Plural Nitrogens In Alcohol Moiety Patents (Class 560/251)
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Patent number: 4448773Abstract: Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or .alpha.-naphthyl, each of which is further substituted,R.sub.1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, .beta.-alkoxyethyl, hydroxymethyl, triazolylmethyl, imidazolylmethyl, pyrazolylmethyl, alkylsulfinyl, alkylsulfonyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkylsulfinyloxy, dialkylaminosulfinyloxy, phosphoric or thiophosphoric esters or amides, or alkylcarbonyloxy,R.sub.7 is hydrogen or optionally-substituted methyl or ethyl, andR.sub.8 is alkyl optionally substituted by alkoxy,are microbicidally, in particular fungicidally, active. Preferred compounds are those in which Ar is 2-methylphenyl, 2-methoxyphenyl, 2-chlorophenyl or .alpha.-naphthyl, each of which is further substituted by azido, and each of R.sub.7 and R.sub.8 is methyl.Type: GrantFiled: April 22, 1982Date of Patent: May 15, 1984Assignee: Ciba-Geigy CorporationInventors: Peter Riebli, Hanspeter Fischer, Rudolph C. Thummel, Adolf Hubele
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Patent number: 4443475Abstract: Novel amides of acyl-carnitines having general formula ##STR1## wherein R' is acetyl, propionyl, butyryl (unsubstituted or halogen-substituted) isobutyryl, .beta.-hydroxybutyryl, acetoacetyl, pantothenyl, and linoleyl, and R" is either an unsubstituted amino radical (provided that R' is ather than acetyl) or a substituted amino radical, are therapeutically effective in treatment of functional arrythmias or arrhythmias secondary to myocardialsclerotic diseases and as psychosti-mulants.Type: GrantFiled: May 26, 1982Date of Patent: April 17, 1984Inventor: Claudio Cavazza
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Patent number: 4436726Abstract: This invention relates to new N-acylpeptide compounds of immunological activity, said compounds being of the formula: ##EQU1## wherein R.sup.1 and R.sup.2 are each alkyl or alkenyl;R.sup.3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, heterocyclic(lower)alkyl or ar(lower)alkyl, wherein the aryl moiety may have hydroxy or protected hydroxy;R.sup.4 is carboxy, esterified carboxy, carboxy(lower)alkyl or esterified carboxy(lower)alkyl;X is bond or lower alkylene;Y is lower alkylene or lower alkylidene; andn is an integer of 0 to 1;or its pharmaceutically acceptable salt.Type: GrantFiled: December 9, 1981Date of Patent: March 13, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuyoshi Umehara, Hirokazu Tanaka, Itsuo Uchida, Masanobu Kohsaka, Hiroshi Imanaka, Keizo Yoshida
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Patent number: 4430346Abstract: The novel compound represented by the general formula (I) ##STR1## (wherein R represents a hydrogen atom, an alkanoyl group of 1 to 14 carbon atoms, or an arylcarbonyl group), and an acid addition salt thereof [on condition that when R is a hydrogen atom, the hydrochloride exhibits an optical rotation of [.alpha.].sub.D.sup.22 -1.degree. .+-.2.degree. (c, 2 water)] has antitumor activity in experimental animals.Type: GrantFiled: May 7, 1982Date of Patent: February 7, 1984Assignee: Bristol-Myers CompanyInventors: Hamao Umezawa, Tomio Takeuchi, Shinichi Kondo, Hironobu Iinuma, Daishiro Ikeda, Teruya Nakamura, Akio Fujii
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Patent number: 4422870Abstract: 2-Aryl-1, 3-cyclohexanedione enol ester compounds exhibit outstanding miticidal,mite ovicidal and herbicidal activity.Type: GrantFiled: March 28, 1977Date of Patent: December 27, 1983Assignee: Union Carbide CorporationInventor: Thomas N. Wheeler
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Patent number: 4402975Abstract: A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.Type: GrantFiled: July 17, 1981Date of Patent: September 6, 1983Assignee: Teijin LimitedInventors: Toru Takeshita, Kenji Hoshina, Akira Ohtsu, Tatsuyuki Naruchi
