Sulfonyl Or Sulfinyl In Acid Moiety Patents (Class 560/150)
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Patent number: 7304175Abstract: The present invention provides a salt of the formula (I) wherein X represents —OH or —Y—OH, n shows an integer of 1 to 9, A+ represents an organic counter ion, Y represents a divalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms. The present invention also provides a chemically amplified resist composition comprising the salt of the formula (I).Type: GrantFiled: February 14, 2006Date of Patent: December 4, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Yukako Harada, Ichiki Takemoto, Kouji Toishi
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Patent number: 7301047Abstract: The present invention provides a salt of the formula (I): wherein ring X represents monocyclic or bicyclic hydrocarbon group having 3 to 30 carbon atoms, and one or more hydrogen atom in the ring X is optionally substituted with alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, alkoxy group having 2 to 6 carbon atoms or perfluoroalkyl group having 1 to 4 carbon atoms; Q1 and Q2 each independently represent fluorine atom or perfluoroalkyl group having 1 to 6 carbon atoms; A+ represents organic counter ion; and n shows an integer of 1 to 12. The present invention also provides a chemically amplified resist composition comprising the salt of the formula (I).Type: GrantFiled: October 26, 2006Date of Patent: November 27, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Isao Yoshida, Yukako Harada, Satoshi Yamaguchi
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Patent number: 7262321Abstract: The present invention provides a salt of the formula (I): wherein X represents divalent or trivalent residue of acyclic hydrocarbon having 1 to 30 carbon atoms or divalent or trivalent residue of hydrocarbon having 3 to 30 carbon atoms which contains monocyclic or bicyclic ring, wherein —CH2— in the hydrocarbon may be substituted with —O— and one or more hydrogen atom in X is optionally substituted with alkoxy group having 1 to 6 carbon atoms, perfluoroalkyl group having 1 to 4 carbon atoms, hydroxyalkyl group having 1 to 6 carbon atoms, hydroxyl group or cyano group; Q1 and Q2 each independently represent fluorine atom or perfluoroalkyl group having 1 to 6 carbon atoms; A+ represents organic counter ion; Y represents hydroxyl group, cyano group or methoxy group; and n shows 1 or 2. The present invention also provides a chemically amplified resist composition comprising the salt of the formula (I).Type: GrantFiled: September 7, 2006Date of Patent: August 28, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Yukako Harada, Isao Yoshida, Yoshiyuki Takata
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Patent number: 6949670Abstract: A fluorocompound denoted by general formula (1) below (wherein R1 denotes a substituted or unsubstituted alkyl group having a total of at least six carbon atoms, with R1 not being an alkyl group substituted with a fluorine atom; Rf denotes a perfluoroalkyl group having not more than six carbon atoms; either X1 or X2 denotes a hydrogen atom and the other denotes SO3M; M denotes a cation; and n denotes an integer of not less than 1) was disclosed. A silver halide photographic light-sensitive material having at least one layer comprising a light-sensitive silver halide emulsion layer on a support and comprising a compound denoted by general formula (1) above was also disclosed.Type: GrantFiled: May 28, 2003Date of Patent: September 27, 2005Assignee: Fuji Photo Film Co., Ltd.Inventors: Junichi Yamanouchi, Terukazu Yanagi, Tomokazu Yasuda
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Patent number: 6927236Abstract: The present invention relates to compounds of the formula which are formed during fermentation by the microorganism Coniochaeta ellipsoidea Udagawa, DSM 13856, or by one of its mutations and/or variants, and chemically derivatized if appropriate. The invention furthermore relates to a process for preparing compounds of the formula (I), and to their use as pharmaceuticals. In addition, the invention relates to the use of a compound of the formula (VI) for producing a pharmaceutical for the treatment and prophylaxis of degenerative neuropathics or of Alzheimer's disease.Type: GrantFiled: September 19, 2002Date of Patent: August 9, 2005Assignee: Aventis Pharma Deutschland GmbH.Inventors: Laszlo Vertesy, Klaus Ehrlich, Michael Kurz, Marian Paul Segeth, Luigi Toti
