JP7631218B2 - （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法 - Google Patents

（６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法 Download PDF

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JP7631218B2
JP7631218B2 JP2021559890A JP2021559890A JP7631218B2 JP 7631218 B2 JP7631218 B2 JP 7631218B2 JP 2021559890 A JP2021559890 A JP 2021559890A JP 2021559890 A JP2021559890 A JP 2021559890A JP 7631218 B2 JP7631218 B2 JP 7631218B2
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compound
added
acid
give
alkyl
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Japanese (ja)
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JP2022526659A (ja
JP2022526659A5 (https=
Inventor
キュニエール，ニコラ
ファン，ユー
コロトゥチン，セルゲイ
ムケルジー，スバ
エム シモンズ，エリック
シン，アマルジット
エス ウェイ，キャロリン
シャオ，イ
ユエン，チャンシア
ジェン，ビン
アルバート ワグシャル，サイモン
フェルナンド ドメニコ ブロッジーニ，ディエゴ
チー トゥルン カオ，ドゥイ
チェルニチェンコ，コスティアンティン
フランソワ エマニュエル ルメール，セバスチャン
ハイム，シリル ベン
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of JP2022526659A publication Critical patent/JP2022526659A/ja
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Priority to JP2025017468A priority Critical patent/JP2025084766A/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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021559890A 2019-04-11 2020-04-10 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法 Active JP7631218B2 (ja)

Priority Applications (1)

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JP2025017468A JP2025084766A (ja) 2019-04-11 2025-02-05 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962832614P 2019-04-11 2019-04-11
US62/832,614 2019-04-11
PCT/US2020/027655 WO2020210613A1 (en) 2019-04-11 2020-04-10 Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one

Related Child Applications (1)

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JP2025017468A Division JP2025084766A (ja) 2019-04-11 2025-02-05 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法

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JP2022526659A JP2022526659A (ja) 2022-05-25
JP2022526659A5 JP2022526659A5 (https=) 2023-04-12
JP7631218B2 true JP7631218B2 (ja) 2025-02-18

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JP2021559890A Active JP7631218B2 (ja) 2019-04-11 2020-04-10 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法
JP2025017468A Pending JP2025084766A (ja) 2019-04-11 2025-02-05 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法

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JP2025017468A Pending JP2025084766A (ja) 2019-04-11 2025-02-05 （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－１－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造における新規合成法

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US (2) US12378246B2 (https=)
EP (2) EP4234555A3 (https=)
JP (2) JP7631218B2 (https=)
KR (2) KR20260047658A (https=)
CN (2) CN114375290B (https=)
AR (1) AR118649A1 (https=)
AU (2) AU2020272973B2 (https=)
BR (1) BR112021020368A2 (https=)
CA (1) CA3132365A1 (https=)
EA (1) EA202192807A1 (https=)
ES (1) ES2969253T3 (https=)
IL (1) IL287102B2 (https=)
MX (2) MX2021012286A (https=)
SG (1) SG11202111132WA (https=)
TW (1) TWI880924B (https=)
WO (1) WO2020210613A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023545129A (ja) * 2020-10-12 2023-10-26 ブリストル－マイヤーズ スクイブ カンパニー （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－ １－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造方法

Families Citing this family (1)

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EP4133064A4 (en) 2020-04-10 2024-07-24 Codexis, Inc. Engineered transaminase polypeptides

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WO2016053455A1 (en) 2014-10-01 2016-04-07 Bristol-Myers Squibb Company Pyrimidinones as factor xia inhibitors

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CN114008047B (zh) * 2019-07-23 2023-03-21 南京明德新药研发有限公司 作为XIa因子抑制剂的大环衍生物
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WO2016053455A1 (en) 2014-10-01 2016-04-07 Bristol-Myers Squibb Company Pyrimidinones as factor xia inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023545129A (ja) * 2020-10-12 2023-10-26 ブリストル－マイヤーズ スクイブ カンパニー （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－ １－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造方法
JP7844457B2 (ja) 2020-10-12 2026-04-13 ブリストル－マイヤーズ スクイブ カンパニー （６ｒ，１０ｓ）－１０－｛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（６ｈ）－ピリミジニル｝－ １－（ジフルオロメチル）－６－メチル－１，４，７，８，９，１０－ヘキサヒドロ－１１，１５－（メタノ）ピラゾロ［４，３－ｂ］［１，７］ジアザシクロテトラデシン－５（６ｈ）－オンの製造方法

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EP3953334A1 (en) 2022-02-16
TWI880924B (zh) 2025-04-21
US20220144836A1 (en) 2022-05-12
IL287102A (en) 2021-12-01
AR118649A1 (es) 2021-10-20
KR20220045105A (ko) 2022-04-12
BR112021020368A2 (pt) 2021-12-07
EP4234555A2 (en) 2023-08-30
JP2022526659A (ja) 2022-05-25
TW202104188A (zh) 2021-02-01
ES2969253T3 (es) 2024-05-17
IL287102B1 (en) 2025-08-01
EP3953334B1 (en) 2023-11-22
CN119775276A (zh) 2025-04-08
CA3132365A1 (en) 2020-10-15
WO2020210613A1 (en) 2020-10-15
AU2020272973B2 (en) 2025-11-27
IL287102B2 (en) 2025-12-01
EP4234555A3 (en) 2024-01-03
KR102929951B1 (ko) 2026-02-24
SG11202111132WA (en) 2021-11-29
EA202192807A1 (ru) 2022-02-24
MX2021012286A (es) 2022-04-06
MX2025014306A (es) 2026-01-07
JP2025084766A (ja) 2025-06-03
AU2020272973A1 (en) 2021-12-02
CN114375290A (zh) 2022-04-19
KR20260047658A (ko) 2026-04-08
US12378246B2 (en) 2025-08-05
CN114375290B (zh) 2024-11-29
AU2026201396A1 (en) 2026-03-19
US20260092066A1 (en) 2026-04-02

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