Sulfur Or Selenium Patents (Class 562/556)
  • Publication number: 20020022744
    Abstract: A process for precipitating cystine from a solution in sulfuric acid, includes forming a mixture of a solution of cystine in aqueous sulfuric acid and of an aqueous solution of a base by simultaneous metering the cystine solution and the aqueous base solution into a mixing container. The metering takes place in such a way that the mixture in the container has a pH between 1.0 and 7.0 and a temperature between 30° C. and the boiling point of the mixture.
    Type: Application
    Filed: July 13, 2001
    Publication date: February 21, 2002
    Applicant: CONSORTIUM FUR ELEKTROCHEMISCHE INDUSTRIE GmbH
    Inventors: Wolfgang Doring, Jurgen Stohrer
  • Publication number: 20020019563
    Abstract: The present invention relates to S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 23, 2001
    Publication date: February 14, 2002
    Inventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Brian S. Hickory, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey S. Snyder, Mahima Trivedi, Sofya Tsymbalov
  • Patent number: 6344483
    Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 31, 2000
    Date of Patent: February 5, 2002
    Assignee: G. D. Searle & Co.
    Inventors: E. Ann Hallinan, Barnett S. Pitzele, Dale P. Spangler, Mihaly V. Toth, R. Keith Webber, Arija A. Bergmanis, Timothy J. Hagen, Sofya Tsymbalov
  • Publication number: 20020010366
    Abstract: The present invention relates to novel amidino compound of formula (I).
    Type: Application
    Filed: August 15, 2001
    Publication date: January 24, 2002
    Inventors: Richard Mansfield Beams, Martin James Drysdale, Karl Witold Franzmann, Anthony Joseph Frend, Harold Francis Hodson, Richard Graham Knowles, Daryl David Rees, David Alan Sawyer
  • Patent number: 6306840
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 23, 2001
    Assignee: Biogen, Inc.
    Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
  • Publication number: 20010027214
    Abstract: Stable and non hygroscopic salts consisting of lower alkanoyl-L-carnitine magnesium citrates are disclosed which are suitable for preparing solid compositions useful as dietary/nutritional supplements for human use and as fodder supplement for veterinary purposes.
    Type: Application
    Filed: September 24, 1999
    Publication date: October 4, 2001
    Inventors: NAZARENO SCAFETTA, MARIA ORNELLA TINTI
  • Publication number: 20010025110
    Abstract: Methods, compositions, and devices for alleviating the problems of toxic discharge of aldehydes present in waste streams are disclosed. The methods relate to reducing neutralized aldehydes wherein the neutalized aldehydes are formed by treating aldehydes with amino acids and thereinafter are reduced. These reduced, neutralized aldehydes do not revert back to toxic aldehydes, but form amino acids and thus allow waste containing aldehyde to be more environmentally safely disposed.
    Type: Application
    Filed: December 22, 2000
    Publication date: September 27, 2001
    Inventors: Peter Zhu, Xiaolan Chen, Charles G. Roberts
  • Patent number: 6277876
    Abstract: Compounds of the formula (I) where X is a —CO2H or —CONHOH group; Y and Z are independently sulphur or oxygen, at least one being sulphur; R1 is hydrogen, hydroxy, (C1-C6)alkyl, (C2-C6)alkenyl, or (C3-C8cycloalkyl; R2 is a (C1-C24)alkyl, phenyl(C1-C6)alkyl, or phenyl(C0-C6alkyl)O)C1-C6)alkyl, any of which may be optionally substituted by (C1-C6)alkyl, (C1-C6)alkoxy, halo or cyano (CN); R3 is the characterising side chain of a natural &agr;-amino acid in which any functional groups may be protected, (C1-C6)alkyl which may be optionally substituted, or cycloalkyl(C1-C6)alkyl; R4 is hydrogen, (C1-C6)alkyl, phenyl(C1-C6)alkyl, optionally substituted phenyl or heteroaryl, or a group of formula —(Q—O)n—Q where Q is a straight or branched (C1-C6)alkyl, where n is an integer >1 and no continuous linear sequence of atoms in the group R4 is >12; or a salt, hydrate or solvate thereof.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 21, 2001
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventor: Mette Knak Christensen
  • Patent number: 6254850
    Abstract: The invention relates to diethylenetriaminepentaacetic acid derivatives, their complexes and complex salts, containing an element of atomic numbers 20-32, 39-51 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and antidotes and process for their production.
