Chalcogen Or Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/28)
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Patent number: 5006665Abstract: Phenolic thiane derivatives of the formula I or II ##STR1## in which n is 0, 1 or 2 and R.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, T and Z are as defined in claim 1, are effective stabilizers for color photography recording materials, in particular for the yellow layer. They act not only as light stabilizers but also as stabilizers against thermal oxidation.Type: GrantFiled: September 29, 1988Date of Patent: April 9, 1991Assignee: Ciba-Geigy AGInventors: Jean Rody, David G. Leppard
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Patent number: 5006150Abstract: Substituted benzoyl-2H-pyran-3,5-(4H,6H)-diones and related compounds, intermediates therefor, synthesis thereof, and the use of said diones for the control of weeds.Type: GrantFiled: May 29, 1990Date of Patent: April 9, 1991Assignee: Sandoz Ltd.Inventors: Shy-Fuh Lee, Richard J. Anderson, Gary W. Luehr, Carole R. Scott
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Patent number: 5001145Abstract: Compounds are described of formula (1) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 represents a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom or a C.sub.1-8 alkyl group and the group >C.dbd.NOR.sup.5 is in the E configuration).These compounds may be used for controlling insect, acarine, nematode or other pests.Type: GrantFiled: January 27, 1989Date of Patent: March 19, 1991Assignee: American Cyanamid CompanyInventors: Michael V. J. Ramsay, Derek N. Evans, Derek R. Sutherland, Edward P. Tiley, John B. Ward, Neil Porter, Hazel M. Noble, Richard A. Fletton, David Noble
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Patent number: 4997820Abstract: Novel macrocyclic compounds of the formual I ##STR1## where the dotted line in the 9,10-position is a saturated bond or a double bond, alternatively, and R is hydrogen, methyl or certain acyl radicals, and R.sub.o is hydrogen, halogen, azido, thiol, hydroxyl or --OY, where Y is, among other radicals, an ether radical, a silyl group, a sulfonyl group, a sugar radical or a (thiol)acyl radical, and R being methyl if there is a double bond in the 9,10-position, have microbicidal properties for the control of phytopathogenic microorganisms. They can be employed in the customary formulation for the control of plant disease.Type: GrantFiled: September 8, 1989Date of Patent: March 5, 1991Assignees: Gesellschaft fur Biotechnologische Forschung mbH, Ciba-Geigy CorporationInventors: Marius Sutter, Norbert Bedorf, Gerhard Hofle, Dietmar Schummer, Bettina Bohlendorf
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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Patent number: 4968813Abstract: Certain new chemical compounds are derivatives of 4H-thiopyran-1,1-dioxides, and are useful as electron-transport agents in electrophotographic elements.Type: GrantFiled: December 22, 1989Date of Patent: November 6, 1990Assignee: Eastman Kodak CompanyInventors: Norman G. Rule, Teh-Ming Kung
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Patent number: 4960758Abstract: The present invention relates to .beta.-D-phenylthioxyloside compounds selected from the group consisting of:(i) the .beta.-D-phenylthioxylosides of the formula: ##STR1## in which: R.sub.1 and R.sub.2, which can be identical or different, which represent a hydrogen atom or a trifluoromethy or cyano group,A represents CHOH or CO andY represents a hydrogen atom or an acyl group; and(ii) epimers thereof when A is CHOH.The said .beta.-D-phenylthioxyloside compounds are useful in therapy as antithrombotics.Type: GrantFiled: November 3, 1988Date of Patent: October 2, 1990Assignee: Fournier Innovation et SynergieInventors: Soth Samreth, Francois Bellamy, Jean Millet
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Patent number: 4959385Abstract: This invention relates to thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl, Y represents an ethylene or methylene radical or a valency bond, and n represents 0 or 1, bioprecursors thereof and pharmaceutically acceptable salts thereof which possess useful pharmacological properties, processes for their preparation and compositions containing them.Type: GrantFiled: January 19, 1989Date of Patent: September 25, 1990Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. Walsh, Jean-Claude Aloup
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Patent number: 4948806Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: June 9, 1989Date of Patent: August 14, 1990Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4946845Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: November 25, 1988Date of Patent: August 7, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
