AR117424A1 - Inhibidores de los receptores erbb - Google Patents
Inhibidores de los receptores erbbInfo
- Publication number
- AR117424A1 AR117424A1 ARP190101206A ARP190101206A AR117424A1 AR 117424 A1 AR117424 A1 AR 117424A1 AR P190101206 A ARP190101206 A AR P190101206A AR P190101206 A ARP190101206 A AR P190101206A AR 117424 A1 AR117424 A1 AR 117424A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- haloalkyl
- substituted
- halogen
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic 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)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se revelan compuestos que inhiben ErbB (por ejemplo HER2), sales farmacéuticamente aceptables, hidratos, solvatos o estereoisómeros de los mismos, y composiciones farmacéuticas que comprenden los compuestos. El compuesto y la composición farmacéutica pueden tratar efectivamente las enfermedades asociadas con los ErbB (especialmente, HER2), incluyendo cáncer. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable, éster, hidrato, solvato o estereoisómero del mismo, caracterizado porque: R¹ es hidrógeno; R² es hidrógeno, halógeno, hidroxilo, alquilo C₁₋₁₂, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, o haloalquilo C₁₋₁₂; G es N o C-CN; W es O, C(=O), S, SO, o SO₂; Y es un enlace o alquileno C₁₋₁₂; R³ es carbociclilo insaturado o saturado de 3 - 10 miembros, o heterociclilo insaturado o saturado de 3 - 10 miembros que puede estar opcionalmente mono-sustituido o independientemente multi-sustituido por halógeno, hidroxilo, amino, alquilo C₁₋₁₂, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, haloalquilo C₁₋₁₂, alquilo C₁₋₁₂ sustituido; i es 0, 1, 2 ó 3, y cada R⁴ es independientemente halógeno, amino, hidroxilo, alquilo C₁₋₁₂, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, o haloalquilo C₁₋₁₂; j es 0, 1, 2 ó 3, y cada R⁵ es independientemente halógeno, amino, hidroxilo, alquilo C₁₋₁₂, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, haloalquilo C₁₋₁₂ o OR⁶, que puede estar opcionalmente mono-sustituido o independientemente multi-sustituido; R⁶ es carbociclilo insaturado o saturado de 3 - 10 miembros, o heterociclilo insaturado o saturado de 3 - 10 miembros opcionalmente mono-sustituido o independientemente multi-sustituido por hidroxilo, halógeno, ciano, alquilo C₁₋₁₂, o haloalquilo C₁₋₁₂; A es O, C(=O), S, SO, o SO₂; E es un compuesto del grupo de fórmulas (2); X¹, X², X³, y X⁴ son, cada uno, independientemente, N o CR⁸; X⁵ y X⁶ son, cada uno, independientemente, N o CR⁸, y X⁷ es O, S, NR⁹ o CR¹⁰R¹¹, en donde al menos uno de X⁵ y X⁶ es N; R⁸, R⁹, R¹⁰, y R¹¹ son, cada uno, independientemente, hidrógeno, halógeno, alquilo C₁₋₁₂, ciano, amino, hidroxilo, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, o haloalquilo C₁₋₁₂; p es 0, 1, 2 ó 3, y cada R⁷ es independientemente halógeno, amino, hidroxilo, alquilo C₁₋₁₂, alcoxilo C₁₋₁₂, alquil C₁₋₁₂-OH, o haloalquilo C₁₋₁₂.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018085998 | 2018-05-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR117424A1 true AR117424A1 (es) | 2021-08-04 |
Family
ID=68467752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190101206A AR117424A1 (es) | 2018-05-08 | 2019-05-07 | Inhibidores de los receptores erbb |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10822334B2 (es) |
| EP (1) | EP3814341B1 (es) |
| JP (2) | JP2021523159A (es) |
| KR (1) | KR20210013071A (es) |
| CN (4) | CN112266384B (es) |
| AR (1) | AR117424A1 (es) |
| BR (1) | BR112020022829A2 (es) |
| CA (1) | CA3099315A1 (es) |
| DK (1) | DK3814341T3 (es) |
| MX (2) | MX2020011868A (es) |
| PT (1) | PT3814341T (es) |
| TW (2) | TWI811358B (es) |
| WO (1) | WO2019214634A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019196622A1 (zh) * | 2018-04-09 | 2019-10-17 | 威尚（上海）生物医药有限公司 | 具有穿过血脑屏障能力的5取代二氟哌啶化合物 |
| CN110357858B (zh) | 2018-04-09 | 2022-02-18 | 威尚（上海）生物医药有限公司 | 具有穿过血脑屏障能力的5取代二氟哌啶化合物 |
| TWI811358B (zh) * | 2018-05-08 | 2023-08-11 | 大陸商迪哲（江蘇）醫藥股份有限公司 | ＥｒｂＢ受體抑制劑 |
