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6391872 |
Indazole bioisostere replacement of catechol in therapeutically active compounds
Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly...
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6376519 |
1-(4-sulfamylaryl)-3-substituted-5-aryl-2-pyrazolines and inhibitors of cyclooxygenase-2
Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C 1 -C 6 alkyl, and a group of formula II: wherein: R 3 and R 4 are independently selected from...
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6365617 |
Indole and indazole urea-peptoids as thrombin receptor antagonists
The invention is directed to novel indole and indazole urea-peptoid compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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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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6323226 |
Treatment of heart disease with cox-2 inhibitors
COX-2 selective inhibitors are disclosed as useful in treating or preventing heart disease, and in particular, congestive heart failure.
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6306887 |
Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
Compounds of Formula (1.0.0): ##STR1## are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably --C(O)--; B is independently selected from a group of moieties,...
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6303624 |
Preventives and remedies for hyperphosphatemia
This invention has for its object to provide a pharmaceutical composition for the prevention and/or treatment of hyperphosphatemia and secondary hyperparathyroidism, inclusive of their accessory...
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6291504 |
Acylsemicarbazides and their uses
The present invention relates to the synthesis of a new lass of indeno[1,2-c]pyrazol-4-ones of formula (I): ##STR1## that are potent inhibitors of the class of enzymes known as cyclin dependent...
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6277847 |
Herbicidal isoindolinonyl-and 3,4-dihydroisoquinolonyl-substituted heterocycles
This invention relates to herbicidal compounds of formula (I), methods of making such herbicidal compounds and methods of using such herbicidal compounds. It has been found that compounds of...
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6265429 |
Method for treating congestive heart failure
The present invention relates to methods for treating congestive heart failure in a mammal by administering a congestive heart failure treating amount of a compound which inhibits phosphodiesterase...
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6262040 |
Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF)
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R 1 , and R 2 , are as defined herein. The invention further relates to pharmaceutical...
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6255327 |
Diphenyl-substituted heterocycles, processes for preparing them and their use as pharmaceutical compositions
The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) ##STR1## wherein A, X and the groups R 1 , R 2 , R 3 , R 4 and R 5 are defined as in the claims,...
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6245796 |
Tricyclic pyrrole or pyrazole derivative
A tricyclic pyrrole or pyrazole derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, which shows strong affinity and selectivity for the 5-HT...
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6239160 |
4-haloalkyl-3-heterocyclylpyridines and 4-haloalkyl-5-heterocyclylpyrimidines, processes for their preparation, compositions comprising them, and their use as pesticides
The present invention relates to 4-haloalkyl-3-heterocyclylpyridines and 4-haloalkyl-5-heterocyclylpyrimidines of the formula (I), to processes for their preparation, to compositions comprising...
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6225329 |
Modulators of protein tyrosine phosphatases (PTPases)
The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are...
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6221878 |
Method for treatment of depression
The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT 3 receptors for the treatment of depression.
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6211222 |
Substituted indazole derivatives and related compounds
The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R 2 a and R 2 b are independently selected from the group consisting...
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RE37029 |
N-[(3-heteroaryl-1-pyrrolidinyl)-alkyl]phthalimides and related compounds and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a...
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6174883 |
3-substituted-2-oxindoles derivatives
This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H 2 synthase,...
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6166055 |
Benzoisothiazole compounds useful as IL-8 receptor antagonists
This invention relates to compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). ##STR1##
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6149928 |
Protection system against subterranean termites
The present invention provides a protection system against subterranean termites including a hollow pipe in which termites are able to circulate, a container for containing bait and a branch...
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6110954 |
Treatment
The use of a non-acidic non-steroidal anti-inflammatory drug (NSAID) such as dipyrone in the manufacture of a medicament for use in the treatment of pain in humans by epidural or intrathecal...
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6090751 |
Emulsifiable concentrate comprising an insecticidal 1-arylpyrazole
A new composition comprising an insecticidal 1-arylpyrazole, an N-alkylpyrrolidinone, a co-solvent and an emulsifier.
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6083969 |
1,3- and 2,3-diarylcycloalkano and cycloalkeno pyrazoles as selective inhibitors of cyclooxygenase-2 and antiinflammatory agents
This invention is directed to certain 1,3- and 2,3-diarylpyrazole antiinflammatory compounds of the general formulae: ##STR1## wherein R 1 and R 2 are independently selected from the group...
