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6503925 1-phenyl-benzimidazole compounds and their use as GABA-A receptor modulators  
Chemical compounds of the formula as well as pharmaceutical compositions containing them and methods for their use in the treatment of disorders and diseases responsive to modulation of the GABAA...
6500842 8-hydroxy-7-substituted quinolines as anti-viral agents  
The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral...
6498154 Cyclic regimens using quinazolinone and benzoxazine derivatives  
This invention relates to cyclic combination therapies utilizing, in combination with progestins, estrogens, or both, compounds which are progesterone receptor antagonists of the general...
6495565 β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α  
The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and...
6495566 Tetrahydroquinoline derivatives as glycine antagonists  
The present invention provides compounds of formula (I) or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the...
6495548 Lactam inhibitors of matrix metalloproteinases, TNF-α and aggrecanase  
The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3...
6495568 Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors  
Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents...
6492366 Cyano-indole serotonin-reuptake inhibitor compound  
A compound selected from those of formula (I): wherein:R1 and R2 each independently represent hydrogen or, alkyl,T1 and T2 each independently represent alkylene,G represents a heterocyclic group...
6486151 N-oxides of heterocyclic esters, amides, thioesters, and ketones  
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...
6486183 Antivirals  
Compounds of formula (I): wherein Rx is cyano or bromo; R1 is halo; R2 is C1-C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.
6482832 Heterocyclically substituted amides, their production and their use  
Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, and also possible physiologically tolerated salts, in which the variables...
6482834 Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases  
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these...
6479488 Tetrahydroquinoline derivatives as EAA antagonists  
Compounds of formula (I) or salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy,...
6479514 Quinoline-aminomethyl-pyridyl derivatives with anti-helicobacter activity  
Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.
6479515 Heterocyclic benzenesulphonamide compounds as bradykinine antagonists  
The invention concerns compounds selected among the group consisting of (i) compounds of formula (I) wherein: Het1 represents a nitrogenous heterocycle with 5 apices, in particular imidazole,...
6472394 MCH antagonists and their use in the treatment of obesity  
Disclosed are compounds represented by structural formula I: or a pharmaceutically acceptable salt, ester or solvate thereof, whereinW is R1—CR3R12NR4C(O)— or R11C(O)NR4—;the dotted line is an...
6472408 Dimeric compounds  
The invention relates to dimeric compounds comprising two 5-amino-5,6,7,8-tetrahydroquinoline fragments joined together by a divalent linking group, processes for their preparation, intermediates...
6472406 Sulfonamidomethyl phosphonate inhibitors of beta-lactamase  
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase...
6472416 Sulfonylphenylpyrazole compounds useful as COX-2 inhibitors  
The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
6465486 Pyridyl/quinolinyl imidazoles  
Certain imidazo pyridines/quinolines of the formula: wheren is 0, 1, 2;X is independently selected from the group consisting of C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy,...
6465482 Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression  
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein:R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl,...
6458789 2-aminopyridine derivatives and combinatorial libraries thereof  
The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1 to R5 have the meanings provided herein. The invention further relates to...
6458805 Formulation of sulfonamides for treatment of endothelin-mediated disorders  
Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the...
6455520 Benzamide derivatives and their use as cytokine inhibitors  
The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno,...
6455541 Suppression, by 5-lipoxygenase inhibitors, of bone resorption  
The present invention focuses upon a method for inhibiting bone resorption. This method involves administering a 5-lipoxygenase inhibitor to a subject in an amount inhibiting the effects of an...
6451812 Farnesyl protein transferase inhibitors for treating arthropathies  
The present invention is concerned with the finding that farnesyl protein transferase inhibitors are useful for preparing a pharmaceutical composition for treating arthropathies such as rheumatoid...
6448265 Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity  
The pyrazoles and pyrazolopyrimidines of the formula wherein R1, R2, R3, R4 and A are as defined herein, have corticotropin releasing factor (CRF) antagonist activity. As such, they are effective...