| AU2019341273A1 (en) | 2018-09-18 | 2020-11-19 | F. Hoffmann-La Roche Ag | Quinazoline derivatives as antitumor agents |
| AR117788A1 (es) * | 2019-01-14 | 2021-08-25 | Pi Industries Ltd | Compuestos de fenilamidina 3-sustituida, preparación y uso |
| WO2023066296A1 (en) * | 2021-10-20 | 2023-04-27 | Suzhou Zanrong Pharma Limited | Crystalline forms of quinazoline derivatives, preparation, composition and use thereof |
| CN114262327B (zh) * | 2021-12-30 | 2023-01-03 | 武汉九州钰民医药科技有限公司 | 一种her2小分子抑制剂图卡替尼的制备工艺 |
| CN114671867B (zh) * | 2022-03-15 | 2023-09-19 | 上海法默生物科技有限公司 | 妥卡替尼中间体7-羟基-[1,2,4]三唑并[1,5-a]吡啶的制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003040108A1 (en) * | 2001-11-03 | 2003-05-15 | Astrazeneca Ab | Quinazoline derivatives as antitumor agents |
| GB0126433D0 (en) * | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| GB0321648D0 (en) * | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
| GB0504474D0 (en) * | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| WO2007034144A1 (en) * | 2005-09-20 | 2007-03-29 | Astrazeneca Ab | 4- (ih-indazol-s-yl-amino)-quinazoline compounds as erbb receptor tyrosine kinase inhibitors for the treatment of cancer |
| CN101273033A (zh) * | 2005-09-20 | 2008-09-24 | 阿斯利康(瑞典)有限公司 | 作为治疗癌症的erbb受体酪氨酸激酶抑制剂的4-（1h-吲哚-5-基-氨基）-喹唑啉化合物 |
| CA2632194C (en) * | 2005-11-15 | 2012-01-03 | Array Biopharma Inc. | N4-phenyl-quinazoline-4-amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases |
| TWI811358B (zh) * | 2018-05-08 | 2023-08-11 | 大陸商迪哲（江蘇）醫藥股份有限公司 | ＥｒｂＢ受體抑制劑 |
-
2019
- 2019-05-07 TW TW108115721A patent/TWI811358B/zh active
- 2019-05-07 TW TW112129260A patent/TW202344253A/zh unknown
- 2019-05-07 AR ARP190101206A patent/AR117424A1/es unknown
- 2019-05-08 WO PCT/CN2019/085949 patent/WO2019214634A1/en unknown
- 2019-05-08 DK DK19800509.2T patent/DK3814341T3/da active
- 2019-05-08 MX MX2020011868A patent/MX2020011868A/es unknown
- 2019-05-08 JP JP2020562751A patent/JP2021523159A/ja active Pending
- 2019-05-08 CA CA3099315A patent/CA3099315A1/en active Pending
- 2019-05-08 CN CN202010657663.6A patent/CN112266384B/zh active Active
- 2019-05-08 PT PT198005092T patent/PT3814341T/pt unknown
- 2019-05-08 EP EP19800509.2A patent/EP3814341B1/en active Active
- 2019-05-08 BR BR112020022829-0A patent/BR112020022829A2/pt unknown
- 2019-05-08 CN CN201980006431.XA patent/CN111587248A/zh active Pending
- 2019-05-08 CN CN202010657654.7A patent/CN111662289A/zh active Pending
- 2019-05-08 CN CN202010656946.9A patent/CN111747953B/zh active Active
- 2019-05-08 KR KR1020207034917A patent/KR20210013071A/ko not_active Application Discontinuation
-
2020
- 2020-06-24 US US16/910,267 patent/US10822334B2/en active Active
- 2020-09-23 US US17/029,074 patent/US11447492B2/en active Active
- 2020-11-06 MX MX2023008954A patent/MX2023008954A/es unknown
-
2024
- 2024-01-22 JP JP2024007265A patent/JP2024050653A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| MX2020011868A (es) | 2021-02-26 |
| CN111662289A (zh) | 2020-09-15 |
| EP3814341A4 (en) | 2022-01-05 |
| CN111747953A (zh) | 2020-10-09 |
| MX2023008954A (es) | 2023-08-18 |
| EP3814341A1 (en) | 2021-05-05 |
| KR20210013071A (ko) | 2021-02-03 |
| US11447492B2 (en) | 2022-09-20 |
| DK3814341T3 (da) | 2024-04-22 |
| AU2019267959A1 (en) | 2020-11-26 |
| WO2019214634A1 (en) | 2019-11-14 |
| US10822334B2 (en) | 2020-11-03 |
| US20210009587A1 (en) | 2021-01-14 |
| TW202344253A (zh) | 2023-11-16 |
| CN111587248A (zh) | 2020-08-25 |
| CN112266384B (zh) | 2022-09-23 |
| US20200317669A1 (en) | 2020-10-08 |
| JP2021523159A (ja) | 2021-09-02 |
| PT3814341T (pt) | 2024-04-11 |
| EP3814341B1 (en) | 2024-03-20 |
| CN111747953B (zh) | 2021-05-07 |
| TW202015690A (zh) | 2020-05-01 |
| TWI811358B (zh) | 2023-08-11 |
| JP2024050653A (ja) | 2024-04-10 |
| CN112266384A (zh) | 2021-01-26 |
| BR112020022829A2 (pt) | 2021-02-02 |
| CA3099315A1 (en) | 2019-11-14 |
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