Substituent Q Is Alkyl Patents (Class 564/98)
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Patent number: 6015822Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastro-intestinal region or for the treatment of diarrheal illnesses.Type: GrantFiled: November 9, 1998Date of Patent: January 18, 2000Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
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Patent number: 5968916Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.Type: GrantFiled: January 12, 1998Date of Patent: October 19, 1999Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Peter Gerrard Ruminski, Gopichand Yalamanchili
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Patent number: 5965588Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 26, 1998Date of Patent: October 12, 1999Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5830917Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 11, 1995Date of Patent: November 3, 1998Assignee: G. D. Searle & Co.Inventors: William M. Moore, E. Ann Hallinan
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Patent number: 5789618Abstract: A method for synthesizing a halogen-containing condensation product, the method comprising the step of:reacting a compound represented by Formula (I) with a compound represented by Formula (II) or (III) in the presence of a halogenating agent whereby dehydration condensation and halogenation are carried out, ##STR1##Type: GrantFiled: June 27, 1996Date of Patent: August 4, 1998Assignee: Konica CorporationInventors: Eisaku Katoh, Osamu Ishige
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Patent number: 5760064Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 6, 1997Date of Patent: June 2, 1998Assignee: G.D. SearleInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5739085Abstract: O-(Oximino)ethylcyclohexenone oxime ethers I ##STR1## (R.sup.1 and R.sup.2 =C.sub.1 -C.sub.6 -alkyl; R.sup.3 =unsubstituted or substituted phenyl, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.3 -C.sub.4 -alkynyl, which in each case can be substituted by halogen, C.sub.1 -C.sub.3 -alkyl, unsubstituted or substituted phenyl or unsubstituted or substituted phenoxy;R.sup.4 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, unsubstituted or substituted phenylthio-C.sub.1 -C.sub.6 -alkyl, N-(C.sub.1 -C.sub.4 -alkylsulfonyl)-N-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, unsubstituted or substituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: May 5, 1995Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5716980Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: February 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5705691Abstract: A process for the preparation of an N-(alkylsulphonyl)amide, the process comprising reacting a primary amide with a sulphonyl halide in the presence of a base which is sufficiently strong to cause at least partial deprotonation of the amide.Type: GrantFiled: July 8, 1996Date of Patent: January 6, 1998Assignee: Zeneca LimitedInventors: Stephen M. Brown, James P. Muxworthy, Gareth DeBoos
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Patent number: 5684195Abstract: A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.Type: GrantFiled: May 31, 1995Date of Patent: November 4, 1997Assignee: G. D. Searle & Co.Inventors: Horng-Chih Huang, Scott R. Harring
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Patent number: 5665877Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: May 17, 1996Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
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Patent number: 5639769Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 17, 1996Date of Patent: June 17, 1997Assignee: G.D. Searle and Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5618976Abstract: A process is disclosed for the conversion of an ammonium or amine salt of an alkanesulfonic acid to its corresponding alkanesulfonamide by heating the salt to at least its melting point to remove the water by-product and recover an alkanesulfonamide.Type: GrantFiled: March 6, 1996Date of Patent: April 8, 1997Assignee: Elf Atochem North America, Inc.Inventor: Stanley R. Sandler
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Patent number: 5614647Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: May 25, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
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Patent number: 5612339Abstract: 2-Hydroxy-3-aminopropylsulfonamides are provided along with methods for synthesizing and using such compounds, and chemical intermediates employed in the synthetic methods.Type: GrantFiled: January 17, 1995Date of Patent: March 18, 1997Assignee: Trustees Of The University Of PennsylvaniaInventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
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Patent number: 5599983Abstract: A method is disclosed for the preparation of alkanesulfonamide containing low amounts of ammonium or alkylammonium-salt impurities wherein alkanesulfonamide is treated with a base to convert ammonium or alkylammonium-salt impurities to their corresponding base salts and to liberate neutral amine or ammonia.Type: GrantFiled: August 21, 1995Date of Patent: February 4, 1997Inventors: Gary S. Smith, Robert Cordova, Thomas H. Overgaard, Marc T. Budrick
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Patent number: 5599982Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.Type: GrantFiled: March 30, 1995Date of Patent: February 4, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons G. M. De Knaep, Luc J. R. Moens, Eduard J. C. Vreysen
