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
- 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
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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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Biochemistry (AREA)
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- 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)
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| PT3515924T (pt) | 2016-09-22 | 2022-03-11 | Idorsia Pharmaceuticals Ltd | Formas cristalinas |
| US11179390B2 (en) | 2017-03-15 | 2021-11-23 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a P2Y12 receptor antagonist |
| EP4181872B1 (en) | 2020-07-15 | 2025-11-26 | Viatris Asia Pacific Pte. Ltd. | Aqueous pharmaceutical composition comprising a p2y12 receptor antagonist |
| 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. |
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| 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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| 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 |
| DE60022508T2 (de) | 1999-06-14 | 2006-06-08 | Eli Lilly And Co., Indianapolis | Inhibitoren von serin proteasen |
| US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| ES2348942T3 (es) | 2002-12-11 | 2010-12-17 | Bayer Schering Pharma Aktiengesellschaft | Compuestos de 2-aminocarbonil-quinolina como antagonistas del receptor plaquetario de adenosin difosfato. |
| CA2521313A1 (en) | 2003-04-09 | 2004-10-28 | Wyeth | Derivatives of 2-(8,9-dioxo-2,6-diazabicyclo(5.2.o)non-1(7)-3n-2-yl)-al kyl phosphonic acid and their use as n-methyl-d-aspartate (nmda) recetor antagonists |
| TW200640877A (en) | 2005-04-28 | 2006-12-01 | Actelion Pharmaceuticals Ltd | Pyrimidine derivatives |
| WO2007046075A1 (en) | 2005-10-21 | 2007-04-26 | 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. |
| 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 |
| MX2009011089A (es) | 2007-04-23 | 2009-10-30 | Sanofi Aventis | Derivados de quinolina-carboxamida en calidad de antagonistas de p2y12. |
| WO2009080227A2 (en) | 2007-12-26 | 2009-07-02 | Sanofi-Aventis | Pyrazole-carboxamide derivatives as p2y12 antagonists |
| WO2009080226A2 (en) | 2007-12-26 | 2009-07-02 | Sanofis-Aventis | Heterocyclic pyrazole-carboxamides 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 |
| MA33260B1 (fr) | 2009-04-08 | 2012-05-02 | Actelion Pharmaceuticals Ltd | 6-(3-azabicyclo[3.1.0.]hex-3-yl)-2-phenylpyrimidines |
| SG175297A1 (en) | 2009-04-22 | 2011-12-29 | Actelion Pharmaceuticals Ltd | Thiazole derivatives and their use as p2y12 receptor antagonists |
| PT3515924T (pt) | 2016-09-22 | 2022-03-11 | Idorsia Pharmaceuticals Ltd | Formas cristalinas |
| US11179390B2 (en) | 2017-03-15 | 2021-11-23 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a P2Y12 receptor antagonist |
| EP4181872B1 (en) | 2020-07-15 | 2025-11-26 | Viatris Asia Pacific Pte. Ltd. | Aqueous pharmaceutical composition comprising a p2y12 receptor antagonist |
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2017
- 2017-09-21 PT PT177714367T patent/PT3515924T/pt unknown
- 2017-09-21 WO PCT/EP2017/073858 patent/WO2018055016A1/en not_active Ceased
- 2017-09-21 HU HUE17771436A patent/HUE057772T2/hu unknown
- 2017-09-21 PL PL17771436T patent/PL3515924T3/pl unknown
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- 2017-09-21 CN CN201780057793.2A patent/CN109715639B/zh active Active
- 2017-09-21 UA UAA201903751A patent/UA124073C2/uk unknown
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- 2017-09-21 EP EP17771436.7A patent/EP3515924B1/en active Active
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- 2017-09-21 EP EP21206477.8A patent/EP3981774A1/en not_active Withdrawn
- 2017-09-21 MY MYPI2019001474A patent/MY193080A/en unknown
- 2017-09-21 ES ES17771436T patent/ES2908572T3/es active Active
- 2017-09-21 JP JP2019536696A patent/JP7097369B2/ja active Active
- 2017-09-21 LT LTEPPCT/EP2017/073858T patent/LT3515924T/lt unknown
- 2017-09-21 IL IL265445A patent/IL265445B2/en unknown
- 2017-09-21 US US16/335,973 patent/US10730896B2/en active Active
- 2017-09-21 DK DK17771436.7T patent/DK3515924T3/da 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
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- 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 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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