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5563154 |
Tetrahydro-quinolinyl/isoquinolinyl-terminal alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment...
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5561128 |
N-[(4-(hete roaryl)-1-piperidinyl)alkyl]-10,11-dihydro-5H-dibenz[B,F]azepines 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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5559126 |
1-[(1,4-benodioxanyl)alkyl]-4-(heteroaryl)piperidines 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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5559116 |
N-[(4-heteroaryl-1-piperazinyl) alkyl]-1H-benz[de]isoquinoline-1,3 (2H-)-diones 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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5559117 |
N-[(4-heteroaryl-1-piperazinyl) alkyl]-2-Benoxazolinines 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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5554633 |
Substituted amines as tachykinin receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR 9 , where R 9 is...
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5552419 |
Arylsulfonamido-substituted hydroxamic acids
The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof;...
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5552410 |
1,2,3,4,-tetrahydroquinoline-8-sulphonic acid chlorides and acids, their preparation and their use as synthetic intermediates
Compounds of the formula: ##STR1## in which R represents a chlorine atom or a hydroxyl group and R 4 represents a (C 1 -C 4 )alkyl group in the R or S form are useful as synthetic intermediates.
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5550130 |
1-[(1,4-benzodioxanyl)alkyl]-4-(heteroaryl)piperidines 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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5545640 |
Protease inhibiting succinic acid derivatives
Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of...
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5543433 |
Azine-substituted phenylacetic acid derivatives and fungicides containing these
Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH 3 ,...
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5541196 |
2-substituted quinolines for the treatment of leishmaniasis
Substituted quinolines having formula (1), wherein R 1 , R 3 , R 4 , R 5 , R 6 , and R 7 each independently represent a hydrogen atom, a linear or branched C 1 -7 alkyl, alkenyl, epoxy-alkyl or...
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5534524 |
Suppression of bone resorption by quinolines
The present invention focuses upon a method for inhibiting bone resorption. This method involves administering a 5-lipoxygenase inhibitor to a subject in an amount inhibiting the effects of an...
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5519022 |
α, α dialkylbenzyl derivatives
The invention concerns α,α-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar 1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen...
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5516784 |
Anti-HIV (AIDS) agents
Compounds of formula ##STR1## wherein Ar, W, Z, Q, R 1 , U, and T are as set forth herein, are described. These compounds are active as agents against retroviruses and in particular against HIV.
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5514690 |
Aminocarbonyl (thiocarbonyl) and cyanoguanidine derivatives of quinoline and indoline
Novel compounds having potassium channel activating activity and useful, for example, as antiischemic agents are disclosed. These compounds have the general formula ##STR1## wherein A is ##STR2##...
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5514694 |
Peptidyl ketoamides
A novel class of peptide α-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally...
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5512581 |
Iminoxycarboxylates and derivatives as inhibitors of leukotriene biosynthesis
The present invention relates to a compound of formula W--X--Q--Y--CH(R 1 )--O--NC(R 2 )--A--COM or a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or...
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5510379 |
Sulfonate ACAT inhibitors
β-Carboxy sulfonates of the formula ##STR1## wherein R 1 is aryl, R 3 and R 4 are hydrogen or alkyl, Y is -O-, -S-, or -NR 2 -, and R 5 is alkyl or aryl are potent inhibitors of the enzyme...
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5506242 |
Arylsufonamido-substituted hydroxamic acids
The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which...
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5506240 |
N-acyl-n-quinolinyl or isoquinounyl alkylamino acids compositions and method of use
The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the...
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5502061 |
Peptidyl substituted benzamides and naphthamies
The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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5500425 |
Chroman derivatives and a method of treating 5-HT mediated disorders
Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.
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5498610 |
Neuroprotective indolone and related derivatives
The present invention is directed to a method of blocking N-methyl-D-aspartic (NMDA) acid receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and...
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5494926 |
2/3-(heterocyclic alkyl amino)-1-(subst.-phenyl-methoxy)-ethanes/propanes as tachykinin-receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR 8 (R 8 is H or C...
