Nitrogen Attached Directly Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/159)
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Patent number: 4289892Abstract: Active hydrogen-containing fluorochemical is used as a foam stabilizer for polyurethane foams. For example, rigid or flexible polyurethane foams with high or low density and uniform cellular structure are prepared using fluoroaliphatic radical-substituted poly(oxyalkylene) polyols as foam stabilizers.Type: GrantFiled: April 30, 1979Date of Patent: September 15, 1981Assignee: Minnesota Mining and Manufacturing CompanyInventor: Fredrich A. Soch
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Patent number: 4288592Abstract: There is provided a process for preparing amides which comprises reacting an amine, or an amide, and an acid halide, or anhydride, in suitable molecular proportions, in an inert organic diluent, in the presence of an effective amount of a molecular sieve, until the reaction is completed, separating the molecular sieve, and recovering the amide from the organic mother liquor.Type: GrantFiled: April 30, 1979Date of Patent: September 8, 1981Assignee: American Cyanamid CompanyInventors: Michael M. Rauhut, Shin-Shyong Tseng
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Patent number: 4283538Abstract: In one embodiment, the present invention is concerned with novel triarylmethane compounds possessing in their triaryl structure a 4'-oxo-1'-naphthylidene (or a 4'-oxo-1'-phenylidene) moiety and a phenyl moiety substituted in the ortho-position to the central carbon atom with the group ##STR1## wherein R is an alkyl group or a phenyl group, unsubstituted or substituted with a solubilizing group; R' is selected from ##STR2## wherein R" is methyl, unsubstituted or substituted with one or two halo groups or substituted with a phenyl, alkoxy or phenoxy group and ##STR3## wherein Y is an electron-withdrawing group; and R and R' taken with said ##STR4## represents ##STR5## In another embodiment the present invention is concerned with a method of synthesizing the aforementioned compounds by reacting, e.g., a 2-R'-3-(4'-hydroxy-1'-phenyl/naphthyl)-3-(phenyl/naphthyl)-2,3-dihydrobenz [d]isothiazole-1,1-dioxide with an alkylation reagent in the presence of base.Type: GrantFiled: December 26, 1979Date of Patent: August 11, 1981Assignee: Polaroid CorporationInventor: James W. Foley
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Patent number: 4281118Abstract: Novel aminoalkylsulfides, aminoalkylsulfoxides and aminoalkylsulfones of the general formula ##STR1## wherein y and z independently represent the integer 0, 1 or 2; a represents the integer 0 or 2; n represents the integer 1, 2, 3 or 4; R.sub.1 independently represent lower alkyl or hydrogen or alternatively R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom represent a 5 or 6 membered heterocyclic ring which may optionally contain an oxygen atom whereby a morpholino, piperidino, or pyrrolidino grouping is formed; R.sub.3 represents halo such as chloro or bromo, lower alkylthio, arloweralkylthio, arylthio such as 4-methylphenylthio, 4-morpholinylloweralkylthio such as 4-morpholinylpropylthio, lower alkyl or arloweralkylamino such as 4-methoxybenzenemethanamino; R.sub.4 represents hydrogen or lower alkyl. The invention also includes the pharmaceutically-acceptable salts of the compounds described herein.Type: GrantFiled: June 18, 1979Date of Patent: July 28, 1981Assignee: The Dow Chemical CompanyInventors: Joseph E. Dunbar, Louis E. Begin
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Patent number: 4266080Abstract: Perfluoroalkyl compounds containing ether groups have the formulaR.sub.f R.sub.1 SCH.sub.2 CH.sub.2 O T Zwherein R.sub.f is a perfluoroalkyl, R.sub.1 is alkylene or alkyleneoxy or aminoalkylene, T is alkylene, and Z is hydrogen; hydroxy; NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 each is alkyl or together with nitrogen form a heterocyclic ring; N.sup.+ R.sub.3 R.sub.4 (R.sub.5)X.sub.z.sup.-y, where R.sub.5 is hydrogen, oxide, alkyl, or substituted alkyl, X is an anion, and y is 1 or 2; z is 0 or 1 or is --OCH.sub.2 CH.sub.2 SR.sub.1 R.sub.f ; can be prepared directly by free-radical catalyzed addition of a perfluoroalkylthiol to a vinyl ether or subsequent reaction. These compounds are useful as surfactants and oil spill collecting agents.Type: GrantFiled: February 2, 1978Date of Patent: May 5, 1981Assignee: Ciba-Geigy CorporationInventors: Robert A. Falk, Karl F. Mueller
