Plural Hetero Rings Patents (Class 549/435)
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Patent number: 4933351Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: January 30, 1989Date of Patent: June 12, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
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Patent number: 4916241Abstract: This invention relates to 4-substituted-5-hydroxy-2(5H)-furanones, to the process for their preparation, to pharmaceutical compositions containing said 4-substituted-5-hydroxy-2(5H)-furanones and to the use of said 4-substituted-5-hydroxy-2(5H)-furanones for modifying the balance between bone production and bone resorption in a host animal, including man.Type: GrantFiled: June 6, 1988Date of Patent: April 10, 1990Assignee: American Home Products CorporationInventors: Marshall A. Hayward, Joseph P. Sabatucci, Ivo L. Jirkovsky, Yvon Lefebvre
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Patent number: 4912131Abstract: 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.Type: GrantFiled: October 11, 1988Date of Patent: March 27, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Julian Adams, Yvan Guindon
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Patent number: 4910313Abstract: The present invention is related to new diselenobis benzoic acid amides of primary heterocyclic amines of the general formula I ##STR1## process for producing the same and process for treating certain diseases in human beings by administration of the same to the humans suffering from such diseases.Type: GrantFiled: August 6, 1987Date of Patent: March 20, 1990Assignee: Nattermann & CIE GmbHInventors: Andre Welter, Axel Roemer, Sigurd Leyck, Michael J. Parnham
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Patent number: 4897109Abstract: A composition for protecting culture plants from the phytotoxic action of herbicidally active chloracetanilides contains as active ingredient an acylamine derivative of the formula I ##STR1## wherein X is oxygen, sulfur, --SO-- or --SO.sub.2 --,Q is an alkyl, alkenyl, alkinyl group, which may be interupted by oxygen, sulfur, sulfinyl or sulfonyul, or a test 1,3-dioxolan-2-yl-alkyl, 1,3-dioxolan-4-alkyl, 2,2-dialkyl-1,3-dioxolan-4-ylalkyl, 1,3-dioxan-2-ylalkyl, 2-benzopyranylalkyl, alkoxycarbonyl alkenyl-oxycarbonyl or tetrahydrofurylalkyl, or the groupOX represents also a halogenoalkyl radical,n is 1, 2 or 3,Z is hydrogen, halogen, alkyl or dioxymethylene,A is a C.sub.1 -C.sub.8 -hydrocarbon radical which may be staight-chained, branched or cyclic and which is unsubstituted or substituted by alkoxy, alkylthio, cyano or halogen,B is hydrogen, a C.sub.1 -C.sub.Type: GrantFiled: October 5, 1987Date of Patent: January 30, 1990Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4885368Abstract: Novel radical ion salts of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another are each hydrogen, methyl, ethyl, phenyl, methoxy, ethoxy, fluorine, chlorine or bromine, or R.sup.1 or R.sup.1 and R.sup.3 may furthermore be tert-butyl and/or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 together may in each case form a radical of the formula ##STR2## where z is 0, 1, 2 or 3, and the fused aromatic rings are unsubstituted or monosubstituted or disubstituted by chlorine, bromine, methyl and/or methoxy, M.sup.m.sym. is an m-valent alkali metal, alkaline earth metal, transition metal, tin, lead, thallium, ammonium, phosphonium, arsonium or stibonium ion, k is from 1 to 5, l is from 0.1 to 4, m is from 1 to 3, n is from 0.1 to 4, x is from 0 to 2 and y is from 0 to 6, and k, l, n, x and y may furthermore be non-integral numbers and (l+x)=n.m, are electrically conductive in the crystalline state. A number of the salts are stable at 300.degree. C. and above.Type: GrantFiled: November 23, 1987Date of Patent: December 5, 1989Assignee: BASF AktiengesellschaftInventors: Siegfried Huenig, Alexander Aumueller, Peter Erk
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Patent number: 4876270Abstract: Novel substituted .alpha.,.alpha.-diphenylethylene derivatives of formula I ##STR1## in which R.sub.1 and R.sub.4 independently of one another each represents hydrogen, hydroxy, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.3 -alkoxy substituted by from 1 to 7 halogen atoms, alkoxyalkoxy having a total of from 2 to 6 carbon atoms, C.sub.3 -C.sub.5 -alkenyloxy or C.sub.3 -C.sub.5 -alkynyloxy;R.sub.2 and R.sub.3 independently of one another each represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.5 -alkoxy or nitro; orR.sub.1 and R.sub.2 together represent a radical --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O--;R.sub.5 and R.sub.6 independently of one another each represents hydrogen, halogen or methyl;R.sub.7 and R.sub.Type: GrantFiled: February 10, 1988Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Rudolf Waespe
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Patent number: 4868207Abstract: Bis(methylenedioxy)biphenyl compounds represented by the formula ##STR1## wherein R is an alkyl group having 1 to 6 carbon atoms or a phenyl group, and R' is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, are disclosed. These compounds are useful as therapeutic agents for liver diseases.Type: GrantFiled: July 28, 1988Date of Patent: September 19, 1989Assignees: Taisho Pharmaceutical Co., Ltd., The Institute of Material Mederia Medica of Chinese Academy of Medical SciencesInventor: Gu Shi-jie
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Patent number: 4806604Abstract: The present invention discloses a new class of calcium chelating compounds which have a decreased affinity for calcium following illumination. These new compounds contain a photolabile nitrobenzyl derivative coupled to a tetracarboxylate Ca.sup.2+ chelating parent compound having the octacoordinate chelating groups characteristic of EGTA or BAPTA. However unlike EGTA or BAPTA-like compounds, in which the two halves of the chelator are linked by a simple 1,2-ethanediyl moiety, the compounds of the present invention modify the stereochemical conformation of this linkage by adding bulky substituents or incorporating the linkage into a carbocyclic or heterocyclic ring. In a first form, the new compounds are comprised of a BAPTA-like chelator coupled to a single 2-nitrobenzyl derivative, which in turn is a photochemical precursor of a 2-nitrosobenzophenone.Type: GrantFiled: May 13, 1987Date of Patent: February 21, 1989Assignee: Regents of the University of CaliforniaInventors: Roger Yonchien Tsien, Stephen R. Adams
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Patent number: 4800228Abstract: 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.Type: GrantFiled: June 18, 1987Date of Patent: January 24, 1989Assignee: Merck Frosst Canada, Inc.Inventors: Julian Adams, Yvan Guindon
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Patent number: 4792635Abstract: Symmetric benzophenones substituted by groups containing fluorine are prepared by reacting aromatic compounds substituted by groups containing fluorine with formaldehyde and/or a formaldehyde derivative, with the addition of hydrogen fluoride, fluorosulphonic acid and/or sulphuric acid, to give the corresponding diphenylmethanes and oxidizing these. The symmetric benzophenones substituted by groups containing fluorine are used for the preparation of polyether ketones by reacting them with diols. New symmetric benzophenones substituted by groups containing fluorine are also disclosed.Type: GrantFiled: March 19, 1985Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Albrecht Marhold, Erich Klauke, Ernst Kysela
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Patent number: 4778805Abstract: 4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention.Type: GrantFiled: June 18, 1987Date of Patent: October 18, 1988Assignee: Merck Frosst CanadaInventors: Julian Adams, Yvan Guindon, Patrice C. Belanger, Michel L. Belley, Joshua Rokach
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Patent number: 4774343Abstract: An active antioxydant containing a compound shown by structural formula ##STR1## is produced by applying an acid catalyst to sesamolin substantially in the absence of active hydrogen compounds.Type: GrantFiled: March 30, 1987Date of Patent: September 27, 1988Assignee: Takemoto Yushi Kabushiki KaishaInventors: Mitsuo Namiki, Toshihiko Osawa, Minoru Isobe, Yasuko Fukuda
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Patent number: 4761491Abstract: 2-Substituted-1,3-dioxacycloalkanes (also known as acetonides) (such as ##STR1## (4-hydroxy-2,2-dimethyl-1,3-benzodioxole)) are prepared by reacting a diol (such as 1,2,3-trihydroxybenzene) and a diunsaturated ether (such as diisopropenyl ether). The reaction is exothermic and produces a ketone as the only by-product. The invention has utility in hydroxyl moiety "protection" and in pesticide synthesis.Type: GrantFiled: October 20, 1986Date of Patent: August 2, 1988Assignee: The Dow Chemical CompanyInventor: Robert H. Heistand, II
