BR9912142A - 6-benzil-4-oxipirimidinas substituìdas, processopara sua preparação e composições contendo-as - Google Patents

6-benzil-4-oxipirimidinas substituìdas, processopara sua preparação e composições contendo-as

Info

Publication number
BR9912142A
BR9912142A BR9912142-5A BR9912142A BR9912142A BR 9912142 A BR9912142 A BR 9912142A BR 9912142 A BR9912142 A BR 9912142A BR 9912142 A BR9912142 A BR 9912142A
Authority
BR
Brazil
Prior art keywords
benzyl
substituted
treatment
oxypyrimidines
preparation
Prior art date
Application number
BR9912142-5A
Other languages
English (en)
Inventor
Paolo La Colla
Marino Artico
Original Assignee
Novirio Pharmaceuticals Ltd
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 Novirio Pharmaceuticals Ltd filed Critical Novirio Pharmaceuticals Ltd
Publication of BR9912142A publication Critical patent/BR9912142A/pt

Links

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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom

Abstract

"6-BENZIL-4-OXIPIRIMIDINAS SUBSTITUìDAS, PROCESSOPARA SUA PREPARAçãO E COMPOSIçõES CONTENDO-AS".A invenção se refere a novas 6-benzil-4-oxopirimidinas substituídasde fórmula geral (A) . Esses compostos impedem a transcriptasereversa codificada pelo vírus da imunodeficiência humana (HIV) oupor sais dos mesmos aceitáveis em termos farmacêuticos, eencontram sua aplicação na prevenção e no tratamento deinfecções por HIV e no tratamento da síndrome daimunodeficiência adquirida resultante (AIDS). Composiçõesfarmacêuticas, que contêm os compostos, e um método de usodos presentes compostos e de outros agentes para o tratamentoda AIDS e de uma infecção viral por HIV também são divisados.
BR9912142-5A 1998-07-17 1999-07-19 6-benzil-4-oxipirimidinas substituìdas, processopara sua preparação e composições contendo-as BR9912142A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT1998CA000015A IT1305313B1 (it) 1998-07-17 1998-07-17 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
PCT/EP1999/005134 WO2000003998A1 (en) 1998-07-17 1999-07-19 Substituted 6-benzyl-4-oxopyrimidines, process for their preparation and pharmaceutical compositions containing them

Publications (1)

Publication Number Publication Date
BR9912142A true BR9912142A (pt) 2001-10-30

Family

ID=11347180

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9912142-5A BR9912142A (pt) 1998-07-17 1999-07-19 6-benzil-4-oxipirimidinas substituìdas, processopara sua preparação e composições contendo-as

Country Status (10)

