CN109715639B - 结晶形式 - Google Patents
结晶形式 Download PDFInfo
- Publication number
- CN109715639B CN109715639B CN201780057793.2A CN201780057793A CN109715639B CN 109715639 B CN109715639 B CN 109715639B CN 201780057793 A CN201780057793 A CN 201780057793A CN 109715639 B CN109715639 B CN 109715639B
- Authority
- CN
- China
- Prior art keywords
- crystalline form
- compound
- piperazine
- propionyl
- amino
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2016072562 | 2016-09-22 | ||
| EPPCT/EP2016/072562 | 2016-09-22 | ||
| PCT/EP2017/073858 WO2018055016A1 (en) | 2016-09-22 | 2017-09-21 | Crystalline forms |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109715639A CN109715639A (zh) | 2019-05-03 |
| CN109715639B true CN109715639B (zh) | 2022-04-19 |
Family
ID=59923448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780057793.2A Active CN109715639B (zh) | 2016-09-22 | 2017-09-21 | 结晶形式 |
Country Status (27)
| Country | Link |
|---|---|
| US (4) | US10730896B2 (enExample) |
| EP (2) | EP3515924B1 (enExample) |
| JP (1) | JP7097369B2 (enExample) |
| KR (1) | KR102552795B1 (enExample) |
| CN (1) | CN109715639B (enExample) |
| AU (1) | AU2017331930B2 (enExample) |
| CA (1) | CA3037794A1 (enExample) |
| CL (1) | CL2019000728A1 (enExample) |
| CY (1) | CY1125052T1 (enExample) |
| DK (1) | DK3515924T3 (enExample) |
| EA (1) | EA201990723A1 (enExample) |
| ES (1) | ES2908572T3 (enExample) |
| HR (1) | HRP20220234T1 (enExample) |
| HU (1) | HUE057772T2 (enExample) |
| IL (1) | IL265445B2 (enExample) |
| LT (1) | LT3515924T (enExample) |
| MA (1) | MA46266B1 (enExample) |
| MX (1) | MX381590B (enExample) |
| MY (1) | MY193080A (enExample) |
| PH (1) | PH12019500567B1 (enExample) |
| PL (1) | PL3515924T3 (enExample) |
| PT (1) | PT3515924T (enExample) |
| RS (1) | RS62946B1 (enExample) |
| SI (1) | SI3515924T1 (enExample) |
| TW (1) | TWI752086B (enExample) |
| UA (1) | UA124073C2 (enExample) |
| WO (1) | WO2018055016A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3515924T3 (da) | 2016-09-22 | 2022-03-21 | Idorsia Pharmaceuticals Ltd | Krystallinske former |
| SG11201908128YA (en) | 2017-03-15 | 2019-10-30 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a p2y12 receptor antagonist |
| RS67649B1 (sr) | 2020-07-15 | 2026-02-27 | Viatris Asia Pacific Pte Ltd | Vodena farmaceutska kompozicija koja sadrži antagonistu p2y12 receptora |
| IL309948A (en) * | 2021-07-13 | 2024-03-01 | Idorsia Pharmaceuticals Ltd | A process for the synthesis of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidin-4-carbonyl]-amino}-3-phosphono- Propionyl)-piperazine-1-carboxylic acid butyl ester |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101868469A (zh) * | 2007-11-29 | 2010-10-20 | 埃科特莱茵药品有限公司 | 膦酸衍生物及其作为p2y12受体拮抗剂 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5373586A (en) | 1976-12-09 | 1978-06-30 | Mitsubishi Chem Ind Ltd | New penicillin derivatives |
| CA2020437A1 (en) | 1989-07-05 | 1991-01-06 | Yoshihide Fuse | Cinnamamide derivative |
| ES2248084T3 (es) | 1999-06-14 | 2006-03-16 | Eli Lilly And Company | Inhibidores de serinproteasa. |
| US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| EA200500899A1 (ru) | 2002-12-11 | 2006-02-24 | Шеринг Акциенгезельшафт | Антагонисты аденозиндифосфатного рецептора тромбоцитов |
| US7253153B2 (en) | 2003-04-09 | 2007-08-07 | Wyeth | Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and methods of use thereof |
| TW200640877A (en) | 2005-04-28 | 2006-12-01 | Actelion Pharmaceuticals Ltd | Pyrimidine derivatives |
| TWI382976B (zh) | 2005-10-21 | 2013-01-21 | Actelion Pharmaceuticals Ltd | 作為抗瘧疾劑之新穎哌 |
| CL2007002920A1 (es) | 2006-10-13 | 2008-06-06 | Actelion Pharmaceuticals Ltd | Compuestos derivados de 2-aminocarbonilpiridina; composicion farmaceutica; y uso para el tratamiento de trastornos vasculares oclusivos. |
| AR063518A1 (es) | 2006-10-25 | 2009-01-28 | Actelion Pharmaceuticals Ltd | Derivados 2-fenil-6-aminocarbonil-pirimidina; composicion farmaceutica; y su uso para tratar y/o prevenir enfermedades vasculares perifericas viscerales, hepaticas y renales, enfermedades cardiovasculares y enfermedades cerebrovasculares asociados con la agregacion de plaquetas, incluyendo trombosis |
| JP4785881B2 (ja) | 2007-02-27 | 2011-10-05 | 大塚製薬株式会社 | 医薬 |
