IL264784B - Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide Preparation methods and its uses - Google Patents
Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide Preparation methods and its usesInfo
- Publication number
- IL264784B IL264784B IL264784A IL26478419A IL264784B IL 264784 B IL264784 B IL 264784B IL 264784 A IL264784 A IL 264784A IL 26478419 A IL26478419 A IL 26478419A IL 264784 B IL264784 B IL 264784B
- Authority
- IL
- Israel
- Prior art keywords
- crystalline form
- compound
- crystalline
- solid
- cell
- Prior art date
Links
Classifications
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016095510 | 2016-08-16 | ||
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL264784A IL264784A (enExample) | 2019-03-31 |
| IL264784B true IL264784B (en) | 2022-07-01 |
Family
ID=61197220
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL264784A IL264784B (en) | 2016-08-16 | 2017-08-15 | Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide Preparation methods and its uses |
| IL293319A IL293319B1 (en) | 2016-08-16 | 2022-05-24 | Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL293319A IL293319B1 (en) | 2016-08-16 | 2022-05-24 | Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof |
Country Status (15)
| Country | Link |
|---|---|
| US (12) | US10927117B2 (enExample) |
| EP (3) | EP4509183A3 (enExample) |
| JP (4) | JP7402685B2 (enExample) |
| KR (3) | KR20250052473A (enExample) |
| CN (3) | CN116478166A (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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| LT2989106T (lt) | 2013-04-25 | 2017-04-10 | Beigene, Ltd. | Kondensuoti heterocikliniai junginiai kaip baltymų kinazės inhibitoriai |
| EA034666B1 (ru) | 2013-09-13 | 2020-03-04 | Бейджин Свитзерланд Гмбх | Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела |
| KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| TWI865873B (zh) | 2016-08-16 | 2024-12-11 | 瑞士商百濟神州瑞士有限責任公司 | (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途 |
| FI3500299T3 (fi) | 2016-08-19 | 2024-02-14 | Beigene Switzerland Gmbh | Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa |
| EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES |
| US11597768B2 (en) | 2017-06-26 | 2023-03-07 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| 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 |
| KR20210100005A (ko) * | 2018-03-29 | 2021-08-13 | 마티 테라퓨틱스 인코포레이티드 | 안과 약제의 서방성 제형 및 건성 증후군 치료 용도 |
| 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 |
| BR112021024131A2 (pt) | 2019-05-31 | 2022-01-11 | Haisco Pharmaceuticals Pte Ltd | Derivado de anel inibidor de btk, método de preparação para o mesmo e aplicação farmacêutica do mesmo |
| 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 |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 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 |
| 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 |
| WO2020249002A1 (zh) * | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 口服胶囊剂及其制备方法 |
| 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 |
| CN110922409A (zh) * | 2019-12-19 | 2020-03-27 | 武汉九州钰民医药科技有限公司 | 制备btk抑制剂泽布替尼的方法 |
| 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 |
| CN115175678B (zh) * | 2020-02-27 | 2024-12-27 | 百济神州瑞士有限责任公司 | 使用btk抑制剂及其组合治疗dlbcl的方法 |
| 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 |
| US20250073238A1 (en) * | 2020-11-20 | 2025-03-06 | Beigene Switzerland Gmbh | Methods of treating systemic lupus erythematosus using btk inhibitors |
| US20240124461A1 (en) | 2020-12-11 | 2024-04-18 | Teva Pharmaceuticals International Gmbh | Processes for the preparation of zanubrutinib and intermediates thereof |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | 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 |
| IT202100025997A1 (it) | 2021-10-11 | 2023-04-11 | Olon Spa | Processo per la preparazione di zanubrutinib |
| 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. |
| CN118307541A (zh) * | 2023-01-09 | 2024-07-09 | 天津济坤医药科技有限公司 | 氘代吡唑并嘧啶衍生物及其制备方法和药物组合物、结合物及应用 |
| CN117430610A (zh) * | 2023-10-11 | 2024-01-23 | 宁夏医科大学 | 一种氘代稠合杂环化合物及其制备方法和应用 |
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