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1. 发明申请

WO2007033444A3 ANTIVIRAL THERAPY WITH CARBOHYDRATE BINDING AGENTS 审中-公开
标题翻译：与碳水化合物结合剂的抗病毒治疗
公开(公告)号：WO2007033444A3
公开(公告)日：2007-12-21
申请号：PCT/BE2006000104
申请日：2006-09-21
申请人： LEUVEN K U RES & DEV , BALZARINI JAN
发明人： BALZARINI JAN
IPC分类号： A61K31/409 , A61K31/165 , A61K31/30 , A61K31/444 , A61K31/69 , A61K31/715 , A61K33/34 , A61K38/16 , A61P31/12
CPC分类号： C07D239/42 , A61K31/165 , A61K31/30 , A61K31/409 , A61K31/444 , A61K31/69 , A61K31/715 , A61K38/168 , C07D213/74
摘要： The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses having glycosilated envelop proteins such as Retroviridae (i.e. Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B or C.
摘要翻译：本发明的领域涉及使用碳水化合物结合化合物作为药物，其用于治疗或预防病毒感染的用途，其用于制造治疗或预防病毒感染的药物及其在疫苗接种策略中的用途。本发明涉及所述化合物用于制备治疗或预防受试者的病毒感染的药物，更特别是具有糖基化包膜蛋白的病毒的感染，例如逆转录病毒科（如Lentivirina），如HIV（人类免疫缺陷病毒），黄病毒科，如HCV（丙型肝炎病毒），Hepadnaviridae，如HBV（乙型肝炎病毒），冠状病毒科，如SARS冠状病毒和正粘病毒科，如A，B或C型流感。

2. 发明申请

WO2008056264A3 NOVEL NUCLEOTIDE ANALOGUES AS PERCURSOR MOLECULES FOR ANTIVIRALS 审中-公开
标题翻译：新型核苷酸类似物作为抗菌药物的选择性分子
公开(公告)号：WO2008056264A3
公开(公告)日：2008-10-30
申请号：PCT/IB2007004233
申请日：2007-11-08
申请人： CT NAT DE RECH SCIENT CNRS , UNIV AIX MARSEILLE II , LEUVEN K U RES & DEV , CANARD BRUNO , ALVAREZ KARINE , BARRAL KARINE , ROMETTE JEAN-LOUIS , NEYTS JOHAN , BALZARINI JAN
发明人： CANARD BRUNO , ALVAREZ KARINE , BARRAL KARINE , ROMETTE JEAN-LOUIS , NEYTS JOHAN , BALZARINI JAN
IPC分类号： C07F9/38 , A61K31/662 , A61P31/12
CPC分类号： C07F9/65616
摘要： This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R 1 -R 3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for treating and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H- phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R 1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C 1-6 haloalkyl group.
摘要翻译：本发明涉及式（I）的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B，X和R 1〜R 3如本文中的类别和亚类所定义。这些化合物可以用作抗病毒前体。本发明还涉及这些化合物的治疗组合物及其用于制备治疗和/或预防患者病毒感染的药物的用途。本发明还提供了制备这些化合物的方法。特别地，本发明提供式（II）的次膦酸盐前体中间体，其中B是如本文所定义的嘌呤或嘧啶碱基，R 1选自氢原子和甲基，乙基，羟甲基，羟乙基和C 1-6卤代烷基。

3. 发明申请

WO2004019970A3 GLYCOPEPTIDE ANTIBIOTIC AND SEMISYNTHETIC DERIVATIVES THEREOF AND THEIR USE AS ANTIVIRAL AGENTS 审中-公开
标题翻译：甘氨酸抗生素和半胱氨酸衍生物及其作为抗病毒剂的用途
公开(公告)号：WO2004019970A3
公开(公告)日：2004-07-22
申请号：PCT/BE0300144
申请日：2003-09-01
申请人： LEUVEN K U RES & DEV , BALZARINI JAN , PREOBRAZHENSKAYA MARIA , DE CLERCQ ERIK
发明人： BALZARINI JAN , PREOBRAZHENSKAYA MARIA , DE CLERCQ ERIK
IPC分类号： A61K38/00 , A61K38/14 , C07K9/00
CPC分类号： A61K38/14 , C07K9/008
摘要： Novel glycopeptide antibiotic derivatives, processes for their preparation, their use as a medicine, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections are provided. The present invention relates to the use of glycopeptide antibiotics and their semisynthetic derivatives to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses belonging to Retroviridae, Herpes viridae, Flaviviridae and the Coronaviridae, like HIV (human immunodeficiency virus), HCV (hepatitis C virus), BVDV (bovine viral diarrhoea virus), SARS (severe acute respiratory syndrome) causing virus, FCV (feline coronavirus), HSV (herpes simplex virus), VZV (varicella zoster virus) and CMV (cytomegalovirus).
摘要翻译：提供了新型糖肽抗生素衍生物，其制备方法，它们作为药物的用途，其用于治疗或预防病毒感染及其用于制造治疗或预防病毒感染的药物的用途。本发明涉及糖肽抗生素及其半合成衍生物用于治疗或预防病毒感染及其用于制造治疗或预防受试者病毒感染的药物，更特别涉及属于逆转录病毒科，疱疹病毒科，黄病毒科的病毒感染和冠状病毒科，如HIV（人类免疫缺陷病毒），HCV（丙型肝炎病毒），BVDV（牛病毒性腹泻病毒），SARS（严重急性呼吸综合征）引起的病毒，FCV（猫冠状病毒），HSV（单纯疱疹病毒） VZV（水痘带状疱疹病毒）和CMV（巨细胞病毒）。

4. 发明申请

WO2009142827A4 COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRAL INFECTION 审中-公开
标题翻译：用于治疗病毒感染的化合物和方法
公开(公告)号：WO2009142827A4
公开(公告)日：2010-09-23
申请号：PCT/US2009038644
申请日：2009-03-27
申请人： US GOV HEALTH & HUMAN SERV , MARGOLIS LEONID , BALZARINI JAN , MCGUIGAN CHRIS , LISCO ANDREA , VANPOUILLE CHRISTOPHE , DERUDAS MARCO
发明人： MARGOLIS LEONID , BALZARINI JAN , MCGUIGAN CHRIS , LISCO ANDREA , VANPOUILLE CHRISTOPHE , DERUDAS MARCO
IPC分类号： C07F9/6561 , A61K31/664 , A61P31/12 , A61P31/18
CPC分类号： C07F9/65616
摘要： The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible (to a viral infection, such as HlV infection.
摘要翻译：本发明涉及用于治疗或预防病毒感染的化合物和方法，其通过将阿昔洛韦或阿昔洛韦前药的单磷酸化衍生物的单磷酸化前药给予患有或易患病毒感染（例如HIV感染）的受试者。

5. 发明申请

WO2009142827A2 COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRAL INFECTION 审中-公开
标题翻译：化合物和治疗病毒感染的方法
公开(公告)号：WO2009142827A2
公开(公告)日：2009-11-26
申请号：PCT/US2009038644
申请日：2009-03-27
申请人： US GOV HEALTH & HUMAN SERV , MARGOLIS LEONID , BALZARINI JAN , MCGUIGAN CHRIS , LISCO ANDREA , VANPOUILLE CHRISTOPHE
发明人： MARGOLIS LEONID , BALZARINI JAN , MCGUIGAN CHRIS , LISCO ANDREA , VANPOUILLE CHRISTOPHE
IPC分类号： A61K31/675
CPC分类号： C07F9/65616
摘要： The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible to a viral infection, such as HIV infection.
摘要翻译：本发明涉及用于治疗或预防病毒感染的化合物和方法，其通过将阿昔洛韦的单磷酸化前药或阿昔洛韦前药的单磷酸化衍生物施用于患有或易感病毒感染如HIV感染的受试者。

6. 发明申请

WO2004062575A3 BICYCLIC CARBOHYDRATE COMPOUNDS USEFUL IN THE TREATMENT OF INFECTIONS CAUSED BY FLAVIVIRIDAE SP., SUCH AS HEPATITIS C AND BOVINE VIRAL DIARRHEA VIRUSES 审中-公开
标题翻译：双环碳水化合物化合物可用于治疗由黄病毒科，如丙型肝炎病毒和牛病毒性腹泻病毒引起的感染
公开(公告)号：WO2004062575A3
公开(公告)日：2004-12-09
申请号：PCT/US0341720
申请日：2003-12-22
申请人： KEMIN PHARMA EUROP BVBA , SAS BENEDIKT , VAN HEMEL JOHAN , VANDENKERCKHOVE JAN , PEYS ERIC , VAN DER EYCKEN JOHAN , RUTTENS BART , BALZARINI JAN , DECLERCQ ERIK , NUYTS JOHAN
发明人： SAS BENEDIKT , VAN HEMEL JOHAN , VANDENKERCKHOVE JAN , PEYS ERIC , VAN DER EYCKEN JOHAN , RUTTENS BART , BALZARINI JAN , DECLERCQ ERIK , NUYTS JOHAN
IPC分类号： A61K31/357 , A61K31/385 , A61K31/519 , A61K31/70 , C07H15/00 , C07D498/02
CPC分类号： C07D493/04 , A61K31/357 , A61K31/385 , A61K31/519 , A61K31/70 , C07H7/04 , C07H9/04 , C07H15/04
摘要： We describe the use of bicyclic carbohydrates for the treatment of hepatitis C virus infections. Different bicyclic carbohydrates were tested in vitro against DNA-viruses, retroviruses and Flaviviridae sp., an important family of human and animal RNA pathogens. Significant activity was observed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), the bicyclic carbohydrates in general and the preferred bicyclic carbohydrates more specifically are expected to be a treatment for hepatitis C viral infections.
摘要翻译：我们描述了使用双环碳水化合物治疗丙型肝炎病毒感染。不同的双环碳水化合物在体外针对DNA病毒，逆转录病毒和黄病毒科（人和动物RNA病原体的重要家族）进行测试。观察到牛病毒性腹泻病毒（BVDV）的显着活性。由于瘟病毒例如BVDV与丙型肝炎病毒（HCV）有许多相似之处，所以通常双环碳水化合物和更具体地优选的双环碳水化合物预期是治疗丙型肝炎病毒感染。

