BR112021020368A2 - Opções sintéticas 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-hexa-hidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona - Google Patents

Opções sintéticas 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-hexa-hidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona

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Publication number
BR112021020368A2
BR112021020368A2 BR112021020368A BR112021020368A BR112021020368A2 BR 112021020368 A2 BR112021020368 A2 BR 112021020368A2 BR 112021020368 A BR112021020368 A BR 112021020368A BR 112021020368 A BR112021020368 A BR 112021020368A BR 112021020368 A2 BR112021020368 A2 BR 112021020368A2
Authority
BR
Brazil
Prior art keywords
chloro
diazacyclotetradecin
methene
pyrazolo
hexahydro
Prior art date
Application number
BR112021020368A
Other languages
English (en)
Portuguese (pt)
Inventor
Amarjit Singh
Bin Zheng
S Wei Carolyn
Changxia Yuan
Ben Haim Cyril
Fernando Domenico Broggini Diego
Chi Trung Cao Duy
M Simmons Eric
Kostiantyn Chernichenko
Nicolas Cuniere
Sergei Kolotuchin
Albert Wagschal Simon
Subha Mukherjee
François Emmanuel Lemaire Sébastien
Yi Xiao
Yu Fan
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 BR112021020368A2 publication Critical patent/BR112021020368A2/pt

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Classifications

    • 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

Landscapes

  • 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)
BR112021020368A 2019-04-11 2020-04-10 Opções sintéticas 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-hexa-hidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona BR112021020368A2 (pt)

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
BR112021020368A2 true BR112021020368A2 (pt) 2021-12-07

Family

ID=70457148

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021020368A BR112021020368A2 (pt) 2019-04-11 2020-04-10 Opções sintéticas 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-hexa-hidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6h)-ona

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
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
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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Legal Events

Date Code Title Description
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07D 213/61 , C07D 401/04 , C07D 471/18

Ipc: C07D 213/61 (2006.01), C07D 401/04 (2006.01), C07D