Abstract: Described are methods for treating, preventing, or reducing the risk of the onset of Alzheimer's disease by administering a therapeutically effective amount of an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (“HMG CoA reductase inhibitor”) to a patient who is at risk for a coronary or cerebrovascular event or at risk for Alzheimer's disease.

Abstract: Liposomal-encapsulated taxane or an antineoplastic derivative thereof or a mixture thereof is provided which is used to effect a therapeutically enhanced method of treating cancer. The liposomal encapsulated paclitaxel allows for administration to a patient in less than one hour.

Abstract: 4-phenylbutyrate treatment of cells from both X-ALD patients and X-ALD knockout mice results in decreased levels of and increased &bgr;-oxidation of very-long-chain fatty acids; increased expression of the peroxisomal protein ALDRP; and induction of peroxisome proliferation. ALDP and ALDRP are functionally related, and ALDRP cDNA can complement X-ALD fibroblasts. Dietary 4-phenylbutyrate treatment is effective, producing a substantial reduction of very-long-chain fatty acid levels in the brain and adrenal glands of X-ALD mice.

Abstract: The present invention relates to fuingicidally effective compositions containing at least one pentacyclic triterpene compound.

Abstract: The present invention relates to compositions for the protection, treatment and repair of connective tissues in humans and animals comprising any or all of anabolic, anti-catabolic, and anti-oxidant agents, including aminosugars, S-adenosylmethionine, arachadonic acid, GAGs, pentosan, collagen type II, tetracyclines or tetracycline-like compounds, diacerin, super oxide dismutase, and L-ergothionine and to methods of treating humans and animals by administration of these novel compositions to humans and animals in need thereof.

Abstract: A composition is described, which comprises a cationic, hydrophilic, amine containing polymer, chosen from the group consisting of native chitosan and cationic derivatives thereof; cationic polyethylene compounds; DEAE-4; or polyornitine; bound to an anionic scavenger substance, which is (a) either chosen from the group consisting of anionic ethylene amine compounds, tetraazacykloalkane-N,N,N,N-tetraacetic acids; and polymer derivatives of porphyrines, or (b) is an endogenous compound.

Abstract: The present invention relates to fungicidally effective compositions containing at least one pentacyclic triterpene compound.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: This invention relates to new propanolamine derivatives presented by the following formula [I]: wherein R1 hydrogen or lower alkenyloxy, R2 is carboxy(lower)alkoxy or protected carboxy(lower)alkoxy, R3 is hydrogen or N-protective group, n is an integer of 1 or 2, and salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-pollakisuria activities, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: The present invention provides compounds which have, particularly, an inhibitory activity on production of melanin, a cell activating activity and an anti-bacterial activity, are derived from natural sources, and are safe and not harmful. One or more compounds represented by the following general formula are contained: wherein R1 represents —CH2OH, —COOR6 or —COOX, whereupon X is a group capable forming a salt and R6 represents hydrogen or a C1 to C3 lower alkyl group; R2 to R5 each represent hydrogen or a methyl group; and . . . A . . . represents ═C(CH3)—, —C(CH3)═, —C(═CH2)—, —CH(CH3)— or —C(OH)(CH3)—.

Abstract: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.

Abstract: The role of the &egr; isozyme of protein kinase C (“PKC&egr;”) in pain perception, particularly hyperalgesia, methods of lessening pain through administration of inhibitors of PKC&egr;, methods of identifying compounds that modulate pain, and pharmaceutical compositions comprising an inhibitor of PKC&egr; and PKC&egr;-independent analgesic agent are disclosed.

