"That the automobile has practically reached the limit of its development is suggested by the fact that during the past year no improvements of a radical nature have been introduced."
Scientific American ; Jan. 2 edition, 1909
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| Number | Title | Issue Date |
| 7417047 | Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for β-secretase modulation The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and ... | 08/26/2008 |
| 7390907 | Vanilloid receptor ligands and their use in treatments Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu... | 06/24/2008 |
| 7354933 | Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use... | 04/08/2008 |
| 7288559 | Carboxamide spirohydantoin CGRP receptor antagonists The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha... | 10/30/2007 |
| 7226940 | Substituted heterocycles for the treatment of diabetes and other diseases The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymph... | 06/05/2007 |
| 7192954 | Monocyclic anilide spirohydantoin CGRP receptor antagonists The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha... | 03/20/2007 |
| 7186727 | Pyridyl-substituted spiro-hydantoin compounds and use thereof A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group... | 03/06/2007 |
| 7129359 | Imidazolidinone compounds This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions compris... | 10/31/2006 |
| 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 |
| 7078420 | Spiro-hydantoin compounds useful as anti-inflammatory agents Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, whe... | 07/18/2006 |
| 6995262 | Use of acylsulfonamido-substituted polymethine dyes as fluorescene dyes and/or markers The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae ... | 02/07/2006 |
| 6977267 | Spiro-hydantoin compounds useful as anti-inflammatory agents Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L... | 12/20/2005 |
| 6974826 | Imidazolidinedione derivatives for the treatment of diabetes and other diseases The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymph... | 12/13/2005 |
| 6884815 | High affinity small molecule C5a receptor modulators This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as anta... | 04/26/2005 |
| 6784298 | Hydantoin-containing glucokinase activators Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes. ... | 08/31/2004 |
| 6784293 | Process for making Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials. ... | 08/31/2004 |
| 6680333 | Imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them The present invention relates to novel imidazolidine derivatives of formula I, ##STR1## wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are... | 01/20/2004 |
| 6620825 | Adenosine A3 receptor antagonists A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophyla... | 09/16/2003 |
| 6613908 | Method for carbamoylating alcohols The present invention includes a method for carbamoylating an alcohol with sodium cyanate in the presence of methanesulfonic acid. The reaction can be conducted under anhydrous conditions. This method is suitable for carbamoylating a molecule including bo... | 09/02/2003 |
| 6602889 | 5-heteroaryl substituted indoles The present invention relates to compounds having general formula (I) as defined herein, or a pharmaceutically acceptable acid addition salt thereof. The compounds are selective 댑 -adrenoceptor ligands. ##STR1##... | 08/05/2003 |
| 6583288 | Hydantoin-containing glucokinase activators Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.... | 06/24/2003 |
| 6569873 | Azolidines as beta-3 adrenergic receptor agonists This invention provides compounds of Formula I having the structure ##STR1## wherein, A, X, Y, Z, W, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt ... | 05/27/2003 |
| 6562832 | Substituted imidazole compounds Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.... | 05/13/2003 |
| 6518293 | Anti-HIV imidazolone derivatives The invention is concerned with novel imidazolone derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human immunodeficiency virus reverse ... | 02/11/2003 |
| 6514993 | Serotonin 5-HT1A and dopamin D2 receptor ligands The present invention relates to a novel series of 4-phenylpiperazines, 4-phenylpiperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compounds of general formula (I) ##STR1## wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene... | 02/04/2003 |
| 6492397 | N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis. Compounds of particular interest are angiotensin II antagonists of Formula I: ##STR1## wherein Ar is selected from ##STR2## wherein m is ... | 12/10/2002 |
| 6462063 | C-proteinase inhibitors The present invention relates to a novel class of N,N'-di substituted hydantoin hydroxamates capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatm... | 10/08/2002 |
| 6455550 | N-alkanoylphenylalanine derivatives Compounds of the formula: ##STR1## are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 ... | 09/24/2002 |
| 6436966 | Adenosine A3 receptor antagonists A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophyla... | 08/20/2002 |
| 6420563 | Small molecule modulators of G protein-coupled receptor six Disclosed herein are small molecule modulators of the G protein coupled receptor six, methods of making such compounds, and methods of using such compounds.... | 07/16/2002 |
| 6384061 | Hydantoin compounds and methods related thereto The present invention relates to novel hydantoin compounds represented by formula (I) which shows an inhibitory activity against farnesyl transferase, and thus can be used as an anti-cancer agent, or pharmaceutically acceptable salts thereof, in which R | 05/07/2002 |
| 6380134 | N-pyridyl herbicide compounds Compounds of the formula I ##STR1## in which A is .dbd.N-- or ##STR2## R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1 -C4 alkyl, C1 -C4 haloalkyl, halogen, R6 O... | 04/30/2002 |
| 6355664 | Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules. Exemplary of the novel compounds are those of the following structural formulas: ##STR1## ##STR2##... | 03/12/2002 |
| 6350763 | Small molecules useful in the treatment of inflammation disease Novel compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 1-acetyl-5-(R)-(4-bromobenzyl)-3-(2,6-dichloropyridin-4-yl)-5-methylimidazo line-2,4-dione; 5-(R)... | 02/26/2002 |
| 6339158 | Process for the preparation of chiral nicotinic, quinolinic or benzoic acid imidazolinone herbicides There is provided a stereospecific process for the preparation of essentially enantiomerically pure imidazolinone herbicides having the R-configuration via (R)2-amino-2,3-dimethylbutyronitrile.... | 01/15/2002 |
| 6331552 | Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them Substituted imidazolidine derivatives of the formula I, ##STR1## in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active com... | 12/18/2001 |
| 6271249 | Diphenyl imidazoles as potassium channel modulators Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrenc... | 08/07/2001 |
| 6232321 | Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn -PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The ... | 05/15/2001 |
| 6200991 | Imidazole derivatives, preparation and therapeutic application thereof A compound of formula (I) ##STR1## the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M3 muscarinic and/or S--HT4 serotoninergic receptors.... | 03/13/2001 |
| 6194438 | Derivatives of 2-(2-oxo-ethylidene)-imidazolidin-4-one, and compositions and methods for inhibiting abnormal cell growth comprising said derivatives The present invention relates to compounds of the formula ##STR1## wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula I... | 02/27/2001 |