| WO2008128647A1 (en) | 2007-04-23 | 2008-10-30 | Sanofi-Aventis | Quinoline-carboxamide derivatives as p2y12 antagonists |
| EP2238127B1 (en) | 2007-12-26 | 2012-08-15 | Sanofi | Pyrazole-carboxamide derivatives as p2y12 antagonists |
| WO2009080226A2 (en) | 2007-12-26 | 2009-07-02 | Sanofis-Aventis | Heterocyclic pyrazole-carboxamides as p2y12 antagonists |
| AR071652A1 (es) | 2008-04-11 | 2010-07-07 | Actelion Pharmaceuticals Ltd | Derivados 2- fenil-piridina substituidos |
| AR071653A1 (es) | 2008-04-11 | 2010-07-07 | Actelion Pharmaceuticals Ltd | Derivados 2-fenil-4-ciclopropil-pirimidina |
| CA2756542C (en) | 2009-04-08 | 2017-08-22 | Actelion Pharmaceuticals Ltd | 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidines |
| CA2756654C (en) | 2009-04-22 | 2017-08-22 | Actelion Pharmaceuticals Ltd | Thiazole derivatives and their use as p2y12 receptor antagonists |
| DK3515924T3 (da) | 2016-09-22 | 2022-03-21 | Idorsia Pharmaceuticals Ltd | Krystallinske former |
| SG11201908128YA (en) | 2017-03-15 | 2019-10-30 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a p2y12 receptor antagonist |
| RS67649B1 (sr) | 2020-07-15 | 2026-02-27 | Viatris Asia Pacific Pte Ltd | Vodena farmaceutska kompozicija koja sadrži antagonistu p2y12 receptora |
-
2017
- 2017-09-21 DK DK17771436.7T patent/DK3515924T3/da active
- 2017-09-21 SI SI201731102T patent/SI3515924T1/sl unknown
- 2017-09-21 IL IL265445A patent/IL265445B2/en unknown
- 2017-09-21 CN CN201780057793.2A patent/CN109715639B/zh active Active
- 2017-09-21 TW TW106132387A patent/TWI752086B/zh active
- 2017-09-21 US US16/335,973 patent/US10730896B2/en active Active
- 2017-09-21 UA UAA201903751A patent/UA124073C2/uk unknown
- 2017-09-21 AU AU2017331930A patent/AU2017331930B2/en active Active
- 2017-09-21 HR HRP20220234TT patent/HRP20220234T1/hr unknown
- 2017-09-21 WO PCT/EP2017/073858 patent/WO2018055016A1/en not_active Ceased
- 2017-09-21 KR KR1020197011330A patent/KR102552795B1/ko active Active
- 2017-09-21 EA EA201990723A patent/EA201990723A1/ru unknown
- 2017-09-21 PH PH1/2019/500567A patent/PH12019500567B1/en unknown
- 2017-09-21 HU HUE17771436A patent/HUE057772T2/hu unknown
- 2017-09-21 CA CA3037794A patent/CA3037794A1/en active Pending
- 2017-09-21 LT LTEPPCT/EP2017/073858T patent/LT3515924T/lt unknown
- 2017-09-21 MX MX2019003093A patent/MX381590B/es unknown
- 2017-09-21 MA MA46266A patent/MA46266B1/fr unknown
- 2017-09-21 PL PL17771436T patent/PL3515924T3/pl unknown
- 2017-09-21 EP EP17771436.7A patent/EP3515924B1/en active Active
- 2017-09-21 PT PT177714367T patent/PT3515924T/pt unknown
- 2017-09-21 MY MYPI2019001474A patent/MY193080A/en unknown
- 2017-09-21 JP JP2019536696A patent/JP7097369B2/ja active Active
- 2017-09-21 RS RS20220163A patent/RS62946B1/sr unknown
- 2017-09-21 EP EP21206477.8A patent/EP3981774A1/en not_active Withdrawn
- 2017-09-21 ES ES17771436T patent/ES2908572T3/es active Active
-
2019
- 2019-03-21 CL CL2019000728A patent/CL2019000728A1/es unknown
-
2020
- 2020-07-24 US US16/938,730 patent/US11365209B2/en active Active
-
2022
- 2022-03-09 CY CY20221100195T patent/CY1125052T1/el unknown
- 2022-05-10 US US17/741,427 patent/US12227532B2/en active Active
-
2025
- 2025-01-17 US US19/028,423 patent/US20250163086A1/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101868469A (zh) * | 2007-11-29 | 2010-10-20 | 埃科特莱茵药品有限公司 | 膦酸衍生物及其作为p2y12受体拮抗剂 |
Non-Patent Citations (3)
| Title |
|---|
| 4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4- carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in;Caroff, Eva et al.;《Journal of Medicinal Chemistry》;20151109;第58卷(第23期);第9133-9153页 * |
| A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial;Baldoni, Daniela et al.;《Clinical Drug Investigation》;20141021;第34卷(第11期);第807-818页 * |
| Baldoni, Daniela et al..A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial.《Clinical Drug Investigation》.2014,第34卷(第11期),第807-818页. * |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20250625 Address after: Singapore Exchange Patentee after: Huizhi Asia Pacific Private Ltd. Country or region after: Singapore Address before: Swiss A Skei Weil Patentee before: ACTELION PHARMACEUTICALS LTD. Country or region before: Switzerland |
|
| TR01 | Transfer of patent right |