AU2015360360B2 - Substituted 2-anilinopyrimidine derivatives as EGFR modulators - Google Patents
Substituted 2-anilinopyrimidine derivatives as EGFR modulators Download PDFInfo
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- AU2015360360B2 AU2015360360B2 AU2015360360A AU2015360360A AU2015360360B2 AU 2015360360 B2 AU2015360360 B2 AU 2015360360B2 AU 2015360360 A AU2015360360 A AU 2015360360A AU 2015360360 A AU2015360360 A AU 2015360360A AU 2015360360 B2 AU2015360360 B2 AU 2015360360B2
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- Australia
- Prior art keywords
- cancer
- methyl
- pharmaceutically acceptable
- compound
- hydrogen
- Prior art date
- Legal status (The legal status 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 status listed.)
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- SEGWIIQNKLKQQT-UHFFFAOYSA-N CN(C)CCCc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2n[n](C)c3ccccc23)ccn1 Chemical compound CN(C)CCCc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2n[n](C)c3ccccc23)ccn1 SEGWIIQNKLKQQT-UHFFFAOYSA-N 0.000 description 3
- JFHZBQRUZXXWCG-UHFFFAOYSA-N CCOc(cc(c(NC(C=C)=O)c1)OCCN(C)C)c1Nc1nc(-c2c[nH]c3ccccc23)ccn1 Chemical compound CCOc(cc(c(NC(C=C)=O)c1)OCCN(C)C)c1Nc1nc(-c2c[nH]c3ccccc23)ccn1 JFHZBQRUZXXWCG-UHFFFAOYSA-N 0.000 description 2
- OAXQKPPMQLREDM-UHFFFAOYSA-N CN(C)CCCc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2c(cccc3)[n]3nc2)ccn1 Chemical compound CN(C)CCCc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2c(cccc3)[n]3nc2)ccn1 OAXQKPPMQLREDM-UHFFFAOYSA-N 0.000 description 2
- ZRQMURIELJVSCH-UHFFFAOYSA-N CN(C)CCOc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2n[n](C)c3ccccc23)ccn1 Chemical compound CN(C)CCOc(c(NC(C=C)=O)c1)cc(OC)c1Nc1nc(-c2n[n](C)c3ccccc23)ccn1 ZRQMURIELJVSCH-UHFFFAOYSA-N 0.000 description 2
- KHOYUEASLIXESL-UHFFFAOYSA-N CCCCc(cc(c(Nc1nc(-c2c[n](C)c3ccccc23)ccn1)c1)OC)c1NC(C=C)=O Chemical compound CCCCc(cc(c(Nc1nc(-c2c[n](C)c3ccccc23)ccn1)c1)OC)c1NC(C=C)=O KHOYUEASLIXESL-UHFFFAOYSA-N 0.000 description 1
- UTDICVFAOMSHNP-UHFFFAOYSA-N C[n]1nc(cccc2)c2c1-c1ccnc(Nc(c(OC)c2)cc(NC(C(Cl)=C)=O)c2OC)n1 Chemical compound C[n]1nc(cccc2)c2c1-c1ccnc(Nc(c(OC)c2)cc(NC(C(Cl)=C)=O)c2OC)n1 UTDICVFAOMSHNP-UHFFFAOYSA-N 0.000 description 1
- NEKLIYWZWBTFEE-UHFFFAOYSA-N Cc([n](C)c1ccccc11)c1-c1ccnc(Nc(cc(c(OCCN(C)C)c2)NC(C=C)=O)c2OC)n1 Chemical compound Cc([n](C)c1ccccc11)c1-c1ccnc(Nc(cc(c(OCCN(C)C)c2)NC(C=C)=O)c2OC)n1 NEKLIYWZWBTFEE-UHFFFAOYSA-N 0.000 description 1
- GVVYBCFPHBMQMN-UHFFFAOYSA-N Cc([n](C)c1ccccc11)c1-c1ccnc(Nc(cc2NC(C=C)=O)c(C)cc2OCCN(C)C)n1 Chemical compound Cc([n](C)c1ccccc11)c1-c1ccnc(Nc(cc2NC(C=C)=O)c(C)cc2OCCN(C)C)n1 GVVYBCFPHBMQMN-UHFFFAOYSA-N 0.000 description 1
- GWSMZIXYBWKXEI-UHFFFAOYSA-N Cc([n](C)c1ccccc11)c1-c1ccnc(Nc2cc(NC(C(Cl)=C)=O)c(CCCN(C)C)cc2OC)n1 Chemical compound Cc([n](C)c1ccccc11)c1-c1ccnc(Nc2cc(NC(C(Cl)=C)=O)c(CCCN(C)C)cc2OC)n1 GWSMZIXYBWKXEI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462090869P | 2014-12-11 | 2014-12-11 | |
| US62/090,869 | 2014-12-11 | ||
| US201562166883P | 2015-05-27 | 2015-05-27 | |
| US62/166,883 | 2015-05-27 | ||
| PCT/US2015/065286 WO2016094821A2 (en) | 2014-12-11 | 2015-12-11 | Substituted 2-anilinopyrimidine derivatives as egfr modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2015360360A1 AU2015360360A1 (en) | 2017-06-08 |
| AU2015360360B2 true AU2015360360B2 (en) | 2020-06-25 |
Family
ID=56108380
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2015360360A Active AU2015360360B2 (en) | 2014-12-11 | 2015-12-11 | Substituted 2-anilinopyrimidine derivatives as EGFR modulators |
