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7582639 |
N-deacetylthiocolchicine derivatives, their use and pharmaceutical formulations containing them
Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I
in which: the linker is a bivalent straight or branched C 1 -C 8 alkyl residue, C 3 -C 8 cycloalkyl, a...
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7427632 |
Factor Xa inhibitors
Compounds of formula (I)
in which R 1 , n, Z, R 3 and R 4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment...
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7384943 |
Substituted chroman derivatives
The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I)
wherein
X is N; Y is NR 2 CH 2 , CH 2 NR 2 , NR 2 CO, CONR...
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7365196 |
Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of...
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7326696 |
Amino-methyl substituted tetracycline compounds
Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
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7271168 |
Piperazine derivatives having SST1 antagonistic activity
The invention provides compounds of formula ( 1 )
wherein X, R 1 and R 2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and...
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6916816 |
Phenanthryl piperazinyl dicarboxylic acids as selective NMDA receptor modulating agents
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than...
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6916812 |
Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the...
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6906046 |
Pharmaceutical uses and synthesis of benzobicyclooctanes
Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse...
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6846925 |
Colchinol derivatives as angiogenesis inhibitors
The invention related to colchinol derivatives of the formula (I): Wherein: R 1 ; R 2 and R 3 are each independently hydroxy, phosphoryloxy (—OP 3 H 2 ), C 1-4 alkoxy or an in vivo hydrolysable...
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6831084 |
Branched adamantyl and noradamantyl aryl- and aralkylpiperazines with serotonin 5-HT1A activity
This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's...
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6821967 |
Substituted piperazine derivatives, the preparation thereof and their use as medicaments
The present invention relates to substituted piperazine derivatives of general formula wherein R a , R b , R c , R f , R g , X, m and n are defined as in claim 1, the isomers and salts thereof,...
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6730784 |
Urea derivatives useful as synthetic intermediates
Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects...
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6703385 |
Tricyclic compounds having sPLA2-inhibitory activities
The present invention provides a compound having sPLA 2 inhibiting activity. The compound represented by the formula (I): wherein R 1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20...
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6593497 |
β2-adrenergic receptor agonists
The present invention is directed to multibinding compounds which are β2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma,...
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6387389 |
Sustained-release derivatives of hydroxylated analogs of substituted 1-&lsqb 2&lsqb bis(aryl)methoxy&rsqb ethyl&rsqb -piperazines and -homopiperazines and their use
The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions...
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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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6133268 |
1,4-disubstituted piperazines
The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R 1 , R 2 and r are as defined in the detailed part of the present description or...
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6096888 |
Anthracyclinone derivatives and their use in amyloidosis
The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of...
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6063924 |
Soluble chromophores containing solubilising groups which can be easily removed
Compounds of formula A(B) x (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone,...
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6048877 |
Tetralone derivatives as antiarrhythmic agents
Tetralone derivatives of the formula ##STR1## where R 1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo),...
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6025493 |
N-piperazinylalkyl-2-anthracenecarboxamides
Disclosed arm compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are the same or...
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6015900 |
N-aminoalkylfluorenecarboxamides
Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R a and R b represent hydrogen,...
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5998615 |
Anthracyclinone derivatives
The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of...
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5994543 |
Antibiotic bravomicins
A novel class of antibiotics, designated bravomicins, is obtained by fermentation of a strain of Micromonospora polytrota. Six bioactive compounds, designated bravomicins A, B, C, D, E and F, are...
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5789587 |
Heterocyclic-fused lactams promote release of growth hormone
There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the...
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5712280 |
Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a...
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5703083 |
N-aminoalkyl-1-biphenylenyl-2-carboxamides; new dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addidon salts thereof wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 independently represent...
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5686586 |
Polycyclic aromatic derivatives, process for preparing the same and pharmaceutical and cosmetic compositions containing the same
A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis. In the formula, X represents --CHCH--, O or S, ...
