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7538104 |
Photoactivable nitrogen bases
Compounds of the formula I R7″N—R6 RS—C,N—R4 H C, R′/I R, 3 R 2 (I) in which R, is an aromatic or heteroaromatic radical which is capable of absorbing light in the wave-length range from...
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7504405 |
Mitotic kinesin inhibitors
The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The...
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7504403 |
Substituted heterocyclic compounds and methods of use
The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation,...
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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...
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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...
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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,...
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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...
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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...
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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:
R 1 , R 2 and R 3 are as defined in the specification. Related pharmaceutical...
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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-on
e of the Formula...
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7271170 |
Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
Compounds of Formula I
are provided, as are methods for their preparation. The variables Z 1 , Z 2 , Z 3 , R 4 , R 5 , R 6 , R 7 , R 8 and Ar in the above formula are defined herein. Such...
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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...
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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...
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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...
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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,...
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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...
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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.
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7125863 |
Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R 1 is H or CN, X 1 is S, O, SO 2 or CH 2 , X 2 is CO, CH 2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The...
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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...
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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...
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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...
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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,...
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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 GABA A ...
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6933300 |
JAK-3 inhibitors for treating allergic disorders
Inhibitors of JAK3 kinase for the treatment of allergy, and others are described.
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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...
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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...
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6875771 |
Pyridopyrimidine derivatives as 5-HT6 antagonists
Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT 6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT 6 receptor...
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6864259 |
Antibacterial agents
The present invention provides compounds of Formula (I):
wherein R 1 -R 6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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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...
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6828326 |
Pyrimidinone fused bicyclic metalloproteinase inhibitors
The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R 1 are as defined in the specification, and to pharmaceutical compositions...
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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...
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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...
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6747032 |
Pyrimidin-4-one compounds
Compound of formula (I): wherein: R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy,...
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6703505 |
Process for the preparation of high purity Pemirolast
A novel process for the purification of Pemirolast, whose potassium salt is an anti-allergic pharmaceutical product, is disclosed.
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6649604 |
Substituted pyridone compounds and methods of use
Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other...
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6528489 |
Mycotoxin derivatives as antimitotic agents
The present invention provides a treatment for mammalian diseases characterized by aberrant cell proliferation. The treatment consists of administering therapeutically active dosages of antibiotic...
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6525056 |
Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders
Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6410628 |
Photoactivatable nitrogen-containing bases based on alpha-amino ketones
The invention relates to organic compounds having a molecular weight of less than 1000 comprising at least one structural unit of the formula (I) in which R 1 is an aromatic or heteroaromatic...
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6384222 |
N-benzenesulfonyl-L-proline compounds, preparation method and method for using the compounds in therapy
The present invention relates to compounds selected from the group consisting of: (i) the compounds of the formula in which X is a halogen atom, A is a group —NH—(CH 2 ) n —NH—CO—,...
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6369002 |
N-heteroaryl-substituted pyridine derivatives and their use as herbicides
Compounds of formula 1 wherein R 1 is hydrogen, fluorine, chlorine, bromine or methyl; R 2 is C 1 -C 4 alkyl, C 1 -C 4 halogenalkyl, halogen, hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 halogenalkoxy,...
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6348457 |
4-&lsqb 3-benzofuranyl&rsqb piperidinyl and 4-&lsqb 3-benzothienyl&rsqb piperidinyl derivatives
The invention is concerned with novel compounds of the formula the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or...
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6346359 |
Pyrrolopyrimidineone compound and heat-sensitive recording material using the same
Disclosed are a pyrrolopyrimidineone compound represented by the following general formula (1) and a heat-sensitive recording material using the pyrrolopyrimidineone compound as a coupler: General...
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6329116 |
Pyrrolo[1,2-a]pyrimidine compound and heat-sensitive recording material using the same
An object of the present invention is to provide a pyrrolo[1,2-a]pyrimidine compound that is useful as a coupler providing excellent hue of a cyan system and sufficient density of formed color. The...
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6320048 |
3-piperidinyl-1,2-benzisoxazoles
There is disclosed a process for preparing an enantiomeric form of the compound having the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein said process...
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6316605 |
Hydrazone dye
A hydrazone dye is provided which forms cyan color having an excellent hue. The hydrazone dye is expressed by the following general formula (I): ##STR1## wherein Ar represents an aryl group or a...
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6303614 |
Tetrahydro gamma-carbolines
The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R 1 is...
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6277986 |
Photoactivatable nitrogen-containing bases based on α-amino ketones
The invention relates to organic compounds having a molecular weight of less than 1000 comprising at lease one structural unit of the formula (I) ##STR1## in which R 1 is an aromatic or...
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6277847 |
Herbicidal isoindolinonyl-and 3,4-dihydroisoquinolonyl-substituted heterocycles
This invention relates to herbicidal compounds of formula (I), methods of making such herbicidal compounds and methods of using such herbicidal compounds. It has been found that compounds of...
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6229016 |
Method for treating tumors using 2-aryl-naphthyridin-4-ones
The present invention provides compounds of Formula I: ##STR1## wherein A and R 1 -R 8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic...
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6228553 |
Pyrrolo [1,2-A] pyrimidine compound and heat-sensitive recording material using the same
A pyrrolo[1,2-a]pyrimidine compound providing an excellent color-forming property is provided. Further, a novel cyan color-forming type diazo heat-sensitive recording material having excellent...
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