Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1. The invention provides recombinant serine protease domains and methods of using peptides comprising a recombinant serine protease domain to screen for compounds that inhibit serine protease activity of matriptase or MTSP1.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: This invention relates to compounds of the Formula (I): 1

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound which is a EP4 agonist.

Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.

Abstract: The present inventors have discovered that 3-Isopropylmalate dehydratase is essential for fungal pathogenicity. Specifically, the inhibition of 3-Isopropylmalate dehydratase gene expression in fungi results in no signs of successful infection or lesions. Thus, 3-Isopropylmalate dehydratase can be used as a target for the identification of antibiotics, preferably antifungals. Accordingly, the present invention provides methods for the identification of compounds that inhibit 3-Isopropylmalate dehydratase expression or activity. The methods of the invention are useful for the identification of antibiotics, preferably antifungals.

Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

Abstract: Derivatives of C2-substituted indan-1-ol compounds, processes for their preparation and their use are disclosed. In particular, the invention relates to compounds of the formula I and to their physiologically acceptable salts and physiologically functional derivatives. The compounds are suitable, for example, for use as anorectics.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compositions and methods of using an MT103 family member, wherein MT103 is the chemical N,N-dicyclohexyl-(1S)-isoborneol-10-sulfonamide. Uses of the compositions include cancer therapy, antibacterials, antifungals, induction of apoptosis, and hormonal antagonists.

Abstract: The present invention provides (bis) sulfonamide derivatives of formula (I) useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: Biphenyl derivatives represented by the following formula (1): 1

Abstract: The present invention provides a preparation containing a compound of the formula (I) 1

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders

Abstract: The present invention relates to novel scyphostatin analogues, which distinguish themselves by acting as SMase inhibitors so that they are of therapeutic use for a number of diseases such as a HIV infection, neurodegenerative diseases, inflammatory diseases, apoplexy, ischemia, myocardial infarction or in the case of atherosclerosis.

Abstract: The present invention relates to microbicides for agricultural or horticultural use containing sulfonamide derivative of, for example, a formula (I): 1

Abstract: Combination therapy comprising anti-diabetic agents and anticonvulsant derivatives useful for the treatment of Type II diabetes mellitus and Syndrome X are disclosed.

Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein. In particular, the invention relates to polysubstituted indan-1-ol compounds of the formula I and their physiologically acceptable salts. The compounds are useful, for example, as anorectics.

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: The present invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.

Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.

Abstract: Sulfonylguanidine compounds corresponding to the tautomeric formulas I and Ia, a method for producing them, pharmaceutical compositions containing them, and methods of using them to prepare medicaments and for treating various medical conditions. The sulfonylguanidine compounds have an affinity for the gabapentin binding site and can be used to treat conditions such as pain, epilepsy, migraine and others.

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

Abstract: The use of bissulfonamides for producing medicines for the treatment of hyperlipidemia. The invention relates to the use of bissulfonamides and their salts for producing medicines for the treatment of hyperlipidemia. The use of compounds of formula I in which the radicals have the stated meanings, and of their salts for producing a medicine for the treatment of hyperlipidemia is described.

Abstract: The present invention is related to anthranilamides of formula I, 1

Abstract: Anticonvulsant derivatives useful for treating depression as monotherapy or combination therapy are disclosed.

Abstract: The present invention includes 16-HETE analogs which are agonists and antagonists of 16-HETE. The compositions may be formulated in pharmaceutically acceptable formulations. The invention also includes methods and products for inhibiting neutrophil adhesion and neutrophil aggregation using the 16-HETE agonists. One method of the invention involves the administration of a 16-HETE agonist in combination with a thrombolytic agent to a patient suffering from, thromboembolic stroke.

Abstract: This invention relates to compounds of the general formula 1

Abstract: Disclosed are compounds of formula X, 1

Abstract: Biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, bicyclic or tricyclic carbon or heterocyclic ring biphenylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: Halo active aromatic sulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to releaser active halogen ions has been utilized in a range of biocidal and fungicidal applications. The most widely used sulfonamide organic compound for these applications has been Chloramine T. This invention deals with nearly discovered halo active aromatic sulfonamide organic compounds and uses of these compounds as biocides, odor control agents, bovine teat cleaners, drugs for cultured fish, soap biocides, stain removal agents, and paint fungicides.

Abstract: The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.

Abstract: The present invention provides improved sulfacetamide and sulfur formulations including sunscreens for the treatment of rosacea.

Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.

Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): 1

Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalk

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 Compound of Formula I and pharmaceutically acceptable sales thereof in the treatment of cyclooxygenase-2 mediated diseases are disclosed.