6448280 Angiotensin II antagonists against disorders associated with impaired neuronal conduction velocity, especially diabetic neuropathy  
This invention relates to the use of angiotensin II antagonists in treating or preventing the development of disease conditions associated with impaired neuronal conduction velocity, such as...
6440995 Quinolin-4-yl derivatives  
Phenyl substituted quinolin 4-yl derivatives and pharmaceutical compositions with activity as NMDA-receptor subtype selective blockers. The compounds of the invention modulate neuronal activity...
6436960 Farnesyl transferase inhibitors having a piperidine structure and process for preparation thereof  
The present invention relates to a novel piperidine derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts...
6432979 Method of treating or inhibiting colonic polyps and colorectal cancer  
This invention provides a method of treating or inhibiting colonic polyps or treating or inhibiting colorectal cancer in a mammal in need thereof which comprises administering to said mammal an...
6429213 Cyclic hydroxamic acids as metalloproteinase inhibitors  
The present application de gibes 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...
6429215 N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses  
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using an N-oxide of a heterocyclic ester, amide, thioester, or ketone.
6423723 FSH mimetics for the treatment of infertility  
The present invention provides non-peptidic amino derivatives, their therapeutic use as well as pharmaceutical compositions that possess activity as Follicle Stimulating Hormone (FSH) agonists and...
6423707 Nitroimidazole ester analogues and therapeutic applications  
Novel nitroimidazole compounds are provided that have a substituent linked via an ester linkage. The ester linkage may be obtained by derivation of the hydroxyl group of metronidazole. These...
6423724 7-(2-imidazolinylamino) quinoline compounds useful as alpha-2 adrenoceptor agonists  
This invention involves involves the use of compounds having the following structure: wherein:(a) R is unsubstituted C1-C3 alkanyl or alkenyl; and(b) R′ is selected from hydrogen; unsubstituted...
6423741 Anti-microbial composition and method for producing the same  
This invention is related to the development of strategic and novel composition comprising α arteether and nalidixic acid or quinolone drugs, said composition useful as an advanced generation drug...
6420375 Fused ring compounds, process for producing the same and use thereof  
To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be...
6420395 Azacyclooctane and heptane derivatives, their preparation and use in therapy  
The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen,...
6417178 Amyloid binding nitrogen-linked compounds for the antemortem diagnosis of alzheimer's disease, in vivo imaging and prevention of amyloid deposits  
Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose...
6417220 Mitochondrial membrane stabilizer  
A prophylactic and/or therapeutic method for treating a disease caused by mitochondrial functional abnormality, or a disease with mitochondrial functional abnormality, including: administering a...
6413990 Arylsulphonamide-substituted benzimidazoles having tryptase-inhibiting activity  
Bezimidazole derivatives of general formula (I) having tryptase-inhibitory activity. Exemplary are:N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5 -yl}-N-diethylaminoethyl-(4-ethoxycarbony...
6413984 8-(heterocyclylmethyl)quinoline derivatives for treating urinary incontinence  
The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being...
6413983 Benzopyranyl heterocycle derivatives, process for preparation thereof, and pharmaceutical compositions containing them  
The present invention relates to novel benzopyranyl heterocycle derivatives of the formula 1, process for preparation thereof and pharmaceutical use of the benzopyranyl heterocycle derivatives....
6410562 Hypoglycemic imidazoline compounds  
This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases...
6410563 Substituted 8-arylquinoline phosphodiesterase-4 inhibitors  
Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
6410574 Fungicidal composition and method for using the same  
The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide...
6403610 Quinolylpropylpiperidine derivatives, their preparation and the compositions which comprise them  
Quinolylpropylpiperidine derivatives of formula (I) which are particularly advantageous antimicrobial agents, their compositions, and their use.
6403577 Hexamethyleneiminyl tachykinin receptor antagonists  
This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This...
6399606 Neuroprotective agents and methods related thereto  
Neuroprotective agents are disclosed having the following structure: wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit...