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7329659 |
Substituted-1-phthalazinamines as vr-1 antagonists
The present invention provides a compound of formula (I): in which Ar and R 1 are phenyl or a heteroaromatic group, R 2 is generally hydrogen, R 3 is hydrogen or alkyl and X, Y and Z are...
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7307078 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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7125869 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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7101879 |
Treatments for neurotoxicity in Alzheimer's Disease
The invention involves identification of a mechanism of β-amyloid peptide cytotoxicity, which enables treatment of conditions caused by β-amyloid peptide aggregates by administration of compounds...
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7019003 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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6984633 |
Method to treat cardiofibrosis with a combination therapy of an angiotensin II antagonist and epoxymexrenone
A therapeutic method is described for treating cardiofibrosis or cardiac hypertrophy using a combination therapy comprising a therapeutically-effective amount of an angiotensin II receptor...
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6972288 |
4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases
The present invention relates to bicyclic heterocycles of general formula
wherein
R a to R d , A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts...
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6924285 |
Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates to bicyclic heterocyclic groups of general formula
wherein
R a , R b , R c , R d and X are defined as in claim 1, the tautomers, the stereoisomers, the...
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6730671 |
Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
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6677333 |
2H-phthalazin-1-one derivatives and drug containing its derivatives as active ingredient
Poly(ADP-ribose)polymerase inhibitors containing as the active ingredient 2H-phthalazin-1-one derivatives represented by general formula (I) (wherein each symbol is as defined in the description)...
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6632813 |
6-subtituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof and processes for the preparation of both
The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and...
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6617329 |
Aminoquinazolines and their use as medicaments
Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the...
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6608057 |
Compounds useful as reversible inhibitors of cathepsin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
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6562830 |
Method of treating a patient having precancerous lesions with phenyl quinazolinone derivatives
Derivatives of 2-phenyl quinazolinones are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.
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6410536 |
Quinoxalinones as serine protease inhibitors such as factor XA and thrombin
This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically...
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6376490 |
Quinoxalinediones
The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is...
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6369057 |
Quinoxalines, processes for their preparation and their use
Compounds of the formula I or Ia in which n and the substituents R 1 , R 5 and x have the meaning mentioned have an antiviral activity.
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6339089 |
Pyrimidine nucleus-containing compound and a medicament containing the same for a blood oxygen partial pressure amelioration, and a method for preparing the same
A pyrimidine nucleus-containing compound represented by the formula (I): wherein ring A represents the ring of the formula (a): in which R 1 is a nitro group, an amino group, a substituted...
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6288065 |
Quinoxaline-carboxylic acid derivatives
The disclosure relates to quinoxaline derivates of Formula I ##STR1## wherein R 1 , R 4 , R 5 , R 6 , R 7 and R 8 are defined in the disclosure, as well as their production and use in...
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6245760 |
Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 lck tyrosine kinase activity, to pharmaceutical compositions comprising these...
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5948775 |
2- or 3-(substitutedaminoalkoxyphenyl)quinazolin-4-ones
This invention relates to 2- or 3-(substituted aminoalkoxyphenyl)quinazolin-4-ones which are partial estrogen agonists and are useful in treating osteoporosis, prostatic hypertrophy, breast cancer...
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RE36256 |
Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of...
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5912245 |
Acid amide derivatives and process for the preparation thereof
The present invention is directed to an acid amide of the formula ##STR1## wherein R 1 represents hydrogen or nitro, R 2 and R 3 stand for, independently from each other, hydrogen, lower...
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5852016 |
Quinoxaline derivatives useful in therapy
Compounds of formula (I), wherein A represents N or CH; R 1 and R 2 independently represent C 1 -4 alkyl, halo or CF 3 ; R 3 represents C 1 -4 alkyl (optionally substituted), C 3 -7 cycloalkyl,...
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5837708 |
Sulphonamides
Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders...
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5783572 |
Quinoxalinedione NMDA receptor antagonists
Compounds of formula (I): ##STR1## and their pharmaceutically acceptable salts, wherein R 1 and R 2 are each independently Cl, Br, CH 3 , CH 2 CH 3 or CF 3 ; R 3 is H, CH 3 or CH 2 CH 3 ;...
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5773444 |
Quinazolines as inhibitors of endothelin converting enzyme
Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated...
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5441959 |
Substituted quinazolinones bearing acidic functional groups as angiotensin II antagonists
Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists. ##STR1##
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5434150 |
Condensed 5-membered heterocyclic compounds, processes for preparing them and pharmaceutical preparations containing these compounds
The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R 1 , Z 1 to Z 6 , X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures...
