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| Number | Title | Issue Date |
| 8071767 | Process for preparation of 9-hydroxy-3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-A]pyrimidin-4-one hydrochloride Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the pali... | 12/06/2011 |
| 7932385 | Paliperidone ketone A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperid... | 04/26/2011 |
| 7915412 | Process for the synthesis of 9-hydroxy risperidone (paliperidone) The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one. ... | 03/29/2011 |
| 7723518 | Preparation of 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4-pyrido[1,2-A]pyrimidin-4-one The present invention concerns a process for preparing crystalline 3-(2-chloro-ethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one substantially free of 2-acetylbutyrolactone. ... | 05/25/2010 |
| 7498434 | Two-phase method for the synthesis of selected pyrazolopyrimidines An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a... | 03/03/2009 |
| 7420056 | Substituted bicyclic imidazo-3-ylamine compounds Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related metho... | 09/02/2008 |
| 7414045 | Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12 | 08/19/2008 |
| 7405298 | Process for making risperidone and intermediates therefor The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel aceti... | 07/29/2008 |
| 7326711 | Pyridino[1,2-a]pyrimidin-4-one compounds as anticancer agents Pyridin[1,2-a]pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least on... | 02/05/2008 |
| 7320980 | Substituted pyrido(1,2-a)pyrimidines and their use as NOS inhibitors The invention relates to substituted pyrido[1,2-a]pyrimidine compounds corresponding to formula (I) wherein: R1, R2 and R3 are as defined in the specification. Relate... | 01/22/2008 |
| 7307168 | Process for the preparation of 3-{2-′4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido′1,2-methyl-4h-pyrido′,2-a!pyrimidin-4-one The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by sub... | 12/11/2007 |
| 7271170 | Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and ... | 09/18/2007 |
| 7256195 | Preparation of risperidone The present invention is directed to the novel forms of risperidone, designated Form A, Form B and Form E. Methods for their preparation are also disclosed. The present invention also relates to processes for making risperidone. Pharmaceutical compositions containin... | 08/14/2007 |
| 7230103 | Substituted 3,4-dihydropyrido[1,2-a]pyrimidines Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I and processes for the production thereof Also disclosed are substance libraries and pharmaceutical compositions containing the compound, and met... | 06/12/2007 |
| 7211572 | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt th... | 05/01/2007 |
| 7205405 | Process for preparing 3-(2-(4-(6-fluorobenzo(d)isoxazol-3-yl)-piperidin-1-yl)-ethyl)-2-methyl- 6,7,8,9-tetrahydro-4h-pyrido-(1,2-a)pyrimidin-4-one The process consists in condensing (2-methyl-6,7,8,9-tetrahydro-4 H-pyrido-[1,2-a]pyrimidin-3-yl)-acetaldehyd with 6-fluoro-3-piperidinyl)-1,2-benzisoxazole to yield the intermediate enamine, 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]vinyl}-2-methyl-6,... | 04/17/2007 |
| 7202360 | Method for preparing risperidone Risperidone is prepared in a high yield by reacting 2,4-difluorophenyl(4-piperidinyl)methanone oxime hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in an aqueous alkali hydroxide solution having an alkali hydroxide co... | 04/10/2007 |
| 7173022 | Bicyclic heterocycles as HIV integrase inhibitors The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also ... | 02/06/2007 |
| 7166655 | Colored particulate dispersion, ink for ink-jet recording using the same, and ink-jet recording method A colored particulate dispersion is provided, in which the particle diameter of colored particulates is small and dispersion stability is excellent. Also provided is an ink for ink-jet recording in which there is little dependency on paper such that excellent color ... | 01/23/2007 |
| 7141564 | Nitrogen-containing bicyclic heterocycles for use as antibacterials Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man. ... | 11/28/2006 |
| 7125863 | Inhibitors of dipeptidyl peptidase IV Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t... | 10/24/2006 |
| RE39197 | Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.... | 07/18/2006 |
| 7074929 | Certain alkylene diamine-substituted heterocycles This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and X... | 07/11/2006 |
| 7067662 | CXCR3 antagonists Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The su... | 06/27/2006 |
| 7067519 | 7,8,9,10-tetrahydro-6-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2-pyrrolo[2,1-]-quinazolinone derivatives The invention relates to novel 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns re... | 06/27/2006 |
| 7056917 | Drug efflux pump inhibitor A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): wherein, R1 and R2 ... | 06/06/2006 |
| 7030128 | Imidazo-pyrimidine derivatives as ligands for GABA receptors A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/o... | 04/18/2006 |
| 7029501 | Hair dye composition Provided is a hair dye composition containing a dissociative direct dye represented by the following formula (1): wherein, R1 to R4 each represents H or substit... | 04/18/2006 |
| 6974815 | Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(═O)— or optionally substituted C1-4alkylene; Ar... | 12/13/2005 |
| 6933300 | JAK-3 inhibitors for treating allergic disorders Inhibitors of JAK3 kinase for the treatment of allergy, and others are described. ... | 08/23/2005 |
| 6897308 | Process for the preparation of anti-psychotic 3-[2-[-4-(6-fluoro-1,2-benziosoxazol-3-yl)-1-piperidinyl] ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one A process for the preparation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one of the formula IIB: where X may be halo, acyloxy, or sulfonyloxy such as tosyloxy or mesyloxy, an interm... | 05/24/2005 |
| 6878700 | Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mamma... | 04/12/2005 |
| 6875771 | Pyridopyrimidine derivatives as 5-HT6 antagonists Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, de... | 04/05/2005 |
| 6864259 | Antibacterial agents The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as a... | 03/08/2005 |
| 6858613 | Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to trea... | 02/22/2005 |
| 6828326 | Pyrimidinone fused bicyclic metalloproteinase inhibitors The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical comp... | 12/07/2004 |
| 6803055 | Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes mic... | 10/12/2004 |
| 6784293 | Process for making Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials. ... | 08/31/2004 |
| 6762181 | Aminomethylpyrrolidine derivatives having aromatic substituents This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th... | 07/13/2004 |
| 6750341 | Preparation of risperidone The present invention is directed to the novel forms of risperidone, designated Form A, Form B and Form E. Methods for their preparation are also disclosed. The present invention also relates to processes for making risperidone. Pharmaceutical compositions containin... | 06/15/2004 |
