| Cyclic sulfone containing retroviral protease inhibitors -> Monitor Keywords |
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Cyclic sulfone containing retroviral protease inhibitorsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Sulfur Containing Hetero Ring, The Hetero Ring Is Six-memberedCyclic sulfone containing retroviral protease inhibitors description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070015818, Cyclic sulfone containing retroviral protease inhibitors. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a continuation of U.S. patent application Ser. No. 10/932,331, filed Sep. 2, 2004, now allowed, which is a continuation of U.S. patent application Ser. No. 10/369,197, filed Feb. 20, 2003, now U.S. Pat. No. 6,875,790, which is a continuation of U.S. patent application Ser. No. 09/973,991, filed Oct. 11, 2001, now U.S. Pat. No. 6,552,203, which is a continuation of U.S. patent application Ser. No. 09/870,748, filed Jun. 1, 2001, now U.S. Pat. No. 6,329,524, which is a divisional of U.S. patent application Ser. No. 09/177,100, filed Oct. 22, 1998, now U.S. Pat. No. 6,265,583, which is a divisional of U.S. patent application Ser. No. 08/556,883, filed Nov. 2, 1995, now U.S. Pat. No. 5,849,784, which is a divisional of U.S. patent application Ser. No. 07/998,187, filed Dec. 29, 1992, now U.S. Pat. No. 5,514,801, each of which applications is hereby incorporated herein by reference in its entirety. BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention relates to retroviral protease inhibitors and, more particularly relates to novel compounds and a composition and method for inhibiting retroviral proteases. This invention, in particular, relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds, a composition and method for inhibiting retroviral proteases such as human immunodeficiency virus infection. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. [0004] 2. Related Art [0005] During the replication cycle of retroviruses, gag and gag-pol gene products are translated as proteins. These proteins are subsequently processed by a virally encoded protease (or proteinase) to yield viral enzymes and structural proteins of the virus core. Most commonly, the gag precursor proteins are processed into the core proteins and the pol precursor proteins are processed into the viral enzymes, e.g., reverse transcriptase and retroviral protease. It has been shown that correct processing of the precursor proteins by the retroviral protease is necessary for assembly of infectious virons. For example, it has been shown that frameshift mutations in the protease region of the pol gene of HIV prevents processing of the gag precursor protein. It has also been shown through site-directed mutagenesis of an aspartic acid residue in the HIV protease that processing of the gag precursor protein is prevented. Thus, attempts have been made to inhibit viral replication by inhibiting the action of retroviral proteases. [0006] Retroviral protease inhibition typically involves a transition-state mimetic whereby the retroviral protease is exposed to a mimetic compound which binds (typically in a reversible manner) to the enzyme in competition with the gag and gag-pol proteins to thereby inhibit replication of structural proteins and, more importantly, the retroviral protease itself. [0007] In this manner, retroviral proteases can be effectively inhibited. [0008] Several classes of mimetic compounds are known to be useful as inhibitors of the. proteolytic enzyme renin. See, for example, U.S. Pat. No. 4,599,198; G.B. 2,184,730; G.B. 2,209,752; EPO 264 795; G.B. 2,200,115 [0009] and U.S. SIR H725; and U.S. Pat. No. 4,599,198 disclose urea-containing hydroxyethylamine renin inhibitors. However, it is known that, although renin and HIV proteases are both classified as aspartyl proteases, compounds which are effective renin inhibitors generally cannot be predicted to be effective HIV protease inhibitors. [0010] Several classes of mimetic compounds have been proposed, particularly for inhibition of proteases, such as for inhibition of HIV protease. Such mimetics include hydroxyethylamine isoteres and reduced amide isosteres. See, for example, EPO 346 847; EPO 342,541; Roberts et al, "Rational Design of Peptide-Bases Proteinase Inhibitors", Science, 248, 358 (1990); and [0011] Erickson et al, "Design Activity, and 2.8 .ANG. Crystal Structure of a C.sub.2 Symmetric Inhibitor Complexed to HIV-1 Protease", Science, 249, 527 (1990). EPO 346 847 discloses certain N-heterocyclic moiety-containing hydroxyethylamine protease inhibitor compounds, but does not suggest or disclose those of the present invention. [0012] Dipeptide isosteres as inhibitors of HIV protease are found in EP application numbers 91309292, 91309028.8 and 91309302.7. BRIEF DESCRIPTION OF THE INVENTION [0013] The present invention is directed to virus inhibiting compounds and compositions. More particularly, the present invention is directed to retroviral protease inhibiting compounds and compositions, to a method of inhibiting retroviral proteases, to processes for preparing the compounds and to intermediates useful in such processes. The subject compounds are characterized as cyclic sulfone- and either urea- or N-heterocyclic moiety-containing hydroxyethylamine inhibitor compounds. DETAILED DESCRIPTION OF THE INVENTION [0014] In accordance with the present invention, there are provided novel retroviral protease inhibiting compounds or a pharmaceutically acceptable salt, prodrug or ester thereof. [0015] Generally, the present invention is a compound of the formula (I'') and a pharmaceutically acceptable salt, prodrug or ester thereof; wherein Q, R.sup.2 and R.sup.6 are as defined below and [0016] W represents wherein Y'' is as defined below; and [0017] t represents 0,1 and 2, preferably 1; [0018] t' represents 1 and 2, preferably 1; [0019] u represents 0, 1 and 2; [0020] R.sup.40, R.sup.41, R.sup.42, R.sup.43, R.sup.48, R.sup.49, R.sup.50 and R.sup.51 independently represent hydrogen and alkyl; Continue reading about Cyclic sulfone containing retroviral protease inhibitors... Full patent description for Cyclic sulfone containing retroviral protease inhibitors Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Cyclic sulfone containing retroviral protease inhibitors patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. 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