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6174879 |
Aminocyclohexylesters and uses thereof
Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a...
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6159959 |
Combined estrogen and antiestrogen therapy
The present invention relates to pharmaceutical compositions containing benzo[a]carbazoles or indenoindoles, which are useful as tissue selective estrogenic agents, having the general structures...
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6153625 |
Indan-1-ol compounds
A compound selected from those of formula (I): ##STR1## wherein: R 1 , R 2 , R 3 and R 4 , which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy,...
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6146656 |
Percutaneous absorption preparation
The present invention provides a percutaneous absorption preparation which comprises a skin contact base containing therein at least one active ingredient selected from the group consisting of...
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6140321 |
Polymorphs of donepezil hydrochloride and process for production
Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the...
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6136803 |
Antidepressants
The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The...
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6136827 |
Cyclic amine modulations of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity....
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6130217 |
Compounds enhancing antitumor activity of other cytotoxic agents
This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and...
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6121325 |
Naphthyl compounds promote release of growth hormone
The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R 1 , R 1a , R 2a , R 3 , R 3a , R 4 , R 5 , R 6 , A, W, and n are as defined herein....
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6117887 |
Inhibition of 26S and 20S proteasome by indanones
This invention is novel indanone compositions useful for inhibiting cell proliferation disorders in mammals.
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6110935 |
Benzofurazan compounds for enhancing glutamatergic synaptic responses
Compounds of the general structural formula ##STR1## are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of...
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6107345 |
Benzocyclobutane compounds
A compound of formula (I): ##STR1## wherein: Z 1 , Z 2 , Z 3 , Z 4 , which may be identical or different, represent a group as defined in the description, X represents oxygen, S(O) p , --(CH 2 )...
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6103700 |
Fluoro labelled anthracyclinone and anthracycline derivatives
Compounds of formula (A), wherein R 1 , R 2 , R 3 , Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their...
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6103720 |
Ketobenzamides as calpain inhibitors
The patent describes ketobenzamides of the formula ##STR1## where R1, R2, R3, R4, X and n have the meanings given in the description, and their preparation. The novel compounds are useful for...
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6083943 |
Substituted azaheterocyclecarboxylic acid
A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C 2 -C 4 alkylene; Z is a valence bond or C 1 -C 6 alkylene; R 1 is substituted or...
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6077852 |
Treatment of central nervous system disorders with selective estrogen receptor modulators
The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating...
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6060486 |
Carbostyril derivative for curing ophthalmological diseases
The present invention provides an agent for curing ophthalmological diseases which contains, as the active ingredient, a carbostyril derivative or salt thereof represented by the general formula...
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6048877 |
Tetralone derivatives as antiarrhythmic agents
Tetralone derivatives of the formula ##STR1## where R 1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo),...
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6046192 |
Phenylethanolaminotetralincarboxamide derivatives
The present invention relates to a phenylethanolaminotetralincarboxamide derivative represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino...
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6043251 |
Use of 1-(2-naphth-2-ylethyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyr idine for preparing drugs for treating amyotrophic lateral sclerosis
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6028103 |
Triaryl methane compounds and analogues thereof useful for the treatment or prevention of sickle cell disease or diseases characterized by abnormal cell proliferation
The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell...
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6022879 |
Bathocuproine treatment of neurologic disease
The present invention provides a method of treating amyotrophic lateral sclerosis and other neurologic diseases by administering bathocuproine or a related analog. Also provided are pharmaceutical...
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6017929 |
Cholinesterase activator
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6017935 |
7-sulfur substituted paclitaxels
The present invention relates to novel taxane derivatives wherein, the taxol ring is substituted by sulfur groups on the C-7, their use as antitumor agents and pharmaceutical formulations.
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6015811 |
Antitumor Chrysene derivatives
Chrysene derivatives having the formula ##STR1## have been found to have antitumor activity. In the above formula, at least one of R 1 -R 12 is --R 13 Z, where R 13 is a substituted or...
