JP2023521411A - （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体 - Google Patents

（９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体 Download PDF

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JP2023521411A
JP2023521411A JP2022562082A JP2022562082A JP2023521411A JP 2023521411 A JP2023521411 A JP 2023521411A JP 2022562082 A JP2022562082 A JP 2022562082A JP 2022562082 A JP2022562082 A JP 2022562082A JP 2023521411 A JP2023521411 A JP 2023521411A
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crystalline form
compound
crystalline
spectrum
diffraction pattern
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JP2023521411A5 (https=
Inventor
ケイ ディルガー，アンドリュー
エイ ガレラ，マイケル
スミス，ダニエル
エム ジーンバ，テリーサ
リュデカー，ダーフィット
シウラス，クリストス
アフジャ，ディパル
アンジェリーナ イェー クレーレン，ディルク
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of JP2023521411A publication Critical patent/JP2023521411A/ja
Publication of JP2023521411A5 publication Critical patent/JP2023521411A5/ja
Priority to JP2025260150A priority Critical patent/JP2026048873A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2022562082A 2020-04-10 2021-04-09 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体 Pending JP2023521411A (ja)

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JP2025260150A JP2026048873A (ja) 2020-04-10 2025-12-17 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体

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US202063008161P 2020-04-10 2020-04-10
US63/008,161 2020-04-10
PCT/US2021/026663 WO2021207659A1 (en) 2020-04-10 2021-04-09 Crystalline forms of (9r, 135s)-13- {4-[5-chloro-2-(4-chloro-1h,2,3- triazol- 1 -yl)phenyl] -6-oxo- 1,6-dihydropyrimidin- 1-yl}-3-(difluoromethyl)-9-methyl-3,4,7,15- tetraazatricyclo [ 12.3.1.02·6] octadeca- 1(18), 2(6), 4, 14, 16-pentaen-8-one

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JP2025260150A Division JP2026048873A (ja) 2020-04-10 2025-12-17 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体

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JP2023521411A true JP2023521411A (ja) 2023-05-24
JP2023521411A5 JP2023521411A5 (https=) 2024-04-18

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JP2022562082A Pending JP2023521411A (ja) 2020-04-10 2021-04-09 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体
JP2025260150A Pending JP2026048873A (ja) 2020-04-10 2025-12-17 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体

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JP2025260150A Pending JP2026048873A (ja) 2020-04-10 2025-12-17 （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体

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Country Link
US (1) US20230151010A1 (https=)
EP (1) EP4132930A1 (https=)
JP (2) JP2023521411A (https=)
KR (1) KR20230008742A (https=)
CN (1) CN115916780A (https=)
AU (1) AU2021253946A1 (https=)
BR (1) BR112022020243A2 (https=)
CA (1) CA3179957A1 (https=)
CL (1) CL2022002786A1 (https=)
CO (1) CO2022016067A2 (https=)
IL (1) IL297206A (https=)
MX (1) MX2022012523A (https=)
PE (1) PE20231071A1 (https=)
WO (1) WO2021207659A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA71692A (fr) 2022-08-01 2025-05-30 Bristol-Myers Squibb Company Utilisation de milvexian pour le traitement ou la prévention d'un accident vasculaire cérébral ischémique
KR20250136432A (ko) 2023-02-06 2025-09-16 브리스톨-마이어스 스큅 컴퍼니 밀벡시안 제약 조성물
WO2025224678A1 (en) 2024-04-25 2025-10-30 Assia Chemical Industries Ltd. Solid state forms of milvexian and process for preparation thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017530157A (ja) * 2014-10-01 2017-10-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としてのピリミジノン

Family Cites Families (2)

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Publication number Priority date Publication date Assignee Title
SG10201908467RA (en) * 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017530157A (ja) * 2014-10-01 2017-10-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としてのピリミジノン

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, vol. 65, no. 9, JPN6010003277, 1 September 2007 (2007-09-01), pages 907 - 913, ISSN: 0005665633 *
川口洋子ら, 生活工学研究, vol. 4, no. 2, JPN6015027394, 2002, pages 310 - 317, ISSN: 0005665631 *
平山令明編, 有機化合物結晶作製ハンドブック −原理とノウハウ−, JPN6011053065, 25 July 2008 (2008-07-25), pages 57 - 84, ISSN: 0005665632 *
芦澤 一英 他, 医薬品の多形現象と晶析の科学, JPN7015003233, 20 September 2002 (2002-09-20), pages 305 - 317, ISSN: 0005665630 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005665634 *

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Publication number Publication date
EP4132930A1 (en) 2023-02-15
BR112022020243A2 (pt) 2022-11-22
JP2026048873A (ja) 2026-03-17
PE20231071A1 (es) 2023-07-17
IL297206A (en) 2022-12-01
AU2021253946A1 (en) 2022-12-15
WO2021207659A1 (en) 2021-10-14
CO2022016067A2 (es) 2023-01-26
CL2022002786A1 (es) 2023-04-14
CN115916780A (zh) 2023-04-04
MX2022012523A (es) 2022-11-07
US20230151010A1 (en) 2023-05-18
CA3179957A1 (en) 2021-10-14
KR20230008742A (ko) 2023-01-16

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