TWI752086B - 結晶型式 - Google Patents
結晶型式 Download PDFInfo
- Publication number
- TWI752086B TWI752086B TW106132387A TW106132387A TWI752086B TW I752086 B TWI752086 B TW I752086B TW 106132387 A TW106132387 A TW 106132387A TW 106132387 A TW106132387 A TW 106132387A TW I752086 B TWI752086 B TW I752086B
- Authority
- TW
- Taiwan
- Prior art keywords
- crystalline form
- compound
- propionyl
- hexahydropyrazine
- pyrrolidin
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 29
- 238000000034 method Methods 0.000 claims abstract description 23
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- C07—ORGANIC CHEMISTRY
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- 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
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- 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
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- 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
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- 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
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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
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Bioinformatics & Cheminformatics (AREA)
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- Animal Behavior & Ethology (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
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- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
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| Publication number | Priority date | Publication date | Assignee | Title |
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| UA124073C2 (uk) | 2016-09-22 | 2021-07-14 | Ідорсія Фармасьютікалз Лтд | Кристалічні форми гідрохлориду складного бутилового ефіру 4-((r)-2-{[6-((s)-3-метоксипіролідин-1-іл)-2-фенілпіримідин-4-карбоніл]-аміно}-3-фосфонопропіоніл)-піперазин-1-карбонової кислоти |
| MY205605A (en) | 2017-03-15 | 2024-10-29 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a p2y12 receptor antagonist |
| MX2023000601A (es) | 2020-07-15 | 2023-02-13 | Idorsia Pharmaceuticals Ltd | Composicion farmaceutica acuosa que comprende un antagonista del receptor p2y12. |
| MX2024000653A (es) | 2021-07-13 | 2024-01-31 | Idorsia Pharmaceuticals Ltd | Un proceso para la sintesis de ester de butilo de acido 4-((r)-2-{[6-((s)-3-metoxi-pirrolidin-1-il)-2-fenil-pirimidin-4-c arbonil]-amino}-3-fosfono-propionil)-piperazin-1-carboxilico. |
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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| CA2375920A1 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Compounds |
| US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| CN1747732A (zh) | 2002-12-11 | 2006-03-15 | 舍林股份公司 | 作为血小板腺苷二磷酸受体拮抗剂的2－氨基羰基喹啉化合物 |
| PL1611144T3 (pl) | 2003-04-09 | 2011-03-31 | Wyeth Llc | Pochodne kwasu 2-(8,9-diokso-2,6-diazabicyklo(5.2.0)non-1(7)-en-2-ylo)alkilofosfonowego i ich zastosowanie jako antagonistów receptora N-metylo-D-asparaginianu (NMDA) |
| TW200640877A (en) | 2005-04-28 | 2006-12-01 | Actelion Pharmaceuticals Ltd | Pyrimidine derivatives |
| EP1940814B1 (en) | 2005-10-21 | 2013-05-22 | Actelion Pharmaceuticals Ltd. | Piperazine derivatives as antimalarial agents |
| 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. |
| CL2007003038A1 (es) | 2006-10-25 | 2008-06-06 | Actelion Pharmaceuticals Ltd | Compuestos derivados de 2-fenil-6-aminocarbonil-pirimidina; composicion farmaceutica; y uso en el tratamiento de trastornos vasculares oclusivos. |
| JP4785881B2 (ja) | 2007-02-27 | 2011-10-05 | 大塚製薬株式会社 | 医薬 |
| CA2684644A1 (en) | 2007-04-23 | 2008-10-30 | Sanofi-Aventis | Quinoline-carboxamide derivatives as p2y12 antagonists |
| WO2009080226A2 (en) | 2007-12-26 | 2009-07-02 | Sanofis-Aventis | Heterocyclic pyrazole-carboxamides as p2y12 antagonists |
| WO2009080227A2 (en) | 2007-12-26 | 2009-07-02 | Sanofi-Aventis | Pyrazole-carboxamide derivatives as p2y12 antagonists |
| AR071653A1 (es) | 2008-04-11 | 2010-07-07 | Actelion Pharmaceuticals Ltd | Derivados 2-fenil-4-ciclopropil-pirimidina |
| AR071652A1 (es) | 2008-04-11 | 2010-07-07 | Actelion Pharmaceuticals Ltd | Derivados 2- fenil-piridina substituidos |
| AU2010233378A1 (en) | 2009-04-08 | 2011-11-24 | Actelion Pharmaceuticals Ltd. | 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidines as ADP receptor antagonists |
| BRPI1015145A2 (pt) | 2009-04-22 | 2018-01-30 | Actelion Pharmaceuticals Ltd | derivados de tiazol e seu uso como receptores antagonistas de p2y12 |
| UA124073C2 (uk) | 2016-09-22 | 2021-07-14 | Ідорсія Фармасьютікалз Лтд | Кристалічні форми гідрохлориду складного бутилового ефіру 4-((r)-2-{[6-((s)-3-метоксипіролідин-1-іл)-2-фенілпіримідин-4-карбоніл]-аміно}-3-фосфонопропіоніл)-піперазин-1-карбонової кислоти |
| MY205605A (en) | 2017-03-15 | 2024-10-29 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a p2y12 receptor antagonist |
| MX2023000601A (es) | 2020-07-15 | 2023-02-13 | Idorsia Pharmaceuticals Ltd | Composicion farmaceutica acuosa que comprende un antagonista del receptor p2y12. |
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2017
- 2017-09-21 UA UAA201903751A patent/UA124073C2/uk unknown
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- 2017-09-21 DK DK17771436.7T patent/DK3515924T3/da active
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- 2017-09-21 TW TW106132387A patent/TWI752086B/zh active
- 2017-09-21 PL PL17771436T patent/PL3515924T3/pl unknown
- 2017-09-21 US US16/335,973 patent/US10730896B2/en active Active
- 2017-09-21 PT PT177714367T patent/PT3515924T/pt unknown
- 2017-09-21 EA EA201990723A patent/EA201990723A1/ru unknown
- 2017-09-21 LT LTEPPCT/EP2017/073858T patent/LT3515924T/lt unknown
- 2017-09-21 PH PH1/2019/500567A patent/PH12019500567B1/en unknown
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- 2017-09-21 KR KR1020197011330A patent/KR102552795B1/ko active Active
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2019
- 2019-03-21 CL CL2019000728A patent/CL2019000728A1/es unknown
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2020
- 2020-07-24 US US16/938,730 patent/US11365209B2/en active Active
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2022
- 2022-03-09 CY CY20221100195T patent/CY1125052T1/el unknown
- 2022-05-10 US US17/741,427 patent/US12227532B2/en active Active
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2025
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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 the Rat Than Clopidogrel,Journal of Medicinal Chemistry,Vol.58,no.23,10 Dec.2015,p.A〜U * |
| 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 the Rat Than Clopidogrel,Journal of Medicinal Chemistry,Vol.58,no.23,10 Dec.2015,p.A〜U。 |
| A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475):Tolerability,Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial, Clin Drug Investig (2014) 34:807–818 * |
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