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4714710Abstract: There are described new compounds of general formula I ##STR1## in which R.sub.1 is aryl or aryl substituted by C.sub.1-4 -alkyl, halo-C.sub.1-4 -alkyl, phenyl-C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.2-4 -alkynyl, halo-C.sub.2-4 -alkynyl, phenyl-C.sub.2-4 -alkynyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, alkylsulphonyloxy, haloalkylsulphonyloxy, arylsulphonyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, halo, cyano, nitro, aryloxy, haloaryloxy, C.sub.1-4 -alkylaryloxy, or nitro-C.sub.1-4 -alkylaryloxy,R.sub.2 and R.sub.3 are the same or different and are hydrogen, fluorine, cyano or ethynyl,R.sub.4 is phenyl or pyridyl or these groups substituted by one or more of C.sub.1-6 -alkyl, halo-C.sub.1-6 -alkyl, phenyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkyl interrupted by an O--, N-- or S-- atom, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.1-4 -alkoxy, halo-C.sub.Type: GrantFiled: September 9, 1986Date of Patent: December 22, 1987Assignee: Schering AktiengesellschaftInventors: Heinrich Franke, Hartmut Joppien, Helga Franke
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Patent number: 4708820Abstract: Phenol-type natural antioxidative materials containing analogs of sesamin or sesamolin are manufactured by processing a processed sesame speed product with an acid catalyst and subsequently condensing and separating the desired materials by a physical means such as extraction, distillation and adsorption.Type: GrantFiled: November 27, 1985Date of Patent: November 24, 1987Assignee: Takemoto Yushi Kabushiki KaishaInventors: Mitsuo Namiki, Toshihiko Osawa, Yasuko Fukuda, Tatsuhiko Ozaki
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Patent number: 4663347Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: April 19, 1985Date of Patent: May 5, 1987Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
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Patent number: 4658033Abstract: New interphenylene prostaglandin (PGH) analogs are prepared by a method which involves reacting a bicyclic olefin, an acetylene compound and a benzylic halide together, in the presence of a palladium(O) catalyst in a single-step synthesis. By this technique a large number of new interphenylene PGH analogs can be prepared, which are useful as inhibitors of arachidonic acid induced platelet aggregation.Type: GrantFiled: September 23, 1985Date of Patent: April 14, 1987Assignee: Iowa State University Research Foundation, Inc.Inventor: Richard C. Larock
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Patent number: 4649206Abstract: This invention relates to a lignan compound having antioxidative characteristics, an antioxidant having this lignan compound as active component, and antioxidants having as active component a product which contains this lignan compound and is obtained by causing .beta.-glucosidase to react with crushed sesame seeds or a solvent extract thereof.Type: GrantFiled: September 3, 1985Date of Patent: March 10, 1987Assignee: Takemoto Yushi Kabushiki KaishaInventors: Mitsuo Namiki, Toshihiko Osawa, Yasuko Fukuda, Tatsuhiko Ozaki
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Patent number: 4643849Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compounds, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: November 14, 1983Date of Patent: February 17, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanagi, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
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Patent number: 4634701Abstract: Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.Type: GrantFiled: May 28, 1985Date of Patent: January 6, 1987Assignee: Ausonia Farmaceutici s.r.l.Inventor: Leonardo De Vincentiis
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Patent number: 4619943Abstract: Novel phenylpropanoid neolignans isolated from Saururus cernuus L and synthetic or semi-synthetic analogs thereof having neuroleptic, insecticidal, or nematicidal activity are disclosed.Type: GrantFiled: September 10, 1984Date of Patent: October 28, 1986Inventor: Koppaka V. Rao
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Patent number: 4617392Abstract: 4-Alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are prepared from 2,3-methylenedioxyacetophenones. The 4-alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are active as cardiotonic agents.Type: GrantFiled: September 29, 1983Date of Patent: October 14, 1986Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Stanley C. Bell, Donald W. Combs, Robert Falotico
