Abstract: A method of extracting benzo-c-phenanthridine alkaloids from plants of the families Papaveraceae, Fumariaceae, and Berberidaceae, comprising grinding the plant, extracting the ground plant with acidulated methanol or acidulated ethanol, precipitating the extract with an acid salt soluble in the solvent used, redissolving the precipitated salt in water, adding sufficient acid to form a precipitate, and collecting the precipitate so formed.
Abstract: Certain 5-phenyl-5H-indeno[1,2-d]pyrimidines, their pharmaceutical formulations, and their use in methods for inhibiting aromatase and treating or preventing estrogen-dependent diseases.
Type:
Grant
Filed:
March 31, 1986
Date of Patent:
September 6, 1988
Assignee:
Eli Lilly and Company
Inventors:
Kenneth S. Hirsch, C. David Jones, Eriks V. Krumkalns, Donald G. Saunders
Abstract: The process which comprises ##STR1## in which R represents hydrogen, alkoxy, alkylamino or dialkylamino or represents optionally substituted radicals from the series comprising alkyl, cycloalkyl and aryl,R.sup.1 represents optionally substituted radicals from the series comprising alkyl, alkoxy, alkylthio, mono- or dialkylamino and phenyl,R.sup.2 represents optionally substituted alkyl,R.sup.3 represents alkyl, alkoxy or aryl,X represents oxygen or sulphur, andY represents halogen or a grouping --OCOR.sup.3.The intermediates do not have to be isolated. Some are new compounds.
Abstract: The present invention relates to a process for the preparation of vincristine.The process for the semisynthesis of vincristine according to the present invention comprises oxidizing vinblastine or its salts with chromic acid or its salts, in ethyl acetate at a low temperature.
Type:
Grant
Filed:
June 2, 1986
Date of Patent:
August 30, 1988
Assignee:
P. F. Medicament
Inventors:
Roger Tarroux, Jacques Fahy, Philippe Hatinguais
Abstract: Alkoxyalkyl and alkylmercaptoalkyl substituted bridged benzofuroisoquinolines have opioid antagonist, and/or appetite-controlling properties. Preferred compounds are kappa receptor selective antagonists. Examples of such preferred compounds are 5-Methoxymethyl-3-n-propyl- 1,2,3,4,5,6,7,7a-octahydro-4a,7-ethanobenzofuro[3,2-e]isoquinolin-9-ol and 3-Cyclopropylmethyl-5-methoxymethyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano benzofuro[3,2-e]isoquinoline-9-ol.
Abstract: A method for extracting benzo-c-phenanthridine alkaloids from plants of the families Papaveracease Fumariaciae, and Berberidacae, comprising extracting ground plant material with acidulated methanol precipitating the extract with an acid salt which is soluble in methanol, redissolving the precipitated salt in water, adding sufficient acid to form a precipitate, and collecting the precipitate so formed. The benzo-c-phenanthridine alkaloids have valuable properties as antimicrobials as well as in treating mouth odors, gingivitis, and periodontitis.
Abstract: A propionate derivative having the general formula (I): ##STR1## wherein R.sup.1 is phenyl which may be substituted with one or more of the same as different substituents selected from the group consisting of halogen, methyl, methoxy, and nitro, R.sup.2 is alkyl, cycloalkyl, or alkenyl, R.sup.3 is alkylthio, cycloalkylthio, alkenylthio, phenylthio, or benzylthio which may be substituted with halogen or methyl and R.sup.4 is imidazol-1-yl or 1,2,4-triazol-1-yl, or the acid addition salt thereof or the metal complex thereof.This novel propionate derivative is suitable for use as an agricultural fungicide.
Abstract: Pharmacologically active, radioactive, and photoactive vinblastine analogs are provided which can be used to bind covalently to cellular polypeptides which have high affinity for Vinca alkaloids. The compounds are N-(p-azido[3,4-.sup.3 H]benzoyl)-N'beta-aminoethylvindesine and N-p-azido-[3-.sup.125 I]-salicyl-N'-beta-aminoethylvindesine. The compounds can be used to identify cellular Vinca alkaloid receptors which may be involved in antineoplastic, cytotoxic and drug resistant mechanisms of actions. In addition to specific interaction with tubulin, these compounds specifically bind to a 150-180 kDa surface membrane glycoprotein which is overexpressed in multidrug resistant cells.
Type:
Grant
Filed:
April 3, 1986
Date of Patent:
August 23, 1988
Assignee:
The United States of America as represented by the Department of Health and Human Services
Abstract: An agent for treatment and prevention of nephritis comprising at least one imidazoquinazoline compound represented by formula ##STR1## wherein R.sub.1 represents a dialkylamino group having 1 to 6 carbon atoms in each alkyl moiety, or an unsubstituted or substituted cyclic amino group; and R.sub.2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, or an alkoxy group having 1 to 6 carbon atoms, or a salt thereof as an active ingredient.
Abstract: Codeine is prepared by reacting morphine with trimethyl phenyl ammonium chloride in the presence of an alkali metal carbonate and a hydrocarbon solvent at a temperature of from 40.degree. to 120.degree. C. Codeine is recovered from the reaction mixture. Codeine is useful as an analgesic and antitussive drug.
