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

Abstract: This invention relates to N-acylamino aryl derivatives of the formula 1

Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.

Abstract: Compounds which have utility in the treatment of conditions associated with altered mitochondrial function.

Abstract: N-(2-aryl-propionyl)-amides of formula (I) are described.

Abstract: Novel thyroid receptor ligands are provided having the general formula I 1

Abstract: Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, &agr;, &bgr;, &ggr;, &dgr;, &egr;, &sgr;, &thgr; and &OHgr;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Abstract: Novel thyroid receptor ligands are provided having the general formula I 1

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The invention relates to novel aryl ketones of the formula (I) 1

Abstract: A method of synthesizing a compound having the formula: 1

Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.

Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

Abstract: Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide.

Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.

Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.

Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.

Abstract: The present invention relates to a novel class of androgen receptor targeting agents (ARTA), which contain a haloacetamide or azide moiety and are alkylating agents.

Abstract: Novel biphenyl derivatives of the general formula I 1

Abstract: The invention related to colchinol derivatives of the formula (I): Wherein; R1; R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazol

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them.

Abstract: The present invention relates to a novel process for producing an N-formyl-neutral-amino acid and N-formylaspartic acid. The present invention also relates to a novel process for producing N-formyl-&agr;-L-aspartyl-L-phenylalanine methyl ester as a precursor of aspartame and aspartame, as well as a method of making a precursor of aspartame and aspartame by using the same.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: The present invention relates to new beta-agonists of general formula 1: 1

Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, &agr;, &bgr;, &ggr;, &dgr;, &egr;, &sgr;, &thgr; and &OHgr;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Abstract: A method for preparing a solid support material for carrying out a chemical reaction, said method comprising the following steps: (i) reacting an amino functionalised solid material with a carboxylic acid having at least two similarly protected amino groups to form amide bonds between them, (ii) removing protecting groups in a single step, (iii) optionally repeating steps (i) and (ii) one or more times using the product of the preceding step as the amino functionalised solid material, and (iv) connecting a linkage agent to at least some of the free NH2 groups of the product. The method increases the loading capacity of the solid support material. It is particularly useful in connection with peptide synthesis.

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: Compounds having Formula I 1

Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water.

Abstract: This invention relates to compounds of the Formula (I): 1

Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.

Abstract: Compounds of the formula I, 1

Abstract: Disclosed are efficient methods for loading amino derivatives onto trityl chloride resins and for cleaving chemically modified amino derivatives from trityl chloride resins. Methods for making a library of discrete chemically modified amino derivatives also disclosed.

Abstract: Amides of the general formula I 1

Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor &bgr;, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.

Abstract: The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of carcinogenic diseases. Further, the invention refers to a a pharmaceutical composition comprising the alkylating peptides of the invention.

Abstract: Compounds of the formula (I) in which R1 is CN, or C(═NH)—NH2, CON(R3)2 or [C(R4)2]nN(R3)2, each of which is unsubstituted or monosubstituted by C(═O)R3, COOR3, or3 or by a conventional amino-protecting group, or W is —NR3CO—, —NR3COC(R4)2, NR3C(R4)2) or —C(R4)2NR3C(4)2—, X is —C(R3)2—, —[C(R3)2]2—, —C(R—3)2O— or —C(R3)2NR3, Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl, T is OR3, N(R3)2, N(R3)2CON(R3)2, a monocyclic or bicyclic, saturated, unsaturated or aromatic heterocyclic radical having from 1 to 4 N, O and/sor S atoms which is unsubstituted or monosubstituted, disubstituted or trisubstituted, or a phenyl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.

Abstract: Novel biphenyl derivatives of the general formula (I) in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the &agr;v&bgr;6 integrin receptor. The novel compounds can be used, in particular, as medicaments.

Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: Described are 6-substituted indanoyl amino acid conjugates as defined in claim 1 of the present invention as potent plant elicitors and efficient mimics of the phytotoxin coronatine. Also, processes for producing the improved elicitors are provided, which allow a rapid and convenient access to large quantifies of the highly active compounds. Furthermore, there are compositions and plant protecting agents described, comprising as active ingredient a compound of the present invention. The plant protecting agents are useful for inducing resistance to pathogens in plants. The compositions may also be used to selectively induce senescence in fruit of plants.

Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: 1

Abstract: A new crystalline form of nateglinide is provided. The new crystalline form is described by X-ray powder diffraction. Processes for making the new crystalline form of nateglinide are also provided.

Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C independently represents a hydrogen atom or a monovalent substituent; and X and X′ independently represents a hydrogen atom or a monovalent substituent.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Abstract: The invention relates to novel compounds having formula (I) 1

Abstract: A compound having general formula 1