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6323206 |
Chemokine receptor antagonists and methods of use therefor
Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically...
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6319929 |
Suksdorfin analogs, compositions thereof, and methods for making and using thereof
The present invention is directed to compounds that are analogs of the natural product suksdorfin. Compounds of the present invention include those having Formula IV: ##STR1## wherein R 20 through...
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RE37421 |
Rapamycin derivatives
Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit...
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6306870 |
N-cinnamoyl derivatives of beta-carboline
Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3',5'-monophoshate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of...
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6303593 |
3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of...
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6303569 |
Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula: ##STR1## wherein: B is H, OH, OSiR 13 , a...
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6291472 |
4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4, 5]furo[3,2-b] pyri-dine-6,8(7H)-dione derivatives for control of endoparasites processes for their preparation
The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7
H)-dione derivatives of the general formula (I) and salts thereof, ##STR1## in...
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6288081 |
Use of 7-(1-aminomethyl-2-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)-quinolone carboxylic acid and naphthyridone carboxylic acid derivatives for treating Helicobacter pylori infections and the gastroduodenal diseases associated therewith
The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl radical, and of...
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6288075 |
Thiazolo[5,4,3-ij]quinolines, preparation and medicines containing the same
Compounds of formula (I): ##STR1## their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments...
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6281224 |
Pranoprofen eyedrops containing organic amine
An ophthalmic solution containing 0.01 to 0.5 weight % of pranoprofen and 0.1 to 5.0 weight % of an organic amine, such as tromethamine or 4-(2-hydroxyethyl)-1-(2-sulfoethyl)piperazine. Such...
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6277860 |
Furopyridine antibacterials
This invention provides a compound of formula (I): ##STR1## or pharmaceutically acceptable salts thereof, wherein X 1 and X 2 are C or N, respectively; R 1 and R 2 are independently phenyl...
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6239128 |
Indole-2,3-dione-3-oxime derivatives for therapeutic use
The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.
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6221377 |
Administration media for analgesic, anti-inflammatory and anti-pyretic drugs containing nitrous oxide and pharmaceutical compositions containing such media and drugs
Administration mediums comprising solutions of nitrous oxide in water, alcohols, ethers or oils, and optionally including essential fatty acids or C 1 -C 6 alkyl esters thereof enhance the action...
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6211227 |
Tricyclic compounds
The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): ##STR1## (wherein ...
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6207679 |
Antimicrobial agents uses and compositions related thereto
The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical...
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6204245 |
Treatment of narcolepsy with immunosuppressants
The invention provides compositions and methods for treatment of narcolepsy or isolated cataplexy. Such methods entail administering a therapeutically effective regime of at least one...
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6201005 |
Method for inhibiting lymphokine production
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation autoimmune diseases,...
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6200985 |
Rapamycin derivatives
Rapamycin derivatives are disclosed of the formula: ##STR1## wherein the variables are in the specification.
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6191138 |
Phenanthridines
Compounds of formula (I), where R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings given in the description, are new active bronchial therapeutic agents. ##STR1##
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6187786 |
Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles
This invention concerns compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an...
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6187784 |
Pipecolic acid derivative hair growth compositions and uses
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pipecolic acid derivatives.
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6184228 |
Anti-sickling agents: selection methods and effective compounds
The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands...
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6180640 |
Di- and tetra-hydroquinoline-indole antimicrobial agents, uses and compositions related thereto
The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical...
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6169092 |
3-Ureido-pyridofurans and -pyridothiophenes for the treatment of inflammatory processes
3-Urea-pyridofurans and -pyridothiophenes are prepared by reacting appropriately substituted 3-amino-pyridofurans or -pyridothiophenes with isocyanates or isothiocyanates. The 3-urea-pyridofurans...
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6166032 |
Method for controlling tobacco use and alleviating withdrawal symptoms due to cessation of tobacco use
A method for controlling tobacco use and alleviating withdrawal symptoms due to the cessation of tobacco use comprising administering to a human desiring to control tobacco use and/or suffering...
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6156757 |
1,2,3,4-tetrahydro-benzofuro[3,2-C]pyridine derivatives
The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R 1 is...
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6150355 |
Phenylpiperidine derivative
A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH 2 --O, CH 2 --S, CH 2 --CH 2 ,...
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6130229 |
Tricyclic compounds having activity as RAS-FPT inhibitors
Compounds of Formula I: ##STR1## wherein: X 1 is hydrogen, halogen, CF 3 , nitro, NH 2 or lower alkyl; each X 2 is independently selected from the group consisting of hydrogen, halogen, lower...