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Patent number: 5587513Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.Type: GrantFiled: January 20, 1995Date of Patent: December 24, 1996Inventors: Klaus Pohmer, Rainer Weber, Cornelia D orzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
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Patent number: 5521219Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 24, 1993Date of Patent: May 28, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5514717Abstract: Novel 3,4,4-trifluorobutenoic acid derivatives of the formula ##STR1## wherein Q is --(C.dbd.W)--R.sub.2 wherein W is O or S, and R.sub.2 is an aliphatic or aromatic group when W.dbd.O; --OR.sub.50 ; --SR.sub.50 ; or --NR.sub.50 R.sub.60 wherein R.sub.60 is hydrogen or R.sub.50 ; NR.sub.7 R.sub.8 ; a heterocyclic group; phenyl substituted by alkyl; or any agronomically acceptable salt thereof having usefulness as nematocides, insecticides and acaricides.Type: GrantFiled: October 26, 1994Date of Patent: May 7, 1996Assignee: Monsanto CompanyInventors: Dennis P. Phillion, Gopichand Yalamanchili, Peter G. Ruminski
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Patent number: 5510388Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5502251Abstract: Fluoroalkyl- and fluoroaryl-group-containing imides and their salts of general formula (I) ##STR1## wherein R.sub.F is a fluoroalkyl group with 1 to 18 carbon atoms, a fluoroaryl group with 6 to 12 carbon atoms or a mixed fluoroalkylaryl group with 7 to 18 carbon atoms, wherein the carbon chain can also be interrupted by oxygen atoms,R.sub.H is an alkyl group with 1 to 30 carbon atoms, an aryl group with 6 to 12 carbon atoms or a mixed alkylaryl group with 7 to 30 carbon atoms, wherein the carbon chain of the group can also be interrupted by oxygen, nitrogen or sulphur atoms,Y.sub.1 and Y.sub.2 independently of each other represent a ##STR2## X is a hydrogen cation or a uni- or multivalent cation, m is a whole number from 0 to 6, andz is a whole number from 1 to 7 corresponding to the charge of the cation X.Type: GrantFiled: February 1, 1995Date of Patent: March 26, 1996Assignee: Bayer AGInventors: Klaus Pohmer, Rainer Weber, Cornelia Do/ rzbach-Lange, Karlheinz Stachulla, Hans-Heinrich Moretto, Manfred Wienand
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Patent number: 5481005Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: November 28, 1994Date of Patent: January 2, 1996Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5455377Abstract: A process to prepare alkansulphonamides of formula RSO.sub.2 NR.sup.1 R.sub.2 --wherein R is an alkyl group containing from 1 to 15 carbon atoms, or an alkyl group containing from 1 to 15 carbon atoms substituted by one or more chlorine or bromine atoms, and R.sup.1 and R.sup.2 are equal or different and may be hydrogen or an alkyl group containing from 1 to 15 carbon atoms--provides to treat an alkansulphonylhalide of formula RSO.sub.2 X--wherein X is chlorine, bromine or iodine--with a suitable quantity of a compound of formula NHR.sup.1 R.sup.2, using as solvent for said treatment an aliphatic nitrile.Type: GrantFiled: July 12, 1994Date of Patent: October 3, 1995Assignee: Oxon Italia S.p.A.Inventors: Nello Ronchi, Edoardo Pallucca, Daniele Tarallo, Claudio Ornati
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Patent number: 5403853Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: June 13, 1994Date of Patent: April 4, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5389633Abstract: Novel compound represented by the formula: ##STR1## wherein R.sup.1 stands for H, an optionally substituted lower alkyl group or a halogen; R.sup.2 and R.sup.3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C.dbd.C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO.sub.2 ; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.Type: GrantFiled: March 17, 1993Date of Patent: February 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
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Patent number: 5262564Abstract: The subject invention provides for novel anti-tumor and anti-retroviral compounds. More specifically, the invention relates to the sulfinic acid adducts of therapeutic C-nitroso compounds. The formation of the adducts increases the stability and more solubility of the C-nitroso compounds. These compounds include the L-cysteinesulfinic acid adducts of 6-nitroso-1,2-benzopyrone and 3-nitrosobenzamide. The invention also provides for compositions containing one or more of the compounds, and for methods of treating retroviral infections, cancer, infectious virus concentration with the subject compounds and compositions.Type: GrantFiled: October 30, 1992Date of Patent: November 16, 1993Assignee: Octamer, Inc.Inventors: Ernest Kun, Jerome Mendeleyev
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Patent number: 5217855Abstract: A photographic processing composition containing at one compoud represented by formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an aliphatic group, or an aromatic group, L.sub.1 and L.sub.2 each represents a divalent bonding group including an alkylene group and/or an arylene group; X represents a ##STR2## group (wherein R.sub.a, R.sub.b and R.sub.c each represents a hydrogen atom, an aliphatic group or an aromatic group, and R.sub.d represents an aliphatic group or an aromatic group); and Y represents a carboxy group, a hydroxy group, a phosphono group, a sulfo group or a salt thereof. The processing composition does not produce precipitate or sludge even when contaminated by metallic ions. A processing method using the processing composition is also disclosed.Type: GrantFiled: July 25, 1991Date of Patent: June 8, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Morio Yagihara, Shigeru Nakamura
