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| Number | Title | Issue Date |
| 8183367 | Methods of preparing polymorphic form A of bazedoxifene acetate The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods. ... | 05/22/2012 |
| 7858781 | Chemokine receptor antagonists A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the variants R, R9, Z, X, Q and Y are defined in the specification. ... | 12/28/2010 |
| 7435833 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme A compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating non-insul... | 10/14/2008 |
| 7429607 | 5-HTreceptor antagonists The present invention relates to compounds of formula I: wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalky... | 09/30/2008 |
| 7407950 | -(heteroaryl)-1-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. | 08/05/2008 |
| 7405209 | Protease inhibitors The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co... | 07/29/2008 |
| 7304048 | Indole-type derivatives as inhibitors of p38 kinase The invention is directed to methods to inhibit p38-α kinase using compounds containing an aromatic system coupled through a 7-membered heterocycle to an indole-type system. ... | 12/04/2007 |
| 7202237 | Pyridylether derivatives, their preparation and use The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the centra... | 04/10/2007 |
| 7196109 | Aminoindazole derivatives as medicaments and pharmaceutical compositions including them The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl... | 03/27/2007 |
| 7179835 | 2-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same. | 02/20/2007 |
| 7173024 | Compounds having prolyl oligopeptidase inhibitory activity, methods for their preparation and their use Compounds of the formula (I), wherein the symbol aa means a residue of an α-amino acid. The invention is also directed to a method for the preparation of the compounds of formula (I), as well as their use as pro... | 02/06/2007 |
| 7138392 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: or which are useful in treat... | 11/21/2006 |
| 7105556 | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2 | 09/12/2006 |
| 7091199 | Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d antagonists The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These condi... | 08/15/2006 |
| 7071184 | Protease inhibitors The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int... | 07/04/2006 |
| 7034029 | 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ... | 04/25/2006 |
| 7030141 | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat... | 04/18/2006 |
| 6949579 | Aminoindazole derivatives and intermediates, preparation thereof, and pharmaceutical compositions thereof The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alk... | 09/27/2005 |
| 6919456 | Catalytic compositions and methods for asymmetric aldol reactions Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I,... | 07/19/2005 |
| 6906090 | Compositions and methods for treating mycobacterial diseases The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease. ... | 06/14/2005 |
| 6887864 | Azepane derivatives This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ... | 05/03/2005 |
| 6833375 | N-[4-(heteroarylmethyl)phenyl]-heteroarylamines The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C | 12/21/2004 |
| 6825217 | Carbinols for the treatment of neuropathic dysfunction Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically acceptable salt or prodrug thereof. ... | 11/30/2004 |
| 6767912 | Heterocyclylindazole and -azaindazole compounds as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. ... | 07/27/2004 |
| 6713473 | Tricyclic compounds A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and t... | 03/30/2004 |
| 6699864 | Substituted phenyl-piperazine derivatives, their preparation and use The present invention provides compounds of the formula: ##STR1## wherein R1 -R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.... | 03/02/2004 |
| 6680314 | Azacyclooctane and heptane derivatives, their preparation and use in therapy Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ... | 01/20/2004 |
| 6673790 | Indolin-2-one derivatives, preparation and their use as ocytocin receptor ligands The present invention relates to novel indolin-2-one derivatives of formula: ##STR1## to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.... | 01/06/2004 |
| 6667303 | Aryl substituted 1,4-diazepanes and method of use thereof Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pha... | 12/23/2003 |
| 6613781 | Heterocyclylaklylindole or -azaindole compounds as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ##STR1##... | 09/02/2003 |
| 6500821 | 4-amino-1-aryl-1,5-dihydropyrrol-2-ones and process for making The invention relates to 1,5-dihydropyrrol-2-ones of Formula 1 which contain an aryl radical in the 1-position and a secondary amine radical in the 4-position, to a process for making and for a process to treat various forms of epilepsies and of states of... | 12/31/2002 |
| 6495568 | Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors Compounds of formula (I): ##STR1## or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH... | 12/17/2002 |
| 6495543 | Polycyclic azaindole compounds The invention relates to compounds of formula (I): ##STR1## wherein: G1 represents an alkylene chain as defined in the description, A represents ##STR2## R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together f... | 12/17/2002 |
| 6492421 | Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g.... | 12/10/2002 |
| 6489354 | 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine ... | 12/03/2002 |
| 6486153 | Phenylindole derivatives as 5-HT2A receptor ligands A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prev... | 11/26/2002 |
| 6479480 | Phenylindole derivatives as 5-ht2a receptor ligands Compounds according to Formula (I) or a salt thereof are selective antagonists of the human 5-HT2A receptor useful for treatment of adverse conditions of the central nervous system: ##STR1##... | 11/12/2002 |
| 6465453 | Azepine derivatives having effects on serotonin related systems The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of s... | 10/15/2002 |
| 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: ##STR1## (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, ... | 09/10/2002 |
| 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, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl ... | 07/16/2002 |
