BRPI9917862B8 - 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
BRPI9917862B8
BRPI9917862B8 BRPI9917862A BR9917862A BRPI9917862B8 BR PI9917862 B8 BRPI9917862 B8 BR PI9917862B8 BR PI9917862 A BRPI9917862 A BR PI9917862A BR 9917862 A BR9917862 A BR 9917862A BR PI9917862 B8 BRPI9917862 B8 BR PI9917862B8
Authority
BR
Brazil
Prior art keywords
preparation
application
dihydropyrimidines
well
compounds
Prior art date
Application number
BRPI9917862A
Other languages
English (en)
Portuguese (pt)
Other versions
BRPI9917862A2 (enExample
BRPI9917862B1 (pt
Inventor
Paessens Arnold
Graef Erwin
Stoelting Joern
Stoltefuss Juergen
Deres Karl
Schlemmer Karl-Heinz
Weber Olaf
Goldmann Siegfried
Lottmann Stefan
Kraemer Thomas
Niewoehner Ulrich
Original Assignee
Bayer Ip Gmbh
Bayer Pharma AG
Bayer Schering Pharma Ag
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 Bayer Ip Gmbh, Bayer Pharma AG, Bayer Schering Pharma Ag filed Critical Bayer Ip Gmbh
Publication of BRPI9917862A2 publication Critical patent/BRPI9917862A2/pt
Publication of BRPI9917862B1 publication Critical patent/BRPI9917862B1/pt
Publication of BRPI9917862B8 publication Critical patent/BRPI9917862B8/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)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)
BRPI9917862A 1998-04-18 1999-04-07 dihidropirimidinas, bem como processo para a preparação e aplicação das mesmas. BRPI9917862B8 (pt)

Applications Claiming Priority (3)

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
BRPI9909730 1999-04-07

Publications (3)

Publication Number Publication Date
BRPI9917862A2 BRPI9917862A2 (enExample) 2010-12-07
BRPI9917862B1 BRPI9917862B1 (pt) 2013-05-07
BRPI9917862B8 true BRPI9917862B8 (pt) 2021-05-25

Family

ID=7864972

Family Applications (2)

