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1. 发明申请

WO1997027179A2 ANTIRETROVIRAL BASES 审中-公开
标题翻译：抗逆转基因
公开(公告)号：WO1997027179A2
公开(公告)日：1997-07-31
申请号：PCT/EP1997000139
申请日：1997-01-14
申请人： NOVARTIS AG , FREI, Jörg , FÄSSLER, Alexander , FLÖRSHEIMER, Andreas , HAMY, François , KLIMKAIT, Thomas
发明人： NOVARTIS AG
IPC分类号： C07D219/12
CPC分类号： C07D221/14 , A61K31/473 , C07D219/04 , C07D219/12 , C07D271/12 , C07D473/40
摘要： The invention relates to the use of a compound of formula (I), wherein R1 and R2 are independently amino, N-alkylamino, N,N-dialkylamino, cycloalkylamino, amidino, N-lower alkylamidino, N,N-di-lower alkylamidino, guanidino, N-lower alkylguanidino, N,N-di-lower alkylguanidino or (a); X and Y are independently selected from the group consisting of -(CH2)b-, (b), (c) and -(CH2)g-Cycloalkylen-(CH2)h-; Z is, independently of X and Y, -(CH2)b-, (d) or (e), wherein R is hydrogen or lower alkyl; Q is aryl, arylcarbonyl, arylaminocarbonyl, heterocyclyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl, aryl or heterocyclyl whenever mentioned containing 2 or more annelated rings, a is 2 to 4, b is 2-7, c, d, e and f is 1 to 3, respectively, g and h is 0 to 3, respectively, i is 2 to 7 and k is 1 to 3, with the proviso that Q is arylcarbonyl, arylaminocarbonyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl only if Z is a bivalent radical of formula (f) or (g); a tautomer thereof, or a salt thereof, as antiretroviral therapeutic (also for prophylaxis) inhibiting the interaction of transcriptional regulators with retroviral response elements.
摘要翻译：本发明涉及式（I）化合物的用途，其中R 1和R 2独立地是氨基，N-烷基氨基，N，N-二烷基氨基，环烷基氨基，脒基，N-低级烷基脒基，N，N-二低级烷基脒基胍基，N-低级烷基胍基，N，N-二低级烷基胍基或（a）; X和Y独立地选自 - （CH 2）b - ，（b），（c）和 - （CH 2）g-环烷基 - （CH 2）h - ; Z独立于X和Y， - （CH 2）b - ，（d）或（e），其中R是氢或低级烷基; Q为芳基，芳基羰基，芳基氨基羰基，杂环基，杂环基羰基或杂环基氨基羰基，芳基或杂环基，每当提到含有2个或更多个环状环时，a为2至4，b为2-7，c，d，e和f为1至3， g和h分别为0至3，i为2至7，k为1至3，条件是Q为芳基羰基，芳基氨基羰基，杂环基羰基或杂环基氨基羰基，只要Z是式（f）的二价基团或（G）; 其互变异构体或其盐作为抗转录病毒治疗剂（也用于预防）抑制转录调节物与逆转录病毒应答元件的相互作用。

