JP2021506920A - 結晶性の置換シクロヘキシルピラゾロ[1,5−a]ピリミジニルカルボキサミド化合物およびその治療的使用 - Google Patents
結晶性の置換シクロヘキシルピラゾロ[1,5−a]ピリミジニルカルボキサミド化合物およびその治療的使用 Download PDFInfo
- Publication number
- JP2021506920A JP2021506920A JP2020534456A JP2020534456A JP2021506920A JP 2021506920 A JP2021506920 A JP 2021506920A JP 2020534456 A JP2020534456 A JP 2020534456A JP 2020534456 A JP2020534456 A JP 2020534456A JP 2021506920 A JP2021506920 A JP 2021506920A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- crystalline
- viii
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- HZILSILAELSWKN-QAQDUYKDSA-N CCCCCO[C@H](CC1)CC[C@@H]1NC(c1c2nc(C)cc(C)[n]2nc1)=O Chemical compound CCCCCO[C@H](CC1)CC[C@@H]1NC(c1c2nc(C)cc(C)[n]2nc1)=O HZILSILAELSWKN-QAQDUYKDSA-N 0.000 description 5
- AAUSQWMVOMYKMF-SOAUALDESA-N CCCCCO[C@H](CC1)CC[C@@H]1N(Cc1ccccc1)Cc1ccccc1 Chemical compound CCCCCO[C@H](CC1)CC[C@@H]1N(Cc1ccccc1)Cc1ccccc1 AAUSQWMVOMYKMF-SOAUALDESA-N 0.000 description 3
- MOULDBOONNJCBF-XYPYZODXSA-N CCCCCO[C@H](CC1)CC[C@@H]1N Chemical compound CCCCCO[C@H](CC1)CC[C@@H]1N MOULDBOONNJCBF-XYPYZODXSA-N 0.000 description 1
- UWWGTDIBDPROEH-UHFFFAOYSA-N Cc([n]1nc2)cc(C)nc1c2C(O)=O Chemical compound Cc([n]1nc2)cc(C)nc1c2C(O)=O UWWGTDIBDPROEH-UHFFFAOYSA-N 0.000 description 1
Images
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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024002729A JP2024050607A (ja) | 2017-12-21 | 2024-01-11 | 結晶性の置換シクロヘキシルピラゾロ[1,5-a]ピリミジニルカルボキサミド化合物およびその治療的使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762608652P | 2017-12-21 | 2017-12-21 | |
| US62/608,652 | 2017-12-21 | ||
| PCT/US2018/067330 WO2019126776A1 (en) | 2017-12-21 | 2018-12-21 | Crystalline substituted cyclohexyl pyrazolo[1,5-a]pyrimidinyl carboxamide compound and therapeutic uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024002729A Division JP2024050607A (ja) | 2017-12-21 | 2024-01-11 | 結晶性の置換シクロヘキシルピラゾロ[1,5-a]ピリミジニルカルボキサミド化合物およびその治療的使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021506920A true JP2021506920A (ja) | 2021-02-22 |
| JP2021506920A5 JP2021506920A5 (https=) | 2022-09-22 |
| JPWO2019126776A5 JPWO2019126776A5 (https=) | 2022-09-22 |
Family
ID=65139206
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020534456A Pending JP2021506920A (ja) | 2017-12-21 | 2018-12-21 | 結晶性の置換シクロヘキシルピラゾロ[1,5−a]ピリミジニルカルボキサミド化合物およびその治療的使用 |
| JP2024002729A Pending JP2024050607A (ja) | 2017-12-21 | 2024-01-11 | 結晶性の置換シクロヘキシルピラゾロ[1,5-a]ピリミジニルカルボキサミド化合物およびその治療的使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024002729A Pending JP2024050607A (ja) | 2017-12-21 | 2024-01-11 | 結晶性の置換シクロヘキシルピラゾロ[1,5-a]ピリミジニルカルボキサミド化合物およびその治療的使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20200339587A1 (https=) |
| EP (1) | EP3728265A1 (https=) |
| JP (2) | JP2021506920A (https=) |
| WO (1) | WO2019126776A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015342883B2 (en) | 2014-11-06 | 2020-07-02 | Bial - R&D Investments, S.A. | Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders |
| HRP20240644T1 (hr) | 2014-11-06 | 2024-08-02 | Bial-R&D Investments, S.A. | Supstituirani pirazolo(1,5-a)pirimidini i njihova uporaba u liječenju medicinskih poremećaja |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US11192892B2 (en) | 2016-04-06 | 2021-12-07 | Bial—R&D Investments, S.A. | Substituted pyrazolo[1,5-a]pyrimidines for the treatment of medical disorders |
| EP3440081A4 (en) | 2016-04-06 | 2019-09-18 | Lysosomal Therapeutics Inc. | PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER |
