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8163916 |
Azaadamantane ester and carbamate derivatives and methods of use thereof
The invention relates to compounds that are substituted azaadamantane ester and carbamate derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
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8097726 |
Huperzine a compound for treatment of alzheimer's disease
A huperzine A compound is provided. The huperzine A compound has following formula: wherein X comprises O or S, Y comprises —O—, —S—, —CH(R4)—, —C(R4)(R5)—, —C(R4)═C(R5)—, —C≡C—, —NH— or —N(R4)...
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8026252 |
Large substituent, non-phenolic opioids and methods of use thereof
8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
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7897766 |
Amino-aza-adamantane derivatives and methods of use
The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and...
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7893256 |
Azabicycloalkane 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 acceptable salt or solvate or stereoisomer thereof....
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7732441 |
Azabicycloalkane 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 acceptable salt or solvate or stereoisomer thereof....
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7557119 |
Large substituent, non-phenolic opioids
8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. One embodiment is the...
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7358244 |
Azabicycloalkane 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 acceptable salt or solvate or stereoisomer thereof....
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7253283 |
Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, ...
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7205300 |
Aryl fused azapolycyclic compounds
This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such...
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7186844 |
Method for producing cyclic carbamate ester
A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two...
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7041674 |
Carbamic acid esters with anticholinergic activity
A compound of formula 1 wherein X−, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical c...
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6982271 |
Tropane 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...
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6939867 |
β3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity, ...
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6858624 |
Aryl fused azapolycyclic compounds
This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such...
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6784186 |
Therapeutic compounds
This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of...
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RE38460 |
Huperzine A derivatives, their preparation and their use
The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is or R″ and Y together form ═CH; R is (C1-C5) alkyl, wherein n is 0 or 1, X is H, (C1-C5) alkyl; (C1...
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6683089 |
N-allyoxyethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocine-10-ols
The present invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3 -benzazocin-10-ols of general formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as set forth...
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6455538 |
1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two...
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6423842 |
Muscarinic agonists and antagonists
The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes...
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6387921 |
Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions
Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein:R1 and R2, which are identical or different, are each hydrogen, C1-C6-alkyl, C1--C6-alkyloxy, OH, F, Cl,...
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6271379 |
Intermediates useful for the synthesis of huperzine A
Intermediates useful for the synthesis of huperzine A represented by the structures below, ##STR1##and methods for their synthesis, wherein: R1 is lower alkyl, benzyl, or substituted benzyl; X is a...
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6245777 |
N-(5-phenyl-tetrahydrofuranyl)methyl- and N-(6-phenyl-tetrahydropyranyl)methyl-substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ols
The present invention relates to N-(5-phenyl-tetrahydrofuranyl)methyl- and N-(6-phenyl-tetrahydropyranyl)methyl-substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ols of general formula...
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6159986 |
Compounds and therapy for resisting memory loss in humans
Therapies and compounds for the inhibition of memory loss. In one embodiment, a combination of Huperzine A and hypericin is employed.
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6140502 |
Heat-based process for the re-racemisation of a (-)-2-phenylmethyl-3,3-dimethyl-piperidin-4-on derivative
A process for the re-racemisation of a (-)-2-phenylmethyl-3,3-dimethyl-piperidin-4-on derivative wherein a (-)-2-phenylmethyl-3,3-dimethyl-piperidin-4-on derivative of the formula 8Bwherein R2...
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6136980 |
Method of preparing norbenzomorphane as an intermediate in the preparation of pharmaceutically useful benzomorphane derivatives, in particular (-)-(1R,5S,2"R)-3'-hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzo morphane
The present invention relates to new processes for preparing norbenzomorphan, the central intermediate step in the preparation of pharmaceutically useful benzomorphan derivatives of general formula...
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6124312 |
Heterocyclic compounds
The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.
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6124459 |
Process for preparing pharmaceutically useful norbenzomorphane derivative
The present invention relates to a new process for preparing norbenzomorphane derivatives of general formula 1 ##STR1##
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6057446 |
Certain 1-aza-tricyclo [3.3.1-13,7 ] decane compounds
A compound having the formula: ##STR1## wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or...
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5990104 |
Polycyclic alcaloid-derivatives as NMDA-receptor antagonists
Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, --C(NH)--NH2, a positively...
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5945535 |
Method of preparing norbenzomorphanes
The present invention relates to a new process for preparing norbenzomorphan, the central intermediate step in the preparation of pharmaceutically useful benzomorphan derivatives of general formula...
