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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Japanese (ja)
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JP2019529553A (ja
JP2019529553A5 (cg-RX-API-DMAC7.html
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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65583Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
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 (cg-RX-API-DMAC7.html) 2020-11-12
JP7097369B2 true JP7097369B2 (ja) 2022-07-07

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ID=59923448

Family Applications (1)

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JP2019536696A Active JP7097369B2 (ja) 2016-09-22 2017-09-21 結晶形

Country Status (27)

Country Link
US (4) US10730896B2 (cg-RX-API-DMAC7.html)
EP (2) EP3981774A1 (cg-RX-API-DMAC7.html)
JP (1) JP7097369B2 (cg-RX-API-DMAC7.html)
KR (1) KR102552795B1 (cg-RX-API-DMAC7.html)
CN (1) CN109715639B (cg-RX-API-DMAC7.html)
AU (1) AU2017331930B2 (cg-RX-API-DMAC7.html)
CA (1) CA3037794A1 (cg-RX-API-DMAC7.html)
CL (1) CL2019000728A1 (cg-RX-API-DMAC7.html)
CY (1) CY1125052T1 (cg-RX-API-DMAC7.html)
DK (1) DK3515924T3 (cg-RX-API-DMAC7.html)
EA (1) EA201990723A1 (cg-RX-API-DMAC7.html)
ES (1) ES2908572T3 (cg-RX-API-DMAC7.html)
HR (1) HRP20220234T1 (cg-RX-API-DMAC7.html)
HU (1) HUE057772T2 (cg-RX-API-DMAC7.html)
IL (1) IL265445B2 (cg-RX-API-DMAC7.html)
LT (1) LT3515924T (cg-RX-API-DMAC7.html)
MA (1) MA46266B1 (cg-RX-API-DMAC7.html)
MX (1) MX381590B (cg-RX-API-DMAC7.html)
MY (1) MY193080A (cg-RX-API-DMAC7.html)
PH (1) PH12019500567B1 (cg-RX-API-DMAC7.html)
PL (1) PL3515924T3 (cg-RX-API-DMAC7.html)
PT (1) PT3515924T (cg-RX-API-DMAC7.html)
RS (1) RS62946B1 (cg-RX-API-DMAC7.html)
SI (1) SI3515924T1 (cg-RX-API-DMAC7.html)
TW (1) TWI752086B (cg-RX-API-DMAC7.html)
UA (1) UA124073C2 (cg-RX-API-DMAC7.html)
WO (1) WO2018055016A1 (cg-RX-API-DMAC7.html)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017331930B2 (en) 2016-09-22 2021-07-15 Viatris Asia Pacific Pte. Ltd. Crystalline forms
MX393334B (es) 2017-03-15 2025-03-24 Idorsia Pharmaceuticals Ltd Administración subcutánea de un antagonista del receptor p2y12.
WO2022013276A1 (en) 2020-07-15 2022-01-20 Idorsia Pharmaceuticals 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)

* Cited by examiner, † Cited by third party
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
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
OA12970A (en) 2002-12-11 2006-10-13 Schering Ag 2-aminocarbonyl-quinoline compounds as platelet adenosine diphosphate receptor antagonists.
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
BRPI0617636A2 (pt) 2005-10-21 2012-04-17 Actelion Pharmaceuticals Ltd composto, composição farmacêutica, e, uso de um composto
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.
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
BRPI0810462A2 (pt) 2007-04-23 2014-10-14 Sanofi Aventis Derivados de quinolina-carboxamida como antagonistas de p2y12
EP2225253B1 (en) 2007-11-29 2012-06-27 Actelion Pharmaceuticals Ltd. Phosphonic acid derivates and their use as p2y12 receptor antagonists
WO2009080227A2 (en) 2007-12-26 2009-07-02 Sanofi-Aventis Pyrazole-carboxamide derivatives as p2y12 antagonists
EP2238128B1 (en) 2007-12-26 2012-08-22 Sanofi 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
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
AU2010240527A1 (en) 2009-04-22 2011-12-01 Actelion Pharmaceuticals Ltd Thiazole derivatives and their use as P2Y12 receptor antagonists
AU2017331930B2 (en) 2016-09-22 2021-07-15 Viatris Asia Pacific Pte. Ltd. Crystalline forms
MX393334B (es) 2017-03-15 2025-03-24 Idorsia Pharmaceuticals Ltd Administración subcutánea de un antagonista del receptor p2y12.
WO2022013276A1 (en) 2020-07-15 2022-01-20 Idorsia Pharmaceuticals 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
TW201813965A (zh) 2018-04-16
WO2018055016A1 (en) 2018-03-29
MY193080A (en) 2022-09-26
HRP20220234T1 (hr) 2022-05-13
EP3515924B1 (en) 2021-12-15
IL265445B2 (en) 2024-05-01
US20200017534A1 (en) 2020-01-16
MX381590B (es) 2025-03-12
US20220275011A1 (en) 2022-09-01
CA3037794A1 (en) 2018-03-29
SI3515924T1 (sl) 2022-04-29
US20250163086A1 (en) 2025-05-22
PH12019500567B1 (en) 2024-01-31
HUE057772T2 (hu) 2022-06-28
IL265445A (en) 2019-05-30
PT3515924T (pt) 2022-03-11
JP2019529553A (ja) 2019-10-17
LT3515924T (lt) 2022-03-10
KR20190052704A (ko) 2019-05-16
MX2019003093A (es) 2019-07-18
AU2017331930B2 (en) 2021-07-15
PH12019500567A1 (en) 2019-11-18
RS62946B1 (sr) 2022-03-31
TWI752086B (zh) 2022-01-11
PL3515924T3 (pl) 2022-04-11
NZ750772A (en) 2023-10-27
US11365209B2 (en) 2022-06-21
US20210009614A1 (en) 2021-01-14
CY1125052T1 (el) 2024-02-16
EA201990723A1 (ru) 2019-10-31
US10730896B2 (en) 2020-08-04
ES2908572T3 (es) 2022-05-03
AU2017331930A1 (en) 2019-03-07
UA124073C2 (uk) 2021-07-14
KR102552795B1 (ko) 2023-07-06
EP3981774A1 (en) 2022-04-13
MA46266B1 (fr) 2022-02-28
BR112019004845A2 (pt) 2019-06-04
CN109715639A (zh) 2019-05-03
IL265445B1 (en) 2024-01-01
CN109715639B (zh) 2022-04-19
DK3515924T3 (da) 2022-03-21
MA46266A (fr) 2019-07-31
EP3515924A1 (en) 2019-07-31
US12227532B2 (en) 2025-02-18
CL2019000728A1 (es) 2019-07-05

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