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5654325 |
Melatonin derivatives for use in treating sleep disorders
The present invention provides a method of treating sleep disorders using various melatonin analogs.
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5654301 |
Amino acid derivative anticonvulsant
The present invention relates to compounds of the formula ##STR1##
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5652269 |
Substituted hydrazinecarboximidamides and methods of use thereof
Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are...
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5641801 |
Method of reducing the period before the onset of sleep
Methods of inducing sleepiness and sleep in an individual by administering to that individual a single dose of melatonin sufficient to induce sleepiness and sleep in the individual.
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5641800 |
1H-indole-1-functional sPLA.sub.2 inhibitors
A class of novel 1H-indole-1-functional compounds is disclosed together with the use of such indole compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of conditions such...
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5637593 |
Tryptamine analogues as 5-ht1-like agonists
A compound of structure (I), in which A 1 is O, S(O) n in which n is 0, 1 or 2, NR, CH 2 , or CH(OH); A 2 is a bond or CH 2 ; or A 1 A 2 is CHCH; R is hydrogen or C 1 -4 alkyl; R 1 is an...
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5635528 |
Intermediates to tetrahydro-beta-carbolines
3-Ethanamine and 3-ethanamine related compounds are provided that are useful intermediates and have beneficial central nervous system activity.
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5635537 |
8-substituted-2-aminotetralins
A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR 1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein...
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5620998 |
N-acyl-N-heterocyclylalkylamino acid compounds and method of use thereof
The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y 1 is O, S or N(R) and R is hydrogen or C 1 -C 7 alkyl; X 1 is --CO-- or --S(O) m -- and the...
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5618834 |
Indole derivatives in the treatment of emesis
Compounds of formula I, ##STR1## wherein R 1 represents hydrogen; R 2 represents hydrogen, halogen, cyano, OR 4 , --(CH 2 ) m CONR 5 R 6 , --(CH 2 ) m SO 2 NR 5 R 6 , --(CH 2 ) m NR 7 COR...
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5616605 |
Peptide derivatives of collagenase inhibitor
This invention is directed to a collagenase inhibitor of the formula: ##STR1##
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5612367 |
Method of enhancing bioavailability of pharmaceutical agents
The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-met
hyl]-3-methoxy...
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5610174 |
Use of α.sub.1A -selective adrenoceptor agonists for the treatment of urinary incontinence
The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the...
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5610176 |
Tachykinin (NK1) receptor antagonists
The invention concerns tachykinin antagonists. The compounds are alcohols, amines and prodrugs of nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are...
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5607961 |
Antidepressant 3-(aminocycloalkenyl)-indole-5-nitrile derivatives
Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R 1 is hydrogen or C 1 -4 alkyl and...
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5607960 |
Indole derivatives as 5-HT1-like agonists for use in migraine
The present invention relates to 3,5-disubstituted indole compounds which are selective agonists which act on 5-hdroxytryptamine receptors useful in the treatment of migraine.
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5607962 |
Substituted indole derivatives
Substituted indole derivatives are prepared by reacting appropriate carboxylic acids, if appropriate in the presence of auxiliaries, with appropriate amines. The substituted indole derivatives are...
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5604253 |
N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a...
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5599832 |
Indoles as insecticides and acaricides
There are provided methods for the control of insects and the protection of crops from the damage caused thereby which comprise the use of compositions comprising an indole compound of formula I...
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5594028 |
Anti-tumor method and compounds
This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.
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5594012 |
Amino acid derivatives and anti-active oxygen agents
A novel anti-active oxygen agent which comprises as active ingredient an amino acid derivative represented by the following general formula (I): ##STR1## wherein Ar represents a 2-hydroxyphenyl,...
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5583152 |
Method for treating vasospastic cardiovascular diseases heterocyclic amide derivatives
The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts...
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5583149 |
Antimigraine derivatives of indolylcycloalkanylamines
A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1##
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5576332 |
Soft β-drenegic blocking agents
New soft β-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0...
