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| Number | Title | Issue Date |
| 8153635 | Compounds and compositions as modulators of GPR119 activity The invention provides compounds of Formula I: wherein A, L, m, q, Q, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention. The invention further provides ... | 04/10/2012 |
| 8143256 | Cyclic amide and ester pyrazinoylguanidine sodium channel blockers The present invention provides compounds represented by formula (I): where the structural variables are defined herein. The compound of the present invention are useful as sodium channel blockers. ... | 03/27/2012 |
| 8129389 | Substituted oxindole derivatives, medicaments containing the latter and use thereof The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter... | 03/06/2012 |
| 8110578 | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compou... | 02/07/2012 |
| 8093248 | Compounds useful for the treatment of conditions associated with weight gain The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mime... | 01/10/2012 |
| 8076341 | Compounds and use thereof A compound of formula (I) wherein R1 is selected from H, F, Cl, Br, CF3, C1-C6 alkoxy and OH; R2 is selected from H and C1-C6 alkyl; n is 1-12; m is O or 1; Y is selected from CH2 | 12/13/2011 |
| 8071600 | Derivatives of 4-piperazin-1-yl-4-benzo[B]thiophene suitable for the treatment of CNS disorders A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a hetero... | 12/06/2011 |
| 8017611 | Pyridine and pyrazine derivatives -083 The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 | 09/13/2011 |
| 7910588 | 5-HT7 receptor antagonists The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═ and R1-7 are as defined herein. | 03/22/2011 |
| 7906515 | Cancer treatment with topoisomerase-II inhibitor, a bis-dioxypiperazine and radiation The present invention relates to a method of treatment of a tumour cell which comprises administering to a subject in need of treatment an effective amount of a topoisomerase-II poison, e.g. etoposide, in combination with a bis-dioxypiperazine, e.g. dexrazoxane wher... | 03/15/2011 |
| 7868005 | Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s... | 01/11/2011 |
| 7842694 | Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for examp... | 11/30/2010 |
| 7829564 | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors α-and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ... | 11/09/2010 |
| 7795261 | Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined N... | 09/14/2010 |
| 7786120 | Pyridones useful as inhibitors of kinases The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, o... | 08/31/2010 |
| 7781437 | Substituted heterocyclic compounds with CXCR3 antagonist activity The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s... | 08/24/2010 |
| 7772236 | Substituted pyrazoles Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ... | 08/10/2010 |
| 7754721 | Arylpiperazine derivatives and uses thereof Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are def... | 07/13/2010 |
| 7652011 | 4-[(arylmethyl)aminomethyl]piperidine derivatives, their preparation and their therapeutic application The invention relates to 4-[(arylmethyl)aminomethyl]piperidine derivatives of general formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation p... | 01/26/2010 |
| 7642259 | Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for examp... | 01/05/2010 |
| 7625902 | Imidazolidinone derivatives The invention is concerned with novel imidazolidinone derivatives of formula (I): wherein R1 to R11 and X are as defined in the description and in the claims, as well as physiologically acceptable salt... | 12/01/2009 |
| 7595319 | Compounds having selective inhibiting effect at GSK3 Selective phenyl substituted aminopyrazine inhibitors of GSK3 useful for the prevention and/or treatment of cognitive disorders. ... | 09/29/2009 |
| 7560460 | Substituted piperazines and methods of use Selected substituted piperazine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions a... | 07/14/2009 |
| 7498332 | Therapy for cerebral vasospasm The present invention relates to a method of treating or preventing cerebral vasospasm that accompanies sub-arachnoid hemorrhage. ... | 03/03/2009 |
| 7456180 | Piperazine derivatives and their use as therapeutic agents Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R2, R3, R | 11/25/2008 |
| 7442699 | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are... | 10/28/2008 |
| 7435736 | Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their us... | 10/14/2008 |
| 7435737 | Inhibitors of macrophage migration inhibitory factor and methods for identifying the same Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: | 10/14/2008 |
| 7432264 | Antimicrobial biaryl compounds Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ... | 10/07/2008 |
| 7432268 | 17β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also ... | 10/07/2008 |
| 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 |
| 7396830 | Piperazine amidines as antiviral agents This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and a... | 07/08/2008 |
| 7381719 | Diaryl ethers as opioid receptor antagonist A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o... | 06/03/2008 |
| 7365073 | 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, a... | 04/29/2008 |
| 7361657 | Respiratory syncytial virus replication inhibitors This invention concerns the use of compounds of formula (I) wherein −a1=a2−a3=a4—is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—C... | 04/22/2008 |
| 7354924 | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral acti... | 04/08/2008 |
| 7332504 | Heterocyclic substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ... | 02/19/2008 |
| 7329672 | 2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a... | 02/12/2008 |
| 7329671 | 2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a... | 02/12/2008 |
| 7320983 | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ... | 01/22/2008 |
