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Class 514/259.41 - Additional hetero ring is attached directly or indirectly to the bicyclo ring system by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system is attached
No. of patents: 106
Last issue date: 02/14/2012


1      
NumberTitleIssue Date
8114883Polymer formulations for delivery of bioactive materials
Delivery of drugs in association with PLGA polymers which have crystallinity resulting from the presence of long chain alkyl groups in terminal units. ...
02/14/2012
8093256Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
The invention relates to use of substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. More specifically, the invention relates t...
01/10/2012
7776866Deuterium-enriched risperidone
The present application describes deuterium-enriched risperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. ...
08/17/2010
7420056Substituted 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
7414045Substituted 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
7393853Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-] pyrimidin-4-one derivatives as therapeutic agents
The invention relates to use of a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein for treating a variety of disease states...
07/01/2008
7371406Preparation of injectable suspensions having improved injectability
Injectable compositions having improved injectability. The injectable compositions include microparticles suspended in an aqueous injection vehicle having a viscosity of at least 20 cp at 20° C. The increased viscosity of the injection vehicle that constitutes the ...
05/13/2008
7326711Pyridino[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
7256195Preparation 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
72476388-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives.
The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. The invention relates also to a medica...
07/24/2007
7232827Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group,...
06/19/2007
7230103Substituted 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
7217715Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein. The invention relates also to a med...
05/15/2007
7214682Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an et...
05/08/2007
7173034Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each ...
02/06/2007
7118763Microencapsulated 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...
10/10/2006
7097868Stable coated microcapsules
A microencapsulated composition containing lipophilic compounds is prepared by reducing the particle size of the lipophilic compound in the presence of a surface active agent to form a first solution; preparing a solution of alkali metal alginate to form a second so...
08/29/2006
69748192-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydoimidazo{1,2-a}pyrimidin-5(1H)one derivatives
Imidazo[1,2-α]pyrimidinones and pyrimido[1,2-α]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3β activity. ...
12/13/2005
6964962Combinations of reboxetine and neuroleptic agents
A composition comprising: (a) a pharmaceutically effective amount of reboxetine; and selected from the group consisting of clozapine, olanzapine, risperidone and mixtures thereof (b) a pharmaceutically effective amount of one or more neurol...
11/15/2005
6924287Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH...
08/02/2005
6887870Heterocyclic sodium/proton exchange inhibitors and method
Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, a...
05/03/2005
6875771Pyridopyrimidine 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
6864259Antibacterial 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
6800639Pharmaceutical combination for the treatment of cancer
In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of cancer comprising at least one active compound of formula (I): and at least one further therapeutic agen...
10/05/2004
6762181Aminomethylpyrrolidine 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
6747032Pyrimidin-4-one compounds
Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, a...
06/08/2004
6696443Piperidine/piperazine-type inhibitors of p38 kinase
Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-଱ kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-଱ kinase activity....
02/24/2004
6649604Substituted pyridone compounds and methods of use
Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-଱, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention enco...
11/18/2003
6620819Anticonvulsant derivatives useful in treating psychosis
The anticonvulsant derivative topiramate useful in treating dementia and/or behavioral and psychotic disturbances in dementia is disclosed....
09/16/2003
6599532Osmotic device containing alprazolam and an antipsychotic agent
The present invention provides an osmotic device containing controlled release alprazolam in the core optionally in combination with an anti-psychotic agent, in a rapid release external coat. A wide range of anti-psychotic agents can be used in this devic...
07/29/2003
6566389Therapeutic uses of melatonin
A method for treating or preventing symptoms of tardive dyskensia comprises administering melatonin to patient exhibiting or liable to develop such symptoms. The melatonin is administered in an amount effective to ameliorate or prevent symptoms of tardive...
05/20/2003
6555544Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters
The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxy-...
04/29/2003
6544559Microencapsulated 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 i...
04/08/2003
6506762Certain alkylene diamine-substituted heterocycles
The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of N...
01/14/2003
6500833(+)-Hydroxyrisperidone compositions and methods
Methods and compositions utilizing a compound represented by Formula III, ##STR1## wherein R is chosen from --OH, --P(O)(OH)2 and --SO3 H, or pharmaceutically acceptable salts thereof, for the treatment of psychoses in humans are dis...
12/31/2002
6444665Method for treating pain
The present invention provides a method for treating pain using an atypical antipsychotic compound....
09/03/2002
6420369Anticonvulsant derivatives useful in treating dementia
Anticonvulsant derivatives useful in treating dementia and/or behavioral and psychotic disturbances in dementia are disclosed....
07/16/2002
6395727Method of treating Bulimia Nervosa and related eating disorders by administration of atypical antipsychotic medications
The invention relates to a method of treating non-psychotic disorders by administration of atypical antipsychotic medications, in particular, risperidone. More specifically, the invention relates to a method of treating the eating disorder Bulimia Nervosa...
05/28/2002
6368632Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Method of treating warm blooded animals suffering from psychotic disorders. The method includes administering a pharmaceutically effective amount of sustained-release microparticles that include risperidone, or a pharmaceutically acceptable acid addition ...
04/09/2002
63484574-[3-benzofuranyl]piperidinyl and 4-[3-benzothienyl]piperidinyl derivatives
The invention is concerned with novel compounds of the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or sulphur; R1 is hydrogen or halo; R2
02/19/2002
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