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Patent number: 4616035Abstract: Combating pests such as insects, arachnids and nematodes with novel N-oxalyl-N-methylcarbamic acid esters of the formula ##STR1## in which R represents alkyl, alkenyl, alkinyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenalkylthio, halogen, nitro, dialkylamino, alkylsulphinyl, alkylsulphonyl, cycloalkyl or a saturated, optionally substituted heterocyclic radical with one or more hetero-atoms from the group comprising O, S and N, or forms a ring which is fused onto the phenyl radical, optionally contains one or more hetero-atoms from the group comprising O, S and N and is optionally substituted.Type: GrantFiled: October 15, 1984Date of Patent: October 7, 1986Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Bernhard Homeyer
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Patent number: 4612313Abstract: The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.Type: GrantFiled: September 10, 1985Date of Patent: September 16, 1986Assignee: Boehringer Mannheim GmbHInventors: Herbert Leinert, Wolfgang Kampe, Klaus Strein, Bernd Muller-Beckmann, Wolfgang Bartsch
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Patent number: 4609397Abstract: Pyrazole sulfonylureas are useful as pre- and post-emergence herbicides. Typical of this group is 3-[[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]aminosulfonylmethyl]-1,5-di methyl-1H-pyrazole-4-carboxylic acid, ethyl ester.Type: GrantFiled: December 11, 1984Date of Patent: September 2, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Barry A. Wexler
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Patent number: 4607026Abstract: This invention relates to stereoisomeric forms and mixtures thereof of compounds of the formula ##STR1## having insecticidal, nematocidal, and acaricidal properties.Type: GrantFiled: September 29, 1982Date of Patent: August 19, 1986Assignee: Roussel UclafInventors: Jean Tessier, Andre Teche
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Patent number: 4602033Abstract: Aryl N-oxalyl-N-methyl-carbamates of the general formula ##STR1## in which X represents an alkoxy, alkenoxy, alkinoxy, aryloxy, alkylthio, alkenylthio, alkinylthio or arylthio radical, each of which may be optionally substituted or represents a radical of the general formula --N R.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl or aryl radical, each of which may be optionally substituted, or the radicals R.sup.3 and R.sup.4, together with the N atom to which they are bonded, form an optionally substituted heterocyclic ring, andR.sup.1 represents an aryl radical which is optionally substituted,are novel and find use as pesticides, especially for combating insects, acarids and nematodes.Type: GrantFiled: January 3, 1985Date of Patent: July 22, 1986Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Wolfgang Behrenz, Ingeborg Hammann, Bernhard Homeyer
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Patent number: 4600709Abstract: The invention relates to novel benzodioxole derivatives of the general formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aliphatic, aromatic or heteroaromatic radical,alk represents an alkylene, alkenylene or alkylidene radical having a maximum of 5 carbon atoms,n.sub.1 represents 0, 1 or 2n.sub.2 represents 0 or 1,R.sub.2, R.sub.3 and R.sub.4 each represents, independently of the others, hydrogen, lower alkyl, lower alkoxy or halogen, andA represents the radical --O--R.sub.5, wherein R.sub.5 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.6 and R.sub.7 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.6 and R.sub.Type: GrantFiled: December 7, 1984Date of Patent: July 15, 1986Assignee: Ciba-Geigy AGInventors: Marc E. Ballenegger, Paul Zbinden
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Patent number: 4595693Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.Type: GrantFiled: June 4, 1984Date of Patent: June 17, 1986Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Thomas W. Doebber, San-Bao Hwang, Thomas R. Beattie, Tsung-Ying Shen, Robert Stevenson
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Patent number: 4570005Abstract: 2-Arylpropyl ether or thioether derivatives represented by the following general formula [I]: ##STR1## wherein Ar stands for an aryl group, R stands for a methyl or ethyl group, Y stands for an oxygen or sulfur atom, and B stands for a group represented by the following formula [II]: ##STR2## or the following general formula [III]: ##STR3## wherein Z stands for an oxygen or sulfur atom or a carbonyl or methylene group, R.sup.1 stands for a hydrogen or halogen atom or a lower alkyl group or a lower alkoxy group, and n is an integer of from 1 to 5 with the proviso that when n is 2 or more, the groups R.sup.1 may be the same or different,are produced by reacting a compound represented by the following formula (V): ##STR4## with a compound represented by the following formula (VI):B--CH.sub.2 --D (VI)wherein Ar, R and B are defined above, A is a halogen atom and D is Y--H in which Y is as defined above,in the presence of a base in dimethylsulfoxide or sulfolane.Type: GrantFiled: July 14, 1983Date of Patent: February 11, 1986Assignee: Mitsuitoatsu Chemicals Inc.Inventors: Kiyoshi Nakatani, Satoshi Numata, Tsuneo Inoue, Kenji Kodaka, Tsutomu Ishii, Teruhiko Toyama, Hajime Tachibana, Takatoshi Udagawa, Masatoshi Gohbara
