Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: The present invention relates to a defined crystalline modification of the compound of the formula (I), to processes for its preparation and to its use in agrochemical preparations.

Abstract: Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are described.

Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.

Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.

Abstract: The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.

Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.

Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.

Abstract: This invention relates to a compound of the following formula: wherein R1, R2, R3, G, and Z are defined herein. It also relates to is methods of treating autoimmune disease, cancer, and atherosclerosis with such a compound.

Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.

Abstract: The invention relates to substituted ?-lactone compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.

Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.

Abstract: Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I) in which A and B independently represent any of the groups —ONO2 and —Z—CO—R, wherein Z is an oxygen atom or sulphur atom and R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, or the group in which R1 is hydrogen, or an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, with the proviso that one of A or B is always —ONO2, but never both of them at the same time, when Z is an sulphur atom R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, and when Z is an oxygen atom R is the group

Abstract: The present invention relates to a compound of the formula (I) or salt thereof in which R1 is identical or different at each occurrence and is H, halogen, CN, nitro, SF5, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, [(C1-C8)alkyl]-carbonyl or (C1-C8)alkylsulfonyl, each of the radicals being unsubstituted or substituted,  or is S(O)p—R7, where p=0, 1 or 2 and R7 is (C1-C8)alkyl, (C1-C8)haloalkyl or NR8R9, where  R8 and R9 independently of one another are identical or different and are H, (C1-C8)alkyl, (C2-C8)alkenyl, (C7-C10)arylalkyl, (C7-C10)alkylaryl or (C6-C10)aryl, each of the last-mentioned five radicals being unsubstituted or substituted,  or is a group of the formula where R10 is (C1-C8)alkyl which is unsubstituted or substituted, and W=O or S, A is optionally substituted aryl or an optionally substituted heterocyclic radical, X is O or S, R2,R3,R4, and R5 are identical or different and are H, hal

Abstract: A process for preparing a compound of the formula 1

Abstract: Disclosed are a novel organic acid salt of amlodipine with superb physicochemical properties, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient.

Abstract: This invention relates to dihydro-furan-2-one derivatives, their intermediates and methods of manufacture.

Abstract: The present invention provides antibacterial agents of formula I described herein.

Abstract: A process for the preparation of phthalazines by preparing intermediate (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.

Abstract: This invention relates to in-situ preparation, and stable topical delivery systems of ascorbic acid salts of organic bases that provide skin beneficial properties, including reduction in signs of skin aging, anti-wrinkle, anti-oxidant, and photo-protection from UV and sunlight. The formulation avoids the use of oils, minimizes the importance of the pH of the formulation, allows the incorporation of an aqueous solution of ascorbic acid or alkali metal salts of ascorbic acid in the formulation, does not require packaging the formulation in air tight containers, allows the use of large amounts of ascorbic acid, its salts, and its derivatives, and does not require the use of expensive coatings. Moreover, several ascorbic acid derivatives of different chemical composition can be made in a stable topical formulation by the in-situ combination of readily available starting materials in a water solution, despite the understanding well known in the prior art that such compositions in water are inherently unstable.

Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: 1

Abstract: The invention concerns a compound of formula (I), wherein, for example: R1 is of the formula —NHC(═O)(1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R4 and R5 are hydrogen or methyl; >A-B- is of the formula >C═CH—, >CHCH2, or >C(OH)CH2—(> represents two single bonds); D is O, S, SO, SO2 or —NR7; wherein R7 is hydrogen, R10CO—, R10SO2—, RaOC(Rb)═CH(C═O)—, RcC(═O)C(═O)—, RdN═C(Re)C(═O)—, RfNHC(Rg)═CHC(═O)— or R14CH(R13)(CH2)m—; wherein R10 is (1-6C)alkyl [optionally substituted by, for example, hydroxy or (1-6C)alkanoyl], R11C(O)O(1-6C)alkyl or R12O—; wherein R11 is optionally substituted (1-6C)alkyl; R12 is optionally substituted (1-6C)alkyl; Ra, Rb, Rc, Rd, Re, Rf, Rg are (1-6)alkyl; m is 0 or 1; R13 is cyano; R14 is hydrogen or (1-4C)alkyl; >X—Y— is of the formula >C═CH— or >CHCH2—; and pharmaceutically acceptable salts thereof

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: Process for the preparation of compounds of formula I 1

Abstract: The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.

Abstract: The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.

Abstract: This invention relates to novel dihydropyridine soft drugs of the formula &PHgr;OOR1, where &PHgr; is a dihydropyridine moiety. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibroncho-constriction activity. Use of such soft drug analogs permits the administration of greater doses of the claimed dihydropyridine compounds without intolerable systemic effects. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasim, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders, while avoiding unwanted systemic effects.

Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a &bgr;-dicarbonyl enol ether leaving group.

Abstract: A process for preparing a compound of the formula 1

Abstract: The present invention relates to a class of compounds represented by the Formula I.

Abstract: Compounds of the formula I in which R1, R2, R3, R4, R5, m and n have the meanings cited in the description, are novel effective PDE-inhibitors.

Abstract: The present invention broadly relates to racemic or optically active 5-substituted 3,4-dihydroxy-2(5H)-furanone compounds and their pharmaceutically acceptable salts, useful for treating a pathology in which reactive oxygen species and inflammatory mediators are contributing deleterious factors, such as acute or chronic inflammatory disorders, for example, asthma, rheumatoid arthritis, inflammatory bowel disease, and acute respiratory distress syndrome; neurodegenerative disorders, such as Alzheimer disease, Parkinson disease, amyotrophic lateral sclerosis, traumatic brain injury and multiple sclerosis; cardiovascular diseases, such as atherosclerosis; viral diseases, such as AIDS; skin diseases, such as psoriasis, sunburn and premature aging; and eye diseases, such as glaucoma, cataract, senile macular degeneration, inflammatory eye conditions, trauma, post-traumatic eye disorders, diabetic retinopathy, and eye infections.

Abstract: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).

Abstract: The present invention relates to derivatives of the formula the process for their preparation, and to their uses in therapeutics, especially as drugs with anti-inflammatory, analgesic and chemopreventive properties.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.