| SG11201809693SA (en) | 2016-05-05 | 2018-11-29 | Lysosomal Therapeutics Inc | SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| EP3452455A4 (en) | 2016-05-05 | 2019-11-13 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO [1,2-] PYRIDINES, SUBSTITUTED IMIDAZO [1,2-] PYRAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF ILLNESSES |
| IL323027A (en) | 2023-03-01 | 2025-10-01 | Bial – R& D Invest S A | Formulation |
| EP4676488A1 (en) | 2023-03-10 | 2026-01-14 | Bial-R&D Investments, S.A. | Treatment of parkinson's disease in a patient using a glucocerebrosidase activator |
| WO2025198486A1 (en) | 2024-03-22 | 2025-09-25 | BIAL – R&D Investments, S.A. | Process for preparing a pyrazolo[1,5-a]pyrimidinyl carboxamide compound |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003519698A (ja) * | 2000-01-07 | 2003-06-24 | トランスフォーム ファーマスーティカルズ,インコーポレイテッド | 多様な固体形態のハイスループットでの形成、同定および分析 |
| JP2017533968A (ja) * | 2014-11-06 | 2017-11-16 | リソソーマル・セラピューティクス・インコーポレイテッドLysosomal Therapeutics Inc. | 置換ピラゾロ[1,5−a]ピリミジンおよび医療疾患の治療におけるその使用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2594562B1 (en) | 2007-05-31 | 2016-07-20 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitors |
| CA2731685A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| EP3078373A1 (en) | 2008-10-03 | 2016-10-12 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitor |
| WO2010091164A1 (en) | 2009-02-06 | 2010-08-12 | Exelixis, Inc. | Inhibitors of glucosylceramide synthase |
| WO2011133915A1 (en) | 2010-04-23 | 2011-10-27 | Isis Pharmaceuticals, Inc. | Modulation of glucosylceramide synthase (gcs) expression |
| AU2012231275A1 (en) | 2011-03-18 | 2013-10-17 | Genzyme Corporation | Glucosylceramide synthase inhibitors |
| WO2013059119A1 (en) | 2011-10-17 | 2013-04-25 | The Regents Of The University Of Michigan | Glucosylceramide synthase inhibitors and therapeutic methods using the same |
| MA37975B2 (fr) | 2012-09-11 | 2021-03-31 | Genzyme Corp | Inhibiteurs de synthase de glucosylcéramide |
| TWI649317B (zh) | 2013-03-15 | 2019-02-01 | 健臻公司 | 製備葡糖基神經醯胺合成酶抑制劑之方法 |
| PT3079695T (pt) | 2013-12-11 | 2021-05-04 | Genzyme Corp | Inibidores de glicosilceramida-sintase |
| WO2015173169A1 (en) | 2014-05-12 | 2015-11-19 | Fondazione Istituto Italiano Di Tecnologia | Substituted benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments |
| WO2015173168A1 (en) | 2014-05-12 | 2015-11-19 | Fondazione Istituto Italiano Di Tecnologia | Benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments |
-
2018
- 2018-12-21 JP JP2020534456A patent/JP2021506920A/ja active Pending
- 2018-12-21 WO PCT/US2018/067330 patent/WO2019126776A1/en not_active Ceased
- 2018-12-21 EP EP18837065.4A patent/EP3728265A1/en active Pending
- 2018-12-21 US US16/955,589 patent/US20200339587A1/en not_active Abandoned
-
2024
- 2024-01-11 JP JP2024002729A patent/JP2024050607A/ja active Pending
- 2024-12-12 US US18/979,274 patent/US20250340558A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003519698A (ja) * | 2000-01-07 | 2003-06-24 | トランスフォーム ファーマスーティカルズ,インコーポレイテッド | 多様な固体形態のハイスループットでの形成、同定および分析 |
| JP2017533968A (ja) * | 2014-11-06 | 2017-11-16 | リソソーマル・セラピューティクス・インコーポレイテッドLysosomal Therapeutics Inc. | 置換ピラゾロ[1,5−a]ピリミジンおよび医療疾患の治療におけるその使用 |
Non-Patent Citations (4)
| Title |
|---|
| ""新医薬品の規格及び試験方法の設定について"", 医薬審発第568号, JPN6010021254, 1 May 2001 (2001-05-01), ISSN: 0005313817 * |
