Benzoic Acid Substituted On Ring With Oxy And Nitrogen Patents (Class 560/46)
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Patent number: 5025036Abstract: The invention relates to catechol carboxylic acid derivatives of the formula ##STR1## wherein, R.sub.1 is ##STR2## acetyl, hydrogen, hydroxy or alkanoyloxy, R.sub.2 is ##STR3## hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2,R.sub.3 is hydrogen, lower alkyl or amino,R.sub.4 is hydrogen, lower alkyl, halogen or aminoA is ##STR4## wherein, R.sub.5 is hydrogen or acyl, R.sub.6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R.sub.7 and R.sub.8, independently, are hydrogen, lower alkyl or halogen, orA is ##STR5## wherein, R.sub.5 is hydrogen or acyl, R.sub.9 is hydrogen, lower alkyl, R.sub.10 is hydrogen, lower alkyl or halogen, R.sub.11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R.sub.1 or R.sub.2 can be hydroxy, alkanoyloxy or ##STR6## and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is --(CH.sub.2).sub.Type: GrantFiled: May 3, 1989Date of Patent: June 18, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
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Patent number: 4999186Abstract: The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are not directly coupled.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.Type: GrantFiled: June 2, 1987Date of Patent: March 12, 1991Assignee: The Procter & Gamble CompanyInventors: Anthony D. Sabatelli, Josephine A. Spirnak
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Patent number: 4983628Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reaction substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: January 3, 1989Date of Patent: January 8, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
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Patent number: 4978772Abstract: Use of bromure d'otilonium, that it otilonii bromidum, for local applications in the gastrointestinal tract of the digestive system and related pharmaceutical formulation appropriate for such use, to obtain the arrest of the motility of the gastrointestinal tract in order to allow endoscopic manoeuvers for diagnostic and therapeutic purposes.Type: GrantFiled: November 4, 1987Date of Patent: December 18, 1990Assignee: A. Menarini S.A.S.Inventors: Alessandro Casini, Sandro Parti, Paolo Bucci
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Patent number: 4908470Abstract: Methyl 4-dimethylamino-3,5-dimethoxybenzoate, an intermediate in the preparation of the antibacterially active aditoprim, is obtained from 4-amino-3,5-dibromobenzoic acid by replacement of the bromine atoms by methoxy groups and subsequent methylation.Type: GrantFiled: November 30, 1988Date of Patent: March 13, 1990Assignee: Hoffman-La Roche Inc.Inventors: Alfredo Guerrato, Martin Karpf, Hanny K. Berger, Ivan Kompis, Markus Schlageter
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Patent number: 4861799Abstract: A benzoylurea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a methyl group, provided that X.sub.1 and X.sub.2 are not simultaneously hydrogen atoms, Y is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, a --CO.sub.2 R.sub.1 group wherein R.sub.1 is a hydrogen atom, a cation or an alkyl group, or a --OR.sub.1 group wherein R.sub.1 is as defined above, A.sub.1 is .dbd.N--or ##STR2## wherein Y is as defined above, W is an oxygen atom, a sulfur atom or ##STR3## wherein R.sub.1 is as defined above, k is an integer of from 1 to 3, l is 0 or 1, and Ar is ##STR4## wherein Z is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, an alkoxy group which may be substituted by halogen, a nitro group, a cyano group or a --S(O).sub.n R.sub.2 group wherein R.sub.2 is an alkyl group which may be substituted by halogen and n is 0, 1 or 2, A.sub.Type: GrantFiled: September 30, 1987Date of Patent: August 29, 1989Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Yasuhiro Fujii, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4861796Abstract: 2-Acetylaminogentisic acid has been isolated from the culture broth after cultivation of a bacterium of the genus Streptomyces. This compound has antibacterial actions against Gram-positive and Gram-negative bacteria.Type: GrantFiled: December 19, 1988Date of Patent: August 29, 1989Assignee: Hoechst AktiengesellschaftInventors: Axel Zeeck, Sabine Breiding-Mack, Susanne Grabley, Hartmut Voelskow, Gerhard Seibert
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Patent number: 4853398Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: April 13, 1987Date of Patent: August 1, 1989Assignee: Eli Lilly and CompanyInventors: F. P. Carr, Robert D. Dillard, Doris E. McCullough
