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6462056 Oxazolidines as 5-HT2A-antagonists  
The invention relates to novel oxazolidine derivatives of the formula in which R 1 , R 2 and R 3 have the meanings stated in claim 1, their salts and processes for preparing the compounds...
6462036 Tricyclic pyrazole derivatives  
This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to...
6455567 Method of treatment  
The invention provides the use of a compound of formula (I) wherein R 1 and R 2 independently represent H or C 1 -C 6 alkyl, or a pharmaceutically acceptable salt thereof, in the manufacture...
6451818 Therapeutic use of 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline  
The invention concerns the use of 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline for preventing and/or treating motor neuron diseases.
6448243 1,4-substituted cyclic amine derivatives  
A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or...
6444685 N-(4-sulfonylaryl)Cyclylamine 2-hydroxyethylamines as beta-3 adrenergic receptor agonists  
This invention provides compounds of Formula I having the structure wherein R 1 , R 2 , R 3 , R 4 , W, X, and Y are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which...
6444665 Method for treating pain  
The present invention provides a method for treating pain using an atypical antipsychotic compound.
6436961 Pharmaceutical agents for the treatment of emesis  
The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active...
6417197 Acylated n-hydroxy methyl thalidomide prodrugs with immunomodulator action  
Thalidomide prodrugs of the formula I: in which R is —CHR 1 —NHR 2 or —(CH 2 ) n COOH; R 1 is H or C 1-4 alkyl; R 2 is H, C 1-3 alkyl, C(O)—CH 2 —NHR 3 or an amino-protective...
6403581 Method of inhibition of farnesyl-protein transferase using substituted benz (cd) indol-2-imine and-amine derivatives  
The invention is a method of treating, inhibiting or controlling a ras-associated disease by inhibiting farnesyl-protein transferase(FPTase) enzyme, treating ras oncogene-dependent tumors, which...
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 invention...
6403640 Method for treating chronic prostatitis or chronic pelvic pain syndrome  
The use of a COX-2 selective inhibitor for the treatment of chronic prostatitis or chronic pelvic pain syndrome is disclosed.
6403613 1-oxo-and 1,3-dioxoisoindolines  
1-Oxo- and 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindolines substituted in the 4- and/or 7-position of the isoindoline ring and optionally further substituted in the 3-position of the...
6399631 Carbazole neuropeptide Y5 antagonists  
Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.
6391891 Bicyclic compounds as ligands for 5-HT1 receptors  
The invention relates to compounds which are ligands for 5HT1, of formula (I) Wherein L, Q, R a , R b and R y are as defined in the specification, processes for their preparation and their...
6387932 Somatostatin agonists  
This invention relates to non-peptide somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the...
6380185 N-substituted benzoyl indoles as estrogenic agents  
The present invention provides compounds of the formula: wherein R 1 , R 2 , R 3 , R 4 , X, n Y and Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well...
6380226 Salts of an anti-migraine indole derivatives  
A crystalline, β-polymorphic form of a compound of formula (I):
6372764 Pyrrolidine modulators of chemokine receptor activity  
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
6369074 Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists  
The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R 1 , R 2 , R 3 , A, X′, Y′ and Z′ are...
6369051 Combinations of SSRI and estrogenic agents  
This invention comprises methods of depression, anxiety, generalized anxiety disorder (GAD), hot flush, post partum depression, premenstrual syndrome, obesity, obsessive compulsive disorder,...
6362201 3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity  
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
6358993 Pharmaceutically active nitrogen ring compounds and methods of use thereof  
The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof,...
6358943 N-substituted indolines as estrogenic agents  
This invention provides compounds of the formula wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X, n and Y, are as defined in the specification, or a pharmaceutically acceptable salt thereof,...
6355642 Tetrahydrobenzindole compounds  
A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR 5 ; each of B and Z is independently N, CH or CR 1 , with the proviso...
6350760 Substituted piperidines as melanocortin-4 receptor agonists  
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
6339095 Therapeutic use of 1, 6-dimethyl-8β-hydroxymethyl-10-α-methoxyergoline  
The invention concerns the use of 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline for preventing and/or treating motor neuron diseases.
