BR112023006200A2 - Processo para a fabricação 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-hexaidro-11,15-(meteno)pirazolo[4,3-b] [1,7]diazaciclotetradecin-5(6h)-ona - Google Patents

Processo para a fabricação 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-hexaidro-11,15-(meteno)pirazolo[4,3-b] [1,7]diazaciclotetradecin-5(6h)-ona

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Publication number
BR112023006200A2
BR112023006200A2 BR112023006200A BR112023006200A BR112023006200A2 BR 112023006200 A2 BR112023006200 A2 BR 112023006200A2 BR 112023006200 A BR112023006200 A BR 112023006200A BR 112023006200 A BR112023006200 A BR 112023006200A BR 112023006200 A2 BR112023006200 A2 BR 112023006200A2
Authority
BR
Brazil
Prior art keywords
chloro
diazacyclotetradecin
pyrazolo
hexahydro
triazol
Prior art date
Application number
BR112023006200A
Other languages
English (en)
Inventor
Mukherjee Subha
p gallagher William
Robert Jamison Christopher
S Wei Carolyn
Kolotuchin Sergei
Singh Amarjit
Cuniere Nicolas
Sfouggatakis Chris
Ortiz Adrian
R Wisniewski Steven
Zheng Bin
Y Luo Helen
François Emmanuel Lemaire Sébastien
Ben Haim Cyril
Chernichenko Kostiantyn
Albert Wagschal Simon
Fernando Domenico Broggini Diego
Reuter Karl
Chi Trung Cao Duy
Koschker Philipp
Schmalzbauer Björn
Skliar Dimitri
D Eastgate Martin
Xiouras Christos
Zhdanko Alexander
Duc Tran Ngoc
Penfield Mower Matthew
Jean-Marie Jusseau Xavier
Rahmani Ramdane
Alessandro Perego Luca
Matcha Kiran
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 BR112023006200A2 publication Critical patent/BR112023006200A2/pt

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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
    • C07D471/16—Peri-condensed systems
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/70—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of the iron group metals or copper
    • B01J23/72—Copper
    • 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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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

PROCESSO PARA A FABRICAÇÃO 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-HEXAIDRO-11,15-(METENO)PIRAZOLO[4,3-B] [1,7]DIAZACICLOTETRADECIN-5(6H)-ONA. A presente invenção refere-se a diversos processos para a preparação 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-hexaidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6H)-ona:
BR112023006200A 2020-10-12 2021-10-11 Processo para a fabricação 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-hexaidro-11,15-(meteno)pirazolo[4,3-b] [1,7]diazaciclotetradecin-5(6h)-ona BR112023006200A2 (pt)

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
BR112023006200A2 true BR112023006200A2 (pt) 2023-05-09

Family

ID=78536589

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112023006200A BR112023006200A2 (pt) 2020-10-12 2021-10-11 Processo para a fabricação 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-hexaidro-11,15-(meteno)pirazolo[4,3-b] [1,7]diazaciclotetradecin-5(6h)-ona

Country Status (17)

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

Families Citing this family (2)

* 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
WO2024167899A1 (en) 2023-02-06 2024-08-15 Bristol-Myers Squibb Company Milvexian pharmaceutical compositions

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2721243T3 (pt) * 2014-10-01 2018-10-20
US9453018B2 (en) * 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
WO2020210613A1 (en) * 2019-04-11 2020-10-15 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
AU2021360411A9 (en) 2024-06-06
CL2023001049A1 (es) 2023-09-22
PE20231310A1 (es) 2023-08-24
CA3195024A1 (en) 2022-04-21
CN117120418A (zh) 2023-11-24
KR20230106611A (ko) 2023-07-13
UY39469A (es) 2022-04-29
WO2022081473A1 (en) 2022-04-21
JP2023545129A (ja) 2023-10-26
EP4225757A1 (en) 2023-08-16
US20230416252A1 (en) 2023-12-28
TW202229280A (zh) 2022-08-01
AR123762A1 (es) 2023-01-11
AU2021360411A1 (en) 2023-06-08
IL301889A (en) 2023-06-01
CO2023005883A2 (es) 2023-08-09
MX2023004237A (es) 2023-07-03

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