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Patent number: 4826876Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinyl-methyl]-thyronine.Type: GrantFiled: December 21, 1987Date of Patent: May 2, 1989Assignee: Smith Kline & French Laboratories LimitedInventors: David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
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Patent number: 4808338Abstract: Intermediate compounds of the formula ##STR1## wherein X is oxy, thio, sulfinyl or sulfonyl; R is halogen; C.sub.1 C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; trifluoromethoxy; difluoromethoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; trifluoromethyl or difluoromethyl; R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, or phenyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene; R.sup.3 hydrogen, C.sub.1 C.sub.4 alkyl, or phenyl with the proviso that R.sup.1 and R.sup.3 are not both phenyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, or phenyl; R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.Type: GrantFiled: February 1, 1988Date of Patent: February 28, 1989Assignee: Stauffer Chemical CompanyInventor: David L. Lee
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Patent number: 4772614Abstract: Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.Type: GrantFiled: June 13, 1986Date of Patent: September 20, 1988Assignee: The Boots CompanyInventors: Roy V. Davies, James Fraser, Kenneth J. Nichol
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Patent number: 4723005Abstract: New anisotropic compounds of the formula (1) are useful in liquid crystal mixtures for electrooptical displays; at least one of the end groups of the compounds (1) is an alkyl group which carries cyano or halogen in a terminal or non-terminal position. This offers advantages for longitudinal polarization and/or cross-polarization of the anisotropic compounds with the aid of the comparatively highly polarizing cyano or halogen substituents, in particular high clear points, low .DELTA..epsilon./.epsilon..perp. values and/or negative .DELTA..epsilon. values.Type: GrantFiled: September 10, 1984Date of Patent: February 2, 1988Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Tuong Huynh-Ba, Maged A. Osman
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Patent number: 4720505Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.Type: GrantFiled: November 13, 1984Date of Patent: January 19, 1988Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, John W. Gillard, Joshua Rokach
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Patent number: 4658054Abstract: A process for the preparation of 5,6-dialkoxyanthranilic acids is described. The 5,6-dialkoxyanthranilic acids are useful in the preparation of substituted quinazolinediones which are active cardiotonic agents.Type: GrantFiled: July 29, 1985Date of Patent: April 14, 1987Assignee: Ortho Pharmaceutical CorporationInventor: Richard A. Conley
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Patent number: 4636387Abstract: A long-acting, local anesthetic, comprising a polymeric phosphazene backbone, and certain radicals having local anesthetic activity and an amino functional group on the ring of said radical through which said radical is covalently attached to the phosphazene backbone by a phosphorous-nitrogen single bond is disclosed along with medicaments containing such anesthetics. The radicals employed are 2-amino-4-picoline, benoxinate, naepaine and phenacaine.Type: GrantFiled: September 21, 1984Date of Patent: January 13, 1987Assignee: Research CorporationInventors: Harry R. Allcock, Paul E. Austin, Thomas X. Neenan
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Patent number: 4634777Abstract: Compounds of the general formula: ##STR1## wherein A and B are both hydrogen, or one of A and B is a group (G) of the formula: ##STR2## and the other is a group R.sup.5 wherein R.sup.1 is an aryl group or a heterocyclic group, both of them being optionally substituted, and R.sup.4 and R.sup.5 are both hydrogen or together form a single chemical bond,R.sup.2 and R.sup.2 ' are independently hydrogen, halogen, nitro, lower alkyl or lower alkoxy, andR.sup.3 and R.sup.3 ' are independently carboxy or its functional derivative, with the proviso that (a) when A and B are both hydrogen, then R.sup.2 and R.sup.2 ' cannot be both hydrogen,and, where applicable, pharmaceuticably acceptable salts thereof are hyaluronidase inhibitors, and useful as anti-allergic agent and anti-ulcerous agent. Among the compound (I'), those wherein when one of A and B is the group (G) and the other is the group R.sup.5 wherein R.sup.4 and R.sup.5 together form a single chemical bond, R.sup.1 is unsubstituted aryl and R.sup.2 and R.sup.Type: GrantFiled: February 1, 1985Date of Patent: January 6, 1987Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