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5409926 |
AT-2 antagonist inhibition of vascular restenosis
Novel disubstituted 6-aminoquinazolinones of the Formula ##STR1## are useful as angiotensin-II receptor (subtype 2) antagonists (AT 2 antagonists) alone or in combination with heparin, and can act...
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5401745 |
Quinazolinones substituted with phenoxyphenylacetic acid derivatives
Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as...
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5380719 |
Quinoxaline biphenyl angiotensin II inhibitors
Angiotensin II inhibition is exhibited by ##STR1## wherein: X is --CH 2 -- or O; R is hydrogen, alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl; R 1 and R 2 are each independently O...
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5312820 |
Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines
Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT 1 and AT 2 activity useful in the treatment of hypertension and...
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RE34201 |
N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides and pharmaceutical compositions and methods employing such compounds
This invention pertains to novel substituted N/aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic...
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5017579 |
Use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure
The present invention is directed to the use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure and compositions suitable for this case.
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4987135 |
Substituted benzene derivatives, processes for their production and antitumor compositions containing them
A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R 1 is --X 1 Z 1 (X 1 is an...
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4937337 |
Substituted heterocyclic compounds and the pharmacologically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them
The present invention provides compounds of the general formula: ##STR1## wherein R 1 is a straight-chained or branched C 1 -C 12 -alkyl radical which can be substituted by a phenyl, naphthyl or...
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4923864 |
Certain heterocyclic-hexanamides useful for treating hypertension
Simple amides and derivatives thereof useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
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4745118 |
Substituted quinazoline-3-oxides providing pharmacological activity
Novel substituted quinazoline-3-oxides are disclosed as are methods of increasing cardiotonic activity and bronchodilation in which an unit dose of a composition containing an effective amount of a...
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4684652 |
Pharmaceutical compositions containing naphthalene-and azanaphthalene-carboxamide derivatives, new naphthalene-and azanaphthalene-carboxamide derivatives and process for their preparation
Compounds of the formula: ##STR1## in which R 1 is C 1 -6 alkyl, phenyl, C 3 -6 cycloalkyl, phenylalkyl, cycloalkyl-alkyl or ##STR2## R 3 and R 4 being H or alkyl, R 5 being alkenyl or alkynyl,...
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4647568 |
Circulation-active hydroxy-tetra-hydropyridinelactones
Hydroxytetrahydropyridinelactones of the formula ##STR1## in which R represents a phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl,...
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4628054 |
Stabilizing quinoxaline di-N-oxides against light degradation
Quinoxaline di-N-oxides used in animal feeds, such as olaquindox, are stabilized against light degradation by substances which absorb light within the wavelength range from 200 to 450 nm, such as...
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4600709 |
Benzodioxole derivatives, processes for the manufacture thereof and corresponding pharmaceutical compositions
The invention relates to novel benzodioxole derivatives of the general formula I ##STR1## in which R 1 represents an unsubstituted or substituted, aliphatic, aromatic or heteroaromatic radical, ...
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4517184 |
Benzodioxole derivatives
The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R 1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an...
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4489073 |
1,3,4-Thiadiazin-5-ones
Heterocyclic compounds of the formula: ##STR1## wherein A is a direct link, or is alkylene of 1 to 4 carbon atoms or alkenylene of 2 to 4 carbon atoms; wherein either X is --CR 1 R 2 -- and Y is...
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4418063 |
Growth promoting quinoxaline-di-N-oxide carboxamides
Novel quinoxaline-di-N-oxide derivatives of the general formula ##STR1## in which R 1 is hydrogen or straight-chain or branched-chain alkyl having 1 to 4 carbon atoms, R 2 and R 3 ...
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4414214 |
Benzodioxole derivatives and pharmaceutical use thereof
The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R 1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an...
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4409219 |
Quinoxaline-1,4-dioxide fodder suppliments
The invention relates to new quinoxaline-1,4-derivatives of the general formula (I) and biologically acceptable salts thereof, ##STR1## wherein Q is a hydrogen atom or a methyl group, R 1 ...
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4333931 |
Method of combatting harmful microorganisms using quinoxaline compounds
Novel quinoxaline-di-N-oxide derivatives of the general formula ##STR1## in which R 1 is hydrogen or straight-chain or branched-chain alkyl having 1 to 4 carbon atoms, R 2 and R 3 ...
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4296114 |
3,4-Dihydro-3-oxopyrido[2,3-b]-pyrazines, compositions and use thereof
There are described compounds of formula I, ##STR1## in which R 1 is phenyl substituted by halogen, alkoxy, alkyl, carboxy-alkyl, --NR 4 R 5 , carboxy or alkoxy carbonyl, R 3 is hydrogen,...
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