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Patent number: 6916850Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: GrantFiled: May 3, 2002Date of Patent: July 12, 2005Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Guy Miller, Wei Zhang
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Publication number: 20040106821Abstract: Lubricating agent containing fluorinated urethanes Lubricants comprising fluorinated urethanes, prepared by reactingType: ApplicationFiled: June 10, 2003Publication date: June 3, 2004Inventors: Ralf Grottenmuller, Norbert Schmitt, Anton Probst
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Patent number: 6703521Abstract: Compounds of formula CH2Y—CH(COOR1)—O—CF2CF2—SO2F, usable in the synthesis of the fluorosulphonic vinylether —CF2═CF—O——CF2CF2—SO2F.Type: GrantFiled: December 27, 2002Date of Patent: March 9, 2004Assignee: Ausimont S.p.A.Inventors: Vito Tortelli, Sara Maculan
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Publication number: 20030229053Abstract: the present invention provides novel compounds represented by formula I: 1Type: ApplicationFiled: June 11, 2002Publication date: December 11, 2003Applicant: Shire BioChem Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
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Publication number: 20030220508Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: September 9, 2002Publication date: November 27, 2003Applicant: 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: 6552079Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.Type: GrantFiled: May 15, 2001Date of Patent: April 22, 2003Assignee: Eli Lilly and CompanyInventors: Robert M. Scarborough, Mark Smyth, Ting Su, Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffry Bernard Franciskovich
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Patent number: 6534495Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.Type: GrantFiled: October 26, 1999Date of Patent: March 18, 2003Assignee: Akzo NebelInventor: Anton Egbert Peter Adang
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Patent number: 6274758Abstract: A process for the preparation of an enantioenriched sulfone of formula (1), which comprises asymmetric hydrogenation of vinyl sulfone of formula (2) wherein R1 and R2 are each independently a hydrocarbon group of less than 20 carbons atoms, optionally substituted at any position, or either of R1 and R3 is H, and X is a coordinating group, in the presence of a stereoselective chiral catalyst.Type: GrantFiled: September 24, 1998Date of Patent: August 14, 2001Assignee: Darwin Discovery, Ltd.Inventors: Jane Marie Paul, Christopher Palmer
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Patent number: 6245922Abstract: A photoactive compound that is the reaction product of an alkenyl azlactone compound and a nucleophilic aromatic ketone is described. Mer units derived from this compound can be used, for example, to crosslink via a hydrogen abstracting mechanism acrylic polymers in which they are incorporated.Type: GrantFiled: November 19, 1996Date of Patent: June 12, 2001Assignee: 3M Innovative Properties CompanyInventors: Steven M. Heilmann, Gaddam N. Babu, Larry R. Krepski, Howell K. Smith, II, Daniel E. Mickus
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Patent number: 6229025Abstract: The present invention relates to a process for alkylating hindered sulfonamides by Michael addition to propiolates, and to novel intermediates prepared in said process. The products of these reactions can be converted into pharmaceutical compounds useful in the treatment of disease states mediated by matrix metalloproteinase enzymes. Novel intermediates prepared according to the present invention include compounds of the formula wherein R1 is (C1-C6)alkyl or optionally substituted benzyl; R2 and R3 are independently (C1-C6)alkyl or R2 and R3 are taken together to form a three to seven membered cycloalkyl, pyran-4-yl ring or a bicyclo ring of the formula wherein the asterisk indicates the carbon atom common to R2 and R3; and group Q is as herein described.Type: GrantFiled: April 9, 1999Date of Patent: May 8, 2001Assignee: Pfizer IncInventor: Joel Michael Hawkins
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Patent number: 6211400Abstract: The present invention relates to sulfinic acid compounds of the formula (I) where the substituents are as defined in the description. The novel sulfinic acid compounds can be used as reducing agents which do not eliminate formaldehyde.Type: GrantFiled: May 27, 1999Date of Patent: April 3, 2001Assignee: L. Bruggemann KGInventors: Josef Berghofer, Harry Rothmann