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.
BRPI9909730-3A BR9909730B1 (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
BRPI9909730-3A BR9909730B1 (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) BRPI9917862B8 (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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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
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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
RU2452733C2 (ru) * 2007-04-27 2012-06-10 Пэдью Фарма Л.П. Антагонисты trpv1 и их применение
KR101173892B1 (ko) 2007-06-18 2012-08-16 선샤인 레이크 파르마 컴퍼니 리미티드 브로모-페닐 치환된 티아졸릴 디하이드로피리미딘
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MY182403A (en) 2012-08-24 2021-01-25 Sunshine Lake Pharma Co Ltd Dihydropyrimidine compounds and their application in pharmaceuticals
KR20150054795A (ko) 2012-09-10 2015-05-20 에프. 호프만-라 로슈 아게 B형 간염 바이러스 감염의 치료 및 예방을 위한 6-아미노산 헤테로아릴다이하이드로피리미딘
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
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JP6524081B2 (ja) 2013-11-19 2019-06-05 サンシャイン・レイク・ファーマ・カンパニー・リミテッドSunshine Lake Pharma Co.,Ltd. ジヒドロピリミジン化合物及び医薬におけるその適用
AU2014356984B2 (en) 2013-11-27 2018-01-04 Sunshine Lake Pharma Co., Ltd. Processes for preparing dihydropyrimidine derivatives and intermediates thereof
KR20160133563A (ko) 2014-03-28 2016-11-22 선샤인 레이크 파르마 컴퍼니 리미티드 다이하이드로피리미딘 화합물 및 이의 약제학적 용도
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
ES2687606T3 (es) * 2014-05-30 2018-10-26 Qilu Pharmaceutical Co., Ltd. Derivado de bucle de dihidropirimido como inhibidor de HBV
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
JP2020525490A (ja) * 2017-06-27 2020-08-27 ヤンセン ファーマシューティカ エヌ.ベー. ヘテロアリールジヒドロピリミジン誘導体及びb型肝炎感染を治療する方法
US10759774B2 (en) 2017-09-28 2020-09-01 The Curators Of The University Of Missouri Inhibitors of hepatitis B virus targeting capsid assembly
MX2020004839A (es) 2017-11-02 2020-10-16 Aicuris Gmbh & Co Kg Nuevas indol-2-carboxamidas sustituidas con amino-tiazol, de alta actividad, activas contra el virus de la hepatitis b (vhb).
AR115131A1 (es) 2017-11-02 2020-12-02 Aicuris Gmbh & Co Kg Altamente activas indolo-2-carboxamidas sustituidas con pirazolo-pirimidina activas contra el virus de la hepatitis b (vhb)
MA52586A (fr) * 2018-05-08 2021-03-17 Janssen Sciences Ireland Unlimited Co Dérivés de dihydropyrimidine et leurs utilisations dans le traitement d'une infection par le virus de l'hépatite b ou de maladies induites par le virus de l'hépatite b
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)
UY38434A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activas contra el virus de la hepatitis b (hbv)
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)
AR117188A1 (es) 2018-11-02 2021-07-21 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)
AR116947A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas-indol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
EP3873913A1 (en) * 2018-11-02 2021-09-08 AiCuris GmbH & Co. KG Novel urea 6,7-dihydro-4h-thiazolo[5,4-c]pyridines active against the hepatitis b virus (hbv)
AU2019409191A1 (en) 2018-12-20 2021-05-27 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis B infections
CN113767102A (zh) 2019-04-30 2021-12-07 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的苯基和吡啶基脲类化合物
WO2020221811A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel oxalyl piperazines active against the hepatitis b virus (hbv)
AU2020265392A1 (en) 2019-04-30 2021-12-23 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis B virus (HBV)
CN113767101A (zh) 2019-04-30 2021-12-07 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的吲哚-2-甲酰胺类化合物
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
PL343481A1 (en) 2001-08-27
CN1159311C (zh) 2004-07-28
SV1999000047A (es) 2000-06-23
DK1080086T3 (da) 2002-12-23
KR20010042788A (ko) 2001-05-25
CA2328780A1 (en) 1999-10-28
AU3813399A (en) 1999-11-08
EP1080086A1 (de) 2001-03-07
EP1080086B1 (de) 2002-09-04
JP2010241837A (ja) 2010-10-28
UA63998C2 (uk) 2004-02-16
US6696451B1 (en) 2004-02-24
CN1305471A (zh) 2001-07-25
ZA200005136B (en) 2001-03-02
TR200003011T2 (tr) 2001-01-22
JP5237332B2 (ja) 2013-07-17
RU2245881C2 (ru) 2005-02-10
WO1999054326A1 (de) 1999-10-28
ID27263A (id) 2001-03-22
JP2002512243A (ja) 2002-04-23
NO321985B1 (no) 2006-07-31
PT1080086E (pt) 2002-12-31
PE20000427A1 (es) 2000-06-25
NO20005215D0 (no) 2000-10-17
BR9909730A (pt) 2000-12-19
NO20005215L (no) 2000-12-13
ES2183548T3 (es) 2003-03-16
RU2245881C9 (ru) 2006-02-10
AR018187A1 (es) 2001-10-31
CZ20003871A3 (cs) 2001-01-17
BRPI9917862A2 (enExample) 2010-12-07
NZ507569A (en) 2002-04-26
US20040167135A1 (en) 2004-08-26
BG104812A (en) 2001-06-29
KR100636771B1 (ko) 2006-10-23
US20070117812A1 (en) 2007-05-24
TW548274B (en) 2003-08-21
NO329020B1 (no) 2010-07-26
SI1080086T1 (en) 2003-02-28
CZ293482B6 (cs) 2004-05-12
BR9909730B1 (pt) 2012-09-04
SK286407B6 (sk) 2008-09-05
DE19817264A1 (de) 1999-10-21
SK15652000A3 (sk) 2001-04-09
AU740318B2 (en) 2001-11-01
PL193898B1 (pl) 2007-03-30
CO5021127A1 (es) 2001-03-27
GT199900056A (es) 2000-10-07
US7514565B2 (en) 2009-04-07
IL138584A0 (en) 2001-10-31
HUP0102372A3 (en) 2003-01-28
HK1039119A1 (en) 2002-04-12
MY126527A (en) 2006-10-31
BG64649B1 (bg) 2005-10-31
DE59902573D1 (en) 2002-10-10
ATE223401T1 (de) 2002-09-15
CU23049A3 (es) 2005-06-24
BRPI9917862B1 (pt) 2013-05-07
CA2328780C (en) 2008-09-23
WO1999054326A8 (de) 1999-12-29
JP4590097B2 (ja) 2010-12-01
HUP0102372A2 (hu) 2001-12-28
IL138584A (en) 2006-09-05

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