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Novel depsipeptides and process for preparing sameRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Phosphorus ContainingNovel depsipeptides and process for preparing same description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060194714, Novel depsipeptides and process for preparing same. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a divisional of U.S. patent application Ser. No. 10/213,389 filed, Aug. 6, 2002, which claims priority from U.S. Provisional Application 60/310,313 filed Aug. 6, 2001. FIELD OF THE INVENTION [0002] The present invention relates to novel depsipeptides compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial agents. The invention also relates to methods of producing these novel depsipeptide compounds and intermediates used in producing these compounds. BACKGROUND OF THE INVENTION [0003] The rapid increase in the incidence of gram-positive infections--including those caused by resistant bacteria--has sparked renewed interest in the development of novel classes of antibiotics. A class of compounds that have shown potential as useful antibiotic agents is the cyclic depsipeptides. A notable member of the cyclic depsipeptides is the A-21978C lipopeptides described in, for example, U.S. Pat. RE 32,333; RE 32,455; RE 32,311; RE 32,310; U.S. Pat. Nos. 4,482,487; 4,537,717; and 5,912,226 and International Patent Applications WO01/44272; WO01/44274; and WO01/44271. Additionally, the A54145 class of compounds described in U.S. Pat. Nos. 4,994,270; 5,039,789; and 5,028,590 have also been shown to possess antibiotic activity. [0004] Daptomycin, also known as LY 146032, is comprised of an n-decanoyl side chain linked to the N-terminal tryptophan of a three-amino acid chain linked to a cyclic 10-amino acid peptide. Daptomycin has potent bactericidal activity in vitro and in vivo against clinically relevant gram-positive bacteria that cause serious and life-threatening diseases. These bacteria include resistant pathogens, such as vancomycin-resistant enterococci (VRE), methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide intermediate susceptible Staphylococcus aureus (GISA), vancomycin-resistant Staphylococcus aureus (VRSA), coagulase-negative staphylococci (CNS), and penicillin-resistant Streptococcus pneumoniae (PRSP), for which there are few therapeutic alternatives. See, e.g., Tally et al., 1999, Ext. Opin. Invest. Drugs 8:1223-1238. [0005] Despite the promise that existing antibacterial agents have shown, the need for novel antibiotics continues. Many pathogens have been repeatedly exposed to commonly used antibiotics. This exposure has led to the selection of variant antibacterial strains resistant to a broad spectrum of antibiotics. The loss of potency and effectiveness of an antibiotic caused by resistant mechanisms renders the antibiotic ineffective and consequently can lead to some life-threatening infections that are virtually untreatable. As new antibiotics come to market pathogens may develop resistance or intermediate resistance to these new drugs, effectively creating a need for a stream of new antibacterial agents to combat these emerging strains. In addition compounds that exhibit bactericidal activity offer advantages over present bacteriostatic compounds. Thus, novel antibacterial agents would be expected to be useful to treat not only "natural" pathogens, but also intermediate drug resistant and drug resistant pathogens because the pathogen has never been exposed to the novel antibacterial agent. New antibacterial agents may exhibit differential effectiveness against different types of pathogens. SUMMARY OF THE INVENTION [0006] The present invention provides novel compounds that have antibacterial activity against a broad spectrum of bacteria, including drug-resistant bacteria, and processes for making these compounds. [0007] The present invention provides, in one aspect, compounds of Formula I: and salts thereof; wherein: [0008] (a) R is 2-butyl, isopropyl or 2-(2'-aminophenacyl); [0009] (b) each R.sup.1 and R.sup.6 is independently hydrido or methyl; [0010] (c) R.sup.2 is methyl or --CH.sub.2CH.sub.2CH.sub.2R.sup.8; [0011] (d) R.sup.3 is methyl or --CH.sub.2CH.sub.2CH.sub.2CH.sub.2R.sup.9; [0012] (e) R.sup.4 is hydrido or methoxy; [0013] (f) R.sup.5 is hydroxy or carboxyamino; [0014] (g) each of R.sup.7, R.sup.8 and R.sup.9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino; [0015] (h) provided that [0016] (1) when R.sup.2 is --CH.sub.2CH.sub.2CH.sub.2R.sup.8, R.sup.7 is other than [0017] wherein R.sup.10 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, iminoamino, or phosphonamino; [0018] (2) when R.sup.2 is methyl, R.sup.7 is other than [0019] wherein each of R.sup.11 and R.sup.12 is hydrido, C.sub.6-C.sub.18 unsubstituted alkanoyl, C.sub.8-C.sub.18 unsubstituted alkenoyl, C.sub.8-C.sub.18 unsubstituted alkyl, or C.sub.8-C.sub.18 select substituted alkyl; or alternatively, R.sup.11 and R.sup.12 together are C.sub.8-C.sub.18 alkylidenyl. [0020] In another aspect, the present invention also provides pharmaceutical compositions including compounds of Formula I and methods of use thereof. [0021] In a further aspect the present invention provides a process for preparing the compounds of Formula I. [0022] In yet a further aspect, the invention provides compounds useful as intermediates for the preparation of the compounds of Fomula I. DETAILED DESCRIPTION OF THE INVENTION Definitions Continue reading about Novel depsipeptides and process for preparing same... Full patent description for Novel depsipeptides and process for preparing same Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Novel depsipeptides and process for preparing same patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. 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