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Patent number: 4634769Abstract: A process for the preparation of 8-halo-5,6-dialkoxyquinazoline-2,4-diones and their metal salts is described. The diones are active cardiotonic agents.Type: GrantFiled: September 25, 1984Date of Patent: January 6, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Robert A. Mallory, Jeffrey B. Press, Harvey M. Werblood
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Patent number: 4515980Abstract: Novel lower-alkyl 2-(hydroxyphenylamino)benzoates, useful as inhibitors of lipoxygenase, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers.Type: GrantFiled: July 11, 1983Date of Patent: May 7, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4476315Abstract: Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.Type: GrantFiled: December 23, 1982Date of Patent: October 9, 1984Assignee: Ethyl CorporationInventors: G. Patrick Stahly, Barbara C. Stahly
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Patent number: 4408059Abstract: Milbemycin and avermectin macrolides are synthesized by the cyclized linking of separately synthesized northern and southern hemisphere intermediates. The northern hemisphere intermediate is a spiroketal alkenyl aldehyde, and the southern hemisphere intermediate is an aryl alkenyl phosphine oxide anion.Type: GrantFiled: December 4, 1981Date of Patent: October 4, 1983Assignee: University Patents, Inc.Inventors: Amos B. Smith, III, Steven R. Schow
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Patent number: 4371547Abstract: 2-Benzylideneglutaraldehydes of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or a substituent selected from the group consisting of halo, lower-alkyl, phenyl, carboxy, lower-alkoxycarbonyl, phenoxycarbonyl, aminocarbonyl, hydroxysulfonyl, nitro, cyano, hydroxy, lower-alkoxy and phenoxy, a method of use thereof as disinfectants, disinfectant compositions comprising them, and 2,6-dialkoxy-3-(.alpha.-alkoxybenzyl)tetrahydropyrans of the formula ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are as defined above and R.sup.4 and R.sup.5 independently are alkyl of one to four carbon atoms, which are intermediates for their preparation are disclosed.Type: GrantFiled: August 21, 1981Date of Patent: February 1, 1983Assignee: Sterling Drug Inc.Inventors: Wolfgang Munzenmaier, Heinz Eggensperger, Helmut H. Ehlers, Wolfgang Beilfuss, Lothar Bucklers, Hans-Peter Harke
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Patent number: 4354033Abstract: Anthranilic acid esters having the generic formula: ##STR1## have been discovered. In the above formula (I) R.sub.1, R.sub.2 and R.sub.3 represent any of hydrogen, chlorine, methoxy and methyl groups and X represents a straight or branched alkyl chain comprising 1 to 4 carbon atoms. These esters are anti-inflaments, blood platelet aggregation inhibitors and prostaglandin synthetase inhibitors.The compounds of the above formula (I) may be prepared by reacting alkali metal salt of a compound of the formula (II): ##STR2## in which R.sub.1, R.sub.2, R.sub.3 and X are the same as before with the compound of formula (III): ##STR3## in which R.sub.3 has the same meaning as before and z represents a chlorine or a bromine radical.Type: GrantFiled: August 31, 1981Date of Patent: October 12, 1982Assignee: Council of Scientific & Industrial ResearchInventors: Nanduri Bhanumati, Pralhad B. Sattur
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Patent number: 4337270Abstract: Novel anthranilic acid derivatives of the general formula: ##STR1## wherein X is a halogen atom, an alkoxyl group having 1-3 carbon atoms, an alkyl group having 1-3 carbon atoms or a nitro group, n is an integer of 1-2, Y is an alkoxyl group having 1-3 carbon atoms, m is an integer of 2-3, Z is --COCH.dbd.CH-- or --CO--, R.sub.1 is a hydrogen atom or an alkyl group having 1-4 carbon atoms, and pharmaceutically acceptable salts thereof, which derivatives and salts possess a strong antiallergic action and are thus useful as therapeutically active agents for diseases caused by allergies, such as asthma, hay fever, urticaria and atopic dermatitis; an antiallergic composition comprising the same; and a method of alleviating diseases caused by allergies using the same.Type: GrantFiled: May 21, 1980Date of Patent: June 29, 1982Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Kanji Noda, Akira Nakagawa, Toshiharu Motomura, Masayoshi Tsuji, Hidetoshi Amano, Hiroyuki Ide