Country Status (17)
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN112375067B (zh) * | 2014-12-11 | 2024-03-15 | 贝达医药公司 | 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂 |
| EA201892311A1 (ru) * | 2016-05-11 | 2019-06-28 | Бета Фарма, Инк. | Производные 2-анилинопиримидина в качестве терапевтических агентов для лечения рака мозга |
| JP7030066B2 (ja) | 2016-05-26 | 2022-03-04 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | Ｅｇｆｒ阻害剤化合物 |
| KR20190018494A (ko) * | 2016-06-17 | 2019-02-22 | 베타 파마, 인크. | N-(2-(2-(디메틸아미노)에톡시)-4-메톡시-5-((4-(1-메틸-1h-인돌-3-일)피리미딘-2-일)아미노)페닐)아크릴아미드의 제약 염 및 그의 결정질 형태 |
| CN106243044A (zh) * | 2016-06-30 | 2016-12-21 | 浙江大学 | 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用 |
| CN110818690B (zh) * | 2016-07-26 | 2021-08-10 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| EP3638241B1 (en) | 2017-06-16 | 2022-05-25 | Beta Pharma, Inc. | Pharmaceutical formulations of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and salts thereof |
| CN109503573A (zh) * | 2017-09-14 | 2019-03-22 | 昆明圣加南生物科技有限公司 | 2-取代苯胺基嘧啶衍生物及其用途 |
| CN107935995A (zh) * | 2017-11-28 | 2018-04-20 | 中山大学 | 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用 |
| CN108017633A (zh) * | 2018-01-30 | 2018-05-11 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用 |
| KR20210028191A (ko) * | 2018-06-18 | 2021-03-11 | 유씨비 바이오파마 에스알엘 | 암을 예방 및 치료하기 위한 gremlin-1 길항제 |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| CN114430681A (zh) * | 2019-09-23 | 2022-05-03 | 贝达医药公司 | 使用egfr和cdk4/6抑制剂的组合治疗egfr突变相关的癌症 |
| US20210161897A1 (en) | 2019-11-12 | 2021-06-03 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CN114980883A (zh) | 2020-01-20 | 2022-08-30 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂 |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| AU2022312430A1 (en) * | 2021-07-13 | 2024-02-29 | ACEA Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| AU2023246862A1 (en) | 2022-03-31 | 2024-10-31 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
| WO2023209086A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds for treating cancer |
| CA3249080A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | CONDENSED BICYCLIC HETEROAROMATIC COMPOUNDS AND THEIR USE IN CANCER TREATMENT |
| 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 |
| KR20250029133A (ko) | 2022-06-27 | 2025-03-04 | 아스트라제네카 아베 | 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제를 포함하는 조합물 |
| 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 |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001047922A2 (en) * | 1999-12-24 | 2001-07-05 | Aventis Pharma Limited | Azaindoles |
| US20080146565A1 (en) * | 2006-12-08 | 2008-06-19 | Roche Palo Alto Llc | JNK modulators |
| WO2010059711A1 (en) * | 2008-11-18 | 2010-05-27 | Wisconsin Alumni Research Foundation | Sigma-1 receptor ligands and methods of use |
| WO2010129053A2 (en) * | 2009-05-05 | 2010-11-11 | Dana Farber Cancer Institute | Egfr inhibitors and methods of treating disorders |
| US7943616B2 (en) * | 2001-06-21 | 2011-05-17 | Aventis Pharmaceuticals Inc. | Azaindoles for inhibiting aurora2 and other kinases |
| US20120316135A1 (en) * | 2011-05-04 | 2012-12-13 | Ariad Pharmaceuticals, Inc. | Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers |
| WO2013014448A1 (en) * | 2011-07-27 | 2013-01-31 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| WO2015195228A1 (en) * | 2014-06-19 | 2015-12-23 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| WO2016070816A1 (zh) * | 2014-11-05 | 2016-05-12 | 上海页岩科技有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6469567B2 (ja) * | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