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Patent number: 4400517Abstract: 1,2,4-triazol-(5)-yl-[thio] phosphates are disclosed having the formula ##STR1## wherein R.sup.1 =alkyl with from 1 to 5 carbon atoms;R.sup.2 =OR.sup.1, R.sup.1, C.sub.6 H.sub.5, NHR.sup.1, N(R.sup.1).sub.2 ;X=O, SR.sup.3 =H, alkyl with from 1 to 5 carbon atoms, C.sub.6 H.sub.5, benzyl, alkenyl with from 2 to 6 carbon atoms, alkynyl with from 2 to 6 carbon atoms; andR.sup.4 =vinyl, halovinyl, polyhalovinyl, vinyl substituted with aryl groups, alkyl groups with from 1 to 4 carbon atoms, O-alkyl groups with from 1 to 4 carbon atoms, S-alkyl groups with from 1 to 4 carbon atoms; haloalkyl, acetyl, cyclohexenyl, benzoyl ##STR2## Also disclosed are 1,2,4-triazole intermediates having the formula ##STR3## wherein: X, R.sup.3 and R.sup.4 have the same meanings as indicated above. The phosphate esters are useful in combatting infestations of pests such as orthoptera, aphides, diptera, lepidoptera, coleoptera, acari, nematodes.Type: GrantFiled: January 29, 1980Date of Patent: August 23, 1983Assignee: Montedison S.p.A.Inventors: Franco Gozzo, Pier M. Boschi, Angelo Longoni
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Patent number: 4396627Abstract: Compounds having the formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Y and X are as defined hereinbelow, are useful for the reduction of abnormally high blood glucose and lipid levels in the treatment of obesity or hyperglycaemia.Type: GrantFiled: March 15, 1982Date of Patent: August 2, 1983Assignee: Beecham Group LimitedInventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4376646Abstract: Novel ureas of the formula I have herbicidal activity and are suitable in small applied amounts for selectively combating weeds in cultivated crops of soya-bean, maize and cereals. They are advantgeously produced by the isocyanate method and correspond to the formula I ##STR1## wherein R.sub.1 is an unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, aralkyl, phenyl, acyl or C.sub.1 -C.sub.4 -alkylsulfonyl group or an aminoalkyl group,R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sub.3 is hydrogen, halogen, cyano or trifluoromethyl,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl or C.sub.1 -C.sub.6 -alkoxy,R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.2 -C.sub.6 -alkenyl, or R.sub.5 together with R.sub.4 and the nitrogen atom to which they are bound also form a 5-6-membered heterocycle, andX is oxygen, sulfur or the sulfinyl or sulfonyl group.Type: GrantFiled: March 6, 1981Date of Patent: March 15, 1983Assignee: Ciba-Geigy CorporationInventors: Otto Rohr, Georg Pissiotas
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Patent number: 4365085Abstract: The present invention relates to novel bicyclic compounds useful as photographic silver halide developing agents, to the preparation of these compounds and to photographic products, processes and compositions employing the same. The subject compounds may be represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, the same or different, each represents hydrogen, a hydrocarbon moiety, preferably an alkyl group, --COOH or --COOR.sup.1 wherein R.sup.1 is an alkyl group; R.sub.3 and R.sub.4, the same or different, each represent hydrogen or an alkyl group, R.sub.5 represents hydrogen or --COR.sup.2 wherein R.sup.2 is an alkyl group; R.sub.6 represents hydrogen when R.sub.5 is hydrogen and represents hydrogen or --OCOR.sup.3 wherein R.sup.3 is an alkyl group the same as R.sup.2 when R.sub.5 represents --COR.sup.2 ; X represents --OH, --NH.sub.2 or --NHCOR.sup.4 wherein R.sup.4 represents an alkyl group the same as R.sup.2 ; Y represents --OH or --OCOR.sup.5 wherein R.sup.Type: GrantFiled: February 5, 1979Date of Patent: December 21, 1982Assignee: Polaroid CorporationInventors: James R. Bartels-Keith, Eva R. Karger
