Abstract: Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT, stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.

Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.

Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.

Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.

Abstract: Methods and topical pharmaceutical formulations are provided for the treatment of nail fungus (onychomycosis). The invention involves a pharmacologically active antifungal agent, plus a pharmaceutically acceptable base in a formulation having a pH of 7.5 to about 13.0, preferably about 8.0 to 11.5, and most preferably about 8.5 to 10.5. These basic formulations permeate the nail and are effective in treating fungal infections of the nail and surrounding tissues.

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 invention provides methods for treating a patient with chronic lymphocytic leukemia of B cells (B-CLL). One method comprises administering to a patient with B-CLL, one or more benzamide derivatives, the benzamide derivatives including MS-275 and related compounds. Another method comprises administering to a patient with B-CLL, one or more of the benzamide derivatives, and additionally administering to the patient one or more antibodies immunospecific for 1D10 antigen. Additional methods for inducing apoptosis of B-CLL cells and for increasing expression of 1D10 antigen in B-CLL cells using the benzamide derivatives are also provided.

Abstract: The present invention provides a compound of formula I: 1

Abstract: The invention provides a method for inhibiting c-jun activation in mammalian or avian cells comprising contacting the cells with a substance that inhibits the activity of Janus family kinase 3 (JAK-3). The invention also provides a therapeutic method for preventing or treating a pathological condition in a mammal wherein c-jun activation is implicated and inhibition of its activation is desired comprising administering to a mammal in need of such therapy, an effective amount of a substance that inhibits the activity of JAK-3. Novel compounds that are JAK-3 inhibitors, as well as pharmaceutical compositions comprising the compounds are also provided.

Abstract: The invention relates to 2-(butyl-1-sulfonylamino)-N-[1(R)-(6-methoxy-pyridin-3-yl)propyl]benzamide of the formula I 1

Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to compositions of such compounds; intermediates for the syntheses of such compounds; methods for making such compounds; and methods for treating conditions associated with MMP, tumor necrosis factors (or “TNFs”), and/or aggrecanase activity, particularly pathological conditions.

Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.

Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: 1

Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions. The instant invention also teaches methods to treat or prevent diabetes associated hyperlipidemia, cellular redox imbalances, hypercholesterolemia, hypertriglyceridemia, and atherosclerosis, comprising administering the compounds of the invention to a mammal in need thereof.

Abstract: The present invention relates to compounds of the Formula 1

Abstract: Novel quaternary amidino-containing compounds of the general formulae (I), (II), (III), (IV), (V) and (VI): including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and the compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: Disclosed are pyridine amido derivatives of the formula wherein X, Y, and R1 to R6 are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.

Abstract: This invention relates to aryl urea compounds in combination with cytotoxic or cytostatic agents for use in treating raf kinase mediated diseases such as cancer.

Abstract: Novel active compound combinations of compounds of the formula (I) 1

Abstract: The present invention relates to a compound of the formula (I) or salt thereof 1

Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: 1

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present invention relates to metabolites of (3-{[4-tert-butyl-benzyl)-(pyridine-3-sulfonyl)-amino]-methyl}-phenoxy)-acetic acid.

Abstract: A method of modulating the level of activated, NF-&kgr;B in cells by contacting cells with a cyanoguanidine compound of general formula I wherein n is 0, 1 or 2; each R independently represents halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, cyano, amino, sulfo or carboxy groups; Q is a straight or branched, saturated or unsaturated C4-20 divalent hydrocarbon radical; X is a bond, O, S, amino, carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino; A is di-(C1-4 alkoxy)phosphinoyloxy, C1-4 alkoxycarbonyl, C1-4 alkoxycarbonylamino, saturated or unsaturated C3-12 carbocyclic ring or C3-12 heterocarbocyclic ring optionally substituted with one or more R1; R1 being independently selected from the group consisting of halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, cyano, amino, carboxy, sulfo, carboxamido,

Abstract: The present invention concerns the use of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea in the pharmaceutical field. In particular, it proposes the use of a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea for the preparation of solid pharmaceutical forms, and likewise a method of synthesis to obtain such a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridiyl)sulphonyl]-urea.

Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: Compounds of the formula I; 1

Abstract: Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents for various diseases concerning &agr;4 integrin.

Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.

Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and assay reagents are substrates for tyrosinase and may be represented by the formula TyrX—B—ThrAg*. The compounds of formula TyrX—B—ThrAg* are capable of releasing a therapeutically active agent or assayable substance (ThrAg) at a desired location. TyrX— being a residue of an optionally substituted tyrosine analogue.

Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: 1

Abstract: This invention relates to aryl substituted pyridines of Formula I: 1

Abstract: A substance for inducing apoptosis represented by specific formulae. A pharmaceutical composition which can be used for an anticancer agent containing said substance.

Abstract: Novel, stable pharmaceutical formulations for the oral administration of high purity torsemide modification II are disclosed. These formulations release high purity torsemide modification II in water at a constant and high purity rate, and the high purity torsemide modification II therein does not rearrange to torsemide modification I over time. Methods for their manufacture are also disclosed.

Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: 1

Abstract: The invention relates to the use of an NK-1 receptor antagonist for the treatment or prevention of benign prostatic hyperplasia (BPH).

Abstract: 4-Substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones having the Formula (I): 1

Abstract: Compositions comprising antimuscarinic compounds that have been modified to render them substantially irreversible, such as by quaternization of the heterocyclic ring nitrogen, have improved properties when administered intravesically for treatment of bladder diseases, particularly urinary incontinence. Pharmaceutical compositions and methods of treatment using these improved compounds or improved routes of administration re disclosed.