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Patent number: 4925590Abstract: Derivatives of 4-cyano-2,3-difluorophenol of the formula I ##STR1## wherein R.sup.1 is an alkyl group which has 1-12 C atoms and in which one or two CH.sub.2 groups can also be replaced by --O--, --CO--, --CO--O-- and/or --CH.dbd.CH--, no two 0 atoms being directly attached to one another,A.sup.1 and A.sup.2 independently of one another are each 1,4-phenylene which is unsubstituted or substituted by one or two F atoms, and in which one or two CH groups can also be replaced by N, or trans-1,4-cyclohexylene in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or S atoms,Z is --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, OCH.sub.2 --, --CH.sub.2 O, --C.tbd.C-- or a single bond,m is 0, 1 or 2 andQ is --CO-- or --CH.sub.2 --.Type: GrantFiled: March 9, 1989Date of Patent: May 15, 1990Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Volker Reiffenrath, Joachim Krause, Andreas Wachtler, Georg Weber, Ulrich Finkenzeller
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4894464Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2 C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.Type: GrantFiled: October 26, 1988Date of Patent: January 16, 1990Assignee: Pfizer Inc.Inventors: Thomas M. Brennan, Michael E. Hendrick
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Patent number: 4889939Abstract: Compounds suitable for being used as lubricants, having general formula:(I) RO--(C.sub.3 F.sub.6 O).sub.m --(CFXO).sub.n --CFX--L, or(II) R"CFXO--(C.sub.3 F.sub.6 O).sub.x (CFXO).sub.y --(C.sub.2 F.sub.4 O).sub.z --CFX--L, whereR=--CF.sub.3, --C.sub.2 F.sub.5, --C.sub.3 F.sub.7X=F, --CF.sub.3R"=F, --CF.sub.3, --C.sub.2 F.sub.5m=an integer from 3 to 100n=a finite integer, or =zero, wherefore m+n ranges from 3 to 100, provided that, if n is finite, m/n ranges from 5 to 20 and R is preferably =CF.sub.3, if n=zero, R is preferably --C.sub.2 F.sub.5 or --C.sub.3 F.sub.7x=a finite integer, or =zeroy, z=finite integers, such that x+y+z ranges from 5 to 200, while (x+z)/y ranges from 5 to 0.5, provided that when x=zero, z/y ranges from 1 to 0.5 and y+z ranges from 5 to 200 n while X is preferably F, and R"=LL=group Y-Z, where:Y=--CH.sub.2 O--, --CH.sub.2 --OCH.sub.2, --CF.sub.2, --CF.sub.Type: GrantFiled: April 11, 1988Date of Patent: December 26, 1989Assignee: Montedison S.p.A.Inventors: Gerardo Caporiccio, Ezio Strepparola, Mario A. Scarati
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Patent number: 4889856Abstract: 7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.Type: GrantFiled: August 31, 1987Date of Patent: December 26, 1989Assignee: Merck & Co., Inc.Inventors: Richard L. Tolman, Arthur F. Wagner, John J. Baldwin, Adolph Pietruszkiewicz
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Patent number: 4888042Abstract: The present compounds have a high herbicidal activity against various problematic weeds in soil treatment and foliage treatment in plow field as well as in treatment under flooded condition in paddy field, and besides they exhibit a high selectivity to the weeds from the main crops, so that they can be used in various applications as an active ingredient for herbicides.Type: GrantFiled: June 20, 1988Date of Patent: December 19, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Kenji Arai, Kouichi Morita, Nobuaki Mito, Naonori Hirata
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Patent number: 4885367Abstract: Sulfonanilide compounds represented by the formula ##STR1## wherein R.sup.1 is a lower alkyl group or a trifluoromethyl group, R.sup.2 is a cycloalkylidenemethyl group, a group of the formula --A--R.sup.3 (wherein A is an oxygen atom, a sulfur atom, a sulfynyl group or a sulfinyl group and R.sup.3 is a cycloalkyl group having 5-8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group, a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methyl-piperidyl group) or a group of the formula --B--R.sup.4 (wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R.sup.4 is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.Type: GrantFiled: November 16, 1988Date of Patent: December 5, 1989Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kensei Yoshikawa, Yutaka Ohuchi, Kazuto Sekiuchi, Shiuji Saito, Katsuo Hatayama, Kaoru Sota
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Patent number: 4883793Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 9, 1988Date of Patent: November 28, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Gerard J. O'Malley
