Ring In Alcohol Moiety Patents (Class 560/32)
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Patent number: 5693617Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain proteasome inhibitors. The structure of the inhibitors are also disclosed.Type: GrantFiled: January 15, 1995Date of Patent: December 2, 1997Assignee: ProScript, Inc.Inventors: Ross L. Stein, Yu-Ting Ma, Stephen Brand
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5684018Abstract: This invention relates to novel acyloxyisopropyl carbamates as bioreversible prodrug moieties for amino drugs and to methods of synthesizng these compounds.Type: GrantFiled: December 13, 1994Date of Patent: November 4, 1997Assignee: Merck & Co., Inc.Inventor: Jose Alexander
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Method for lowering oxygen affinity of hemoglobin in redcell suspensions, in whole blood and in vivo
Patent number: 5661182Abstract: Drug compounds are used as allosteric modifiers of hemoglobin present in red blood cells. The compounds bind to only a single pair of symmetry related sites in the central water cavity of hemoglobin at the Lys 99.alpha., Arg 141.alpha., and Asn 108 .beta. residues. When one of the drug compounds is bound to hemoglobin, it will join three separate sub-units of the hemoglobin molecule and stabilize the hemoglobin in a lower oxygen affinity state. Because the compounds used in this method are either not bound by serum albumin or only interact to small degrees with serum albumin, the compounds are active in whole blood and in vivo. The process of allosterically modifying hemoglobin towards a low oxygen affinity state in whole blood and in vivo could be used in a wide variety of applications including in treatments for ischemia, heart disease, wound healing, Alzheimer's, depression, schizophrenia, adult respiratory distress syndrome (ARDS), etc.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Claude Poyart -
Patent number: 5656660Abstract: The present invention describes compounds, methods and compositions effective to treat mast cell mediated inflammatory conditions, such as conjunctivitis, asthma and allergic rhinitis. The compounds of the invention comprise novel mono- and di-aminomethylbenzyl, aminobenzyl, guanidylbenzyl and benzyl tryptase inhibitors. The compositions for treating mast cell mediated inflammatory conditions include oral, inhalant and topical preparations as well as devices comprising such preparations.Type: GrantFiled: May 31, 1995Date of Patent: August 12, 1997Assignee: Arris Pharmaceutical CorporationInventors: Robert T. Lum, Heinz W. Gschwend, Barr E. Bauer, Elaine Kuo, Ken Rice
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Patent number: 5654467Abstract: The invention relates to a process for the production of C-substituted diethylenetriamines of general formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have different meanings.Type: GrantFiled: October 12, 1995Date of Patent: August 5, 1997Assignee: Schering AktiengesellschaftInventors: Orlin Petrov, Jean-Claude Hilscher, Klaus Nickisch, Heribert Schmitt-Willich, Heinz Gries, Bernd Raduchel, Johannes Platzek
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Patent number: 5650508Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M.sub.1 --AA--NH--CHR.sub.2 --CO--CO--NR.sub.3 R.sub.4, M.sub.1 --AA.sub.2 --AA.sub.1 --CO--NR.sub.3 R.sub.4, M.sub.1 --AA--AA--AA--CO--NR.sub.3 R.sub.4, M.sub.1 --AA--AA--AA--AA--CO--NR.sub.3 R.sub.4, or M.sub.1 --AA--CO--NR.sub.3 R.sub.4.Type: GrantFiled: October 6, 1995Date of Patent: July 22, 1997Assignee: Georgia Tech Research CorporationInventor: James C. Powers
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Patent number: 5648375Abstract: Allosteric hemoglobin modifier compound activity on p50 is potentiated by using the compound in combination with a hydrophobic compound such as an anesthetic.Type: GrantFiled: June 7, 1995Date of Patent: July 15, 1997Assignee: Virginia Commonwealth UniversityInventor: Donald J. Abraham
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Patent number: 5637759Abstract: Novel organic compounds and metal ion-containing amino acid chelates are described which are useful in solid phase synthesis of polypeptides and as magnetic resonance imaging (MRI) enhancing agents. The present invention also relates to a convenient and straightforward method to synthesize a metal-ligating amino acid suitable as MRI enhancing agents or for introducing a strong metal binding site at any chosen position in a peptide. Some compounds are designed to be compatible with N-.alpha.-Fmoc peptide synthesis strategy, and can easily be prepared on large scale. Thus, flexible linkers of different lengths and containing various structures can be placed between the .alpha.-carbon backbone of peptides and metal binding moieties. These peptides will provide a variety of affinity cleaving reagents which can be directed against protein or nucleic acid targets. Therefore, these molecules can serve as an important tool to study protein folding, protein-protein and protein-nucleic acid interactions.Type: GrantFiled: July 30, 1992Date of Patent: June 10, 1997Assignee: The Regents of the University of CaliforniaInventors: John E. Hearst, Tariq M. Rana, Matt Ban
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Patent number: 5616776Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.Type: GrantFiled: April 7, 1995Date of Patent: April 1, 1997Assignee: Abbott LaboratoriesInventors: Timothy L. Stuk, Anthony R. Haight, Francis A. J. Kerdesky, M. Robert Leanna, Howard E. Morton, Timothy A. Robbins, David Scarpetti, Jien-Heh J. Tien
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Patent number: 5610297Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M.sub.1 -AA-NH--CHR.sub.2 --CO--CO--NR.sub.3 R.sub.4, M.sub.1 -AA.sub.2 -AA.sub.1 -CO--NR.sub.3 R.sub.4, M.sub.1 -AA-AA-AA-CO--NR.sub.3 R.sub.4, M.sub.1 -AA-AA-AA-AA-CO--NR.sub.3 R.sub.4, or M.sub.1 -AA-CO--NR.sub.3 R.sub.4.Type: GrantFiled: October 6, 1995Date of Patent: March 11, 1997Assignee: Georgia Tech Research Corp.Inventor: James C. Powers
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Patent number: 5602275Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5600035Abstract: Photoreactive compounds are synthesized from 2,5- or 2,6-dintrobenzyl groups. Also disclosed are methods of synthesizing reactive monomers containing 2,5- or 2,6-dintrobenzyl groups.Type: GrantFiled: July 13, 1994Date of Patent: February 4, 1997Assignee: PPG Industries, Inc.Inventors: Charles F. Kahle, II, Neil D. McMurdie, Raphael O. Kollah, Daniel E. Rardon, Gregory J. McCollum
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Patent number: 5587506Abstract: A process for preparing N-protected N-alkylated amino acids of the formula ##STR1## where R.sup.s and R.sup.1 -R.sup.3 have the meanings indicated in the description comprises adding a compound of the abovementioned formula where R.sup.3 is hydrogen to a solution of a base in a non-protic solvent and subsequently adding an alkylating agent.Type: GrantFiled: October 6, 1995Date of Patent: December 24, 1996Assignee: BASF AktiengesellschaftInventors: Klaus Kn uhl, Ulrich Karl, Stefan M uller, Bernd de Potzolli
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Patent number: 5565606Abstract: The invention relates to compounds of the formula I ##STR1## in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes --[CH.sub.2 ].sub.n -- or --O--[CH.sub.2 ].sub.n --, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.Type: GrantFiled: June 8, 1994Date of Patent: October 15, 1996Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breiphol, Jochen Knolle
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Patent number: 5565490Abstract: p-Hydroxyaniline derivatives of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, or unsubstituted or substituted alkyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy;R.sup.4 is unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl,OR.sup.5 or NR.sup.6 R.sup.7, whereR.sup.5, R.sup.6 are unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl, andR.sup.7 is hydrogen or alkyl,and their salts, processes for their preparation, compositions containing them and their use for controlling harmful fungi or pests, and also compounds of the formula VI ##STR2## and their salts, processes for their preparation, compositions containing them and their use as intermediates and for controlling pests are described.Type: GrantFiled: November 10, 1994Date of Patent: October 15, 1996Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Norbert G otz, Harald Rang, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5545640Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.Type: GrantFiled: April 4, 1995Date of Patent: August 13, 1996Assignee: Bio-Mega/Boehringer Ingeleheim Research Inc.Inventors: Pierre L. Beaulieu, Ingrid Guse
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Patent number: 5543553Abstract: Novel functionalized peroxides which may be used as crosslinking, grafting and curing agents, initiators for polymerization reactions and as monomers for condensation polymerizations to form peroxy-containing polymers, which in turn can be used to prepare block and graft copolymers, have the following Formula I: ##STR1## R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y.sup.1, Y.sup.2, Y.sup.3, Z.sup.1, Z.sup.2, x, y and z are as defined in the Summary of the Invention.Type: GrantFiled: June 6, 1995Date of Patent: August 6, 1996Assignee: Elf Atochem North America, Inc.Inventor: Daryl L. Stein
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Patent number: 5504242Abstract: The present invention provides the compound containing one hydroxyl group and one acyl carbamate group per molecule, which is useful for introducing the acyl carbamate group in chemical materials. By employing the present compound, it becomes possible to introduce the acyl carbamate group in various chemical materials other than acrylic polymers. According to the present process, the compound containing one hydroxyl group and one acyl carbamate group per molecule is provided in excellent yield with a suppressed amount of by-product.Type: GrantFiled: May 5, 1995Date of Patent: April 2, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Masami Yabuta, Satoshi Urano
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Patent number: 5498740Abstract: Compositions which, in the form of aqueous dispersions or of solutions in organic solvents, are suitable for the treatment of fiber materials can be obtained by reaction of organic phosphites and quinones and subsequent reaction with mono-, di- or polyisocyanates. Flame-retardant properties having a good permanence are imparted, above all, to fabrics comprising polyester fibers by this procedure.Type: GrantFiled: March 5, 1993Date of Patent: March 12, 1996Assignee: Ciba-Geigy CorporationInventors: Salman Dermeik, Martina Wanner, Karl-Heinz Lemmer, Reinhold Braun
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Patent number: 5491253Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)--wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.Type: GrantFiled: July 27, 1994Date of Patent: February 13, 1996Assignee: Abbott LaboratoriesInventors: Timothy L. Stuk, Michael S. Allen, Anthony R. Haight, Francis A. Kerdesky, Denton C. Langridge, M. Robert Leanna, Linda M. Lijewski, Laura Melcher, Howard E. Morton, Daniel W. Norbeck, Daniel S. Reno, Timothy A. Robbins, David Scarpetti, Hing L. Sham, Thomas J. Sowin, Jien-Heh J. Tien, Chen Zhao
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Patent number: 5488132Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: April 22, 1994Date of Patent: January 30, 1996Assignee: Monsanto CompanyInventor: John J. Talley
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Patent number: 5484463Abstract: Poly(oxyalkylene) hydroxy and amino aromatic carbamates having the formula: ##STR1## or a fuel-soluble salt thereof; wherein X is hydroxy or amino;R is hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, lower alkoxy having 1 to 6 carbon atoms, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms;R.sub.3 and R.sub.4 are each independently hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sub.5 is hydrogen, alkyl having 1 to 30 carbon atoms, phenyl, aralkyl or alkaryl having 7 to 36 carbon atoms, or an acyl group having the formula: ##STR2## wherein R.sub.6 is alkyl having 1 to 30 carbon atoms, phenyl, or aralkyl or alkaryl having 7 to 36 carbon atoms;and n is an integer from 5 to 100.Type: GrantFiled: May 2, 1994Date of Patent: January 16, 1996Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5481013Abstract: Compounds of the formula ##STR1## in which A is oxygen, sulfur or --NR.sub.1 --;B is C.sub.2 -C.sub.6 alkylene,D-E is --O--E, --S--E, --O--CH.sub.2 --E, --O--C(.dbd.O)--E, --O--C(.dbd.O)--O--E, --O--C(.dbd.O)--N(H)--E or --O--C(.dbd.S)--N(H)--E;E is phenyl; phenyl which is substituted by one to three substituents; a five-membered aromatic heterocycle having one to three hetero atoms; a five-membered aromatic heterocycle which has one to three hetero atoms and which is substituted by one or two substituents; a six-membered aromatic heterocycle which has one to three nitrogen atoms; or a six-membered aromatic heterocycle which has one to three nitrogen atoms and which is substituted by one or two substituents;L is halogen or methyl;X is fluorine;Y is chlorine or fluorine;Z is hydrogen, fluorine or methyl;m is the number zero, one, two, three, four or five;n is the number zero, one or two andR.sub.1 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: June 23, 1993Date of Patent: January 2, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Thomas Pitterna, Manfred Boger
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Patent number: 5459222Abstract: Polyurethanes and polyesters are described which are the reaction products of an aromatic, aliphatic or cycloaliphatic diisocyanate, or of a diacid or diacid derivative respectively, with a diol containing a pendent UV-absorbing moiety, optionally also with one or more other diols or diamines. These UV-absorbing polycondensates can be applied to the surfaces of substrates by exhaustion methods or by spraying and act to protect polymers and dyes from degradation by UV radiation. They are therefore useful, either alone or in combination with other coating materials, for the treatment of wood, paper, textiles, leather or other surfaces which are exposed to degrading radiation.Type: GrantFiled: June 4, 1993Date of Patent: October 17, 1995Assignee: Ciba-Geigy CorporationInventors: Juliana Rodgers, Istvan Borsody, Athanasios Karydas, Robert A. Falk, Karl F. Mueller, Michele Kovaleski
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Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
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Patent number: 5432191Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: July 30, 1993Date of Patent: July 11, 1995Assignee: The Center for Innovative TechnologyInventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad, Gajanan S. Joshi, Jayashree Panikker
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Patent number: 5413614Abstract: Mannich condensation products prepared by the condensation of a compound of the formula: ##STR1## wherein R is hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 is hydrogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, alkyl, phenyl, aralkyl, alkaryl, or an acyl group of the formula: ##STR2## wherein R.sub.6 is alkyl, phenyl, aralkyl or alkaryl; and n is an integer from 5 to 100;with an aldehyde and a nitrogen base selected from ammonia, lower alkylamine, a polyamine and mixtures thereof.The Mannich condensation products and their fuel soluble salts are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: May 2, 1994Date of Patent: May 9, 1995Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5411964Abstract: A phenylalanine-glycine compound of formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described. The novel conjugate of the phenylalanine-glycine compound and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered alone or as a mixture with phenylalanine.Type: GrantFiled: March 15, 1993Date of Patent: May 2, 1995Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koichi Niimura, Takako Kawabe, Takao Ando, Kenichi Saito
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Patent number: 5391571Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.Type: GrantFiled: May 13, 1993Date of Patent: February 21, 1995Assignee: American Home Products CorporationInventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
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Patent number: 5374769Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: December 24, 1992Date of Patent: December 20, 1994Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5364961Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: June 15, 1992Date of Patent: November 15, 1994Assignee: Monsanto CompanyInventor: John J. Talley
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Patent number: 5318989Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.Type: GrantFiled: December 18, 1992Date of Patent: June 7, 1994Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Mark D. Wittman
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Patent number: 5312831Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 12, 1993Date of Patent: May 17, 1994Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5306842Abstract: A method for manufacturing a purified aromatic urethane. Aromatic urethanes are synthesized from a N,N'-disubstituted urea and an organic hydroxyl compound in a reaction medium. The organic hydroxyl compound and the primary aromatic amine side product which are present in the reaction mixture is distilled off and removed from the reaction mixture leaving a distillation bottom. The N,N'-disubstituted urea is separated and removed from the distillation bottom by solvent extraction of the aromatic urethane, and the aromatic urethane in the extract phase obtained in said solvent extraction is separated and purified.Type: GrantFiled: April 29, 1992Date of Patent: April 26, 1994Assignee: NKK CorporationInventors: Takao Ikariya, Masanori Itagaki, Masatsugu Mizuguchi, Makoto Miyazawa, Sachiko Yamamoto
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Patent number: 5302742Abstract: N-acylated p-amino-phenols can be prepared by catalytical hydrogenation of the underlying aromatic nitro compounds in a reaction medium of aqueous sulfuric acid in the sense of a Bamberger type reaction at elevated temperature, optionally in the presence of a water-miscible organic solvent, and subsequent reaction of this reaction mixture with an acid chloride, optionally in the presence of an acid binder and optionally in the presence of a diluent.Type: GrantFiled: May 5, 1993Date of Patent: April 12, 1994Assignee: Bayer AktiengesellschaftInventors: Heinz Landscheidt, Alexander Klausener, Heinz-Ulrich Blank
