski spojevi
HRP20160135TT HRP20160135T1 (hr) 2011-07-27 2016-02-05 Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za lijeäśenje raka

Family Applications After (1)

Application Number Title Priority Date Filing Date
HRP20200624TT HRP20200624T1 (hr) 2011-07-27 2020-04-20 Derivati 2-(2,4,5-supstituiranog-anilino)pirimidina kao modulatori egfr korisni za liječenje raka

Country Status (39)

Country Link
US (6) US8946235B2 (hr)
EP (7) EP4119551A1 (hr)
JP (3) JP5427321B2 (hr)
KR (3) KR101410902B1 (hr)
CN (7) CN104109161B (hr)
AR (1) AR087336A1 (hr)
AU (1) AU2012288626C1 (hr)
BR (4) BR122014026114B1 (hr)
CA (5) CA2843109C (hr)
CL (1) CL2013003281A1 (hr)
CO (1) CO6811863A2 (hr)
CR (1) CR20130629A (hr)
CY (4) CY1117431T1 (hr)
DK (5) DK3009431T3 (hr)
DO (1) DOP2013000263A (hr)
EA (3) EA024421B1 (hr)
EC (1) ECSP13013033A (hr)
ES (5) ES2654177T3 (hr)
GT (1) GT201300288A (hr)
HK (4) HK1192549A1 (hr)
HR (4) HRP20211682T1 (hr)
HU (4) HUE056365T2 (hr)
IL (6) IL229199A (hr)
LT (3) LT3686194T (hr)
ME (3) ME03785B (hr)
MX (2) MX2014000528A (hr)
MY (2) MY161925A (hr)
NI (1) NI201300134A (hr)
PE (1) PE20141700A1 (hr)
PH (1) PH12015501326B1 (hr)
PL (5) PL3686193T3 (hr)
PT (4) PT3686194T (hr)
RS (4) RS54653B1 (hr)
SG (5) SG194783A1 (hr)
SI (4) SI3009431T1 (hr)
SM (1) SMT201600070B (hr)
TW (3) TWI555743B (hr)
UY (1) UY34219A (hr)
WO (1) WO2013014448A1 (hr)

Families Citing this family (209)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
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
PL2467387T3 (pl) 2009-08-20 2015-08-31 Karus Therapeutics Ltd Tricykliczne związki heterocykliczne jako inhibitory kinazy 3-fosfoinozytydu
WO2012151561A1 (en) 2011-05-04 2012-11-08 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN104109161B (zh) 2011-07-27 2016-08-17 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
EP2951182B1 (en) * 2013-01-29 2020-03-18 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
LT2951183T (lt) 2013-01-29 2019-05-27 Aptinyx Inc. Spiro-laktamo nmda receptorių moduliatoriai ir jų panaudojimas
CN108283644B (zh) 2013-03-15 2022-03-18 G1治疗公司 在化学疗法期间对正常细胞的瞬时保护
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
BR112016005199B1 (pt) 2013-08-23 2022-02-22 Neupharma, Inc Certos compostos químicos, composições, e métodos
PT3060550T (pt) * 2013-10-21 2019-08-27 Merck Patent Gmbh Compostos de heteroarilo como inibidores de btk e utilizações dos mesmos
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
ES2890556T3 (es) * 2014-04-04 2022-01-20 Astrazeneca Ab Combinación de inhibidor de EGFR e inhibidor de MEK para su uso en el tratamiento del cáncer con mutación de NRAS
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
JP6468611B2 (ja) * 2014-05-13 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 キナーゼ阻害のためのヘテロアリール化合物
CN111875585B (zh) * 2014-06-12 2023-06-23 上海艾力斯医药科技股份有限公司 一类激酶抑制剂
AP2017009690A0 (en) * 2014-06-19 2017-01-31 Ariad Pharma Inc Heteroaryl compounds for kinase inhibition
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
CN106661000B (zh) * 2014-10-11 2019-04-09 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
EP3604294B1 (en) * 2014-10-13 2021-05-05 Yuhan Corporation Compounds and compositions for modulating egfr mutant kinase activities
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
WO2016090174A1 (en) * 2014-12-03 2016-06-09 Auckland Uniservices, Ltd. Kinase inhibitor prodrug for the treatment of cancer
CA2970185C (en) * 2014-12-11 2023-10-17 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as egfr modulators
CN107406442B (zh) * 2014-12-23 2021-08-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
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
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
AU2016220219B2 (en) 2015-02-17 2020-05-14 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2016173438A1 (zh) 2015-04-29 2016-11-03 南京明德新药研发股份有限公司 稠环或三环芳基嘧啶化合物用作激酶抑制剂
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
US20210323976A1 (en) * 2015-05-13 2021-10-21 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
JP6949726B2 (ja) 2015-05-15 2021-10-13 ノバルティス アーゲー Ｅｇｆｒ変異癌を治療する方法
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
AU2016292450B2 (en) * 2015-07-16 2021-03-25 Centaurus Biopharma Co., Ltd. Aniline pyrimidine derivatives and uses thereof
