JP7097369B2 - 結晶形 - Google Patents

結晶形 Download PDF

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Publication number
JP7097369B2
JP7097369B2 JP2019536696A JP2019536696A JP7097369B2 JP 7097369 B2 JP7097369 B2 JP 7097369B2 JP 2019536696 A JP2019536696 A JP 2019536696A JP 2019536696 A JP2019536696 A JP 2019536696A JP 7097369 B2 JP7097369 B2 JP 7097369B2
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Japan
Prior art keywords
amino
butyl ester
carboxylic acid
carbonyl
methoxy
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JP2019536696A
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English (en)
Japanese (ja)
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JP2019529553A (ja
JP2019529553A5 (enExample
Inventor
ロイエンバーガー ダニエル
リーバー ステファン
フォン ラウマー マルクス
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Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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Publication of JP2019529553A5 publication Critical patent/JP2019529553A5/ja
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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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2019536696A 2016-09-22 2017-09-21 結晶形 Active JP7097369B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPPCT/EP2016/072562 2016-09-22
EP2016072562 2016-09-22
PCT/EP2017/073858 WO2018055016A1 (en) 2016-09-22 2017-09-21 Crystalline forms

Publications (3)

Publication Number Publication Date
JP2019529553A JP2019529553A (ja) 2019-10-17
JP2019529553A5 JP2019529553A5 (enExample) 2020-11-12
JP7097369B2 true JP7097369B2 (ja) 2022-07-07

Family

ID=59923448

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019536696A Active JP7097369B2 (ja) 2016-09-22 2017-09-21 結晶形

Country Status (27)

Country Link
US (4) US10730896B2 (enExample)
EP (2) EP3981774A1 (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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3981774A1 (en) 2016-09-22 2022-04-13 Idorsia Pharmaceuticals Ltd Crystalline forms
EA201992123A1 (ru) 2017-03-15 2020-02-25 Идорсия Фармасьютиклз Лтд Подкожное введение антагониста p2yрецептора
EP4181872B1 (en) 2020-07-15 2025-11-26 Viatris Asia Pacific Pte. Ltd. Aqueous pharmaceutical composition comprising a p2y12 receptor antagonist
US20240317784A1 (en) 2021-07-13 2024-09-26 Viatris Asia Pacific Pte. Ltd. Process for the synthesis of 4-((r)-2-{[6-((s)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester

Family Cites Families (22)

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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
EP1192132B1 (en) 1999-06-14 2005-09-07 Eli Lilly And Company Serine protease inhibitors
US6861424B2 (en) 2001-06-06 2005-03-01 Schering Aktiengesellschaft Platelet adenosine diphosphate receptor antagonists
EP1578423B1 (en) 2002-12-11 2010-08-18 Bayer Schering Pharma Aktiengesellschaft 2-aminocarbonyl-quinoline compounds as platelet adenosine diphosphate receptor antagonists
MXPA05010760A (es) 2003-04-09 2005-12-12 Wyeth Corp Derivados de acido 2-(8,9-dioxo-2,6-diazabiciclo[5.2.0]non-1(7)-en-2-il)alquil fosfonico y su uso como antagonistas de receptor de n-metil-d-aspartato (nmda).
TW200640877A (en) 2005-04-28 2006-12-01 Actelion Pharmaceuticals Ltd Pyrimidine derivatives
JP5164847B2 (ja) 2005-10-21 2013-03-21 アクテリオン ファーマシューティカルズ リミテッド 抗マラリア薬としての新規のピペラジン
AR063258A1 (es) 2006-10-13 2009-01-14 Actelion Pharmaceuticals Ltd Derivados de 2-aminocarbonil-piridina, una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento 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
MY153427A (en) 2007-04-23 2015-02-13 Sanofi Aventis Quinoline-carboxamide derivatives as p2y12 antagonists
TWI361690B (en) 2007-11-29 2012-04-11 Actelion Pharmaceuticals Ltd Phosphonic acid derivatives
WO2009080226A2 (en) 2007-12-26 2009-07-02 Sanofis-Aventis Heterocyclic pyrazole-carboxamides as p2y12 antagonists
EP2238127B1 (en) 2007-12-26 2012-08-15 Sanofi Pyrazole-carboxamide derivatives 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
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
WO2010122504A1 (en) 2009-04-22 2010-10-28 Actelion Pharmaceuticals Ltd Thiazole derivatives and their use as p2y12 receptor antagonists
EP3981774A1 (en) 2016-09-22 2022-04-13 Idorsia Pharmaceuticals Ltd Crystalline forms
EA201992123A1 (ru) 2017-03-15 2020-02-25 Идорсия Фармасьютиклз Лтд Подкожное введение антагониста p2yрецептора
EP4181872B1 (en) 2020-07-15 2025-11-26 Viatris Asia Pacific Pte. Ltd. Aqueous pharmaceutical composition comprising a p2y12 receptor antagonist

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Baldoni, Daniela; Bruderer, Shirin; Krause, Andreas; Gutierrez, Marcello; Gueret, Pierre; Astruc, Beatrice; Dingemanse, Jasper，A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial，Clinical Drug Investigation，2014年，34(11),，807-818
Ｃ．Ｇ．ＷＥＲＭＵＴＨ編，最新 創薬化学 下巻，p.347-365，株式会社 テクノミック，1999年
STAHLY，P.，医薬品の塩選択,結晶多形のスクリーニングの重要性について，薬剤学，2006年，Vol.66，No.6，p.435-439

Also Published As

Publication number Publication date
CN109715639A (zh) 2019-05-03
KR20190052704A (ko) 2019-05-16
IL265445A (en) 2019-05-30
PH12019500567A1 (en) 2019-11-18
LT3515924T (lt) 2022-03-10
HRP20220234T1 (hr) 2022-05-13
EP3981774A1 (en) 2022-04-13
JP2019529553A (ja) 2019-10-17
US12227532B2 (en) 2025-02-18
US20200017534A1 (en) 2020-01-16
KR102552795B1 (ko) 2023-07-06
MA46266B1 (fr) 2022-02-28
AU2017331930B2 (en) 2021-07-15
DK3515924T3 (da) 2022-03-21
MA46266A (fr) 2019-07-31
PL3515924T3 (pl) 2022-04-11
SI3515924T1 (sl) 2022-04-29
CY1125052T1 (el) 2024-02-16
WO2018055016A1 (en) 2018-03-29
RS62946B1 (sr) 2022-03-31
CN109715639B (zh) 2022-04-19
MX2019003093A (es) 2019-07-18
HUE057772T2 (hu) 2022-06-28
BR112019004845A2 (pt) 2019-06-04
US20220275011A1 (en) 2022-09-01
IL265445B2 (en) 2024-05-01
US11365209B2 (en) 2022-06-21
CL2019000728A1 (es) 2019-07-05
TW201813965A (zh) 2018-04-16
MY193080A (en) 2022-09-26
EP3515924B1 (en) 2021-12-15
US10730896B2 (en) 2020-08-04
EA201990723A1 (ru) 2019-10-31
EP3515924A1 (en) 2019-07-31
US20250163086A1 (en) 2025-05-22
PH12019500567B1 (en) 2024-01-31
NZ750772A (en) 2023-10-27
UA124073C2 (uk) 2021-07-14
AU2017331930A1 (en) 2019-03-07
US20210009614A1 (en) 2021-01-14
TWI752086B (zh) 2022-01-11
CA3037794A1 (en) 2018-03-29
MX381590B (es) 2025-03-12
IL265445B1 (en) 2024-01-01
ES2908572T3 (es) 2022-05-03
PT3515924T (pt) 2022-03-11

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