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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JP2019529553A5 (enExample
JP2019529553A (ja
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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    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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
EP2016072562 2016-09-22
EPPCT/EP2016/072562 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) 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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (22)

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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
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
JP4729133B2 (ja) 2007-11-29 2011-07-20 アクテリオン ファーマシューティカルズ リミテッド ホスホン酸誘導体及びｐ２ｙ１２受容体拮抗剤としてのそれらの使用
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

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

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