BR9909730B1 - dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas. - Google Patents

dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas.

Info

Publication number
BR9909730B1
BR9909730B1 BRPI9909730-3A BR9909730A BR9909730B1 BR 9909730 B1 BR9909730 B1 BR 9909730B1 BR 9909730 A BR9909730 A BR 9909730A BR 9909730 B1 BR9909730 B1 BR 9909730B1
Authority
BR
Brazil
Prior art keywords
dihydropyrimidines
processes
preparation
well
application
Prior art date
Application number
BRPI9909730-3A
Other languages
English (en)
Portuguese (pt)
Other versions
BR9909730A (pt
Inventor
Juergen Stoltefuss
Siegfried Goldmann
Thomas Kraemer
Karl-Heinz Schlemmer
Ulrich Niewoehner
Arnold Paessens
Erwin Graef
Stefan Lottmann
Karl Deres
Olaf Weber
Joern Stoelting
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 filed Critical
Publication of BR9909730A publication Critical patent/BR9909730A/pt
Publication of BR9909730B1 publication Critical patent/BR9909730B1/pt

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (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)
BRPI9909730-3A 1998-04-18 1999-04-07 dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas. BR9909730B1 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19817264A DE19817264A1 (de) 1998-04-18 1998-04-18 Neue Dihydropyrimidine
PCT/EP1999/002344 WO1999054326A1 (de) 1998-04-18 1999-04-07 Dihydropyrimidine

Publications (2)

Publication Number Publication Date
BR9909730A BR9909730A (pt) 2000-12-19
BR9909730B1 true BR9909730B1 (pt) 2012-09-04

Family

ID=7864972

Family Applications (2)

Application Number Title Priority Date Filing Date
BRPI9909730-3A BR9909730B1 (pt) 1998-04-18 1999-04-07 dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas.
BRPI9917862A BRPI9917862B8 (pt) 1998-04-18 1999-04-07 dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas.

Family Applications After (1)

Application Number Title Priority Date Filing Date
BRPI9917862A BRPI9917862B8 (pt) 1998-04-18 1999-04-07 dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas.

Country Status (36)