2. 发明申请

WO9727179A3 ANTIRETROVIRAL BASES 审中-公开
标题翻译：抗病毒基地
公开(公告)号：WO9727179A3
公开(公告)日：1997-12-31
申请号：PCT/EP9700139
申请日：1997-01-14
申请人： CIBA GEIGY AG , FREI JOERG , FAESSLER ALEXANDER , FLOERSHEIMER ANDREAS , HAMY FRANCOIS , KLIMKAIT THOMAS
发明人： FREI JOERG , FAESSLER ALEXANDER , FLOERSHEIMER ANDREAS , HAMY FRANCOIS , KLIMKAIT THOMAS
IPC分类号： A61K31/473 , C07D219/04 , C07D219/12 , C07D221/14 , C07D271/12 , C07D473/40 , A61K31/435
CPC分类号： C07D221/14 , A61K31/473 , C07D219/04 , C07D219/12 , C07D271/12 , C07D473/40
摘要： The invention relates to the use of a compound of formula (I), wherein R1 and R2 are independently amino, N-alkylamino, N,N-dialkylamino, cycloalkylamino, amidino, N-lower alkylamidino, N,N-di-lower alkylamidino, guanidino, N-lower alkylguanidino, N,N-di-lower alkylguanidino or (a); X and Y are independently selected from the group consisting of -(CH2)b-, (b), (c) and -(CH2)g-Cycloalkylen-(CH2)h-; Z is, independently of X and Y, -(CH2)b-, (d) or (e), wherein R is hydrogen or lower alkyl; Q is aryl, arylcarbonyl, arylaminocarbonyl, heterocyclyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl, aryl or heterocyclyl whenever mentioned containing 2 or more annelated rings, a is 2 to 4, b is 2-7, c, d, e and f is 1 to 3, respectively, g and h is 0 to 3, respectively, i is 2 to 7 and k is 1 to 3, with the proviso that Q is arylcarbonyl, arylaminocarbonyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl only if Z is a bivalent radical of formula (f) or (g); a tautomer thereof, or a salt thereof, as antiretroviral therapeutic (also for prophylaxis) inhibiting the interaction of transcriptional regulators with retroviral response elements.
摘要翻译：本发明涉及式（I）化合物的用途，其中R1和R2独立地为氨基，N-烷基氨基，N，N-二烷基氨基，环烷基氨基，脒基，N-低级烷基脒基，N，N-二低级烷基脒基，胍基，N-低级烷基胍基，N，N-二低级烷基胍基或（a）。 X和Y独立地选自 - （CH 2）b - ，（b），（c）和 - （CH 2）g - 亚环烷基 - （CH 2）h - Z独立于X和Y， - （CH2）b-，（d）或（e），其中R是氢或低级烷基; Q为芳基，芳基羰基，芳基氨基羰基，杂环基，杂环基羰基或杂环基氨基羰基，芳基或杂环基，每当含有2个或多个稠环时，a为2至4，b为2至7，c，d，e和f为1至3，只要Z是式（f）的二价基团，则g和h分别为0至3，i为2至7且k为1至3，条件是Q为芳基羰基，芳基氨基羰基，杂环基羰基或杂环基氨基羰基。（G）; 其互变异构体或其盐作为抗逆转录病毒治疗剂（也用于预防）抑制转录调节剂与逆转录病毒应答元件的相互作用。

3. 发明申请

WO1996040759A1 ANTIVIRAL PEPTOID COMPOUNDS 审中-公开
标题翻译：抗生素PEPTOID化合物
公开(公告)号：WO1996040759A1
公开(公告)日：1996-12-19
申请号：PCT/EP1996002424
申请日：1996-06-04
申请人： CIBA-GEIGY AG , FELDER, Eduard , HAMY, François , HEIZMANN, Gerhard , KLIMKAIT, Thomas , LAZDINS, Janis, Karlis
发明人： CIBA-GEIGY AG
IPC分类号： C07K14/00
CPC分类号： C07K14/005 , A61K38/00 , C07K14/001 , C12N2740/16322
摘要： Described are peptoid compounds of the formula (I): R1-(A)k-(X)m-(B)n-R2 wherein k, n, R1, R2, A and B have the meanings given in the specification, m is 3 to 10, and any X independently of the others being present represents a bivalent radical of partial formula (II), wherein each of R3, R4 and R5, independently of the others, represents hydrogen or a side chain of an alpha -amino acid other than glycine, or R3 and R4 together form an alkylene bridge and R5 is hydrogen, or R4 and R5 together form an alkylene bridge and R3 is hydrogen; with the proviso, that a) at least one of these bivalent radicals has an R3 which is a side chain of an alpha -amino acid other than glycine and proline; b) that at least one R3 other than alkyl or benzyl is present; and c) that the bivalent radicals X together form a TAR-binding, transactivation-deficient oligopeptide analogue of the basic domain of the HIV Tat protein, and any B independently of the others being present represents a bivalent radical of an alpha -amino acid, or salts thereof if a salt-forming group is present. The compounds act, for example, as inhibitors of HIV growth by inhibition of the Tat/TAR-interaction.
摘要翻译：描述了式（I）的拟肽化合物：R1-（A）k-（X）m-（B）n-R2其中k，n，R1，R2，A和B具有说明书中给出的含义，m 是3至10，并且存在的其它任何X独立地表示部分式（II）的二价基团，其中R 3，R 4和R 5各自独立地表示氢或α-氨基的侧链除了甘氨酸以外，还有R3和R4一起形成亚烷基桥，R5是氢，R4和R5一起形成亚烷基桥，R3是氢; 条件是a）这些二价基团中的至少一个具有R3，其是除了甘氨酸和脯氨酸之外的α-氨基酸的侧链; b）存在至少一种不同于烷基或苄基的R 3; 和c）二价基团X一起形成HIV Tat蛋白质的碱性结构域的TAR结合，反式激活缺陷的寡肽类似物，并且与存在的其它B独立的任何B代表α-氨基酸的二价基团，或其盐，如果存在成盐基团。该化合物例如通过抑制Tat / TAR-相互作用而作为HIV生长抑制剂。

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