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5731318 |
Benzomorphan derivatives
Novel benzomorphan derivatives of the formula ##STR1## wherein R1 -R8 are as defined herein. The benzomorphan derivatives are useful for treating cerebral ischaemia of various origins, epilepsy and...
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5717098 |
Process for the preparation of azanoradamantane benzamides
A process for the preparation of a γ-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce ...
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5663344 |
Method for the synthesis of huperzine A and analogs thereof and compounds useful therein
The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A....
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5650406 |
Adamantane derivative, process for producing the same, and use thereof
A compound represented by general formula (1) or an innocuous salt thereof, a process for producing the same, and a schizophrenia remedy containing the same as the active ingredient (wherein the...
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5607941 |
Useful for treating neurodegenerative diseases
Novel benzomorphan derivatives of the formula ##STR1## wherein R1 -R8 are as defined herein. The benzomorphan derivatives are useful for treating cerebral ischaemia of various origins, epilepsy and...
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5594002 |
Benzazabicyclic carbamates as novel cholinesterase inhibitors
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5587481 |
Preparation of (S)-decahydroisoquinoline-3-carboxylic acid t-butylamide
Methods for preparing (S)-N-tert-butyl-1,2,3,4-tetrahydro-3-isoquinoline-carboxami
de ("tic-c"), and converting tic-c to (S)-decahydroisoquinoline-3-carboxylic acid t-butylamide ("tic-d") are...
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5567818 |
Processes for preparing 2-(1-azabicyclo[2.2.2]oct-3-yl)-1H-benz[de] isoquinolin-1-one derivatives and intermediates useful therein
This invention relates to processes for preparing 2-(1-azabicyclo[2.2.2]oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-b
enz[de]isoquin olin-1-one, particularly 2-(1-azabicyclo[2.2.2]oct-3S-yl)-2,...
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5462960 |
Pyrazole-3-carboxamide derivatives, process for their preparation and pharmaceutical compositions in which they are present
The present invention relates to novel pyrazole-3-carboxamide derivatives of the formula ##STR1## in which the substituents are as defined in the specification. The present invention further...
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5420136 |
Eradication of pathogenic biological contaminants using non-azo naphthalimide dyes
A class of predominantly hydrophobic non-azo N-substituted 1,8-naphthalimide compounds, each bearing, at its 3-position, a nucleofuge and, at its 4-position, a heteroatomic electron-releasing...
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5399562 |
Indolones useful as serotonergic agents
This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT4 agonists or antagonists and 5-HT3 antagonists.
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5354758 |
Benzomorphans useful as NMDA receptor antagonists
Compounds of the formula I ##STR1## are disclosed. In this formula, R is a member selected from the group consisting of --CR1 R2 R3, hydroxy, an alkoxy group having 1 to 4 carbon atoms and --NR4...
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5240935 |
Substituted 2-azabicyclo[2.2.2]octane derivatives and compositions and method of use thereof
Novel substituted 2-azabicyclo[2.2.2]octane derivatives, pharmaceutical compositions containing them, methods for treating central nervous system disorders utilizing them, and processes for...
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5177082 |
Huperzines and analogs
The invention relates to compounds of the formulas ##STR1## wherein R1, R2 and R3 independently are hydrogen or lower alkyl, and the dotted ( . . . ) line is an optional double bond, and their...
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5145965 |
2,6-methanopyrrolo-3-benzazocines
Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
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5104880 |
Huperzine a analogs as acetylcholinesterase inhibitors
An acetylcholinesterase inhibitor is provided of the general formula (I): ##STR1## wherein R1 is H, (C1 -C8)alkyl or halo; R2 is H or (C1 -C8)alkyl; R3 and R4 are individually H, (C1 -C8)alkyl,...
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4985430 |
9-acylamino-tetrahydroacridine derivatives and memory enhancing agent containing said derivative as active ingredient
There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or...
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4871842 |
Piperidine derivatives
Novel compounds of the formula: ##STR1## [wherein A is an α-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R4 is hydrogen, lower alkyl, aralkyl or amino-lower ...
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4777254 |
Cyclic imides as H1 -antagonists
Polycyclic 1,3-dione imides N-alkylated with variously N-substituted alkyl- or cycloalkyl amines afford histamine H1 -receptor antagonists of the formula ##STR1## wherein R is polycyclic alkyl...
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