CN109715639B - 结晶形式 - Google Patents

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Publication number
CN109715639B
CN109715639B CN201780057793.2A CN201780057793A CN109715639B CN 109715639 B CN109715639 B CN 109715639B CN 201780057793 A CN201780057793 A CN 201780057793A CN 109715639 B CN109715639 B CN 109715639B
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China
Prior art keywords
crystalline form
compound
piperazine
propionyl
amino
Prior art date
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CN201780057793.2A
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English (en)
Chinese (zh)
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CN109715639A (zh
Inventor
丹尼尔·洛伊恩贝格尔
斯蒂芬·雷伯
马库斯·冯劳默尔
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Huizhi Asia Pacific Private Ltd
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Actelion Pharmaceuticals Ltd
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Publication of CN109715639A publication Critical patent/CN109715639A/zh
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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)
  • 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)
CN201780057793.2A 2016-09-22 2017-09-21 结晶形式 Active CN109715639B (zh)

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 (2)

Publication Number Publication Date
CN109715639A CN109715639A (zh) 2019-05-03
CN109715639B true CN109715639B (zh) 2022-04-19

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CN201780057793.2A Active CN109715639B (zh) 2016-09-22 2017-09-21 结晶形式

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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
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.

Citations (1)

* Cited by examiner, † Cited by third party
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

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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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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;Caroff, Eva et al.;《Journal of Medicinal Chemistry》;20151109;第58卷(第23期);第9133-9153页 *
A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial;Baldoni, Daniela et al.;《Clinical Drug Investigation》;20141021;第34卷(第11期);第807-818页 *
Baldoni, Daniela et al..A New Reversible and Potent P2Y12 Receptor Antagonist (ACT-246475): Tolerability, Pharmacokinetics, and Pharmacodynamics in a First-in-Man Trial.《Clinical Drug Investigation》.2014,第34卷(第11期),第807-818页. *

Also Published As

Publication number Publication date
WO2018055016A1 (en) 2018-03-29
DK3515924T3 (da) 2022-03-21
US11365209B2 (en) 2022-06-21
MA46266B1 (fr) 2022-02-28
JP2019529553A (ja) 2019-10-17
RS62946B1 (sr) 2022-03-31
TW201813965A (zh) 2018-04-16
HRP20220234T1 (hr) 2022-05-13
KR102552795B1 (ko) 2023-07-06
IL265445A (en) 2019-05-30
PH12019500567B1 (en) 2024-01-31
MY193080A (en) 2022-09-26
EP3515924A1 (en) 2019-07-31
US20220275011A1 (en) 2022-09-01
EP3515924B1 (en) 2021-12-15
BR112019004845A2 (pt) 2019-06-04
MX381590B (es) 2025-03-12
AU2017331930B2 (en) 2021-07-15
CA3037794A1 (en) 2018-03-29
TWI752086B (zh) 2022-01-11
CY1125052T1 (el) 2024-02-16
US12227532B2 (en) 2025-02-18
PT3515924T (pt) 2022-03-11
MX2019003093A (es) 2019-07-18
AU2017331930A1 (en) 2019-03-07
HUE057772T2 (hu) 2022-06-28
CL2019000728A1 (es) 2019-07-05
SI3515924T1 (sl) 2022-04-29
EP3981774A1 (en) 2022-04-13
US20250163086A1 (en) 2025-05-22
UA124073C2 (uk) 2021-07-14
US10730896B2 (en) 2020-08-04
NZ750772A (en) 2023-10-27
MA46266A (fr) 2019-07-31
US20210009614A1 (en) 2021-01-14
US20200017534A1 (en) 2020-01-16
IL265445B2 (en) 2024-05-01
LT3515924T (lt) 2022-03-10
PL3515924T3 (pl) 2022-04-11
JP7097369B2 (ja) 2022-07-07
IL265445B1 (en) 2024-01-01
CN109715639A (zh) 2019-05-03
KR20190052704A (ko) 2019-05-16
EA201990723A1 (ru) 2019-10-31
ES2908572T3 (es) 2022-05-03
PH12019500567A1 (en) 2019-11-18

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