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
- 108060006698 EGF receptor Proteins 0.000 title 1
- 102000001301 EGF receptor Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 C1−12 alkyl-OH Chemical group 0.000 abstract 10
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 7
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 abstract 2
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 abstract 2
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (15)
| Country | Link |
|---|---|
| US (2) | US10822334B2 (es) |
| EP (2) | EP3814341B1 (es) |
| JP (1) | JP7540953B2 (es) |
| KR (1) | KR102806778B1 (es) |
| CN (4) | CN111587248A (es) |
| AR (1) | AR117424A1 (es) |
| AU (1) | AU2019267959B2 (es) |
| BR (1) | BR112020022829A2 (es) |
| CA (1) | CA3099315A1 (es) |
| DK (1) | DK3814341T3 (es) |
| ES (1) | ES2977196T3 (es) |
| MX (2) | MX2020011868A (es) |
| PT (1) | PT3814341T (es) |
| TW (2) | TWI858848B (es) |
| WO (1) | WO2019214634A1 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP3778589B1 (en) * | 2018-04-09 | 2022-05-11 | Weishang (Shanghai) Bio-Pharmaceutical Co., Ltd. | 5-substituted difluoropiperidine compound capable of passing through blood-brain barrier |
| AR117424A1 (es) * | 2018-05-08 | 2021-08-04 | Dizal Jiangsu Pharmaceutical Co Ltd | Inhibidores de los receptores erbb |
| JP7546550B2 (ja) | 2018-09-18 | 2024-09-06 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 抗腫瘍剤としてのキナゾリン誘導体 |
| AR117788A1 (es) * | 2019-01-14 | 2021-08-25 | Pi Industries Ltd | Compuestos de fenilamidina 3-sustituida, preparación y uso |
| TWI879751B (zh) * | 2020-03-23 | 2025-04-11 | 印度商皮埃企業有限公司 | 3-被取代的苯基脒化合物及其製備和用途 |
| AU2021357081A1 (en) * | 2020-10-05 | 2023-06-01 | Dana-Farber Cancer Institute, Inc | Potent and selective inhibitors of her2 |
| MX2023012060A (es) | 2021-04-13 | 2024-01-22 | Nuvalent Inc | Heterociclos con sustitucion amino para tratar canceres con mutaciones de egfr. |
| PE20242106A1 (es) * | 2021-10-20 | 2024-10-28 | Hoffmann La Roche | Formas cristalinas de derivados de quinazolina, preparacion, composicion y uso de estas |
| 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 |
| CA3253847A1 (en) * | 2022-03-28 | 2025-07-04 | Shanghai Hengrui Pharmaceutical Co., Ltd. | HETEROCYCLIC COMPOUND CONTAINING NITROGEN, ITS PREPARATION PROCESS AND PHARMACEUTICAL USE |
| EP4578457A1 (en) | 2022-08-24 | 2025-07-02 | Toray Industries, Inc. | Pharmaceutical for treating and/or preventing cancer |
| US20240279230A1 (en) | 2022-12-22 | 2024-08-22 | Boehringer Ingelheim International Gmbh | Crystalline forms of a her2 inhibitor |
| CN116102491A (zh) * | 2023-02-17 | 2023-05-12 | 浙江晖石药业有限公司 | 一种利用连续流技术进行金属催化偶联的应用 |
| TW202446386A (zh) * | 2023-04-14 | 2024-12-01 | 大陸商迪哲（江蘇）醫藥股份有限公司 | 喹唑啉ＥｒｂＢ抑制劑的藥物形式 |
| CN116903615A (zh) * | 2023-06-21 | 2023-10-20 | 江苏丽源医药有限公司 | 一种妥卡替尼及其中间体的制备方法 |
| TW202521538A (zh) | 2023-07-28 | 2025-06-01 | 德商百靈佳殷格翰國際股份有限公司 | 製備her2抑制劑之方法 |
| CN119320383A (zh) * | 2023-09-05 | 2025-01-17 | 北京鞍石生物科技股份有限公司 | 含氮杂芳基化合物及其制备方法和应用 |
| CN117658818B (zh) * | 2023-11-03 | 2025-02-07 | 江西巍华化学有限公司 | 一种4-氟-3-硝基三氟甲苯的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5994071A (en) | 1997-04-04 | 1999-11-30 | Albany Medical College | Assessment of prostate cancer |
| GB0126433D0 (en) * | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| ATE423104T1 (de) * | 2001-11-03 | 2009-03-15 | Astrazeneca Ab | Quinazolin derivate als antitumor-mittel |
| GB0321648D0 (en) | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
| GB0504474D0 (en) | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| DE602006018331D1 (de) * | 2005-09-20 | 2010-12-30 | Astrazeneca Ab | 4-(1h-indazol-5-ylamino)chinazolinverbindungen als inhibitoren der erbb-rezeptortyrosinkinase zur behandlung von krebs |
| 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 |
| CN102887891B (zh) * | 2005-11-15 | 2016-03-09 | 阿雷生物药品公司 | N4-苯基-喹唑啉-4-胺衍生物和相关化合物 |
| AR117424A1 (es) * | 2018-05-08 | 2021-08-04 | Dizal Jiangsu Pharmaceutical Co Ltd | Inhibidores de los receptores erbb |
-
2019
- 2019-05-07 AR ARP190101206A patent/AR117424A1/es unknown
- 2019-05-07 TW TW112129260A patent/TWI858848B/zh active
- 2019-05-07 TW TW108115721A patent/TWI811358B/zh active
- 2019-05-08 MX MX2020011868A patent/MX2020011868A/es unknown
- 2019-05-08 CN CN201980006431.XA patent/CN111587248A/zh active Pending
- 2019-05-08 PT PT198005092T patent/PT3814341T/pt unknown
- 2019-05-08 AU AU2019267959A patent/AU2019267959B2/en active Active
- 2019-05-08 WO PCT/CN2019/085949 patent/WO2019214634A1/en not_active Ceased
- 2019-05-08 EP EP19800509.2A patent/EP3814341B1/en active Active
- 2019-05-08 JP JP2020562751A patent/JP7540953B2/ja active Active
- 2019-05-08 KR KR1020207034917A patent/KR102806778B1/ko active Active
- 2019-05-08 ES ES19800509T patent/ES2977196T3/es active Active
- 2019-05-08 CA CA3099315A patent/CA3099315A1/en active Pending
- 2019-05-08 DK DK19800509.2T patent/DK3814341T3/da active
- 2019-05-08 EP EP24164213.1A patent/EP4410291A3/en active Pending
- 2019-05-08 BR BR112020022829-0A patent/BR112020022829A2/pt active Search and Examination
- 2019-05-08 CN CN202010656946.9A patent/CN111747953B/zh active Active
- 2019-05-08 CN CN202010657654.7A patent/CN111662289A/zh active Pending
- 2019-05-08 CN CN202010657663.6A patent/CN112266384B/zh active Active
-
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
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