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Patent number: 5300678Abstract: A process for the preparation of a .omega.-(O-substituted urethano)alkylcarboxylate, wherein a lactam having from 4 to 9 ring members, which can have alkyl, alkenyl, cycloalkyl, or aralkyl groups containing up to 12 carbon atoms as substituents, is reacted with a carbonic diester of an alkanol, alkenol, cycloalkanol, or aralkanol containing up to 16 carbon atoms, at a temperature of from 25.degree. to 300.degree. C. in the presence of a catalytically effective amount of a base.Type: GrantFiled: February 5, 1993Date of Patent: April 5, 1994Assignee: BASF AktiengesellschaftInventors: Franz Merger, Martin Brudermueller
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Patent number: 5290803Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: January 19, 1993Date of Patent: March 1, 1994Assignee: The Center of Innovative TechnologyInventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad
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Patent number: 5260439Abstract: The present invention relates to a high surface hardness transparent resin having excellent scratch resistance, heat resistance and chemical resistance, a glazing material, a protective cover for display devices, an optical lens and a hard coat material comprising the aforesaid resin, and a novel polymerizable monomer which is useful as a raw material of the above-mentioned resin.The monomer is represented by the formula (I) ##STR1## (wherein R is an aliphatic residue having or not having an halogen atom, an oxygen atom, an alicyclic ring, a heterocyclic ring or an aromatic ring, an alicyclic residue, or a heterocyclic residue, n is an integer of 1 to 4, when n=1, X is oxygen or sulfur, when n.gtoreq.2, X's are all oxygen or all sulfur, one X is oxygen while the other X or X's are sulfur, one X is sulfur while the other X or X's are oxygen, or two X's are oxygen while the other X's are sulfur).Type: GrantFiled: December 16, 1991Date of Patent: November 9, 1993Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Toshiyuki Suzuki, Katsuyoshi Sasagawa, Masao Imai, Yoshinobu Kanemura
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Patent number: 5252745Abstract: Antimicrobial compounds of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of H, an amine protective group, and a moiety of the formula ##STR2## wherein R.sup.2, R.sup.5, and R.sup.6 are independently selected from H and an amine protective group;R.sup.3 and R.sup.4 are independently selected from H, lower alkyl, aryl, arylalkyl, CH.sub.2 OR, CH.sub.2 SR or CH(CH.sub.3)OR;R=H, propargyl lower alkyl, arylalkyl or aryl;wherein R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 can be joined to form a ring; and wherein when R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 are both H, the compound is either in free base form or in salt form.Type: GrantFiled: May 21, 1991Date of Patent: October 12, 1993Assignee: Rohm and Haas CompanyInventors: Margaret M. Bowers-Daines, Barry C. Lange
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Patent number: 5250701Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: January 19, 1993Date of Patent: October 5, 1993Assignee: Center for Innovative TechnologyInventors: Donald J. Abraham, Ramnarayan Randad
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Patent number: 5248785Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: May 18, 1992Date of Patent: September 28, 1993Assignees: Virginia Commonwealth University, Center for Innovative TechnologyInventors: Donald J. Abraham, Ramnarayan Randad
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Patent number: 5247121Abstract: The alkyl esters of N-carboalkyloxy-11-aminoundecanoic acids have the following general formula: ##STR1## wherein R is linear or branched C.sub.7-30 alkyl, linear or branched C.sub.4-22 alkenyl or a radical of formula: ##STR2## wherein n is 0 to 5 R" is linear or branched C.sub.7-30 alkyl, andR' is linear C.sub.10-18 alkyl.These esters, and esters wherein R is additionally hydrogen or C.sub.1-6, have an application as thickening agents in organic media particularly in the cosmetic field.Type: GrantFiled: February 4, 1992Date of Patent: September 21, 1993Assignee: L'OrealInventors: Henri Sebag, Didier Semeria
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Patent number: 5237090Abstract: A vinyl polymerizable reaction product useful in preparing pigment grind vehicles having improved grind time, viscosity properties and color properties is disclosed. The reaction product can be prepared by reaction of an ester with isopropenyl-.alpha.,.alpha.-dimethylbenzylisocyanate. The resulting product is a urethane ester which can be homopolymerized or copolymerized with other vinyl monomers. The invention is also directed toward the resulting polymeric grind vehicle and pigment pastes made therewith.Type: GrantFiled: September 27, 1991Date of Patent: August 17, 1993Assignee: PPG Industries, Inc.Inventors: Shanti Swarup, Gregory J. McCollum, Ronald M. Shewchuk, Jonathan T. Martz
