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6498172 |
Prostaglandin agonists and their use to treat bone disorders
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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6492332 |
Irrigation solution and methods for inhibition of tumor cell adhesion, pain and inflammation
This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell...
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6486185 |
3-heteroarylidene-2-indolinone protein kinase inhibitors
The present invention relates to novel 3-heteroarylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are...
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6479532 |
Antifungal compositions
This invention relates to an antimycotic composition comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and an...
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6479531 |
Gastrin and cholecystokinin receptor ligands
Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R 5 )—═CH—, —S— or...
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6472416 |
Sulfonylphenylpyrazole compounds useful as COX-2 inhibitors
The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
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6472406 |
Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase...
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6469032 |
3-(4′-bromobenzylindenyl)-2-indolinone and analogues thereof for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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6469036 |
Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment...
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6465506 |
Instillation techniques for ophthalmic agents to enhance treatment effect
The present invention provides methods for instilling an ophthalmic agent. One embodiment of a method according to the invention includes causing a patient to refrain from blinking for at least a...
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6462065 |
Use of 5-HT3 receptor antagonists for treating musculoeskeletal diseases
The present invention relates to a new use for compounds having 5-HT 3 (serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for...
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6458830 |
Tetrahydropyran derivatives and their use as therapeutic agents
The present invention relates to compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and n are defined herein. The compounds are of particular use...
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6455537 |
Methods for treating opiate intolerance
Provided are compositions comprising an opiate analgesic and an active compound containing the R isomer of N-methylnalorphine in a pharmaceutically acceptable carrier. Also provided are methods of...
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6451833 |
N-substituted (α-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
A class of N-substituted (α-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the...
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6436999 |
Diacyl-substituted guanidines, a process for their preparation, their use as medicine or diagnostic aid, and medicine containing them
Diacyl-substituted guanidines of the formula I are described where X( 1 ) and X( 2 ) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a...
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6429222 |
1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical preparations comprising them
The invention relates to novel 1-(p-thienylbenzy)imidazoles of formula (I) where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of...
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6426356 |
Imidazoethyl thiophenes
Certain imidazoethyl thiophenes/thiazoles and benzothiophenes of the formula: where Z is CH or N; and X is independently selected from the group consisting of hydrogen, C 1-4 alkyl, bromine,...
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6423712 |
2,4-Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to imidazolidine compounds of the formula I, The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the...
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6423707 |
Nitroimidazole ester analogues and therapeutic applications
Novel nitroimidazole compounds are provided that have a substituent linked via an ester linkage. The ester linkage may be obtained by derivation of the hydroxyl group of metronidazole. These...
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6420412 |
Eprosartan dihydate and a process for its production and formulation
The invention relates to (E)-α-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1-H-imidazol-5
-yl]methylene-2-thiopheneproprionic acid monomethanesulfonate dihydrate, a process for its production,...
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6420395 |
Azacyclooctane and heptane derivatives, their preparation and use in therapy
The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen,...
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6420375 |
Fused ring compounds, process for producing the same and use thereof
To provide a novel compound of the formula: [wherein A 1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A 2 is an aromatic ring which may be...
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6417219 |
Hetero-substituted cyclic amine metalloprotease inhibitors
The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular,...
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6410539 |
Imidazole derivatives and their use as farnesyl protein transferase inhibitors
The present invention relates to a compound of Formula (1) wherein Ar 1 represent (A) or (B) or (C); R 1 is hydrogen, C 1-4 alkyl or C 1-4 alkanoyl; R 12 and R 13 are independently hydrogen or...
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6410582 |
Thienylazolylalcoxyethanamines, their preparation and their application as medicaments
The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az...
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6410576 |
Thiazolidine derivatives
An object of the present invention is to provide novel thiazolidine derivatives which are useful as drugs. The thiazolidine derivatives according to the present invention are compounds represented...
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6403581 |
Method of inhibition of farnesyl-protein transferase using substituted benz (cd) indol-2-imine and-amine derivatives
The invention is a method of treating, inhibiting or controlling a ras-associated disease by inhibiting farnesyl-protein transferase(FPTase) enzyme, treating ras oncogene-dependent tumors, which...
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6399643 |
Spiroimidazolidine derivatives, their preparation, their use and pharmaceutical preparations formed therefrom
The present invention relates to spiroimidazolidine derivatives of the formula I in which E, V, W, X, R 1 and R 2 have the meanings indicated in the claims. The compounds of the formula I are...
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6395764 |
2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agnonists
This invention involves compounds having the following structure: wherein: a) R 1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R 2 and R 3 are each independently selected...
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6391901 |
Thrombin inhibitors
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical...
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6391327 |
Pesticidal composition
A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient wherein, A represents a 6-chloro-3-pyridyl,...
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6391879 |
Therapeutic anti-fungal nail preparation
A therapeutic solution and application procedure for curing and preventing nail fungus and athlete's foot infections or Onychomycosis comprising a combination of an anti-fungal agent with DMSO in a...
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6387906 |
2,4,4-trisubstituted-1,3-dioxolane antifungals
The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or...
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6384042 |
Systemic use of 5-HT3 receptor antagonists against rheumatic inflammatory processes
The present invention relates to a new use for compounds having 5-HT 3 (serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for...
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6376497 |
Antifungal azole derivatives having a fluorinated vinyl group and process for preparing same
An antifungal compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: X is CH or N; Y is O, R 1 and R 2 are each independently F or Cl; R 3 is a thiophenyl, naphthyl,...
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6376509 |
Melanocortin receptor agonists
Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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6372772 |
Inhibitors of redox signaling and methods of using same
The present invention is directed to a composition or formulation which inhibits or interferes with cellular redox function, and method of using same to restore normal cellular function. More...
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6369076 |
5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.
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6365615 |
Small molecules useful in the treatment of inflammatory disease
Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are:...
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6362212 |
Oxime derivative and bactericide containing the same as active ingredient
A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as...
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6362207 |
Methods of treating viral infections with benzimidazoles
This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a...
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6358993 |
Pharmaceutically active nitrogen ring compounds and methods of use thereof
The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof,...
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6355672 |
Benzothiepin derivatives, process for the preparation of the same and uses thereof
The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R 1 is an optionally substituted non-aromatic heterocyclic group; R 2 and R 3 ...
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6346518 |
Itraconazole and saperconazole stereoisomers
The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid...
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6342516 |
Phenylazole compounds, process for producing the same and drugs for hyperlipemia
Phenylazole compounds represented by general formula (1) or pharmaceutically acceptable salts thereof and drugs for hyperlipemia which contain these compounds as the active ingredient, wherein A...
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6329369 |
Methods of treating pain and other conditions
Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s)....
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6329148 |
Combined therapy of diterpenoid triepoxides and death domain receptor ligands for synergistic killing of tumor cells
A synergistic combination of ligands that interact with death domain receptors, and diterpenoid triepoxides is used to increase tumor cell killing by induction of apoptosis. Ligands useful in the...
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6323228 |
3-substituted indole angiogenesis inhibitors
3-Substituted indole carbohydrazides having the formula ##STR1## are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting...
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6313164 |
Dithiolin derivatives, their preparation and their therapeutic effect
Compounds of the formula (I): ##STR1## wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R 1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an...
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6310067 |
Urocanic acid derivatives
Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R 2 denotes hydrogen or lower...
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