Sulfur In Acid Moiety Patents (Class 560/147)
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Patent number: 5676923Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Ulrich Niedballa, Peter Mareski, Bernd Raduchel, Hanns-Joachim Weinmann, Andreas Muhler, Bernd Misselwitz
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Patent number: 5637616Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.Type: GrantFiled: October 5, 1993Date of Patent: June 10, 1997Assignee: Arcturus Pharmaceutical CorporationInventors: Richard J. Sharpe, Maureen H. McAloon, Stephen J. Galli, Kenneth A. Arndt
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Patent number: 5637758Abstract: Disclosed are detergent compositions comprising critical amounts of divalent cations and a minimum amount of a mixture of a salt of alpha-sulfonated methyl ester of a fatty acid, anionic surfactants and foam stabilizing auxiliary surfactants.Type: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: Stepan CompanyInventors: Branko Sajic, Irma Ryklin, Brian L. Frank, Y. Kameshwer Rao
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Patent number: 5618941Abstract: Compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is (CH.sub.2).sub.m NHSO.sub.2 R.sup.6 or (CH).sub.m NHCOR.sup.6 ; R.sup.6 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl optionally substituted by aryl, aryl or heteroaryl; R.sup.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, OCF.sub.3, CN, CONH.sub.2, or S(O).sub.n (C.sub.1 -C.sub.4 alkyl); X is CH.sub.2, CHCH.sub.3, CH(OH), C(OH)CH.sub.3, C.dbd.CH.sub.2, CO or O; m is 0 or 1 and n is 0, 1 or 2, and their pharmaceutically acceptable salts and biolabile esters, are antagonists of thromboxane A.sub.2 of utility, particulary in combination with a thromboxane synthetase inhibitor, in the treatment of atherosclerosis and unstable angina and for prevention of reocclusion after percutaneous transluminal angioplasty.Type: GrantFiled: March 15, 1995Date of Patent: April 8, 1997Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele
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Patent number: 5616781Abstract: Disclosed are detergent compositions comprising critical amounts of divalent cations and a minimum amount of a mixture of a salt of alpha-sulfonated methyl ester of a fatty acid, anionic surfactants and foam stabilizing auxiliary surfactants.Type: GrantFiled: March 27, 1995Date of Patent: April 1, 1997Assignee: Stepan CompanyInventors: Branko Sajic, Irma Ryklin, Brian L. Frank
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Patent number: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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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: 5574184Abstract: A lubricant additive having antiwear and antioxidant properties is the reaction product of a sulfur-containing carboxylic acid and an etheramine, preferably 3,3'-thiodipropionic acid and N-isoeicosyloxypropyl-1,3-diaminopropane which is post reacted with an aliphatic alcohol, preferably oleyl alcohol, an aliphatic amine, preferably a tert-C.sub.12 to C.sub.14 amine and/or a trialkyl phosphite, preferably a tributylphosphite. The post-reaction product contains at least one ester, amide and/or phosphonate functional group.Type: GrantFiled: March 10, 1995Date of Patent: November 12, 1996Assignee: Mobil Oil CorporationInventors: Shi-Ming Wu, Andrew G. Horodysky
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Patent number: 5571937Abstract: This invention relates to new derivatized solid supports and compounds having the formula: ##STR1## wherein S may be a solid support; L may be a chemical bond or a suitable inorganic or organic linker; Z may be --SO.sub.2 -- or --S--S--; R may be --OH, an H-phosphonate, an alkanephosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, --OR.sup.1 --SR.sup.1, a nucleotide, N, which may be substituted or modified in its sugar, phosphate or base or an oligonucleotide of the formula --(N).sub.g, --R.sup.2, wherein N is as defined above which may be the same or different; g is an integer from one to two hundred; R.sup.1 is a suitable protecting group; and R.sup.2 may be an H-phosphonate, an alkane-phosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, --OH, --OR.sup.1, --SR.sup.1, or --O--P(OCH.sub.2 CH.sub.Type: GrantFiled: May 13, 1994Date of Patent: November 5, 1996Assignees: Sloan-Kettering Institute for Cancer Research, ZW Biomedical Research AGInventors: Kyoichi A. Watanabe, Wu-Yun Ren, Roger Weil
