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6143757 |
Chemical compounds
Compounds of the general structural formula ##STR1## and use of the compounds and salts and solvates thereof, as therapeutic agents.
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6136817 |
Opioid receptor antagonist compounds
New morphinane derivatives of the formula ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in the manufacture of pharmaceutical preparations.
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6127355 |
High molecular weight polymer-based prodrugs
The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety; X is an electron withdrawing group; Y and Y' are independently...
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6110933 |
Amino acid derivatives and their use as phospholipase A.sub.2 inhibitor
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6100273 |
Water soluble camptothecin derivatives
The present invention relates to water soluble, camptothecin derivatives of formula (I). ##STR1## wherein A represents a moiety of the formula (IIA), (IIB) or (IIC): ##STR2## X is selected from the...
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6096755 |
N-substituted azabicycloalkane derivatives, their preparation and use
Compounds of the formula I ##STR1## where B, R 1 , R 2 , n, R 3 , A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel compounds are suitable...
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6048867 |
Biologically active rupununines
A method of therapy wherein there is administered to a person in need of such therapy a pharmacologically effective amount of a rupununine having the formula: ##STR1##
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6046209 |
Water soluble camptothecin analogs
The present invention provides water soluble camptothecin analogs of Formula I: ##STR1## which are particularly useful as antineoplastic agents; pharmaceutical compositions thereof; and a method of...
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6030980 |
Agent for the treatment of infections
The present invention relates an agent for the treatment of infections, which comprises as the active ingredient at least one member selected from the group consisting of aconite-alkaloids, aconite...
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6008225 |
Derivatives of antibiotic GE2270 factors C.sub.2a, D.sub.2 and E
Mono- or di-substituted derivatives of GE2270 factors C 2a , D 2 and E of general formula (I), wherein W represents a moiety of formula (a), (b) or (c), R 1 and R 2 representing a variety of...
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6004977 |
N-(pyridinylamino) isoindolines and related compounds
Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing...
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6004969 |
Transdermal delivery of buprenorphine preparations
Buprenorphine is a potent analgesic agent, it has been shown to be as effective as morphine. The main clinical application of buprenorphine is to relief postoperative pains or for patients in the...
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5994327 |
Process for the preparation of morphinans
A process for the preparation of 14-alkoxyindolomorphinans and 14-alkoxybenzofuranomorphinans is disclosed. The process facilitates the preparation of a large variety of 14-alkoxy substituted...
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5990120 |
Hexacyclic camptothecin analogues, and process for preparing them
The present invention relates to novel hexacyclic camptohecin analogues, having a five-membered aza-heterocycle fused to ring (A) of camptothecin at positions 9 and 10. Such compounds possess high...
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5985877 |
Combination of tyrosine kinase inhibitor and chemical castration to treat prostate cancer
A method of treating prostate cancer by co-administering a tyrosine kinase inhibitor such as an indolocarbazole and a chemical castration agent is disclosed. A composition containing a tyrosine...
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5985887 |
Aza-anthracyclinone derivatives
Compounds of formula I ##STR1## wherein X 1 and X 2 are CO, CNH or CH 2 , X 3 is CH 2 , CO, CHOH, ##STR2## wherein n=2 or, 3 or CN(R 9 ) wherein R 9 is hydroxy or amino-aryl, and each...
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5981541 |
Substituted heterocycles as anti-tumor agents
The present invention provides compounds of formula (I): ##STR1## wherein R 1 -R 7 , W, X, Y, and Z have any of the values defined in the specification, and pharmaceutically acceptable salt...
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5981540 |
Heterocycle-condensed morphinoid derivatives
Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders. ##STR1##
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5977077 |
Xanthone analogs for the treatment of infectious diseases
Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also...
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5972952 |
Neuroprotective pharmaceutical composition containing stereoisomers of arylcyclohexylamines
The invention relates to pharmaceutical compositions for neuroprotection containing the compound (1S,2R) 1-[1-(2-thienyl)-2-alkylcyclohexyl]piperidine or (1S,2R)...
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5968824 |
Agents for inducing apoptosis and applications of said agents in therapy
Agents which modulate pathways of apoptotic induction or repression in which products of opioid peptide precursors genes participate, useful as inducers of apoptosis in cells and in tumor cells in...
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5932588 |
Camptothecin compounds with combined topoisomerase I inhibition and DNA alkylation properties
Camptothecin compounds having a --CH 2 --L group are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and DNA of associated topoisomerase I-DNA complexes.
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5908835 |
Anti-tumor compositions containing taxane derivatives
Disclosed are antitumor compositions comprising taxol, taxotere or their derivatives in combination with an anthracycline antibiotic, the combination having a pharmacologic activity greater than...
