ES2186354T3 - Uso de dihidropirimidinas como medicamentos y nuevas sustancias para el tratamiento de hepatitis b. - Google Patents

Uso de dihidropirimidinas como medicamentos y nuevas sustancias para el tratamiento de hepatitis b.

Info

Publication number
ES2186354T3
ES2186354T3 ES99920604T ES99920604T ES2186354T3 ES 2186354 T3 ES2186354 T3 ES 2186354T3 ES 99920604 T ES99920604 T ES 99920604T ES 99920604 T ES99920604 T ES 99920604T ES 2186354 T3 ES2186354 T3 ES 2186354T3
Authority
ES
Spain
Prior art keywords
alkyl
phenyl
formula
substituted
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES99920604T
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English (en)
Inventor
Jurgen Stoltefuss
Siegfried Goldmann
Arnold Paessens
Erwin Graef
Stefan Lottmann
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Bayer AG
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Bayer AG
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Filing date
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Application filed by Bayer AG filed Critical Bayer AG
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Publication of ES2186354T3 publication Critical patent/ES2186354T3/es
Anticipated expiration legal-status Critical
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Uso de dihidropirimidinas de la fórmula general (I)**Fórmula** o su forma isomérica (Ia)**Fórmula** en las que R1 representa fenilo, furilo, tienilo, triazolilo, piridilo, cicloalquilo con 3 a 6 átomos de carbono o a restos de las fórmulas**Fórmula** estando los sistemas cíclicos antes mencionados eventualmente mono o polisustituidos de forma igual o distinta por sustituyentes seleccionados del grupo de halógeno, trifluorometilo, nitro, ciano, trifluorometoxi, carboxilo, hidroxilo, alcoxi (C1-C6), alcoxicarbonilo (C1-C6) y alquilo (C1-C6), que a su vez puede estar sustituido por arilo con 6 a 10 átomos de carbono o halógeno, y/o los sistemas cíclicos mencionados están sustituidos eventualmente por grupos de las fórmulas -SR6, NR7R8, CO-NR9R10, SO2-CF3 y -A-CH2-R11, donde R6 significa fenilo sustituido eventualmente por halógeno, R7, R8, R9 y R10 son iguales o distintos y significan hidrógeno, fenilo, fenilo sustituido por hidroxi, hidroxi, acilo (C1-C6) o alquilo (C1-C6) que, a su vez, puede estar sustituido por hidroxi, alcoxicarbonilo (C1-C6), fenilo o fenilo sustituido por hidroxi, A significa un resto O, S, SO o SO2, R11 significa fenilo que está, eventualmente, mono o polisustituido, de forma igual o distinta, por sustituyentes seleccionados del grupo de halógeno, nitro, trifluorometilo, alquilo (C1-C6) y alcoxi (C1-C6), R2 representa un resto de la fórmula -XR12 ó -NR13R14, donde X significa un enlace u oxígeno, significa hidrógeno, alcoxicarbonilo (C1-C6) de cadena lineal o ramificado o un resto hidrocarburo (C1-C8) de cadena lineal, ramificado o cíclico, saturado o insaturado, que contiene eventualmente uno o dos miembros de heterocadena iguales o distintos del grupo de O, CO, NH, -NH-alquilo(C1C4), -N-(alquilo(C1-C4))2, S ó SO2 y que está sustituido eventualmente por halógeno, nitro, ciano, hidroxi, arilo con 6 a 10 átomos de carbono o aralquilo con 6 a 10 átomos de carbono, heteroarilo o un grupo de la fórmula -NR15R16, donde R15 y R16 son iguales o distintos, significando hidrógeno, bencilo o alquilo (C1-C6), R13 y R14 son iguales o distintos, significando hidrógeno, alquilo (C1-C6) o cicloalquilo con 3 a 6 átomos de carbono, R3 representa hidrógeno, amino o a un resto de la Fórmula**Fórmula** a formilo, ciano, alquiltio (C1-C6) sustituido por hidroxi, trifluorometilo o piridilo, o a un resto hidrocarburo de cadena lineal, ramificado o cíclico, saturado o insaturado con hasta 8 átomos de carbono que eventualmente está mono o polisustituido, de forma igual o distinta, por ariloxi con 6 a 10 átomos de carbono, por azido, por halógeno, por ciano, por hidroxi, por carboxilo, por alcoxicarbonilo (C1-C6), por un anillo heterocíclico con 5 a 7 miembros, por alquiltio (C1-C6) o por alcoxi (C1-C6) que, a su vez, puede estar sustituido por azido o amino, y/o que está sustituido por triazolilo que, a su vez, puede estar sustituido hasta 3 veces por alcoxicarbonilo (C1-C6), y/o por grupos de las fórmulas -OSO2-CH3 ó (CO)a-NR17R18, donde a significa un número 0 ó1, R17 y R18 son iguales o distintos y significan hidrógeno o arilo, aralquilo con 6 a 10 átomos de carbono, o significan alquilo (C1-C6) que está sustituido eventualmente por alcoxicarbonilo (C1-C6), amino, hidroxilo, fenilo o bencilo, estando el fenilo o bencilo eventualmente mono o polisustituidos, de forma igual o distinta, por hidroxi, carboxilo, alquilo (C1-C6) o alcoxi (C1-C6), o estando alquilo (C1-C6) eventualmente sustituido por grupos de las fórmulas NH-CO-CH3 ó NH-CO-CF3, o bien R17 y R18 forman, junto con el átomo de nitrógeno, un anillo morfolino, piperidinilo o pirrolidinilo, o R3 representa fenilo que está sustituido eventualmente por metoxi, o bien R2 y R3 forman juntos un resto de la fórmula**Fórmula** R4 representa hidrógeno, a alquilo (C1-C4), a alquenilo (C2-C4), a benzoílo o a acilo con 2 a 6 átomos de carbono, R4 representa hidrógeno, a metilo, a benzoílo o a acilo (C2-C6), R5 representa piridilo, a pirimidilo o a piracinilo, y sus sales, para preparar medicamentos para el tratamiento y la profilaxis de la hepatitis B.
ES99920604T 1998-04-18 1999-04-07 Uso de dihidropirimidinas como medicamentos y nuevas sustancias para el tratamiento de hepatitis b. Expired - Lifetime ES2186354T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19817265A DE19817265A1 (de) 1998-04-18 1998-04-18 Verwendung von Dihydropyrimidinen als Arzneimittel und neue Stoffe