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Patent number: 4263293Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; andn is an integer of 1 to 20.Type: GrantFiled: May 30, 1980Date of Patent: April 21, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, Tamara Dejneka
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Patent number: 4252804Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.Type: GrantFiled: January 13, 1978Date of Patent: February 24, 1981Assignee: Metabio-JoullieInventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
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Patent number: 4248779Abstract: A thiolcarbamate having the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and respectively represent an alkyl, alkoxy, alkenyl, cycloalkyl, hydroxyalkyl, phenyl or benzyl group and R.sub.1 and R.sub.2 can form a ring by binding each other with or without oxygen atom; and R.sub.3 represents a lower alkyl or benzyl group or a substituted benzyl group having one or two substituent of halogen atom, alkyl, alkoxy, alkylthio, nitro, or cyano group, which comprises reacting carbonyl sulfide with a sec-amine having the formula ##STR2## wherein R.sub.1 and R.sub.2 are defined above, in an aqueous medium and then reacting a halogenated hydrocarbon having the formulaX--R.sub.3 (IV)wherein R.sub.3 is defined above and X represents a halogen atom, in an aqueous medium.Type: GrantFiled: October 4, 1978Date of Patent: February 3, 1981Assignee: Ihara Chemical Industry Company, LimitedInventors: Zenichi Sato, Fumiya Tabuchi, Keiichiro Takagi, Yoji Imamiya
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Patent number: 4246260Abstract: The invention relates to new substituted o-phenylenediamine derivatives of the general formula ##STR1## in which R represents optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkinyl,X represents O, S, SO or SO.sub.2 andR.sup.1 and R.sup.2 are different from one another and individually represent ##STR2## in which R.sup.3 and R.sup.4 are identical or different and represent alkyl andR.sup.5 represents hydrogen, optionally substituted alkyl or optionally substituted alkoxy, and salts thereof.Also included in the invention are (1) methods for preparing the above-described compounds, (2) compositions containing the above-described compounds and (3) methods for the treatment of helminthiasis.Type: GrantFiled: March 19, 1979Date of Patent: January 20, 1981Assignee: Bayer AktiengesellschaftInventors: Heinrich Kolling, Ekkehard Niemers, Hartmund Wollweber, Herbert Thomas
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Patent number: 4237132Abstract: A series of new 4,6-disubstituted 2-morpholinone derivatives were prepared either by a reaction of corresponding epoxide derivatives with phenylglycine derivatives or by the reaction of isopropanol derivatives with carboxylic acid derivatives. The new morpholinone derivatives are useful for the prevention or the treatment of arteriosclerosis.Type: GrantFiled: June 4, 1976Date of Patent: December 2, 1980Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Katsuya Ohata, Hiroshi Enomoto, Shoichi Chokai, Mitsuhiro Maehara, Katsuhide Saito, Takayuki Ozaki
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Patent number: 4225708Abstract: 2-Sulfamoyl-5-sulfamido-1-naphthols represented by the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be the same or different and each represent a hydrogen atom, a straight-chain alkyl group, a branched alkyl group or a cycloalkyl group; or R.sup.1 and R.sup.Type: GrantFiled: August 22, 1979Date of Patent: September 30, 1980Assignee: Konishiroku Photo Industry Co., Ltd.Inventors: Masaru Kanbe, Kazumasa Watanabe, Morito Uemura, Jiro Takahashi, Ryuichiro Kobayashi, Tatsuhiko Kobayashi
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Patent number: 4216326Abstract: N-{3- and 4-[R.sub.1 -(phenyl)-C(.dbd.X)]-phenyl-lower-alkyl}amines, useful as anti-inflammatory agents, are prepared either by reduction of 3- or 4-[R.sub.1 -(phenyl)-CO]-phenyl-lower-alkanoylamines, which are also useful as anti-inflammatory agents; by benzoylating a phenyl-lower-alkylamine; by reaction of a 3- or 4-lithiophenyl-lower-alkylamine with a R.sub.1 -(phenyl)-carboxaldehyde, a R.sub.1 -(phenyl)-lower-alkyl ketone or a R.sub.1 -(phenyl)-carbonitrile or by transformations involving manipulations of a carbonyl or carbinol group.Type: GrantFiled: May 3, 1978Date of Patent: August 5, 1980Assignee: Sterling Drug Inc.Inventor: Bernard L. Zenitz
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Patent number: 4204064Abstract: A method, composition and compounds useful in said compositions for treating the skin and scalp characterized by an excessive secretion of sebum to improve the condition thereof by reducing said excessive secretion of sebum includes topically applying to a human having skin and/or a scalp so characterized a cosmetic composition containing as an active ingredient a derivative of cysteine or cysteamine. The composition contains about 0.1-5 weight percent of said derivative and also contains as a carrier for the active ingredient, water, a mixture of water and a lower alkanol, a lower alkanol, a mixture of a lower alkanol and a cosmetic resin, a reducing agent, a neutralizing agent or a vegetable oil.Type: GrantFiled: January 24, 1978Date of Patent: May 20, 1980Assignee: L'OrealInventor: Gregoire Kalopissis
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Patent number: 4183927Abstract: Novel substituted phenylthioalkylamines, salts and pharmaceutical compositions thereof wherein the sulfur may appear as a sulfide, sulfinyl or sulfonyl are disclosed as antithrombotic agents.Type: GrantFiled: September 13, 1977Date of Patent: January 15, 1980Assignee: The Dow Chemical CompanyInventors: Louis E. Begin, Robert J. Broersma, Jr., George D. Dickerson, Joseph E. Dunbar
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Patent number: 4177290Abstract: Novel acetamide derivatives have been discovered to have useful pharmaceutical activity on the central nervous system. They may be prepared by reacting the corresponding ester or acid halide with the appropriately substituted amine.Type: GrantFiled: March 9, 1978Date of Patent: December 4, 1979Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4168151Abstract: o-Amidophenylmorpholine compounds having a halo, haloalkyl, lower alkylsulfonyl, halo-lower alkylsulfonyl, or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The compounds are useful as herbicides.Type: GrantFiled: December 13, 1978Date of Patent: September 18, 1979Assignee: United States Borax & Chemical CorporationInventors: Kelvin K. Shen, Wayne S. Belles
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Patent number: 4166072Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.Type: GrantFiled: April 18, 1978Date of Patent: August 28, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4161590Abstract: The invention is directed to fluorinated compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxy-perfluoroalkyl group, R.sup.1 is a branched or straight chain alkylene, alkylenethioalkylene, alkyleneoxy-alkylene or alkyleneiminoalkylene group, X is oxygen or an amino group, Q is an organic group containing at least one amino group and y is zero or 1, and the corresponding succinimides. These compounds are useful as surfactants.Type: GrantFiled: January 12, 1978Date of Patent: July 17, 1979Assignee: Ciba-Geigy CorporationInventor: Karl F. Mueller
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Patent number: 4156011Abstract: The sulphur- and oxygen-containing diaryl compounds of the formula: ##STR1## in which A and B, which may be the same or different, represent O, S, SO or SO.sub.2,Alk is a C.sub.1 -C.sub.4 hydrocarbon radical with a straight or branched chain, R represents COOH, an esterified COOH group, a carboxylic amide group, OH, O-SO.sub.2 CH.sub.3, NH.sub.2, NHR.sub.1, NR.sub.1 R.sub.2, NHZOH, NHZNR.sub.1 R.sub.2, C(.dbd.NH)NH.sub.2, C(.dbd.NH)NHOH or 2-.DELTA..sup.2 -imidazolinyl, Z is a C.sub.2 -C.sub.4 hydrocarbon radical with a straight or branched chain, and R.sub.1 and R.sub.2 each represent a C.sub.1 -C.sub.Type: GrantFiled: April 5, 1977Date of Patent: May 22, 1979Assignee: Societe Anonyme dite: Laboratoire L. LafonInventors: Victor Lafon, Louis Lafon
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Patent number: 4156079Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: June 19, 1978Date of Patent: May 22, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4154828Abstract: N.sup.2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: October 21, 1977Date of Patent: May 15, 1979Assignees: Mitsubishi Chemical Industries, Ltd., Shosuke 0KAMOTOInventors: Shosuke Okamoto, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Shinji Tonomura
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Patent number: 4153443Abstract: o-Amidophenylmorpholine compounds having a halo, haloalkyl, lower alkylsulfonyl, halo-lower alkylsulfonyl, or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The compounds are useful as herbicides.Type: GrantFiled: August 3, 1978Date of Patent: May 8, 1979Assignee: United States Borax & Chemical CorporationInventors: Kelvin K. Shen, Wayne S. Belles
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Patent number: 4151353Abstract: N-(aminosulfenyl)carbamoyl halide compositions are useful intermediates in the production of carbamate compounds.Type: GrantFiled: June 26, 1975Date of Patent: April 24, 1979Assignee: Union Carbide CorporationInventor: Duane E. Thurman
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Patent number: 4151354Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: August 2, 1978Date of Patent: April 24, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4144271Abstract: N-substituted mercaptomethylacetamidines are prepared, and are useful as immunoregulants for correcting an imbalance of immune homeostasis, particularly, as immunostimulants in the treatment of autoimmune and immune deficient diseases and disorders.Type: GrantFiled: October 25, 1977Date of Patent: March 13, 1979Assignee: Merck & Co., Inc.Inventors: Howard Jones, Conrad P. Dorn
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Patent number: 4139529Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides and the pharmaceutically acceptable acid addition salts thereof which have antithrombotic properties.Type: GrantFiled: August 31, 1977Date of Patent: February 13, 1979Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Hyogi Kikumoto, Yoshikuni Tamao, Kazdo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4138485Abstract: This invention relates to certain derivatives of phenylalanine having interesting pharmaceutical properties, in particular, a lipid-lowering activity.Type: GrantFiled: February 24, 1977Date of Patent: February 6, 1979Assignee: Kyowa Hakko Kogyo Kabushiki KaishaInventors: Nobuhiro Nakamizo, Masayuki Teranishi, Ikuo Matsukuma, Katsuichi Shuto, Koji Yamada
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Patent number: 4133880Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: July 28, 1977Date of Patent: January 9, 1979Assignees: Mitsubishi Chemical Industries Ltd., Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4132786Abstract: The invention relates to new N-substituted benzenesulphonamides of general formula ##STR1## in which N IS 2 OR 3,R.sub.1 and R.sub.2 are hydrogen atoms, methyl, ethyl groups, or jointly form with the nitrogen a nitrogenized heterocyclic ring having 5 or 6 members, in particular a piperidino, pyrrolidino or morpholino group,R.sub.3 is a hydrogen atom, an NO.sub.2 group, an NH.sub.2 group, or a halogen,R.sub.4 is a hydrogen, a halogen, an NH.sub.2 group or a sulphonamide group.These compounds are useful as active substances of medicaments, in particular as antiemetic.Type: GrantFiled: June 8, 1976Date of Patent: January 2, 1979Inventors: Robert C. Moreau, Jean-Paul Fournier
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Patent number: 4128643Abstract: (2-Amino-4-quinazolinyl)-quanidines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the defined meanings, and their physiologically tolerable acid addition salts, process for preparing these compounds, pharmaceutical preparations containing them and their use as medicines.Type: GrantFiled: May 26, 1977Date of Patent: December 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
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Patent number: 4126691Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.Type: GrantFiled: December 6, 1976Date of Patent: November 21, 1978Assignee: Ciba-Geigy CorporationInventors: Richard W. J. Carney, George DEStevens
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Patent number: 4125604Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: June 7, 1977Date of Patent: November 14, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4123251Abstract: o-Amidophenylmorpholine compounds having a halo, haloalkyl, lower alkylsulfonyl, halo-lower alkylsulfonyl, or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The compounds are useful as herbicides.Type: GrantFiled: June 2, 1977Date of Patent: October 31, 1978Assignee: United States Borax & Chemical CorporationInventors: Kelvin K. Shen, Wayne S. Belles
