"Flight by machines heavier than air is unpractical and insignificant, if not utterly impossible."
Simon Newcomb, astronomer ; Said in 1902, less than two years before the first flight at Kitty Hawk
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| Number | Title | Issue Date |
| 8183366 | 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. ... | 05/22/2012 |
| 7456279 | Coupling process for preparing quinolone intermediates Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process. ... | 11/25/2008 |
| 7419990 | Piperidine derivatives as melanocortin-4 receptor agonists Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disor... | 09/02/2008 |
| 7414047 | Piperazinyl and diazapanyl benzamides and benzthioamides Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ... | 08/19/2008 |
| 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 |
| 7393845 | Heteroaryl derivates, their preparation and use A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord... | 07/01/2008 |
| 7361682 | Indole derivatives as H3 inverse agonists The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ... | 04/22/2008 |
| 7323456 | Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient A compound of formula (I) (wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a ... | 01/29/2008 |
| 7307074 | Diazepan derivatives or salts thereof To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such a... | 12/11/2007 |
| 7304052 | Substituted homopiperidinyl benzimidazole analogues as fundic relaxants The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres... | 12/04/2007 |
| 7291613 | Inhibitors of p38 kinase The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system. ... | 11/06/2007 |
| 7285547 | Amidinophenylalanine derivatives as thrombin inhibitors The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. T... | 10/23/2007 |
| 7276524 | Pyridyl alkane acid amides as cytostatics and immunosuppressives The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression ... | 10/02/2007 |
| 7259158 | Naphthaline derivatives as H3 inverse agonists The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are usef... | 08/21/2007 |
| 7241745 | Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m... | 07/10/2007 |
| 7223750 | Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl,... | 05/29/2007 |
| 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 |
| 7183274 | Piperidine-2,6-diones heterocyclically substituted in the 3-position Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment. ... | 02/27/2007 |
| 7135466 | Quinoline and quinazoline derivatives and drugs containing the same There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy. The compounds are those represented by formula (I) or pharm... | 11/14/2006 |
| 7115596 | Thiazole compounds as integrin receptor antagonists derivatives The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of ... | 10/03/2006 |
| 7115635 | Benzylpiperidine compound The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following ben... | 10/03/2006 |
| 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 |
| 7087628 | N-heterocyclyl hydrazides as neurotrophic agents This invention relates to a series of N-heterocyclyl hydrazides of Formula I, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treat... | 08/08/2006 |
| 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 |
| 7067532 | Substituted quinolines as antitumor agents The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) a... | 06/27/2006 |
| 7041675 | Heterocyclic compounds and their use as PARP inhibitors The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors. ... | 05/09/2006 |
| 7026310 | Heteroaryl derivatives and their use as medicaments The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ... | 04/11/2006 |
| 7022695 | Thioether-substituted benzamides as inhibitors of Factor Xa Thioether-substituted benzamide compounds having the formula: are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding. ... | 04/04/2006 |
| 7012073 | Quinoline derivatives Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1,... | 03/14/2006 |
| 6992092 | Anti-diabetic agents The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2 | 01/31/2006 |
| 6984637 | Cyclic amine derivatives-CCR-3 receptor antagonists This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compound... | 01/10/2006 |
| 6974870 | Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore us... | 12/13/2005 |
| 6964956 | Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore us... | 11/15/2005 |
| 6962926 | Antagonist of MCP-1 function, and compositions and methods of use thereof Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of ... | 11/08/2005 |
| 6953792 | Cyclohexyl derivatives and their use as therapeutic agents The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3 | 10/11/2005 |
| 6939867 | β3 agonists and uses thereof Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and ... | 09/06/2005 |
| 6919368 | N-ureidoalkyl-piperidines as modulators of chemokine receptor activity The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ... | 07/19/2005 |
| 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 |
| 6908929 | Phenyl-substituted imidazopyridines The invention features pharmaceutically-active imidazopyridines and derivatives that are substituted with phenyl, methods of making them, and methods of using them. ... | 06/21/2005 |
| 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 |