    Type: Grant
    Filed: January 10, 2000
    Date of Patent: July 3, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Krause, Franz-Karl Maier, Michael Bauer, Gabriele Schuhmann-Giampieri, Wolf-Rudiger Press, Peter Muschik
  • Patent number: 6255277
    Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.
    Type: Grant
    Filed: May 10, 1995
    Date of Patent: July 3, 2001
    Assignees: Brigham and Women's Hospital, NitroMed, Inc.
    Inventors: Jonathan Stamler, Joseph Loscalzo, John D. Folts
  • Patent number: 6239111
    Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: May 29, 2001
    Assignee: Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Toru Moriguchi, Hiromichi Matsuura, Hiroshi Saito
  • Patent number: 6201122
    Abstract: 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: Grant
    Filed: December 8, 1992
    Date of Patent: March 13, 2001
    Assignee: 3M Innovative Properties Company
    Inventor: Rudolf J. Dams
  • Patent number: 6180826
    Abstract: 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: Grant
    Filed: January 30, 1998
    Date of Patent: January 30, 2001
    Assignee: Laboratoire 3 S
    Inventors: Istvan Szonyi, Stephane Szonyi, Francois Szonyi
  • Patent number: 6156908
    Abstract: The invention is directed to a process for the preparation of lactams of Formula I. It is further directed to new advantageous intermediates of Formula II and the use thereof. By the cyclization of compounds of Formula II, compounds of Formula I are obtained.
    Type: Grant
    Filed: September 10, 1999
    Date of Patent: December 5, 2000
    Assignee: Rohm Gesellschaft, GmbH
    Inventors: Karlheinz Drauz, Ingo Klement, Gunter Knaup
  • Patent number: 6127573
    Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jing Li, Zhiguo Song, David M. Tschaen, Mangzu Zhao
  • Patent number: 6103931
    Abstract: It is described a process for preparing (R)-2-bromo-3-phenyl-propionic acid starting from (D)-phenyl-alanine, sodium nitrite and concentrated hydrobromic acid in a mixture of an aqueous solvent and a solvent selected from the group consisting of halogenated hydrocarbons and aromatic hydrocarbons.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: August 15, 2000
    Assignee: Zambon Group S.p.A.
    Inventors: Pietro Allegrini, Giorgio Soriato
  • Patent number: 6077971
    Abstract: Disclosed is a method for purifying homocystine comprising treating crude homocystine with a base, a method for purifying homocystine comprising recovering homocystine by neutralizing an alkaline aqueous solution of crude homocystine with an acid, and a homocystine powder containing 1,000 ppm or less of a polysulfide.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: June 20, 2000
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Jun Takehara, Shuji Ichikawa, Hiroshi Iwane, Hirotaka Ryutou, Kenichi Sugimoto, Toshihiko Yahata
  • Patent number: 6040432
    Abstract: The invention relates to diethylenetriaminepentaacetic acid derivatives, their complexes and complex salts, containing an element of atomic numbers 20-32, 39-51 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and antidotes and process for their production.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 21, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Krause, Franz-Karl Maier, Michael Bauer, Gabriele Schuhmann Giampieri, Wolf-Rudiger Press, Peter Muschik
  • Patent number: 5998412
    Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: December 7, 1999
    Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
  • Patent number: 5994539
    Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: November 30, 1999
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
  • Patent number: 5990349
    Abstract: A process for the preparation of methionine or a salt of methionine by reaction of the components 3-methylmercaptopropionaldhyde, hydrogen cyanide, ammonia and carbon dioxide or components from which the above-mentioned components can be prepared, optionally in the presence of water, to 5-(2-methylmercaptoethyl)-hydantoin and further reaction thereof to methionine or the salt thereof, characterised in that the reaction of the components is initiated by means of at least one premixture in such a way that a first mixture is formed containing at least the predominant proportion (at least 5/10) of the 3-methylmercaptopropionaldeyde and at least 1/10 of the hydrogen cyanide component or corresponding quantities of components from which these components can be prepared, and less than 5/10 of one of the components ammonia, carbon dioxide or of the components from which ammonia or carbon dioxide can be prepared, and in that this first mixture is combined with the other component(s) for the reactive conversion to 5-(2
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: November 23, 1999
    Assignee: Degussa Aktiengesellschaft
    Inventors: Friedhelm Geiger, Baudouin Halsberghe, Hans-Joachim Hasselbach, Klaus Hentschel, Klaus Huthmacher, Martin Korfer, Sven-Peter Mannsfeld, Herbert Tanner, Ferdinand Theissen, Jose Vanrobaeys, Klaus Willigerodt
  • Patent number: 5973200
    Abstract: A process for the free-radical addition of a mercaptan to a nonconjugated olefinic substrate having a terminal carbon-carbon double bond is disclosed. 2-Hydroxy-4-(ethylthio)butanoic acid (HMBA) or methionine can be prepared using this method. The nonconjugated olefinic substrate has the general formula: ##STR1## wherein R is selected from the group consisting of --COOH, --COOR.sup.2, --CONR.sup.3 R.sup.4, --CN and --CCl.sub.3, R.sup.1 is selected from the group consisting of --OH, --OCOR.sup.2, --NHCOR.sup.2 and --NH.sub.2, R.sup.2 is selected from the group consisting of alkyl, cycloalkyl and aryl and R.sup.3 and R.sup.4 are independently selected from the group consisting of --H and R.sup.2.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: October 26, 1999
    Assignee: Novus International, Inc.