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Patent number: 5536723Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5534651Abstract: .gamma.-Mercaptocarboxylic acids and their derivatives, in particular esters and amides, are prepared from .gamma.-butyrolactones via the corresponding thiolactones. The thiolactones are obtained by reaction of a .gamma.-lactone with thiocarboxylates in polar solvents and are converted by ring opening using nucleophilic reagents, such as, alkali metal alkoxides, into the .gamma.-mercaptocarboxylic acid derivatives. These are intermediates, for example, for the synthesis of leucotriene antagonists.Type: GrantFiled: August 30, 1994Date of Patent: July 9, 1996Assignee: Lonza Ltd.Inventors: Wilhelm Quittmann, John McGarrity
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Patent number: 5525628Abstract: Crystalline non-hygroscopic salt of glutathione alkylester of the formula (I) ##STR1## wherein AA is an amino acid are disclosed.Type: GrantFiled: November 28, 1994Date of Patent: June 11, 1996Assignee: Edmond Pharma S.R.L.Inventors: Massimo Nicola, Marco Inglesi, Giancarlo B. Fregnan, Guido Vandoni
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Patent number: 5510510Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:x is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --C(O)--, --O--, --NR.sup.1 -- or --(S).sub.q --;Y is --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O) (OR.sup.2) (R.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.3 is --(O).sub.t R.sup.4 ;R.sup.1, R.sup.2 and R.sup.4 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p and t are each independently 0 or 1; andq is an integer from 1 to 2.Type: GrantFiled: June 28, 1994Date of Patent: April 23, 1996Assignee: Bristol-Meyers Squibb CompanyInventors: Dinesh V. Patel, Scott A. Biller
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Patent number: 5475134Abstract: An improved process for the production of sulfonated fatty acid alkyl ester surfactants containing low levels of impurities including disalt and dimethyl sulfate (DMS) impurities, said process comprising sulfonating fatty acid alkyl esters, forming a substantially anhydrous alkoxide solution, over-neutralizing to a pH of at least about 10 with the alkoxide solution, and re-neutralizing to a pH of about 5 to about 9. The substantially anhydrous alkoxide solution is formed by combining an alkoxide solution containing an alkoxide of the formula (RO.sup.-).sub.n M.sup.n+, a C.sub.1 to C.sub.8 alcohol, and no more than 1% by weight water with a sacrificial ester of the formula R.sup.1 COOR.sup.2, wherein the molar ratio of the sacrificial ester to water is from about 0.5:1 to about 2:1.Type: GrantFiled: December 16, 1993Date of Patent: December 12, 1995Assignee: The Procter & Gamble Co.Inventor: Keith H. Baker
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Patent number: 5470832Abstract: The compounds disclosed am analogs of the CAAX motif of proteins that can be modified by geranylgeranylation in vivo that selectively inhibit the geranylgeranylation of several proteins. The relatively poor activity of the compounds against the farnesyl protein transferase, which modifies several proteins important in cellular replication, allows the use of the compounds of the instant invention to treat diseases which which am regulated by the function of a geranylgeranylated protein, such as certain cancers and inflammatory diseases. Further contained in this invention are chemotherapeutic compositions containing these geranylgeranyl protein transfcrase type I inhibitors and methods for their production.Type: GrantFiled: January 31, 1994Date of Patent: November 28, 1995Assignee: Merck & Co., Inc.Inventors: Jackson B. Gibbs, Samuel L. Graham
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Patent number: 5453533Abstract: An influenza virus neuraminidase inhibitor, its analogs, its pharmaceutically acceptable salts, derivatives, and mixtures thereof having the following formula: ##STR1## where A is CO.sub.2 H, CO.sub.2 H.sub.3, NO.sub.2, SO.sub.3 H or PO.sub.3 H.sub.2, B is CH, N, O or S, R.sub.1 and R.sub.2 are H, NO.sub.2 or (CH.sub.m).sub.n X.sub.1 where m=1 or 2, n is an integer from 0 to 4 and X.sub.1 is guanidino, OH, NH.sub.2, SH, NO.sub.2, F, Cl, Br, I, CN, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2, R.sub.3 and R.sub.4 are H, (CH.sub.o).sub.p X.sub.2, (CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NH(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NHCO(CH.sub.o).sub.p CH.sub.2 X.sub.2 or NHCO(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2 where o=1 or 2, p is an integer from 0 to 4 and X.sub.2 is H, guanidino, OH, NH.sub.2, SH, NO.sub.2, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2 , R.sub.5 =H, OH, NH.sub.2, (CH.sub.k).sub.1 X.sub.3, CO(CH.sub.k).sub.1 X.sub.3, SO(CH.sub.k).sub.1 X.sub.3 or SO.sub.2 (CH.sub.Type: GrantFiled: April 14, 1994Date of Patent: September 26, 1995Assignee: The University of Alabama at BirminghamInventors: Ming Luo, Wayne J. Brouillette, Gillian Air
