CO2023005883A2 - Procedimiento para la fabricación de (6r,10s)-10-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1-il)fenil]-6-oxo-1(6h)-pirimidinil}- 1-(difluorometil)-6-metil-1 4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona - Google Patents

Procedimiento para la fabricación de (6r,10s)-10-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1-il)fenil]-6-oxo-1(6h)-pirimidinil}- 1-(difluorometil)-6-metil-1 4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona

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Publication number
CO2023005883A2
CO2023005883A2 CONC2023/0005883A CO2023005883A CO2023005883A2 CO 2023005883 A2 CO2023005883 A2 CO 2023005883A2 CO 2023005883 A CO2023005883 A CO 2023005883A CO 2023005883 A2 CO2023005883 A2 CO 2023005883A2
Authority
CO
Colombia
Prior art keywords
chloro
metheno
pyrazolo
hexahydro
triazol
Prior art date
Application number
CONC2023/0005883A
Other languages
English (en)
Inventor
Nicolas Cuniere
Subha Mukherjee
William P Gallagher
Christopher Robert Jamison
Carolyn S Wei
Sergei Kolotuchin
Amarjit Singh
Chris Sfouggatakis
Adrian Ortiz
Steven R Wisniewski
Bin Zheng
Helen Y Luo
Sébastien François Emmanuel LEMAIRE
Haïm Cyril Ben
Kostiantyn Chernichenko
Diego Fernando Domenico Broggini
Simon Albert Wagschal
Duy Chi Trung Cao
Karl Reuter
Björn Schmalzbauer
Philipp Koschker
Martin D Eastgate
Dimitri Skliar
Alexander Zhdanko
Christos Xiouras
Matthew Penfield Mower
Ngoc Duc Tran
Ramdane Rahmani
Xavier Jean-Marie Jusseau
Kiran Matcha
Luca Alessandro Perego
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 CO2023005883A2 publication Critical patent/CO2023005883A2/es

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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
    • C07D471/16Peri-condensed systems
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/70Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of the iron group metals or copper
    • B01J23/72Copper
    • 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
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Materials Engineering (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente solicitud se refiere en general a varios procesos para la preparación de (6R, 10S)-10-{4-[5-cloro-2-(4-cloro-1H-1,2,3-triazol-1-il)fenil]-6-oxo-1(6H)-pirimidinil}-1-(difluorometil) -6-metil-1,4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3 -b][1,7]diazaciclotetradecina-5(6H)-ona: Compuesto (I).
CONC2023/0005883A 2020-10-12 2023-05-08 Procedimiento para la fabricación de (6r,10s)-10-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1-il)fenil]-6-oxo-1(6h)-pirimidinil}- 1-(difluorometil)-6-metil-1 4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona CO2023005883A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063090558P 2020-10-12 2020-10-12
PCT/US2021/054413 WO2022081473A1 (en) 2020-10-12 2021-10-11 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

Publications (1)

Publication Number Publication Date
CO2023005883A2 true CO2023005883A2 (es) 2023-08-09

Family

ID=78536589

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2023/0005883A CO2023005883A2 (es) 2020-10-12 2023-05-08 Procedimiento para la fabricación de (6r,10s)-10-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1-il)fenil]-6-oxo-1(6h)-pirimidinil}- 1-(difluorometil)-6-metil-1 4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona

Country Status (17)

Country Link
US (1) US20230416252A1 (es)
EP (1) EP4225757A1 (es)
JP (1) JP2023545129A (es)
KR (1) KR20230106611A (es)
CN (1) CN117120418A (es)
AR (1) AR123762A1 (es)
AU (1) AU2021360411A1 (es)
BR (1) BR112023006200A2 (es)
CA (1) CA3195024A1 (es)
CL (1) CL2023001049A1 (es)
CO (1) CO2023005883A2 (es)
IL (1) IL301889A (es)
MX (1) MX2023004237A (es)
PE (1) PE20231310A1 (es)
TW (1) TW202229280A (es)
UY (1) UY39469A (es)
WO (1) WO2022081473A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024030409A1 (en) 2022-08-01 2024-02-08 Bristol-Myers Squibb Company Use of milvexian for treating or preventing ischemic stroke

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9453018B2 (en) * 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
NO2721243T3 (es) * 2014-10-01 2018-10-20
EP3953334B1 (en) * 2019-04-11 2023-11-22 Bristol-Myers Squibb Company 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

Also Published As

Publication number Publication date
CN117120418A (zh) 2023-11-24
MX2023004237A (es) 2023-07-03
WO2022081473A1 (en) 2022-04-21
AR123762A1 (es) 2023-01-11
EP4225757A1 (en) 2023-08-16
CL2023001049A1 (es) 2023-09-22
AU2021360411A1 (en) 2023-06-08
BR112023006200A2 (pt) 2023-05-09
TW202229280A (zh) 2022-08-01
IL301889A (en) 2023-06-01
PE20231310A1 (es) 2023-08-24
JP2023545129A (ja) 2023-10-26
US20230416252A1 (en) 2023-12-28
UY39469A (es) 2022-04-29
KR20230106611A (ko) 2023-07-13
CA3195024A1 (en) 2022-04-21

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