    Inventor: Karl E. Koenig
  • Patent number: 5962726
    Abstract: The invention relates to amphiphilic compounds of the general formula I ##STR1## with at least two hydrophilic and at least two hydrophobic groups based on alkoxylated amines and/or alkoxylated fatty acid amides and di-, oligo- or polycarboxylic acids (spacer A). Y and Z are hydrogen or functional groups. The amphiphilic compounds according to this invention are usually surface-active and are suitable as emulsifiers, demulsifiers, detergents, dispersants and hydrotropes in industry and domestically, for example in the areas of metal processing, ore production, surface treatment, washing and cleaning hard surfaces, such as, for example, the manual cleaning of crockery, washing and cleaning skin and hair, cosmetics, medicine and food processing and preparation.
    Type: Grant
    Filed: January 29, 1998
    Date of Patent: October 5, 1999
    Assignee: Huls Aktiengesellschaft
    Inventors: Klaus Kwetkat, Herbert Koch, Wulf Ruback
  • Patent number: 5955053
    Abstract: The present invention relates to novel metal chelates, exemplified as technetium-99m or rhenium chelates, and to the process of preparing such metal chelates from corresponding ligands. These ligands and their corresponding metal chelates are synthesized to have a cysteinylethylene (EC) structure, a thioacetamidethiourea (TATU) structure, or a dithiourea (DTU) structure. The present invention further relates to a pharmaceutical composition comprising a metal chelate, for example, a .sup.99m Tc-chelate, to the use of the composition for renal imaging and examination of renal function, and to a kit for preparing such a composition prior to use.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: September 21, 1999
    Assignee: Emory University
    Inventors: Luigi Gaetano Marzilli, Malgorzata Lipowska, Lory Hansen, Andrew Taylor, Jr.
  • Patent number: 5945548
    Abstract: Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II).
    Type: Grant
    Filed: May 21, 1998
    Date of Patent: August 31, 1999
    Assignee: Societe Civile Bioproject
    Inventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
  • Patent number: 5942601
    Abstract: Methods and compositions are provided for synthesizing peptides with sulfonyl protecting groups. In the subject methods, an sulfonyl group .alpha.-amino protected amino acid is contacted with a second amino acid monomeric unit under coupling conditions so that the protected amino acid and second amino acid monomeric unit are joined by a peptide bond. The contacting step may be repeated one more additional times to obtain a peptide of desired length. Also provided are methods of site specific modification using the subject sulfonyl protecting groups. The subject methods find particular use in methods of solid phase peptide synthesis.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: August 24, 1999
    Assignee: The Reagents of The University of California
    Inventors: Stephen C. Miller, Thomas S. Scanlan
  • Patent number: 5932595
    Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: August 3, 1999
    Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
  • Patent number: 5905127
    Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: May 18, 1999
    Assignee: The University of Southern Mississippi
    Inventors: Robert Y Lochhead, Lon J Mathias
  • Patent number: 5889056
    Abstract: 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: Grant
    Filed: December 27, 1996
    Date of Patent: March 30, 1999
    Assignee: 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
  • Patent number: 5883293
    Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
    Type: Grant
    Filed: December 5, 1996
    Date of Patent: March 16, 1999
    Assignees: Peptor Ltd., Yissum Research Development Co. of the Hebrew University
    Inventors: Chaim Gilon, Doron Eren, Irina Zeltser, Alon Seri-Levy, Gal Bitan, Dan Muller
  • Patent number: 5874468
    Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ disfunction, in which oxidants are overproduced.
