Additional Nitrogen In Acid Moiety Patents (Class 560/159)
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Patent number: 6777443Abstract: Compounds of the formula wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.Type: GrantFiled: May 9, 2002Date of Patent: August 17, 2004Assignee: Novartis AGInventor: Cynthia Anne Fink
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Patent number: 6740741Abstract: Novel diazo derivatives useful for the deacidification of paper material and the process for their preparation comprising three steps starting from an amine and ethyl chlorocarbonate, are described.Type: GrantFiled: July 3, 2002Date of Patent: May 25, 2004Assignees: Consiglio Nazionale delle Ricerche, Universita'degli Studi di UdineInventors: Antonio Zappala', Andrea Gorassini, Angelo Guimanini, Giancarlo Verardo
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Patent number: 6720306Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof, Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, CType: GrantFiled: January 12, 2001Date of Patent: April 13, 2004Assignee: Enzon Pharmaceuticals, Inc.Inventors: Richard B. Greenwald, Hong Zhao
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Patent number: 6710085Abstract: The present invention is directed to new compositions of matter comprising the reaction products of a carboxylic acid and a urea having the formula: where R1, R2, R3 and R4 are the same or different and are selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, allyl, vinyl and alkoxyl groups having from 1-6 carbon atoms, substituted and unsubstituted phenyl groups and the halides. Preferably, the reaction product of the present invention is N,N′-diformylurea or N,N′-diacetylurea. These reaction products, e.g., diformylurea, have been found to produce significantly improved growth in a variety of agricultural products when applied to the seed, to the surrounding soil or to the foliage of the emerging plant. Because of the similarity in the carbon, nitrogen, oxygen structure of these reaction products with many biological compounds, it is believed that the reaction products of the present invention may find use in a variety of biological applications.Type: GrantFiled: July 29, 2002Date of Patent: March 23, 2004Assignee: Stoller Enterprises, Inc.Inventor: Frank William Dean
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Publication number: 20040044072Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: December 6, 2002Publication date: March 4, 2004Inventors: Ruth TenBrink, Michel Maillard, Martha Warpehoski
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Publication number: 20040039224Abstract: A process for amino acid derivatives shown by the below general formula (I): 1Type: ApplicationFiled: April 7, 2003Publication date: February 26, 2004Inventors: Hisafumi Ikeda, Isao Saito, Yushin Nakamura
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Publication number: 20040014940Abstract: The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.Type: ApplicationFiled: June 11, 2003Publication date: January 22, 2004Inventors: Stephen P. Raillard, Cindy X. Zhou, Fenmei Yao, Suresh Kumar Manthati, Jia-Ning Xiang, Mark A. Gallop
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Publication number: 20040006224Abstract: A method of preparing a 2-alkyl amino acid involves the aziridination of an alkylacrylate and the opening of the aziridine ring by addition of a side chain. This method can result in the preparation of enantiomeric excess of a 2-alkyl amino acid. The invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: January 8, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 6670393Abstract: The present invention provides novel carbamate-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof, wherein (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an integer from 1 to 8; (d) X is an anion or polyanion; and (e) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions, and a kit for preparing the same.Type: GrantFiled: June 25, 2001Date of Patent: December 30, 2003Assignee: Promega Biosciences, Inc.Inventors: David Aaron Schwartz, Bob Dale Brown, Brian Patrick Dwyer
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Publication number: 20030199577Abstract: The present invention relates to a substrate useful to bio-chips comprising a molecular layer having low surface density of amines, and it provides a compound of Chemical Formula (1) represented by N—CBZ-[1]amine-[9]acid having a carboxylic acid, a substrate comprising a surface having a molecular layer prepared by reacting amine groups of aminosilylated surface of the substrates with a compound of Chemical Formula (1) having a cone shape, and methods for preparing the same.Type: ApplicationFiled: March 5, 2003Publication date: October 23, 2003Inventors: Joon-Won Park, Jeo-Young Shim, Joong-Ho Moon, Bong-Jin Hong
