摘要:
The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen, wherein R7 and R8 are independently H or an alkyl. Substituents R1 or R2 are each H or an alkyl. Substituent R3 is a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH2, or SH. Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.
摘要:
The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen. R7 and R8 are H or alkyl, R1 and R2 are H or alkyl, and R3 is a non-aromatic substituent. Substituent A is OH, NH2, or SH. Substituents B and B1 include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R′ together with the nitrogen to which they are bonded, and/or B′ and R2 together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention. The present invention further provides therapeutic methods that include administering a therapeutically effective amount of at least one compound of the present invention
摘要翻译:本发明提供式(I)化合物,其中a,b,c,d和e分别是R 7,OR 7,SR 7,NR 7 R 8,NHCOR 7,CO 2 R 7,CN,NO 2,NH 2,N 3或卤素。 R 7和R 8是H或烷基,R 1和R 2是H或烷基,R 3是非芳族取代基。 取代基A是OH,NH 2或SH。 取代基B和B1包括酰胺和磺酰胺基团,其可以是环状,非环状或氨基酸衍生物。 或者,B和R'与它们所键合的氮一起,和/或B'和R 2与它们所键合的氮一起定义杂环。 本发明还提供了包含载体和治疗有效量的至少一种本发明化合物的药物组合物。 本发明进一步提供治疗方法,其包括施用治疗有效量的至少一种本发明化合物
摘要:
The present invention provides novel retroviral agents containing anthranilamide, substituted benzamide, amino acid, and other subunits, a pharmaceutical composition comprising such compound, and a method of using such compounds to treat retroviral infections in mammals, specifically HIV and more specifically HIV-1 and HIV-2, in humans.
摘要:
The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.
摘要:
The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.
摘要:
The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.
摘要:
The present invention is concerned with This invention relates to C34 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.
摘要:
Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.
摘要:
The invention provides compositions and methods that are useful for preventing and treating a coronavirus infection in a subject. More specifically, the invention provides peptides and conjugates and pharmaceutical compositions containing those peptides and conjugates that block fusion of a coronavirus, such as the SARS virus, to a target cell. This blocking mechanism prevents or treats a coronavirus infection, such as a SARS infection, in a subject, such as a human subject.
摘要:
A lubrication system for moveable machine parts within a housing have a sump containing a fluid and a rotatable shaft comprising a ring eccentrically encircling and being frictionally rotated by shaft, ring being at least partially immersed in sump fluid to carry fluid during rotation for machine parts, a plurality of fluid carrying fins attached to ring to increase the fluid carrying capacity of ring, fins commencing from each outer edge and extending partially inwardly along the ring width towards each other thereby forming an annular space between fins and ring, conduit means having an inlet located within annular space for receiving fluid carried in annular space and delivering fluid to moveable machine parts, and first and second abutments attach to shaft, one on each side of ring and spaced from ring sufficiently to form an axial gap for a fluid film which transmits rotational power from abutments to ring.