BR112017012272A2 - derivados de 2-anilinopirimidina como moduladores de egfr - Google Patents
derivados de 2-anilinopirimidina como moduladores de egfrInfo
- Publication number
- BR112017012272A2 BR112017012272A2 BR112017012272-3A BR112017012272A BR112017012272A2 BR 112017012272 A2 BR112017012272 A2 BR 112017012272A2 BR 112017012272 A BR112017012272 A BR 112017012272A BR 112017012272 A2 BR112017012272 A2 BR 112017012272A2
- Authority
- BR
- Brazil
- Prior art keywords
- anilinopyrimidine derivatives
- egfr modulators
- egfr
- anilinopyrimidine
- derivatives
- Prior art date
Links
- 108060006698 EGF receptor Proteins 0.000 title abstract 2
- XGXNTJHZPBRBHJ-UHFFFAOYSA-N n-phenylpyrimidin-2-amine Chemical class N=1C=CC=NC=1NC1=CC=CC=C1 XGXNTJHZPBRBHJ-UHFFFAOYSA-N 0.000 title abstract 2
- 102000009024 Epidermal Growth Factor Human genes 0.000 abstract 1
- 101800003838 Epidermal growth factor Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 229940116977 epidermal growth factor Drugs 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 abstract 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 (1)
| Publication Number | Publication Date |
|---|---|
| BR112017012272A2 true BR112017012272A2 (pt) | 2018-01-30 |
Family
ID=56108380
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017012272-3A BR112017012272A2 (pt) | 2014-12-11 | 2015-12-11 | derivados de 2-anilinopirimidina como moduladores de egfr |
Country Status (17)
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| SG10201909060SA (en) * | 2014-12-11 | 2019-11-28 | Beta Pharma Inc | Substituted 2-anilinopyrimidine derivatives as egfr modulators |
| BR112018072887A2 (pt) | 2016-05-11 | 2019-03-06 | Beta Pharma, Inc. | método de tratamento de câncer de cérebro em um indivíduo, e utilização de um composto |
| SG11201809751XA (en) | 2016-05-26 | 2018-12-28 | Zeno Royalties & Milestones Llc | Egfr inhibitor compounds |
| AU2017285448B2 (en) * | 2016-06-17 | 2021-02-04 | Beta Pharma, Inc. | Pharmaceutical salts of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof |
| 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 |
| JP6740452B2 (ja) * | 2016-07-26 | 2020-08-12 | 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． | プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物 |
| BR112019026483A2 (pt) * | 2017-06-16 | 2020-07-14 | Beta Pharma, Inc. | formulação farmacêutica de n-(2-(2-(dimetilamina)etoxi)-4-metoxi-5-((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amina)fenil)acrilamida e seus sais |
| 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 |
| PT3806898T (pt) * | 2018-06-18 | 2025-12-02 | UCB Biopharma SRL | Antagonista de gremlin-1 para utilização no tratamento do cancro |
| SG11202102377YA (en) | 2018-09-10 | 2021-04-29 | Mirati Therapeutics Inc | Combination therapies |
| EP4034121A4 (en) * | 2019-09-23 | 2023-10-18 | Beta Pharma, Inc. | TREATMENT OF EGFR MUTANT-RELATED CANCERS USING A COMBINATION OF EGFR AND CDK4/6 INHIBITORS |
| US20210161897A1 (en) | 2019-11-12 | 2021-06-03 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| AU2021211871A1 (en) | 2020-01-20 | 2022-09-08 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| KR20240063865A (ko) * | 2021-07-13 | 2024-05-10 | 아세아 테라퓨틱스 인코포레이티드 | 헤테로사이클릭 화합물 및 이의 용도 |
| 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 |
| WO2023209090A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their application in the treatment of cancer |
| JP2025516171A (ja) | 2022-04-28 | 2025-05-27 | アストラゼネカ・アクチエボラーグ | 縮合二環式ヘテロ芳香族化合物及び癌の治療におけるその使用 |
| WO2023209088A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their use in the treatment of cancer |
| WO2023209086A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds for treating cancer |
| CA3259492A1 (en) | 2022-06-27 | 2024-01-04 | Astrazeneca Ab | COMBINATIONS INVOLVING EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER |
| CN119654152A (zh) | 2022-07-08 | 2025-03-18 | 阿斯利康(瑞典)有限公司 | 与hgf-受体抑制剂组合用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK288019B6 (sk) | 1999-12-24 | 2012-11-05 | Aventis Pharma Limited | Azaindoles derivatives, their use and pharmaceutical composition containing thereof |
| GB0115109D0 (en) * | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| CA2670375A1 (en) * | 2006-12-08 | 2008-06-12 | F. Hoffmann-La Roche Ag | Substituted pyrimidines and their use as jnk modulators |
| WO2010059711A1 (en) | 2008-11-18 | 2010-05-27 | Wisconsin Alumni Research Foundation | Sigma-1 receptor ligands and methods of use |
| US9908884B2 (en) | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
| AU2012250517B2 (en) * | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| PL3009431T3 (pl) * | 2011-07-27 | 2018-02-28 | Astrazeneca Ab | Pochodne 2-(2,4,5-podstawionej-anilino) pirymidyny jako modulatory egfr użyteczne do leczenia nowotworu |
| 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 |
| PH12016502453B1 (en) | 2014-06-19 | 2022-11-23 | Takeda Pharmaceuticals Co | Heteroaryl compounds for kinase inhibition |
| WO2016029839A1 (zh) | 2014-08-25 | 2016-03-03 | 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 |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| SG10201909060SA (en) | 2014-12-11 | 2019-11-28 | Beta Pharma Inc | Substituted 2-anilinopyrimidine derivatives as egfr modulators |
-
2015
- 2015-12-11 SG SG10201909060S patent/SG10201909060SA/en unknown
- 2015-12-11 BR BR112017012272-3A patent/BR112017012272A2/pt not_active IP Right Cessation
- 2015-12-11 CN CN202011112988.2A patent/CN112375067B/zh active Active
- 2015-12-11 CN CN201580067776.8A patent/CN108024993B/zh active Active
- 2015-12-11 KR KR1020177019147A patent/KR20170098865A/ko not_active Ceased
- 2015-12-11 HK HK18104991.1A patent/HK1245634A1/zh unknown
- 2015-12-11 AU AU2015360360A patent/AU2015360360B2/en active Active
- 2015-12-11 EP EP15867768.2A patent/EP3229798A4/en not_active Ceased
- 2015-12-11 JP JP2017530208A patent/JP6709786B2/ja active Active
- 2015-12-11 CN CN202011112986.3A patent/CN112457298B/zh active Active
- 2015-12-11 CA CA2970185A patent/CA2970185C/en active Active
- 2015-12-11 SG SG11201704685TA patent/SG11201704685TA/en unknown
- 2015-12-11 WO PCT/US2015/065286 patent/WO2016094821A2/en not_active Ceased
- 2015-12-11 US US15/534,838 patent/US10590111B2/en active Active
- 2015-12-11 EA EA201790921A patent/EA036453B1/ru unknown
- 2015-12-11 MX MX2017007664A patent/MX382869B/es unknown
- 2015-12-11 TW TW104141810A patent/TWI618704B/zh not_active IP Right Cessation
-
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
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A ANUIDADE. |
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| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2700 DE 04-10-2022 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |