Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/349)
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Patent number: 4777270Abstract: A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.Type: GrantFiled: September 4, 1986Date of Patent: October 11, 1988Assignee: Pfizer Inc.Inventor: Frank J. Urban
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Patent number: 4745198Abstract: The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.Type: GrantFiled: November 12, 1985Date of Patent: May 17, 1988Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, Peter W. R. Caulkett
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Patent number: 4581166Abstract: A process is proposed for the isolation and purification of antibiotics wherein an antibiotic containing solution is extracted with an extraction agent at a temperature of from 0.degree. to 40.degree. C. and at a pressure which lies between the critical pressure and the ten-fold value of the critical pressure of the extraction agent, with the weight ratio of antibiotic containing solution to the extraction agent being 1:5 to 1:20, wherein the antibiotics are precipitated from the antibiotic containing extraction agent by reducing its density and wherein the extraction agent is recirculated. An entrainer may be added to the extraction agent. The reduction in density of the antibiotic containing extraction agent may be effected by expansion to a pressure of from 30 to 70 bar.Type: GrantFiled: May 11, 1984Date of Patent: April 8, 1986Assignee: Fried. Krupp Gesellschaft mit beschrankter HaftungInventors: Siegfried Peter, Hubert Coenen, Rainer Hagen
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Patent number: 4554363Abstract: Process for the preparation of bicyclic ketones containing blocked hydroxy groups, of general Formula I ##STR1## wherein R.sub.1 is the residues --CH.sub.2 OR.sub.2 wherein R.sub.2 means benzyl, dimethyl-tert-butylsilyl, diphenyl-tert-butylsilyl, dimethylphenylsilyl, tribenzylsilyl, or tetrahydropyranyl, ##STR2## with R.sub.2 having the meanings given above, R.sub.4 meaning hydrogen or methyl, and R.sub.5 meaning a straight-chain or branched-chain, saturated or unsaturated alkyl residue which can contain fluorine, chlorine, 1,2-methylene, 1,1-trimethylene, or methoxy substitutents, or a CH.sub.2 --X-Aryl residue with X meaning CH.sub.2 or O and Aryl meaning phenyl or a heterocyclic residue, which residues can be substituted by methyl, methoxy, fluorine, chlorine, bromine, or trifluoromethyl, or ##STR3## with the meanings for R.sub.2, R.sub.4, and R.sub.5 as indicated above, and R.sub.3 having the meanings set forth for R.sub.2, it being possible for R.sub.3 to be identical to R.sub.2 or different from R.sub.Type: GrantFiled: June 23, 1983Date of Patent: November 19, 1985Assignee: Schering AktiengesellschaftInventor: Helmut Vorbrueggen
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Patent number: 4521607Abstract: New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, halogen, lower alkyl, hydroxyl, lower alkyloxy or aralkyloxy, or R.sup.1 and R.sup.2 jointly represent lower alkylenedioxy; R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl or --CH.sub.2 SR.sup.7 (R.sup.7 represents hydrogen or acyl); R.sup.6 represents hydrogen or acyl, or R.sup.6 and R.sup.7 jointly represent a single bond; X represents --CH.sub.2 --, --O-- or >N--R.sup.8 (R.sup.8 represents hydrogen, acyl or lower alkyl); and n represents 2, 3 or 4, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.Type: GrantFiled: April 2, 1982Date of Patent: June 4, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshikazu Oka, Kohei Nishikawa, Akio Miyake
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Patent number: 4503062Abstract: This invention relates to novel alicyclic alcohol compounds of the formula ##STR1## wherein Az is imidazole or 1,2,4-triazole, R.sup.6 is optionally substituted phenyl and A is an alicyclic ring optionally benzo-fused, which compounds possess pharmaceutical, veterinary, agricultural and horticultural antifungal properties; together with a process for their manufacture, compositions containing them, and a method of combatting plant fungal diseases.Type: GrantFiled: March 28, 1983Date of Patent: March 5, 1985Assignee: Imperial Chemical Industries PLCInventor: Michael B. Gravestock
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Patent number: 4459306Abstract: This invention relates to novel tricyclic ethers, pharmaceutically acceptable addition salts and optical isomers therefrom. The compounds described herein are useful as psychotropic agents in the treatment of depression and anxiety. Also included herein are methods of preparing said compounds, pharmaceutical compositions including them and methods of treating human or animal beings by administering these pharmaceutical compositions.Type: GrantFiled: April 6, 1981Date of Patent: July 10, 1984Assignee: Science Union et CieInventors: Charles Malen, Jean-Claude Poignant
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Patent number: 4447541Abstract: A reagent mixture is admixed with soil to first desorb and then hydrolyze and thereby increase the biodegradability of a toxic or otherwise hazardous polyhalogenated organic compound with which the soil is contaminated. Essential constituents of the reagent mixture are: (1) an alkali metal hydroxide, an alkali metal hydroxide/alcohol or alkali metal hyroxide/glycol mixture, or an alkoxide; and (2) a sulfoxide catalyst. The hydrolyzed compounds can be biologically degraded into compounds which pose little if any hazard to the environment or its inhabitants by naturally occurring or artifically introduced Pseudomonas sp. and other microorganisms with adjustment of soil pH (and perhaps orther parameters) to provide a viable environment for the bacteria being carried out after the chemical treatment if inoculation with bacterial cultures is employed.Type: GrantFiled: June 6, 1983Date of Patent: May 8, 1984Assignee: Galson Research CorporationInventor: Robert L. Peterson