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Patent number: 4115381Abstract: Dyestuffs of the formula ##STR1## wherein D is a diazo component of the benzene series,R.sub.1 is an alkyl radical,R.sub.2 is alkylene andR is alkyl, aryl or di-substituted amino, dye polyester fibers in red and blue shades with good fastness. The dyestuffs can be used in the thermosol process.Type: GrantFiled: September 14, 1976Date of Patent: September 19, 1978Assignee: Ciba-Geigy CorporationInventor: Visvanathan Ramanathan
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Patent number: 4111937Abstract: 3-Amino-2,4,6-triiodobenzoic acids optionally substituted in the 5-position by amino or carboxy or a derivative thereof react with dibasic acid anhydrides to give the corresponding cyclic imides (A), which can be hydrolyzed to the corresponding anilic acids (B). The latter can be further alkylated on the anilide nitrogen atom. Compounds A and B are useful as cholecystographic and urographic agents.Type: GrantFiled: October 18, 1976Date of Patent: September 5, 1978Assignee: Sterling Drug Inc.Inventor: James H. Ackerman
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Patent number: 4111953Abstract: A process is disclosed for preparing 5-sulfamoylbenzoic acids substituted in 4-position by various substituents and in 3-position by a cyclic amino group having sali-diuretic properties. Novel intermediate compounds are also disclosed.Type: GrantFiled: December 6, 1976Date of Patent: September 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Dieter Bormann, Wulf Merkel, Dieter Mania
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Patent number: 4105790Abstract: The invention concerns .alpha.-aminoacyl derivatives of phenyl-, phenoxy-, thiophenoxy- and phenylsulphinylalkanoic acids together with their amides, esters and pharmaceutically acceptable salts; processes for their preparation; and pharmaceutical compositions for therapeutic use in inhibiting the formation of thrombi and also in reducing the persistence of thrombi formed in the blood of warm blooded animals. Representative compounds of the invention are methyl 4-(aminoacetyl)phenoxyacetate, 4-(aminoacetyl)phenoxyacetic acid and methyl 4-(aminoacetyl)-thiophenoxyacetate, preferably as their hydrochlorides.Type: GrantFiled: November 9, 1976Date of Patent: August 8, 1978Assignee: Imperial Chemical Industries LimitedInventors: Clifford R. Hughes, Stephen J. Jackson, John Preston, Peter L. Walton
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Patent number: 4098789Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.Type: GrantFiled: March 2, 1977Date of Patent: July 4, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4098889Abstract: Novel antithrombotic 2-(aminoalkylthio)-N,N'-p-phenylenebissulfonamides, a method for inhibiting blood platelet aggregation, and pharmaceutical compositions.Type: GrantFiled: September 1, 1977Date of Patent: July 4, 1978Assignee: The Dow Chemical CompanyInventor: Joseph E. Dunbar
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Patent number: 4096255Abstract: N.sup.2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: September 14, 1976Date of Patent: June 20, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Shosuke Okamoto, Akiko Hijikata
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Patent number: 4096267Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]aklanoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.Type: GrantFiled: June 10, 1975Date of Patent: June 20, 1978Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4093712Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: January 19, 1977Date of Patent: June 6, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4087550Abstract: A method and composition for combatting the greasy and unaesthetic appearance of the hair and to improve the appearance of the skin comprises in a carrier at least one active component of the formula ##STR1## wherein R.sub.1 and R.sub.2 are methyl, ethyl, isopropyl, cyclohexyl, benzyl or .beta.-hydroxyethyl, or R.sub.1 and R.sub.2 taken together form --(CH.sub.2).sub.2 --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.2 --CH.sub.2 --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, ##STR2## and R is (i) linear or branched alkyl having 1-18 carbon atoms, (ii) alkenyl having 3-18 carbon atoms, (iii) alkyl having 2-3 carbon atoms and substituted by 1-2 alcohol functions, (iv) --(CH.sub.2).sub.m --CH(OR.sub.3).sub.2 wherein R.sub.3 is alkyl having 1-4 carbon atoms and m is 1-2, (v) --(CH.sub.2).sub.n R.sub.4 wherein n is 0, 1 or 2 and R.sub.4 is 2-pyridyl or phenyl, (vi) --(CH.sub.2).sub.q R'.sub.4 wherein q is 0 or 1 and R'.sub.Type: GrantFiled: April 15, 1976Date of Patent: May 2, 1978Assignee: L'OrealInventors: Claude Bouillon, Charles Vayssie
