Abstract: The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Abstract: NHE-1 inhibitor, methods of using the NHE-1 inhibitor and pharmaceutical compositions containing the NHE-1 inhibitor. The NHE-1 inhibitor is useful for the reduction of tissue damage resulting from tissue ischemia.

Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.

Abstract: Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided.

Abstract: The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.

Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

Abstract: A silicone oil-based anhydrous cosmetic or dermatological anhydrous composition having a homogeneous fatty phase wherein said fatty phase contains a silicone oil having the formula wherein R represents alkyl having 1 to 30 carbon atoms, aryl or aralkyl, n represents a whole number between 0 and 100, and m represents a whole number between 0 and 100, provided that the sum of n + m is between 1 and 100; and (ii) a wax in an amount ranging from 3 to 50 percent by weight based on the total weight of said fatty phase having a melting point between 50 and 135° C., comprising at least polymer having a molecular weight between 200 and 1,500 and selected from ethylene homopolymers and copolymers, and a monomer having the formula: ?CH2?CH—R???(II) wherein R? represents alkyl having 1 to 30 carbon atoms, aryl or aralkyl.

Abstract: Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched alkyl group or, taken together with the nitrogen atom to which each is bonded, a non-aromatic heterocyclic ring. Ring A and Ring B are independently further substituted with zero, one or two substituents. Physiologically acceptable salts of structural formula shown above are also included. Also disclosed is a method promoting growth, efficiency of feed utilization and/or production of lean body mass in a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by the structural formula as shown or a physiologically acceptable salt thereof.

Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Abstract: The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selected from the group of immune response modifiers comprising imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines and 1,2-bridged imidazoquinoline amines.

Abstract: The present invention relates to tricyclic compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.

Abstract: Compounds having immunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. are represented by formula I: and pharmaceutically acceptable salts thereof.

Abstract: A metal complex and its use for binding or cleaving a nucleic acid. The metal complex has the formula: M is Pt, Pd, Ni, Co, or Cu; X is aryl, heteroaryl, cyclyl, or heterocyclyl; Y is halogen, tosylate, mesylate, triflate, pyrophosphate, or carboxylate; each of A1 and A2, independently, is N or C; each of A3 and A4, independently, is N, S, or O, wherein A1, A2, A3, and A4 taken together have one positive charge; and each of R1 and R2, independently, is alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, heteroaryloxyl, alkoxylcarbonyl, aryloxylcarbonyl, or heteroaryloxylcarbonyl.

Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

Abstract: The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.

Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; for use as a medicament wherein: n is 0-1; Y is selected from —NH—, —O—, —S—, or —NR7— where R7 is alkyl of 1-6 carbon atoms R5 is chloro or bromo; Y is selected from —NH—, —O—, —S—, or —NR7— where R7 is alkyl of 1-6 carbon atoms R6 is a specified cyclic group which may be substituted by various specified substituents, or R6 is a group —R8—X—R9 where R8 is selected from various cycloalkyl, pyridinyl, pyimidinyl, or phenyl ring; any of which may be optionally subsituted as described, where X is selected from CH2, —NH—, —O—, —S—, CH2 or —NR5— where R5 is alkyl of 1-6 carbon atoms, and R9 is a group (CH2)mR10 where m is 0, or an integer of from 1-3 and R10 is an optionally substituted aryl or optionally substituted cycloalkyl ring of up to 10 carbon atoms,

Abstract: Perylene-3,4:9,10-tetracarboxylic diimides of the general formula I where R1, R2, R3 and R4 are independently hydrogen, chlorine, bromine or substituted or unsubstituted aryloxy, arylthio, arylamino, hetaryloxy or hetarylthio; R5, R6, R7, R8, R9 and R10 are independently hydrogen or long-chain alkyl, alkoxy or alkylthio whose carbon chain may in each case contain up to four double bonds, with the proviso that at least four of these radicals are not hydrogen are prepared and used as liquid-crystalline materials for electronic, optoelectronic and photonic applications, for coloration of macromolecular organic and of inorganic materials, as fluorescent dyes and as laser dyes and also as organic materials for solar collectors and electroluminescence applications.

Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.