Type:
Grant
Filed:
December 10, 1986
Date of Patent:
August 16, 1988
Assignee:
Council of Scientific & Industrial Research
Inventors:
Nagaraj R. Ayyangar, Anil R. Choudhary, Uttam R. Kalkote, Vasant K. Sharma
Abstract: Novel pyrimido[2,1-b]benzothiazoles of the formula ##STR1## wherein R and R.sub.3 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the carbon to which they are attached form a cycloalkyl of 3 to 6 carbon atoms, R.sub.1 is selected from the group consisting of hydroxy, alkoxy of 1 to 12 carbon atoms, cycloalkyl of 7 to 12 carbon atoms, and ##STR2## R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the nitrogen form piperidino or morpholino, R.sub.
Type:
Grant
Filed:
July 31, 1986
Date of Patent:
August 9, 1988
Assignee:
Roussel Uclaf
Inventors:
David A. Rowlands, Julian M. C. Golec, Saroop S. Matharu, Peter W. Hairsine
Abstract: The aluminum salt of saccharin and a method for its preparation are disclosed. Chewing gum compositions comprising the novel salt are prepared.
Abstract: Alkyl-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the formula ##STR1## in which X.sup.1, X.sup.2 and X.sup.3 each independently is hydrogen, a nitro group, a halogen atom or an alkyl radical with 1 to 3 carbon atoms, with the proviso that at least one of them is an alkyl radical,or pharmaceutically acceptable salts or hydrates thereof, are antibacterially active and promote animal growth.
Type:
Grant
Filed:
November 5, 1985
Date of Patent:
August 9, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Grohe, Michael Schriewer, Hans-Joachim Zeiler, Karl G. Metzger
Abstract: A 13-propylberberine salt, which is represented by the following general formula (I): ##STR1## wherein X.sup.- means HSO.sub.4 or H.sub.2 PO.sub.4, has strong inhibitory effect against secretion, good stability and high water solubility. Its effects are shown promptly after its oral administration.
Abstract: Trifluoromethyl substituted tetracyclic compounds including optical isomers thereof having the formula: ##STR1## wherein n is 1 or 2 and p is 0 or 1, are useful as CNS agents with tranquilizing effects.
Type:
Grant
Filed:
February 13, 1986
Date of Patent:
July 26, 1988
Inventors:
Goetz E. Hardtmann, William J. Houlihan, Rudolf K. A. Giger
Abstract: The invention relates to the use of 3-acylaminobenzisothiazole-S,S-dioxides of the formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl, or C.sub.1 -C.sub.10 alkyl which is substituted by halogen or C.sub.1 -C.sub.5 alkoxy, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, trifluoromethyl, amino or nitro, for controlling insects and representatives of the order Acarina. The invention further relates to novel compounds of the formula I, wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl, or C.sub.1 -C.sub.10 alkyl which is substituted by halogen or C.sub.1 -C.sub.5 alkoxy, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, trifluoromethyl, amino or nitro, with the proviso that R.sub.2, R.sub.3, R.sub.4 and R.sub.
Abstract: Process for preparing yellow shade modification of gamma quinacridone whereby the .gamma..sub.II form is converted to the .gamma..sub.I form (1) by milling in an alcohol and in the presence of a base or (2) by premilling the .gamma..sub.II form to the .gamma..sub.I form and then refluxing or milling the resulting .gamma..sub.I form in an alcohol in the presence of a base, the resulting product being a highly crystalline, bright, yellow shade, ready dispersable .gamma..sub.I quinacridone pigment.
Abstract: A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a long-acting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 23, 1985
Date of Patent:
July 26, 1988
Assignee:
Nova Pharmaceutical Corporation
Inventors:
Waclaw J. Rzeszotarski, Babu J. Mavunkel
Abstract: This invention is for the compound 17.beta.-(N-t-butylcarbamoyl)-4-aza-5.alpha.-androst-1-en-3-one, pharmaceutical compositions containing the compound, methods of inhibiting testosterone 5.alpha.-reductase with the compound and methods of treating hyperandrogenic conditions with the compound, particularly benign prostatic hypertrophy.
Abstract: Process for the preparation of linear quinacridones of the formula (1) ##STR1## in which R denotes a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.3 -alkoxy or phenyl group or a fused benzene ring or a phenylamino or phenoxy group which can be substituted on the aromatic nucleus by fluorine, chlorine or bromine atoms or C.sub.1 -C.sub.4 -alkyl groups, and n denotes a number from 0 to 2, it being possible, in the event that n.noteq.0, for the substituents R present on the same benzene ring or on the two benzene rings to be identical or different, by the oxidation of linear 6,13-dihydroquinacridones of the formula (2) ##STR2## in which R and n have the meanings mentioned above, which comprises heating, at temperatures from about 180.degree. C. to about 280.degree. C., 1 mole of the last-mentioned compounds with 1 to 2 moles of iodine in a high-boiling organic solvent which is inert towards the reactants.