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Patent number: 5407960Abstract: Mercaptocycloacyl aminoacid inhibitors of endopeptidase of the formula ##STR1## or a pharmaceutically acceptable salt thereof, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, and treatment of nephrotoxicity pain conditions, and pharmaceutical compositions containing said compounds are disclosed.Type: GrantFiled: June 11, 1992Date of Patent: April 18, 1995Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5405550Abstract: Molecular bulding beams, liquid crystals, and surfactants in the form of compounds based on [1.1.1]propellane, including poly[1.1.1]propellanes. Molecular building beams having a telomeric or polymeric chain staff, and linking groups functionalized on one or both ends of the staff. A system for linking the beams to connecting units to construct molecular structures of various forms, such as whips, combs, scaffoldings, nets, or stars. Other broad aspects of the invention provide liquid crystals and surfactants. The liquid crystals include telomeric or polymeric compounds functionalized with flexible end groups, while the surfactant compounds are functionalized with surface active end groups. Methods of synthesizing the various compounds ar also provided.Type: GrantFiled: August 10, 1992Date of Patent: April 11, 1995Assignee: Josef MichlInventors: Josef Michl, Piotr Kaszynski, Andrienne C. Friedli
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Patent number: 5401880Abstract: The present invention relate to methods and pharmaceutical reagents for decreasing the phase separation temperature and inhibiting the formation of high molecular with aggregates in eye lenses, thereby inhibiting or reversing cataract formation.Type: GrantFiled: January 2, 1992Date of Patent: March 28, 1995Assignee: Oculon CorporationInventors: John I. Clark, Kerry W. Fowler, Mark W. Orme, Louis J. Theodore
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Patent number: 5401869Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.Type: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
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Patent number: 5391820Abstract: Facile process for the production of 3-mercaptopropionitrile and 3-mercaptopropionic acid by reacting thiodipropionitrile with alkaline hydrosulfide in the presence of alkaline hydroxide. Acidification of the resulting reaction product with a strong acid, or saponification, yields the desired mercaptopropionic acid, which can be isolated in high yield.Type: GrantFiled: April 13, 1994Date of Patent: February 21, 1995Assignee: Hampshire Chemical Corp.Inventors: Richard P. Woodbury, F. David Wood
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Patent number: 5359128Abstract: The invention comprises compositions and methods for the treatment of psoriasis.Type: GrantFiled: February 11, 1993Date of Patent: October 25, 1994Inventor: Izhak Blank
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Patent number: 5352757Abstract: The present invention relates to new sulfur compounds which are polyol esters of mercaptocarboxylic acids. It also relates to the use of these sulfur esters for preparing polymers exhibiting a refractive index higher than 1.50. The manufacture of optical discs and of waveguides may be mentioned among the optical applications of these polymers.Type: GrantFiled: September 16, 1992Date of Patent: October 4, 1994Assignee: Rhone-Poulenc ChimieInventors: Sylvie Lavault, Gerard Velleret
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Patent number: 5348978Abstract: Angiotensin converting enzyme inhibitors have the formula Z(CH.sub.2).sub.n CHR.sub.1 COOCHR.sub.2 COOHin which Z is --SR.sub.3, --COCHR.sub.4 NHCOR.sub.5, ##STR1## or --NHCHR.sub.7 COOH, R.sub.4, R.sub.5, R.sub.6, and R.sub.7, which may be the same or different, are each phenyl or alkylphenyl C.sub.7-12,R.sub.4 is hydrogen, alkyl C.sub.1-6, NHR.sub.8 or (CH.sub.2).sub.p R.sub.9,R.sub.2 is (CH.sub.2).sub.m XR.sub.10, alkyl C.sub.1-6 optionally substituted by a saturated 5- or 6-membered carbocyclic or heterocyclic ring, alkylhalo C.sub.1-6, alkylcyano C.sub.1-6, or alkyl phenyl C.sub.7-12, the phenyl being optionally substituted by NO.sub.2 or NH.sub.2,X is O, S(O).sub.q, C.dbd.O or NR.sub.11, andR.sub.10 is alkyl C.sub.1-6, alkylhalo C.sub.1-6, alkoxy C.sub.1-6, alkoxy C.sub.1-6 substituted by halogen, alkanoyl C.sub.1-6, S(O).sub.r R.sub.12, NR.sub.13 R.sub.14, phenyl, alkylphenyl C.sub.Type: GrantFiled: December 10, 1992Date of Patent: September 20, 1994Assignee: Fisons plcInventors: Andrew J. G. Baxter, Premji Meghani
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Patent number: 5347039Abstract: This invention is directed to a method for stereoselectively preparing a syn-dihydroxylated compound comprising reacting a 3-hydroxyket-1-one with a borohydride in the presence of titanium derivative.Type: GrantFiled: August 11, 1993Date of Patent: September 13, 1994Assignee: Rhone-Poulenc Rorer S.A.Inventors: Patrick Leon, Xavier Radisson, Viviane Massonneau
