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  Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesisUSPTO Application #: 20070021354Title: Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis Abstract: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described. Compounds of the formula: (end of abstract) Agent: Fitzpatrick Cella Harper & Scinto - New York, NY, US Inventors: Stacie S. Canan Koch, Therese N. Alexander, Benjamin J. Burke, Tanya M. Jewell, David J. Kucera, Maria Angelica Linton, Lennert J. Mitchell, Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Mark Barvian, Gary Bolton, Frederick Earl Boyer, Jeffrey J. Machak, Tod Holler, Sean T. Murphy, Michael Melnick, Vara Prasad Josyula USPTO Applicaton #: 20070021354 - Class: 514019000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 2 Peptide Repeating Units In Known Peptide Chain The Patent Description & Claims data below is from USPTO Patent Application 20070021354. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This application is a continuation of U.S. patent application Ser. No. 10/166,979, filed Jun. 11, 2002, which claims the benefit of U.S. Provisional Application No. 60/297,460, filed on Jun. 11, 2001, and U.S. Provisional Application 60/297,729, filed on Jun. 11, 2001. BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] This invention relates to novel compounds useful as HIV protease inhibitors and to the use of such compounds as antiviral agents for treatment of HIV infected individuals. This invention also relates to methods of preparation of these compounds and to intermediates that are useful in the preparation thereof. [0004] 2. Related Background Art [0005] Acquired Immune Deficiency Syndrome (AIDS) causes a gradual breakdown of the body's immune system as well as progressive deterioration of the central and peripheral nervous systems. Since its initial recognition in the early 1980's, AIDS has spread rapidly and has now reached epidemic-proportions within a relatively limited segment of the population. Intensive research has led to the discovery of the responsible agent, human T-lymphotropic retrovirus III (HTLV-III), now more commonly referred to as the human immunodeficiency virus or HIV. [0006] HIV is a member of the class of viruses known as retroviruses. The retroviral genome is composed of RNA which is converted to DNA by reverse transcription. This retroviral DNA is then stably integrated into a host cell's chromosome and, employing the replicative processes of the host cells, produces new retroviral particles and advances the infection to other cells. HIV appears to have a particular affinity for the human T-4 lymphocyte cell which plays a vital role in the body's immune system. HIV infection of these white blood cells depletes this white cell population. Eventually, the immune system is rendered inoperative and ineffective against various opportunistic diseases such as, among others, pneumocystic carini pneumonia, Kaposi's sarcoma, and cancer of the lymph system. [0007] Although the exact mechanism of the formation and working of the HIV virus is not understood, identification of the virus has led to some progress in controlling the disease. For example, the drug azidothymidine (AZT) has been found effective for inhibiting the reverse transcription of the retroviral genome of the HIV virus, thus giving a measure of control, though not a cure, for patients afflicted with AIDS. The search continues for drugs that can cure or at least provide an improved measure of control of the deadly HIV virus. [0008] Retroviral replication routinely features post-translational processing of polyproteins. This processing is accomplished by virally encoded HIV protease enzyme. This yields mature polypeptides that will subsequently aid in the formation and function of infectious virus. If this molecular processing is stifled, then the normal production of HIV is terminated. Therefore, inhibitors of HIV protease may function as anti-HIV viral agents. [0009] HIV protease is one of the translated products from the HIV structural protein pol gene. This retroviral protease specifically cleaves other structural polypeptides at discrete sites to release these newly activated structural proteins and enzymes, thereby rendering the virion replication-competent. As such, inhibition of the HIV protease by potent compounds may prevent proviral integration of infected T-lymphocytes during the early phase of the HIV-I life cycle, as well as inhibit viral proteolytic processing during its late stage. Additionally, the protease inhibitors may have the advantages of being more readily available, longer lived in virus, and less toxic than currently available drugs, possibly due to their specificity for the retroviral protease. [0010] Related inhibitors of HIV proteases have been described in, e.g., U.S. Pat. No. 5,962,640, U.S. Pat. No. 5,932,550, Australian Patent No. 705193, Canadian Patent Application No. 2,179,935, Europan Patent Application No. 0 751 145, and Japanese Patent Application No.100867489. Other related HIV protease inhibitors have been described in K. Yoshimura, et al., Proct. Natl. Acad. Sci. USA, 96, 8675-8680 (1999) and T. Mimoto, et al., J. Med. Chem., 42, 1789-1802 (1999). [0011] On-going treatment of HIV-infected individuals with compounds that inhibit HIV protease has led to the development of mutant viruses that possess protesases that are resistant to the inhibitory effect of these compounds. Thus, to be effective, new HIV protease inhibitors must be effective not only against wild-type strains of HIV, but must also demonstrate efficacy against the newly emerging mutant strains that are resistant to the commercially available protease inhibitors. Accordingly, there continues to be a need for new inhibitors targeting the HIV protease in both wild type and mutant strains of HIV. SUMMARY OF THE INVENTION [0012] This invention relates to compounds useful for inhibiting the activity of HIV-protease of Formula I: [0013] wherein: [0014] R.sup.1 is an aliphatic, carbocyclic or heterocyclic group, or a group having the formula: OR.sup.1', SR.sup.1', NHR.sup.1', N(R.sup.1')R.sup.1'' or C(O)R.sup.1', wherein R.sup.1' is an aliphatic, carbocyclic or heterocyclic group, and R.sup.1'' is H or a C.sub.1-C.sub.6 aliphatic group or R.sup.1' and R.sup.1'' together with the atom to which they are attached form a substituted or unsubstituted heterocyclic ring; [0015] V is C.dbd.O, C.dbd.S or SO.sub.2; [0016] R.sup.2 is an aliphatic group, a carbocyclic group, a carbocyclic-aliphatic group, a heterocyclic group, a heterocyclic-aliphatic group or N(R.sup.2a)R.sup.2b, wherein R.sup.2a is an aliphatic, carbocyclic or heterocyclic group, and R.sup.2b is H or a C.sub.1-C.sub.6 aliphatic group; [0017] W is N, O, C or CH; [0018] when W is N, C or CH, R.sup.2' is H or a C.sub.1-C.sub.6 aliphatic group or R.sup.2 and R.sup.2' taken together with the atom W to which they are attached form an unsubstituted or substituted carbocyclic or heterocyclic ring; [0019] when W is O, R.sup.2' is absent; [0020] X is [0021] where Y' and Y'' are independently selected from H, halo, or a C.sub.1-C.sub.6 aliphatic group; [0022] n is 0, 1 or 2; Continue reading... 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