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7569582 |
Aminotropane derivatives, preparation thereof and therapeutic use thereof
The present invention relates to compounds of formula (I) as defined herein that are melanocortin receptor agonists, to the preparation thereof and to the therapeutic use thereof in the treatment...
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7485650 |
High affinity ligands for nociceptin receptor ORL-1
The compound of the formula
or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors...
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7479494 |
3-monosubstituted tropane derivatives as nociceptin receptor ligands
Compounds of the formula
or a pharmaceutically acceptable salt thereof, wherein
R 1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl,...
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7381733 |
Tropane 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...
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7186731 |
2-cyanopyrrolidinecarboxamide compound
A compound of the formula (I) or a pharmaceutically acceptable salt thereof:
[wherein
X 1 and X 2 each is independently lower alkylene; X 3 is ═CH 2 , ═CHF or ═CF 2 ; R 1 is...
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7105678 |
Boat 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...
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6964972 |
8-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 R 1 is 3-thienyl, 2-thienyl,...
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6843979 |
4-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...
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6645977 |
8-azabicyclo(3,2,1)oct-2-ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein - - - - is a single or a double...
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6537522 |
Neuroprobes for mapping monoamine reuptake sites
Iodinated neuroprobes for mapping monoamine reuptake sites in the brain, and particularly iodinated neuroprobes that can also serve as radiotracers for use in single-photon emission computed...
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6399042 |
4-fluoroalkyl-3-halophenyl nortropanes
A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These...
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6383490 |
Anti-cocaine vaccine
An anti-cocaine vaccine employs a cocaine hapten conjugated to a carrier protein. The anti-cocaine vaccine elicits an immune response which reduces the psychoactive effects of cocaine consumption...
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6358492 |
Dopamine transporter imaging ligand
The 3α isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a...
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6350758 |
Tropane derivatives and method for their synthesis
A compound of formula (I) wherein R 1 -R 6 have any of the values defined in the specification are described, as well as pharmaceutical compositions comprising a compound of formula (I), and...
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6344179 |
Fluoralkenyl nortropanes
Provided are compounds of the following formula: wherein R is C2-C6 mono- or multi-unsaturated hydrocarbon having one or more ethylene, acetylene or allene groups, A is 18 or 19, and X is H or...
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6316624 |
Process for the preparation of substituted 8-azabicyclo[3,2,1]octanes
A process for preparing a compound of formula (IV) wherein R 1 is C 1 -4 alkyl, C 1 -4 haloalkyl, benzyl, C 3 -6 alkenyl or C 3 -6 alkyny, (provided that the α-carbon atom of R 1 is neither...
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6241963 |
Dopamine and serotonin transporter ligands and imaging agents
This invention presents a series novel tropane-based derivatives complexed with either technetium or rhenium that are specific for central nervous system receptors, in particular, dopamine or...
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6221879 |
8-azabicyclo[3.2.1] octane-3-methanamine derivatives as ligands of D2 and D3 dopamine and 5HT1A and 5HT2 serotonin receptors
Compounds of general formula (I) ##STR1## in which U represents a group of general formula (A) or (B) ##STR2## in which formulae V represents a hydrogen or halogen atom, a (C 1 -C 3 )alkyl group...
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6180083 |
Tropane derivatives useable in particular for in vivo detection of dopamine transporters
The present invention relates to tropane derivatives having particular use for the in vivo detection of dopamine transporters. These derivatives meet the formula ##STR1## in which R 1 is I or Sn...
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6171576 |
Dopamine transporter imaging agent
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...
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6123917 |
Method for making cocaine receptor binding ligands and intermediates therefor
An improved method for preparation of cocaine receptor binding ligands is provided. The method calls for the preparation of the silylaryl intermediate prepared from phenyl trimethylsilane and a...
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6054127 |
Hapten-carrier conjugates for use in drug-abuse therapy and methods for preparation of same
Hapten-carrier conjugates capable of eliciting anti-hapten antibodies in vivo are disclosed. Methods of preparing the hapten-carrier conjugates and therapeutic compositions are also disclosed....
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6013242 |
Tropane derivatives with selective binding to the serotonin reuptake transporters for treatment of mental illness and as intermediates in the formation of imaging diagnostic agents for depression
Biologically active derivatives of the tropane ring system are provided which selectively bind either to the 5-HT or DA reuptake site, leading to compounds which have use for the treatment of...
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5990312 |
Method for the preparation of esters of anhydroecgonine
The present invention discloses compounds of the formula any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in the...