6335326 Benzisoxazole derivatives having d4-antagonistic activity  
The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R...
6335349 Substituted 2(2,6-dioxopiperidin-3-yl)isoindolines  
Substituted 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindolines and 1-oxo-2-(2,6-dioxo-piperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal and are useful in treating oncogenic...
6333339 3-Benzylpiperidine  
The invention relates to piperidine derivatives of the formula I ##STR1## in which R 1 , R 2 , m and k have the meanings indicated in claim 1, and their salts, novel intermediates and processes for...
6329366 Pharmaceutical compounds  
A pharmaceutical compound of the formula ##STR1## in which R 1 and R 2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, ##STR2## where R 4 and R 5...
6323217 Piperidine-4 sulphonamide compounds  
A compound of formula (I): ##STR1## wherein: R 1 represents hydrogen or alkyl, R 2a and R 2b represent a group selected from hydrogen, halogen, alkyl, hydroxy, alkoxy, trihaloalkyl, cyano,...
6316437 Spirohydantoin compounds and uses thereof  
Spirohydantoin compounds 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...
6316468 Phenylindole derivatives as 5-HT2A receptor antagonists  
3-(Piperidin-4-yl)-1H-indole derivatives bearing an optionally substituted phenyl moiety at the 2-position of the indole ring system and an alkyl or aryl-alkyl substituent on the nitrogen atom of...
6313143 Substituted pyrroles  
Disclosed are novel substituted pyrroles having the formula ##STR1## These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion...
6306859 N-substituted imide derivatives with serotonergic activity  
Compounds of the Formula (I) ##STR1## wherein R 2 , Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic...
6306879 Stable aqueous solution of 3-(1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2-6-dione  
An aqueous solution 3-(1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione (EM 12) is described which is suitable for parenteral administration, particularly for intravenous administration of EM...
6303627 Inhibitors of serotonin reuptake  
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
6303610 Method of treating gout with certain indole compounds  
This invention relates to a method of treating gout with certain indole compounds and other aromatic compounds.
6303633 Heteroaryl amines as novel acetylcholinesterase inhibitors  
Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R 2 , R 3 , R 4 , R 5 , R 6 , R 11 , R 12 , R 13 , E, G, X and P are as defined below. The compounds of formula I are...
6303626 Pharmaceutical formulations in dry form for the oral administration of a cyclic quaternary ammonium compound  
The pharmaceutical formulations according to the invention contain from 0.5 to 50% by weight of a cyclic quaternary ammonium compound and pharmaceutically appropriate excipients and are formulated...
6297247 Sulfonamide inhibitors of matrix metalloproteinases  
Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment...
6294537 Compounds which are specific antagonists of the human NK3 receptor and their use as medicinal products and diagnostic tools  
A method for treating diseases which involve interaction of neurokinin B with NK 3 receptors in humans. The method comprises administering a therapeutically effective amount of a NK 3 antagonist...
6294551 N-linked sulfonamides of heterocyclic thioesters  
This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as...
6288058 Substituted tetracyclic tetrahydrofuran derivatives  
This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and...
6277877 Substituted n-(indole-2-carbonyl)glycinamides and derivates as glycogen phosphorylase inhibitors  
Compounds of Formula (I) ##STR1## wherein R 6 is carboxy, (C 1 -C 8 )alkoxycarbonyl, benzyloxycarbonyl, C(O)NR 8 R 9 or C(O)R 12 as glycogen phosphorylase inhibitors, pharmaceutical...
6262080 3-(thio-substitutedamido)-lactams useful as inhibitors of matrix metalloproteinase  
The present invention provides novel thio-substitutedamido lactam derivatives of the formula ##STR1## useful in as inhibitors of matrix metallo-proteinases (MMPs).
6262087 Indane or dihydroindole derivatives  
The present invention relates to substituted indane or dihydroindole compounds of Formula (I) ##STR1## wherein A is an indole. These compounds have high affinity for D 4 receptors.
6258815 Specific immunophilin ligands as antiasthmatics and immunosuppressants  
The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs. ##STR1##
6255306 4-indole derivatives as serotonin agonists and antagonists  
The present invention relates to compounds of the formula ##STR1##