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5492915 |
Substituted quinolyl compounds exhibiting selective leukotriene B.sub.4 antagonist activity
This invention relates to compounds having selective LTB 4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB 4 ...
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5491151 |
Antitumor treatment method
This invention relates to an antitumor agent containing as the effective ingredient a cyanine dye, shown by the general formula: ##STR1## where X - is a physiologically-acceptable anion; Z + , a...
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5489583 |
2-substituted 3-(4-amidinophenyl)propionic acid derivatives
2-Substituted 3-(4-amidinophenyl)propionic acid derivatives of the formula ##STR1## in which A, Ar and B have the meanings stated in the description, and the preparation thereof are described. The...
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5482942 |
(3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants
This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to...
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5480912 |
Method of treating HIV-1 with α-substituted benzenemethanamine derivatives
The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and...
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5476846 |
Substituted sulfonamides, process of preparation and medicines containing same
The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined...
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5462934 |
Condensed heterocyclic ketone derivatives and their use
A compound of the formula: ##STR1## wherein R 1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R...
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5459149 |
Penta-2,4-dienamides and use as pesticides
The present Application discloses pesticidally active compounds of formula (I): Q(CH 2 ) a (O) b Q 1 CR 2 =CR 3 CR 4 =CR 5 CXNR 1 R x or a salt or propesticide thereof, wherein Q is an...
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5457108 |
5-oxo-dibenzo[a,d]cyclohepta-1,4-dienes
The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
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5455252 |
Optionally substituted 6,8-quinolines
A compound of the formula ##STR1## wherein: R 1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl,...
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5441963 |
Potentiation of NMDA antagonists
The present invention is directed to a composition and method for poteniating the therapeutic effects of a class of known NMDA antagonists.
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5434162 |
Quinolinyl/isoquinolinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of...
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5428033 |
Saturated hydroxyalkylquinoline acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and...
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5424323 |
Sterilant composition
A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde...
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5422355 |
Composition for treating depression with (N-heteroaryl)alkylamines
The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar 1 --A 1 --; Ar and Ar 1 are the same or different aryl...
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5416095 |
Tetrahydro-quinolinyl-terminated non-peptidyl α-succinamidoacyl aminodiols as anti-hypertensive agents
Non-peptidyl compounds characterized generally as α-succinamidoacyl aminodiols having a tetrahydro-quinolinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of...
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5416117 |
Cyclopropenone derivatives
A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent...
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5407961 |
α-substituted benzenemethanamine derivatives and pharmaceutical use
The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and...
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5401753 |
Substituted n-heteroaryl-1, 2-diaminocyclobutene-3, 3-diones
The compounds of the formula: ##STR1## wherein: R 1 and R 2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is quinoline group which may be...
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5391569 |
New chromene compounds having a triene side chain
A compound selected from those of formula (I): ##STR1## in which the groups R 1 to R 8 are as defined the description. Medicaments.
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5391555 |
Methods for treating inflammatory bowel disease with leukotriene synthesis inhibitors
Described are methods for ameliorating symptoms associated with inflammatory bowel disease such as ulcerative colitis and Crohn's disease (regional enteritis) with four specific quinoline...
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5389645 |
Substituted tyrosyl diamine amide compounds
The present invention provides substituted tyrosyl diamine amide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia...
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5387591 |
Pyrrolidine compounds
Compounds of formula (I): ##STR1## in which: R 1 represents: optionally substituted alkyl, optionally substituted phenyl, pyridyl, optionally substituted phenylsulfonyl, acyl, ...
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5378711 |
α-arylacrylates substituted by a heterocyclic radical, and fungicides which contain these compounds
α-Arylacrylates substituted by a heterocyclic radical and of the general formula I ##STR1## where R 1 is alkoxy or alkylthio, R 2 is alkyl, Het is quinolyl, which is unsubstituted or...
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5369109 |
Optically active esters of 7-substituted 3,5-difunctionalized 6-heptenoic acids
The present invention provides optically active esters of 7-substituted 3,5-difunctionalized 6-heptenoic acids represented by the following formula: ##STR1## wherein R is a substituted or...
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