    Type: Grant
    Filed: December 26, 1996
    Date of Patent: February 23, 1999
    Assignees: Yissum, Mor
    Inventors: Daphne Atlas, Eldad Melamed, Daniel Ofen
  • Patent number: 5872286
    Abstract: Dithiocarbamyl carboxylic acids, useful as multifunctional additives for lubricating oils, possess the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each independently is a hydrocarbyl group of from 1 to about 60 carbon atoms and R.sup.3 is a divalent alkylene group of from 1 to about 20 carbon atoms.
    Type: Grant
    Filed: February 13, 1998
    Date of Patent: February 16, 1999
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: John R. Baranski, Cyril A. Migdal, Robert G. Rowland
  • Patent number: 5866604
    Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: February 2, 1999
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo
  • Patent number: 5863931
    Abstract: 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: Grant
    Filed: June 22, 1994
    Date of Patent: January 26, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard Mansfield Beams, Harold Francis Hodson, Richard Michael John Palmer
  • Patent number: 5847205
    Abstract: Homocystine is produced by heating methionine in the presence of sulfuric acid and a hydrogen halide.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: December 8, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Jun Takehara, Shuji Ichikawa, Hiroshi Iwane
  • Patent number: 5750043
    Abstract: This invention relates to water soluble fluorochemical foam stabilizers and film formers derived from polyamines, perfluoroalkyl group containing esters or acid halides and hydrophilic and hydrophobic group containing compounds which react with primary, secondary and tertiary amino groups. The novel foam stabilizers and film formers are useful as additives for aqueous film forming foam fire fighting agents improving the foam stability against polar solvents and enhancing the fire fighting performance.
    Type: Grant
    Filed: August 25, 1994
    Date of Patent: May 12, 1998
    Assignee: Dynax Corporation
    Inventor: Kirtland P. Clark
  • Patent number: 5731459
    Abstract: The invention relates to a process for removing amino acids and/or aminosulphonic acids from preferably aqueous solutions which contain these as impurities by adsorbing the amino acids on zeolites. Solutions to which the process according to the invention can be applied are produced, for example, from the industrial synthesis of oligopeptides in which the amino acids serving as starting materials are always present in solution, sometimes to a not inconsiderable residual concentration, together with the desired end product.
    Type: Grant
    Filed: August 28, 1996
    Date of Patent: March 24, 1998
    Assignee: Degussa Aktiengesellschaft
    Inventors: Stefan Stockhammer, Wiltrud Schafer-Treffenfeldt, Gunter Knaup, Karlheinz Drauz, Elfriede Sextl
  • Patent number: 5723655
    Abstract: The present invention relates to an amine compound represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 represent individually a linear or branched C.sub.1 -C.sub.24 alkyl or alkenyl group which may be substituted by a hydroxyl group, X.sup.1 represents a C.sub.1 -C.sub.6 alkylene or alkenylene group which may be substituted by a hydroxyl, sulfonic or carboxyl group, Y.sup.1 represents a carboxyl or sulfonic group, or a sulfuric acid residue, Y.sup.2 represents a hydroxyl group, a sulfuric acid residue or a group --OCO--X.sup.1 --COOH, Z represents a sulfoalkyl group or a group obtained by removing an amino group from an amino acid or a salt thereof, and n represents a number of 0 or 1, or a salt or quaternized product thereof, an intermediate useful for the preparation thereof, and detergent compositions containing such an amine compound.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: March 3, 1998
    Assignee: Kao Corporation
    Inventors: Mitsuru Uno, Tomohito Kitsuki, Katsumi Kita
  • Patent number: 5686472
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 27, 1993
    Date of Patent: November 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, S. Jane deSolms, Ta Jyh Lee, deceased
  • Patent number: 5676923
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Johannes Platzek, Ulrich Niedballa, Peter Mareski, Bernd Raduchel, Hanns-Joachim Weinmann, Andreas Muhler, Bernd Misselwitz
  • Patent number: 5672599
    Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: September 30, 1997
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Jeffrey A. Robl
  • Patent number: 5646313