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Patent number: 4360531Abstract: [2-Amino(substituted cycloaliphatic)]benzeneacetamide and benzamide compounds, e.g., trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec-8 -yl]benzeneacetamide, have useful analgesic activity and low abuse or physical dependence liability, or are useful as chemical intermediates for producing such analgesic compounds. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 23, 1982Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4359476Abstract: N-[2-Amino(oxy or thio group) substituted-cycloaliphatic]phenylacetamide and -benzamide compounds, having the oxy- or thio group substituents on a cycloaliphatic ring carbon adjacent to either of the nitrogen bearing carbons of the cycloaliphatic ring, e.g., cis- and trans-4-bromo-N-[3-methoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzamide , and trans-3,4-dichloro-N-methyl-N-[7-(1-pyrridolinyl)-1,4-dioxaspiro[4.5]dec-6 -yl]benzeneacetamide, and salts thereof, have useful analgesic activity and low abuse liability in humans and valuable warm blooded animals. Processes for their production and pharmaceutical compositions and method of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 16, 1982Assignee: The Upjohn CompanyInventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4353842Abstract: A novel method of treating gastrointestinal, spasmolytic and ulcerogenic disorders by the administration of amidinoureas is disclosed.Type: GrantFiled: February 5, 1980Date of Patent: October 12, 1982Assignee: William H. Rorer, Inc.Inventors: Julius Diamond, George H. Douglas
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Patent number: 4332738Abstract: The esterification of neo acids catalyzed by the presence of a macro-reticular structured sulfonic acid cation exchange resin proceeds under mild conditions with a wide variety of alcohols to give readily recoverable esters in high yields and high purity and an easily recoverable and reusable catalyst.Type: GrantFiled: November 24, 1980Date of Patent: June 1, 1982Assignee: Exxon Research & Engineering Co.Inventors: Francisco M. Benitez, Michael F. English
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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: 4313889Abstract: Soft quaternary surface active agents having the formula: ##STR1## wherein ##STR2## represents a tertiary open chain or cyclic aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.20 open chain or cyclo alkyl group, a C.sub.1 -C.sub.20 alkoxyalkyl group, a C.sub.1 -C.sub.20 acyloxyalkyl group, a C.sub.1 -C.sub.20 haloalkyl group, a C.sub.1 -C.sub.20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C.sub.1 -C.sub.4 alkyl group, an O--C.sub.1 -C.sub.8 acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 represents a C.sub.9 -C.sub.22 straight or branched alkyl group, a --(CH.sub.2).sub.n -- ##STR4## wherein R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C.sub.0 -C.sub.Type: GrantFiled: June 10, 1980Date of Patent: February 2, 1982Assignee: Merck & Co., Inc.Inventor: Nicolae S. Bodor
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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: 4293557Abstract: Phenoxypropylamine derivatives of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl or ethyl group, R.sub.2 and R.sub.3, independently from each other, represent a lower alkyl group, or together form a linear alkylene group having 4 to 7 carbon atoms which may be optionally substituted by a hydroxyl or hydroxymethyl group, and R.sub.4 represents a hydrogen atom or a group of the formula --R.sub.5 --Z in which R.sub.5 represents a lower alkylene group, and Z represents a hydrogen atom or an amino, mono- or di-(lower alkyl)-amino, hydrdoxy lower alkylamino, lower alkanoylamino, hydroxyl, lower alkoxy, lower alkanoyloxy, phenoxy, halophenoxy, benzoyloxy or halobenzoyloxy group, andthe salts thereof; to a process for production thereof; and to their medicinal use, particularly to antiulcer agents comprising these phenoxypropylamine derivatives or their salts.Type: GrantFiled: June 30, 1980Date of Patent: October 6, 1981Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Kenyu Shibata, Toshihisa Itaya, Nobuaki Yamakoshi, Shigeru Kurata, Naoyuki Koizumi, Masaaki Tarutani, Hideki Sakuma, Kunihiro Konishi
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Patent number: 4291176Abstract: Insecticidally active vinyl-cyclopropane carboxylic acid esters of the formula ##STR1## are prepared by reacting ##STR2## in which R.sup.12 is a radical selected from the group consisting of ##STR3## with an alcoholate of the formulaM--O--R.sup.8.Various processes for making the intermediates are also described. Many of the intermediates and end products are new.Type: GrantFiled: August 24, 1977Date of Patent: September 22, 1981Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Willy Hartmann