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Patent number: 6201122Abstract: Novel fluoroaliphatic radical-containing anionic sulfonamido compounds, methods of preparation and methods of use, including use as surfactants, are disclosed. Said compounds are conveniently prepared by the Michael addition of a fluoroaliphatic radical-containing compound to an ethylenically unsaturated compound.Type: GrantFiled: December 8, 1992Date of Patent: March 13, 2001Assignee: 3M Innovative Properties CompanyInventor: Rudolf J. Dams
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Patent number: 6180826Abstract: New water-soluble polyperfluoroalkyl surfactants derived from functional polycarboxylic polymers, characterized by the fact they have alco-oleophobic properties, to be used in the make-up of protein or synthetic foam for extinguishing fires caused not only by hydrocarbons, but also by polar liquids (alcohol, ethers, esters, etc.) without requiring the use of thickening agents, such as polysaccharides.Type: GrantFiled: January 30, 1998Date of Patent: January 30, 2001Assignee: Laboratoire 3 SInventors: Istvan Szonyi, Stephane Szonyi, Francois Szonyi
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Patent number: 6180667Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: March 28, 1997Date of Patent: January 30, 2001Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria Ornella Tinti, Nazareno Scafetta
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6153609Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: February 16, 1999Date of Patent: November 28, 2000Assignee: Pfizer IncInventors: Ralph P. Robinson, Todd A. Blumenkopf
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Patent number: 6111133Abstract: Substituted styrenes are synthesized by a simple, low temperature technique. A protected phenol styrene is reacted with an acid anhydride, dicarbonate, a halogen substituted alkyl, or an acid chloride in the presence of base to form a carbonyl substituted styrene. Unexpected yield decrease due to distillation is avoided because the product is sufficiently pure to be used without such distillation.Type: GrantFiled: September 23, 1992Date of Patent: August 29, 2000Assignee: Lucent Technologies Inc.Inventor: Francis Michael Houlihan
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Patent number: 5997610Abstract: The invention concerns amphiphilic compounds of general formula (I) ##STR1## with at least two hydrophilic and at least two hydrophobic groups based on diacarboxylic acid diamides. The amphiphilic compounds according to the invention are mostly surface-active and are suitable for use as emulsifiers, demulsifiers, detergents, dispergents and hydrotropic agents in industry and households, for example, in the treatment of metals, ore processing, surface finishing, washing, cleaning, cosmetics, medicine and food processing and preparation.Type: GrantFiled: August 18, 1997Date of Patent: December 7, 1999Assignee: Huels AktiengesellschaftInventors: Klaus Kwetkat, Wulf Ruback
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Patent number: 5889056Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.Type: GrantFiled: December 27, 1996Date of Patent: March 30, 1999Assignee: Glaxo Wellsome Inc.Inventors: Harold Francis Hodson, Richard Michael John Palmer, David Alan Sawyer, Richard Graham Knowles, Karl Witold Franzmann, Martin James Drysdale, Patricia Ifeyinwa Davies, Helen Alice Rebecca Clark, Barry George Shearer, Steven Smith
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Patent number: 5877140Abstract: The present invention relates to anionic compounds and their application in detergent compositions. The compounds have the dual benefits of surfactancy and suds suppression.Type: GrantFiled: March 20, 1997Date of Patent: March 2, 1999Inventors: Frederick Edward Hardy, Barry Thomas Ingram, Christian Leo Marie Vermote
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Patent number: 5863931Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.Type: GrantFiled: June 22, 1994Date of Patent: January 26, 1999Assignee: Glaxo Wellcome Inc.Inventors: Richard Mansfield Beams, Harold Francis Hodson, Richard Michael John Palmer