US10550112B2 (en) 2015-07-20 2020-02-04 Dana-Farber Cancer Institute, Inc. Pyrimidines as EGFR inhibitors and methods of treating disorders
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
GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514751D0 (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
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
WO2017035753A1 (zh) * 2015-08-31 2017-03-09 无锡双良生物科技有限公司 2-芳胺基吡啶、嘧啶或三嗪衍生物及其制备方法和用途
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
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
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
US10844074B2 (en) * 2015-12-03 2020-11-24 Zhejiang Jianfeng-Yien Biotechnology Co., Ltd. Heterocycle compounds and uses thereof
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
CN109328059B (zh) 2016-01-07 2021-08-17 Cs制药技术有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
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
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
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
CN110590749B (zh) * 2016-03-07 2020-11-06 上海艾力斯医药科技股份有限公司 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
WO2017161937A1 (zh) 2016-03-22 2017-09-28 江苏豪森药业集团有限公司 Egfr抑制剂游离碱或其酸式盐的多晶型、其制备方法和应用
AU2017264839B2 (en) 2016-05-11 2021-08-05 Beta Pharma, Inc. 2-Anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
MX2018014202A (es) 2016-05-19 2019-06-20 Aptinyx Inc Moduladores del receptor espiro-lactama n-metil-d-aspartato y usos de los mismos.
WO2017201285A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
AU2017269335B2 (en) * 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
US10844045B2 (en) * 2016-06-17 2020-11-24 Beta Pharma, Inc. Pharmaceutical salts 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
CA3031539C (en) 2016-08-01 2023-11-28 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
CN109843889B (zh) 2016-08-01 2022-03-15 阿普廷伊克斯股份有限公司 螺-内酰胺nmda调节剂和使用其的方法
KR102503590B1 (ko) 2016-08-01 2023-02-24 앱티닉스 인크. 스피로-락탐 nmda 수용체 조정제 및 그의 용도
CA3031537A1 (en) 2016-08-01 2018-02-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
KR102462288B1 (ko) 2016-08-01 2022-11-01 앱티닉스 인크. 스피로-락탐 및 비스-스피로-락탐 nmda 수용체 조정제 및 그의 용도
JP7101165B2 (ja) 2016-08-15 2022-07-14 ニューファーマ， インコーポレイテッド 特定の化学的実体、組成物、および方法
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
US11672801B2 (en) * 2016-10-19 2023-06-13 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
EP3514153B1 (en) 2017-01-26 2021-07-07 Hanmi Pharm. Co., Ltd. Pyrimidine compound and pharmaceutical use thereof
WO2018156812A1 (en) * 2017-02-22 2018-08-30 G1 Therapeutics, Inc. Treatment of egfr-driven cancer with fewer side effects
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer 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
CN108558835A (zh) * 2017-05-24 2018-09-21 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
ES2963921T3 (es) * 2017-06-13 2024-04-03 Beijing Avlstone Biotechnology Co Ltd Compuestos de aminopirimidina, su método de preparación y uso de los mismos
EA201992744A1 (ru) 2017-06-16 2020-05-27 Бета Фарма, Инк. Фармацевтические композиции n-(2-(2-(диметиламино)этокси)-4-метокси-5-((4-(1-метил-1h-индол-3-ил)пиримидин-2-ил)амино)фенил)акриламида и его солей
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
WO2019022485A1 (en) * 2017-07-28 2019-01-31 Yuhan Corporation IMPROVED PROCESS FOR THE PREPARATION OF AMINOPYRIMIDINE DERIVATIVES
SI3658547T1 (sl) * 2017-07-28 2023-10-30 Yuhan Corporation Postopek za pripravo n-(5-(4-(4-formil-3-fenil-1h-pirazol-1-1l)pirimidin-2-ilamino)-4-metoksi -2-morfolinofenil)akrilamida
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
WO2019040348A1 (en) 2017-08-21 2019-02-28 Eli Lilly And Company COMBINATIONS OF EGFR INHIBITORS AND ANTI-VEGFR -2 HUMAN ANTIBODIES
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
KR20200090771A (ko) * 2017-11-17 2020-07-29 더 보오드 오브 트러스티스 오브 더 유니버시티 오브 일리노이즈 이중 mek 신호 전달 분해를 통한 암 치료
CN111837146A (zh) 2018-01-08 2020-10-27 G1治疗公司 G1t38优异剂量方案
WO2019152696A1 (en) * 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
CN112204031A (zh) 2018-01-31 2021-01-08 阿普廷伊克斯股份有限公司 螺-内酰胺nmda受体调节剂及其用途
EP3749310A4 (en) * 2018-02-08 2021-08-18 Neupharma, Inc. CERTAIN CHEMICAL SUBSTANCES, COMPOSITIONS AND PROCEDURES