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Patent number: 4289903Abstract: There are provided certain p-phenylalkoxy phenylurea and thiourea compounds useful for the control of undesirable plants in the presence of agronomic crops and to methods for the preparation of said phenylalkoxy phenylurea and thiourea compounds.Type: GrantFiled: June 25, 1979Date of Patent: September 15, 1981Assignee: American Cyanamid CompanyInventors: David M. Spatz, Barrington Cross
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Patent number: 4284620Abstract: Novel x-ray contrast agents, i.e., N-(2-hydroxyethyl)-2,4,6-triiodo-3,5-bis-(2-keto-L-gulonamido)benzamide and intermediates.Type: GrantFiled: March 23, 1979Date of Patent: August 18, 1981Assignee: Mallinckrodt, Inc.Inventors: Youlin Lin, Kenneth R. Smith
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Patent number: 4281188Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N--R.sup.7 in which R.sup.Type: GrantFiled: September 11, 1980Date of Patent: July 28, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4260684Abstract: The invention relates to a new enzymatic process for the stereoselective resolution of a DL-phenylglycine derivative comprising hydrolyzing an ester or amide group on an N-acyl-L-phenylglycine ester or amide in an N-acyl-DL-phenylglycine ester or amide in solution by the action of an enzyme bonded to a carrier, separating the N-acyl-D-phenylglycine ester or amide from the N-acyl-L-phenylglycine and then, if desired, hydrolyzing under acid conditions, the ester or amide group of the D-enantiomer and the acyl group.D-Phenylglycine and D-4-hydroxyphenylglycine are used as starting substances for the preparation of semisynthetic antibiotics of the penicillin series. L-Phenylglycine is a starting substance for L-aspartyl-L-phenylglycine methyl ester, which is used as a sweetener.Type: GrantFiled: February 1, 1979Date of Patent: April 7, 1981Assignee: Bayer AktiengesellschaftInventor: Hermann Schutt
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Patent number: 4256729Abstract: Novel X-ray contrast agents, i.e., N,N'-bis-(2,3-dihydroxypropyl)-2,4,6-triiodo-5-(2-keto-L-gulonamido)isopht halamide, and intermediates.Type: GrantFiled: March 23, 1979Date of Patent: March 17, 1981Assignee: Mallinckrodt, Inc.Inventor: Youlin Lin
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Patent number: 4243678Abstract: Compounds of the formula ##STR1## wherein R is (a) optionally-substituted and optionally-hydrogenated biphenylyl, (b) optionally-substituted and optionally-hydrogenated bicyclic aryl having from 8 to 12 ring carbon atoms or (c) a radical of the formula ##STR2## R.sup.1 is aliphatic hydrocarbyl, alicyclic hydrocarbyl or optionally-substituted phenyl;R.sup.2 is --H or lower aliphatic hydrocarbyl;R.sup.3 is --H, lower alkyl, cycloalkyl, optionally-substituted phenyl or, with R.sup.4, alkylene;R.sup.4 is lower alkyl, cycloalkyl, optionally-substituted phenyl, optionally-(nuclearly)-substituted phenalkyl or, with R.sup.3, alkylene;or R.sup.2,R.sup.3 and R.sup.4, together with the carbon to which each is bound, are adamantyl; andn is 3, 4 or 5;and salts thereof with a base are pharmacologically active. Esters thereof are valuable intermediates for the preparation of the pharmacologically-active compounds. Physiologically-acceptable embodiments are administered, e.g.Type: GrantFiled: December 15, 1978Date of Patent: January 6, 1981Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Walter Krastinat
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Patent number: 4243606Abstract: The present invention relates to new N-substituted anilines which correspond to the general formula: ##STR1## in which R.sub.1 represents an alkyl radical or substituted alkyl radical, R.sub.2 represents a hydrogen atom, an alkyl radical or substituted alkyl radical, R.sub.3 represents a cyano, carbamoyl, carboxy or carbalkoxy radical and R.sub.4 represents a hydrogen or halogen atom or an alkyl or alkoxy radical. These compounds are valuable intermediates for the preparation of coloring materials, especially as coupling compounds for the synthesis of azo dyes.Type: GrantFiled: September 30, 1977Date of Patent: January 6, 1981Assignee: Produits Chimiques Ugine KuhlmannInventors: Paul M. C. Bourdauducq, Claude M. H. E. Brouard, Claude L. E. Moerel, Jean-Pierre H. Stiot
