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Class 546/124 - Tropanes (including nor and dehydro forms)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the bicyclo ring system has the following
No. of patents: 153
Last issue date: 12/29/2009


1        
NumberTitleIssue Date
7638629Piperidines and related compounds for treatment of alzheimer's disease
Compounds of formula I: selectively inhibit production of Aβ(1-42) and hence are useful in treatment or prevention of disease associated with deposition of β-amyloid in the brain. ...
12/29/2009
7544802Process for the preparation of 2-(ethoxymethyl)-tropane derivatives
The present invention relates to a process for preparing a 2-(ethoxymethyl)-tropane derivative or a pharmaceutically acceptable salt thereof, by reacting the corresponding 2-(hydroxymethyl)-tropane derivative with ethyl bromide in the presence of a base, and a phase...
06/09/2009
7476740Tropane compounds
The present invention provides novel tropane compounds and methods for their use. ...
01/13/2009
7439255Muscarinic acetylcholine receptor antagonists
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided. ...
10/21/2008
7432376Tropane prodrugs with central nervous system activity
Disclosed are tropane-based prodrug compounds bearing fatty ester and aromatic substituents. The compounds can be used for alleviating symptoms of CNS disorders. ...
10/07/2008
74079708-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions c...
08/05/2008
7405332Chemical process
The invention provides a process for preparation of a fluorohaloalkane, preferably an [18F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon compound of formu...
07/29/2008
7381733Tropane derivatives having dopamine reuptake inhibitor activity for the treatment of ischemic diseases
The present invention relates to the use of tropane derivatives having dopamine reuptake inhibitor activity for the treatment of diseases associated with reduced blood flow to the brain or with instances of a temporary break in blood supply to the brain, such as isc...
06/03/2008
7378526Azacyclic ethynyl derivatives
This invention relates to novel azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of...
05/27/2008
7375114Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 re...
05/20/2008
73616674′,4″-substituted 3α-(diphenylmethoxy) tropane analogs for treatment of mental disorders
The present invention describes a method for the treatment of attention deficit hyperactivity disorder (ADHD), conduct disorder, alcohol addiction, tobacco addiction, nicotine addiction, parkinsonism including Parkinson's disease, female and male orgasmic disorders,...
04/22/2008
7358244Azabicycloalkane compounds
This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acc...
04/15/2008
7345056Bridged N-cyclic sulfonamido inhibitors of gamma secretase
The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1...
03/18/2008
7321042Process for preparing N-substituted 3-β-aminonortropanes
The invention relates to a process for preparing N-substituted 3β-aminonortropanes of formula I wherein R1 has the meaning given in the claims, from the corresponding 3-oxonortropane or the correspond...
01/22/2008
7307087Treatment of affective disorders by the combined action of a nicotinic receptor agonist and a monoaminergic substance
This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances f...
12/11/2007
7294636Chemical compounds
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal) ...
11/13/2007
7291737Cocaine receptor binding ligands
A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and ...
11/06/2007
7276521Muscarinic acetylcholine receptor antagonists
Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided. ...
10/02/2007
72738662-aryl thiazole derivatives as KCNQ modulators
Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraine
09/25/2007
7268232Androgen receptor modulators and method of treating disease using the same
Disclosed herein are bicycloaryl compounds of Formula (I) that selectively modulate nuclear receptors, preferably the androgen receptor, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, and methods of treating disease comprising administering...
09/11/2007
7259250C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
08/21/2007
72504258-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprisi...
07/31/2007
7250426Tiotropium-containing pharmaceutical combination for inhalation
The present invention relates to new pharmaceutical compositions for inhalation containing one or more, preferably one, tiotropium salt combined with one or more pharmacologically acceptable acid addition salts of a compound of formula 2′, ...
07/31/2007
72476438-aza-bicyclo (3.2.1) octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 8-aza-bicyclop[3.2.1]octane derivatives useful as monoamine neurotransmitter re-up-take inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions compri...
07/24/2007
7217716N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain ...
05/15/2007
7219073Method for extracting information utilizing a user-context-based search engine
A data extraction tool is provided for cataloging information in an information source for searching by a user. The tool mines information from the information source and organizes the information, or the locations of that information, within a database. A user may ...
05/15/2007
7199132Tropane analogs and methods for inhibition of monoamine transport
New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Ce...
04/03/2007
7192969Ester derivatives
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); ...
03/20/2007
7115628Bridged piperidine derivatives as melanocortin receptor agonists
Certain novel bridged piperidine 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 diseases a...
10/03/2006
7105678Boat tropanes
Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter o...
09/12/2006
RE39128Pleuromutilin derivatives as antimicrobials
The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy. ...
06/13/2006
7049308C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
05/23/2006
7041667CCR5 modulators
Compounds of Formula 1 [Region α]—[Region β]—[Region γ]—[Region δ]  (1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/09/2006
7011813Cocaine receptor binding ligands
Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as...
03/14/2006
6989396Tropane alkaloid multidrug resistance inhibitors from and use of the same
Compounds and methods of modulating the activity of P-glycoproteins are disclosed. The method utilizes compounds derived from Erythroxylum pervillei. The compounds overcome multidrug resistance and can be used therapeutically to enhance performance of therape...
01/24/2006
6982271Tropane analogs
The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and/or norepinephrine reuptake. Also provided ...
01/03/2006
69649728-Azabicyclo(3,2,1)oct-2 ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
The invention disclosed herein relates to novel a 8-azabicyclo[3.2.1]oct-2-ene compound of Formula II, wherein R is hydrogen, methyl, ethyl or benzyl; and R1 is 3-thienyl, 2-thienyl...
11/15/2005
68439794-haloethenylphenyl tropane:serotonin transporter imaging agents
A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes and 4-haloethenylphenyl tropane families are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transpor...
01/18/2005
6815452Fluorenecarboxylic acid esters, process for the manufacture thereof, and use thereof as medicaments
Fluorenecarboxylic acid esters of general formula 1 wherein X− and the groups A, R, R1, R2, R3, R3′, R4, and R4′ have the meanings give...
11/09/2004
6790857Benzoylecgonine compositions and methods for producing them
This invention provides a method for preparing a benzoylecgonine composition comprising the steps of: (a) contacting benzoylmethylecgonine and propylene glycol in the presence or absence of water to form a reaction mixture; (b) maintaining the reaction...
09/14/2004
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