Patents Examined by Dara Dinner
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Patent number: 4697022Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: May 21, 1984Date of Patent: September 29, 1987Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert
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Patent number: 4687844Abstract: A process for the direct preparation of N,N-di-substituted derivatives of 4,13-diaza-18-crown-6 in which the substituents on both nitrogen atoms are identical and derive originally from an amine, by reacting a 1,8-diiodo-3,6-dioxooctane or derivatives thereof in which the substituents are located on positions 1, 2, 4, 5, 7 or 8 or combinations thereof, with a molar equivalent of a primary amine in the presence of a base and solvent.Type: GrantFiled: April 11, 1986Date of Patent: August 18, 1987Assignee: University of MarylandInventors: George W. Gokel, Vincent J. Gatto
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Patent number: 4666937Abstract: There are disclosed novel compounds which are derived from 22,23-dihydro avermectin Bla aglycone, 13-deoxy-22,23 dihydro overmectin Bla aglycone and 13-deoxy-22,23-dihydro overmectin Blb aglycone. The six compounds are hydroxy adducts of the substrate avermectin compound at the 12a, 24, 24a, 26, 26a and 27 positions. The hydroxy adducts are prepared by incubating the substrate with the microorganism Cunninghamella blakesleeana and isolating the hydroxy adducts from the fermentation broth. The compounds are highly potent antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: February 20, 1986Date of Patent: May 19, 1987Assignee: Merck & Co., Inc.Inventors: Robert T. Goegelman, Edward S. Inamine, Raymond F. White
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Patent number: 4659843Abstract: The invention relates to a process for preparing 3-methyl-2-butene-4-olide by the codimerization of methylenecyclopropane with carbon dioxide (CO.sub.2) in the presence of organic complex compounds of transistion metals, which process is characterized in that the codimerization is carried out at a temperature of 100.degree. C. to 200.degree. C. in the presence of palladium(O) compounds which are stable in the reaction mixture up to 200.degree. C. and with CO.sub.2 under a pressure of 10 to 110 bar, optionally in the presence of a solvent.Type: GrantFiled: February 1, 1985Date of Patent: April 21, 1987Assignee: Studiengesellschaft Kohle mbHInventors: Paul Binger, Hans-Joachim Weintz
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Patent number: 4604471Abstract: Furan-3-carbohydroxamates of the formula ##STR1## where R.sup.1 is alkyl, unsubstituted or substituted cycloalkyl or unsubstituted or substituted phenyl, R.sup.2 is methyl or ethyl, R.sup.3 and R.sup.4 independently of one another are each hydrogen, bromine, chlorine, unsubstituted or substituted alkyl, or --CH.sub.2 --COOR.sup.5, where R.sup.5 is unsubstituted or substituted alkyl, and Me is divalent nickel or cobalt, stabilize plastics against the action of light, oxygen and heat. The compounds (I) have only slight intrinsic color.Type: GrantFiled: November 21, 1984Date of Patent: August 5, 1986Assignee: BASF AktiengesellschaftInventors: Peter Neumann, Michael Thomas, Stefan Weiss, Hubert Trauth
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Patent number: 4604472Abstract: Compounds of formula (I): ##STR1## [wherein X represents a hydrogen atom or a 2-methylbutyryl group, Y represents a hydrogen atom or a methyl group and R.sup.1 and R.sup.2 are the same or different and each represents an oxygen atom or a group of formula .dbd.N--OR.sup.3 (wherein R.sup.3 represents a hydrogen atom or an alkyl group)], the free hydroxy-carboxylic acids corresponding thereto and salts and esters of said acids may be prepared by oxidizing and, if necessary, oximating a corresponding ML-236A, ML-236B, MB-530A or MB-530B compound, and these compounds have valuable antihypercholesteraemic activity.Type: GrantFiled: July 9, 1985Date of Patent: August 5, 1986Assignee: Sankyo Company LimitedInventors: Junya Ide, Shigeki Muramatsu, Yoshio Tsujita, Masao Kuroda