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Patent number: 4233209Abstract: Hindered phenol hydrazones of the formula ##STR1## wherein R.sub.1 and R.sub.2 are alkyl of 1 to 8 carbons or R.sub.1 can also be hydrogen, n is 1 to 6, R' is hydrogen or alkyl, R.sub.3 is alkyl, phenyl, substituted phenyl, alkylenethioalkyl or alkylenethioether ester of a carboxylic acid or a group ##STR2## where T is a direct bond, alkylene, sulfur or oxygen interrupted alkylene or phenylene, said compounds being useful as diene rubber stabilizers.Type: GrantFiled: November 15, 1978Date of Patent: November 11, 1980Assignee: Ciba-Geigy CorporationInventors: Martin Dexter, David H. Steinberg
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Patent number: 4220590Abstract: New optically active bis phosphine compounds which are usful in optically active catalysts. Such catalysts are particularly useful in catalytic asymmetric hydrogenation.Type: GrantFiled: July 31, 1978Date of Patent: September 2, 1980Assignee: Monsanto CompanyInventors: William S. Knowles, Milton J. Sabacky, Billy D. Vineyard
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Patent number: 4216166Abstract: Certain nitro-benzamido-naphthalenemonosulfonic acids and salts thereof useful in the preparation of the corresponding amino precursors to the final product ureides which are useful as inhibitors of connective tissue destruction.Type: GrantFiled: December 20, 1978Date of Patent: August 5, 1980Assignee: American Cyanamid CompanyInventor: Seymour Bernstein
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Patent number: 4216164Abstract: Certain ureides of substituted naphtholmonosulfonic acids and salts useful as inhibitors of connective tissue destruction.Type: GrantFiled: December 20, 1978Date of Patent: August 5, 1980Assignee: American Cyanamid CompanyInventor: Seymour Bernstein
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Patent number: 4216165Abstract: Certain amino-benzamido-naphthalenemonosulfonic acids and salts thereof useful in the preparation of the corresponding ureides useful as inhibitors of connective tissue destruction.Type: GrantFiled: December 20, 1978Date of Patent: August 5, 1980Assignee: American Cyanamid CompanyInventor: Seymour Bernstein
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Patent number: 4215215Abstract: Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.Type: GrantFiled: July 6, 1979Date of Patent: July 29, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
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Patent number: 4203920Abstract: A new class of chemical compounds and their process of preparation is described. These compounds have valuable properties as anti-diarrheal agents.Type: GrantFiled: July 21, 1978Date of Patent: May 20, 1980Assignee: William H. Rorer, Inc.Inventors: Julius Diamond, George H. Douglas
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Patent number: 4162331Abstract: New carboxylic acid derivatives are proposed for use as agents in the treatment or prevention of arteriosclerosis. 1-(p-chlorophenoxy)-3-(N-phenyl-N-carbomethoxymethylamino)-2-propanol is a typical compound.Type: GrantFiled: January 24, 1977Date of Patent: July 24, 1979Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Katsuya Ohata, Hiroshi Enomoto, Shoichi Chokai, Mitsuhiro Machara, Katsuhide Saito, Takayuki Ozaki
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Patent number: 4159991Abstract: .alpha.-Acyloxy-N,N'-diacylmalonamides of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, straight chain or branched alkyl radicals having from one to eleven carbon atoms, or hydrocarbon radicals with six to twelve carbon atoms and comprising at least one aromatic ring, are novel compounds prepared by the action of a mixture of carboxylic acids R.sub.3 COOH and R.sub.4 COOH upon an .alpha.-acyloxymalononitrile, R.sub.1 COO--C(CN).sub.2 --R.sub.2, in the presence of an acid catalyst and are useful as intermediates in organic synthesis and low temperature activators in bleaching or scouring compositions.Type: GrantFiled: August 22, 1977Date of Patent: July 3, 1979Assignee: Produits Chimiques Ugine KuhlmannInventors: Bernard Dubreux, Serve Y. Delavarenne, Jean-Pierre Schirmann