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

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WO2000058302A1 (de) * 1999-03-25 2000-10-05 Bayer Aktiengesellschaft Dihydropyrimidine und ihre verwendung zur behandlung von hepatitis b
AU5568400A (en) 1999-06-23 2001-01-09 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
DE10013126A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013125A1 (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
AU2008265397C1 (en) * 2007-06-18 2013-08-29 Sunshine Lake Pharma Co., Ltd. Bromo-phenyl substituted thiazolyl dihydropyrimidines
NZ582443A (en) 2007-07-12 2011-04-29 Novartis Ag Oral pharmaceutical solutions containing telbivudine
US20130267517A1 (en) 2012-03-31 2013-10-10 Hoffmann-La Roche Inc. Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
TWI668217B (zh) 2012-08-24 2019-08-11 廣東東陽光藥業有限公司 二氫嘧啶類化合物及其在藥物中的應用
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.
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
RU2015121940A (ru) * 2012-11-09 2016-12-27 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Альтернативные применения эффекторов сборки вируса гепатита в (hbv)
BR102014028162A2 (pt) * 2013-11-12 2015-09-08 Dow Agrosciences Llc processo para fluoração de compostos
EP3071564B1 (en) 2013-11-19 2020-08-05 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and their application in pharmaceuticals
RU2688193C1 (ru) 2013-11-27 2019-05-21 Саншайн Лейк Фарма Ко., Лтд. Процессы приготовления производных дигидропиримидина и их промежуточных соединений
WO2015144093A1 (en) 2014-03-28 2015-10-01 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and their application in pharmaceuticals
EP3150600B1 (en) 2014-05-30 2018-06-27 Qilu Pharmaceutical Co., Ltd. Dihydropyrimido loop derivative as hbv inhibitor
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
CN105859708B (zh) 2015-02-07 2020-01-21 广东东阳光药业有限公司 二氢嘧啶衍生物的盐及其在药物中的应用
WO2019001420A1 (en) * 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING INFECTIONS WITH HEPATITIS B VIRUS
US10759774B2 (en) 2017-09-28 2020-09-01 The Curators Of The University Of Missouri Inhibitors of hepatitis B virus targeting capsid assembly
MA50520A (fr) 2017-11-02 2020-09-09 Aicuris Gmbh & Co Kg Nouveaux indole-2-carboxamides à substitution pyrazolo-pipéridine hautement actifs agissant contre le virus de l'hépatite b (vhb)
BR112020008762A2 (pt) 2017-11-02 2020-10-20 Aicuris Gmbh & Co. Kg indol-2-carboxamidas amino-tiazol substituídas altamente ativas inovadoras ativas contra o vírus da hepatite b (hbv)
JP2021523160A (ja) * 2018-05-08 2021-09-02 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誘導性疾患の治療におけるその使用
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
AU2019373679A1 (en) * 2018-11-02 2021-05-27 Aicuris Gmbh & Co. Kg Novel urea 6,7-dihydro-4H-thiazolo(5,4-c)pyridines active against the hepatitis B virus (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)
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)
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)
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)
MA54560A (fr) 2018-12-20 2021-10-27 Janssen Pharmaceutica Nv Dérivés d'hétéroaryldihydropyrimidine et procédés de traitement d'infections par le virus de l'hépatite b
US20220227737A1 (en) 2019-04-30 2022-07-21 Aicuris Gmbh & Co. Kg Novel oxalyl piperazines active against the hepatitis b virus (hbv)
WO2020221824A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv)
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WO2020221826A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel indole-2-carboxamides active against the hepatitis b virus (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
CZ20003871A3 (cs) 2001-01-17
UA63998C2 (uk) 2004-02-16
KR20010042788A (ko) 2001-05-25
SI1080086T1 (en) 2003-02-28
HK1039119A1 (en) 2002-04-12
BRPI9917862A2 (enExample) 2010-12-07
PL343481A1 (en) 2001-08-27
ZA200005136B (en) 2001-03-02
JP5237332B2 (ja) 2013-07-17
WO1999054326A1 (de) 1999-10-28
CZ293482B6 (cs) 2004-05-12
MY126527A (en) 2006-10-31
US20070117812A1 (en) 2007-05-24
NO20005215L (no) 2000-12-13
IL138584A0 (en) 2001-10-31
CU23049A3 (es) 2005-06-24
CA2328780C (en) 2008-09-23
JP2002512243A (ja) 2002-04-23
ID27263A (id) 2001-03-22
EP1080086B1 (de) 2002-09-04
NZ507569A (en) 2002-04-26
DK1080086T3 (da) 2002-12-23
BR9909730A (pt) 2000-12-19
SK286407B6 (sk) 2008-09-05
PE20000427A1 (es) 2000-06-25
DE59902573D1 (en) 2002-10-10
CO5021127A1 (es) 2001-03-27
CN1305471A (zh) 2001-07-25
NO329020B1 (no) 2010-07-26
RU2245881C9 (ru) 2006-02-10
SK15652000A3 (sk) 2001-04-09
AU740318B2 (en) 2001-11-01
CA2328780A1 (en) 1999-10-28
CN1159311C (zh) 2004-07-28
AR018187A1 (es) 2001-10-31
HUP0102372A2 (hu) 2001-12-28
IL138584A (en) 2006-09-05
KR100636771B1 (ko) 2006-10-23
BRPI9917862B1 (pt) 2013-05-07
US20040167135A1 (en) 2004-08-26
DE19817264A1 (de) 1999-10-21
RU2245881C2 (ru) 2005-02-10
US7514565B2 (en) 2009-04-07
SV1999000047A (es) 2000-06-23
JP2010241837A (ja) 2010-10-28
ES2183548T3 (es) 2003-03-16
PT1080086E (pt) 2002-12-31
BRPI9917862B8 (pt) 2021-05-25
ATE223401T1 (de) 2002-09-15
TR200003011T2 (tr) 2001-01-22
HUP0102372A3 (en) 2003-01-28
BG104812A (en) 2001-06-29
GT199900056A (es) 2000-10-07
NO321985B1 (no) 2006-07-31
TW548274B (en) 2003-08-21
AU3813399A (en) 1999-11-08
BG64649B1 (bg) 2005-10-31
PL193898B1 (pl) 2007-03-30
WO1999054326A8 (de) 1999-12-29
EP1080086A1 (de) 2001-03-07
NO20005215D0 (no) 2000-10-17
JP4590097B2 (ja) 2010-12-01
US6696451B1 (en) 2004-02-24

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