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Patent number: 5223638Abstract: The present invention provides a process for preparing urethanes and carbonates from an amine or an alcohol, carbon dioxide and a hydrocarbyl halide. The amine or alcohol is reacted with carbon dioxide in a suitable solvent system and in the presence of an amidine or guanidine base, to form the ammonium carbamate or carbonate salt which is then reacted in a polar aprotic solvent with a hydrocarbyl halide. Polymer products can also be prepared utilizing this process or utilizing the resulting urethanes and carbonates under standard polymerization conditions.Type: GrantFiled: April 29, 1991Date of Patent: June 29, 1993Assignee: Monsanto CompanyInventors: William D. McGhee, Barry L. Parnas, Dennis P. Riley, John J. Talley
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Patent number: 5202483Abstract: Ethylenically unsaturated compounds of the general formula I ##STR1## where R.sub.1 is alkyl of 1 to 4 carbon atoms, cyclopropyl, cyclopentyl, cyclohexyl, phenyl or phenyl in which some or all of the hydrogen atoms have been replaced by radicals R.sup.4, not more than two substituents R.sup.4 being identical, or R.sup.1 together with R.sup.2 or together with R.sup.6 forms a --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --CH.sub.2 -- bridge,R.sup.4 is alkyl of 1 to 24 carbon atoms, --OH, --O--R.sup.7, --S--R.sup.7, ##STR2## R.sup.2 or R.sup.6, independently of one another, both are hydrogen, or one of the radicals R.sup.4, or, where R.sup.1 is aryl,R.sup.2 or R.sup.6 is a direct bond to R.sup.1 in the ortho-position with respect to the carbonyl group, andR.sup.3 and R.sup.5 are each hydrogen, one of the radicals R.sup.4 or a group the general formula II ##STR3## where R.sup.7 and R.sup.8 are each alkyl of 1 to 4 carbon atoms,R.sup.9 is cycloalkyl of 5 or 6 carbon atoms,R.sup.Type: GrantFiled: March 1, 1991Date of Patent: April 13, 1993Assignee: BASF AktiengesellschaftInventors: Gerd Rehmer, Kaspar Bott
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Patent number: 5202486Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.Type: GrantFiled: July 31, 1990Date of Patent: April 13, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Joel C. Barrish, Steven H. Spergel
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Patent number: 5194660Abstract: Processes for producing carbamates comprise contacting a first reactant selected from primary amine components, secondary amine components, urea components and mixtures thereof; carbon monoxide; at least one organic hydroxyl component and at least one oxygen-containing oxidizing agent in the presence of a catalyst composition comprising at least one metal macrocyclic complex, preferably in the further presence of a halogen component.Type: GrantFiled: December 21, 1990Date of Patent: March 16, 1993Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Tak W. Leung, Bernard D. Dombek
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Patent number: 5194661Abstract: Substituted benzyl carbamates of the formula ##STR1## in which: R is a member selected from the group consisting of halogen, trifluoromethyl, cyano, NO.sub.2, C.sub.1 -C.sub.3 haloalkyloxy, phenoxy, pyridyloxy, and substituted phenoxy and substituted pyridyloxy substituted with one or more members of the group consisting of halogen and trifluoromethyl;R.sub.1 is C.sub.1 -C.sub.4 alkyl; andR.sub.2 is a member selected from the group consisting of pyridyl, phenyl and substituted pyridyl and substituted phenyl substituted with one or more of the group consisting of H, cyano, halogen,C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 haloalkyl;and their use as herbicides are disclosed herein.Type: GrantFiled: August 20, 1990Date of Patent: March 16, 1993Assignee: ICI Americas Inc.Inventor: Don R. Baker
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Patent number: 5191083Abstract: This invention is directed to the preparation of polymerizable monomers that are prepared from 1-(1-isocyanato-1-methylethyl)-3-(1-methylethenyl) benzene (m-TMI) and 1-(1-isocyanato-1-methylethyl)-4-(1-methylethenyl) benzene (p-TMI). The monomers prepared from m- and p-TMI can contain numerous chemical moieties, and when polymerized, produce polymers that have chemically bonded to the polymeric backbone the functional moiety. More specifically, these TMI derived monomers may contain chain breaking antioxidant moieties, peroxide decomposing antioxidant moieties, ultraviolet stabilizing moieties, triplet quenching moieties, and other chemical moieties that are useful in polymers.Type: GrantFiled: February 28, 1989Date of Patent: March 2, 1993Assignee: The Goodyear Tire & Rubber CompanyInventors: Howard A. Colvin, Kirkwood S. Cottman, Dane K. Parker