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Patent number: 4158672Abstract: Polyfluoroalkylthio alcohols and esters thereof are disclosed with utility as intermediates for the synthesis of fluorochemicals with low free surface energies having oil and water repellent properties. The novel alcohols and esters are obtained by a free radical catalyzed addition of polyfluoroalkylthiols to acetylenic alcohols or esters thereof. The alcohols are employed in preparation of fluorine containing polyurethanes which are useful as finishes to provide oil and water repellency to textiles and as additives to plastics to provide mold release and other desirable properties.Type: GrantFiled: December 23, 1977Date of Patent: June 19, 1979Assignee: Ciba-Geigy CorporationInventors: Robert E. A. Dear, Neal O. Brace
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Patent number: 4146385Abstract: The invention provides novel phenoxyalkylcarboxylic acids which are useful in therapy as metabolic regulators and in agriculture as selective herbicides.Type: GrantFiled: August 16, 1976Date of Patent: March 27, 1979Assignee: Societe de Recherches Industrielles S.O.R.I.Inventor: Bernard Majoie
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Patent number: 4137322Abstract: ML-236B carboxylic acid derivatives having the formula ##STR1## wherein R represents an alkyl group, a benzyl group optionally substituted with alkyl, alkoxy or halogen or a phenacyl group optionally substituted with alkyl, alkoxy or halogen; a group of 1/n M in which M represents a metal and n represents a valency of said metal; or a group of AH.sup.+ in which A represents an amino acid. These derivatives are derived from ML-236B by conventional procedures and have an antihyperlipemic activity.Type: GrantFiled: October 31, 1977Date of Patent: January 30, 1979Assignee: Sankyo Company LimitedInventors: Akira Endo, Akira Terahara, Noritoshi Kitano, Akira Ogiso, Seiji Mitsui
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Patent number: 4128663Abstract: Anilide derivative compounds of the formula ##STR1## e.g., trans-N-(2-hydroxycyclopentyl)-3',4'-dichloropropionanilide, have been found to possess potent Central Nervous System (CNS) antidepressant properties.These compounds are promising antidepressant drugs which are characterized by less toxicity than imipramine, and long-acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are also disclosed.Type: GrantFiled: May 16, 1977Date of Patent: December 5, 1978Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4125599Abstract: 5-Gluconamido-2,4,6-triiodo-N-methylisophthalamic acid, 3-acetamido-2,4,6-triiodo-5-trishydroxymethylacetamidobenzoic acid, related compounds and salts and esters thereof are useful as x-ray contrast agents. The corresponding acyl halides are useful as intermediates.Type: GrantFiled: August 19, 1976Date of Patent: November 14, 1978Assignee: Mallinckrodt, Inc.Inventor: Philip E. Wiegert
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Patent number: 4125619Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: January 19, 1977Date of Patent: November 14, 1978Assignees: Mitsubishi Chemical Industries, Ltd., Shosuke OkamotoInventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Yoshikuni Tamao, Akiko Hijikata
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Patent number: 4123614Abstract: The present invention relates to novel assay reagents, their composition, methods of preparation, and use in the detection and measurement of various biological systems and/or components, e.g. enzymes, antibodies, antigens, and periodate concentration. This invention in its basic form utilizes a class of compounds having, inter alia., a backbone chain, an indicator group, and vicinal oxidizable groups.Type: GrantFiled: October 18, 1976Date of Patent: October 31, 1978Assignee: Syntex (U.S.A.) Inc.Inventor: David H. Rammler