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Patent number: 5326755Abstract: The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.Type: GrantFiled: September 10, 1992Date of Patent: July 5, 1994Assignee: Roussel UCLAFInventors: Robert J. Blade, George S. Cockerill
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Patent number: 5310536Abstract: Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include a tertiary amine strategically located to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to a thermodynamically stable amide-thiolate complex. The amide-thiolate ligands of the present invention may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.Type: GrantFiled: February 6, 1992Date of Patent: May 10, 1994Assignee: Mallinckrodt Medical, Inc.Inventor: Ananthachari Srinivasan
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Patent number: 5292926Abstract: This invention relates to cysteine derivatives of the formula[I] and salts thereof. ##STR1## The compounds of this invention are useful for immunomodulator and treatment of liver disorder.Type: GrantFiled: April 8, 1993Date of Patent: March 8, 1994Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takakazu Morita, Tadashi Iso, Shiro Mita, Yoichi Kawashima
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Patent number: 5286746Abstract: Antihypercholesterolemic activity is exhibited by compounds of the formula ##STR1## wherein: X is hydrogen, alkali metal or ammonium;Y is hydrogen, alkyl, cycloalkyl, aryl, or aralkyl; ##STR2## R is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal (such as Na, Li, or K); andn is 1 or 2.Type: GrantFiled: December 20, 1991Date of Patent: February 15, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Kathleen M. Poss
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Patent number: 5279811Abstract: Radiopharmaceuticals consisting essentially of a lipophilic, charge neutral radionuclide complex of a diaminedithiol ligand having 1-4 ester groups of the formula --A--COOR where A is a straight or branched chain alkylene of 0-10 carbon atoms and R is an alkyl group of 1-10 carbon atoms are useful in radioimaging brain perfusion in primates. Ester-substituted diaminedithiols in sterile, pharmaceutically acceptable form, and kits of the diaminedithiols and sterile, non-pyrogenic reducing agents for reducing preselected radionuclides are also provided. Technetium-99m is a preferred radionuclide.Type: GrantFiled: January 26, 1988Date of Patent: January 18, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Paul L. Bergstein, Edward H. Cheesman, Alan D. Watson
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Patent number: 5279764Abstract: The invention relates to dihalogenobenzene derivatives of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --(Z.sup.2 --A.sup.3).sub.n --R.sup.2wherein R.sup.1, R.sup.2, A.sup.1, A.sup.2, A.sup.3, Z.sup.1, Z.sup.2 and n are as defined in the specification.Type: GrantFiled: November 23, 1992Date of Patent: January 18, 1994Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Volker Reiffenrath, Joachim Krause, Georg Weber, Ulrich Finkenzeller, Andreas Wachtler, Thomas Geelhaar, David Coates, Ian C. Sage, Simon Greenfield
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Patent number: 5266713Abstract: Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.Type: GrantFiled: August 12, 1992Date of Patent: November 30, 1993Assignee: Miles Inc.Inventors: Trevor S. Abram, Peter Norman, Stephen R. Tudhope, Harold C. Kluender, Robert N. Schut, Heinrich Meier, Ulrich Rosentreter
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Patent number: 5256818Abstract: A novel method for making .beta.-mercaptopropionic acid which comprises adding alkaline hydroxide to thiodipropionic acid to obtain alkaline thiodipropionate, mixing thus obtained alkaline thiodipropionate with an aqueous solution of alkaline sulfide, then reacting the mixed solution with addition of heating in a required time, and acidifying the reacted solution with a strong acid.Type: GrantFiled: November 12, 1991Date of Patent: October 26, 1993Inventor: Tetsuzo Tomioka
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Patent number: 5241099Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H-acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of simple inorganic bases, where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.8 and X.sup..crclbar. have the meanings given in the description.Type: GrantFiled: March 16, 1992Date of Patent: August 31, 1993Assignee: Bayer AktiengesellschaftInventors: Heinz-Ulrich Blank, Helmut Kraus