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6075023 |
Method for combatting fish mycoses and one-celled ectoparasites
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6069163 |
Azapeptide acids as cell adhesion inhibitors
Azapeptide acids of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These...
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6043240 |
3-heteroaryl-1-pyrrolidinealkylamines and derivatives thereof and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a...
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6030971 |
Methods and compositions for controlling biofouling using amides
The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one amide to...
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6025353 |
Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents
This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating angiogenic disorders.
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6020356 |
Pharmaceutical composition for the treatment of autoimmune diseases
A pharmaceutical composition comprising an anti-inflammatory drug capable of suppressing the production of cytokines (CSAID) an immunosuppressant and a pharmaceutically acceptable excipient.
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6011059 |
Acyl guanidine sodium/proton exchange inhibitors and method
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R 5 wherein R 5 is H, halo, alkenyl, alkynyl,...
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6001865 |
3-substituted 1-benzyl-1H-indazole derivatives as antifertility agents
An indazole derivative of formula (I) ##STR1## wherein R is selected from the group comprising --CONHNH 2 , --CONHN(CH 3 ) 2 and --CHCH--COOH, X and Y, the same or different from each other,...
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5998450 |
Heterocyclically substituted biphenylamine derivatives, their preparation and their use as fungicides
Biphenylamides of the general formula I ##STR1## and their salts (A= ##STR2## R 1 =F; R 2 =H, halogen, alkyl, CF 3 , alkoxy, alkylthio; R 3 =Cl, CF 3 ; R 4 =H, CH 3 ; R 5 =Cl, CH 3 , CHF 2 ,...
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5981554 |
Method of treatment of sugar plant to improve the sugar content
A method for improving and/or increasing the sugar content and/or preventing reduction of the sugar content of sugar plants, preferably sugar cane, which comprises treating said plants with an...
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5968944 |
Substituted pyrazoles as corticotropin-releasing factor (CRF) antagonists
The compounds of the formula wherein A, R 1 , R 3 , X 1 , Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses...
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5968916 |
Fluoroalkenyl compounds and their use as pest control agents
Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of...
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5962492 |
2 cyclo(alkyl and alkenyl) phenyl-alkenylyl heteroaryl compounds and pharmaceutical compositions containing same
Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR 1 , wherein R 1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R 6 ),...
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5958881 |
Composition containing VIP for injection and a method of enhancing visualization of tissues during medical procedures
A method of inducing a temporary substantial paralysis of an area of interest in a patient undergoing a medical procedure is provided. The method involves administering a therapeutically effective...
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5955489 |
Taxane derivatives, the preparation thereof and formulations containing them
The present invention relates to the preparation of taxane derivatives starting from 10-deacetyl-baccatine III, 14-hydroxy-10-deacetyl-baccatine 111, 19-hydroxy-10-deacetyl-baccatine III and their...
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5952316 |
2-amino-1,3-propanediol compound and immunosuppressant
2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted...
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5932598 |
Prodrugs of benzenesulfonamide-containing COX-2 inhibitors
Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
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5932589 |
Antitussive composition containing dextromethorphan and benzydamine
Oral antitussive pharmaceutical composition which allows a significant contact of its components with mucous membranes of the buccal cavity and comprises a centrally acting antitussive or a...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5922763 |
Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof,...
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5914344 |
Substituted carboxanilide derivative and plant disease control agent comprising same as active ingredient
A substituted carboxanilide derivative represented by the formula (1): ##STR1## wherein A is a hydrogen atom or methyl, B is a methyl or ethyl, and Het is 1-methyl-3-substituted-4-pyrazolyl or...
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5914335 |
Pesticidal 1-arylpyrazole-5-sulfinilimine derivatives
Compounds of formula (I): ##STR1## compositions containing them and methods of use to control pests.
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5889035 |
1-(Arylthioalkyl, arylaminoalkyl or arylmethylenealkyl)-3-(heteroaryl) pyrrolidines and related compounds useful as antipsychotics and analgesics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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5886016 |
Benzopyranopyrazolyl derivatives for the treatment of inflammation
A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1##...
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5872144 |
4-aminoethoxyindazole derivatives
This invention relates to dopamine D 2 agonists of the formula ##STR1## wherein: Y is hydrogen, halogen, or C 1 -C 6 alkoxy; R 1 is hydrogen or C 1 -C 6 alkyl; X is methylene, oxygen or...
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5872134 |
5-HT4 receptor antagonists
The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the treatment of artrial arrhythmia, stroke or CNS disorders X--CO--CH 2 --Z ...
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