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Patent number: 4118587Abstract: Novel 3-(butylamino) or (1-pyrrolidinyl)-4-phenoxy-5-sulfamylbenzoic acid derivatives where the butyl group contains either a double bond or a hydroxy, ketone, acid or ester functional group or groups, said compounds being useful as diuretics.Type: GrantFiled: November 1, 1976Date of Patent: October 3, 1978Assignee: Hoffmann-La Roche Inc.Inventor: David Llewellyn Coffen
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Patent number: 4117154Abstract: Oxime-carbamates of fluorinated ketones of the formula ##STR1## in which X represents hydrogen or fluorine,R represents alkyl, cycloalkyl, phenyl or phenylalkyl, any of which can optionally be substituted,R.sup.1 and R.sup.2, which may be identical or different, each represent hydrogen, alkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl or optionally substituted phenyl, andR.sup.2 can also represent the --SR.sup.3 grouping,R.sup.3 represents alkyl, halogenoalkyl, optionally substituted phenyl or alkoxycarbonyl, or represents a radical identical to that to which the --SR.sup.3 grouping is bonded, or represents the ##STR2## grouping, WHEREINR.sup.4 represents alkyl andR.sup.5 represents alkyl, dialkylamino or optionally substituted phenyl,And acid addition salts thereof, which possess insecticidal, acaricidal, nematicidal and fungicidal properties.Type: GrantFiled: July 12, 1977Date of Patent: September 26, 1978Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Ingeborg Hammann, Bernhard Homeyer, Wolfgang Behrenz
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Patent number: 4113972Abstract: 1,1-Diphenyl-2-hydroxy-3-aminopropane derivatives are useful for their psychotropic activity and, in particular are useful as antidepressants.Type: GrantFiled: June 21, 1976Date of Patent: September 12, 1978Assignee: Beecham Group LimitedInventor: Judith Ann Clark
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Patent number: 4111683Abstract: Compounds of the formula ##STR1## wherein R is aliphatic hydrocarbyl, alicyclic hydrocarbyl or aryl suitably substituted, if desired, or a heterocyclic group, R.sup.1 is hydrogen or alkyl, R.sup.2 is alkyl or alkoxy, R.sup.3 is ##STR2## wherein a is 0 or 1, R.sup.4 is hydrogen or CW'.sub.3, the W' being hydrogen or halogen, Z is halogen and X is halogen, hydroxy, alkoxy, acetoxy, carbethoxyalkoxy, phenoxy, alkylthio, carbethoxyalkylthio, phenylthio, phosphono, dithiophosphonoxy, phosphoramido, isocyanato, isothiocyanato, alkyl- and dialkylthiocarbamoylthio, alkyl- and dialkylcarbamoyloxy, alkylsulfonyl, etc., have herbicidal activity.Type: GrantFiled: November 12, 1976Date of Patent: September 5, 1978Assignee: Chevron Research CompanyInventor: Malcolm Scott Singer
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Patent number: 4094991Abstract: New carboxylic acid derivatives are proposed for use as agents in the treatment of prevention of arteriosclerosis. 1-(p-chlorophenoxy)-3-(N-phenyl-N-carbomethoxymethylamino)-2-propanol is a typical compound.Type: GrantFiled: January 24, 1977Date of Patent: June 13, 1978Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Katsuya Ohata, Hiroshi Enomoto, Shoichi Chokai, Mitsuhiro Machara, Katsuhide Saito, Takayuki Ozaki
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Patent number: 4094966Abstract: The present invention provides new iodobenzene derivatives which have at least two benzene nuclei and one carboxylic group.These derivatives possess a low toxicity and may be used as X-ray contrast media.Type: GrantFiled: December 7, 1976Date of Patent: June 13, 1978Assignee: Laboratoires Andre GuerbetInventors: Guy Tilly, Michel Jean Charles Hardouin, Jean Lautrou
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Patent number: 4093742Abstract: Novel polyhaloisopropyl-substituted arylureas having potent antihypertensive properties are disclosed herein.Type: GrantFiled: May 4, 1976Date of Patent: June 6, 1978Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 4072705Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholesterolaemiant and cholagogic agents or in the preparation of such agents.Type: GrantFiled: February 9, 1976Date of Patent: February 7, 1978Assignee: Orchimed S.A.Inventor: Andre Mieville