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5622950 |
Pyrrolo-pyridine derivatives
A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a...
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5618815 |
1,9-bridged thiazolo[3,2-a]quinoline derivatives
The present invention relates to 1,9-bridged thiazolo[3,2-a]quinoline derivatives of the general formula (I) ##STR1## in which the substituents Z, X, R 1 have the meaning given in the description,...
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5616586 |
Tricyclic quinoxalinediones
Tricyclic quinoxalinediones of the formula: ##STR1## wherein X is alkyl, halogen, cyano, trifluoromethyl, nitro, hydroxy, amino, etc.; R 1 is H, etc.; R 2 is H, alkyl, cycloalkyl, alkenyl,...
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5604224 |
Substituted heterocyclylisoquinolinium salts and compositions and methods of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5599809 |
Method for improving reproductive efficiency in farm animals
Oxytocin receptor antagonists of the formula ##STR1## wherein R 12 is hydrogen, alkoxycarbonyl or unsubstituted of substituted alkyl; R 13 is hydrogen, alkoxyl, aralkoxyl, alkoxycarbonyl,...
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5599812 |
Tricyclic pyrrolopyrazine 5-HT.sub.3 -active compounds
The present invention relates to a compound selected from these of formula (I): ##STR1## in which A and R 1 are as defined in the description, and medicinal product containing the same which is...
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5597823 |
Tricyclic substituted hexahydrobenz [e]isoindole alpha-1 adrenergic antagonists
The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an α-1 adrenergic...
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5589476 |
Imidazol-4-ylpiperidine derivatives, their preparation and their application in therapeutics
A compound of formula (I): ##STR1## in which R 1 represents a hydrogen atom or a straight or branched (C 1 -C 4 )alkyl group; and A represents a 5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl...
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5585347 |
Methods for the determination and adjustment of prolactin daily rhythms
Disclosed are methods for detecting abnormalities in prolactin daily rhythms. The methods involve comparing a prolactin profile of a vertebrate (including a human) subject being tested that has...
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5569658 |
Tricyclic derivatives
The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R 1 and R 2 together form an optionally substituted group of the formula --NCH--NH--, --NCH--O--,...
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5569655 |
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5559106 |
Heterocyclic compounds, their use and preparation
Quinoxaline compounds of the general formula ##STR1## wherein R 1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R 6 , R 7 , R 8 ...
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5550107 |
Combination therapy for the treatment of estrogen-sensitive disease
A method of treatment of breast and endometrial cancer in susceptible warm-blooded animals may include inhibition of ovarian hormonal secretion by surgical (ovariectomy) or chemical (use of an LHRH...
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5538972 |
Imidazoloquinoxalinones for the treatment of central nervous disorders
The use of imidazoloquinoxalinones for the production of drugs for controlling central nervous disorders is described. The imidazoloquinoxalinones have the formula ##STR1## in which R 1 , R 2 and...
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5538971 |
Benzoquinoxalines, pharmaceutical compositions containing them and their use in treating schizophrenia
6-hydroxy or 6-alkoxy-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoxalines bearing in position 4 an optionally substituted phenyl group may be used in the treatment of schizophrenia, drug abuse or...
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5536715 |
Combinations of anthelmintically active agents
Pharmaceutical compositions comprising a compound of formula (I) and at least one other anthelmintically active compound, being an avermectin or a milbemycin, are useful in the treatment of...
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5536660 |
Streptomyces viridodiastaticus subsp. "Littus" NRRL-21082N capable of producing antibiotics
This invention relates to antibiotics 31F508α 1 , 31F508α 2 , 31F508β 1 and 31F508β 2 , produced by the microorganism Streptomyces viridodiastaticus subsp. "littus" NRRL-2108211. The...
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5532236 |
[1,2,4]triazolo[4,3-a]quinoxaline compounds
The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R 1 and R 2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which...
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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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5512564 |
Tricyclic thiazole and oxazole derivatives and pharmaceutical agents containing them
The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be...
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5504085 |
Triazolo quinoxalines and their preparation and use
Quinoxaline compounds represented by formulas I or II, ##STR1## wherein R 1 and R 2 are independently hydrogen, C 1 -6 -alkyl, halogen, NO 2 , NH 2 , CN, CF 3 , SO 2 NR 4 R 5 wherein R 4 and...
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5502055 |
Treatment of endotoxic shock with putrescine
The present invention provides a method for protecting a living subject from endotoxic shock. The method involves administering to the subject a pharmaceutical composition including an effective...
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5489590 |
Method of treating with therapeutic composition comprising photoactive compound
A therapeutic composition derived from a pre-activated photoactive compound and a conveyor for destroying tumor or other pathogenic biological contaminants infecting animal body tissues. The...
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5484717 |
Antibiotic 31F508α.sub.1, 31F508α.sub.2, 31F508β.sub.1, 31F508β.sub.2
This invention relates to antibiotic 31F508α 1 , 31F508α 2 , 31F508β 1 and 31F508β 2 , derived from the microorganism Streptomyces viridodiastaticus subsp. "littus" which are useful as an...
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5478823 |
Composition for suppressing infiltration of eosinophils
An agent for suppressing infiltration of eosinophils comprising as an effective ingredient a tricyclic triazolo derivative, which strongly suppresses infiltration of eosinophils into inflammatory...