7. 发明申请

WO2008059130A9 THIONUCLEOSIDES AND PHARMACEUTICAL APPLICATIONS 审中-公开
标题翻译：噻唑类和药物应用
公开(公告)号：WO2008059130A9
公开(公告)日：2009-07-23
申请号：PCT/FR2007001784
申请日：2007-10-29
申请人： UNIV GRENOBLE 1 , DECOUT JEAN-LUC , GERLAND BEATRICE , DESIRE JEROME , LEPOIVRE MICHEL , BALZARINI JAN
发明人： DECOUT JEAN-LUC , GERLAND BEATRICE , DESIRE JEROME , LEPOIVRE MICHEL , BALZARINI JAN
IPC分类号： C07D405/04 , A61K31/695 , A61K31/7068 , A61K31/7072 , C07F7/08 , C07F7/10 , C07H19/06 , C07H19/067 , C07H19/073
CPC分类号： C07D405/04 , C07H19/00 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/173
摘要： The invention relates to a pharmaceutical composition containing as an active ingredient at least one compound selected from the compounds of the formula (II), in which the S atom is bonded to the nucleoside carbon at T or to the nucleoside carbon at 3', and from the compounds of the following formula (III): formulae in which B is a nucleotide natural or modified base, x is 0, 1 or 2, and R1 and R represent a carbonated group or a molecular hydrocarbon remnant that can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si, X where X is halogen. The invention also relates to pharmaceutically acceptable carrier.
摘要翻译：本发明涉及一种药物组合物，其含有至少一种选自式（II）化合物中的至少一种化合物，其中S原子在T处与核苷碳键合或在3'与核苷碳结合，以及由下式（III）的化合物：其中B是核苷酸天然或修饰碱基的式，x是0,1或2，R1和R表示可被取代的碳酸化基团或分子碳氢化合物残余物，和/ 或被一个或多个原子和/或被一个或多个含有一个或多个原子的基团中断，所述原子选自N，O，P，S，Si，X，其中X是卤素。本发明还涉及药学上可接受的载体。

