TW548274B - Dihydropyrimidines having hepatitis B therapeutic efficacy - Google Patents

Dihydropyrimidines having hepatitis B therapeutic efficacy Download PDF

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Publication number
TW548274B
TW548274B TW088106067A TW88106067A TW548274B TW 548274 B TW548274 B TW 548274B TW 088106067 A TW088106067 A TW 088106067A TW 88106067 A TW88106067 A TW 88106067A TW 548274 B TW548274 B TW 548274B
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Taiwan
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patent application
scope
cns
national standard
paper size
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TW088106067A
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English (en)
Chinese (zh)
Inventor
Jorn Stolting
Juergen Stoltefuss
Siegfried Goldmann
Thomas Kramer
Karl-Heinz Schlemmer
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Bayer Ag
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • 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
    • A61K31/505Pyrimidines; 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Saccharide Compounds (AREA)
TW088106067A 1998-04-18 1999-04-16 Dihydropyrimidines having hepatitis B therapeutic efficacy TW548274B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19817264A DE19817264A1 (de) 1998-04-18 1998-04-18 Neue Dihydropyrimidine

Publications (1)

Publication Number Publication Date
TW548274B true TW548274B (en) 2003-08-21

Family

ID=7864972

Family Applications (1)

Application Number Title Priority Date Filing Date
TW088106067A TW548274B (en) 1998-04-18 1999-04-16 Dihydropyrimidines having hepatitis B therapeutic efficacy

Country Status (36)

Country Link
US (3) US6696451B1 (OSRAM)
EP (1) EP1080086B1 (OSRAM)
JP (2) JP4590097B2 (OSRAM)
KR (1) KR100636771B1 (OSRAM)
CN (1) CN1159311C (OSRAM)
AR (1) AR018187A1 (OSRAM)
AT (1) ATE223401T1 (OSRAM)
AU (1) AU740318B2 (OSRAM)
BG (1) BG64649B1 (OSRAM)
BR (2) BR9909730B1 (OSRAM)
CA (1) CA2328780C (OSRAM)
CO (1) CO5021127A1 (OSRAM)
CU (1) CU23049A3 (OSRAM)
CZ (1) CZ293482B6 (OSRAM)
DE (2) DE19817264A1 (OSRAM)
DK (1) DK1080086T3 (OSRAM)
ES (1) ES2183548T3 (OSRAM)
GT (1) GT199900056A (OSRAM)
HU (1) HUP0102372A3 (OSRAM)
ID (1) ID27263A (OSRAM)
IL (2) IL138584A0 (OSRAM)
MY (1) MY126527A (OSRAM)
NO (2) NO321985B1 (OSRAM)
NZ (1) NZ507569A (OSRAM)
PE (1) PE20000427A1 (OSRAM)
PL (1) PL193898B1 (OSRAM)
PT (1) PT1080086E (OSRAM)
RU (1) RU2245881C9 (OSRAM)
SI (1) SI1080086T1 (OSRAM)
SK (1) SK286407B6 (OSRAM)
SV (1) SV1999000047A (OSRAM)
TR (1) TR200003011T2 (OSRAM)
TW (1) TW548274B (OSRAM)
UA (1) UA63998C2 (OSRAM)
WO (1) WO1999054326A1 (OSRAM)
ZA (1) ZA200005136B (OSRAM)