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Patent number: 4076836Abstract: Acylated phenylamino thiopropionates of the formula I shown hereinafter are effective microbicides. They may be used for combatting plantpathogenic fungi or for preventing plants from fungi attack.Type: GrantFiled: September 24, 1976Date of Patent: February 28, 1978Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Walter Kunz, Wolfgang Eckhardt
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Patent number: 4066758Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substitured with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.Type: GrantFiled: March 29, 1976Date of Patent: January 3, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Shinji Tonomura, Yoshikuni Tamao, Tohru Tezuka, Akiko Hijikata
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Patent number: 4064239Abstract: Novel substituted benzenedisulfonamides are disclosed which compounds are active anthelmintic agents being particularly useful against fascioliasis in sheep and cattle. Specifically the active compounds are 4-amino-1,3-benzenedisulfonamide with an unsaturated substituted alkyl group. Compositions and methods containing the novel substituted benzenedisulfonamides for use in anthelmintic therapy particularly against liver fluke are also disclosed.Type: GrantFiled: September 26, 1975Date of Patent: December 20, 1977Assignee: Merck & Co., Inc.Inventor: Helmut H. Mrozik
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Patent number: 4064270Abstract: A new class of N'-(aminoacylaminophenyl) acetamidines: ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R.sup.3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics.The products are obtained by treating a suitable amino-acid or a carbonyl-activated amino-acid, with the appropriate N'-(4-aminophenyl)-N,N-dimethylacetamidine. In addition, the products are obtained by treating a suitable N'-(haloacylaminophenylacetamidine with an appropriate amine.Type: GrantFiled: September 13, 1974Date of Patent: December 20, 1977Assignee: Bayer AktiengesellschaftInventors: Hartmund Wollweber, Ekkehard Niemers, Hans Peter Schulz, Herbert Thomas, Peter Andrews
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Patent number: 4062963Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.Type: GrantFiled: March 29, 1976Date of Patent: December 13, 1977Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Shinji Tonomura, Yoshikuni Tamao
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Patent number: 4059623Abstract: Substituted 2-(carbamoyl)oxyimino-3-iminobutyramides and 2-(carbamoyl)oxyimino-3-iminobutyrates of the formula ##STR1## where Q is --OR.sub.4 or --NR.sub.5 R.sub.6, and A, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as hereinafter defined are useful as aphicides. The compounds are made by reacting an amine with a substituted 2-hydroxyiminoacetoacetamide (or 2-hydroxyiminopropionylacetamide) or an alkyl 2-hydroxyiminoacetoacetate (or 2-hydroxyiminopropionylacetate), then carbamylating the resulting substituted 2-hydroxyimino-3-iminobutyramide (or 2-hydroxyimino-3-iminovaleramide) or 2-hydroxyimino-3-iminobutyrate (or 2-hydroxyimino)-3-iminovalerate).Type: GrantFiled: April 25, 1974Date of Patent: November 22, 1977Assignee: E. I. Du Pont de Nemours and CompanyInventor: Russell Frank Bellina
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Patent number: 4058532Abstract: The invention relates to novel 1-(4-R.sub.1 O-phenyl)-2-(4-R.sub.2 -phenyl)-6-R.sub.3 -1,2,3,4-tetrahydroquinolines having antifertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.Type: GrantFiled: May 13, 1976Date of Patent: November 15, 1977Assignee: Sterling Drug Inc.Inventor: Malcolm R. Bell