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Patent number: 5241070Abstract: This invention is directed to novel nucleophilic polysubstituted aryl acridinium esters and to novel conjugates thereof. The novel nucleophilic polysubstituted aryl acridinium esters and novel conjugates thereof are useful in biological assays, including novel assays for the determination of Vitamin B.sub.12, folate, cortisol, estradiol, and thromboxane B.sub.2.Type: GrantFiled: April 17, 1992Date of Patent: August 31, 1993Assignee: Ciba Corning Diagnostics Corp.Inventor: Say-Jong Law
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Patent number: 5235101Abstract: An improved process for the separation of enantiomers of a mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process involves adding an inert liquid to the reaction solution formed by: (i) forming a salt solution comprising said racemic mixture of a C.sub.1 to C.sub.6 linear or branched aliphatic carboxylic acid and an organic or inorganic base; (ii) treating said salt solution with less that equimolar equivalents of a chiral organic nitrogenous base; (iii) precipitating from the reaction solution formed in step (ii) the less soluble diastereomeric salt; (iv) addition of a countersolvent to the slurry formed in step (iii); (v) extracting the more soluble diastereomeric salt or the salt of carboxylic acid and the base added in step (i) into the countersolvent. The inert liquid and the countersolvent must be of sufficiently different density.Type: GrantFiled: January 24, 1992Date of Patent: August 10, 1993Assignee: Ethyl CorporationInventors: Deepak R. Patil, Azfar A. Choudhury, Abbas Kadkhodayan
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Patent number: 5235095Abstract: An improved process for the separation of enantiomers of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process involves: (i) forming a salt solution comprising said racemic mixture of a C.sub.1 to C.sub.6 linear or branched aliphatic carboxylic acid and an organic or inorganic base; (ii) treating said salt solution with one-half molar equivalent of a chiral organic nitrogenous base having a base strength no stronger than said organic or inorganic base; and (iii) precipitating from the reaction solution formed in step (ii) the less soluble diastereomeric salt, the improvement being adding to the salt solution of step (ii) an inert organic or inorganic base that is soluble in the salt solution.Type: GrantFiled: January 24, 1992Date of Patent: August 10, 1993Assignee: Ethyl CorporationInventors: Abbas Kadkhodayan, Deepak R. Patil, Azfar A. Choudhury
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Patent number: 5235100Abstract: A process for the separation of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process comprises:i) separating a racemic mixture of an aliphatic carboxylic acid or ester thereof having the formula: ##STR1## where R.sub.1 is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; cycloalkyl; alkyl-substituted cycloalkyl; C.sub.6 to C.sub.14 aryl; C.sub.1 to C.sub.6 alkylthio; C.sub.2 to C.sub.8 cycloalkylthio; C.sub.6 to C.sub.10 arylthio; C.sub.6 to C.sub.10 arylcarbonyl; C.sub.4 to C.sub.8 cycloalkenyl; trifluoromethyl; halo; or C.sub.4 to C.sub.Type: GrantFiled: January 24, 1992Date of Patent: August 10, 1993Assignee: Ethyl CorporationInventors: Azfar A. Choudhury, Abbas Kadkhodayan, Deepak R. Patil
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Patent number: 5219886Abstract: Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.Type: GrantFiled: October 1, 1991Date of Patent: June 15, 1993Assignee: Schering CorporationInventors: Elizabeth M. Smith, Philip M. DeCapite, Bernard R. Neustadt
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Patent number: 5198131Abstract: Dialkanol- and trialkanol amine-derived thioesters have been found to be effective multifunctional antiwear additives for lubricants and fuels.Type: GrantFiled: December 27, 1991Date of Patent: March 30, 1993Assignee: Mobil Oil CorporationInventors: Shih-Ying Hsu, Andrew G. Horodysky
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Patent number: 5198568Abstract: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment.Type: GrantFiled: September 9, 1991Date of Patent: March 30, 1993Assignee: Sepracor, Inc.Inventors: Charles M. Zepp, Stephen A. Wald, David R. Dodds
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Patent number: 5198569Abstract: The asymmetric hydrogenation of aliphatic .alpha.-keto esters in the presence of rhodium catalysts which contain as chiral ligand a diphosphine of formula IV(R.sub.3).sub.2 P--Q--P(R.sub.3)hd 2 (IV)wherein R.sub.3 is phenyl, C.sub.1 -C.sub.6 alkylphenyl or C.sub.1 -C.sub.6 alkoxyphenyl, and Q is [2,2,1]-bicyloheptan-1,2-ylene or [2,2,1]-bicyclohept-4,5-en-1,2-ylene, gives the corresponding (R)- or(S)-.alpha.-hydroxycarboxylic acid esters in high rates of chemical conversion and in high enantiomer excesses.Type: GrantFiled: September 11, 1991Date of Patent: March 30, 1993Assignee: Ciba-Geigy CorporationInventors: Hans-Ulrich Blaser, Ulrich Pittelkow, Felix Spindler