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Patent number: 5210299Abstract: A method for the production of N-(2-chloroethyl) methanesulfonamide of high purity, which method comprises causing methanesulfonyl chloride to react with ethylene imine in the presence of ethylene dichloride and then distilling there resultant reaction mixture thereby separating therefrom N-(2-chloroethyl) methanesulfonamide, if necessary subjecting the resultant reaction mixture to extraction from water, separating the aqueous layer consequently formed, and subjecting the organic layer resulting from said extraction to distillation thereby separating N-(2-chloroetyl) methanesulfonamide.Type: GrantFiled: February 10, 1992Date of Patent: May 11, 1993Assignee: Nippon Shokubai Co., Ltd.Inventors: Yujiro Goto, Mitsuaki Yagisawa, Masao Kitano
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Patent number: 5166431Abstract: A method for the preparation of alkanesulfonamides in high purity and high yield using solvents selected from C.sub.3 to C.sub.8 cyclic ethers or mixtures thereof is disclosed. The final products have use as synthetic intermediates for the manufacture of useful final products.Type: GrantFiled: June 20, 1991Date of Patent: November 24, 1992Assignee: Elf Atochem North America, Inc.Inventors: Stanley R. Sandler, James S. Perilli, John F. Kennoy
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Patent number: 5159112Abstract: A process for the preparation of alkanesulfonamides is disclosed. It comprises reacting an alkanesulfonyl chloride with ammonia or with an alkylamine in the presence of a chemically inert liquid diluent. The diluent is first supersaturated with ammonia or with the alkylamine before bringing it into contact with the alkanesulfonyl chloride.Type: GrantFiled: July 24, 1991Date of Patent: October 27, 1992Assignee: Societe Nationale Elf Aquitaine (Production)Inventors: Jean Ollivier, Michele Larrouy
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Patent number: 5145996Abstract: Heteroatom containing perfluoroalkyl terminated neopentyl mercapto-alcohols of the formulas I and IIHS--[CH.sub.2 C(CH.sub.2 X--E--R.sub.f).sub.2 CH.sub.2 ]--OH (I)HS--[CH.sub.2 C(CH.sub.2 X.sub.1 --R.sub.f).sub.2 CH.sub.2 ]--OH (II)are prepared from the corresponding perfluorinated neopentyl oxetans where R.sub.f is a straight or branched chain perfluoroalkyl of 1 to 18 carbon atoms or said perfluoroalkyl substituted by perfluoroalkoxy of 2 to 6 carbon atoms, E is a linking group, and X and X.sub.1 are heteroatom moieties.The reaction products of these fluorinated mercapto-alcohols with electrophiles are disclosed as are certain functional derivatives. Compositions containing such materials provide improved thermal stability and useful low surface energy oil and water repellent coatings for textiles, glass, paper, leather, and other materials.Type: GrantFiled: February 25, 1991Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: Michael Jacobson, Kirtland P. Clark
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Patent number: 5124343Abstract: The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.Type: GrantFiled: January 6, 1988Date of Patent: June 23, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Hernd Raduechel, Werner Skuballa, Norbert Schwarz, Jorge Casals-Stenzel, Gerda Mannesmann, Michael H. Town
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Patent number: 5101072Abstract: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl. Such methylating agents are useful as antitrypanosomal and anticancer agents.Type: GrantFiled: September 6, 1989Date of Patent: March 31, 1992Assignee: Yale UniversityInventors: Alan C. Sartorelli, Alan A. Divo, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5068427Abstract: A process for the preparation of alkane- and arenesulfonamides in high purity and yield is provided. Ammonia or alkylamine is reacted under boiling conditions with an alkane- or arenesulfonyl halide in the absence of an added solvent. The heat of reaction is dissipated by the heat of vaporization of the ammonia or alkylamine.Type: GrantFiled: November 16, 1989Date of Patent: November 26, 1991Assignee: Atochem North America, Inc.Inventors: Stanley R. Sandler, Steven G. Schon, David M. Gardner
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Patent number: 5028733Abstract: Bicyclooctane and bicycloheptane prostaglandin intermediates have been synthesized.Type: GrantFiled: December 12, 1989Date of Patent: July 2, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5025034Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: February 7, 1990Date of Patent: June 18, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4983629Abstract: 11-Haloprostane derivatives of general Formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or a --C.tbd.C--group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.Type: GrantFiled: June 21, 1989Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Claus-Steffen Sturzebecher, Walter Elger
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Patent number: 4970339Abstract: A method for the preparation of alkanesulfonamides in high purity and high yield using solvents selected from C.sub.4 to C.sub.8 cyclic ethers or mixtures thereof is disclosed. The final products have use as synthetic intermediates for the manufacture of useful final products.Type: GrantFiled: November 30, 1988Date of Patent: November 13, 1990Assignee: Atochem North America, Inc.Inventors: Stanley R. Sandler, James S. Perilli, John F. Kennoy
