摘要:
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
摘要:
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
摘要:
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
摘要:
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
摘要:
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS. The compounds of the invention for the general Formula I: wherein: Z is Q is selected from the group consisting of: —W— is
摘要:
This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine diamide derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
摘要:
This invention provides compounds of Formula I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19–R23;W is O or —NH;T is Z1 is CR1 or N;Z2 is CR2 or N;Z3 is CR3 or N;Z4 is CR4 or N;Z5 is CR5 or N;Z6 is CR6 or N;Z7 is CR7 or N;Z8 is CR8 or N.
摘要翻译:本发明提供具有药物和生物影响性质的式I化合物,其药物组合物和使用方法。 特别地,本发明涉及酰胺哌嗪衍生物。 这些化合物具有独特的抗病毒活性,无论是单独使用还是与其他抗病毒药,抗感染剂,免疫调节剂或HIV进入抑制剂组合使用。 更具体地说,本发明涉及艾滋病毒和艾滋病的治疗。 A选自C 1-6 - 烷氧基,C 1-6 - 烷基,C 3-7环烷基,苯基和 - 杂芳基; 其中所述杂芳基可以是单环或双环的,并且可以由选自C,N,NR 9,O和S的3至11个原子组成,并且其中所述苯基和 杂芳基任选被一至五个相同或不同的选自下组的取代基取代:R 20 -R 23; W是O或-NH; T是Z 1是CR 1或N; Z 2是CR 2或N; Z 3是CR 3或N; Z 4是CR 4或N; Z 5是CR 5或N; Z 6是CR 6或N; N是7或N; Z 8是CR 8或N.
摘要:
The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.
摘要:
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.