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Patent number: 5814110Abstract: Distillate fuel is treated with additives whose structure match the crystal planes of the wax which crystallizes from the fuel to produce crystals below 4000 nanometres in size, suitable additive include novel sulpho-carboxylic materials particularly their esters and amine derivatives such as the amine salts and/or amides of ortho-sulpho benzoic acid.Type: GrantFiled: November 23, 1994Date of Patent: September 29, 1998Assignee: Exxon Chemical Patents Inc.Inventors: Kenneth William Bartz, Jacqueline Dawn Bland, David Paul Gillingham, Richard Dix Kerwood, Edwin William Lehmann, Kenneth Lewtas, John Edward Maddox, Albert Rossi, Robert Dryden Tack
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Patent number: 5756822Abstract: An acetamide derivative having the general formula (I): ##STR1## or a pharmacologically acceptable salt thereof; a synthetic intermediate of the above-mentioned acetamide derivative; a treating agent for peptic ulcer and for gastritis which comprises the above-mentioned compound having the general formula (I) as an effective ingredient, and a process for treating peptic ulcer and gastritis using the above-mentioned compound having the general formula (I), are disclosed.Type: GrantFiled: April 4, 1997Date of Patent: May 26, 1998Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Nobuo Ishiyama, Toshihiro Koyama, Mitsuo Hayashida, Katsuyuki Otsuka, Masahiro Fujii, Kunio Kimura, Yoshiyuki Hata, Nobuko Miyao
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Patent number: 5739140Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.Type: GrantFiled: October 23, 1996Date of Patent: April 14, 1998Assignee: Monsanto CompanyInventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
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Patent number: 5637619Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.Type: GrantFiled: July 5, 1995Date of Patent: June 10, 1997Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5625085Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: July 14, 1994Date of Patent: April 29, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria O. Tinti, Nazareno Scafetta
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Patent number: 5614522Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 24, 1995Date of Patent: March 25, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5601806Abstract: Taurine analogues are used for scavenging active oxygen compounds and preventing and minimizing damage to the skin from ultraviolet rays. The taurine analogues have the following formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification.Type: GrantFiled: September 20, 1994Date of Patent: February 11, 1997Assignee: Sogo Pharmaceutical Company LimitedInventors: Manabu Katsumata, Keiko Kiuchi, Tomoyasu Tashiro, Saburo Uchikuga
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Patent number: 5587499Abstract: These compounds are denoted by the following formula (I): ##STR1## in which: Z denotes H or a linear or branched alkyl radical,X denotes O or S,each of A and B independently denotes an alkylene radical, it being possible for this radical to be substituted,R denotes H or an alkali metal, or else a linear or branched alkyl radical,x has the value of 0 or 1, andy has the value of 0, 1 or 2,the radical A not existing if x and y are both equal to 0, X being incapable of denoting O when R=alkyl and when R=H with x=y=0, and B being incapable of denoting optionally substituted methylene when X=S, x=y=0 and R=alkyl.According to the invention, different simple and efficient processes are proposed for preparing these new compounds, which can be applied to the preparation of new polymers and copolymers.Type: GrantFiled: May 11, 1995Date of Patent: December 24, 1996Assignee: ELF Atochem S.A.Inventors: Mich ele Curci, Jean-Luc Mieloszynski, Daniel Paquer
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Patent number: 5583132Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: February 2, 1995Date of Patent: December 10, 1996Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5491170Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5491145Abstract: Novel compound of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R.sup.2 or R.sup.3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O).sub.p (p stands for an integer from 0 to 2; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for a hydrogen atom 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 a hydrogen atom, an optionally substituted lower lakyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.Type: GrantFiled: November 21, 1994Date of Patent: February 13, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