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Patent number: 4877808Abstract: The present invention relates, by way of novel industrial products, to osides selected from the group consisting of:(i) the .beta.-D-phenylthioxylosides of the formula: ##STR1## in which: R represents a hydrogen atom, a halogen atom, a nitro group or a cyano group,A represents the sulfur atom or the oxygen atom,B represents a CH.sub.2, CHOH or CO group andY represents the hydrogen atom or an acyl group; and(ii) epimers thereof when B is CHOH.These products are useful in therapy as antithrombotics.Type: GrantFiled: April 25, 1988Date of Patent: October 31, 1989Assignee: Fournier Innovation et SynergieInventors: Soth Samreth, Francois Bellamy, Jean Millet
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Patent number: 4855455Abstract: A hydroxy-carboxylate ester is converted to an amino-acid-amide by replacement of the --OH group with --N.sub.3, via, e.g., CH.sub.3 SO.sub.2 Cl and NaN.sub.3 ; reacting with amine to convert the ester to amide; and hydrogenating --N.sub.3 to --NH.sub.2. The present process alleviates the conventional use of blocking-deblocking procedures.Type: GrantFiled: January 22, 1988Date of Patent: August 8, 1989Assignee: W. R. Grace & Co.-Conn.Inventor: Robert J. Kupper
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Patent number: 4853410Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.Type: GrantFiled: October 9, 1987Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4853151Abstract: Dispirotetradecanes of the formula I ##STR1## wherein R.sup.1 and R.sup.2 are each independently of each other alkyl containing 1 to 12 carbon atoms wherein one or more non-adjacent CH.sub.2 groups may also be replaced by --O--, --CO--, --CO--O--, --O--CO--, --O--COO-- and/or --CH.dbd.CH-- (trans), one of the radicals R.sup.1 and R.sup.2 also being H, F, Cl, Br, I, CN, NO.sub.2, NCS,A.sup.1 and A.sup.2 are each independently of each other trans-1,4-cyclohexylene wherein one or two non-adjacent CH.sub.2 groups may be replaced by --O-- and/or --S--, or 1,4-phenylene wherein one or more CH groups may also be replaced by N, with it also being possible optionally for A.sup.1 and A.sup.2 to be substituted laterally or axially by F, Cl, CN, CH.sub.3,Z.sup.1 and Z.sup.2 are each independently of each other --C--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 -- or a single bond,m and n are each 0, 1 or 2,(m+n) 0, 1 or 2,X.sup.1, X.sup.2, X.sup.3 and X.sup.Type: GrantFiled: August 11, 1987Date of Patent: August 1, 1989Assignee: Merck Patent Gesellschaft Mit Beschrankfter HaftungInventors: Fritz Vogtle, Wolfgang Calaminus
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Patent number: 4842638Abstract: Tetrahydro(thio)pyran-2,4-dione derivatives of the formula ##STR1## where R.sup.1 is hydrogen, a cation, alkylcarbonyl, C.sub.2 -C.sub.10 -alkenylcarbonyl, or benzoyl which is unsubstituted or substituted by alkyl, R.sup.2 is alkyl, R.sup.3 is a non-aromatic, unsubstituted or alkyl-substituted heterocyclic compound of 5 to 7 ring members and having at most one double bond in the heterocyclic ring, X is oxygen or sulfur, and Z is oxygen or the radical NO--R.sup.4, R.sup.4 denoting alkyl, alkenyl, alkynyl, haloalkyl, hal oalkenyl, alkoxyalkyl or the radical CH.sub.2 --R.sup.5, where R.sup.5 is a he terocyclic compound of 5 ring members and containing from 1 to 3 hetero-atoms and from 0 to 2 double bonds and bearing either no substituents or one or two substituents selected from the group consisting of alkyl, alkoxy, halogen, trifluoromethyl, alkoxymethyl, alkylthiomethyl and vinyl, or R.sup.Type: GrantFiled: January 12, 1988Date of Patent: June 27, 1989Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Michael Keil, Dieter Kolassa, Ulrich Schirmer, Bruno Wuerzer, Norbert Meyer, Wilhelm Rademacher, Johann Jung
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Patent number: 4810717Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: March 10, 1986Date of Patent: March 7, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier
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Patent number: 4808733Abstract: An intermediate compound having the structural formula ##STR1## wherein X is oxygen or sulfur;R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.n --wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.1 and R.sup.3 together are alkylene having 2-5 cation atoms; orR.sup.2 and R.sup.4 together are alkylene having 2-5 carbon atoms; andR.sup.5 and R.sup.6 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifuoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n --wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.C R.sup.d wherein R.Type: GrantFiled: December 21, 1987Date of Patent: February 28, 1989Assignee: Stauffer Chemical CompanyInventors: Christopher G. Knudsen, William J. Michaely, Donald R. James, Hsiao-Ling M. Chin
