KR102793825B1 - (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 - Google Patents
(s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 Download PDFInfo
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- KR102793825B1 KR102793825B1 KR1020237039678A KR20237039678A KR102793825B1 KR 102793825 B1 KR102793825 B1 KR 102793825B1 KR 1020237039678 A KR1020237039678 A KR 1020237039678A KR 20237039678 A KR20237039678 A KR 20237039678A KR 102793825 B1 KR102793825 B1 KR 102793825B1
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- 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
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- 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
- C07B2200/07—Optical isomers
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020257011064A KR20250052473A (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로[1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/095510 | 2016-08-16 | ||
| CN2016095510 | 2016-08-16 | ||
| KR1020197007529A KR102604975B1 (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
| PCT/IB2017/054955 WO2018033853A2 (en) | 2016-08-16 | 2017-08-15 | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197007529A Division KR102604975B1 (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020257011064A Division KR20250052473A (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로[1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20230162137A KR20230162137A (ko) | 2023-11-28 |
| KR102793825B1 true KR102793825B1 (ko) | 2025-04-11 |
Family
ID=61197220
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020257011064A Ceased KR20250052473A (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로[1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
| KR1020237039678A Active KR102793825B1 (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
| KR1020197007529A Active KR102604975B1 (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020257011064A Ceased KR20250052473A (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로[1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197007529A Active KR102604975B1 (ko) | 2016-08-16 | 2017-08-15 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
Country Status (15)
| Country | Link |
|---|---|
| US (12) | US10927117B2 (enExample) |
| EP (3) | EP3500575B1 (enExample) |
| JP (4) | JP7402685B2 (enExample) |
| KR (3) | KR20250052473A (enExample) |
| CN (3) | CN109563099B (enExample) |
| AU (3) | AU2017314178B2 (enExample) |
| CA (1) | CA3033827A1 (enExample) |
| EA (1) | EA201990519A1 (enExample) |
| IL (2) | IL264784B (enExample) |
| MX (1) | MX384627B (enExample) |
| NZ (1) | NZ751418A (enExample) |
| SG (1) | SG11201901141WA (enExample) |
| TW (3) | TWI865873B (enExample) |
| WO (1) | WO2018033853A2 (enExample) |
| ZA (1) | ZA201900919B (enExample) |
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| CN104884458B (zh) | 2013-04-25 | 2017-04-12 | 百济神州有限公司 | 作为蛋白质激酶抑制剂的稠合杂环化合物 |
| SG11201601844TA (en) | 2013-09-13 | 2016-04-28 | Beigene Ltd | Anti-pd1 antibodies and their use as therapeutics and diagnostics |
| CN110156892B (zh) | 2014-07-03 | 2023-05-16 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
| EA201990519A1 (ru) | 2016-08-16 | 2019-08-30 | Бейджин, Лтд. | КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ |
| AU2017313085B2 (en) | 2016-08-19 | 2024-06-20 | Beone Medicines I Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
| TWI774726B (zh) | 2017-01-25 | 2022-08-21 | 英屬開曼群島商百濟神州有限公司 | (S)-7-(1-(丁-2-炔醯基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑并[1,5-a]嘧啶-3-甲醯胺的晶型、及其製備和用途 |
| TWI877099B (zh) | 2017-06-26 | 2025-03-21 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| CA3095460A1 (en) * | 2018-03-29 | 2019-10-03 | Mati Therapeutics, Inc. | Ophthalmic drug sustained release formulation and uses for dry eye syndrome treatment |
| CN111675711A (zh) * | 2019-03-11 | 2020-09-18 | 百济神州(苏州)生物科技有限公司 | Btk抑制剂化合物的单晶及其制备方法 |
| CN117820311A (zh) * | 2019-05-08 | 2024-04-05 | 百济神州(苏州)生物科技有限公司 | Btk抑制剂及其中间体的制备方法 |
| CN113544130B (zh) | 2019-05-31 | 2024-01-09 | 西藏海思科制药有限公司 | 一种btk抑制剂环衍生物及其制备方法和药学上的应用 |
| EP3981400A4 (en) * | 2019-06-10 | 2023-07-12 | BeiGene Switzerland GmbH | Oral capsule and preparation method therefor |
| CN112057432A (zh) * | 2019-06-10 | 2020-12-11 | 百济神州(苏州)生物科技有限公司 | 口服胶囊剂及其制备方法 |
| CN112057427B (zh) * | 2019-06-10 | 2024-09-03 | 百济神州(苏州)生物科技有限公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| EP3981399A4 (en) * | 2019-06-10 | 2023-05-31 | BeiGene Switzerland GmbH | ORAL SOLID TABLET WITH A TYROSINE KINAS INHIBITOR AND METHOD OF MANUFACTURE THEREOF |
| CN110563733A (zh) * | 2019-09-12 | 2019-12-13 | 安帝康(无锡)生物科技有限公司 | 作为选择性btk抑制剂的咪唑并吡嗪类化合物 |
| JP7389905B2 (ja) * | 2019-12-04 | 2023-11-30 | 河南知微生物医薬有限公司 | ブルトン型チロシンキナーゼ阻害剤としてのイミダゾールカルボキサミド誘導体 |
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| CN110845504A (zh) * | 2019-12-19 | 2020-02-28 | 武汉九州钰民医药科技有限公司 | 合成赞布替尼的新方法 |
| CN110938077B (zh) * | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
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| WO2021259732A1 (en) | 2020-06-24 | 2021-12-30 | Sandoz Ag | Multi-component compounds comprising zanubrutinib and a benzoic acid derivative |
| CN116134028A (zh) | 2020-07-07 | 2023-05-16 | 四川海思科制药有限公司 | 一种具有降解btk激酶的化合物及其制备方法和药学上的应用 |
| WO2022101939A1 (en) * | 2020-11-13 | 2022-05-19 | Msn Laboratories Private Limited, R&D Center | Novel process for the preparation of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide or its salts thereof |
| JP2023550416A (ja) * | 2020-11-20 | 2023-12-01 | ベイジーン スウィッツァーランド ゲーエムベーハー | Btk阻害剤を用いて全身性エリテマトーデスを治療する方法 |
| EP4259633A1 (en) | 2020-12-11 | 2023-10-18 | Teva Pharmaceuticals International GmbH | Processes for the preparation of zanubrutinib and intermediates thereof |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2023014817A1 (en) | 2021-08-03 | 2023-02-09 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating lymphomas with a cdk7 inhibitor in combination with a btk inhibitor |
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| IT202200009872A1 (it) * | 2022-05-12 | 2023-11-12 | Olon Spa | Processo di preparazione di Zanubrutinib in forma amorfa. |
| IT202200024192A1 (it) * | 2022-11-24 | 2024-05-24 | Olon Spa | Processo per la preparazione di Zanubrutinib. |
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