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5476851 |
Pyrazolo[3,4-g]quinoxaline compounds which inhibit PDGF receptor protein tyrosine kinase
This invention relates to pyrazolo[3,4-g]quinoxaline compounds exhibiting protein tyrosine kinase inhibition activity of the formula: ##STR1## where: ------ may be a double bond; R, R 2 , R 3 ...
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5470846 |
Treatment of neurological and mental disorders
A method of treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in...
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5468748 |
9H-indeno[1,2-b]pyrazine derivatives
The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and...
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5468747 |
Fungicidal compositions and methods of use employing pyrimidine derivatives
Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C 1 -4 alkyl, C 3 -6 cycloalkyl, C 2 -4...
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5462963 |
Chelator compositions comprising α-diamine compounds
The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising...
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5459141 |
Compounds 31668P and 31668U, a process for their production and their use
Compounds 31668P and 31668U, a process for their production and their use. Compound 31668P and compound 31668U with the formulae ##STR1## have an antibiotic and an antitumor action.
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5441956 |
Hydroisoquinoline derivatives
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5441955 |
Indolo[2,1-biquinazoline-6,12-dione antibacterial compounds and methods of use thereof
Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using...
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5438050 |
Indolocarbazole derivatives, processes for their preparation and compositions containing them
New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the...
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5436240 |
Heterocyclic amines having central nervous system activity
Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , and R...
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5433954 |
Method and composition for treating psoriasis, seborrheic dermatitis and eczema
Psoriasis, seborrheic dermatitis and eczema are treated by oral administration of inorganic nickel compound(s), with or without inorganic bromide(s). In an especially preferred embodiment, the...
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5426108 |
Antibiotic 31F508 ALPHA1, ALPHA2, BETA1 and BETA2
This invention relates to antibiotic 31F508α 1 of the formula ##STR1## 31F508α 2 , 31F508β 1 and 31F508β 2 , derived from the microorganism Streptomyces viridodiastaticus subsp. "littus"...
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5405847 |
4,5-dihydro-4-oxo-pyrrolo[1,2-a]quinoxalinones and corresponding aza analogs and a process for their preparation
Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R 1 is C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, hydroxy, C 1 -C 6 -alkoxy,...
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5393756 |
5H-[1,2]benzisothiazolo[2,3-a]quinoline-5-ones and analogs as antiinflammatory agents
The present invention relates to 5H-[1,2]benzisothiazolo[2,3-a]quinoline-5-ones, pharmaceutical compositions thereof and to methods of using these compounds for the treatment of inflammatory...
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5356890 |
S-nitroso derivatives of ace inhibitors and the use thereof
The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically...
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5352680 |
Delta opioid receptor antagonists to block opioid agonist tolerance and dependence
A motion provided to alleviate the tolerance to, or dependence on, an opiate analgesic, by the administration of an effective amount of a selective delta opioid receptor antagonist to a human...
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5350749 |
Pteridine derivatives
4-substituted-pyrido[3,2-d]pyridmidine, -pyrido[4,3-d]pyrimidine, -pyrido[3,4-d]pyrimidine, pyrido[2,3-d]pyrimidine, -pteridine, -pyrimido[4,5-d]pyrimidine, -pyrimido[4,5-c]pyridazine,...
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5308842 |
Tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds
Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase...
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5308845 |
Quinoxaline compounds and their preparation and use
Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R 1 is hydroxy; and R 5 and R 6 together form a fused phenyl, cyclohexyl or pyridyl ring, which is optionally...
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5304559 |
Compositions containing a 4-quinolone derivative complexed with a divalent metal ion
The present invention concerns a fluid pharmaceutical composition intended to be brought into contact with a physiological fluid, characterized in that it contains, as active principle, at least...
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5300505 |
Stable salts of 5,10-methylenetetrahydrofolic acid
Salts of 5,10-methylene-(6R)-, (6R,S)-, and (6S)-tetrahydrofolic acid with sulfuric acid or a sulfonic acid are stable in solid form and can be used as a constituent and/or as a starting material...
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5292732 |
Pyrrolopyrazine derivatives
The novel pyrrolopyrazines of the general formula ##STR1## wherein one of R 1 and R 2 signifies aryl and the other signifies hydrogen, lower alkyl or aryl or R 1 and R 2 together with the two...
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5286727 |
N-methylepiamauromine, epiamauromine and cycloechinulin antiinsectan metabolites
Diketopiperazine compounds designated N-methylepiamauromine, epiamauromine and cycloechinulin have been isolated from the sclerotia of the fungi Aspergillus ochraceus. The compounds are effective...
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5283244 |
Fused pyrazine derivatives
The present invention is a pyrazine derivative which has glutamate receptor antagonizing activity, represented by formula: ##STR1## wherein Z represents C or N, provided that two Zs are not N atoms...
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5276028 |
Imidazoquinoxaline compounds
The heterocyclic compounds having the general formula I ##STR1## wherein R 3 is ##STR2## wherein R' is H, C 1 -6 -alkyl or C 3 -7 -cycloalkyl; --B-- is --C(R")N-- or --NC(R")-- wherein R" is...
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