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Patent number: 6635621Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.Type: GrantFiled: January 30, 2002Date of Patent: October 21, 2003Assignee: Naeja Pharmaceutical Inc.Inventors: Rajeshwar Singh, Nian Zhou, Andhe V. N. Reddy, George Thomas, Qizhu Ding, Jadwiga Kaleta, Ronald George Micetich, Mark Whittaker
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Publication number: 20030153784Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1Type: ApplicationFiled: February 25, 2003Publication date: August 14, 2003Inventors: Fabio Giannessi, Natalina Dell'uomo, Maria Ornella Tinti, Francesco De Angelis
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Publication number: 20030144214Abstract: GABA-related pro-drugs of the formula (III) are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present.Type: ApplicationFiled: November 21, 2002Publication date: July 31, 2003Inventors: David Clive Blakemore, Justin Stephen Bryans, Sophie Caroline Williams
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Publication number: 20030144542Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: ApplicationFiled: November 28, 2001Publication date: July 31, 2003Inventors: Gunnar J. Hanson, John S. Baran
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Publication number: 20030135066Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: ApplicationFiled: November 28, 2001Publication date: July 17, 2003Inventors: Gunnar J. Hanson, Baran S. John
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Publication number: 20030130522Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: ApplicationFiled: November 28, 2001Publication date: July 10, 2003Inventors: Gunnar J. Hanson, John S. Baran
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Publication number: 20030100512Abstract: Compounds of formula (I) are disclosed which are diasteroisomers of a known class of protease inhibitors. The compounds inhibit &ggr;-secretase, and find use in the treatment and/or prevention of Alzheimer's disease.Type: ApplicationFiled: October 7, 2002Publication date: May 29, 2003Inventors: Alan John Nadin, Graeme Irvine Stevenson
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Patent number: 6569411Abstract: Serine carbonates of formula I are precursors for organoleptic compounds, masking agents and antimicrobial agents. Further they are alternative substrates for malodor producing enzymes. The symbols in formula I are defined in claim 1.Type: GrantFiled: August 15, 2002Date of Patent: May 27, 2003Assignee: The Gillette CompanyInventors: Georg Frater, Denise Anderson, Frank Kumli, Jens Wittenberg, Virginia Streusand Goldman
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Publication number: 20030023017Abstract: The invention relates to positional isomer diethyloctandioldicarbamates and diethyloctandioldiallophanates, to a method for the production thereof and to the use thereof as synthetic building blocks and constituents of adhesives, luting compounds and coating materials.Type: ApplicationFiled: July 22, 2002Publication date: January 30, 2003Inventors: Heinz-Peter Rink, Jochem Henkelmann, Werner-Alfons Jung, Paul J Harris, Swaminathan Ramesh
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Publication number: 20020193432Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.Type: ApplicationFiled: March 5, 2002Publication date: December 19, 2002Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Chris Wysong
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Publication number: 20020173469Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: May 30, 2002Publication date: November 21, 2002Applicant: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Publication number: 20020103190Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 1, 2002Inventors: David Lauffer, Michael Mullican
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Patent number: 6414158Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.Type: GrantFiled: July 6, 2000Date of Patent: July 2, 2002Assignee: Bayer AKtiengesellschaftInventors: Hubert Dyker, Andrew Plant, JĂĽrgen Scherkenbeck, Christoph Erdelen, Achim Harder
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Patent number: 6395763Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.Type: GrantFiled: June 23, 2000Date of Patent: May 28, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean P. Stamos, Randy S. Bethiel
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Patent number: 6395713Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.Type: GrantFiled: July 21, 1998Date of Patent: May 28, 2002Assignee: Ribozyme Pharmaceuticals, Inc.Inventors: Leonid Beigelman, Jasenka Matulic-Adamic, Alex Karpeisky, Peter Haeberli, David Sweedler, Mark Reynolds, Nilabh Chaudhary, John Min
