-
公开(公告)号：EP1856125B1
公开(公告)日：2009-08-26
申请号：EP06724879.9
申请日：2006-02-24
IPC分类号： C07D493/04 , A61K31/34 , A61P31/12
CPC分类号： C07D493/04
摘要： The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.
-
2.发明授权AMINOBENZIMIDAZOLES AND BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权氨基苯并咪唑和苯并咪唑为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1697343B1
公开(公告)日：2009-07-01
申请号：EP04804949.8
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06 , A61K31/4184 , C07D401/14 , C07D405/14 , C07D401/12 , A61P11/00 , A61P31/12
CPC分类号： C07D401/06 , C07D235/20 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/02 , C07D405/14 , C07D471/04 , C07F9/65583
摘要： Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula (I) the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1Cl-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(-CH2-CH2-O)n-, C1-6alkyloxy(-CH2-M2-O)n- or Ar1Cl-6alkyloxy(-CH2-C2-O)n-; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or -C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
-
3.发明公开METHODS AND MEANS FOR ASSESSING HIV GAG/PROTEASE INHIBITOR THERAPY 审中-公开的方法和手段进行评估HIV GAG /蛋白酶抑制剂治疗
公开(公告)号：EP2010680A2
公开(公告)日：2009-01-07
申请号：EP07765259.2
申请日：2007-04-13
发明人： DE BAERE, Inky Paul Madeleine , KRAUS, Guenter , RIMSKY, Laurence Tatiana , MAES, Bart Anna Julien , AZIJN, Hilde , DE BETHUNE, Marie-Pierre T.M.M.G
CPC分类号： C12Q1/703 , G01N2333/161
摘要： The present invention relates to methods and means for the evaluation of HIV treatment. In particular, molecular events at the HIV gag and protease proteins and their effect on therapeutic efficacy of drugs are determined. The methods rely on providing HIV gag and protease nucleic acid material and evaluating a treatment either through genotyping or phenotyping. Said method may find use in multiple fields including diagnostics, drug screening, pharmacogenetics and drug development.
-
公开(公告)号：EP1981506A2
公开(公告)日：2008-10-22
申请号：EP07712053.3
申请日：2007-01-19
IPC分类号： A61K31/505 , A61P31/18
CPC分类号： A61K31/505
摘要： This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week.
-
公开(公告)号：EP1881848A2
公开(公告)日：2008-01-30
申请号：EP06725539.8
申请日：2006-04-04
IPC分类号： A61K47/10 , A61K47/16 , A61P31/18 , A61K31/505
CPC分类号： A61K31/505 , A61K9/0019 , A61K47/10 , A61K47/16
摘要： This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
-
公开(公告)号：EP1856125A1
公开(公告)日：2007-11-21
申请号：EP06724879.9
申请日：2006-02-24
IPC分类号： C07D493/04 , A61K31/34 , A61P31/12
CPC分类号： C07D493/04
摘要： The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.
-
7.发明公开
公开(公告)号：EP1853568A1
公开(公告)日：2007-11-14
申请号：EP06707872.5
申请日：2006-01-27
发明人： HEERES, Jan , LEWI, Paulus Joannes , LEEMANS, Rudolf , MOENS, Luc Jozef Raphael , JANSSEN, Paul, Adriaan, Jan
IPC分类号： C07D239/50 , C07D239/48 , A61K31/505 , A61P31/18
CPC分类号： C07D239/50 , C07D239/48
摘要： HIV replication inhibitors of formula (I) pharmaceut ically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.
-
8.发明授权
公开(公告)号：EP1505980B1
公开(公告)日：2007-10-24
申请号：EP03730208.0
申请日：2003-05-13
IPC分类号： A61K31/505 , A61K31/506 , A61K31/535 , A61P15/02 , A61P31/02 , A61P31/18
CPC分类号： A61K31/505 , A61K9/0014 , A61K9/0034 , A61K9/0036 , A61K9/06 , A61K31/506 , A61K31/535 , A61K45/06 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/38
摘要： The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.
-
公开(公告)号：EP1624897B1
公开(公告)日：2007-10-10
申请号：EP04741542.7
申请日：2004-05-10
IPC分类号： A61K47/48 , C07D473/00 , C07H15/252
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; R1 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4akloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R2 is arylC1-4alkyl; R3 is C1-10alkyl, C2-6alkenyl or C3-7cycloalkyIC1-4alkyl; R4 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： 本发明提供了作为治疗性化合物和肽的缀合物的新型前体药物，其中缀合物可被二肽基肽酶，更优选CD26（也称为DPPIV（二肽基氨基二肽酶IV））裂解。 本发明的前体药物具有式（I），其立体异构形式和盐，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（硫代脯氨酸），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彼此独立地选择并独立于其他重复; 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为芳基，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; R2是芳基C1-4烷基; R3是C1-10烷基，C2-6链烯基或C3-7环烷基C1-4烷基; R4是氢或C1-4烷基。 本发明还提供所述前药作为药物的用途以及生产所述前药的方法。
-
10.发明授权BROADSPECTRUM SUBSTITUTED BENZISOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权取代的BENZISOXAZOLSULFONAMIDEBREITBÄNDIGERHIV蛋白酶抑制效果
公开(公告)号：EP1517899B1
公开(公告)日：2007-08-29
申请号：EP03735707.6
申请日：2003-05-16
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , VERGOUWEN, Bernhard, Joanna, Bernard , DE KOCK, Herman, Augustinus
IPC分类号： C07D261/20 , C07D493/04 , C07D413/12 , C07D417/12 , A61K31/423 , A61K31/427 , A61P31/18
CPC分类号： C07D413/12 , C07D261/20 , C07D417/12 , C07D493/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs esters and metabolites thereof. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
-
-
-
-
-
-
-
-
-
搜索结果
140 条记录 (耗时 0.024 秒)
