Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.

Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.

Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.

Abstract: Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly(ADP-ribose)polymerase-1 inhibitors (PARP-1 inhibitors).

Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic benzophenone derivative of formula (1), selected from the crystal modifications (B) and (C), wherein the crystal modification (B) is characterized by a peak in the X-ray diffraction pattern at a d-spacing of about 7.70; and wherein the crystal modification (C) is characterized by a peak in the X-ray diffraction pattern at a d-spacing of about 7.06; and (b) a dispersing agent selected from anionic, non-ionic and amphoteric surfactants; for protecting the human skin from browning and skin aging. The new crystal modification (C) represents a thermodynamically stable compound of formula (1) at 25° C. This modification is therefore suitable in dispersions comprising micro-fine particles.

Abstract: The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate.

Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.

Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.

Abstract: The present invention provides 4,6-disubstituted pyrimidine compound useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.

Abstract: The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.

Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic compound which has a UV-Vis spectrum with a maximum from 380 to 420 nm; and (b) an anionic dispersing agent for protecting the human skin from browning and skin aging.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.

Abstract: The present invention relates to the preparation of 3-hydroxyamidino-phenylalanine derivatives in highly pure form which can be used for example as urokinase inhibitors. The present invention further relates to the use of high-purity 3-hydroxyamidinophenylalanine derivatives for preparing 3-amidinophenylalanine derivatives.

Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.

Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative.

Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.

Abstract: The present invention provides a compounds the formula (IV): and methods for producing an ?-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.

Abstract: The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates in particular to compounds containing hydroxyamidine or hydroxyguanidine groups.

Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic compound which has a UV-Vis spectrum with a maximum from 380 to 420 nm; and (b) an anionic dispersing agent for protecting the human skin from browning and skin aging.

Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2? together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is formula (ii): where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof; inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases i

Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted piperazines, according to Formula I A compound of formula I wherein Z is bond or NH; R1 is aryl or optionally substituted heteroaryl; R2 is H, optionally substituted C1-6alkyl, or optionally substituted C2-6alkenyl; R3 and R7 are independently H, optionally substituted C1-6alkyl, or aryl; R4 is H or optionally substituted C1-6alkyl; R5 is H or C1-6alkyl; R6 is H or C1-6alkyl; and X and X? are independently O or H2; or wherein R3 and R4 together form a part of morpholinyl, piperadinyl, or aziridinyl ring; and pharmaceutically acceptable salts thereof.

Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.

Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.

Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.

Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycoalkyl or (CH2)n-aryl, wherein aryl is a heteromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.

Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Abstract: Compounds of the following formula (I): where A, a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.