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Patent number: 4549030Abstract: The present invention provides a novel process for preparing known prostaglandins, particularly 9-deoxo-9-methylene-16,16-dimethyl-PGE.sub.2. This well known and useful prostaglandin is prepared from D-glucose through a series of efficient reactions. Also provided are novel intermediates which are useful for preparation of a wide variety of prostaglandins.Type: GrantFiled: October 31, 1983Date of Patent: October 22, 1985Assignee: The Upjohn CompanyInventor: Bruce A. Pearlman
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Patent number: 4540690Abstract: 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.Type: GrantFiled: August 16, 1982Date of Patent: September 10, 1985Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4535173Abstract: The present invention provides a novel process for preparing known prostaglandins, particularly 9-deoxo-9-methylene-16,16-dimethyl-PGE.sub.2. This well known and useful prostaglandin is prepared from D-glucose through a series of efficient reactions. Also provided are novel intermediates which are useful for preparation of a wide variety of prostaglandins.Type: GrantFiled: December 13, 1982Date of Patent: August 13, 1985Assignee: The Upjohn CompanyInventor: Bruce A. Pearlman
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Patent number: 4522943Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: April 21, 1982Date of Patent: June 11, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4507292Abstract: Aryl N-oxalyl-N-methyl-carbamates of the general formula ##STR1## in which X represents an alkoxy, alkenoxy, alkinoxy, aryloxy, alkylthio, alkenylthio, alkinylthio or arylthio radical, each of which may be optionally substituted, or represents a radical of the general formula --N R.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl or aryl radical, each of which may be optionally substituted,or the radicals R.sup.3 and R.sup.4, together with the N atom to which they are bonded, form an optionally substituted heterocyclic ring, andR.sup.1 represents an aryl radical which is optionally substituted,are novel and find use as pesticides, especially for combating insects, acarids and nematodes.Type: GrantFiled: January 27, 1983Date of Patent: March 26, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Wolfgang Behrenz, Ingeborg Hammann, Bernhard Homeyer
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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: 4482728Abstract: Certain polybutylbenzylphenols and benzyl-3,4-methylenedioxybenzenes are useful for insect control especially as insect chemosterilants and oviposition inhibitors. The benzyl-3,4-methylenedioxybenzenes also find utility as growth inhibitors for mosquito larvae.Type: GrantFiled: April 20, 1982Date of Patent: November 13, 1984Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Leonard Jurd
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Patent number: 4472427Abstract: Compounds of the formula Het--O--CH.sub.2 --CHOR--CH.sub.2 --NHaralkyl where Het are ##STR1## disclosed. The compounds are useful as pharmaceuticals.Type: GrantFiled: August 30, 1982Date of Patent: September 18, 1984Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David E. McClure
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Patent number: 4456586Abstract: Non-ionic surface-active agents of the formula are disclosed: ##STR1## in which a=0 or 1, R denotes a C.sub.8 -C.sub.30 aliphatic or alicyclic radical, x+y totals a number from 1 to 10 and, in each unit, one of Z.sub.1 and Z.sub.2 denotes hydrogen and the other denotes the radical ##STR2## in which R.sub.1 denotes methyl or ethyl. These products can be prepared simply and are suitable for use in cosmetic or pharmaceutical compositions and in particular in cosmetic compositions for treating the hair or skin.Type: GrantFiled: October 23, 1981Date of Patent: June 26, 1984Assignee: L'OrealInventors: Guy Vanlerberghe, Henri Sebag, Rene Pierre
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Patent number: 4450276Abstract: The stereospecific preparation of D(+)-biotin is improved by a synthetic route involving the conversion of 3,4-isopropylidene-D-arabinose in which the OH group in the 2-position is not protected, into an ester of 6,9-dihydroxy-7,8-isopropylidenedioxynona-2,4-dienoic acid, the latter then being catalytically hydrogenated and subsequently converted into D(+)-biotin in a manner known per se.Type: GrantFiled: June 7, 1982Date of Patent: May 22, 1984Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Jurgen Gehlhaus, Claus P. Herz
