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
Other languages
English (en)
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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Epidemiology (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
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
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

Family Applications After (1)

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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 (ja)
EP (2) EP3954691A1 (ja)
JP (1) JP6672471B2 (ja)
KR (2) KR102255228B1 (ja)
CN (1) CN108718527B (ja)
AR (1) AR107633A1 (ja)
AU (2) AU2017219189B2 (ja)
BR (1) BR112018016932A2 (ja)
CA (1) CA3011650A1 (ja)
ES (1) ES2899369T3 (ja)
HR (1) HRP20211816T1 (ja)
IL (2) IL260153B (ja)
MX (1) MX2018009944A (ja)
PL (1) PL3416966T3 (ja)
SG (2) SG10202110927VA (ja)
SI (1) SI3416966T1 (ja)
WO (1) WO2017140750A1 (ja)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106061978B (zh) * 2014-03-07 2018-10-23 豪夫迈·罗氏有限公司 用于治疗和预防乙型肝炎病毒感染的新的6-稠合的杂芳基二氢嘧啶
CN109111451B (zh) 2017-06-26 2020-08-11 广东东阳光药业有限公司 二氢嘧啶类化合物及其在药物中的应用
CA3066857A1 (en) 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
CA3079557A1 (en) * 2017-10-18 2019-04-25 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and uses thereof in medicine
TW201945003A (zh) 2018-03-01 2019-12-01 愛爾蘭商健生科學愛爾蘭無限公司 2,4-二胺基喹唑啉衍生物及其醫學用途
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
WO2020125729A1 (en) 2018-12-20 2020-06-25 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
TW202035412A (zh) * 2018-12-20 2020-10-01 比利時商健生藥品公司 雜芳基二氫嘧啶衍生物和治療b型肝炎感染之方法
WO2020193459A1 (en) * 2019-03-25 2020-10-01 F. Hoffmann-La Roche Ag Solid forms of a compound of hbv core protein allosteric modifier
JP2022535112A (ja) 2019-06-06 2022-08-04 エフ.ホフマン-ラ ロシュ アーゲー 4-フェニル-5-アルコキシカルボニル-2-チアゾール-2-イル-1,4-ジヒドロピリミジン-6-イル]メチル]-3-オキソ-5,6,8,8a-テトラヒドロ-1H-イミダゾ[1,5-a]ピラジン-2-イル]-カルボン酸を調製するための代替方法
US20220241402A1 (en) 2019-06-18 2022-08-04 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and quinazoline derivatives
JP2022542420A (ja) * 2019-07-31 2022-10-03 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー ジヒドロピリミジン誘導体及びhbv感染又はhbv誘導性疾患の処置におけるその使用
WO2021078221A1 (zh) * 2019-10-24 2021-04-29 广东东阳光药业有限公司 二氢嘧啶类化合物及其在药物中的应用
IL297595A (en) * 2020-04-28 2022-12-01 Hoffmann La Roche A 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 (de) 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10125131A1 (de) 2001-05-23 2002-12-05 Bayer Ag Verfahren zur Spaltung des Methyl 4-(2-chlor-4-fluorphenyl)-2-(3,5-difluor-2-pyridinyl)-6-methyl-1,4-dihydro-5-pyrmidincarboxylat-Racemats
CN100453542C (zh) 2007-04-30 2009-01-21 广东东阳光药业有限公司 2-杂环取代的二氢嘧啶消旋化合物的拆分方法
WO2010069147A1 (zh) 2008-12-17 2010-06-24 张中能 二氢嘧啶类化合物、其组合物及其应用
PL2888241T3 (pl) 2012-08-24 2017-12-29 Sunshine Lake Pharma Co., Ltd. 2,4,5,6-Podstawione pochodne 3,6-dihydropirymidyny jako inhibitory polimerazy wirusa zapalenia wątroby typu B (HBV) do leczenia np. przewlekłego zapalenia wątroby
MX2015002954A (es) 2012-09-10 2015-06-05 Hoffmann La Roche Nuevas 6-aminoacido-heteroarilhidropirimidinas para el tratamiento y profilaxis de la infeccion del virus de la hepatitis b.
CN105209470B (zh) 2013-05-17 2018-02-06 豪夫迈·罗氏有限公司 用于治疗和预防乙型肝炎病毒感染的6‑桥连的杂芳基二氢嘧啶
CN106061978B (zh) * 2014-03-07 2018-10-23 豪夫迈·罗氏有限公司 用于治疗和预防乙型肝炎病毒感染的新的6-稠合的杂芳基二氢嘧啶
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
WO2016102438A1 (en) 2014-12-23 2016-06-30 F. Hoffmann-La Roche Ag Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidine analogues

Also Published As

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

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