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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Images
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- 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
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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
-
- 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)
- 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)
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| UA (1) | UA124073C2 (enExample) |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE057772T2 (hu) | 2016-09-22 | 2022-06-28 | Idorsia Pharmaceuticals Ltd | Kristályos formák |
| MA49887A (fr) | 2017-03-15 | 2020-06-24 | Idorsia Pharmaceuticals Ltd | Administration sous-cutanée d'un antagoniste du récepteur p2y12 |
| JP7490881B2 (ja) | 2020-07-15 | 2024-05-27 | イドルシア・ファーマシューティカルズ・リミテッド | Ｐ２ｙ１２受容体アンタゴニストを有する水性医薬組成物 |
| KR20240033005A (ko) | 2021-07-13 | 2024-03-12 | 이도르시아 파마슈티컬스 리미티드 | 4-((r)-2-｛[6-((s)-3-메톡시-피롤리딘-1-일)-2-페닐-피리미딘-4-카르보닐]-아미노｝-3-포스포노-프로피오닐)-피페라진-1-카르복실산부틸 에스테르의 합성 방법 |
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 |
| ATE303988T1 (de) | 1999-06-14 | 2005-09-15 | Lilly Co Eli | Inhibitoren von serin proteasen |
| US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| PL377053A1 (pl) | 2002-12-11 | 2006-01-23 | Schering Aktiengesellschaft | Związki 2-aminokarbonylo-chinoliny jako antagonisty receptora płytkowego difosforanu adenozyny |
| JP4621659B2 (ja) | 2003-04-09 | 2011-01-26 | ワイス・エルエルシー | ［２−（８，９−ジオキソ−２，６−ジアザビシクロ［５．２．０］ノナ−１（７）−エン−２−イル）アルキル］ホスホン酸の誘導体およびｎ−メチル−ｄ−アスパルテート（ｎｍｄａ）受容体アンタゴニストとしてのその使用 |
| TW200640877A (en) | 2005-04-28 | 2006-12-01 | Actelion Pharmaceuticals Ltd | Pyrimidine derivatives |
| NZ568335A (en) | 2005-10-21 | 2011-07-29 | 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 |
| EP2148871A1 (en) | 2007-04-23 | 2010-02-03 | Sanofi-Aventis | Quinoline-carboxamide derivatives as p2y12 antagonists |
| EP2238127B1 (en) | 2007-12-26 | 2012-08-15 | Sanofi | Pyrazole-carboxamide derivatives as p2y12 antagonists |
| JP5504171B2 (ja) | 2007-12-26 | 2014-05-28 | サノフイ | Ｐ２ｙ１２アンタゴニストとしてのヘテロサイクリックピラゾール−カルボキサミド |
| 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 |
| CN102369197B (zh) | 2009-04-08 | 2013-11-06 | 埃科特莱茵药品有限公司 | 作为adp受体拮抗剂的6-(3-氮杂-二环[3.1.0]己-3-基)-2-苯基-嘧啶 |
| CA2756654C (en) | 2009-04-22 | 2017-08-22 | Actelion Pharmaceuticals Ltd | Thiazole derivatives and their use as p2y12 receptor antagonists |
| HUE057772T2 (hu) | 2016-09-22 | 2022-06-28 | Idorsia Pharmaceuticals Ltd | Kristályos formák |
| MA49887A (fr) | 2017-03-15 | 2020-06-24 | Idorsia Pharmaceuticals Ltd | Administration sous-cutanée d'un antagoniste du récepteur p2y12 |
| JP7490881B2 (ja) | 2020-07-15 | 2024-05-27 | イドルシア・ファーマシューティカルズ・リミテッド | Ｐ２ｙ１２受容体アンタゴニストを有する水性医薬組成物 |
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2017
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- 2017-09-21 PH PH1/2019/500567A patent/PH12019500567B1/en unknown
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- 2017-09-21 AU AU2017331930A patent/AU2017331930B2/en active 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 KR KR1020197011330A patent/KR102552795B1/ko active Active
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- 2017-09-21 TW TW106132387A patent/TWI752086B/zh active
- 2017-09-21 JP JP2019536696A patent/JP7097369B2/ja active Active
- 2017-09-21 PT PT177714367T patent/PT3515924T/pt unknown
- 2017-09-21 CA CA3037794A patent/CA3037794A1/en active Pending
- 2017-09-21 RS RS20220163A patent/RS62946B1/sr unknown
- 2017-09-21 EP EP17771436.7A patent/EP3515924B1/en active Active
- 2017-09-21 DK DK17771436.7T patent/DK3515924T3/da active
- 2017-09-21 PL PL17771436T patent/PL3515924T3/pl unknown
- 2017-09-21 ES ES17771436T patent/ES2908572T3/es active Active
- 2017-09-21 EA EA201990723A patent/EA201990723A1/ru unknown
- 2017-09-21 LT LTEPPCT/EP2017/073858T patent/LT3515924T/lt unknown
- 2017-09-21 EP EP21206477.8A patent/EP3981774A1/en not_active Withdrawn
- 2017-09-21 MA MA46266A patent/MA46266B1/fr unknown
- 2017-09-21 CN CN201780057793.2A patent/CN109715639B/zh active Active
- 2017-09-21 MX MX2019003093A patent/MX381590B/es unknown
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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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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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