| Oxadiazolones and derivatives thereof as ppar delta agonists -> Monitor Keywords |
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Oxadiazolones and derivatives thereof as ppar delta agonistsRelated 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, Five-membered Hetero Ring Containing At Least One Nitrogen Ring Atom (e.g., 1,2,3-triazoles, Etc.), 1,3,4-thiadiazoles (including Hydrogenated), Oxadiazoles (including Hydrogenated)Oxadiazolones and derivatives thereof as ppar delta agonists description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070179191, Oxadiazolones and derivatives thereof as ppar delta agonists. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application is a continuation of International Application No. PCT/EP2005/002950 filed on Mar. 19, 2005 which is incorporated herein by reference in its' entirety which also claims the benefit of priority of European Patent Application No. 04/007879.2 filed on Apr. 1, 2004. FIELD OF THE INVENTION [0002] The invention relates to compounds useful in the treatment of metabolic disorders and diseases affecting the central nervous system. More specifically, the present invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator-activated receptor delta (PPARdelta) agonist activity. BACKGROUND OF THE INVENTION [0003] The peroxisome proliferator-activated receptors (PPAR) are transducer proteins belonging to the steroid/thyroid/retinoid receptor superfamily. The PPARs were originally identified as orphan receptors without known ligands, but were known for their ability to mediate the pleiotropic effects of fatty acid peroxisome proliferators. These receptors function as ligand-regulated transcription factors that control the expression of target genes by binding to their responsive DNA sequences as heterodimers with RXR. The target genes encode enzymes involved in a number of metabolic and cell growth/cell proliferation/cell differentiation inductions. These then provide targets for the development of therapeutic agents for the treatment of metabolic and central nervous system disorders, among others. [0004] PPAR agonists are well known and have been described in the prior art, see U.S. Pat. No. 6,200,995 to De La Brouse-Elwood et. al.; WO 03/043997 to Johnston et. al. and WO 01/00603 and WO 02/092590 to Keil et. al.). Compounds comprising an oxadiazolone feature as inhibitors of factor Xa were disclosed in DE 101 12 768 A1 and oxodiazolones have also been described as oral hypoglycemic agents in WO 96/13264. [0005] The present invention then, comprises compounds which provide therapeutic variable moderation of lipid and/or carbohydrate metabolism and are thus suitable for the prevention and/or treatment of diseases such as type-2 diabetes, atherosclerosis and the diverse disease states that are a result thereof. Another purpose of the invention is to treat neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving inflammation of the central nervous system and/or other peripheral neuropathies. SUMMARY OF THE INVENTION [0006] The present invention comprises a series of compounds which moderate the activity of peroxisome proliferators--activated receptors (PPAR) has been found. The compounds are suitable in particular for activating PPARdelta and PPARalpha receptors, however the extent of the relative activation of the receptor will vary depending on the specific compound administered. DETAILED DESCRIPTION OF THE INVENTION [0007] Compounds of the present invention are generically described by formula I, below: wherein, [0008] X is --CH.sub.2 or a bond; [0009] R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently selected from the group comprising H, F, Cl, Br, --CF.sub.3, (C.sub.1-C.sub.4) alkyl, (C0-C.sub.4) alkylenee-O--(C0-C.sub.4) alkylenee-H, SCH.sub.3, S(O)CH.sub.3, S(O).sub.2CH.sub.3, CN, --OCF.sub.3, --OCHF.sub.2, and --OCH.sub.2F; [0010] Z is a bond or --CH.sub.2; [0011] Y is O, --S--, --S(O) or --S(O).sub.2; [0012] W is --CH.sub.2 or --CH.sub.2CH.sub.2; [0013] one of U and V is N the other is --S-- or --O--; [0014] R.sub.5 is selected from the group comprising of (C.sub.1-C.sub.8) alkyl, (C.sub.1-C.sub.6) alkylenee-O--(C.sub.0-C.sub.4) alkylenee-H, (C.sub.0-C.sub.6) alkylene-phenyl, (C.sub.1-C.sub.6) alkylene-O--(C.sub.0-C.sub.4) alkylene-phenyl, (C.sub.3-C.sub.6) cycloalkyl, (C.sub.2-C.sub.8) alkenyl, and where (C.sub.1-C.sub.8) alkyl or alkylene can be substituted 1-2 times by --OH or --O--(C.sub.1-C.sub.4) alkyl; [0015] R.sub.6, R.sub.7 are independently selected from the group comprising H, F, Br, --CF.sub.3, --OCF.sub.3, (C.sub.1-C.sub.6) alkyl, (C.sub.0-C.sub.4) alkylene-O--(C.sub.0-C.sub.4) alkylene-H, --SCF.sub.3, --SF.sub.5, --OCF.sub.2, --CHF.sub.2, --OCHF.sub.2, --OCH.sub.2F, O-phenyl, phenyl, NO.sub.2; as well as their physiologically acceptable salts and tautomeric forms. [0016] Another embodiment of this invention is a compound of the formula I in which [0017] X is a bond. [0018] Another embodiment of this invention is a compound of the formula I wherein one or more substituents have the following meaning: [0019] U is S and, [0020] V is N or [0021] U is --N-- and [0022] V is --S-- or [0023] U is --O-- and, [0024] V is --N-- or [0025] U is --N-- and [0026] V is --O--; [0027] and/or [0028] U is --S--, [0029] V is --N--, [0030] Z is a bond; [0031] and/or [0032] U is N, [0033] V is O, [0034] Z is a bond, [0035] X is a bond; [0036] and/or [0037] X is a bond, [0038] Z is a bond; [0039] and/or [0040] R.sub.6 is in para position; [0041] and/or [0042] R.sub.7 is H or F, preferably H; [0043] and/or [0044] R.sub.2, R.sub.3, and R.sub.4 are H, and, [0045] R.sub.1 is selected from the group consisting of H, F, Cl, Br, CF.sub.3, (C.sub.1-C.sub.4) alkyl, (C.sub.0-C.sub.4) alkylene-O--(C.sub.0-C.sub.4) alkylene-H, --SCH.sub.3, S(O)CH.sub.3, S(O).sub.2CH.sub.3, --CN; [0046] and/or [0047] Y is O or S, preferably 0; [0048] and/or [0049] W is CH.sub.2 [0050] and/or [0051] R.sub.5 is (C.sub.1-C.sub.4) alkyl, (C.sub.1-C.sub.4) alkylene-O--(C0-C4) alkylene-H or (C.sub.1-C.sub.4) alkylene-O--(C.sub.0-C.sub.4) alkylene-phenyl, where alkylene can be substituted by O--(C.sub.0-C.sub.4) alkylene-H. [0052] Another embodiment of this invention is a compound of the formula I in which [0053] X is a bond or CH.sub.2, preferably a bond; [0054] R.sub.1 is selected from the group comprising H, F, Cl, Br, CF.sub.3, (C.sub.1-C.sub.4) alkyl, O--(C.sub.1-C.sub.4) alkyl, SCH.sub.3, S(O)CH.sub.3, S(O).sub.2CH.sub.3, CN; [0055] R.sub.2 is H or F; [0056] R.sub.3 is H, Br or O--(C.sub.1-C.sub.4) alkyl; [0057] R.sub.4 is H; [0058] Z is a bond or CH.sub.2, preferably a bond; [0059] Y is O, S, S(O) or S(O).sub.2, preferably O; [0060] W is CH.sub.2 or CH.sub.2CH.sub.2, preferably CH.sub.2; [0061] U is --S-- and [0062] V is --N-- or [0063] U is --N-- and [0064] V is --S-- or [0065] U is --N-- and [0066] V is O; [0067] R.sub.5 is (C.sub.1-C.sub.6) alkyl or (C.sub.2-C.sub.6) alkenyl, wherein the (C.sub.1-C.sub.6) alkyl can be substituted 1-2 times by --OH; [0068] R.sub.6 is in para position and is CF.sub.3, SF.sub.5, OCH.sub.3, phenyl; [0069] R7 is H or F. [0070] Another embodiment of this invention is a compound of the formula I in which X is a bond; R.sub.1 is --Cl or --CH.sub.3; R.sub.2, R.sub.3 and R.sub.4 are H; Z is a bond; Y is O; W is --CH.sub.2; U is --S-- and Continue reading about Oxadiazolones and derivatives thereof as ppar delta agonists... Full patent description for Oxadiazolones and derivatives thereof as ppar delta agonists Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Oxadiazolones and derivatives thereof as ppar delta agonists 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. Each week you receive an email with patent applications related to your keywords. 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