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5889013 |
Pyrimidine acyclonucleoside derivatives
The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active...
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5886002 |
Use of rifaximin and of pharmaceutical compositions containing it in the treatment of the diarrhoea from cryptosporidiosis
The use of therapeutically effective amounts of rifaxmin and of pharmaceutical compositions containing it in the treatment of the diarrhoeal symptomatology in case of cryptosporidiosis in patients...
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5886001 |
Agonist compounds
New morphinane derivatives of the formula (I) ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in therapy. The variables in the above structure are as...
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5861411 |
4-Acylaminopyridine derivative
A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for...
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5856333 |
Substituted camptothecin derivatives and process for their preparation
The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R 1 , R 2 and R 3 are as defined under (a) or...
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5849731 |
Indole derivatives and medical application thereof
The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present...
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5849750 |
Dynemicin analogs
Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.
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5780479 |
Use of opioid antagonists to treat impulse-control disorders
A method is provided for treating an individual afflicted with an impulse-control disorder by administering thereto an amount of one or more opioid receptor antagonists.
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5776954 |
Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon...
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5776942 |
Bronchodilating pyrido 2,3-d!pyrimidine derivatives
A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido 2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts...
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5770607 |
Aqueous liquid composition for external use
This invention relates to an aqueous liquid composition for external use which contains a tricyclo compound of the chemical formula (I) presented here-under or a pharmaceutically acceptable salt...
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5770605 |
Method for treating leukemia with a hexa-cyclic compound
A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the...
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5770604 |
Aconitine compound and an antipyretic/analgesic/anti-inflammatory agent
This invention provides novel aconitine compounds of the formula (I) or salt thereof ##STR1## wherein, R 1 is a hydrogen atom or hydroxyl group; R 2 is an acetyloxy group; R 3 is an alkyl having...
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5736156 |
Liposomal anf micellular stabilization of camptothecin drugs
The present invention provides water soluble, stable, highly pharmacologically active camptothecin drugs by solubilizing the camptothecin drugs in liposomes composed of lipids or in micelles...
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5728709 |
Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that stimulate platelet production
Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R 1 is lower alkyl or aralkyl; R 2 is hydrogen,...
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5679671 |
Amino acid derivative
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase...
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5672597 |
Acetamide derivative
An acetamide derivative having the general formula (I): ##STR1## or a pharmacologically acceptable salt thereof; a synthetic intermediate of the above-mentioned acetamide derivative; a treating...
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5658920 |
Substituted 1H,12H-benz-[DE]pyrano[3',4':6,7] indolizino[1,2-B]quinoline-10,13(9H,15H)-dione compound
A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the...
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5654312 |
Treatment of inflammatory and/or autoimmune dermatoses with thalidomide alone or in combination with other agents
Methods of treatment for inflammatory and autoimmune dermatoses which comprises topical and/or systemic administration of a therapeutically-effective amount of thalidomide alone or in combination...
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5648359 |
Tumor necrosis factor production inhibitors
There is provided a composition for inhibiting the production or secretion of tumor necrosis factor effective for the treatment of cachexia, septic shock, multiple organ failure, rheumatoid...
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5643915 |
Treatment of ischemia/reperfusion injury with thalidomide alone or in combination with other therapies
In accordance with the present invention, a method is provided for treating reperfusion injury, ischemia and runaway inflammatory conditions with thalidomide alone or in combination with other...
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5641500 |
Use of purinergic receptor agonists as antineoplastic agents
The instant invention is directed to the use of a pharmaceutical composition containing an effective amount of adenosine or an adenosine analog or derivative as an agent useful in the treatment of...
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5639753 |
Insecticidal pteridines and 8-deazapteridines
This invention relates to pteridine and 8-deazapteridine compounds and compositions containing the same which are useful for controlling insects in agricultural crops. These pteridines may be...
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5631263 |
Use of delta opioid receptor antagonists to treat immunoregulatory disorders
A therapeutic method is provided to elevate a depressed mammalian autologous mixed lymphocyte response and to alleviate the diseases associated therewith by the administration of an effective...
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5631264 |
Substituted 6,11-ethano-6,11-dihydrobenzo[B]quinolizinium salts and compositions and methods of use thereof
Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or...
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5622957 |
Benzopyrrolizinoquinolizinones
A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical ##STR2## and R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , R 8 , R 9 and Z are as defined in the...
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5622723 |
Procedure for encapsulating chlorpheniramine
An improvement in the process of coacervation of chlorpheniramine maleate is provided whereby a predetermined amount of chlorpheniramine maleate charged to the process is maintained in the...
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