BR112018016932A2 - processo para a preparação de ácido 4 -fenil -5 -alcoxicarbonil -2 -tiazol -2 -il -1,4 -diidropirimidin -6 -il[metil] -3 -oxo -5,6,8,8a -tetrahidro -1h -imidazo[1,5 -a]pirazin -2 -il] -carboxil acid - Google Patents

processo para a preparação de ácido 4 -fenil -5 -alcoxicarbonil -2 -tiazol -2 -il -1,4 -diidropirimidin -6 -il[metil] -3 -oxo -5,6,8,8a -tetrahidro -1h -imidazo[1,5 -a]pirazin -2 -il] -carboxil acid

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Publication number
BR112018016932A2
BR112018016932A2 BR112018016932A BR112018016932A BR112018016932A2 BR 112018016932 A2 BR112018016932 A2 BR 112018016932A2 BR 112018016932 A BR112018016932 A BR 112018016932A BR 112018016932 A BR112018016932 A BR 112018016932A BR 112018016932 A2 BR112018016932 A2 BR 112018016932A2
Authority
BR
Brazil
Prior art keywords
phenyl
dihydropyrimidin
pyrazin
thiazol
imidazo
Prior art date
Application number
BR112018016932A
Other languages
English (en)
Inventor
Chen Junli
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 BR112018016932A2 publication Critical patent/BR112018016932A2/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses

Abstract

a presente invenção refere-se a um processo para sintetizar um composto de fórmula (i), em que r1 é compreendido por fenil, que é não substituído ou substituído por um, dois ou três substituintes selecionados de forma independente a partir de halogênio e c1-6 alquila; r2 é compreendido por c1-6 alquila; r3 é compreendido por -cxh2x-; x é compreendido por 1, 2, 3, 4, 5, 6 ou 7; ou seu sal ou diastereômero farmaceuticamente aceitável, que é de utilidade para a profilaxia e tratamento de uma enfermidade viral em um paciente relacionada a infecção pela hepatite b ou uma enfermidade causada por infecção da hepatite b.
BR112018016932A 2016-02-19 2017-02-16 processo para a preparação de ácido 4 -fenil -5 -alcoxicarbonil -2 -tiazol -2 -il -1,4 -diidropirimidin -6 -il[metil] -3 -oxo -5,6,8,8a -tetrahidro -1h -imidazo[1,5 -a]pirazin -2 -il] -carboxil acid BR112018016932A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2016074132 2016-02-19
PCT/EP2017/053443 WO2017140750A1 (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

Publications (1)

Publication Number Publication Date
BR112018016932A2 true BR112018016932A2 (pt) 2019-01-08

Family

ID=58054130

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018016932A BR112018016932A2 (pt) 2016-02-19 2017-02-16 processo para a preparação de ácido 4 -fenil -5 -alcoxicarbonil -2 -tiazol -2 -il -1,4 -diidropirimidin -6 -il[metil] -3 -oxo -5,6,8,8a -tetrahidro -1h -imidazo[1,5 -a]pirazin -2 -il] -carboxil acid

Country Status (17)

Country Link
US (1) US10927116B2 (pt)
EP (2) EP3416966B1 (pt)
JP (1) JP6672471B2 (pt)
KR (2) KR20210059801A (pt)
CN (1) CN108718527B (pt)
AR (1) AR107633A1 (pt)
AU (2) AU2017219189B2 (pt)
BR (1) BR112018016932A2 (pt)
CA (1) CA3011650A1 (pt)
ES (1) ES2899369T3 (pt)
HR (1) HRP20211816T1 (pt)
IL (2) IL260153B (pt)
MX (1) MX2018009944A (pt)
PL (1) PL3416966T3 (pt)
SG (2) SG10202110927VA (pt)
SI (1) SI3416966T1 (pt)
WO (1) WO2017140750A1 (pt)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT3114128T (lt) * 2014-03-07 2019-03-25 F. Hoffmann-La Roche Ag Nauji 6 padėtyje kondensuoti heteroarildihidropirimidinai, skirti hepatito b virusinės infekcijos gydymui ir profilaktikai
AU2018290511B2 (en) 2017-06-26 2022-01-27 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and uses thereof in medicine
WO2019001420A1 (en) 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING INFECTIONS WITH HEPATITIS B VIRUS
CN109678859B (zh) * 2017-10-18 2020-12-29 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
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
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
KR20210106421A (ko) * 2018-12-20 2021-08-30 얀센 파마슈티카 엔.브이. 헤테로아릴디히드로피리미딘 유도체 및 b형 간염 감염의 치료 방법
BR112021019054A2 (pt) 2019-03-25 2021-11-30 F Hoffmann La Roche Ag Formas sólidas de um composto do modificador alostérico da proteína do núcleo do vhb
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
CA3146992A1 (en) * 2019-07-31 2021-02-04 Janssen Sciences Ireland Unlimited Company Dihydropyrimidine derivatives and uses thereof in the treatment of hbv infection or of hbv-induced diseases
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

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* 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
CN103626752B (zh) 2012-08-24 2015-08-12 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
EP2892893B2 (en) 2012-09-10 2019-10-16 F.Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
EA201592126A1 (ru) 2013-05-17 2016-05-31 Ф. Хоффманн-Ля Рош Аг 6-мостиковые гетероарилдигидропиримидины для лечения и профилактики заражения вирусом гепатита b
LT3114128T (lt) * 2014-03-07 2019-03-25 F. Hoffmann-La Roche Ag Nauji 6 padėtyje kondensuoti heteroarildihidropirimidinai, skirti hepatito b virusinės infekcijos gydymui ir profilaktikai
AR101319A1 (es) * 2014-07-31 2016-12-07 Hoffmann La Roche Resolución quiral de los ésteres del ácido 4-aril-2-tiazol-2-il-1,4-dihidropirimidin-5-carboxílico
AR103222A1 (es) 2014-12-23 2017-04-26 Hoffmann La Roche Procedimiento para la preparación de análogos de 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidina

Also Published As

Publication number Publication date
US20190010155A1 (en) 2019-01-10
SG11201805595TA (en) 2018-07-30
EP3416966A1 (en) 2018-12-26
US10927116B2 (en) 2021-02-23
JP2019507144A (ja) 2019-03-14
KR20180104177A (ko) 2018-09-19
AR107633A1 (es) 2018-05-16
JP6672471B2 (ja) 2020-03-25
ES2899369T3 (es) 2022-03-11
CN108718527A (zh) 2018-10-30
KR20210059801A (ko) 2021-05-25
MX2018009944A (es) 2018-11-09
CA3011650A1 (en) 2017-08-24
SI3416966T1 (sl) 2022-01-31
WO2017140750A1 (en) 2017-08-24
SG10202110927VA (en) 2021-11-29
IL286912A (en) 2021-10-31
IL260153B (en) 2021-10-31
HRP20211816T1 (hr) 2022-03-04
IL260153A (en) 2018-07-31
AU2017219189B2 (en) 2021-04-01
AU2021203860A1 (en) 2021-07-08
CN108718527B (zh) 2022-06-28
EP3416966B1 (en) 2021-09-29
KR102255228B1 (ko) 2021-05-25
EP3954691A1 (en) 2022-02-16
PL3416966T3 (pl) 2022-01-17
AU2017219189A1 (en) 2018-06-28

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Legal Events

Date Code Title Description
B350 Update of information on the portal [chapter 15.35 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: A CLASSIFICACAO ANTERIOR ERA: C07D 487/04

Ipc: C07D 487/04 (2006.01), A61K 31/4985 (2006.01), A61

B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]