| 山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, vol. 65, no. 9, JPN6010003277, 1 September 2007 (2007-09-01), pages 907 - 69, ISSN: 0005313819 * |
| 川口洋子ら: "医薬品と結晶多形", 生活工学研究, vol. 4, no. 2, JPN6014015069, 2002, pages 310 - 317, ISSN: 0005313816 * |
| 高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005313818 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2019126776A1 (en) | 2019-06-27 |
| US20200339587A1 (en) | 2020-10-29 |
| EP3728265A1 (en) | 2020-10-28 |
| US20250340558A1 (en) | 2025-11-06 |
| JP2024050607A (ja) | 2024-04-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2021506920A (ja) | 結晶性の置換シクロヘキシルピラゾロ[1,5−a]ピリミジニルカルボキサミド化合物およびその治療的使用 | |
| JP7519221B2 (ja) | 置換ピラゾロ[1,5-a]ピリミジンおよび医療疾患の治療におけるその使用 | |
| EP2477991B1 (en) | Process for preparing azabicyclic compounds | |
| US9682987B2 (en) | Solid forms of an antiviral compound | |
| UA80018C2 (en) | Alpha-2-delta-proteins related aminoacids | |
| US7098364B2 (en) | Phenylethanolamine compounds as β2-receptor agonists, and methods of use and preparation thereof | |
| EP1650186B1 (en) | Novel dicarboxylic acid derivatives | |
| WO2023091565A1 (en) | Nsd2-targeted chemical degraders and compositions and methods of use thereof | |
| JPWO1999031045A1 (ja) | フェニルアミノアルキルカルボン酸誘導体およびそれを含有する医薬組成物 | |
| TW202412741A (zh) | 一種製備2-羥乙基胺基己酸酯類化合物方法及其應用 | |
| JPH07500604A (ja) | 高血圧治療用エチルアラニンアミノジオール化合物 | |
| CN119110795A (zh) | 用于治疗与lpa受体活性相关的病症的化合物和组合物 | |
| CN104781244A (zh) | 用于制备(1s,4s,5s)-4-溴-6-氧杂二环[3.2.1]辛烷-7-酮的方法 | |
| WO2015101294A1 (zh) | 镇痛活性化合物及其医药用途 | |
| WO2019042443A1 (zh) | 一类具有降解酪氨酸蛋白激酶jak3活性的化合物 | |
| EP4139290A1 (en) | Antiviral 1,3-di-oxo-indene compounds | |
| DE60021859T2 (de) | 1, 2, 3, 4-tetrahydro-1-naphthalenamin verbindungen zur therapeutsichen verwendung | |
| CA2551128A1 (en) | Catalytic hydrogenation of nitriles to produce capsaicinoid derivatives and amine compounds, and methods for purifiying and obtaining the polymorphs thereof | |
| WO2025198486A1 (en) | Process for preparing a pyrazolo[1,5-a]pyrimidinyl carboxamide compound | |
| KR20230107808A (ko) | 신규한 글루타민 유사체 | |
| CN109280028B (zh) | 喹啉类化合物及其在dpp-4酶抑制剂的应用 | |
| CN114920697A (zh) | 杂环基取代的茚满丙酰胺类化合物及其应用 | |
| Takahashi et al. | 19, United States i, Patent Application Publication | |
| HK40041775B (zh) | 三氮唑类化合物及其制备方法与用途 | |
| WO1997003968A1 (en) | 4a-ARYLDECAHYDROISOQUINOLINE COMPOUNDS AND MEDICINAL USES THEREOF |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20211220 |
|
| A711 | Notification of change in applicant |
Free format text: JAPANESE INTERMEDIATE CODE: A711 Effective date: 20220805 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220819 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20221226 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20230110 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20230404 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20230605 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20230707 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20230912 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20240111 |
|
| A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20240226 |
|
| A912 | Re-examination (zenchi) completed and case transferred to appeal board |
Free format text: JAPANESE INTERMEDIATE CODE: A912 Effective date: 20240502 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20260123 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20260227 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20260330 |