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Patent number: 5187183Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: June 14, 1991Date of Patent: February 16, 1993Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5173105Abstract: An herbicide compound of the formula ##STR1## wherein 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; 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 oxo;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.5 and R.sup.6 together are alkylene having 2 to 5 carbon atoms;R.sup.7 and R.sup.8 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: February 5, 1991Date of Patent: December 22, 1992Assignee: Imperial Chemical Industries PlcInventor: Christopher G. Knudsen
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Patent number: 5159105Abstract: Pentafluorosulfanyl fluoroaliphatic carbonyl and sulfonyl fluorides, derivatives of the acid fluorides and the preparation and use of the acid fluorides and derivatives. The fluoroaliphatic moiety of said acid fluorides comprise at least three fully-fluorinated carbon atoms. The derivatives of the acid fluorides are useful as surface-active agents and surface-treating agents.Type: GrantFiled: February 28, 1990Date of Patent: October 27, 1992Assignee: Minnesota Mining and Manufacturing CompanyInventors: John C. Hansen, Patricia M. Savu
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Patent number: 5157147Abstract: A process is provided for the preparation of mercaptopropionic acid esters by reaction of an acrylic acid ester with hydrogen sulfide in the presence of a weakly basic amine as a catalyst, a polyether as a co-catalyst, a polythiodipropionic acid ester as a reactive solvent, and added elemental sulfur.Type: GrantFiled: November 5, 1990Date of Patent: October 20, 1992Assignee: Witco CorporationInventors: Daniel R. Chisholm, George A. Seubert, Jr.
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Patent number: 5118835Abstract: Thio-bis-(hydrocarbyl substituted diacid materials), such as thio-bis-(polyalkyl lactone acid) and/or their precursors, the adducts of sulfur chloride and unsaturated diacid materials, e.g., 4,8-bis-polyalkyl-4,8-dichloro-6-thiaundecane-1,2,10,11-tetracarboxylic acid bis-anhydride and their dehydrochlorinated analogs, when esterified with an alcohol, preferably a polyol, such as pentaerythritol, polypentaerythritol or a polyalkylene glycol with or without acid catalysts and/or metal template reagents yield thio-bis-(alkyl lactone acid esters) and thio-bis-(hydrocarbyl diacid esters) which can be characterized in part, as macrocyclic and/or macrocyclic-like structures, are useful as stable additives in lubricating compositions, e.g. as varnish inhibiting dispersants for lubricating oils and fuels.Type: GrantFiled: July 18, 1990Date of Patent: June 2, 1992Assignee: Exxon Research & Engineering Co.Inventors: Stanley J. Brois, Antonio Gutierrez
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Patent number: 5095138Abstract: The invention relates to production of esters of mercaptocarboxylic acids and alcohols forming an azeotrope with water.The esterification is carried out continuously in the presence of an excess of alcohol and the water formed is removed by entraining azeotropically under vacuum at a temperature such that the residual water concentration in the reaction mixture remains constantly below 0.5% by weight.The process according to the invention applies more particularly to the synthesis of octyl esters of thioglycolic acid.Type: GrantFiled: October 5, 1990Date of Patent: March 10, 1992Assignee: Societe Nationale Elf Aquitaine (Production)Inventors: Yves Labat, Jean-Pierre Muller, Daniel Litvine
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Patent number: 5095133Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of alkoxides of the formulaM.sup.1 OR.sup.10 (IV)where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.10, X.sup.- and M.sup.1 have the meaning mentioned in the description.Type: GrantFiled: July 16, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz U. Blank, Helmut Kraus
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Patent number: 5087733Abstract: Processes for conditioning human hair by treatment with selected sulfur containing quaternary ammonium compounds, compositions useful for such processes and novel quaternary compounds useful in the processes.Type: GrantFiled: August 3, 1990Date of Patent: February 11, 1992Assignee: Clairol, Inc.Inventors: Thomas M. Deppert, Janusz Z. Jachowicz, Bryan P. Murphy