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Patent number: 4433051Abstract: There are provided novel labelled derivatives, namely .alpha.-difluoromethylornithine tagged with rhodamine or with biotin. These are of value in analysis and in the cytochemical localization of enzymes.Type: GrantFiled: October 14, 1981Date of Patent: February 21, 1984Assignee: Yeda Research and Development Co., Ltd.Inventors: Gad Gilad, Varda Gilad, Meir Wilchek
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Patent number: 4431808Abstract: A technique is described for the preparation of a wide variety of basic derivatives of linearly condensed tricyclic systems formed by two external benzene nuclei and a 7-membered central ring having 2 chalcogen atoms as hetero atoms.Derivatives of 11H-dibenzo(b,e)-1,4-dioxepin are obtained when the chalcogens are both oxygen atoms; derivatives of 11H-dibenzo(b,f)-1,4-dithiepin are obtained when the chalcogens are both sulfur atoms; derivatives of 6H-dibenz(b,e)-1,4-oxathiepin and 11H-dibenz(b,f)-1,4-oxathiepin are obtained with combinations of sulfur and oxygen atoms as chalcogens.Type: GrantFiled: March 9, 1982Date of Patent: February 14, 1984Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Miroslav Protiva, Karel Sindelar, Antonin Dlabac, Jirina Metysova
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Patent number: 4421923Abstract: There is provided a new class of crown ethers characterized by an --OH functional group attached to a carbon atom in the heterocyclic ether ring portion and derivatives thereof. A novel process for making such crown ethers is also provided which is characterized by reacting a bisphenol ether with an epihalohydrin to effect ring closure and provide the appendant --OH group.These products are especially useful as complexing agents.Type: GrantFiled: December 12, 1980Date of Patent: December 20, 1983Assignee: PCR Research Chemicals, Inc.Inventor: Richard A. Bartsch
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Patent number: 4377518Abstract: Dyestuffs of the formulaD--N.dbd.N--A Iin whichD represents the radical of a diazo component andA represents the radical of a coupling component of the formulae ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 designate hydrogen or non-ionic radicals,R designates hydrogen or an optionally substituted alkyl, cycloalkyl, aryl, aralkyl or heterocyclic radical,X designates OH or ##STR2## T designates the remaining members of a fused-on ring and Y and Z designate hydrogen, optionally substituted alkyl or optionally substituted aryl,processes for their preparation and process for pigmenting organic material using the dyestuffs of the formula I.Type: GrantFiled: September 3, 1980Date of Patent: March 22, 1983Assignee: Bayer AktiengesellschaftInventors: Dieter vor der Bruck, Hans-Joachim Kabbe
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Patent number: 4347254Abstract: A compound of the formula: ##STR1## wherein A.sub.1 is a single bond or a C.sub.1 -C.sub.5 alkylene group bonding at the 2-, 2'- or 3-position, A.sub.2 is a C.sub.1 -C.sub.3 alkylene group, A.sub.3 is a C.sub.1 -C.sub.4 alkylene group, X is --O-- or --SO.sub.n -- and B is a carboxy group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a cyano group, an amino group of the formula: ##STR2## or a carbamoyl group of the formula: ##STR3## which is useful as an antiviral agent with no side effect.Type: GrantFiled: July 22, 1980Date of Patent: August 31, 1982Assignee: Sumitomo Chemical Company, LimitedInventors: Junki Katsube, Hiromi Shimomura, Shun Inokuma, Akihiko Sugie
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Patent number: 4343742Abstract: 2,3-Perfluoro-1,4-dioxanes of the formula I ##STR1## wherein X and Y independently from one another mean F or CF.sub.3, are manufactured by reacting carbonyl compounds of the formula II ##STR2## wherein X has the same meaning as in formula I,Y' has the same meaning as Y in formula I (F, CF.sub.3), and additionally can be Cl andZ=Cl, mesylate [=OSO.sub.2 CH.sub.3 ] or tosylate=[OSO.sub.2 C.sub.4 H.sub.6 --CH.sub.3 (p)],with alkali metal fluorides and/or with ammonium fluoride. The reaction products I, among which those wherein at least one of both radicals X and Y is CF.sub.3 are novel compounds, are solvents for highly fluorinated compounds and intermediates in various application fields.Type: GrantFiled: January 14, 1981Date of Patent: August 10, 1982Assignee: Hoechst AktiengesellschaftInventors: Herbert Muffler, Gunter Siegemund, Werner Schwertfeger
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Patent number: 4335122Abstract: The invention relates to diuretic dihydro-dibenzoxepines-thiepines and -morphanthridones of the formula ##STR1## wherein R is ##STR2## where R.sup.4 is a hydrogen or an alkyl; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen, alkyl or R.sup.2 and R.sup.3 are fused to form a pyrrolidino, morpholino, piperidino or azepino ring substituent; Y is hydrogen, halogen and alkoxy, X is ##STR3## where R.sup.4 is as defined above; m is an integer of 0 or 1; and n is an integer of 2 or 3; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: March 18, 1981Date of Patent: June 15, 1982Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Arthur R. McFadden, Daniel E. Aultz
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Patent number: 4328168Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of a cyclic polyether compound and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.Type: GrantFiled: October 27, 1980Date of Patent: May 4, 1982Assignee: Emery Industries, Inc.Inventor: Richard G. Fayter, Jr.