Abstract: The invention relates to novel anthracene compounds useful in the treatment of allergic, inflammatory conditions, tumor conditions and therapeutic compositions containing such compounds. The compounds of the present invention are 9-acyloxy-substituted 1,5-dichloroanthracene or analogs thereof. According to the practice of the invention, there are provided 9-acyloxy substituted 1,5-dichloroanthracene compounds according to formula III: wherein R represents a straight or branched chain alkyl group having 1 to 6 carbons which may be substituted with one or more groups of R1, or R represents phenyl or benzyl which may be substituted with one or two groups of R2; wherein R1 is selected from the group consisting of halogen, —NO2, —OCH3, OCH2CH3, and —OCH2CH2CH3; and wherein R2 is selected from the group consisting of a straight or branched chain alkyl group having 1 to 4 carbons, halogen, —NO2, —OCH3, —OCH2CH3, and —OCH2CH2CH3.

Abstract: The present invention is directed to a formulation comprising a lipid-regulating agent dissolved or dispersed in at least one oil and an emulsifier or emulsifier blend, the resulting mixture being capable of forming an emulsion upon dilution in an aqueous medium.

Abstract: Novel compounds are disclosed that have the chemical structure of Formula (IIB), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases. wherein the R groups include the following: R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C1-C12 esters, C1-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, C1-C12 alcohols, (C1-C12)( C1-C12) ethers, C1-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls; R2 is selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, and C1-C12 acyl, and C5-C12 aryl.

Abstract: A method of treating cancer with a pharmaceutical composition containing a pine root (Deutero Mycetes) fungal metabolite or an analog or derivative thereof.

Abstract: 4-phenylbutyrate treatment of cells from both X-ALD patients and X-ALD knockout mice results in decreased levels of and increased &bgr;-oxidation of very-long-chain fatty acids; increased expression of the peroxisomal protein ALDRP; and induction of peroxisome proliferation. ALDP and ALDRP are functionally related, and ALDRP cDNA can complement X-ALD fibroblasts. Dietary 4-phenylbutyrate treatment is effective, producing a substantial reduction of very-long-chain fatty acid levels in the brain and adrenal glands of X-ALD mice.

Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.

Abstract: This invention relates to new propanolamine derivatives presented by the following formula [I]: 1

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.

Abstract: Methods are described for preventing or reducing the risk of a first occurrence of a cardiovascular event using an HMG-CoA reductase inhibitor alone or in combination with another lipid altering agent. Subjects to be treated are those having an average serum total cholesterol level, an average to mildly elevated serum low-density lipoprotein cholesterol level, and a below average serum high-density lipoprotein cholesterol level, with no history of clinically evident coronary disease.

Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano and crop protection agents containing these compounds.

Abstract: Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.

Abstract: Compounds of formula 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, Y is cyclopropyl optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and —CR1═CR1—CR1═CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, —CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, 13 COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 indep

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: The present invention relates to fungicidally effective compositions containing at least one pentacyclic triterpene compound.

Abstract: A compound of formula (I), wherein R1 is carboxy or protected carboxy, R2 and R3 are each independently hydrogen, hydroxy, or protected hydroxy, R4 is hydrogen or halogen, R5 is aryl substituted with halogen, amino, hydroxy or protected hydroxy, R6 is aryl optionally substituted with halogen, amino, hydroxy or protected hydroxy, A1 and A2 are each independently lower alkylene, and (II) is (III), (IV), (V) or (VI) or its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.

Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries,

Abstract: A compound represented by general formula (I-2) or a pharmaceutically acceptable acid-addition salt thereof, useful as an anti-microbial against Helicobacter pylori and as a medicinal composition for treating Helicobacter pylori infection, wherein Ar represents phenyl, biphenyl or naphthyl each having a at least one substituent selected from the group consisting of halogen, cyano, nitro, carboxy, C1-C18 alkyl, C1-C18 alkoxy, C3-C18 cycloalkyl, C7-C18 aralkyl, C8-C18 arylalkenyl, C7-C18 aralkyloxy, optionally substituted phenoxy, optionally substituted C2-C19 alkoxycarbonyl, and optionally substituted C8-C19 aralkyloxycarbonyl, provided the case where Ar represents phenyl substituted by halogen, cyano, nitro, carboxy, C1-C18 alkyl, optionally substituted C2-C19 alkoxycarbonyl or C8-C19 aralkyloxycarbonyl is expected.