CA3090010A1 (en) 2018-02-12 2019-08-15 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
EP3755337A4 (en) * 2018-02-20 2021-11-03 Dana-Farber Cancer Institute, Inc. EGFR INHIBITOR PHARMACEUTICAL COMBINATIONS AND METHODS OF USE
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
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
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
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
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
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
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
WO2020140934A1 (zh) * 2019-01-05 2020-07-09 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
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
US20220175783A1 (en) 2019-03-29 2022-06-09 Astrazeneca Ab Osimertinib for use in the treatment of non-small cell lung cancer
EA202100252A1 (ru) * 2019-04-09 2022-03-10 Хэнань Дженьюин Биотек Ко., Лтд. Производная 2-(2,4,5-замещенного фениламино)пиримидина и его кристаллическая форма "в"
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
CN112292378B (zh) * 2019-05-22 2024-02-06 上海翰森生物医药科技有限公司 含吲哚类衍生物抑制剂、其制备方法和应用
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
US20210161897A1 (en) 2019-11-12 2021-06-03 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
WO2021127404A1 (en) 2019-12-20 2021-06-24 Erasca, Inc. Tricyclic pyridones and pyrimidones
MX2022008874A (es) 2020-01-20 2022-08-11 Astrazeneca Ab Inhibidores de la tirosina cinasa del receptor del factor de creciminto epidermico para el tratamiento del cancer.
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
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
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
CN113929663A (zh) * 2020-06-29 2022-01-14 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
US20220119409A1 (en) 2020-09-23 2022-04-21 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
WO2022105882A1 (zh) * 2020-11-19 2022-05-27 上海翰森生物医药科技有限公司 一种含吲哚类衍生物的盐、晶型及其制备方法和应用
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
EP4355330A1 (en) 2021-06-15 2024-04-24 Genentech, Inc. Egfr inhibitor and perk activator in combination therapy and their use for treating cancer
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
CA3229553A1 (en) 2021-09-02 2023-03-09 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
JP2023043050A (ja) * 2021-09-15 2023-03-28 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
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
WO2023187037A1 (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
WO2023194531A1 (en) 2022-04-07 2023-10-12 Astrazeneca Ab Improved process for the manufacture of osimertinib
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2023209084A1 (en) 2022-04-28 2023-11-02 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
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023213850A1 (en) * 2022-05-03 2023-11-09 Deutsches Zentrum Für Neurodegenerative Erkrankungen E. V. (Dzne) Inhibitors of tau proteins
WO2024002938A1 (en) 2022-06-27 2024-01-04 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of 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
CN115650974A (zh) * 2022-08-04 2023-01-31 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

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
CZ291386B6 (cs) 1996-02-13 2003-02-12 Zeneca Limited Chinazolinové deriváty jako inhibitory VEGF, způsob jejich přípravy a farmaceutický prostředek, který je obsahuje
US6291455B1 (en) 1996-03-05 2001-09-18 Zeneca Limited 4-anilinoquinazoline derivatives
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
PL205557B1 (pl) 1999-02-10 2010-05-31 Astrazeneca Ab Pochodne indolu
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
EP1301498A1 (en) 2000-07-07 2003-04-16 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
US20050277627A1 (en) 2000-07-07 2005-12-15 Arnould Jean C Colchinol derivatives as vascular damaging agents
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
CN113952459A (zh) 2005-02-03 2022-01-21 综合医院公司 治疗吉非替尼耐药性癌症的方法
AR056763A1 (es) 2005-11-03 2007-10-24 Vertex Pharma Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen.