| 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 |
| 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 |
| 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 |
| CN112375067B (zh) | 2014-12-11 | 2024-03-15 | 贝达医药公司 | 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂 |
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2015
- 2015-12-11 CN CN202011112988.2A patent/CN112375067B/zh active Active
- 2015-12-11 EA EA201790921A patent/EA036453B1/ru unknown
- 2015-12-11 JP JP2017530208A patent/JP6709786B2/ja active Active
- 2015-12-11 US US15/534,838 patent/US10590111B2/en active Active
- 2015-12-11 WO PCT/US2015/065286 patent/WO2016094821A2/en not_active Ceased
- 2015-12-11 TW TW104141810A patent/TWI618704B/zh not_active IP Right Cessation
- 2015-12-11 MX MX2017007664A patent/MX382869B/es unknown
- 2015-12-11 EP EP15867768.2A patent/EP3229798A4/en not_active Ceased
- 2015-12-11 CN CN202011112986.3A patent/CN112457298B/zh active Active
- 2015-12-11 KR KR1020177019147A patent/KR20170098865A/ko not_active Ceased
- 2015-12-11 CN CN201580067776.8A patent/CN108024993B/zh active Active
- 2015-12-11 AU AU2015360360A patent/AU2015360360B2/en active Active
- 2015-12-11 BR BR112017012272-3A patent/BR112017012272A2/pt not_active IP Right Cessation
- 2015-12-11 SG SG10201909060S patent/SG10201909060SA/en unknown
- 2015-12-11 HK HK18104991.1A patent/HK1245634A1/zh unknown
- 2015-12-11 SG SG11201704685TA patent/SG11201704685TA/en unknown
- 2015-12-11 CA CA2970185A patent/CA2970185C/en active Active
-
2017
- 2017-05-28 IL IL252554A patent/IL252554A0/en active IP Right Grant
- 2017-06-07 PH PH12017501057A patent/PH12017501057A1/en unknown
- 2017-07-11 CO CONC2017/0006962A patent/CO2017006962A2/es unknown
-
2020
- 2020-03-16 US US16/819,539 patent/US11414401B2/en active Active
- 2020-05-25 JP JP2020090467A patent/JP7181558B2/ja active Active
Patent Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001047922A2 (en) * | 1999-12-24 | 2001-07-05 | Aventis Pharma Limited | Azaindoles |
| US7943616B2 (en) * | 2001-06-21 | 2011-05-17 | Aventis Pharmaceuticals Inc. | Azaindoles for inhibiting aurora2 and other kinases |
| US20080146565A1 (en) * | 2006-12-08 | 2008-06-19 | Roche Palo Alto Llc | JNK modulators |
| WO2010059711A1 (en) * | 2008-11-18 | 2010-05-27 | Wisconsin Alumni Research Foundation | Sigma-1 receptor ligands and methods of use |
| WO2010129053A2 (en) * | 2009-05-05 | 2010-11-11 | Dana Farber Cancer Institute | Egfr inhibitors and methods of treating disorders |
| US20120316135A1 (en) * | 2011-05-04 | 2012-12-13 | Ariad Pharmaceuticals, Inc. | Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers |
| WO2013014448A1 (en) * | 2011-07-27 | 2013-01-31 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| US20130053409A1 (en) * | 2011-07-27 | 2013-02-28 | Astrazeneca Ab | 2-(2,4,5-substituted-anilino) pyrimidine compounds |
| WO2015195228A1 (en) * | 2014-06-19 | 2015-12-23 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| WO2016070816A1 (zh) * | 2014-11-05 | 2016-05-12 | 上海页岩科技有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
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| HB | Alteration of name in register |
Owner name: BETA PHARMA, INC. Free format text: FORMER NAME(S): BETA PHARMA, INC. Owner name: BETA PHARMA (SHANGHAI) CO., LTD. Free format text: FORMER NAME(S): BETA PHARMA, INC. |
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