KR20260047658A - (6r,10s)-10-｛4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐｝-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의제조를 위한 신규 합성 옵션 - Google Patents

(6r,10s)-10-｛4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐｝-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의제조를 위한 신규 합성 옵션

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Publication number
KR20260047658A
KR20260047658A KR1020267004972A KR20267004972A KR20260047658A KR 20260047658 A KR20260047658 A KR 20260047658A KR 1020267004972 A KR1020267004972 A KR 1020267004972A KR 20267004972 A KR20267004972 A KR 20267004972A KR 20260047658 A KR20260047658 A KR 20260047658A
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added
hours
solution
mixture
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English (en)
Korean (ko)
Inventor
니콜라스 쿠니에레
유 판
세르게이 콜로투친
수바 무케르지
에릭 엠. 시몬스
아마르지트 싱
캐롤린 에스. 웨이
이 샤오
창시아 유안
빈 젱
시몬 알버트 바그샬
디에고 페르난도 도메니코 브로기니
뒤 치 트룽 카오
코스티안틴 체르니첸코
세바스티엔 프랑수아 엠마누엘 르메르
시릴 벤 하임
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
얀센 파마슈티카 엔브이
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Publication of KR20260047658A publication Critical patent/KR20260047658A/ko
Pending legal-status Critical Current

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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
    • 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
    • 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)
KR1020267004972A 2019-04-11 2020-04-10 (6r,10s)-10-｛4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐｝-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의제조를 위한 신규 합성 옵션 Pending KR20260047658A (ko)

Applications Claiming Priority (4)

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
KR1020217036807A KR102929951B1 (ko) 2019-04-11 2020-04-10 (6r,10s)-10-{4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐}-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의 제조를 위한 신규 합성 옵션

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020217036807A Division KR102929951B1 (ko) 2019-04-11 2020-04-10 (6r,10s)-10-{4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐}-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의 제조를 위한 신규 합성 옵션

Publications (1)

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KR20260047658A true KR20260047658A (ko) 2026-04-08

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Application Number Title Priority Date Filing Date
KR1020267004972A Pending KR20260047658A (ko) 2019-04-11 2020-04-10 (6r,10s)-10-｛4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐｝-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의제조를 위한 신규 합성 옵션
KR1020217036807A Active KR102929951B1 (ko) 2019-04-11 2020-04-10 (6r,10s)-10-{4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐}-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의 제조를 위한 신규 합성 옵션

Family Applications After (1)

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KR1020217036807A Active KR102929951B1 (ko) 2019-04-11 2020-04-10 (6r,10s)-10-{4-[5-클로로-2-(4-클로로-1h-1,2,3-트리아졸-1-일)페닐]-6-옥소-1(6h)-피리미디닐}-1-(디플루오로메틸)-6-메틸-1,4,7,8,9,10-헥사히드로-11,15-(메테노)피라졸로[4,3-b][1,7]디아자시클로테트라데신-5(6h)-온의 제조를 위한 신규 합성 옵션

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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=)

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EP4133064A4 (en) 2020-04-10 2024-07-24 Codexis, Inc. Engineered transaminase polypeptides
TW202229280A (zh) * 2020-10-12 2022-08-01 美商必治妥美雅史谷比公司 （６ｒ，１０ｓ）－１０－｛４－［５－氯－２－（４－氯－１ｈ－１，２，３－三唑－１－基）苯基］－６－側氧基－１（６ｈ）－嘧啶基｝－１－（二氟甲基）－６－甲基－１，４，７，８，９，１０－六氫－１１，１５－（亞甲橋基）吡唑并［４，３－ｂ］［１，７］二氮雜環十四炔－５（６ｈ）－酮之製備方法

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WO2012125797A1 (en) 2011-03-15 2012-09-20 Abbott Laboratories Nuclear hormone receptor modulators
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2721243T3 (https=) 2014-10-01 2018-10-20
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
CN105294496A (zh) * 2015-09-28 2016-02-03 中山大学 一种西酞普兰中间体的制备方法
CN110062757B (zh) 2017-01-18 2022-03-04 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途
WO2020211781A1 (zh) * 2019-04-16 2020-10-22 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
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
JP7747337B2 (ja) * 2020-04-10 2025-10-01 コデクシス， インコーポレイテッド 速度論的光学分割のためのカルボキシエステラーゼポリペプチド

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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
JP7631218B2 (ja) 2025-02-18
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
US12378246B2 (en) 2025-08-05
CN114375290B (zh) 2024-11-29
AU2026201396A1 (en) 2026-03-19
US20260092066A1 (en) 2026-04-02

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