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5659033 |
N-aminoalkylfluorenecarboxamides; a new class of dopamine receptor subtype specific ligands
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R a and R b represent hydrogen, or...
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5612479 |
Polyphenols containing mesogenic moieties as lateral substituents
Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more...
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5607937 |
Piperazides of substituted phenylalanine derivatives as thrombin inhibitors
The present invention relates to D,L-, L- and D-phenylalanine piperazides of formula (I) defined in claim 1 that inhibit blood coagulation, and thrombin and/or trypsin, respectively. The compounds...
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5565457 |
Substituted sulfonamides
The compounds are N-(2,3,4-trimethoxybenzyl)piperazines N'-substituted by a radical containing a sulfonamide group, and pharmaceutically tolerable salts thereof, useful for treating myocardial...
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5508280 |
5H-Dibenzo (A,D) cycloheptenes as muscarinic receptor antagonists
This invention relates to novel derivatives of 5H-dibenzo (a,d)cycloheptenes, to the processes for their preparation, to their muscarinic receptor antagonist properties and to their end-use...
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5493036 |
Fibre-reactive anthraquinone dyes, their preparation and the use thereof
The invention relates to fibre-reactive anthraquinone dyes of formula ##STR1## wherein R 1 , R 2 , B, U, R and n are as defined in claim 1. The anthraquinone dyes of formula (1) are suitable for...
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5488119 |
Polymerisable photochromic naphthacenediones, polymers of these monomers, process for their preparation and the use thereof
Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R 1 to R 4 are H or a substituent such as phenylthio, and one of the substituents R 1 , R 2 , R 3 and R 4 ...
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5446146 |
Piperazine derivative having substituted phenyl groups
A therapeutic agent for liver disease containing as an active ingredient a piperazine derivative having the formula: ##STR1## wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group...
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5439940 |
Benz[e]indene derivatives
The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the...
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5436243 |
Aminoanthraquinone derivatives to combat multidrug resistance
Potentiating agents inhibit the development of multidrug resistance, reduce drug-resistance in drug-resistant tumors, or sensitize tumors to antineoplastic drugs, thereby potentiating the effect of...
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5380725 |
Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity
There are disclosed compounds of the formula (I) ##STR1## wherein R 1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and...
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5292726 |
N,N-diacylpiperazines
Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT 2 ) subtype useful in the treatment of cerebrovascular, cognitive, and CNS...
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5216178 |
Process of reducing olefins
Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of...
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5215992 |
Ethanobicyclic amine derivatives for CNS disorders
Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of...
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5141960 |
Tricyclic glycinamide derivatives as anti-convulsants
A class of tricyclic glycinamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula...
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5112826 |
Vasodilatory dihydrodibenzocycloheptyliden-ethylpiperazine derivatives
The dihydrodibenzocycloheptyliden-ethylpiperazine derivative has the formula: ##STR1## wherein R represents a substituent selected from the group consisting of --CHCH 2 ; --CO 2 C 2 H 5 ;...
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5098916 |
Propanobicyclic amine derivatives for CNS disorders
Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are...
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5091526 |
Process for the enantiospecific synthesis of intermediates for hexahydro-benzo[d]-naphtho[2,1-b]azepines
Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared. The present invention involves a process for preparing...
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5030631 |
Tricylclic arylsulfonamides
Novel tricyclic arylsulfonamides useful for treating hypertension and bronchoconstiction, as well as to their pharmaceutical compositions and methods for using the same.
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5001160 |
1-aryl-1-hydroxy-1-substitute d-3-(4-substituted-1-piperazinyl)-2-propanones and their use in treatment of neurogenic bladder disorders
Compounds are disclosed having the formula: ##STR1## in which R 1 is a C 1 l to C 12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or...
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4997836 |
Trisubstituted piperazine compounds, their production and use
Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R 1 , R 2 and R 3 are lower alkyl groups; A is a phenyl group, a...
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