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Patent number: 5491169Abstract: Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction), the blood-brain barrier and having the following formula :H.sub.2 N--CH(R.sub.1)--CH(R.sub.2)--S--S--CH(R.sub.3)--CH(R.sub.4)--A--B--Zwherein: AB preferably represents a CO amide bond, R.sub.2 et R.sub.3 preferably represent a hydrogen atom, R.sub.1 et R.sub.4 preferably represent, independently of each other, a benzyl grouping, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 --CH.sub.2 --S(O)--CH.sub.3 or --CH.sub.2 --CH(CH.sub.3) .sub.2, Z may represent a --CH(R.sub.5)[CH(R.sub.6)].sub.n --COO(R.sub.7) grouping wherein: R.sub.5 may represent a hydrogen atom, a methyl grouping, a benzyl grouping or a phenyl grouping, R.sub.6 may represent a hydrogen atom and may also form a hydrocarbon cycle with R.sub.5, or Z may represent a heterocyclic grouping, and preferably a morpholinyl grouping. No drawings.Type: GrantFiled: September 26, 1994Date of Patent: February 13, 1996Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Bernard Roques, Marie C. Fournie-Zaluski
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Patent number: 5476966Abstract: This invention relates to certain S-substituted homocysteine sulfoximines and their uses. Buthionine sulfoximine (BSO) appears to have significant uses for chemotherapy and radio therapy, especially combination chemotherapy and radiation therapy and for treatment of subjects with parasitic infections. The compounds of the invention have the same above-mentioned utilities as BSO but have one or more superior attributes when compared to BSO.Type: GrantFiled: January 13, 1995Date of Patent: December 19, 1995Assignee: Cornell Research Foundation, Inc.Inventors: Mary Anderson, Alton Meister
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Patent number: 5468904Abstract: A fluorine-containing benzophenone derivative of the formula (1), (2) or (3):.PHI..sup.1 (--X.sup.1 --Q.sup.1 --R.sub.f.sup.1).sub.n (1).PHI..sup.2 --X.sup.2 --Q.sup.2 --R.sub.f.sup.2 --Q.sup.3 --X.sup.3 --.PHI..sup.3 (2).PHI..sup.4 --X.sup.4 --Q.sub.f --X.sup.5 --.PHI..sup.5 (3)wherein .PHI..sup.1 is a 2-hydroxybenzophenone structure of the formula ka-1: ##STR1## (wherein Y is a hydrogen atom or a hydroxyl group, each of k and m indicates the number of bond sites, k is an integer of from 0 to 3, and m is an integer of from 0 to 3, provided that 1.ltoreq.(k+m).ltoreq.4), n corresponds to (k+m) and is an integer of from 1 to 4, each of .PHI..sup.2, .PHI..sup.3, .PHI..sup.4 and .PHI..sup.5 is a 2-hydroxybenzophenone structure of the formula ka-1 wherein (k+m) is 1, each of X.sup.1, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 is a single bond or an oxygen atom, Q.sup.1 is a single bond or a bivalent linking group having a carbon atom directly bonded to X.sup.1, each of Q.sup.2 and Q.sup.Type: GrantFiled: February 4, 1994Date of Patent: November 21, 1995Assignee: Asahi Glass Company Ltd.Inventors: Ryoko Osawa, Takashige Maekawa, Tatsuo Momii, Satoshi Kamata
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Patent number: 5442088Abstract: Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this processL-amino acids of the formula I and salts thereof, ##STR1## in which R.sup.1 to R.sup.5 are defined as in claim 1 and n is 0 or 1, are obtained according to the invention bya) reacting an optically active S-homoserine lactone of the formula II, ##STR2## with hydrogen chloride in the presence of an alcohol of the formula R.sup.5 --OH to give novel compounds of the formula III, ##STR3## in which R.sup.3, R.sup.4 and R.sup.5 are defined as in formula I, except that R.sup.5 =H, andb) reacting the resulting compound of formula III with a compound of formula IV,R.sup.1 (O).sub.n -R(OR.sup.2).sub.2 (IV)and if desired, hydrolyzing the product to give a compound of formula I, in which R.sup.5 =H.Type: GrantFiled: July 7, 1994Date of Patent: August 15, 1995Assignee: Hoechst AktiengesellschaftInventor: Michael Hoffmann