Publications (1)

Publication Number Publication Date
ES2186354T3 true ES2186354T3 (es) 2003-05-01

Family

ID=7864973

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99920604T Expired - Lifetime ES2186354T3 (es) 1998-04-18 1999-04-07 Uso de dihidropirimidinas como medicamentos y nuevas sustancias para el tratamiento de hepatitis b.

Country Status (12)

Country Link
US (1) US6436943B1 (es)
EP (1) EP1073642B1 (es)
JP (1) JP2002512233A (es)
AR (1) AR023308A1 (es)
AU (1) AU3813499A (es)
CA (1) CA2328733A1 (es)
DE (2) DE19817265A1 (es)
ES (1) ES2186354T3 (es)
GT (1) GT199900054A (es)
PE (1) PE20000426A1 (es)
SV (1) SV1999000048A (es)
WO (1) WO1999054312A1 (es)

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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
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KR100502395B1 (ko) * 2003-06-04 2005-07-19 (주) 비엔씨바이오팜 4-[4-(4-모르포리노)아닐리노]피리미딘 유도체, 그제조방법 및 이를 포함하는 항바이러스용 약학적 조성물.
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CN104672223B (zh) 2013-11-27 2018-03-13 广东东阳光药业有限公司 二氢嘧啶衍生物的制备方法及其中间体
RU2682672C2 (ru) 2014-03-28 2019-03-20 Саншайн Лейк Фарма Ко., Лтд. Соединения дигидропиримидина и их применение в фармацевтических препаратах
CN105859709B (zh) 2015-02-07 2018-12-04 广东东阳光药业有限公司 二氢嘧啶衍生物的复合物及其在药物中的应用
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CN116514761A (zh) 2016-07-29 2023-08-01 赛诺维信制药公司 化合物、组合物及其用途
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Also Published As

Publication number Publication date
JP2002512233A (ja) 2002-04-23
PE20000426A1 (es) 2000-06-25
US6436943B1 (en) 2002-08-20
GT199900054A (es) 2000-10-07
EP1073642A1 (de) 2001-02-07
DE59903174D1 (de) 2002-11-28
CA2328733A1 (en) 1999-10-28
AU3813499A (en) 1999-11-08
AR023308A1 (es) 2002-09-04
SV1999000048A (es) 2000-07-04
EP1073642B1 (de) 2002-10-23
WO1999054312A1 (de) 1999-10-28
DE19817265A1 (de) 1999-10-21

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