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AU4289100A (en) * 1999-03-25 2000-10-16 Bayer Aktiengesellschaft Dihydropyrimidines and their use in the treatment of hepatitis
WO2000078730A1 (en) 1999-06-23 2000-12-28 Ajinomoto Co., Inc. Novel dihydropyrimidine derivatives
AU3009801A (en) * 1999-12-22 2001-07-03 Bayer Aktiengesellschaft Combinations of medicaments for treating viral diseases
DE10012823A1 (de) 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013125A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013126A1 (de) * 2000-03-17 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
US20040092735A1 (en) * 2002-11-08 2004-05-13 Orchid Chemicals & Pharmaceuticals Limited Process for the preparation of cefuroxime sodium
CN101104617B (zh) * 2006-07-10 2010-06-23 北京摩力克科技有限公司 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
CN101104604B (zh) * 2006-07-10 2011-03-02 北京摩力克科技有限公司 光学纯二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
RU2452733C2 (ru) * 2007-04-27 2012-06-10 Пэдью Фарма Л.П. Антагонисты trpv1 и их применение
PT2159224E (pt) * 2007-06-18 2012-10-24 Sunshine Lake Pharma Co Ltd Tiazolil dihidropirimidinas substituídas com bromo-fenilo
WO2009007426A1 (en) 2007-07-12 2009-01-15 Novartis Ag Oral pharmaceutical solutions containing telbivudine
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DK2888241T3 (en) 2012-08-24 2017-10-23 Sunshine Lake Pharma Co Ltd 2,4,5,6-Substituted 3,6-dihydropyrimidine derivatives such as hepatitis B virus (HBV) polymerase inhibitors for the treatment of, for example, chronic hepatitis
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
CN103664899B (zh) * 2012-09-11 2017-06-16 广东东阳光药业有限公司 杂芳基取代的二氢嘧啶类化合物及其在药物中的应用
US20150292045A1 (en) * 2012-11-09 2015-10-15 Indiana University Research And Technology Corporation Alternative uses for hbv assembly effectors
BR102014028162A2 (pt) * 2013-11-12 2015-09-08 Dow Agrosciences Llc processo para fluoração de compostos
RU2678990C1 (ru) 2013-11-19 2019-02-05 Саншайн Лейк Фарма Ко., Лтд. Соединения дигидропиримидина и их применение в фармацевтических препаратах
AU2014356986B2 (en) 2013-11-27 2018-01-04 Sunshine Lake Pharma Co., Ltd. Processes for preparing dihydropyrimidine derivatives and intermediates thereof
WO2015144093A1 (en) 2014-03-28 2015-10-01 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and their application in pharmaceuticals
RU2693897C2 (ru) * 2014-05-30 2019-07-05 Килу Фармасьютикал Ко., Лтд. Производное на основе дигидропиримидо-кольца в качестве ингибитора hbv
CN105153164B (zh) * 2014-05-30 2018-10-30 齐鲁制药有限公司 作为hbv抑制剂的二氢嘧啶并环衍生物
WO2016124126A1 (en) 2015-02-07 2016-08-11 Sunshine Lake Pharma Co., Ltd. Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals
EP3645516A4 (en) * 2017-06-27 2021-07-07 Janssen Pharmaceutica NV HETEROARYLDIHYDROPYRIMIDE DERIVATIVES AND METHODS OF TREATMENT OF HEPATITIS B INFECTIONS
US10759774B2 (en) 2017-09-28 2020-09-01 The Curators Of The University Of Missouri Inhibitors of hepatitis B virus targeting capsid assembly
US11267825B2 (en) 2017-11-02 2022-03-08 Aicuris Gmbh & Co. Kg Highly active amino-thiazole substituted indole-2-carboxamides active against the hepatitis B virus (HBV)
CU20200045A7 (es) 2017-11-02 2021-03-11 Aicuris Gmbh & Co Kg Derivados de indol-2-carboxamidas sustituidos con pirazolo-piperidina activos contra el virus de la hepatitis b (vhb)
AU2019266729A1 (en) * 2018-05-08 2021-03-11 Janssen Sciences Ireland Unlimited Company Dihydropyrimidine derivatives and uses thereof in the treatment of HBV infection or of HBV-induced diseases
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
UY38439A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Novedosas urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb)
UY38437A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (hbv)
AR117189A1 (es) 2018-11-02 2021-07-21 Aicuris Gmbh & Co Kg Derivados de 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activos contra el virus de la hepatitis b (vhb)
KR20210098985A (ko) * 2018-11-02 2021-08-11 아이쿠리스 게엠베하 운트 코. 카게 B형 간염 바이러스 (hbv)에 대해 활성인 신규 우레아 6,7-디히드로-4h-티아졸로[5,4-c]피리딘
AR116948A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb)
UY38436A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a] pirazinindol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
CA3124317A1 (en) 2018-12-20 2020-06-25 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
CN113748111A (zh) 2019-04-30 2021-12-03 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新型草酰哌嗪类化合物
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BR112021021564A2 (pt) 2019-04-30 2022-01-04 Aicuris Gmbh & Co Kg Indol-2-carboxamidas inovadoras ativas contra o vírus da hepatite b (hbv)
WO2020255016A1 (en) 2019-06-18 2020-12-24 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and dihydropyrimidine derivatives as capsid assembly modulators