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Patent number: 4806604Abstract: The present invention discloses a new class of calcium chelating compounds which have a decreased affinity for calcium following illumination. These new compounds contain a photolabile nitrobenzyl derivative coupled to a tetracarboxylate Ca.sup.2+ chelating parent compound having the octacoordinate chelating groups characteristic of EGTA or BAPTA. However unlike EGTA or BAPTA-like compounds, in which the two halves of the chelator are linked by a simple 1,2-ethanediyl moiety, the compounds of the present invention modify the stereochemical conformation of this linkage by adding bulky substituents or incorporating the linkage into a carbocyclic or heterocyclic ring. In a first form, the new compounds are comprised of a BAPTA-like chelator coupled to a single 2-nitrobenzyl derivative, which in turn is a photochemical precursor of a 2-nitrosobenzophenone.Type: GrantFiled: May 13, 1987Date of Patent: February 21, 1989Assignee: Regents of the University of CaliforniaInventors: Roger Yonchien Tsien, Stephen R. Adams
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Patent number: 4803286Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.Type: GrantFiled: August 19, 1987Date of Patent: February 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
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Patent number: 4797456Abstract: Water-soluble sulfonium salts are converted, without the elimination of odorous volatile by-products, to water-insoluble products useful as binders in coating formulations by heating a water-soluble cyclic sulfonium salt in which the sulfonium sulfur is bonded only to aliphatic carbons.Type: GrantFiled: December 9, 1982Date of Patent: January 10, 1989Assignee: The Dow Chemical CompanyInventors: Ritchie A. Wessling, Donald L. Schmidt, Kiyoshi I. Aikawa
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Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
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Patent number: 4780124Abstract: Compounds having the formula ##STR1## wherein X is sulfur;R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together form a single bond; orR.sup.1 and R.sup.3 together are alkylene having 2-5 carbon atoms; orR.sup.2 and R.sup.4 together are alkylene having 2-5 carbon atoms; andR.sup.5 and R.sup.6 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.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10)--NR.sup.Type: GrantFiled: December 21, 1987Date of Patent: October 25, 1988Assignee: Stauffer Chemical CompanyInventors: Christopher G. Knudsen, William J. Michaely, Donald R. James, Hsiao-Ling M. Chin
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Patent number: 4777272Abstract: Compounds of the formula ##STR1## wherein X is oxygen, sulfur or sulfonyl;R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.m - wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together are alkylene having 2 to 5 carbon atoms;R.sup.5 and R.sup.6 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.n -wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.Type: GrantFiled: November 13, 1987Date of Patent: October 11, 1988Assignee: Stauffer Chemical CompanyInventors: Charles G. Carter, Jeff K. Curtis
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Patent number: 4758369Abstract: There are disclosed novel, highly stable sulfone peroxycarboxylic acids useful in detergent compositions alone or as bleaching agents which are represented by the formula ##STR1## wherein A and B are organic moieties bonded to the sulfur atom by a carbon atom and at least one of A and B containing at least one ##STR2## group bonded to a carbon atom.Type: GrantFiled: September 17, 1987Date of Patent: July 19, 1988Assignee: Monsanto CompanyInventors: David R. Dyroff, Daniel P. Getman, Joan K. Glascock
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Patent number: 4757153Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, --O(CH.sub.2).sub.n phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.Type: GrantFiled: July 14, 1986Date of Patent: July 12, 1988Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Daniel R. Pilipauskas, Michael Clare
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Patent number: 4741755Abstract: Compounds having the formula ##STR1## wherein X is oxygen or sulfur;R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together form a single bond; orR.sup.1 and R.sup.3 together are alkylene having 2-5 carbon atoms; orR.sup.2 and R.sup.4 together are alkylene having 2-5 carbon atoms; andR.sup.5 and R.sup.6 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.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.Type: GrantFiled: June 9, 1986Date of Patent: May 3, 1988Assignee: Stauffer Chemical CompanyInventors: Christopher G. Knudsen, William J. Michaely, Donald R. James, Hsiao-Ling M. Chin