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6121257 |
Sulfamate containing macrocyclic immunomodulators
The present invention relates to novel compounds of formula I: ##STR1## which are useful as immunomodulators, in particular, macrolide immunosuppressants. The invention also relates to the...
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6121278 |
Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity
A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: Y represents the atoms necessary...
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6117881 |
N-cinnamoyl derivatives of (β) carbolines
Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of...
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6093723 |
4-substituted beta-carbolines and analogs thereof
This invention relates to 4-substituted β-carbolines and β-carboline analogs that inhibit Ca +2 influx and interleukin-2 (IL-2) production. The 4-substituted β-carbolines and β-carboline...
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6083956 |
Optically pure androgen mediator
This invention relates to an optically pure androgen mediator, pharmaceutical compositions containing the stereoisomer and the use of the stereoisomer to aid in the prevention and restoration of...
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6080753 |
Stimulating nerve growth with immunophilins
Immunophilin ligands act by binding to receptor proteins, immunophilins, which in turn can bind to and regulate the Ca 2 + dependent phosphatase, calcineurin, and the Ca 2 + release channel, the...
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6080752 |
Tricyclic amine derivatives
A compound of formula (I): ##STR1## wherein R 1 represents a group of formula (A) or (B): ##STR2## R 2 , R 3 , Ar, Y Ar 1 are as defined herein; or a pharmaceutically acceptable salt thereof,...
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6028097 |
Method of immunosuppression
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases,...
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6004973 |
Pharmaceutical compositions comprising rafamycin coprecipitates
Disclosed are pharmaceutical compositions containing solid dispersions in the form of co-precipitates, which solid dispersions contain rapamycin and a carrier medium, and methods of treatment...
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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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5990106 |
Bicyclic amino group-substituted pyridonecarboxylic acid derivatives, esters thereof and salts thereof, and bicyclic amines useful as intermediates thereof
This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formula A--Pri esters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic...
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5972935 |
Biphenyl(thio)amide and bipennylethan(thi) one derivatives, their preparation and their use as 5-HT.sub.1D receptor antagonists
The invention relates to novel heterocyclic compounds of formula (I) or a salt or N-oxide thereof, in which R is a group of formulae (i), (ii) or (iii), where R 1 is hydrogen, halogen, C 1 -6...
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5962465 |
Aminomethyl-2,3,8,9-tetrahydro-7H-1,4-dioxino- 2,3-e!-indol-8-ones and derivatives
The compounds of formula I: ##STR1## wherein R 1 and R 2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R 1 and R 2 , taken together, are benzylidene optionally substituted with R 3 ...
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5958941 |
Use of L-carnitine and its alkanoyl derivatives for reducing the toxic effects of cyclosporin-A and other immunosuppressant drugs
The use of L-carnitine or of an alkanoyl L-carnitine or their pharmacologically acceptable salts is described for producing a medicament for inhibiting nephrotoxicity and vasculotoxicity resulting...
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5955469 |
Pharmaceutical composition
A pharmaceutical emulsion composition or solution composition in an organic solvent containing a compound represented by the following chemical formula and having immunosuppressive activity is...
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5952337 |
Remedy and preventive for nervous system disorders
An agent comprising a 4-aminoacyltetrahydrofuro 2,3-b!quinoline derivative represented by formula (I): ##STR1## (wherein R 1 represents an alkyl group having 2 to 6 carbon atoms, etc.) or an acid...
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5952344 |
Tetrahydroisoquinoline derivatives
The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula ##STR1## wherein A is aryl R 1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or...
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5952338 |
Agent for prophylaxis and treatment of disturbance of visual function
An agent for the prophylaxis and treatment of disturbance of visual function, which comprises a compound of the formula I! ##STR1## wherein A ring is optionally substituted; R 1 is a hydrogen...
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5939432 |
Thiophenes useful for modulating the adenosine receptor
The present invention relates to compounds of formulas (IA), (IB), and (IC): ##STR1## the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine...
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5939427 |
Lotion for FK 506
A lotion comprising a tricyclic compound, typically 17-allyl-1,14-dihydroxy-12- 2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l!-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-aza
tricyclo...
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5925649 |
Ascomycins
The invention provides novel ascomycins bearing one or more physiologically hydrolyzable and acceptable oxycarbonyl moieties or carboxy moieties, such compounds being found useful as...
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5922730 |
Alkylated rapamycin derivatives
This invention relates to compounds which possess immunosuppressive and/or anti tumor and/or antinflammatory activity in vivo and/or inhibit thymocyte proliferation in vitro. These compounds are...
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