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5576321 |
Compounds having effects on serotonin-related systems
A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The...
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5571833 |
Tryptamine analogues, their synthesis and their use as 5-HT.sub.1 -like or 5-HT.sub.2 receptor agonists
The present invention relates to known and novel tryptamine analogues, processes and intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy,...
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5571700 |
Process for preparing melanin pigments by bioconversion and use of the pigments obtained in cosmetics
The present invention relates to a method for the preparation of a melanic pigment by enzymatic bioconversion, implementing a melanin precursor substrate and plant cells, characterized in that: (a)...
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5559150 |
N,N-disulfonylated aminobenzene carboxlic acids and the use thereof as thrombin inhibitors
The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R 1...
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5556864 |
α-ω-diarylalkane compounds serotonin-2 receptor agonists
Compounds of formula (I): ##STR1## [wherein: R 1 is aryl; R 2 is hydrogen, alkyl, alkoxy, halogen or cyano; R 3 is a group of formula --B--NR 4 R 5 , where R 4 and R 5 are independently...
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5554641 |
Nonpeptides as tachykinin antagonists
The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK 3 antagonists expected to be useful in the treatment of pain,...
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5554640 |
Use of propanolamine derivatives as selective 5-HT.sub.1 antagonists
This invention provides a method of selectively antagonizing-the 5-HT 1A receptor in mammals by administering aryloxypropanolamines. Aryloxypropanolamines are also claimed.
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5552428 |
Compounds effective in the treatment of circadian rhythms and related disorders, the novel pharmaceutical preparations and novel method of application
The novel compounds of formula: ##STR1## in which R is isopropyl, cyclohexyl, phenyl, CH 3 , Br or I; or H R 1 is CH 3 or cyclopropyl and R 2 is H or Br, and when R 1 is cyclopropyl and R 2 is...
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5550134 |
Methods for inhibiting bone loss
The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series 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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5541204 |
Aryloxypropanolamine β 3 adrenergic agonists
Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R 1 to R 9 are as defined herein and m is the integer 0 or 1. These compounds are beta 3 adrenergic...
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5538752 |
Melanin compositions and uses thereof and resulting products
Compositions comprising melanin or melanin precursors are useful for preventing or controlling decay of substrates such as cellulosic and other porous organic substrates. The compositions provide...
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5536749 |
Method for attenuation of sympathetic nervous system activity or onset of migraine by selectively metabolized beta-blocking agents
Disclosed is a method for attenuating sympathetic nervous system hyperactivity or onset of migraine in a patient in need of such treatment, by the sublingual, buccal or intranasal administration to...
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5532237 |
Indole derivatives with affinity for the cannabinoid receptor
Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating...
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5532243 |
Antipsychotic nitrogen-containing bicyclic compounds
There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced...
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5521183 |
Use of 5-HT ligands as anti-pruritic agents
The present invention is based on the finding that 5-HT receptor ligands are useful in treating experimental models of clinically encountered pruritus (itch). A 5-HT ligand as used in this...
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5519033 |
Azabicyclo derivatives for treatment of urinary incontinence
The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of...
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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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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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5510353 |
Certain aminoguanidine compounds, pharmaceutical compositions containing them and their use in treating gastrointestinal motility disorders and disorders associated with cephalic pain
Compounds of formula A--X--Y--NH--B wherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen,...
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5504101 |
5-HT-1D receptor ligands
Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1Dβ receptor, of the formula: ##STR1## wherein R 1 is a group selected from aryl-C 1 -7...
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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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5498636 |
Treatment of angina pectoris
This invention relates to a method for treating angina pectoris. Pursuant to this method, a β-adrenergic-blocking agent is administered acutely to a person having angina to provide an essentially...
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5496844 |
Indole derivatives
The present invention provides indole derivatives of the general formula: ##STR1## The indole derivatives of the invention have potent antiestrogen activity and are useful as drugs for the...
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5494928 |
Indole derivatives
The invention releates to indole derivatives of the formula ##STR1## wherein R 1 to R 4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R 5 and R 6 are,...
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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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