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| Number | Title | Issue Date |
| 7893068 | Physiologically active substances The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydrox... | 02/22/2011 |
| 7419980 | Fused-aryl and heteroaryl derivatives and methods of their use The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms... | 09/02/2008 |
| 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 |
| 7363075 | Transdermal delivery system for dried particulate or lyophilized medications The present invention provides a system for transdermal delivery of dried or lyophilized pharmaceutical compositions and methods using thereof. The system comprises an apparatus for facilitating transdermal delivery of an agent that generates hydrophilic micro-chann... | 04/22/2008 |
| 7354919 | Isoxazole compositions useful as inhibitors of ERK Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo... | 04/08/2008 |
| 7335377 | Transdermal delivery system for dried particulate or lyophilized medications The present invention provides a system for transdermal delivery of dried or lyophilized pharmaceutical compositions and methods using thereof. The system comprises an apparatus for facilitating transdermal delivery of an agent that generates hydrophilic micro-chann... | 02/26/2008 |
| 7282519 | Nitrosated and nitrosylated diuretic compounds, compositions and methods of use The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide ... | 10/16/2007 |
| 7232818 | Compounds for enzyme inhibition Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited b... | 06/19/2007 |
| 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 |
| 7189739 | Compounds and methods to treat cardiac failure and other disorders The invention is directed to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Ar1 is indole, benzimidazole, or benzotriazole, optionally substituted with ... | 03/13/2007 |
| 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 |
| 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 |
| 7115658 | Inhibitors of hepatitis C virus RNA-dependent RNA polymerase Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus ... | 10/03/2006 |
| 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 |
| 7084144 | Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ... | 08/01/2006 |
| 7034046 | NR1H4 nuclear receptor binding compounds The present invention relates to compounds according to the general formula (I) which bind to the nuclear receptor, NR1H4, and act as agonists and antagonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through... | 04/25/2006 |
| 7026323 | Platelet adenosine diphosphate receptor antagonists Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmace... | 04/11/2006 |
| 7019007 | CCR-3 receptor antagonists (I) The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions c... | 03/28/2006 |
| 6995269 | Guanidinobenzamides Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and ... | 02/07/2006 |
| 6949538 | Compounds, compositions, and methods Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ... | 09/27/2005 |
| 6936611 | Serine protease inhibitors Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardi... | 08/30/2005 |
| 6927217 | HIV protease inhibitors The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development o... | 08/09/2005 |
| 6916926 | Process for the preparation of (±) 1-3-dioxolanes and the optical resolution thereof (±) 3-(4-Phenyl-1-piperazinyl)-1,2-propanediol cyclic acetals, a process for the optical resolution thereof and their use as intermediates for the preparation of (−) 3-(4-phenyl-1-piperazinyl)-1,2-propanediol (levodropropizine) and salts thereof are described her... | 07/12/2005 |
| 6916812 | Alpha-aminoamide derivatives as melanocortin agonists Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present inven... | 07/12/2005 |
| 6916797 | α-arylethylpiperazine derivatives as neurokinin antagonists The invention relates to new α-arylethylpiperazine of the formula wherein Z represents 0 or S; n′ represents 1 or 2; R2 represents a hy... | 07/12/2005 |
| 6906073 | Piperazine CCR-3 receptor antagonists The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions co... | 06/14/2005 |
| 6903120 | Modulators of dopamine neurotransmission New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, O... | 06/07/2005 |
| 6900213 | Bisaryl derivatives having FSH modulatory activity The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV ... | 05/31/2005 |
| 6884803 | Phenylalkynes Disclosed are substituted phenylalkynes of formula (I), wherein R1, R2, R3, R4, R5 and n are as defined, compositions containing them, and methods of making and us... | 04/26/2005 |
| 6861432 | Piperazine derivatives that destabilize androgen receptors This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the inventio... | 03/01/2005 |
| 6849660 | Antimicrobial biaryl compounds Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1′ is —C(O)NR5R5′ | 02/01/2005 |
| 6835734 | 1,3-dioxolanes with antitussive activity (S)-3-(4-Phenyl-1-piperazinyl)-1,2-propanediol cyclic acetals useful as antitussive agents and as intermediates for the preparation of levodropropizine and the salts thereof, as well as a process for the preparation of said acetals, are disclosed. ... | 12/28/2004 |
| 6770650 | 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 compounds.... | 08/03/2004 |
| 6706719 | Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity 4-(4-(-Chlorophenyl)piperazin-1-yl)sulfonylmethyl)-tetrahydor yran-4-carboxylic acid and the corresponding N-hydroxy amide, and derivatives thereof, are useful as therapeutic agents. ... | 03/16/2004 |
| 6696447 | Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain The present application describes compounds of general formula I ##STR1## where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independen... | 02/24/2004 |
| 6689785 | Epoxysuccinamide derivatives Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R1 and R3 are each hydrogen, al... | 02/10/2004 |
| 6680321 | Compounds with analgesic effect Compounds of the formula (I) ##STR1## as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.... | 01/20/2004 |
| 6649611 | Piperazine derivatives A compound of the formula ##STR1## or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disord... | 11/18/2003 |
| 6642238 | Oxazolidinone thioamides with piperazine amide substituents The present invention provides a compound of formula I ##STR1## which have potent activities against gram-positive and gram-negative bacteria.... | 11/04/2003 |
| 6638927 | Guanidinobenzamides Compounds of formula IA and IB are new ##STR1## where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceut... | 10/28/2003 |
