SG11202111132WA - 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

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Publication number
SG11202111132WA
SG11202111132WA SG11202111132WA SG11202111132WA SG11202111132WA SG 11202111132W A SG11202111132W A SG 11202111132WA SG 11202111132W A SG11202111132W A SG 11202111132WA SG 11202111132W A SG11202111132W A SG 11202111132WA SG 11202111132W A SG11202111132W A SG 11202111132WA
Authority
SG
Singapore
Prior art keywords
chloro
diazacyclotetradecin
metheno
pyrazolo
hexahydro
Prior art date
Application number
SG11202111132WA
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
Sébastien François Emmanuel LEMAIRE
Ηαϊμ Cyril Ben
Original Assignee
Bristol Myers Squibb Co
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co, Janssen Pharmaceutica Nv filed Critical Bristol Myers Squibb Co
Publication of SG11202111132WA publication Critical patent/SG11202111132WA/en

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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)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)
SG11202111132WA 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 SG11202111132WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962832614P 2019-04-11 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
SG11202111132WA true SG11202111132WA (en) 2021-11-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202111132WA SG11202111132WA (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 (1) US20220144836A1 (en)
EP (2) EP3953334B1 (en)
JP (1) JP2022526659A (en)
KR (1) KR20220045105A (en)
CN (1) CN114375290A (en)
AR (1) AR118649A1 (en)
AU (1) AU2020272973A1 (en)
BR (1) BR112021020368A2 (en)
CA (1) CA3132365A1 (en)
EA (1) EA202192807A1 (en)
ES (1) ES2969253T3 (en)
IL (1) IL287102A (en)
MX (1) MX2021012286A (en)
SG (1) SG11202111132WA (en)
TW (1) TW202104188A (en)
WO (1) WO2020210613A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021207200A2 (en) 2020-04-10 2021-10-14 Codexis, Inc. Engineered transaminase polypeptides
TW202229280A (en) * 2020-10-12 2022-08-01 美商必治妥美雅史谷比公司 A process toward 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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2013145912A (en) * 2011-03-15 2015-04-20 Эббви Инк. MODULATORS OF NUCLEAR HORMONE RECEPTORS
IL298983B2 (en) 2014-01-31 2024-03-01 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
NO2721243T3 (en) * 2014-10-01 2018-10-20
CN105294496A (en) * 2015-09-28 2016-02-03 中山大学 Preparation method of citalopram intermediate
WO2018133793A1 (en) * 2017-01-18 2018-07-26 广东东阳光药业有限公司 Blood coagulation factor xia inhibitor and uses thereof
WO2020211781A1 (en) * 2019-04-16 2020-10-22 南京明德新药研发有限公司 Macrocyclic derivatives acting as xia factor inhibitor
WO2021013209A1 (en) * 2019-07-23 2021-01-28 南京明德新药研发有限公司 Macrocyclic derivatives as factor xia inhibitors
US20230159904A1 (en) * 2020-04-10 2023-05-25 Codexis, Inc Carboxyesterase polypeptides for kinetic resolution

Also Published As

Publication number Publication date
ES2969253T3 (en) 2024-05-17
CA3132365A1 (en) 2020-10-15
BR112021020368A2 (en) 2021-12-07
EP4234555A2 (en) 2023-08-30
MX2021012286A (en) 2022-04-06
EA202192807A1 (en) 2022-02-24
AU2020272973A1 (en) 2021-12-02
EP3953334B1 (en) 2023-11-22
US20220144836A1 (en) 2022-05-12
JP2022526659A (en) 2022-05-25
AR118649A1 (en) 2021-10-20
IL287102A (en) 2021-12-01
EP3953334A1 (en) 2022-02-16
EP4234555A3 (en) 2024-01-03
KR20220045105A (en) 2022-04-12
CN114375290A (en) 2022-04-19
WO2020210613A1 (en) 2020-10-15
TW202104188A (en) 2021-02-01

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