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| Number | Title | Issue Date |
| 8003790 | Salt of proline derivative, solvate thereof, and production method thereof The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and repro... | 08/23/2011 |
| 7732605 | Synthesis of diketopiperazines Disclosed herein are methods for synthesizing diketopiperazines with enantiomeric excess by inducing cyclization of an α-keto acid with an acid catalyst. ... | 06/08/2010 |
| 7534887 | Thiazoline derivative and use of the same A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which... | 05/19/2009 |
| 7432269 | Arylpiperaszine derivatives, to the process for the production thereof and to the use thereof as therapeutic agents The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands for the dopamine D3 receptor. Th... | 10/07/2008 |
| 7396834 | 4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the ma... | 07/08/2008 |
| 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 |
| 7390825 | Process for the preparation of oxazolidinones and method of use thereof Substituted oxazolidinone of the formula: wherein R2 is alkyl selected from the group consisting of methyl, ethyl, and isopropyl moieties, are described. The compounds are antibacterial. ... | 06/24/2008 |
| 7365077 | Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same. ... | 04/29/2008 |
| 7361658 | 2-acylaminothiazole derivative or salt thereof 2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytop... | 04/22/2008 |
| 7335660 | Isochroman compounds for treatment of CNS disorders This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre... | 02/26/2008 |
| 7329749 | Piperazinylcarbonylquinolines and -isoquinolines Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins... | 02/12/2008 |
| 7320978 | Oxazole derivatives, preparation and therapeutic use thereof This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The i... | 01/22/2008 |
| 7300939 | Substituted 1-propiolylpiperazine compounds, their preparation and use Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine com... | 11/27/2007 |
| 7273881 | Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure ... | 09/25/2007 |
| 7265134 | Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen... | 09/04/2007 |
| 7229994 | 4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is indepen... | 06/12/2007 |
| 7220744 | Monocyclic substituted phenyl methanones The present invention relates to compounds of formula I wherein R1, R2, X1, and X2 are as defined in the specification an... | 05/22/2007 |
| 7214679 | Piperidine/piperazine-type inhibitors of p38 kinase Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase. ... | 05/08/2007 |
| 7214694 | 3-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP. ... | 05/08/2007 |
| 7211668 | PNA monomer and precursor This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: | 05/01/2007 |
| 7189712 | 1,3-Oxazole compounds for the treatment of cancer Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. | 03/13/2007 |
| 7166608 | -aroyl piperazine derivatives as orexin receptor antagonists This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C═O, SO2, or CH═CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl grou... | 01/23/2007 |
| 7160886 | Acylated piperazine derivatives as melanocortin-4 receptor agonists Certain novel N-acylated piperazine 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 disease... | 01/09/2007 |
| 7157464 | Substituted piperazines Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ... | 01/02/2007 |
| 7119086 | Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopress... | 10/10/2006 |
| 7119203 | Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop... | 10/10/2006 |
| 7105507 | Cyclohexane derivatives and their use as therapeutic agents The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R | 09/12/2006 |
| 7098212 | Piperazine derivatives The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 | 08/29/2006 |
| 7087576 | Dipeptide phenyl ethers Novel dipeptide ethers are effective for lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels. The dipeptide ethers are also useful for the treatment and/or prophylaxis of diabetes, obesity, inflammation and autoimmune disease... | 08/08/2006 |
| 7056924 | Substituted heterocyclic compounds Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ... | 06/06/2006 |
| 7026314 | Therapeutic chromone compounds Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds ... | 04/11/2006 |
| 7026321 | Substituted heterocyclic compounds Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ... | 04/11/2006 |
| 7012075 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 03/14/2006 |
| 7001909 | Substituted heterocyclic compounds Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ... | 02/21/2006 |
| 6984652 | Gyrase inhibitors Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylax... | 01/10/2006 |
| 6969711 | Cyclic diamine compounds and medicine containing the same The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. | 11/29/2005 |
| 6969713 | Piperidine and piperazine acetamide derivatives The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy | 11/29/2005 |
| 6956040 | Oxazolidinone piperazinyl derivatives as potential antimicrobials The present invention relates to certain substituted phenyl piperazinyl oxazolidinones, for example, to those having the structure of Formula I with the variables as defined within, and to processes for the synthesis o... | 10/18/2005 |
| 6953796 | Use of 2-amino-thiazoline derivatives as inhibitors of inducible No-synthase The present invention relates to the use of 2-amino-thiazoline derivatives of formula (I): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N—Bn, N... | 10/11/2005 |
| 6936715 | Lipoic acid heterocyclic or benzene derivatives, preparation and use thereof as medicines Compounds of the formulae wherein the substituents are as defined in the specification useful for inhibiting NO synthase and regenerate antioxidants. ... | 08/30/2005 |