Abstract: The claimed invention pertains to methods for treating a patient who is at risk for a vascular (e.g., cardiovascular, cerebrovascular) event comprising administering to the patient an effective amount of a lipid-modifying drug. The claimed methods are particularly effective in patients having a lipid profile comprising a low Low Density Lipoprotein and a low High Density Lipoprotein.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

Abstract: A pharmaceutical composition is described, comprising a lipid-lowering drug such as lovastatin, simvastatin, pravastatin and fluvastatin and L-carnitine or an alkanoyl L-carnitine, which, while conserving the efficacy of the lipid-lowering drug, is substantially devoid of the toxic or side effects typical of such drugs.

Abstract: An object of the present invention is to provide an agricultural/horticultural preparation having improved photostability, comprising MK 8383 substance. A composition according to the present invention comprises a compound of formula (I): wherein R1 represents hydrogen atom, or a lower alkyl or alkyl carbonyl group, and R2 represents hydroxyl group or a lower alkoxy group, or its salt, and cyclodextrins.

Abstract: A benzenesulfonamide compound of the formula (I) (R1 is hydroxy, C1˜4 alkoxy, NR6R7 (each R6 and R7 is, independently, H or C1˜4 alkyl.); R2 is H, C1˜4 alkyl; R3, R4 are C1˜4 alkyl, halogen trifluoromethyl; R5 is H, C1˜4 alkyl, halogen, trifluoromethyl; Y is cis-vinylene, trans-vinylene; and the symbol (i) is single bond, double bond.), non-toxic salt thereof or cyclodextrin clathrate thereof and an antagonist of EP1 receptor which is a prostaglandin E2 receptor subtype comprising it as an active ingredient. The present invention compounds of the of the formula (I) can bind strongly to EP1 receptor which is a prostaglandin E2 receptor subtype and scarcely bind to the other receptor subtypes. Therefore, they are considered to be useful as antipyretic agents, as analgesics or as treating agent for pollakiuria having little side effect.

Abstract: Use of betulinic acid and/or its derivatives for inhibiting and/or preventing angiogenesis is described. Compositions containing betulinic acid derivatives with or without betulinic acid can be used for these purposed.

Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.

Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: where R1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or —(CH2)mCOOX, where m is 2 or 3 and X is H, methyl, or ethyl; R2 is halo or NHY, where Y is hydrogen, loweralkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or —(CH2)mCOOX, where m and X are as defined for R1 above; and R4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.

Abstract: Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sup.1 or Ar.sup.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sup.1 and Ar.sup.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.

Abstract: A pharmaceutical composition for inhibiting cysteine protease which comprises a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group; R.sup.2, R.sup.3 and R.sup.4, same or different, are a bond, an amino acid residue or a group of the formula:--Y--R.sup.5 --in which R.sup.5 is a group resulting from imino group removal from an amino acid residue;Y is --O--, --S-- or --NR.sup.6 -- in which R.sup.6 is a hydrogen atom or a lower alkyl group;A is ##STR2## Z is a hydrogen atom, an acyl group or an optionally substituted hydrocarbon group; n is 1 or 2;provided that when n is 1, then A is ##STR3## and Y is --S-- or --NR.sup.6 --, and, at least one of R.sup.2, R.sup.3 and R.sup.4 is the formula --Y--R.sup.5 --, provided that when further all Y are --NR.sup.6 --, at least one of the amino acid residues is not bound to amhydrogen atom at the .alpha.-carbon thereof but substituted via carbon;provided that when n is 2 and Z is an aldehyde group, then R.sup.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

Abstract: Liposomal-encapsulated taxane or an antineoplastic derivative thereof or a mixture thereof is provided which is used to effect a therapeutically enhanced method of treating cancer. The liposomal encapsulated paclitaxel allows for administration to a patient in less than one hour.

Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.