Country Link
US (2) US6635636B1 (pt)
EP (1) EP1098887A1 (pt)
KR (1) KR100578478B1 (pt)
CN (1) CN1309647A (pt)
AU (2) AU771209B2 (pt)
BR (1) BR9912142A (pt)
CA (1) CA2338014A1 (pt)
HK (1) HK1039122A1 (pt)
IT (1) IT1305313B1 (pt)
WO (1) WO2000003998A1 (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1305313B1 (it) * 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
US6136335A (en) * 1998-12-31 2000-10-24 Hughes Institute Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity
WO2001007027A2 (en) * 1999-07-22 2001-02-01 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives for the treatment of viral diseases
US6545007B2 (en) 2000-11-17 2003-04-08 Idenix (Cayman) Limited Methods for inhibiting the transmission of HIV using topically applied substituted 6-benzyl-4-oxopyrimidines
AU2003287389B2 (en) 2002-10-31 2010-08-12 Metabasis Therapeutics, Inc. Novel cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs
US7642277B2 (en) 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors
US20050014774A1 (en) * 2003-04-28 2005-01-20 Richard Storer Oxo-pyrimidine compounds
JP4675959B2 (ja) * 2004-07-27 2011-04-27 エフ．ホフマン−ラ ロシュ アーゲー 非ヌクレオシド逆転写酵素阻害剤としてのベンジルトリアゾロン化合物
US8293778B2 (en) 2004-07-27 2012-10-23 Roche Palo Alto Llc Heterocyclic antiviral compounds
KR100803481B1 (ko) * 2004-07-27 2008-02-14 에프. 호프만-라 로슈 아게 비-뉴클레오사이드 역전사효소 억제제로서의벤질트라이아졸론 화합물
ITRM20050512A1 (it) * 2005-10-13 2007-04-14 Univ Siena Derivati 6-pirimidinici e pirimidinonici, e loro uso.
BRPI0720436A2 (pt) * 2006-12-13 2014-01-07 Hoffmann La Roche Inibidores de transcriptase reversa de não-nucleosídeo
CN100519540C (zh) * 2007-01-09 2009-07-29 云南大学 S-dabo类化合物、其合成方法和用途
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
WO2015123352A1 (en) 2014-02-13 2015-08-20 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
SI3125894T1 (sl) 2014-04-01 2020-12-31 Merck Sharp & Dohme Corp. Predzdravila inhibitorjev reverzne transkriptaze HIV
JP2017520545A (ja) 2014-07-02 2017-07-27 リガンド・ファーマシューティカルズ・インコーポレイテッド プロドラッグ化合物およびそれらの使用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3956302A (en) * 1974-05-24 1976-05-11 The Upjohn Company Substituted pyrimidines
GB9012592D0 (en) 1990-06-06 1990-07-25 Smithkline Beecham Intercredit Compounds
US5314917A (en) 1991-03-22 1994-05-24 E. B. Michaels Research Associates, Inc. Method for inactivating enveloped viruses and sperm
KR0151811B1 (ko) * 1993-12-21 1998-10-15 강박광 신규한 항바이러스성 2,4-피리미딘디온 유도체 및 그의 제조방법
KR100187475B1 (ko) * 1996-05-17 1999-05-01 이서봉 1-아릴-4-옥소 피롤로(3,2-c)퀴놀린 유도체의 제조방법
US5998411A (en) * 1998-03-17 1999-12-07 Hughes Institute Heterocyclic nonnucleoside inhibitors of reverse transcriptase
IT1305313B1 (it) 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
US6177437B1 (en) 1998-09-04 2001-01-23 University Of Massachusetts Medical Center Inhibitors of Herpes Simplex virus uracil-DNA glycosylase
US6136335A (en) * 1998-12-31 2000-10-24 Hughes Institute Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity
US6117904A (en) 1999-09-03 2000-09-12 Murphy; Donald M. Treatment of pruritus
US6545007B2 (en) * 2000-11-17 2003-04-08 Idenix (Cayman) Limited Methods for inhibiting the transmission of HIV using topically applied substituted 6-benzyl-4-oxopyrimidines
ATE451921T1 (de) * 2001-04-11 2010-01-15 Idenix Cayman Ltd Phenylindole zur behandlung von hiv

Also Published As

Publication number Publication date
AU2004200446A1 (en) 2004-03-11
US20040092539A1 (en) 2004-05-13
CN1309647A (zh) 2001-08-22
ITCA980015A1 (it) 2000-01-17
KR20010099594A (ko) 2001-11-09
EP1098887A1 (en) 2001-05-16
US6635636B1 (en) 2003-10-21
CA2338014A1 (en) 2000-01-27
KR100578478B1 (ko) 2006-05-11
WO2000003998A1 (en) 2000-01-27
AU5284899A (en) 2000-02-07
AU771209B2 (en) 2004-03-18
IT1305313B1 (it) 2001-05-04
HK1039122A1 (zh) 2002-04-12