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6013656 |
2-(arylalkenyl) azacycloalkane derivatives as ligands for sigma receptors
New 2-(arylalkenyl)azacycloalkane derivatives which are ligands for sigma receptors, of the formula (I) ##STR1## in which: Ar is aryl or heteroaryl, optionally mono- to trisubstituted, m has the...
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6011046 |
Quinone compound, its production and use as antioxidant
A compound of the formula (I): ##STR1## wherein R 1 , R 2 and R 3 independently represent H, an optionally acylated hydroxyl group, an optionally substituted amino group, an optionally...
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6001885 |
Retinoid inhibition of expression of VEGF
The retinoids, in particular the anti-AP-1 retinoids, effectively inhibit the expression of VEGF, and thus are useful for the therapeutic treatment of disease states manifesting an overexpression...
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5998442 |
Benzo [B] thiophene compounds, and compositions for treating bone loss, and hyperlipidemia
The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological...
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5998444 |
Piperidinyl compounds as NK1 or NK2 antagonists
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , Q 4 , and Q 5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are...
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5994370 |
Indene compounds having activity as SERMS
The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus...
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5985895 |
2-naphthamide derivatives and their therapeutic applications
The invention relates to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z-Y entity represents an N--CH 2 ,...
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5968954 |
2-aminoindan compounds as 5HT.sub.1B antagonists
New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X 1 , X 2 , X 3 , and X 4 are as defined in the description, in the form of a racemic mixture and in the form of optical...
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5965562 |
Aroyl-piperidine derivatives
The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl
-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or...
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5965575 |
N-aryl piperidine compounds as 5HT.sub.1B antagonists
New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically...
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5958917 |
Benzofluorene compounds, intermediates, compositions, and methods
The present invention provides compounds of formula I ##STR1## wherein R 1 is --H, --OH, --O(C 1 -C 4 alkyl), --OCO(C 1 -C 6 alkyl), --OCOO(C 1 -C 6 alkyl), --OCOAr, --OCOOAr, or --OSO 2 (C...
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5952350 |
Naphthyl compounds and compositions, as estrogen receptor binding agents
The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of...
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5952354 |
Tris carbamic acid esters: inhibitors of cholesterol absorption
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are...
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5935973 |
Heterocyclcarboxamide derivatives and their use as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R 1 is an optional substituent; U is an alkylene...
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5932595 |
Matrix metalloprotease inhibitors
The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of...
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5929090 |
2-aryl-3-aminoaryloxynaphthy1 compounds, intermediates, compositions and methods
The present invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; having activity as a selective estrogen receptor modulator, pharmaceutical...
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5919797 |
Halogenated naphthyl methoxy piperidines for mapping serotonin transporter sites
Halogenated naphthyl methoxy piperidines having a strong affinity for the serotonin transporter are disclosed. Those compounds can be labeled with positron-emitting and/or gamma emitting halogen...
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5916916 |
1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods
The instant invention provides a series of naphthyl compounds having an oxygen linker at the 1-position which are useful as selective estrogen receptor modulators.
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5910508 |
Polycyclic polyenic compounds and pharmaceutical/cosmetic compositions comprised thereof
Novel pharmaceutically/cosmetically-active polycyclic polyenic compounds have the structural formula (I): ##STR1## and are useful for modulating cellular hormone receptors.
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5900418 |
Method for treatment of obesity
A method is provided for the control of obesity comprising administering to a mammal including humans suffering from obesity an acetylcholine esterase reactivator or prodrug derivative thereof...
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5885990 |
Substituted amidinonaphthyl ester derivative
Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1##...
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5885999 |
Serine derivatives and their use as therapeutic agents
The present invention relates to compounds of formula (I): ##STR1## wherein m is zero, 1 or 2; and n is zero or 1, with the proviso that the sum total of m+n is 1 or 2; R 1 represents phenyl;...
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5874447 |
4-Phenylpiperidine compounds for treating depression
The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: ##STR1## wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group...
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5869501 |
Amidinonaphthyl derivative or salt thereof
An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof,...
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5840735 |
Sex steroid activity inhibitors
Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress...
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