SG10202110927VA - Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid - Google Patents

Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid

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Publication number
SG10202110927VA
SG10202110927VA SG10202110927VA SG10202110927VA SG10202110927VA SG 10202110927V A SG10202110927V A SG 10202110927VA SG 10202110927V A SG10202110927V A SG 10202110927VA SG 10202110927V A SG10202110927V A SG 10202110927VA SG 10202110927V A SG10202110927V A SG 10202110927VA
Authority
SG
Singapore
Prior art keywords
dihydropyrimidin
pyrazin
thiazol
imidazo
alkoxycarbonyl
Prior art date
Application number
SG10202110927VA
Inventor
Junli Chen
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of SG10202110927VA publication Critical patent/SG10202110927VA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
SG10202110927VA 2016-02-19 2017-02-16 Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid SG10202110927VA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2016074132 2016-02-19

Publications (1)

Publication Number Publication Date
SG10202110927VA true SG10202110927VA (en) 2021-11-29

Family

ID=58054130

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201805595TA SG11201805595TA (en) 2016-02-19 2017-02-16 Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid
SG10202110927VA SG10202110927VA (en) 2016-02-19 2017-02-16 Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG11201805595TA SG11201805595TA (en) 2016-02-19 2017-02-16 Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid

Country Status (17)

Country Link
US (1) US10927116B2 (en)
EP (2) EP3954691A1 (en)
JP (1) JP6672471B2 (en)
KR (2) KR102255228B1 (en)
CN (1) CN108718527B (en)
AR (1) AR107633A1 (en)
AU (2) AU2017219189B2 (en)
BR (1) BR112018016932A2 (en)
CA (1) CA3011650A1 (en)
ES (1) ES2899369T3 (en)
HR (1) HRP20211816T1 (en)
IL (2) IL260153B (en)
MX (1) MX2018009944A (en)
PL (1) PL3416966T3 (en)
SG (2) SG11201805595TA (en)
SI (1) SI3416966T1 (en)
WO (1) WO2017140750A1 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS58384B1 (en) * 2014-03-07 2019-04-30 Hoffmann La Roche Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
CA3068128A1 (en) 2017-06-26 2019-01-03 North & South Brother Pharmacy Investment Company Limited Dihydropyrimidine compounds and uses thereof in medicine
WO2019001420A1 (en) 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
WO2019076310A1 (en) * 2017-10-18 2019-04-25 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and uses thereof in medicine
TW201945003A (en) 2018-03-01 2019-12-01 愛爾蘭商健生科學愛爾蘭無限公司 2,4-diaminoquinazoline derivatives and medical uses thereof
US11053235B2 (en) 2018-08-09 2021-07-06 Janssen Sciences Ireland Unlimited Company Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases
US20220048919A1 (en) * 2018-12-20 2022-02-17 Janssen Phrmaceutica NV Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
TW202035412A (en) * 2018-12-20 2020-10-01 比利時商健生藥品公司 Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
MX2021011614A (en) * 2019-03-25 2021-10-13 Hoffmann La Roche Solid forms of a compound of hbv core protein allosteric modifier.
US20220315588A1 (en) 2019-06-06 2022-10-06 Hoffmann-La Roche Inc. Alternative process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid
WO2020255039A1 (en) 2019-06-18 2020-12-24 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and quinazoline derivatives
US20230083012A1 (en) * 2019-07-31 2023-03-16 Janssen Sciences Ireland Unlimited Company Dihydropyrimidine derivatives and uses thereof in the treatment of hbv infection or of hbv-induced diseases
CN112707910A (en) * 2019-10-24 2021-04-27 广东东阳光药业有限公司 Dihydropyrimidine compound and application thereof in medicine
AU2021266084A1 (en) * 2020-04-28 2022-10-20 F. Hoffmann-La Roche Ag Process for the preparation of a chiral piperazine-2-carboxylic acid

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10012823A1 (en) 2000-03-16 2001-09-20 Bayer Ag New alkyl-6-aminoalkyl-dihydropyrimidine-5-carboxylate derivatives, useful for the treatment of viral, especially hepatitis B, infections
DE10125131A1 (en) 2001-05-23 2002-12-05 Bayer Ag Process for the cleavage of the methyl 4- (2-chloro-4-fluorophenyl) -2- (3,5-difluoro-2-pyridinyl) -6-methyl-1,4-dihydro-5-pyrmidinecarboxylate racemate
CN100453542C (en) 2007-04-30 2009-01-21 广东东阳光药业有限公司 Resolution method for 2-hetero ring substituted dihydropyrimidine racemic compounds
WO2010069147A1 (en) 2008-12-17 2010-06-24 张中能 Dihydropyrimidine derivatives, compositions thereof and their use
AU2013305390C1 (en) 2012-08-24 2015-12-24 Ruyuan Wei Xiang Technology Co., Ltd. Dihydropyrimidine compounds and their application in pharmaceuticals
SG11201500377UA (en) 2012-09-10 2015-02-27 Hoffmann La Roche 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
AU2014267198A1 (en) 2013-05-17 2015-11-05 F. Hoffmann-La Roche Ag 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of Hepatitis B virus infection
RS58384B1 (en) 2014-03-07 2019-04-30 Hoffmann La Roche Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
WO2016016196A1 (en) * 2014-07-31 2016-02-04 F. Hoffmann-La Roche Ag Novel chiral resolution of 4-aryl-2-thiazol-2-yl-1,4-dihydropyrimidine-5-carboxylic acid esters
AR103222A1 (en) 2014-12-23 2017-04-26 Hoffmann La Roche PROCEDURE FOR THE PREPARATION OF ANALOGS OF 4-PHENYL-5-ALCOXICARBONIL-2-THIAZOL-2-IL-1,4-DIHYDROPIRIMIDINE

Also Published As

Publication number Publication date
JP6672471B2 (en) 2020-03-25
BR112018016932A2 (en) 2019-01-08
KR20210059801A (en) 2021-05-25
AU2021203860A1 (en) 2021-07-08
US10927116B2 (en) 2021-02-23
IL260153B (en) 2021-10-31
CA3011650A1 (en) 2017-08-24
EP3416966A1 (en) 2018-12-26
WO2017140750A1 (en) 2017-08-24
IL286912A (en) 2021-10-31
JP2019507144A (en) 2019-03-14
MX2018009944A (en) 2018-11-09
EP3416966B1 (en) 2021-09-29
KR20180104177A (en) 2018-09-19
HRP20211816T1 (en) 2022-03-04
US20190010155A1 (en) 2019-01-10
AU2017219189B2 (en) 2021-04-01
AR107633A1 (en) 2018-05-16
PL3416966T3 (en) 2022-01-17
ES2899369T3 (en) 2022-03-11
SG11201805595TA (en) 2018-07-30
KR102255228B1 (en) 2021-05-25
IL260153A (en) 2018-07-31
EP3954691A1 (en) 2022-02-16
CN108718527B (en) 2022-06-28
CN108718527A (en) 2018-10-30
AU2017219189A1 (en) 2018-06-28
SI3416966T1 (en) 2022-01-31

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