Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is  wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.

Abstract: Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): 1

Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.

Abstract: The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: Compound of formula (I): 1

Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.

Abstract: The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.

Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: The invention relates to compounds of the formula 1

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Abstract: Compounds having therapeutic utility are of the formula wherein NB2 is heterocycloalkyl and R1 and R2 are each various substituents or a cyclic group.

Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: The invention concerns novel ary1-{4-fluoro-4-[(2-pyridin-2-yl-ethylamino)-methyl]-piperidin-1-yl}-methanone derivatives of formula(1) wherein X is a hydrogen, fluorine or chlorine atom useful as medicines in particular having antidepressant, analgesic, anxiolytic and neuroprotective effects.

Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.

Abstract: Compounds of the formula 1

Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Abstract: The invention is directed to physiologically active compounds of general formula (I): 1

Abstract: A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.

Abstract: This invention provides caspase inhibitors having the formula 1

Abstract: Described herein are compounds that are useful as caspase inhibitors having the formula: 1

Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).

Abstract: Compounds of formula I 1

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.

Abstract: This invention relates to compounds of formula 1

Abstract: Phenylalanine derivatives of formula (1) are described: 1

Abstract: The invention relates to compounds of formula (I):

Abstract: Novel hydrazones of formula [2] having the following structural formula are provided, which are useful intermediates to form active ingredients of herbicides, wherein R3 is hydrogen, alkyl, haloalkyl, or alkoxy alkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4] or [Q-5] as defined herein.

Abstract: Compounds according to the formula: 1

Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.

Abstract: Dipropargyl acetamide derivatives of following Formula 1 which are photoresist monomers, polymers thereof, and photoresist compositions containing the same. The photoresist polymer has high etching resistance, adhesiveness and post-exposure delay stability. As a result, the photoresist composition is suitable to form a fine pattern in a deep ultraviolet region.

Abstract: A process for the preparation of a 4-aryl-3-oxymethyl-piperidine of structure (1) 1

Abstract: Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

Abstract: A thrombin receptor antagonist having the formula 1

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: Herbicidal fluorovinyloxyacetamide compounds of formula (I) are useful for protecting crops from weeds: wherein: R1 is a phenyl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy and halogen; R2 is a C1-6 alkyl; or R1 and R2 together with the nitrogen atom to which they are bound form a 5-, 6- or 7-membered nitrogen heterocycle optionally having one or more ring oxygen atoms, double bonds and C1-6 alkyl substituents; R3 is a phenyl or thiophen-2-yl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, methylenedioxy and halogen; and R4is a perfluoro C1-6 alkyl group.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The present disclosure describes novel compounds and compositions which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair growth. The present compounds and compositions may also be useful against a variety of disorders including, for example, multi-drug resistance, human immunodeficiency virus (HIV), cardiac injury, and neurological disorders, and may be useful for controlling parasites and invoking immunosuppression.

Abstract: The present invention relates to a process for the racemization of N-acylamino acids of the formula (I)

Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: Novel arylalkylamino compounds exhibiting calcilytic properties are provided.

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

Abstract: The subject-matter of the present invention is novel compounds of the type of esters derived from alkylenediaminediacetic acid or alkylenediaminetriacetic acid and their-process of preparation. The invention also relates to the use of these compounds in cosmetic and pharmaceutical compositions, in particular for protecting the body against oxidative stress.