    Abstract: New amino acid derivatives, processes for their preparation, and their therapeutic application are described.These amino acid derivatives correspond to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Societe Civile Bioprojet
    Inventors: Denis Danvy, Thierry Monteil, Christophe Lusson, Jean-Charles Schwartz, Claude Gros, Nadine Noel, Jeanne-Marie LeComte, Pierre Duhamel, Lucette Duhamel
  • Patent number: 5616563
    Abstract: A compound of the formula ##STR1## with R being hydrogen, alkyl, cycloalkyl or aryl, which may be substituted with halogen or alkyl, and R' and R.sup.a being hydroxyl, or --O-alkyl, pharmaceutically acceptable salts thereof; or mixtures thereof. An anti-neoplastic composition comprises the compound described above and a pharmaceutically acceptable carrier. In vitro and in vivo methods of preventing or inhibiting the growth and proliferation of neoplastic cells and/or tumors comprise contacting the cells with or administering to a subject an anti-growth and proliferation effective amount of the compound described above.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: April 1, 1997
    Assignee: University of Maryland Baltimore Campus
    Inventors: Donald J. Creighton, Diana S. Hamilton
  • Patent number: 5616312
    Abstract: The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## Wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are the same or different and are --CO--(CH.sub.2).sub.y --SH, --(CH.sub.2).sub.2 --SH, --SO.sub.2 --(SH.sub.2).sub.t --SH,--SH,--(CH.sub.2).sub.q --COOH, and --(CH.sub.2).sub.v --CONR.sup.6 R.sup.7, provided at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a sulfur containing moiety; n is 0 to about 10; i is 2 to about 5; j is 2 to about 5; y is 1 to about 5; z is 1 to about 6; t is 1 to about 5; q is 1 to about 5; v is 1 to about 5; R.sup.6 is H, alkyl, hydroxyalkyl, polyhydroxyalkyl, arylalkyl or alkoxyalkyl; R.sup.7 is H, alkyl, hydroxyalkyl, polyhydroxyalkyl, arylalkyl or alkoxyalkyl; and R.sup.7 can be polyamine when R.sup.6 is H.Methods for imaging using compositions of the invention are also provided.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: April 1, 1997
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: Leonard O. Rosik
  • Patent number: 5614522
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 24, 1995
    Date of Patent: March 25, 1997
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5574184
    Abstract: 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: Grant
    Filed: March 10, 1995
    Date of Patent: November 12, 1996
    Assignee: Mobil Oil Corporation
    Inventors: Shi-Ming Wu, Andrew G. Horodysky
  • Patent number: 5574017
    Abstract: The present invention provides methods and pharmaceutical preparations for inhibiting the growth of bacterial microorganisms.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: November 12, 1996
    Inventor: William G. Gutheil
  • Patent number: 5571940
    Abstract: In this method, one attaches one or more chelatant molecules to a mono- or polyamino intermediate compound I which is temporarily immobilized on a solid phase by a splittable bond. Thereafter, said bond is split to release the desired conjugate moiety, whereby a reactive site is generated at the splitting site. The conjugate can be coupled to a protein homing factor using said reactive site; the latter being single per chelatant molecule, undesirable cross-linking during conjugation is substantially avoided.
    Type: Grant
    Filed: February 3, 1995
    Date of Patent: November 5, 1996
    Assignee: Bracco International B.V.
    Inventor: Paul Palacios
  • Patent number: 5536750
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: July 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham
  • Patent number: 5525629
    Abstract: Hydroxamic acid derivatives of formula (I): ##STR1## wherein R.sup.1 represents hydrogen or an (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl, phenacyl or substituted phenacyl group;R.sup.2 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group,R.sup.3 represents a group --CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl or --CH.sub.2 CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl;R.sup.4 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl or phenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.5 represents hydrogen or a methyl group;n is 0, 1 or 2;and A represents a (C.sub.1 -C.sub.6)hydrocarbon chain optionally substituted with one or more (C.sub.1 -C.sub.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: June 11, 1996
    Assignee: British Bio-Technology Limited
    Inventors: Michael J. Crimmin, William A. Galloway, Andrew J. Gearing