Abstract: The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The present invention provides compounds that can modulate the activity of a target protein, such as a phosphatase, that selectively binds phosphorylated peptides or proteins. The present compounds can be useful in treating diseases or disorders, including, for example, diabetes and obesity, that are connected directly or indirectly to the activity of the target protein.

Abstract: The present invention relates to novel compounds of the formula (I) in which A, B, W, G and Het are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases.

Abstract: The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, P-M are rings substituted by a linear group. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

Abstract: The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity

Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.

Abstract: This invention relates to novel arylalkyl cyclic amine derivatives. This invention also relates to chemokine receptor antagonists that are be effective as therapeutic agents and/or preventive agents for diseases such as atherosclerosis, rheumatoid arthritis, transplant rejection, psoriasis, asthma, ulcerative colitis, glomerulonephritis, multiple sclerosis, pulmonary fibrosis, and myocarditis, in which tissue infiltration of blood monocytes and lymphocytes plays a major role in the initiation, progression or maintenance of the disease. Furthermore, chemokine receptor antagonists also inhibit the interaction of viruses, which attack blood monocytes and lymphocytes, through the use of a chemokine receptor. One such example is the HIV virus.

Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

Abstract: The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors.

Abstract: Compounds of formula (I) in free or salt form, where A is a C6-C15 monovalent aromatic group. R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy, C1–C8-alkoxy-C1–C8-alkyl or acyloxy, or a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or CON(R3)R4, provided that R2 is C1–C8-alkyl, acyl or CON(R3)R4 when R1 is hydrogen, R3 and R4 are each independently hydrogen, or C1–C8-alkyl, together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, and Zl, Z2, Z3 and Z4 are each independently N or CR5, at least one of them being CR5, and R5 is hydrogen, C1–C8-alkyl or C1–C8-alkoxy.

Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.

Abstract: Methods for making UV screening compositions by combining benzoxazolyl benzene derivatives of formula (I): wherein R1 is hydrogen, C1-20-alkyl or C2-20-alkenyl; R2 and R3 are independently a group —C(R4,R5)C(R6)?C(R7,R8) (a) or a group —C(R4?,R5?)CH(R6?)CH(R7?,R8?) (b), wherein R4, R5, R6, R7, R8, R4?, R5?, R6?, R7? and R8? are independently, hydrogen, C1-10-alkyl or C2-10-alkenyl, or C2-10-alkyl or C3-10-alkenyl containing at least one oxygen atom interrupting the hydrocarbon chain; or wherein R4, R5, R6, R4?, R5? and R6? are hydrogen, C1-10-alkyl or C2-10-alkyl containing at least one oxygen atom interrupting the hydrocarbon chain, or alkyl substituted by silane or oligosiloxane moiety, and one of R7 and R8 or R7? and R8? is a silane or oligosiloxane moiety and the other one of R7 and R8 or R7? and R8? is hydrogen; and X is phenylene or naphthylene, or substituted phenylene or naphthylene with a cosmetic base.

Abstract: Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.

Abstract: The present invention relates to certain sulfonamido-substituted geometrically restricted indolinones of the formula: wherein R1–R12 and X are variables defined herein. The sulfonamido-substituted geometrically restricted indolinones of the preferred embodiments of the present invention modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I wherein Ar1, X, n, R1, R2, R3 and Q are as defined herein.