PE07762015A1 - 6-amino-heteroarildihidropirimidinas for the treatment and prophylaxis of infection of the Hepatitis B Virus - Google Patents

6-amino-heteroarildihidropirimidinas for the treatment and prophylaxis of infection of the Hepatitis B Virus

Info

Publication number
PE07762015A1
PE07762015A1 PE2015000297A PE0002972015A PE07762015A1 PE 07762015 A1 PE07762015 A1 PE 07762015A1 PE 2015000297 A PE2015000297 A PE 2015000297A PE 0002972015 A PE0002972015 A PE 0002972015A PE 07762015 A1 PE07762015 A1 PE 07762015A1
Authority
PE
Peru
Prior art keywords
compounds
hepatitis
heteroarildihidropirimidinas
prophylaxis
virus
Prior art date
Application number
PE2015000297A
Other languages
Spanish (es)
Inventor
Lei Guo
taishan Hu
Yimin Hu
Buelent Kocer
Xianfeng Lin
Haixia Liu
Alexander V Mayweg
Zongxing Qiu
Hong Shen
Guozhi Tang
Lisha Wang
Guolong Wu
Shixiang Yan
Weixing Zhang
Mingwei Zhou
Wei Zhu
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
Family has litigation
Priority to CNPCT/CN2012/081190 priority Critical
Priority to CNPCT/CN2013/080301 priority
Priority to CNPCT/CN2013/081196 priority
Priority to CNPCT/CN2013/081287 priority
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE07762015A1 publication Critical patent/PE07762015A1/en
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49212746&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE07762015(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

La invencion proporciona nuevos compuestos que tienen la formula general: en la que R1, R2, R3, R4 y A tienen los significados aqui definidos, composiciones que contienen los compuestos y metodos de uso de los compuestos. The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A have the meanings defined here, compositions containing the compounds and methods of using the compounds. Los compuestos actuan como inhibidores del virus de la Hepatitis B. Son compuestos preferidos: 6-((S)-2-carboxi-4, 4-difluor-pirrolidin-1-ilmetil)-4-(2-cloro-4-fluor-fenil)-2-tiazol-2-il-1, 4-dihidro-pirimidina-5-carboxilato de metilo; The compounds act as inhibitors of the Hepatitis B. Preferred compounds are: 6 - ((S) -2-carboxy-4, 4-difluoro-pyrrolidin-1-ylmethyl) -4- (2-chloro-4-fluoro -phenyl) -2-thiazol-2-yl-1, 4-dihydro-pyrimidine-5-carboxylate; (R)-6-((S)-2-carboxi-4, 4-difluor-pirrolidin-1-ilmetil)-4-(2-cloro-4-fluor-fenil)-2-tiazol-2-il-1, 4-dihidro-pirimidina-5-carboxilato de metilo; (R) -6 - ((S) -2-carboxy-4, 4-difluoro-pyrrolidin-1-ylmethyl) -4- (2-chloro-4-fluoro-phenyl) -2-thiazol-2-yl- 1, 4-dihydro-pyrimidine-5-carboxylate; entre otros among others
PE2015000297A 2012-09-10 2013-09-06 6-amino-heteroarildihidropirimidinas for the treatment and prophylaxis of infection of the Hepatitis B Virus PE07762015A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CNPCT/CN2012/081190 2012-09-10
CNPCT/CN2013/080301 2013-07-29
CNPCT/CN2013/081196 2013-08-09
CNPCT/CN2013/081287 2013-08-12

Publications (1)

Publication Number Publication Date
PE07762015A1 true PE07762015A1 (en) 2015-05-21

Family

ID=49212746

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015000297A PE07762015A1 (en) 2012-09-10 2013-09-06 6-amino-heteroarildihidropirimidinas for the treatment and prophylaxis of infection of the Hepatitis B Virus

Country Status (22)

Country Link
US (1) US9447086B2 (en)
EP (1) EP2892893B2 (en)
JP (1) JP6113285B2 (en)
KR (1) KR20150054795A (en)
CN (1) CN104603125A (en)
AR (1) AR092503A1 (en)
AU (1) AU2013311705A1 (en)
BR (1) BR112015004113A2 (en)
CA (1) CA2881322A1 (en)
CL (1) CL2015000482A1 (en)
CO (1) CO7170160A2 (en)
EA (1) EA201590384A1 (en)
ES (1) ES2617906T3 (en)
HK (1) HK1210152A1 (en)
IL (1) IL236691D0 (en)
MX (1) MX2015002954A (en)
PE (1) PE07762015A1 (en)
PH (1) PH12015500347A1 (en)
SG (1) SG11201500377UA (en)
TW (1) TW201416360A (en)
WO (1) WO2014037480A1 (en)
ZA (1) ZA201500580B (en)

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