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Patent number: 4728745Abstract: Compounds of the formula ##STR1## wherein X is oxygen, sulfur or sulfonyl;R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.m -- wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together are alkylene having 2 to 5 carbon atoms;R.sup.5 and R.sup.6 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.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.Type: GrantFiled: June 9, 1986Date of Patent: March 1, 1988Assignee: Stauffer Chemical CompanyInventors: Charles G. Carter, Jeff K. Curtis
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Patent number: 4725682Abstract: Sulfur-containing bis-amino carbamate compounds exhibit outstanding acaricidal, nematocidal and insecticidal activity.Type: GrantFiled: December 2, 1986Date of Patent: February 16, 1988Assignee: Rhone-Poulenc Nederland, B.V.Inventor: Themistocles D. J. D'Silva
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Patent number: 4701536Abstract: Disclosed are a compound of Formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a protective group for a hydroxyl group; and Z represents a direct bond (2,3-cis-5R*, 8S*) or an oxygen atom which forms an oxirane ring having a configuration of (2R*, 3R*, 5R*, 8S*),and a process for preparing the same.By use of the above compound as an intermediate, there can be synthesized periplanone-B which is a sex pheromone of periplaneta.Type: GrantFiled: July 7, 1986Date of Patent: October 20, 1987Assignee: UBE Industries, Ltd.Inventors: Jiro Tsuji, Takashi Takahashi
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Patent number: 4638060Abstract: Antibacterial activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 29, 1985Date of Patent: January 20, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, William H. Koster, Robert Zahler
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Patent number: 4638064Abstract: Unsaturated heterocyclic carbonyl-containing compounds, such as 2-oxathiolone, are prepared by the oxylation of saturated heterocyclic carbonyl-containing precursors of the above compounds in a C.sub.1-4 alcohol or carboxylic acid solvent in the presence of a supporting electrolyte followed by dehydroxylation of the oxylated intermediate.The products formed may be polymerized or copolymerized with other ethylenically unsaturated monomers to prepared resins, films, etc. or they may be employed as reaction intermediates.Type: GrantFiled: April 1, 1985Date of Patent: January 20, 1987Assignee: The Dow Chemical CompanyInventors: Pen-Chung Wang, James M. Renga
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Patent number: 4636245Abstract: Novel substituted tetrahydrothiopyran-2,4-dione herbicides of the formula ##STR1## in which R.sup.1 is hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, cycloalkyl or optionally substituted aryl,R.sup.2 is alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, halogenoalkenyl, alkoxycarbonylalkyl, alkoximinoalkyl, optionally substituted aralkyl or optionally substituted heterocyclylalkyl, andR.sup.3 and R.sup.4 each independently is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, optionally substituted aryl, optionally substituted aryloxyalkyl or optionally substituted aralkyl,or metal salts thereof.Type: GrantFiled: May 23, 1985Date of Patent: January 13, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Wroblowsky, Jorg Stetter, Ludwig Eue, Robert R. Schmidt, Hans-Joachim Santel
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Patent number: 4628060Abstract: Novel substituted tetrahydrothiopyran-3,5-dione-4-carboxamide fungicides of the formula ##STR1## in which R is alkyl, cycloalkyl, optionally substituted aralkyl or optionally substituted aryl,R.sup.1, R.sup.2 and R.sup.3 each independently is hydrogen or alkyl, andR.sup.4 is alkyl,excepting the compounds in whichR.sup.1 and R.sup.3 are hydrogenR.sup.4 is methyl,R is alkyl, phenyl or phenyl which is substituted by halogen and/or methyl, andR.sup.2 is hydrogen, or methyl.Many of the intermediates are also new.Type: GrantFiled: May 2, 1984Date of Patent: December 9, 1986Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Wolfgang Kramer, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4612036Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where A is an unsubstituted or substituted, saturated or unsaturated 4-membered to 7-membered ring which contains 1 or 2 sulfinyl or sulfonyl groups, R.sup.1 is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, R.sup.2 is alkyl and R.sup.3 is alkyl, alkenyl, haloalkenyl or propargyl, and salts of these compounds are used for controlling undesirable plant growth.Type: GrantFiled: July 2, 1985Date of Patent: September 16, 1986Assignee: BASF AktiengesellschaftInventors: Dieter Jahn, Rainer Becker, Michael Keil, Bruno Wuerzer
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Patent number: 4612326Abstract: Sulfur-containing bis-amino carbamate compounds exhibit outstanding acaricidal, nematocidal and insecticidal activity.Type: GrantFiled: June 18, 1982Date of Patent: September 16, 1986Assignee: Union Carbide CorporationInventor: Themistocles D. D'Silva