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Patent number: 4331674Abstract: 4-Phenoxy-4-(azolyl-1-yl)-butanoic acid derivatives of the formula ##STR1## in which A is --CO-- or CH(OH)--,Y is --CH.dbd. or --N.dbd.,Z is halogen, alkyl, alkenyl, halogenoalkyl, cycloalkyl, alkoxy, alkylthio, alkoxycarbonyl, phenyl, phenoxy, phenylalkyl, substituted phenyl, phenoxy or phenylalkyl, amino, cyano or nitro,R is cyano, --CO--OR.sup.3 or --CO--NR.sup.4 R.sup.5,R.sup.1 and R.sup.2 each independently is alkyl, phenyl or substituted phenyl, or conjointly form a carbocyclic ring,R.sup.3 is alkyl,R.sup.4 is hydrogen, alkyl, phenyl or substituted phenyl andR.sup.5 is hydrogen or alkyl, orR.sup.4 and R.sup.5 conjointly form a methylene bridge --(CH.sub.2).sub.m -- which can contain a further hetero-atom,m is 2, 3, 4, 5, 6 or 7,n is 0, 1, 2, 3, 4 or 5,and salts thereof, which possess fungicidal properties.Type: GrantFiled: July 27, 1977Date of Patent: May 25, 1982Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Jorg Stetter, Karl H. Buchel, Paul-Ernst Frohberger, Wilhelm Brandes
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Patent number: 4330677Abstract: The invention relates to polyethers having an an average molecule weight of 3000 to 5000 and having a propylene oxide proportion of 60 to 80% and an ethylene oxide proportion of 20 to 40%. Also included in the invention are compositions containing said polyethers and methods for the use of said polyethers and compositions, particularly for their anti-lipidaemic effect.Type: GrantFiled: October 31, 1979Date of Patent: May 18, 1982Assignee: Bayer AktiengesellschaftInventors: Siegfried Linke, Mithat Mardin, Hans P. Krause, Rudiger Sitt
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Patent number: 4313956Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.Type: GrantFiled: December 28, 1979Date of Patent: February 2, 1982Assignee: INTERx Research Corp.Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4311706Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.Type: GrantFiled: January 22, 1980Date of Patent: January 19, 1982Assignee: INTERx Research CorporationInventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4310677Abstract: Alkyl anthranilates are prepared by reacting an isatin with an alkanol and hydrogen peroxide in the presence of an alkali metal alkanolate.The alkyl anthranilates obtainable by the process of the invention are valuable starting materials for the preparation of pesticides, dyes and drugs.Type: GrantFiled: December 17, 1980Date of Patent: January 12, 1982Assignee: BASF AktiengesellschaftInventors: Gernot Reissenweber, Dietrich Mangold
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Patent number: 4281181Abstract: Novel L-.gamma.-glutamyl-3-carboxy-4-hydroxyanilide of the formula, ##STR1## an acid addition salt thereof, or an alkali metal or amine salt thereof, which is useful for determining the activity of .gamma.-glutamyl transpeptidase.Type: GrantFiled: November 14, 1979Date of Patent: July 28, 1981Assignees: Nitto Boseki Co., Ltd., Iatron Laboratories, Inc.Inventors: Takeshi Nagasawa, Katsumasa Kuroiwa, Katsuyuki Takabayashi, Norimasa Takizawa, Kazuyo Hagihara, Tadami Akatsuka
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Patent number: 4276431Abstract: Alkali metal salts of hydroxybenzoates are claimed which are substantially anhydrous and free from hydrobenzoic acid and have the formula ##STR1## in which R.sup.1 denotes alkyl, alkenyl, cycloalkyl or aralkyl,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, halogen, hydroxyl, amino, alkylamino, alkyl, alkoxy, aralkyl or aryl andMe denotes an alkali metal.Furthermore a process for the preparation of the said alkali metal salts of hydroxybenzoates, which are substantially anhydrous and free from hydrobenzoic acid, characterized in that a solution or suspension of a hydroxybenzoate of the formula ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meaning, is neutralized with an alkali metal hydroxide at -10.degree. to +50.degree. C. until the degree of neutralization is 0.95 to 1.05, a degree of neutralization of 1.Type: GrantFiled: September 20, 1979Date of Patent: June 30, 1981Assignee: Bayer AktiengesellschaftInventors: Peter Schnegg, Walter Rapp, Bernhard Vosteen
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Patent number: 4242523Abstract: An improved process for the preparation of para-nitroso-diphenyl-hydroxylamines is discussed. In the improved process the dimerizing rearrangement of a nitroso benzene is performed in the presence of at least 0.5 mole of a Lewis acid per mole of nitroso compound.Type: GrantFiled: August 20, 1979Date of Patent: December 30, 1980Assignee: Akzona IncorporatedInventors: Paul K. Battey, Manfred Bergfeld, Peter Hope