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Also Published As

Publication number Publication date
NO20045259L (no) 2000-12-13
US6696451B1 (en) 2004-02-24
CN1305471A (zh) 2001-07-25
RU2245881C2 (ru) 2005-02-10
ATE223401T1 (de) 2002-09-15
SK286407B6 (sk) 2008-09-05
AU3813399A (en) 1999-11-08
AR018187A1 (es) 2001-10-31
BG64649B1 (bg) 2005-10-31
EP1080086A1 (de) 2001-03-07
JP4590097B2 (ja) 2010-12-01
ES2183548T3 (es) 2003-03-16
BG104812A (en) 2001-06-29
AU740318B2 (en) 2001-11-01
DE59902573D1 (en) 2002-10-10
US20040167135A1 (en) 2004-08-26
JP2002512243A (ja) 2002-04-23
CN1159311C (zh) 2004-07-28
CA2328780C (en) 2008-09-23
EP1080086B1 (de) 2002-09-04
NO20005215D0 (no) 2000-10-17
HUP0102372A2 (hu) 2001-12-28
IL138584A (en) 2006-09-05
DE19817264A1 (de) 1999-10-21
PT1080086E (pt) 2002-12-31
CU23049A3 (es) 2005-06-24
HK1039119A1 (en) 2002-04-12
CZ20003871A3 (cs) 2001-01-17
PE20000427A1 (es) 2000-06-25
ID27263A (id) 2001-03-22
HUP0102372A3 (en) 2003-01-28
KR100636771B1 (ko) 2006-10-23
PL193898B1 (pl) 2007-03-30
GT199900056A (es) 2000-10-07
BR9909730B1 (pt) 2012-09-04
JP5237332B2 (ja) 2013-07-17
NO321985B1 (no) 2006-07-31
BRPI9917862B1 (pt) 2013-05-07
BR9909730A (pt) 2000-12-19
NO329020B1 (no) 2010-07-26
PL343481A1 (en) 2001-08-27
IL138584A0 (en) 2001-10-31
CZ293482B6 (cs) 2004-05-12
US7514565B2 (en) 2009-04-07
UA63998C2 (uk) 2004-02-16
RU2245881C9 (ru) 2006-02-10
TR200003011T2 (tr) 2001-01-22
WO1999054326A8 (de) 1999-12-29
US20070117812A1 (en) 2007-05-24
MY126527A (en) 2006-10-31
BRPI9917862A2 (OSRAM) 2010-12-07
SI1080086T1 (en) 2003-02-28
BRPI9917862B8 (pt) 2021-05-25
KR20010042788A (ko) 2001-05-25
NZ507569A (en) 2002-04-26
SK15652000A3 (sk) 2001-04-09
DK1080086T3 (da) 2002-12-23
NO20005215L (no) 2000-12-13
SV1999000047A (es) 2000-06-23
WO1999054326A1 (de) 1999-10-28
CA2328780A1 (en) 1999-10-28
ZA200005136B (en) 2001-03-02
JP2010241837A (ja) 2010-10-28
CO5021127A1 (es) 2001-03-27

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