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| Number | Title | Issue Date |
| 7563896 | Process of obtaining type II dehydroquinase enzyme inhibitors and precursors thereof The present invention relates to a process of obtaining type II dehydroquinase enzyme inhibitors and the precursors thereof from (−)-quinic acid. The described compounds have a carboxycyclohexene structure. The process of preparing the compounds and their applicat... | 07/21/2009 |
| 7439356 | Substituted indan derivatives The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C | 10/21/2008 |
| 7427632 | Factor Xa inhibitors Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of ... | 09/23/2008 |
| 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 |
| 7365076 | Substituted aryl cycloalkanol derivatives and methods of their use The present invention is directed to substituted aryl cycloalkanoyl 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 sym... | 04/29/2008 |
| 7294736 | Process for preparation of probucol derivatives A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R | 11/13/2007 |
| 7265223 | Intermediate compounds for the preparation of mirtazapine and production methods thereof The present invention is directed to intermediate compounds of mirtazapine and methods for obtaining same. A method is described for obtaining (±)-3-phenyl-1-methylpiperazine, an important intermediate for obtaining mirtazapine, which is based on imposing a cycliza... | 09/04/2007 |
| 7094779 | Piperazine oxime dervatives having NK-1 receptor antagonistic activity The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents f... | 08/22/2006 |
| 7041826 | Process for preparing 1-methyl-3-phenylpiperazine using a novel intermediate The present invention describes an industrially advantageous process to prepare highly pure 1-Methyl-3-phenylpiperazine of Formula I that makes use of a novel piperazine derivative, 4-Benzyl-1-methyl-2-oxo-3-phenylpiper... | 05/09/2006 |
| 6960588 | Tryptase inhibitors Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors. ... | 11/01/2005 |
| 6943250 | Protected aminofunctionalized polymerization initiators and methods of making and using same Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality is part of a heterocyclic radical and includes a protecting group. ... | 09/13/2005 |
| 6919482 | β2-adrenergic receptor agonists Disclosed are multibinding compounds which are β2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.... | 07/19/2005 |
| 6906074 | 2-phenylpiperazine derivatives A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X... | 06/14/2005 |
| 6875759 | Substituted guanidines and the use thereof A method for the treatment of cancer and pain in an animal subject is disclosed, comprising administering to said animal in need of such treatment an effective amount of a compound of formula I: wherein R1-R... | 04/05/2005 |
| 6872826 | Stereoselective alkylation of chiral 2-methyl-4-protected piperazines In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process: ... | 03/29/2005 |
| 6737425 | N,N-substituted cyclic amine derivatives The invention provides an N,N-substituted cyclic amine compound represented by the following formula (VIII): wherein A represents an aryl group etc.; E represents a group represented by the formula —CO— or a group re... | 05/18/2004 |
| 6734177 | Certain salts of discodermolide acid, pharmaceutical compositions containing them and their use in treating tumors The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts. ... | 05/11/2004 |
| 6686353 | Diarylalkyl cyclic diamine derivatives as chemokine receptor antagonists Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-1a and/or MCP-1 on target cells, and are useful as a thera... | 02/03/2004 |
| 6649616 | Substituted phenylcyclohexanecarboxamides and their use The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) ##STR1## to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.... | 11/18/2003 |
| 6603003 | Method for the preparation of piperazine and its derivatives A novel method for the synthesis of piperazine and its derivatives of formula 1, ##STR1## wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; R... | 08/05/2003 |
| 6579881 | Indoles A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: ##STR1## wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3 | 06/17/2003 |
| 6548498 | Substituted indan derivatives The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives of the formula I ##STR1## as (R)-enantiomers, (S)-enantiomers, or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof. T... | 04/15/2003 |
| 6479485 | Benzamidine derivatives and their use as anti-coagulants This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states... | 11/12/2002 |
| 6472397 | Nitrogen-containing heterocyclic compounds having antiplatelet aggregation effect and medicinal use thereof The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D repres... | 10/29/2002 |
| 6469011 | Benzenesulfonamide compounds useful as TXA2 and 5-HT2 receptor antagonists Compound of formula (I): ##STR1## which is useful as a TXA2 and 5-HT2 receptor antagonist and pharmaceutical compositions containing the same.... | 10/22/2002 |
| 6448243 | 1,4-substituted cyclic amine derivatives A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: ##STR1## (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, ... | 09/10/2002 |
| 6420560 | H1--histamine receptor antagonists This invention relates to novel multibinding compounds (agents) that are H1 histamine receptor antagonists and pharmaceutical compositions comprising such compounds. Accordingly, the multibinding compounds and pharmaceutical compositions of this invention... | 07/16/2002 |
| 6376492 | Compounds and methods for inhibition of HIV and related viruses The present invention is directed to compounds, compositions and methods of inhibiting and treating HIV and related viruses, and methods for cocrystallizing reverse transcriptase in vitro, inhibition of the replication of HIV and related viruses thereof.... | 04/23/2002 |
| 6221868 | Remedies/preventives for frequent urination/urinary incontinence and tropone derivatives Remedies/preventives (therapeutic or preventive agents) against frequent urination (pollakiuria)/urinary incontinence which contain as an active ingredient compound having a tropone structure or pharmacologically acceptable salt thereof and a novel compou... | 04/24/2001 |
| 6166041 | 2-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH2 --CH2 --, --CH2 --, a single or ... | 12/26/2000 |
| 6153611 | Piperazinyl-cyclohexanes and cyclohexenes Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R1 and is independently H, C1-4 alky C1-4 alkoxy, C1-4 trihaloalkyl or halogen, or R and R1 may be taken together ... | 11/28/2000 |
| 6136803 | Antidepressants The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment ... | 10/24/2000 |
| 6130221 | Pharmaceutical agents that impede the initiation and progression of primary and secondary DMS disruptions Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the comp... | 10/10/2000 |
| 5935585 | Biaromatic amido compounds and pharmaceutical/cosmetic compositions comprised thereof Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment ... | 08/10/1999 |
| 5935958 | Muscarinic antagonists Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R1, R2, R3, R4, R21 | 08/10/1999 |
| 5919930 | Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates. In a process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluo... | 07/06/1999 |
| 5861535 | Reductive alkylation process to prepare tertiary aminoaryl compounds Tertiary aminoaryl compounds, such as N,N'dialkylaminoaryl compounds, are prepared using successive reductive steps without isolation therebetween, at high temperature and pressure. A nitroaryl compound is reduced using a ketone as both solvent and reacta... | 01/19/1999 |
| 5817489 | Di-nitrogen heterocycle compositions Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as antibacterial and as other pharmaceutical agents and as intermediat... | 10/06/1998 |
| 5807855 | 1-piperazino-1,2-dihydroindene derivatives Trans isomers of 1-piperazino-1,2-dihydroindene compounds having formula (I), ##STR1## wherein X and Y are hydrogen, halogen, trifluoromethyl, alkyl, alkylthio, trifluoromethylthio, alkoxy, hydroxy, alkylsulfonyl, amino, alkylamino, nitro or cya... | 09/15/1998 |
| 5753661 | Fused benzo compounds containing a nitrogen heterocycle for the treatment of central nervous system disorders Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroat... | 05/19/1998 |