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Patent number: 4965279Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.Type: GrantFiled: November 18, 1988Date of Patent: October 23, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
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Patent number: 4945106Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: July 6, 1989Date of Patent: July 31, 1990Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4900867Abstract: A process for producing N-fluorosulfonamides by reaction of a sulfonamide with fluorine in a solvent mixture of halogenated hydrocarbon an nitrile is described together with new N-fluorosulfonamides which are produced in accordance with this process.Type: GrantFiled: July 2, 1987Date of Patent: February 13, 1990Assignee: Kali-Chemie AktiengesellschaftInventors: Bernd Wilkes, Dieter Naumann, Werner Rudolph, Ruediger Sander
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Patent number: 4899249Abstract: A dielectric medium composition comprising a fluorine-containing amide or a fluorine-containing sulfonamide and capacitors or other electric devices incorporating said composition, are disclosed herein.Type: GrantFiled: April 21, 1988Date of Patent: February 6, 1990Assignee: Pennwalt CorporationInventors: James L. Reilly, Ludwig K. Huber, Gordon R. Leader
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Patent number: 4870104Abstract: 11-Haloprostane derivatives of general formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH-group,B is a --CH.sub.2 --CH.sub.2 -- or trans-CH.dbd.CH-- or a --C.tbd.C-group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C-bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.Type: GrantFiled: November 12, 1986Date of Patent: September 26, 1989Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Claus-Steffen Sturzebecher, Walter Elger
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Patent number: 4852989Abstract: This invention relates to bleaching compounds and compositions that provide effective and efficient surface bleaching of textiles over a wide range of bleach solution temperatures. The bleaching compounds of the invention yield a peroxyacid with a polar amide link in the hydrophobic chain when used in the bleaching compositions. In a preferred embodiment, the bleaching compositions of the invention are also detergent compositions.Type: GrantFiled: May 8, 1987Date of Patent: August 1, 1989Assignee: The Procter & Gamble CompanyInventors: Michael E. Burns, Frederick E. Hardy
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Patent number: 4824996Abstract: There are disclosed compounds of the formulaR.sup.1 -XwhereinR.sup.1 is alkyl of 8-22 carbon atoms;X is ##STR1## R.sup.2 is --(CH.sub.2).sub.n NR.sup.4 R.sup.5 ; R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or lower alkyl;R.sup.5 is hydrogen or lower alkyl; andn is 0-7, with the proviso that when X is ##STR2## n is 6-7; and their use in the prevention and/or treatment of conditions such as allergic rhinitis, allergic bronchial asthma and other naso-bronchial obstructive air-passageway conditions, other immediate hypersensitivity reactions such as allergic conjunctivitis and various inflammatory conditions.Type: GrantFiled: November 6, 1986Date of Patent: April 25, 1989Assignee: American Home Products CorporationInventors: William H. McGregor, Joseph Y. Chang
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Patent number: 4816576Abstract: The invention relates to a sulphonic acid amidamine corresponding to the following general formula I: ##STR1## wherein R.sup.1 represents a C.sub.8 -C.sub.30 linear, saturated aliphatic hydrocarbon group or said group which is substituted by one or more chlorine atoms;R.sup.2 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkyl which is substituted with one of the groups: hydroxyl, amino, mercapto, cyano, carboxyl or carbamoyl, and/or is interrupted by at least one oxy (--O--) or thio (--S--) group;R.sup.3 and R.sup.4 independently represent C.sub.2 -C.sub.13 alkylene or C.sub.5 -C.sub.7 cycloalkylene or said alkylene or cycloalkylene groups which are substituted with one of the groups: hydroxyl, amino, mercapto, cyano, carboxyl or carbamoyl;p represents zero or an integer of from 1 to 3;q represents zero or an integer of from 1 to 12; andn represents an integer of from 1 to 8.Type: GrantFiled: June 23, 1986Date of Patent: March 28, 1989Assignee: Bayer AkteingesellschaftInventors: Hans-Josef Buysch, Wolfgang Wellner, Hermann Gruber
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Patent number: 4812463Abstract: Alkane sulfonamides with an electron withdrawing function .beta. to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.Type: GrantFiled: December 10, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Thomas H. Scholz
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Patent number: 4780504Abstract: Novel supports useful in solid phase synthesis of oligonucleotides of the formula ##STR1## wherein .circle. is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene of 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x is an integer from 0 to 20, x.sub.1 is an integer from 0 to 10 and the amino group may be in the m-, p- or o-position, a process for the preparation of said supports, the use of said supports and intermediates.Type: GrantFiled: June 5, 1986Date of Patent: October 25, 1988Assignee: Roussel UclafInventors: Jean Buendia, Jeanine Nierat