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Patent number: 4430341Abstract: Water soluble quaternary ammonium salt compounds exhibit outstanding insecticidal and miticidal activity coupled with reduced mammalian toxicity and acceptable phytotoxicity.Type: GrantFiled: August 24, 1977Date of Patent: February 7, 1984Assignee: Union Carbide CorporationInventor: Barbara W. Kaplan
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Patent number: 4393228Abstract: The epoxysuccinic acid derivatives of this invention are prepared by esterification of an epoxysuccinic acid or a halide thereof, by partial hydrolysis of an epoxysuccinic acid diester, by amidation of an epoxysuccinic acid monoester, or by hydrolysis of an epoxysuccinic acid amide monoester. These epoxysuccinic acid derivatives have excellent thiol protease inhibitory activity and anti-inflammatory activity without the acceleration of vascular permeability.Type: GrantFiled: February 22, 1978Date of Patent: July 12, 1983Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Jiro Sawada, Kazunori Hanada, Masaharu Tamai, Shigeo Morimoto, Sadafumi Omura
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Patent number: 4386101Abstract: Unsymmetrical bis-carbamates of the formula ##STR1## wherein R.sub.1 is a phenyl, dihydrobenzofuranyl, naphthyl, pyrimidyl, pyrazolyl, triazolyl, quinolinyl or tetrahydroquinolinyl group, andR.sub.2 is a benzyl group,processes for producing them and their use for combating pests are described.Type: GrantFiled: November 9, 1981Date of Patent: May 31, 1983Assignee: Ciba-Geigy CorporationInventors: Jozef Drabek, Manfred Boger
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Patent number: 4357344Abstract: Certain polybutylbenzylphenols and benzyl-3,4-methylenedioxybenzenes are useful for insect control especially as insect chemosterilants and oviposition inhibitors. The benzyl-3,4-methylenedioxybenzenes also find utility as growth inhibitors for mosquito larvae.Type: GrantFiled: March 29, 1979Date of Patent: November 2, 1982Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Leonard Jurd
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Patent number: 4350705Abstract: Derivatives of 2-substituted-cyclohexane-1,3-diones possessing antihypertensive activity.Type: GrantFiled: March 25, 1980Date of Patent: September 21, 1982Assignee: Eisai Co., Ltd.Inventors: Sachiyuki Hamano, Shinichi Kitamura, Toshiji Igarashi, Yoshikage Nakajima
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Patent number: 4350636Abstract: A process for the preparation of phenylacetonitriles, carrying basic substituents, of the formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: August 27, 1981Date of Patent: September 21, 1982Assignee: BASF AktiengesellschaftInventors: Gerhard Kastner, Hardo Siegel, Karl-Heinz Geiss
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Patent number: 4342777Abstract: Certain polybutylbenzylphenols and benzyl-3,4-methylenedioxybenzenes are useful for insect control especially as insect chemosterilants and oviposition inhibitors. The benzyl-3,4-methylenedioxybenzenes also find utility as growth inhibitors for mosquito larvae.Type: GrantFiled: November 5, 1981Date of Patent: August 3, 1982Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Leonard Jurd
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Patent number: RE31061Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or amino, R.sub.2 is hydrogen or alkyl of 1 to 6 carbon atoms, with the provisos that (1) at least one of R.sub.1 and R.sub.2 is not a tertiary alkyl group and (2) R.sub.2 is hydrogen when R.sub.1 is amino, orR.sub.1 and R.sub.2 taken together and with the nitrogen atom to which they are joined are pyrrolidino, piperidino or N'-2-hydroxyethylpiperazino,each X' is independently alkyl or 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, or two X's on adjacent carbon atoms together are methylenedioxy, andn is 0, 1, 2 or 3,and the pharmaceutically acceptable acid addition salts thereof, are useful as anti-obesity and anti-diabetic agents. The compounds wherein R.sub.1 is alkyl and R.sub.2 is hydrogen are synthesized by a two-step synthesis from 2-alkyl-5-arylisoxazolium salts and ethylenediamine. The compounds wherein R.sub.1 and R.sub.Type: GrantFiled: March 27, 1980Date of Patent: October 19, 1982Assignee: Sandoz, Inc.Inventor: William R. Simpson