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  Therapeutic compositions and methods of treatment with capsianoside-type compoundsUSPTO Application #: 20080103102Title: Therapeutic compositions and methods of treatment with capsianoside-type compounds Abstract: The present invention discloses the use of certain compounds as therapeutic agents, and in particular as analgesics and anti-inflammatory agents. Such compounds include, for example, certain diterpene monoglycosides and diterpene diglycosides. The compounds of the present invention may be synthesized or isolated from the fruit of the genus Capsicum, and in particular may be isolated from sweet bell peppers (C. annuum). Pharmaceutically-acceptable salts, enantiomers, diasteriomers, racemic mixtures, enantiomerically-enriched mixtures, solvates, and prodrugs of such compounds are also disclosed. Pharmaceutical compositions and methods of using such compounds, including pharmaceutical compositions and methods of using such compounds in combination with one or more active ingredients, are also disclosed. (end of abstract) Agent: Keith R. Lange - Lincoln University, PA, US Inventor: Barry Miles Belgorod USPTO Applicaton #: 20080103102 - Class: 514025000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), O-glycoside The Patent Description & Claims data below is from USPTO Patent Application 20080103102. Brief Patent Description - Full Patent Description - Patent Application Claims
RELATED APPLICATION DATA [0001] This application claims priority to U.S. Provisional Patent Application No. 60/863,302, filed on Oct. 27, 2006, the entirety of which is hereby incorporated by reference. FIELD OF THE INVENTION [0002] The present invention relates to analgesic compositions and methods with compounds known as capsianosides and related compounds. The compounds may be synthesized or they may be isolated from the fruit of the genus Capsicum, in particular Capsicum annuum. This invention further relates to the therapeutic uses of such compounds as analgesics and as anti-inflammatory agents. BACKGROUND OF RELATED TECHNOLOGY [0003] A primary focus of drug research is the development of analgesics for pain management. Analgesics render sensory pathways insensible or less sensible to pain, whereas anesthetics act on all sensory pathways rendering them insensible to pain, temperature, touch, proprioception and skeletal muscle tone. As such, although anesthetics can be used for pain management, their utility is limited by their inhibition of these other sensory pathways. For example, it may be desired to control a patient's pain associated with an oral mucosal lesion without interfering with senses of touch, proprioception (to avoid biting of the tongue) or taste (so as not to interfere with appetite), which is not generally possible with topical anesthetics (for example, Benzocaine) which are not able to selectively inhibit pain. The use of analgesics to control pain in such circumstances is therefore desirable. [0004] Analgesics are generally classified as either narcotic (opioids) or non-narcotic. Narcotic analgesics primarily act on the central nervous system and carry potentially life-threatening side-effects such as addiction, impaired higher cortical function and depressed respiration. As a result, their use is regulated and they may only be prescribed by licensed practitioners. Non-narcotic analgesics include salicylates, such as aspirin; acetaminophen; and non-steroidal anti-inflammatory drugs ("NSAIDS"), such as cyclooxygenase-2 ("Cox-2") inhibitors. Such non-narcotic analgesics can be limited in their ability to control pain and may have the side effects of chemical irritation, anticoagulation, myocardial infarction and stroke. Accordingly, there is a continuing need for the discovery and development of new analgesics, and in particular non-narcotic analgesics, that are useful for the localized management of pain without an undesirable side effects profile. [0005] In this regard, various plant-derived compounds have been investigated for their analgesic properties. For example, capsaicin, a vanillyl alkaloid that is the source of pungency in hot peppers, has been used to treat the pain of arthritis, osteoarthritis, and various peripheral neuropathies. See, for example, Cordell and Araujo, The Annals of Pharmacotherapy, (1993) 27:330; Levinson, (January/February 1995) The Sciences, pp. 13-15. However, the therapeutic usefulness of capsaicin is limited due to an adverse side effects profile that includes burning sensations and erythema, and such side effects may persist over time. By way of further example, extracts of sweet bell peppers (Capsicum annuum) have been shown to exhibit analgesic properties (see, for example, U.S. Pat. Nos. 6,060,060 and 6,086,888), but the specific compounds responsible for such analgesic effects have not been identified. Furthermore, as such extracts must be derived from naturally-occurring fruit, their production and practical use is limited. [0006] Moreover, certain capsianosides (diterpene glycosides) that occur naturally in sweet bell peppers have been identified, for example capsianosides A-F and I-V reported both by Izumitani et al. ("Novel Acyclic Diterpene Glycosides, Capsianosides A-F and I-V from Capsicum Plants" (Solanaceous Studies. XVI) Chem. Pharm. Bull. (1990), 38(5):1299-1307) and by Iorizzi et al. ("New Glycosides from Capsicum annuum L. Var. acuminatum. Isolation, Structure Determination, and Biological Activity" J. Agric. Food Chem. (2001), 49:2022-2029), some of which have been shown to inhibit the activity of angiotensin-converting enzyme in vitro, and therefore may be useful as anti-hypertensive agents (see, for example, published Japanese Patent Application No. 02-138289 (1990)). However, no experimental or clinical data is known to have been reported that establishes the therapeutic utility of such compounds. SUMMARY OF THE INVENTION [0007] The present invention is directed to certain compounds and their use as therapeutic agents, and in particular as analgesics and anti-inflammatory agents. Such compounds include, for example, various diterpene monoglycosides and diterpene diglycosides which may be synthetically or semi-synthetically produced, or which may be isolated from the fruit of the genus Capsicum, and in particular may be isolated from sweet bell peppers (C. annuum). Pharmaceutically-acceptable salts, enantiomers, diasteriomers, racemic mixtures, enantiomerically-enriched mixtures, solvates, and prodrugs of such compounds are also included in the present invention. Pharmaceutical compositions, combinations of compounds of the present invention and other therapeutic ingredients, such as analgesics and anti-inflammatory agents, are also provided by the present invention, as are methods of using such pharmaceutical compositions, compounds and combinations. Objects of the present invention include providing pharmaceutical compositions, compounds, and combinations for the treatment of pain, discomfort and inflammation, in a safe and effective manner. [0008] In one aspect, the present invention is directed to pharmaceutical compositions that includes a therapeutically effective amount of a compound according to Formula I: or a pharmaceutically-acceptable salt, enantiomer, diasteriomer, racemic mixture, enantiomerically-enriched mixture, solvate, or prodrug of Formula I, in a pharmaceutically effective carrier, wherein R.sub.1 is a carbohydrate moiety; R.sub.2 is H or C(O)R.sub.4; R.sub.3 is H, a carbohydrate moiety, or a substituted or unsubstituted C.sub.1-C.sub.20 group; and R.sub.4 is a substituted or unsubstituted C.sub.1-C.sub.20 group. In certain embodiments, R.sub.1 and R.sub.3 are independently selected from the group consisting of glucose, galactose, rhamnose, xylose, and arabinose; R.sub.1 is glucose, R.sub.2 and R.sub.3 are each H; and each of R.sub.2, R.sub.3, and R.sub.4 independently comprises one or more aromatic rings. The compound may be present in an amount that is therapeutically effective to treat analgesia or reduce inflammation in a mammal. [0009] In certain embodiments, the compound according to Formula I is a compound of Formula II: [0010] In certain embodiments, a prodrug of a compound according to Formula I is a compound according to Formula III: [0011] , wherein R.sub.5 is a hydrolyzable sugar, such as glucose. [0012] In certain embodiments, a prodrug of a compound according to Formula I is a compound of Formula IV: [0013] Further, pharmaceutical compositions of the present invention may be in the form of an immediate-release, controlled-release, or sustained-release orally-administrable composition, such as a pill, tablet, capsule, gelcap, lozenge, throat spray, solution, emulsion, cream, paste, gel, cough drop, dissolvable strip, lollipop, or gum; in the form of a topically-administrable composition, such as a liquid solution, liquid spray, emulsion, cream, paste, gel, lotion, foam, or impregnated dressing; in the form of an occularly-administrable composition, such as eye-drops; and may be administered to the sinuses, throat, or lungs, for example in the form of inhalable particles, an inhalable solution, droplets, or an aerosol. [0014] Compounds of the of the present invention may be produced synthetically or semi-synthetically; or may be isolated and purified from a naturally occurring organism, such as from a fruit of the genus Capsicum, such as C. annuum, in which case they may be isolated and purified away from the cellular debris of the naturally occurring organism. [0015] In certain embodiments, the present invention is directed to pharmaceutical compositions including one or more therapeutic agents in combination with a compound of the present invention, such as an analgesics and/or anti-inflammatory agents, for example an NSAID selected from the group consisting of salicylates, acetaminophen, ibuprofen and COX-2 inhibitors. [0016] In another aspect, the present invention is directed to pharmaceutical compositions including a therapeutically effective amount of a compound according to Formula II in a pharmaceutically effective carrier. The compound of Formula II may be provided in an analgesically-effective amount, and may be provided in combination with one or more therapeutic agents, such as those discussed above. [0017] In another aspect, the present invention is directed to pharmaceutical compositions including a therapeutically effective amount of a compound according to Formula I, as defined above, or a pharmaceutically-acceptable salt, enantiomer, diasteriomer, racemic mixture, enantiomerically-enriched mixture, solvate, or prodrug of Formula I, in a pharmaceutically effective carrier, and which is present in an analgesically-effective amount. The substituents and compounds of Formula I may be those noted above. Such compounds may be present in an analgesically-effective amount of between about 0.01 mg to about 500 mg per unit dose, and between about 1 mg to about 100 mg per unit dose. Such pharmaceutical compositions may be administered as noted above. [0018] In another aspect, the present invention is directed to a method for effecting analgesia or reducing inflammation in a mammal, comprising administering to a patient in need thereof a pharmaceutical composition comprising a therapeutically effective amount, which may be an analgesically-effective amount, of a compound according to Formula I, defined above, or a pharmaceutically-acceptable salt, enantiomer, diasteriomer, solvate, or prodrug of Formula I, in a pharmaceutically effective carrier. The substituents and compounds of Formula I may be those noted above. Such methods may include administering compounds of the present invention in the manners noted above alone or in combination with other noted therapeutic agents, and in a therapeutically effective amount of between about 0.01 mg to about 500 mg per unit dose, and between about 1 mg to about 100 mg per unit dose. BRIEF DESCRIPTION OF THE DRAWINGS [0019] FIG. 1 shows HPLC chromatograms and UV spectra of fraction BMBW-M40i. 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