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
WO2007067506A2 (en) * 2005-12-05 2007-06-14 Smithkline Beecham Corporation 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
AU2007261440A1 (en) 2006-06-22 2007-12-27 Merck & Co., Inc. Tyrosine kinase inhibitors
US20100010025A1 (en) * 2006-07-21 2010-01-14 Norvartis Ag Pyrimidine Derivatives
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
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
JP2011526299A (ja) * 2008-06-27 2011-10-06 アビラ セラピューティクス， インコーポレイテッド ヘテロアリール化合物およびそれらの使用
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
US9908884B2 (en) 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
EP2496574A1 (en) * 2009-11-02 2012-09-12 Abbott Laboratories Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition
US20110207736A1 (en) 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, 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
LT2975042T (lt) 2010-06-23 2019-01-25 Hanmi Science Co., Ltd. Naujieji kondensuoti pirimidino dariniai, skirti tirozino kinazės aktyvumo slopinimui
TW201219383A (en) 2010-08-02 2012-05-16 Astrazeneca Ab Chemical compounds
WO2012151561A1 (en) * 2011-05-04 2012-11-08 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN104109161B (zh) 2011-07-27 2016-08-17 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症

Also Published As

Publication number Publication date
MY194532A (en) 2022-11-30
AU2012288626A1 (en) 2013-05-02
PE20141700A1 (es) 2014-11-20
AU2012288626A8 (en) 2013-09-26
BR122014026150A2 (pt) 2019-05-28
HRP20160135T1 (hr) 2016-03-11
BR112014001768B1 (pt) 2019-02-05
CN103702990B (zh) 2015-09-09
SG10201910984XA (en) 2020-01-30
KR20140030089A (ko) 2014-03-11
IL242284A0 (en) 2015-11-30
DOP2013000263A (es) 2014-01-31
CA2881987C (en) 2017-04-25
TWI583386B (zh) 2017-05-21
CA2881993C (en) 2017-05-09
ES2914854T3 (es) 2022-06-17
EP3686193B1 (en) 2022-03-02
SI3009431T1 (en) 2018-01-31
KR20140062181A (ko) 2014-05-22
SG194783A1 (en) 2013-12-30
PL3333161T3 (pl) 2020-08-24
HUE049060T2 (hu) 2020-08-28
DK3686194T3 (da) 2021-11-22
KR101422619B1 (ko) 2014-07-24
DK2736895T3 (da) 2016-02-29
BR122014026094B1 (pt) 2020-10-13
US8946235B2 (en) 2015-02-03
CN105254616B (zh) 2017-10-17
EP2736895A1 (en) 2014-06-04
CA2881987A1 (en) 2013-01-31
AR087336A1 (es) 2014-03-19
PT3333161T (pt) 2020-05-18
ME03785B (me) 2021-04-20
ECSP13013033A (es) 2014-01-31
CA2881991A1 (en) 2013-01-31
IL229199A (en) 2015-11-30
JP5977779B2 (ja) 2016-08-24
CY1123210T1 (el) 2021-10-29
TW201700099A (zh) 2017-01-01
IL242279A0 (en) 2015-11-30
CA2843109C (en) 2015-06-16
CN104109151A (zh) 2014-10-22
DK3009431T3 (en) 2018-01-08
BR122014026114B1 (pt) 2021-01-12
DK3333161T3 (da) 2020-05-18
US10017493B2 (en) 2018-07-10
MY161925A (en) 2017-05-15
EP2736895B1 (en) 2016-01-06
CN105348266B (zh) 2018-04-10
