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6028080 |
Quinolin-2-(1H)-ones
The invention relates to quinoline-2-(1H)-one derivatives of the general formula I ##STR1## in which R 1 , R 2 and R 3 are in each case independently of one another H, Hal, A or OA; R 4 is H,...
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6025357 |
Anthelmintic paste
The present invention relates to hexahydropyrazino-derivative-based anthelmintic pastes for horses, dogs and cats, which are characterized in that they comprise corn starch and glycerol in addition...
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6025367 |
Sulfonamide derivatives as 5HT.sub.7 receptor antagonists
The invention relates to sulphonamide compounds of formula (I) or a salt thereof having pharmacological activity, processes for their preparation, to compositions containing them and to their use...
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6022895 |
Substituted amino compounds and their use as substances having an analgesic effect
Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.
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6022899 |
Substituted benzyloxy-carbonylguanidines, a process for their preparation, their use as a medicament or diagnostic, and a medicament containing them
There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are...
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6015837 |
Method for treating scoliosis with β2-adrenoceptor agonists
A method of treating scoliosis by adminstering β 2 adrenergic agonists in amounts sufficient to correct the condition.
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6011037 |
Thiazole derivatives with phosphodiesterase-inhibiting action
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6008228 |
Pharmaceutical compositions containing proteinase inhibitors
Compositions which increase the bioavailability of proteinase inhibitors are disclosed. Compositions which include a pharmaceutically acceptable carrier comprising monoglycerides of medium...
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6004977 |
N-(pyridinylamino) isoindolines and related compounds
Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing...
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6001807 |
Use of CRF-antagonists for treating emesis
CRF-antagonists are useful in the treatment of emesis.
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6001851 |
HIV protease inhibitors
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These...
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5998379 |
Serine protease inhibitors-proline analogs
The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase....
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5981521 |
Tetrahydroisoquinoline derivatives as LHRH antagonists
Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical...
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5972958 |
4-aminoalkoxy-1,3-dihydro-benzoimidazol-2-thiones
This invention relates to a novel series of compounds having potency at the dopamine D 2 receptor which are illustrated by the following Formula I: ##STR1## wherein: R 1 is hydrogen or C 1 -C 6 ...
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5972972 |
Pyrazoles as human non-pancreatic secretory phospholipase A.sub.2 inhibitors
A class of novel pyrazoles is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of conditions such as septic shock.
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5972975 |
Substituted 2-aminopyridines as inhibitors of nitric oxide synthase
Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders....
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5972959 |
Oxime derivatives, their preparation and their therapeutic use
Compounds of formula (I): ##STR1## wherein: R 1 is hydrogen or alkyl; R 2 is alkylene; R 3 is hydrogen, alkyl, alkoxy, alkylthio, halogen, nitro group, amino group, monoalkylamino, dialkylamino,...
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5968949 |
Substituted hydroisoquinoline derivatives and their use as pharmaceuticals
According to the present invention, there is provided a compound, or a solvate or salt thereof of formula (I): ##STR1## Substituted hydroisoquinoline derivatives are potent and selective delta...
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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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5968950 |
Apo B-secretion/MTP inhibitor hydrochloride salt
A hydrochloride salt of an Apo B secretion/MTP inhibitor, methods of making the salt, methods of using the salt and pharmaceutical compositions containing the salt are disclosed.
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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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5965582 |
N-benzylindole and benzopyrazole derivatives with anti-asthmatic, anti-allergic, anti-inflammatory and immunemodulating effect
The N-benzylindole- and benzopyrazole derivatives of the general formula 1 ##STR1## possess anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulating effect and are suitable for the...
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5962469 |
Cyclic nitrones
The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in...
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5958918 |
Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N- (aminominomethyl)phenylalkyl!-azaheterocyclylamide compounds
The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain...
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5955471 |
Tetrahydroisoquinolinealkanol derivatives and pharmaceutical compositions containing same
The present invention provides novel 1,2,3,4-tetrahydroisoquinoline carbamate and thiocarbamate derivatives represented by Formula I ##STR1## wherein: X 1 and X 2 are the same or different from...
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5955491 |
Method for treating osteoporosis
The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R 1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which...
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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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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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5948436 |
Pharmaceutical composition
A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable...
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5948779 |
Substituted condensation products of n-benzyl-3-indenyl acetamides with heterocyclic aldehydes
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell...
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5948778 |
Difluoro statone antiviral analogs
This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.
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5945413 |
Aspartyl protease inhibitors
This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized...
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5945425 |
Method of using (H.sup.+ /K.sup.+)ATPase inhibitors as antiviral agents
A class of compounds which are (H + /K + )ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula III: ##STR1## wherein D is N...
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5939430 |
Combinations of retroviral inhibitors
The combination of compounds of formula I and II can be used for the treatment of retroviraI infections. The combination can be used to treat AIDS and ARC and other diseases caused by the...
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5925651 |
Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to...
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5925631 |
Alkylated styrenes as prodrugs to COX-2 inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions...
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5922725 |
Benzimidazole compounds and their use as modulators of the GABA.sub.A receptor complex
The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R 3 is ##STR2## wherein A, B and D each is...
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5919794 |
Methods of using pharmaceutical tetrahydroisoquinolines
Methods of using pharmaceutical tetrahydroisoquinoline compounds for learning and/or memory enhancement, and for treatment of dementia, cocaine dependence, depression, eating disorders, anxiety, or...
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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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5910509 |
Antimicrobial agent for agriculture
The invention provides a method of treating or preventing a fungal infection comprising administering to a plant having a fungal infection a composition comprising an effective amount of a compound...
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5905077 |
Inhibitors of HIV protease useful for the treatment of AIDS
The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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5905086 |
Remedy for anxiety neurosis
N-(2-Hydroxyethyl)nicotinamide nitrate or its salt prevents or ameliorates anxiety neurosis or panic disorder, or the following anxiety. This compound or its salt has few side effects and exhibits...
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5889018 |
Heterocyclic compounds, pharmaceutical compositions comprising them and process for the preparation thereof
The invention relates to anxiolytic pharmaceutical compositions comprising as active ingredient 1-sytrylisoquinoline derivatives of general formula (I), wherein n is 1, 2, 3 or 4; R may be...
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5885985 |
Guanidine derivatives useful in therapy
Guanidine derivatives of formula I ##STR1## wherein R 8 represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from...
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5880135 |
Substituted 4-phenylaminothiazoles, their process of preparation and the pharmaceutical compositions containing them
A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R 1 , and R 21 ...
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5874451 |
Propanolamine derivatives, processes for their preparation, pharmaceuticals comprising these compounds, and their use
The invention relates to substituted propanolamine derivatives and their acid addition salts. Propanolamine derivatives of formula I, ##STR1## in which R 1 to R 8 have the meanings indicated in...
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5874444 |
Poly (ADP-ribose) polymerase inhibitors to treat diseases associated with cellular senescence
Inhibition of the enzyme poly (ADP-ribose) polymerase can delay the onset of senescence and inhibitors of the enzyme can be used to treat diseases caused or exacerbated by cellular senescence.
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5871780 |
Pest-controlling composition
A pest-controlling composition comprised of a borate compound and a compound resulting in elevated concentrations of cyclic AMP, such as a phosphodiesterase enzyme (PDE) inhibitor, or a...
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5872129 |
Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents
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5872117 |
1,2-ethanediol derivative and salt thereof, process for producing the same, and cerebral function-improving agent comprising the same
This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral...
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