Similar Documents

Publication Publication Date Title
BR9912142A (pt) 6-benzil-4-oxipirimidinas substituìdas, processopara sua preparação e composições contendo-as
BRPI0413469A (pt) derivados de piperazina para o tratamento de infecções por hiv
TR200002761T2 (tr) HIV enfeksiyonlarının tedavisi için üç-ikameli 1,3,5-triazin türevleri.
BR0210350A (pt) Nucleosìdeos 4'-substituìdos
BRPI9810519A (pt) derivados de 4''-substituído-9-desoxo-9a-aza-9a-homoeritromicina a e composição farmacêutica compreendendo os mesmos.
BR0213242A (pt) Composto ou um seu sal ou solvato, composto e seus sais de adição de ácido fisiologicamente aceitáveis, composição farmacêutica, método de tratamento de um ou mais distúrbios, uso de um composto, e, processo de preparação de um composto
MX9403380A (es) Inhibidores de proteasa de vih utiles para el tratamiento de sida.
BR0213522A (pt) Composto, composição farmacêutica, métodos de inibir a hiv integrase e para prevenir ou tratar a infecção pelo hiv ou para prevenir, tratar ou retardar o inìcio da aids em um paciente, e, combinação útil para tratar ou prevenir a infecção pelo hiv ou para prevenir, tratar ou retardar o inìcio da aids
AR024227A1 (es) Pirimidinas inhibidoras de replicacion de hiv, un proceso para su preparacion, el uso de las mismas para la manufactura de un medicamento, composiciones farmaceuticas, y un proceso para prepararlas
BR0209267A (pt) Pirimidinas fundidas como antagonistas do fator de liberação de corticotropina (crf)
BR9811055A (pt) Composto , uso do mesmo, composição farmacêutica, e, processo para tratamento de doença ou condição médica mediada pelo fator xa
BR0013771A (pt) Composto, métodos de tratamento de uma infecção viral em um mamìfero, de inibir a transcriptase reversa do hiv, e de prevenção da infecção do hiv ou de tratar a infecção do hiv, uso de um composto, e, composição farmacêutica
BR0113710A (pt) Compostos, processo para a preparação e utilização dos mesmos, composição farmacêutica, processo para o tratamento e profilaxia de artrite, enfermidades cardiovasculares, diabetes, insuficiência renal, distúrbios alimentares e obesidade
BR9712672A (pt) Derivados heterocìclicos que inibem o fator xa
BR9915967A (pt) Derivados de propanolamina substituìdos por arila, proceso para sua preparação, medicamentos contendo estes compostos e seu uso
BRPI0208811B8 (pt) derivados de pirazol, seu uso e processo de preparação, bem como composição farmacêutica compreendendo os mesmos
EA199901031A1 (ru) Производные бензимидазола
BR9815166A (pt) "método de inibição da replicação de vìrus, composto, método de inibição da replicação de citomegalovìrus, composto antiviral, utilização de um composto, composição farmacêutica, composição farmacêutica inibidora da replicação de vìrus e de citomegalovìrus e composição farmacêutica antiviral"
BR0207752A (pt) Composto, sais de sódio, cálcio, potássio, magnésio, colina, etanolamina e trietilamina dos compostos, formas dos mesmos, métodos de tratamento ou de prevenção de uma infeção viral em um ser humano e de tratamento dos vìrus mutantes hiv uso de um composto, composição farmacêutica, e, processo para a preparação dos compostos
BR9909976A (pt) Composto, processo para a obtenção de compostos, derivado litiado, composições farmacêuticas, e, processos de tratamento de doenças relacionadas com hiv e de tratamento de infecção de hiv
BRPI0608245A2 (pt) compostos; processo para a sua fabricação; composições farmacêuticas; método para o tratamento e/ou prevenção de doenças que estejam associadas à modulação de receptores de sst subtipo 5 e uso dos compostos
BR9910179A (pt) Composto, composição farmacêutica, uso de um composto, e, processo para tratar uma doença ou condição mediada por fator xa em um animal de sangue quente
BR0212069A (pt) Agentes antidiabéticos orais
BR9906373A (pt) Compostos pirimidinona, composições farmacêuticas contendo os compostos e processos para a preparação dos mesmos
PT92949A (pt) Processo para a preparacao de composicoes farmaceuticas contendo derivados da cisteina para o tratamento de doencas associadas com infeccoes provocadas por virus da imunodeficiencia humano

Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: IDENIX PHARMACEUTICALS, INC (KY)

Free format text: ALTERADO DE: NOVIRIO PHARMACEUTICALS LIMITED

B25A Requested transfer of rights approved

Owner name: IDENIX (CAYMAN) LIMITED (KY)

Free format text: TRANSFERIDO DE: IDENIX PHARMACEUTICALS, INC.

B07A Technical examination (opinion): publication of technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PRESENTE PEDIDO DE ACORDO COM OS ARTIGOS 8O, 10 (INCISO VIII) E 25 DA LPI.

B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL.