Abstract: The present invention relates to anti-viral uses of leflunomide product, alone or in combination with other anti-viral agents, or in combination with a pyrimidine such as uridine.

Abstract: Disclosed is a method of inhibiting acute and chronic tissue transplant rejection in a subject with a tissue transplant. The method comprises the step of administering to the subject an effective amount of a compound represented by Formula (I): The values of the variables in Formula (I) are described herein.

Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.

Abstract: Methods of inducing immune tolerance by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed: Additionally methods of suppressing an immune response by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed. Further disclosed are methods for treating autoimmune diseases by administering an immunosuppressive agent and a compound represented by Formula (I). The variables of Formula (I) are described herein.

Abstract: The present invention is directed to gelatinous elastomer compositions that are useful for topical application of biologically active agents. In certain embodiments, the invention is directed to a gelatinous elastomer composition comprising about 1.0% to 50.0% block copolymer, about 0% to 98% mineral and/or synthetic oil, and about 0.0% to 98% triglyceride oil, about 0-15.0% free fatty acids, about 0-30% of a tack modification agent, about 0-20.0% of a biologically active agent and, optionally a phytosterol, ceramide and/or bisabolol. The gelatinous elastomer compositions are useful for applying a biologically active agent to a mammal. In certain embodiments, the gelatinous elastomer composition is formed into a molded article.

Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.

Abstract: Disclosed are compositions and methods related to the ceramide synthesis pathway and various diseases and disorders associated therewith, such as insulin resistance and inflammation.

Abstract: This disclosure generally relates to chemicals that affect sensory processes. More particularly, this present invention relates to peripheral sensory compounds (including, e.g., 2-Isopropyl-5-methyl-cyclohexanecarboxylic acid [2?-hydroxy-2?-(3?-hydroxy-phenyl)-ethyl]-N-methyl-amide) that are useful in sensory refreshment, inhibit the perception of itch and pain, and alleviation of skin irritation, itch, and pain. These compositions have surprising pharmacokinetic properties that allow a prolonged duration of pharmacological actions and may be administered topically or systemically.

Abstract: A method of treating a hyperproliferative disorder, including a cancer, in a subject in need of such treatment, comprising administering to said subject a pharmaceutical combination containing a treatment effective amount of: (a) a vitamin A derivative (i.e., a retinoid), or a pharmaceutically acceptable salt thereof, and an inhibitor of microtubule structure or function; or (b) a combination containing fenretinide (i.e., N-(4-hydrophenyl) retinamide, 4-HPR) and ABT-751 (i.e., N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide). Vitamin A derivatives that may be useful for this invention according to (a) include, but are not limited to, all-trans-retinoic acid, 13-cis-retinoic acid, and fenretinide. Microtubule inhibitors that may be useful for this invention according to (a) include, but are not limited to, inhibitors of the Vinca binding domain (e.g., vincristine, vinblastine, vinorelbine, and cryptophycin 52), inhibitors of the Taxane domain (e.g.

Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.

Abstract: The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.

Abstract: Provided is a substance which is a safe material such as a food component and an extract of a natural product and has a stronger effect of ameliorating a cerebral function (effect of ameliorating a metabolism of monoamines as an intracerebral neurotransmitter and ameliorating deterioration in memory and learning due to hypofunction of a cholinergic neuron). The present invention provides a composition for ameliorating a cerebral function, comprising an alkali-stable lipid from an acetic acid bacterium, N-acylsphinganine or N-2?-hydroxypalmitoyl-sphinganine, as an active ingredient.

Abstract: The present invention relates to the induction of hypothermia in humans in a predictable and dose responsive fashion by use of a pharmaceutical composition comprising a combination of (1) vanilloid receptor agonists, capsaicinoids or capsaicinoid-like agonists reaching and binding to vanilloid receptors, and (2) cannabinoids or cannabimimetic agonists reaching and binding to cannabinoid receptors, thereby inducing hypothermia, thus benefiting patients suffering from illnesses characterized by tissue anoxia.

Abstract: The method and process for producing youthful appearing, small-pored, and smooth skin comprises pre-treating the skin topically with retinoic acid, applying a contaminant in oil to the skin, and removing the contaminate by exploding or rupturing it with laser light. When treating the face, removing the contaminant requires only about 4 minutes. The laser light itself does not injure the skin but the rupture of the contaminant produces thermal injury in the high dermis leaving the epidermis intact. Repeated intermittent laser treatments and applications of topical retinoic acid produces the desired results in the skin indefinitely as long as the treatment and applications are continued.

Abstract: The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: Small molecule screening via high-throughput screening (HTS) methods was employed to identify compounds useful for treating or preventing cancer (such as compounds that enable cells to overcome E6-oncoprotein-mediated drug resistance) or neurodegenerative disorders (such as Huntington's disease, HD). Compounds were identified that potentiate the lethality of anti-tumor agents as well as rescue a disease-state lethality. These compounds are acylated secondary amines referred to herein as indoxins and revertins.

Abstract: The present invention relates to a new medical use of fenretinide or bioactive derivatives thereof, particularly to the use of fenretinide or bioactive derivatives thereof in the preparation of a medicament for eliminating or killing tumor stem cells in a subject or for treating and/or preventing a tumor disease originating from tumor stem cells in a subject.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract: The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.

Abstract: A cooling topical cosmetic or dermatological preparation which comprises (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexane carboxamide and/or (1R,2S,5R)-N-(4-cyanomethyl-phenyl)-2-isopropyl-5-methylcyclohexane carboxamide, in combination with menthoxypropanediol.

Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.

Abstract: Provided is a hair cleansing composition comprising (A) an amphipathic amide lipid, (B) an anionic surfactant and (C) a silicone. The hair cleansing composition of the present invention has advantages such as protecting hair from physical or chemical stimulation and preventing split ends or hair breakage without impairing its cleansing ability and feeling upon use, and moreover, gives to hair after shampooing a pleasant feeling to the touch and moisture retention properties such as natural smoothness, moist feeling, and suppleness which healthy hair inherently possesses, and has excellent stability.

Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.

Abstract: The disclosure concerns substituted pyrroles of formula (I): wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same and uses thereof, in particular as anti-cancer agents.

Abstract: Disclosed are compounds comprising analogs of quinic acids or shikimic acids having anti-inflammatory properties. The compounds are suitable for oral administration, stable, and demonstrate significant efficacy in inhibiting NF-kB, inhibiting leukocyte adhesion, and inhibiting other factors and cytokines known to be involved in inflammatory disease.

Abstract: The present invention relates to a pseudoceramide represented by the following formula (I) and a cosmetic composition comprising the same: wherein Z represents —OH and Y represents —OH, ?with the proviso that X is Z represents —OH and X represents —OH, with the proviso that Y is Y represents —OH and X represents —OH, with the proviso that Z is R represents a linear or branched, saturated or unsaturated aliphatic hydrocarbon group; and when substituted, R has one or more —OH groups.

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The present invention includes methods for treatment and prophylaxis of diseases, post-surgical disorders and bacterial infections associated with lactosylceramide. The methods generally provide for administration to a subject one or more compounds that alter the activity of VEGF pathway members, including LacCer synthase (GalT-V/VI), PECAM1, VEGFR, VEGF or related pathway members to treat a subject suffering from or susceptible to a condition caused or contributed to by VEGF. The present invention also relates to methods for detecting and analyzing compounds with therapeutic capacity to treat such condition.

Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: Disclosed are merocyanine derivatives of formula (1), wherein R1 and R2 independently from each other are branched C4-C22alkyl; or branched C4-C12 alkenyl; R3 and R4 independently from each other are cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; wherein at least one of R3 and R4 is cyano; R5 and R6 independently from each other are hydrogen; C1-C6alkyl; C5-C8cycloalkyl which may be substituted by one or more than one C1-C4alkyl; and R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl. The compounds are useful as UV absorbers for protecting human hair and skin against the damaging effect of UV radiation.

Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.

Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis.

Abstract: Combination therapy comprising the administration of an 11?-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: A fragrance composition having an excellent diffusivity and long-lasting property of fragrance and a cosmetic, toiletry, bath composition, food and drink and pharmaceutical having an excellent diffusivity and long-lasting property of fragrance by using a novel fixative. A compound represented by the following general formula (1) is incorporated in a fragrance composition or the foregoing products. The amount of the compound of the general formula (1) to be incorporated in the fragrance composition is preferably from 0.01 to 90% by weight. The amount of the compound of the general formula (1) to be incorporated directly in the foregoing products is preferably from 0.0001 to 2.0 times (by weight) the weight of the aroma composition and/or composition to be incorporated therein. In this arrangement, a fragrance composition or products having an enhanced diffusivity and long-lasting property of fragrance can be obtained without causing any safety problem on human being.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.

Abstract: The disclosure provides methods for treating fatty liver disease and associated conditions by inhibiting the synthesis of glucosphingolipids, as exemplified by the use of glucosylceramide synthase substrate analogs.

Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.

Abstract: Compounds that cause reversible night blindness may be used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. Provided are methods and compositions using such compounds and their derivatives to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions. Such compounds and their derivatives may be used as single agent therapy or in combination with other agents or therapies.

Abstract: The present invention is directed to a topical composition comprising a counterirritant active ingredient and a sensate that provides a cooling sensation to the skin that is topically perceptible to an adult human subject for greater than about 90 minutes, e.g. greater than about 120 minutes, say greater than about 150 minutes, when applied in an effective amount over an area on the back of a hand, elbow, lower back or shoulder region. In one embodiment, the sensate can be encapsulated. The sensate can alternatively be bound to an ion exchange resin or adsorbed onto an adsorbant.

Abstract: Invented are novel polyamine conjugates which have been readily obtained using as key-step the condensation of linear, conformationally restricted, cyclic and branched polyamines or suitably protected derivatives with vitamin A derivatives. These compounds inhibit the ribozyme ribonuclease P (RNase P) and the production of interleukin-2 (IL-2) and interferon-? (INF-?) by peripheral blood mononuclear cells in vitro.

Abstract: The present invention relates to compounds with the formula (I) or a pharmaceutically acceptable salt thereof: The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of 11-?-hsd-1, the method comprising administering to a mammal an effective amount of a compound of formula (I).

Abstract: The present invention relates to compounds as inhibitors of enzymes having histone deacetylase activity, to the processes for the preparation of those compounds, and to their use for the treatment of diseases which are associated with hypoacetylation of histones and/or other molecules, or in which induction of hyperacetylation has a beneficial effect for example by inhibition of proliferation and/or induction of differentiation and/or induction of apoptosis in transformed cells, such as cancer. Furthermore, the compounds are useful for the treatment of other proliferative diseases, for therapy or prophylaxis of conditions associated with abnormal gene expression.

Abstract: A clonogenic neurosphere assay is described that carries out high throughput screens (HTS) to identify potent and/or selective modulators of proliferation, differentiation and/or renewal of neural precursor cells, neural progenitor cells and/or self-renewing and multipotent neural stem cells (NSCs). Compositions comprising the identified modulators and methods of using the modulators and compositions, in particular to treat neurological disorders (e.g. brain or CNS cancer) or damage are also disclosed.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.