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Patent number: 5429773Abstract: A process for improving the color and purity of dark-colored potassium or magnesium alkyl ester sulfonate surfactant compositions, and particularly alpha-sulfo fatty acid methyl ester compositions, without the need for bleaching or other process steps. The process comprises the steps of (1) forming a mixture comprising (i) an alkyl ester sulfonate surfactant composition containing impurities including dark-colored impurities, organic and inorganic salts, and disalts, and (ii) water, and (2) separating the ester sulfonate surfactant from the mixture. The process may further comprise step (3) recovering the alkyl ester sulfonate surfactant. Methyl ester sulfonate surfactant compositions are most preferred. After processing in accordance with the invention, the alkyl ester sulfonate surfactant composition has improved color, purity, and odor properties.Type: GrantFiled: February 5, 1993Date of Patent: July 4, 1995Assignee: The Procter & Gamble CompanyInventors: Alan E. Sherry, Benjamin E. Chapman, Michael T. Creedon
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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: 5369104Abstract: Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.Type: GrantFiled: December 28, 1992Date of Patent: November 29, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
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Patent number: 5336800Abstract: Oxamides useful as dye intermediates have the formula ##STR1## where R.sup.1 and R.sup.2 are independently of each other hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,X is hydroxyl, nitro or a radical of the formula --NR.sup.3 R.sup.4, where R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkanoyl and R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,Z is C.sub.2 -C.sub.8 -alkylene, substituted or unsubstituted phenylene or substituted or unsubstituted naphthylene, or X--Z and R.sup.1 are, together with the nitrogen atom joining them together, the radical of the formula ##STR2## where R.sup.3 is as defined above,L is a bridge member andY is vinyl or a radical of the formula --C.sub.2 H.sub.4 --A, where A is hydroxyl or a group which is detachable under alkaline reaction conditions.Type: GrantFiled: January 4, 1993Date of Patent: August 9, 1994Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Manfred Patsch, Knut Kessel
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Patent number: 5260424Abstract: Silylketene acetals, including "living" GTP polymers, are acylated or sulfonylated in the presence of GTP-effective catalysts with acyl or sulfonyl compounds to produce .beta.-ketoesters or .beta.-sulfonylesters; polymeric products, including capped, coupled and chain-extended polymers and block copolymers can be prepared.Type: GrantFiled: February 3, 1992Date of Patent: November 9, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: Gordon M. Cohen, Hans J. Reich
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Patent number: RE39576Abstract: A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m?R13 wherein m? is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydrogeType: GrantFiled: June 14, 1995Date of Patent: April 17, 2007Assignee: Smithkline Beecham CorporationInventors: Harold Francis Hodson, Richard Michael John Palmer, David Alan Sawyer, Richard Graham Knowles, Karl Witold Franzmann, Martin James Drysdale, Patricia Ifeyinwa Davies, Helen Alice Rebecca Clark, Barry George Shearer, Steven Smith
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Patent number: RE34652Abstract: Novel fluorinated, acrylamide monomers are prepared from 2-alkenyl azlactones reacted with fluorinated alcohols. The novel monomers have the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen or methyl;R.sup.2 and R.sup.3 independently can be an alkyl, cycloalkyl, or aryl group, or R.sup.2 and R.sup.3 taken together with the carbon to which they are joined can form a carbocyclic ring containing 4 to 12 ring atoms;R.sup.4 and R.sup.5 are independently hydrogen or lower alkyl;a is 0 or 1;b is 1 or 2;X is a single bond, CH.sub.2, CH.sub.2 OCH.sub.2, and CH.sub.2 CH.sub.2 OCH.sub.2 ; andR.sub.F is a substantially perfluorinated alkyl, cycloalkyl, or aryl group when b is 1 and perfluorinated alkylene when b is 2.Novel polymers and copolymers can be prepared from the monomers of the invention.Type: GrantFiled: June 3, 1992Date of Patent: June 28, 1994Assignee: Minnesota Mining and Manufacturing CompanyInventors: Steven M. Heilmann, Larry R. Krepski, Dean M. Moren, Jerald K. Rasmussen, Howell K. Smith, II