8. 发明申请

WO2004099135A3 HIV PRODRUGS CLEAVABLE BY CD26 审中-公开
公开(公告)号：WO2004099135A3
公开(公告)日：2005-02-17
申请号：PCT/EP2004050753
申请日：2004-05-10
申请人： TIBOTEC PHARM LTD , DE KOCK HERMAN AUGUSTINUS , WIGERINCK PIET TOM BERT PAUL , BALZARINI JAN
发明人： DE KOCK HERMAN AUGUSTINUS , WIGERINCK PIET TOM BERT PAUL , BALZARINI JAN
IPC分类号： A61K38/00 , A61K47/48 , C07D493/04 , C07H15/252 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/083 , C07K5/103 , C07K5/11 , C07K5/113 , C07K7/06 , C07K9/00 , C07D473/00
CPC分类号： C07D493/04 , A61K38/00 , A61K47/64 , C07H15/252 , C07K5/06052 , C07K5/06113 , C07K5/0808 , C07K5/1008 , C07K5/101 , C07K5/1019 , C07K5/1021 , C07K7/06 , C07K9/003
摘要： The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present prodrugs have the formula (I), the stereoisomeric forms and salts thereof, wherein n is I to 5; Y is proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine; X is selected from any amino acid in the D- or L-configuration; X and Y in each repeat of [Y-X] are chosen independently from one another and independently from other repeats; Z is a direct bond or a bivalent straight or branched saturated hydrocarbon group having from 1 to 4 carbon atoms; R is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4akloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R is arylC1-4alkyl; R is C1-10alkyl, C2-6alkenyl or C3-7cycloalkyIC1-4alkyl; R is hydrogen or C1-4alkyl. The present invention furthermore provides the use of said prodrugs as medicines as well as a method of producing said prodrugs.
摘要翻译：本发明提供了新的前体药物，其是治疗化合物和肽的缀合物，其中缀合物可被二肽基肽酶切割，更优选通过CD26，也称为DPPIV（二肽基氨基二肽酶IV））。本发明的前药具有式（I），其立体异构形式及其盐，其中n为1至5; Y是脯氨酸，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸; X选自D-或L-构型中的任何氨基酸; [Y-X]的每个重复中的X和Y彼此独立地独立地选自其它重复; Z是直接键或具有1至4个碳原子的二价直链或支链饱和烃基; R 1是芳基，杂芳基，芳氧基，杂芳氧基，芳氧基C 1-4烷基，杂环烷氧基，杂环烷基C 1-4烷氧基，杂芳氧基C 1-4烷基，杂芳基C 1-4烷氧基; R 2是芳基C 1-4烷基; R 3是C 1-10烷基，C 2-6烯基或C 3-7环烷基C 1-4烷基; R 4是氢或C 1-4烷基。本发明还提供所述前体药物作为药物的用途以及制备所述前体药物的方法。

9. 发明申请

WO2009138507A3 ANTI-CANCER COMBINATION THERAPY 审中-公开
标题翻译：抗癌联合治疗
公开(公告)号：WO2009138507A3
公开(公告)日：2010-04-29
申请号：PCT/EP2009055955
申请日：2009-05-15
申请人： UNIV LEUVEN KATH , BALZARINI JAN , LIEKENS SANDRA
发明人： BALZARINI JAN , LIEKENS SANDRA
IPC分类号： A61K31/7068 , A61K31/513 , A61K31/7076
CPC分类号： A61K45/06 , A61K31/513 , A61K31/7068 , A61K31/7076 , A61K2300/00
摘要： The present invention relates to a combination of therapeutic agents comprising: (a) a cytosine-based anti-cancer drug and/or a purine-based anticancer drug and (b) a therapeutic agent selected from the group consisting of thymidine phosphorylase inhibitors, and antibiotics against Mollicutes bacteria. The present invention also relates to the simultaneous, separate or sequential use of said combination for the treatment of cancer in mammals, especially in humans. The present invention also relates to methods of treatment of cancer, preferably in mammals infected with Mollicutes bacteria.
摘要翻译：本发明涉及治疗剂的组合，其包含：（a）基于胞嘧啶的抗癌药物和/或嘌呤类抗癌药物和（b）选自胸苷磷酸化酶抑制剂和抗生素对Mollicute细菌。本发明还涉及用于治疗哺乳动物，特别是人类中的癌症的所述组合的同时，分开或顺序使用。本发明还涉及治疗癌症的方法，优选在用Mollicutes细菌感染的哺乳动物中。

10. 发明申请

WO03039450A2 IMPROVEMENTS IN OR RELATING TO INHIBITION OF VIRUSES 审中-公开
标题翻译：改善或相关于病毒的抑制
公开(公告)号：WO03039450A2
公开(公告)日：2003-05-15
申请号：PCT/GB0205031
申请日：2002-11-07
申请人： MEDICAL RES COUNCIL , LOAKES DAVID , BROWN DANIEL , BALZARINI JAN , MORIYAMA KEI , NEGISHI KAZUO , CAMERON CRAIG , ARNOLD JAMIE , CASTRO CHRISTIAN , KORNEEVA VICTORIA , GRACI JASON
发明人： LOAKES DAVID , BROWN DANIEL , BALZARINI JAN , MORIYAMA KEI , NEGISHI KAZUO , CAMERON CRAIG , ARNOLD JAMIE , CASTRO CHRISTIAN , KORNEEVA VICTORIA , GRACI JASON
IPC分类号： C07H19/067 , A01N43/90 , A61K31/519 , A61K31/52 , A61K31/675 , A61K31/7068 , A61K31/7076 , A61P31/14 , C07H19/16 , C07H19/167 , A61K
CPC分类号： C07H19/16
摘要： Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula (I) or (II) as herein defined , in admixture with a physiologically acceptable excipient diluent or carrier.
摘要翻译：公开了包含根据本文定义的通式（I）或（II）的核糖核苷类似物与生理上可接受的赋形剂稀释剂或载体的混合物的药物组合物。

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