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Patent number: 4602935Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where R.sup.1 is alkyl, R.sup.2 is alkyl, unsubstituted or halogen-substituted alkenyl or alkynyl, X is a saturated or unsaturated five-membered or six-membered heterocyclic structure which carries one or more substituents, and Z is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, and salts of these compounds are used for controlling undesirable plant growth.Type: GrantFiled: July 6, 1984Date of Patent: July 29, 1986Assignee: BASF AktiengesellschaftInventors: Rainer Becker, Dieter Jahn, Michael Keil, Walter Himmele, Bruno Wuerzer
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Patent number: 4594430Abstract: Geminal dinitro compounds are prepared by reacting an organic nitro compound having a replaceable hydrogen on the carbon to which the nitro group is attached with a source of nitrite ions in the presence of an oxidizing agent and a catalytic amount of an alkali metal ferricyanide.Type: GrantFiled: January 31, 1985Date of Patent: June 10, 1986Assignee: United States of America as represented by the Secretary of the Air ForceInventors: Vytautas Grakauskas, Lee C. Garver, Kurt Baum
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Patent number: 4585793Abstract: Certain novel heterocyclic compounds, aromatic thioesters, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity and in the treatment of diseases such as emphysema which involve tissue proteolysis.Type: GrantFiled: May 9, 1983Date of Patent: April 29, 1986Assignee: Georgia Tech Research InstituteInventor: James C. Powers
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Patent number: 4559344Abstract: The invention relates to new pyridine-pyrimidinone derivatives corresponding to the following general formula ##STR1## wherein R.sup.1 represents linear C.sub.1-6 alkyl or cycloalkyl and R.sup.2 represents linear C.sub.1-6 alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom form a pyrrolidine or piperidine ring;Alk represents a linear alkylene chain C.sub.1-6 ;Q represents a benzene ring, furan ring, thiophene ring or thiazole ring;X represents oxygen, Y is a single bond and m is 2, 3 or 4 when Q represents benzene;X represents methylene, Y represents sulfur and m is 2 or 3 when Q is furan, thiophene or thiazole; andR.sup.3 represents a hydrogen atom or a lower alkyl group.These compounds show improved H.sub.2 -antagonistic activity.Type: GrantFiled: January 26, 1984Date of Patent: December 17, 1985Assignee: Ludwig Heumann & Co. GmbHInventors: Helmut Schickaneder, Peter Morsdorf, Stefan Postius, Istvan Szelenyi, Rolf Herter, Herbert Hansen, Kurt H. Ahrens
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Patent number: 4555396Abstract: Disclosed herein is an improvement in a method for distinguishing cells in a biological sample by staining with a dye, wherein the improvement comprises employing as the dye a compound of the formula ##STR1## wherein G is O or S;R.sup.1, R.sup.3, and R.sup.5 are independently selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, amino, styryl, bis(diaryl)vinylene, and ##STR2## wherein R is hydrogen or alkyl;Z represents the elements necessary to complete a basic heterocyclic ring system of the type used in cyanine dyes;n is 0 or 1;R.sup.2 is hydrogen or, taken together with either R.sup.1 or R.sup.3, represents the elements needed to complete an aromatic or a carbocyclic ring system;R.sup.4 is hydrogen or, taken together with either R.sup.3 or R.sup.5, represents the elements needed to complete an aromatic or a carbocyclic ring system; andX.sup.- is an anion.Type: GrantFiled: December 22, 1982Date of Patent: November 26, 1985Assignee: Eastman Kodak CompanyInventors: David S. Frank, Robert T. Belly
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Patent number: 4551472Abstract: Unsymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.Type: GrantFiled: January 9, 1984Date of Patent: November 5, 1985Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4508911Abstract: 1,2-Cycloaliphatic diamines and protected diamines of the formulas II and IIa ##STR1## and ##STR2## wherein the wavy line bonds, p, n, R, R.sub.1, R.sub.2, Z, m and Q are as defined in the specification, e.g., (.+-.)-(5.xi.,6.alpha.,7.beta.)-1-[6-methylamino-1-oxaspiro[4.5]dec-7-yl]p yrrolidine, are disclosed and claimed herein. These diamines and protected diamines are useful as intermediates for preparing mono-oxa, and thiaspirocyclic-benzene acetamide and benzamide analgesic compounds.Type: GrantFiled: February 14, 1984Date of Patent: April 2, 1985Assignee: The Upjohn CompanyInventor: Lester J. Kaplan