CA3132365A1 - 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 - Google Patents

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 Download PDF

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Publication number
CA3132365A1
CA3132365A1 CA3132365A CA3132365A CA3132365A1 CA 3132365 A1 CA3132365 A1 CA 3132365A1 CA 3132365 A CA3132365 A CA 3132365A CA 3132365 A CA3132365 A CA 3132365A CA 3132365 A1 CA3132365 A1 CA 3132365A1
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compound
acid
formula
yield
alkyl
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Pending
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CA3132365A
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English (en)
French (fr)
Inventor
Nicolas Cuniere
Yu Fan
Sergei KOLOTUCHIN
Subha MUKHERJEE
Eric M. SIMMONS
Amarjit Singh
Carolyn S. WEI
Yi Xiao
Changxia YUAN
Bin Zheng
Simon Albert WAGSCHAL
Diego Fernando Domenico BROGGINI
Duy Chi Trung CAO
Kostiantyn CHERNICHENKO
Sebastien Francois Emmanuel Lemaire
Cyril BEN HAIM
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Bristol Myers Squibb Co
Original Assignee
Janssen Pharmaceutica NV
Bristol Myers Squibb Co
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Filing date
Publication date
Application filed by Janssen Pharmaceutica NV, Bristol Myers Squibb Co filed Critical Janssen Pharmaceutica NV
Publication of CA3132365A1 publication Critical patent/CA3132365A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/61Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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)
CA3132365A 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 Pending CA3132365A1 (en)

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

Publications (1)

Publication Number Publication Date
CA3132365A1 true CA3132365A1 (en) 2020-10-15

Family

ID=70457148

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3132365A Pending CA3132365A1 (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

Country Status (16)

Country Link
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=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
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
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
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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