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Patent number: 4219660Abstract: There are disclosed herein derivatives of bisfunctionalized compounds, wherein said compounds have been formed by the introduction of a nitro group and a hydroxyl group in the form of an ester into a conjugated diene molecule by treatment of said conjugated dienes with nitric acid in the presence of a carboxylic acid anhydride. The novel compounds produced by this process are useful as bactericides, fungicides and valuable organic synthesis intermediates.Type: GrantFiled: June 24, 1977Date of Patent: August 26, 1980Assignee: Hoffmann-La Roche Inc.Inventor: Pius A. Wehrli
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Patent number: 4159384Abstract: Phenenyltris(carbonylimino) multi-anionic substituted triphenyl acids and salts useful as complement inhibitors.Type: GrantFiled: September 1, 1978Date of Patent: June 26, 1979Assignee: American Cyanamid CompanyInventors: Ransom B. Conrow, Seymour Bernstein
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Patent number: 4145364Abstract: Fluorinated anilines, especially p-fluoroaniline and 2,4-difluoroaniline, are prepared by treating aromatic azides with anhydrous hydrogen fluoride. The aromatic azides, in turn, are prepared from the corresponding anilines by treatment with nitrous acid or salt thereof and an alkali metal azide in the presence of a mineral acid, and in an aqueous-nonaqueous, two-phase environment.Type: GrantFiled: November 30, 1977Date of Patent: March 20, 1979Assignee: Merck & Co., Inc.Inventors: Dennis M. Mulvey, Leonard M. Weinstock
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Patent number: 4135050Abstract: Anthranilic esters are obtained in good yield and high purity by transesterification when using potassium carbonate as transesterification catalyst.Type: GrantFiled: August 11, 1977Date of Patent: January 16, 1979Assignee: Hoechst AktiengesellschaftInventors: Peter Hess, Bernhard Mees
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Patent number: 4129740Abstract: An improved process for the preparation of para-nitroso-diphenylhydroxylamines is disclosed. One member of the group consisting of nitrosobenzene, ortho-substituted nitrosobenzenes, meta-substituted nitrosobenzenes, ortho-meta-disubstituted nitrosobenzenes and para-substituted nitrosobenzenes is reacted with one member selected from the group consisting of nitrosobenzene, ortho-substituted nitrosobenzenes, meta-substituted nitrosobenzenes, and ortho-meta-disubstituted nitrosobenzenes, in the presence of an acid catalyst. The improvement comprises utilizing as the acid catalyst an acid selected from the group consisting of aliphatic, cycloaliphatic, and aromatic sulfonic acids, having a pK.sub.a equal to or less than one, perchloric acid, and trifluoroacetic acid, in an amount equal to or greater than 0.5 mol of acid per mol of nitroso reactants, and performing the reaction at a temperature from about -20.degree. C to about 60.degree. C.Type: GrantFiled: January 30, 1978Date of Patent: December 12, 1978Assignee: Akzona IncorporatedInventors: Hans Zengel, Manfred Bergfeld
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Patent number: 4117159Abstract: N-Phenyl and N-benzyl .DELTA..sup.8 -dihydropimaramides are antiphlogistic and serum cholesterol lowering agents. The compounds, of which N-(2-ethylphenyl)-.DELTA..sup.8 -dihydropimaramide is a representative embodiment, are prepared from reactive derivatives of .DELTA..sup.8 -dihydropimaric acid and the appropriate amine.Type: GrantFiled: February 14, 1977Date of Patent: September 26, 1978Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Yukio Fujita, Tamiki Mori, Hiroshi Enomoto, Yoshiaki Yoshikuni
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Patent number: 4098816Abstract: Pharmaceutical compositions having hypolipidaemic and/or hypoglycaemic activity, contain a substituted (4-carboxyphenoxy) phenyl alkane derivative.Type: GrantFiled: January 9, 1976Date of Patent: July 4, 1978Assignee: Beecham Group LimitedInventors: David Edward Thorne, Keith Howard Baggaley, Brian Morgan
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Patent number: 4069250Abstract: Certain N-[poly(hydroxyalkyl)alkyl], 2,4,6-triiodoisophthalamic acids are useful as x-ray contrast agents.Type: GrantFiled: April 12, 1976Date of Patent: January 17, 1978Assignee: Mallinckrodt, Inc.Inventor: Philip E. Wiegert