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5958945 |
Naphthamide derivatives of 3-beta-amino azabicyclo octane or nonane as neuroleptic agents
The invention pertains to novel azabicyclo-naphthalene-carboxamide derivatives, a method for preparing same and the use thereof as a medicament. The compounds of the invention are of formula (I)....
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5935953 |
Methods for controlling invertebrate pests using cocaine receptor binding ligands
The invention relates to a method of controlling an invertebrate pest, comprising contacting the pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a...
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5888475 |
Labeled cocaine analogs
Novel methods for positron emission tomography or single photon emission spectroscopy using tracer compounds having the structure: ##STR1## where X in β configuration is phenyl, naphthyl; 2,3...
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5834484 |
Cocaine analogs
Cocaine analogs are disclosed. The analogs, certain 6-alkyl substituted tropane derivatives, bind to the cocaine binding site on dopamine transporter, without interfering with the dopamine...
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5821249 |
Anhydroecogonine compounds and their use as anticholinergic agents
Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings...
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5736556 |
Tropane-2-aldoxime derivatives as nevro transmitter reuptake inhibitors
The present invention discloses compounds of the formula, ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5591854 |
Enantioselective synthesis of seven-membered carbocycles and tropanes
A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.
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5552407 |
Anhydroecgonine compounds and their use as anticholinergic agents
Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings...
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5416092 |
3-azabicyclo[3.2.1]-oct-8-yl-terminated non-peptidyl α-succinamidoacyl aminodiols as anti-hypertensive agents
Non-peptidyl compounds characterized generally as α-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment...
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5374636 |
2,3-trans-disubstituted tropane compounds which have useful pharmaceutical utility
The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5340936 |
8-azabicyclo[3.2.1]octane methanone and corresponding oximes
This invention relates to compounds of the formula ##STR1## where X is --0--, --S--or --NH--; Y is hydrogen, halogen and loweralkoxy; p is 1 or 2; n is 2, 3 or 4; R is hydrogen,...
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5288872 |
Compounds for treatment of neurodegenerative diseases
Novel tropane ring system compounds useful for treatment of neurological disorders and for synthetic starting materials for production of cocaine analogs.
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5234931 |
Heteroaryl-8-azabicyclo[3.2.1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin
This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--; Y is hydrogen, halogen and loweralkoxy; p is 1 or 2; n is 2, 3 or 4; R is hydrogen,...
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5128118 |
Cocaine receptor binding ligands
3β-[4-iodophenyl]-tropan-2β-carboxylic acid methyl ester tartrate is a high affinity binding ligand for neurotransmitters in mammalian brains. It and its congeners may be employed for imaging and...
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4889849 |
Spasmolytically active tertiary amine derivatives
The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is...
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4877785 |
Non-peptidyl beta-succinamidoacyl aminodiols as anti-hypertensive agents
Non-peptidyl compounds characterized generally as β-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.
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4379936 |
Nortropane derivatives
3α-Benzoylamino-2β-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding...
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4366154 |
Tropyl derivatives
Tropyl derivatives of the formula: ##STR1## in which R 1 is (a) phenyl linked through a direct bond, --O--, ##STR2## (in which m=2 or 3); (b) diphenylmethyl; or (c) 10H-phenothiazin-10-yl; (each...
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4350691 |
Certain azabicyclocarboxamides and compositions containing same
Compounds of the formula (III) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R 1 is a C 1 -6 alkoxy or C 1 -6 alkylthio group; R 2 and R 3 are the same or different and are...
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4341895 |
Tropane derivatives
3α-Benzylamino-2β-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding...
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4179567 |
2-Aryltropane compounds
Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substiutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a...
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4160099 |
Labile, non-heterocyclic quaternary ammonium salt/esters as transient derivatives
Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated...
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3718660 |
ARYLSULPHONYL UREAS CONTAINING HETEROCYCLIC ACYLAMINO GROUPS
Blood sugar lowering compounds useful as oral anti-diabetics are provided. The compounds have low toxicity and are well tolerated. They are arylsulphonyl ureas having heterocyclic acylamino groups...
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3445470 |
HETEROCYCLIC DERIVATIVES OF ARYL SULFONYL CARBAMIC ACID
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3340267 |
Certain n-(ethoxycarbonyl)-nortropane and 9-azabicyclo [3. 3. 1] nonane derivatives
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3120537 |
3-(monocarbocyclic aryl)-3-carboxytropanes and esters thereof
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