Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.

Abstract: The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.

Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.

Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5 R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.

Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided Methods of administration and preparation are provided as well.

Abstract: Compounds of the formula where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.

Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.

Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Abstract: 1 A compound of formula (I) where D is a VLA-4 specificity determinant which does not impart significant IIB/IIIa activity; R41 is a group of the formula (V): U - (CH2)d - V - T wherein U is selected from oxygen, sulphur, a direct bond or —CH2O—, V is selected from nitrogen, oxygen, sulphur, S(O), S(O)2 or a direct bond, d is zero or a number from 1 to 4, and T is selected from a range of variables defined in the application; and other variables are defined in the application, or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof. The compounds are useful in the treatment of disease mediated by the interaction between VCAM-1 and/or fibronectin and the integrin receptor &agr;4&bgr;1. Pharmaceutical compositions and methods of use or treatment are also described and claimed.

Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnostic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: The present invention relates to 2-(benzoylamino)benzoic acid derivatives of the formula I 1

Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1

Abstract: Benzene butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: Phenylalkanoic acid derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a covalent bond or a linker atom or group; A is an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: A compound of formula I′ and pharmaceutically acceptable derivatives thereof including, for example, where applicable or appropriate pharmaceutically acceptable salts thereof. Ar and Ar′ are aromatic or aryl type groups. The compounds have HIV integrase inhibitory properties. Ar, Ar′ and W may be as defined in the specification.

Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

Abstract: Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

Abstract: The present application relates to carboxylic acid amides of general formula wherein A, B and R1 to R3 are defined as in claim 1, processes for preparing them, pharmaceutical compositions containing these compounds and the use thereof and their preparation.

Abstract: Compounds of formula (I) 1

Abstract: The invention relates to a process for the production of dipeptide crystals (generic formula AcXYNH2) with high purity (>95 %), by enzymatic synthesis with a protease in organic media of reversed micelles, starting from derivatives of the two constituent amino acids (AcXOEt and YNH2). A membrane and hydro-cyclone reactor was designed which enables the continuous and simultaneous synthesis and crystallisation of the dipeptides. The dipeptide crystals thus prepared are continuously removed and further separated from the remaining liquid by filtration or centrifugation. After drying, the crystals are dissolved in hot methanol. By decreasing the temperature, the dipeptide re-crystallises, originating a high purity product. After re-crystallisation the product is filtered and dried.

Abstract: Compounds having a structure according to the following formula: are effective in treating disorders such as bone disorders and glaucoma in a subject in need thereof.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.

Abstract: Compounds which are specific or selective agonists of RAR&agr; receptors in preference over RAR&bgr; and RAR&ggr; receptors, and particularly compounds of the formula where R is a H, lower alkyl of 1 to 6 carbons, or a pharmaceutically acceptable salt, are useful for treating a malignant disease or condition in a mammal. In treatment of solid tumors the compound exhibit synergistic anti-proliferative effect with human recombinant interferon.

Abstract: Compounds having Formula 2 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: An hydroxyphenyl derivative selected from the group consisting of a compound of formula and when a compound of formula I comprises a carboxylic acid group pharmaceutically acceptable salts thereof and when a compound of formula I comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein n is 1, 2 or 3, e is 1, 2 or 3, Hal represents a halogen atom (e.g. Cl, Br, F or I), p is 0, 1 or 2, r is 0, 1 or 2, X and X′ each independently represents a single bond, a saturated straight or branched hydrocarbon group of 1 to 4 carbon atoms or a straight or branched hydrocarbon group of 2 to 4 carbon atoms comprising a carbon to carbon double bond, Ra represents H or —CH3, and Raa represents H or —CH3; W may represent an amino acid residue or fragment. These compounds may be used to inhibit the activity of HIV integrase.

Abstract: The present inventintion relates to the formation of an amido ester having the formula:

Abstract: A process for preparing folic acid, which comprises reacting a tetraalkoxypropanol of the general formula I, in which the substituents R are C1-C4-alkyl, with triaminopyrimidone of the formula II and p-aminobenzoyl-L-glutamic acid of the formula III

Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.

Abstract: Disclosed is the (R)-enantiomer of the formula which has unexpectedly been found to possess all of the biological activity of the racemic compound disclosed in the prior art as an RAR&ggr;-specific agonist.

Abstract: The caged amino acid in accordance with the present invention has the structure represented by the following formula 1: where X and Y each represent a halogen atom, an alkyl group, an alkyloxy group, an alkylamino group, or a benzo group; R1 represents a hydrogen atom or an alkyl group; R2 and R3 each represent a hydrogen atom or an alkyl group; A represents an amino acid residue; and M represents a hydrogen atom, an alkali metal, or an alkaline-earth metal.

Abstract: Compounds which are specific or selective agonists of RAR&agr; receptors in preference over RAR&bgr; and RAR&ggr; receptors, and particularly compounds of the formula 1

Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 is

Abstract: A method of separating a racemic mixture of amino acid enantiomers, which entails reacting the mixture with a 4-pentenoyl compound, thereby derivatizing the enantiomers to form two diastereomers, and separating the diastereomers.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: The present invention provides new retinoid compounds and uses of the compounds in humans and animals for chemoprevention of skin and/or breast cancer and for therapy of leukemia.

Abstract: A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HANBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.

Abstract: A class of novel naphthyl glyoxamide compounds of formula (I) is disclosed together with a process for making the novel naphthyl glyoxamide compounds and the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: The present invention provides a bis (aminocarbonylnaphthol) derivative which is useful as a raw material for novel azo pigments by bisamidation of each one carboxyl group of two 2-hydroxynaphthalene-3,6-dicarboxylic acids using an aliphatic or aromatic diamine.

Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopolesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##