MX2018009944A - Procedimiento para la preparacion del acido 4-fenil-5-alcoxicarbon il-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]3-oxo-5,6,8,8a- tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxilico. - Google Patents

Procedimiento para la preparacion del acido 4-fenil-5-alcoxicarbon il-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]3-oxo-5,6,8,8a- tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxilico.

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Publication number
MX2018009944A
MX2018009944A MX2018009944A MX2018009944A MX2018009944A MX 2018009944 A MX2018009944 A MX 2018009944A MX 2018009944 A MX2018009944 A MX 2018009944A MX 2018009944 A MX2018009944 A MX 2018009944A MX 2018009944 A MX2018009944 A MX 2018009944A
Authority
MX
Mexico
Prior art keywords
phenyl
tetrahyd
thiazo
dihydropyrimidin
pyrazin
Prior art date
Application number
MX2018009944A
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 MX2018009944A publication Critical patent/MX2018009944A/es

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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

La presente invención, se refiere a un procedimiento para la sintetización de un compuesto de la fórmula (I), (ver fórmula) (I), R1 es fenilo, el cual se encuentra sustituido o insustituido con uno, dos o tres sustituyentes, independientemente seleccionados de entre halógeno y alquilo C1-6; R2, es alquilo C1-6; R3, es -CxH2x-; x, es 1, 2, 3, 4, 5, 6 ó 7; ó una sal o un diastereómero de éste, farmacéuticamente aceptable, el cual es de utilidad, para la profilaxis y el tratamiento de una enfermedad vírica, en un paciente, relativa a una infección por hepatitis B, o a una enfermedad causada por la infección por hepatitis B.
MX2018009944A 2016-02-19 2017-02-16 Procedimiento para la preparacion del acido 4-fenil-5-alcoxicarbon il-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]3-oxo-5,6,8,8a- tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxilico. MX2018009944A (es)

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
MX2018009944A true MX2018009944A (es) 2018-11-09

Family

ID=58054130

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018009944A MX2018009944A (es) 2016-02-19 2017-02-16 Procedimiento para la preparacion del acido 4-fenil-5-alcoxicarbon il-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]3-oxo-5,6,8,8a- tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxilico.

Country Status (17)

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

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PT3114128T (pt) * 2014-03-07 2019-02-27 Hoffmann La Roche Novas heteroarildihidropirimidinas fundidas em 6 para o tratamento e profilaxia da infeção pelo vírus da hepatite b.
JP7260488B2 (ja) 2017-06-26 2023-04-18 サンシャイン・レイク・ファーマ・カンパニー・リミテッド ジヒドロピリミジン化合物、及び医薬におけるその使用
CN110809574A (zh) 2017-06-27 2020-02-18 詹森药业有限公司 杂芳基二氢嘧啶衍生物和治疗乙型肝炎感染的方法
KR20200072512A (ko) * 2017-10-18 2020-06-22 선샤인 레이크 파르마 컴퍼니 리미티드 디하이드로피리미딘 화합물 및 약제에서의 이의 용도
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
US20220048919A1 (en) * 2018-12-20 2022-02-17 Janssen Phrmaceutica NV Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
CN113614088A (zh) * 2019-03-25 2021-11-05 豪夫迈·罗氏有限公司 Hbv核心蛋白变构修饰剂化合物的固体形式
CN114026095A (zh) 2019-06-06 2022-02-08 豪夫迈·罗氏有限公司 用于制备4-苯基-5-烷氧基羰基-2-噻唑-2-基-1,4-二氢嘧啶-6-基]甲基]-3-氧代-5,6,8,8a-四氢-1H-咪唑并[1,5-a]吡嗪-2-基]-甲酸的替代方法
CA3140707A1 (en) 2019-06-18 2020-12-24 Helen Horton Combination of hepatitis b virus (hbv) vaccines and quinazoline derivatives
EP4003355A4 (en) * 2019-07-31 2023-07-26 Janssen Sciences Ireland Unlimited Company DIHYDROPYRIMIDE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR HBV-INDUCED DISEASE
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
CA3179165A1 (en) * 2020-04-28 2021-11-04 F. Hoffmann-La Roche Ag Process for the preparation of a chiral piperazine-2-carboxylic acid

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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
HUE034919T2 (en) 2012-08-24 2018-03-28 Sunshine Lake Pharma Co Ltd 2,4,5,6-substituted 3,6-dihydropyrimidine derivatives such as hepatitis B virus (HBV) polymerase inhibitors, for example, for the treatment of chronic hepatitis
KR20150054795A (ko) 2012-09-10 2015-05-20 에프. 호프만-라 로슈 아게 B형 간염 바이러스 감염의 치료 및 예방을 위한 6-아미노산 헤테로아릴다이하이드로피리미딘
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
PT3114128T (pt) * 2014-03-07 2019-02-27 Hoffmann La Roche Novas heteroarildihidropirimidinas fundidas em 6 para o tratamento e profilaxia da infeção pelo vírus da hepatite b.
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
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
SG11201805595TA (en) 2018-07-30
KR102255228B1 (ko) 2021-05-25
CN108718527B (zh) 2022-06-28
CN108718527A (zh) 2018-10-30
AU2017219189B2 (en) 2021-04-01
IL260153B (en) 2021-10-31
EP3954691A1 (en) 2022-02-16
SI3416966T1 (sl) 2022-01-31
JP6672471B2 (ja) 2020-03-25
IL286912A (en) 2021-10-31
AU2017219189A1 (en) 2018-06-28
BR112018016932A2 (pt) 2019-01-08
IL260153A (en) 2018-07-31
ES2899369T3 (es) 2022-03-11
HRP20211816T1 (hr) 2022-03-04
KR20180104177A (ko) 2018-09-19
PL3416966T3 (pl) 2022-01-17
US10927116B2 (en) 2021-02-23
KR20210059801A (ko) 2021-05-25
EP3416966A1 (en) 2018-12-26
JP2019507144A (ja) 2019-03-14
EP3416966B1 (en) 2021-09-29
US20190010155A1 (en) 2019-01-10
AR107633A1 (es) 2018-05-16
SG10202110927VA (en) 2021-11-29
AU2021203860A1 (en) 2021-07-08
CA3011650A1 (en) 2017-08-24
WO2017140750A1 (en) 2017-08-24

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