JP2014094930A (ja) 2014-05-22
AU2012288626C1 (en) 2015-09-17
PT3686193T (pt) 2022-05-20
SG10201402860QA (en) 2014-08-28
CN104109161B (zh) 2016-08-17
HK1256370A1 (zh) 2019-09-20
JP5427321B2 (ja) 2014-02-26
HK1192549A1 (zh) 2014-08-22
EP3333161B1 (en) 2020-02-19
ES2791308T3 (es) 2020-11-03
EP3686193A1 (en) 2020-07-29
MX2020013020A (es) 2022-06-14
HUE056365T2 (hu) 2022-02-28
EA029488B1 (ru) 2018-04-30
CY1125405T1 (el) 2023-03-24
KR20140047741A (ko) 2014-04-22
TWI465445B (zh) 2014-12-21
CN105198862A (zh) 2015-12-30
CY1120072T1 (el) 2018-12-12
US20210130318A1 (en) 2021-05-06
US9732058B2 (en) 2017-08-15
CA2881993A1 (en) 2013-01-31
EA201792394A2 (ru) 2018-03-30
KR101691268B1 (ko) 2016-12-29
EA033733B1 (ru) 2019-11-20
SI3686194T1 (sl) 2022-01-31
EA201792394A3 (ru) 2018-07-31
CN104109161A (zh) 2014-10-22
JP5537704B2 (ja) 2014-07-02
CN105348266A (zh) 2016-02-24
LT3686194T (lt) 2021-11-25
RS56679B1 (sr) 2018-03-30
US20190389834A1 (en) 2019-12-26
EP3333161A1 (en) 2018-06-13
US10858336B2 (en) 2020-12-08
CA2843109A1 (en) 2013-01-31
IL242285A0 (en) 2015-11-30
GT201300288A (es) 2017-10-09
LT3333161T (lt) 2020-05-11
BR122014026094A2 (pt) 2019-08-20
HK1221216A1 (zh) 2017-05-26
US20130053409A1 (en) 2013-02-28
IL242278A (en) 2016-12-29
CN105254616A (zh) 2016-01-20
BR122014026114A2 (pt) 2019-08-20
HUE037645T2 (hu) 2018-09-28
HK1192554A1 (en) 2014-08-22
TW201319057A (zh) 2013-05-16
CA2882018C (en) 2017-04-25
EP3009431B1 (en) 2017-10-25
PH12015501326A1 (en) 2015-09-14
WO2013014448A1 (en) 2013-01-31
EP4086246A1 (en) 2022-11-09
EP3686194B1 (en) 2021-09-15
PH12015501326B1 (en) 2015-09-14
US11524951B2 (en) 2022-12-13
PL3686193T3 (pl) 2022-06-13
TWI555743B (zh) 2016-11-01
IL242279A (en) 2016-07-31
CN105175396A (zh) 2015-12-23
AU2012288626B2 (en) 2015-05-07
NI201300134A (es) 2014-02-12
EA201690328A1 (ru) 2016-11-30
CN105198862B (zh) 2018-01-23
SG10201402857QA (en) 2014-08-28
RS54653B1 (en) 2016-08-31
ES2564671T3 (es) 2016-03-28
CA2881991C (en) 2016-10-25
IL242285A (en) 2016-07-31
IL242286A0 (en) 2015-11-30
ES2900230T3 (es) 2022-03-16
PT3009431T (pt) 2017-12-26
CL2013003281A1 (es) 2014-07-25
MX2014000528A (es) 2014-05-01
JP2014139226A (ja) 2014-07-31
US20180162832A1 (en) 2018-06-14
ES2654177T3 (es) 2018-02-12
ME02887B (me) 2018-04-20
EA201391491A1 (ru) 2014-08-29
HRP20211682T1 (hr) 2022-03-04
CN105175396B (zh) 2018-01-16
CA2882018A1 (en) 2013-01-31
PL3686194T3 (pl) 2022-01-17
TW201443040A (zh) 2014-11-16
KR101410902B1 (ko) 2014-06-20
SMT201600070B (it) 2016-04-29
EA024421B1 (ru) 2016-09-30
DK3686193T3 (da) 2022-05-30
PL2736895T3 (pl) 2016-05-31
BR112014001768A2 (pt) 2017-02-14
RS60190B1 (sr) 2020-06-30
US20150119379A1 (en) 2015-04-30
LT3009431T (lt) 2018-01-10
HRP20200624T1 (hr) 2020-07-10
SI2736895T1 (sl) 2016-03-31
IL242284A (en) 2016-07-31
RS62542B1 (sr) 2021-12-31
CR20130629A (es) 2014-03-12