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Patent number: 4598089Abstract: Novel compounds of the formula ##STR1## wherein A signifies the group ##STR2## or --(CH.sub.2).sub.5 --, which inhibit pancreas lipase and can be used for the control or prevention of obesity and hyperlipaemia, are disclosed. The inventive compounds can be produced by the cultivation of microorganism Streptomyces toxytricini, identified as NRRL 15443.Type: GrantFiled: June 18, 1984Date of Patent: July 1, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hadvary, Erich Hochuli, Ernst Kupfer, Hans Lengsfeld, Ernst K. Weibel
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Patent number: 4596801Abstract: Novel 4H-3,1-benzoxazine derivative of the formula: ##STR1## wherein X and Y each independently represent a halogen atom of a lower alkyl group; m and n each independently represent an integer of 0 to 2, and when m or n is 2, the plurality or each of X or Y may have the same or different meanings; R is a hydrogen atom, an alkyloxy group, an alkynyloxy group, an alkylthio group or an alkenylthio group, and a process for their production are provided. The compounds are highly effective against pathogenic fungi while being well tolerated by cultivated plants.Type: GrantFiled: March 13, 1984Date of Patent: June 24, 1986Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Sugiyama, Keizo Hosoda, Yoshikazu Kumagai, Masaki Takeuchi, Masanori Okada
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Patent number: 4596799Abstract: Disclosed are the novel compounds of formula I ##STR1## wherein ring A is unsubstituted or substituted by one or two identical or different substituents selected from lower alkyl, halogen, trifluoromethyl, lower alkoxy, hydroxy and acyloxy; or ring A is substituted on adjacent carbon atoms by lower alkylenedioxy; R represents hydrogen, halogen or lower alkyl; and Ar represents carbocyclic aryl or heteroaryl;which are useful as benzodiazepine receptor agonists, processes for preparing the same, pharmaceutical compositions comprising said compounds and methods of treating nervous system disorders, such as anxiety and epilepsy, by administration of said compounds and pharmaceutical compositions to mammals.Type: GrantFiled: January 29, 1985Date of Patent: June 24, 1986Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4594430Abstract: Geminal dinitro compounds are prepared by reacting an organic nitro compound having a replaceable hydrogen on the carbon to which the nitro group is attached with a source of nitrite ions in the presence of an oxidizing agent and a catalytic amount of an alkali metal ferricyanide.Type: GrantFiled: January 31, 1985Date of Patent: June 10, 1986Assignee: United States of America as represented by the Secretary of the Air ForceInventors: Vytautas Grakauskas, Lee C. Garver, Kurt Baum
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Patent number: 4594428Abstract: The present invention concerns compound useful as intermediates in the preparation of heterocyclic phenoxy amines of the formula ##STR1## wherein Y is hydroxyl or chlorine and R is 1-cyclohexenylmethyl.Type: GrantFiled: January 7, 1983Date of Patent: June 10, 1986Assignee: Societe d'Etudes Scientifiques et Industrielles de L'ile-de-FranceInventors: Michel L. Thominet, Jacqueline F. Franceschini
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Patent number: 4584314Abstract: The compound of formula I ##STR1## wherein R.sub.2 is methyl, ethyl, isopropyl or sec-butyl, can be prepared by selective chlorination of an appropriate milbemycin derivative either with hypochlorous acid (HOCl) or sulfuryl chloride (SO.sub.2 Cl.sub.2) in the temperature range from -10.degree. to +60.degree. C. It is employed as pesticide for controlling Arthropode species such as injurious insects or ecto- or endoparasites of animals, and is applied in the form of compositions. This compound is also used as intermediate for obtaining further milbemycin derivatives.Type: GrantFiled: November 16, 1984Date of Patent: April 22, 1986Assignee: Ciba-Geigy CorporationInventor: Urs Burckhardt