BR122014026150B1 (pt) 2020-10-13
CO6811863A2 (es) 2013-12-16
EP3686194A1 (en) 2020-07-29
CN104109151B (zh) 2017-04-12
UY34219A (es) 2013-02-28
IL229199A0 (en) 2014-01-30
IL242278A0 (en) 2015-11-30
CN103702990A (zh) 2014-04-02
IL242286A (en) 2016-07-31
SG10201910986QA (en) 2020-01-30
EP3009431A1 (en) 2016-04-20
SI3333161T1 (sl) 2020-07-31
PT3686194T (pt) 2021-11-11
CY1117431T1 (el) 2017-04-26
NZ617393A (en) 2014-11-28
JP2013544273A (ja) 2013-12-12
HUE026429T2 (en) 2016-05-30
PL3009431T3 (pl) 2018-02-28
US20190092746A1 (en) 2019-03-28
EP4119551A1 (en) 2023-01-18
ME02382B (me) 2016-06-20

Similar Documents

Publication Publication Date Title
HRP20171957T1 (hr) Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
HRP20151399T1 (hr) Kinazni inhibitor koji regulira signalni put apoptoze
CY1118135T1 (el) Παραγωγα 2-(φαινυλο ή πυριδ-3-υλο) αμινοπυριμιδινης ως ρυθμιστες κινασης lrrk2 για τη θεραπευτικη αντιμετωπιση της νοσου του parkinson
EA201690752A1 (ru) Ингибиторы g12c kras
HRP20220864T1 (hr) Derivati n-piridinil acetamida kao inhibitori signalnog puta wnt
EA201492125A1 (ru) НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2
EA201690848A1 (ru) Производные бициклического пиридила с конденсированными кольцами в качестве ингибиторов fgfr4
WO2014120808A8 (en) Pyridone amides as modulators of sodium channels
EA201490016A1 (ru) Комбинация панобиностата и руксолитинаба при лечении рака, такого как миелопролиферативное новообразование
EA201691242A1 (ru) Фармацевтические композиции, содержащие azd9291
EA201592256A1 (ru) Производные имидазопирролидинона и их применение при лечении заболеваний
CL2012003604A1 (es) Compuestos heterociclicos derivados de piridina carboxamida sustituida; proceso de preparacion; composicion farmaceutica; combinacion farmaceutica; uso en el tratamiento de trastornos proliferativos celulares, enfermedad de parkinson, cancer, entre otros.
IN2014CN00408A (hr)
NZ612000A (en) Bicyclo[3.2.1]octyl amide derivatives and uses of same
EA201291220A1 (ru) Производные аминопиримидина в качестве модуляторов lrrk2
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
PE20130405A1 (es) Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
EA201001724A1 (ru) Производные изоксазола и их применение в качестве потенциирующих средств для метаботропных глутаматных рецепторов
UA115881C2 (uk) Алкоксипіразоли як активатори розчинної гуанілатциклази
EA201591195A1 (ru) Новые хинолоновые производные
EA201400161A1 (ru) Замещенные гетероароматические пиразолсодержащие карбоксамидные и мочевинные производные в качестве лигандов ваниллоидных рецепторов
EA201692542A1 (ru) Индановые и индолиновые производные и их применение в качестве активаторов растворимой гуанилатциклазы
PH12016500885A1 (en) Novel heterocyclic compounds
EA201300436A1 (ru) Совместные кристаллы и соли ингибиторов ccr3