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Patent number: 6392001Abstract: The present invention relates to a process for the production of polyisocyanates containing allophanate groups and having aliphatically and/or cycloaliphatically bound isocyanate groups by reacting organic compounds containing urethane groups with organic polyisocyanates containing aliphatically and/or cycloaliphatically bound isocyanate groups in the presence of tin compounds and to the use of these polyisocyanates, optionally blocked with blocking agents for isocyanate groups, as an isocyanate component in the production of polyurethanes, in particular polyurethane coatings.Type: GrantFiled: May 1, 1995Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Harald Mertes, Josef Pedain, Reinhard Halpaap
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Patent number: 6380323Abstract: The invention provides a resin composition comprising (A) a polymer comprising at least 1 primary carbamate functional group and 1 or more quaternary ammonium groups, and (B) a carbamate functional reactive additive that is generated in situ during the production of polymer (A).Type: GrantFiled: December 15, 1999Date of Patent: April 30, 2002Assignee: BASF CorporationInventor: Timothy S. December
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Patent number: 6362359Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer, X represents OR′ or NHR′ and R′ represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I, R″ represents a divalent, linear or branched aliphatic group containing 2 to 10 carbon atoms, provided that there are at least two carbons between the oxygen atoms wherein the aliphatic group may optionally be substituted by heteroatoms to form ether or ester groups, and n is 2 to 6.Type: GrantFiled: December 1, 2000Date of Patent: March 26, 2002Assignee: Bayer CorporationInventors: Sze-Ming Lee, Karen M. Henderson, Patricia B. Jacobs, Robert A. Sylvester, Douglas A. Wicks
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Patent number: 6339103Abstract: The new compound, dimethy[3-(propoxycarbonylamino)propyl]ammonium O-ethylphosphonate, having fungicidal activity, its preparation, compositions comprising it and methods for its use in agriculture.Type: GrantFiled: December 12, 2000Date of Patent: January 15, 2002Assignee: Aventis CropScience UK LimitedInventors: Norman John De'Ath, John Klostermyer, Albert Schirring, Michael Alan Webb, Geoffrey Gower Briggs
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Patent number: 6331542Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: April 19, 2000Date of Patent: December 18, 2001Assignee: SmithKline Beecham CorporationInventors: Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
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Patent number: 6316662Abstract: Carbamate solutions are obtainable by reacting at least one alkanolamine with carbon dioxide in, as solvent, at least one organic compound having a molecular weight of from 60 to 600 and containing at least one hydroxyl group, wherein the carbamate contains at least 0.Type: GrantFiled: November 12, 1999Date of Patent: November 13, 2001Assignee: BASF AktiengesellschaftInventors: Peter Woo, Anke Schulze, Edmund Stadler, Dieter Tintelnot, Udo Hadick, Ralf Hinrichs, Horst HĂĽrkamp, Klaus Sobolewski
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Patent number: 6284777Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, inducing osteoporosis; gingival disease including gingivitis and periodontists; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: April 19, 2000Date of Patent: September 4, 2001Assignee: SmithKline Beecham CorporationInventors: Stacie Marie Halbert, Scott Kevin Thompson
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Patent number: 6265590Abstract: Protected amino acid derivatives of general formula (I) and methods for the prepatation of the derivatives are provided.Type: GrantFiled: July 12, 1999Date of Patent: July 24, 2001Assignee: Hyundai Pharm, Ind. Co., Ltd.Inventors: Vladimir V. Samukov, Aydar N. Sabirov, Pavel I. Pozdnyakov, Hack-Joo Kim, Young-Deug Kim
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Patent number: 6258976Abstract: Disclosed are processes for the preparation of compounds of the formula (I): H2N—(CH2)n—A—(CH2)m—NH2, or (II): H2N—(CH2)n—NH—C(═NR1)—NH—(CH2)m—NH2, wherein n and m are each independently an integer from 2 to 8; A is selected from the group consisting of —NR1—, —NR1—(CH2)r—NR1— and —NR1—(CH2)r—NR1—(CH2)z—NR1—, wherein r and z are an integer ranging from 2 to 8; and R1 is hydrogen or a protecting group having a carbonyl group.Type: GrantFiled: March 19, 1999Date of Patent: July 10, 2001Inventors: Francis Johnson, Ramesh C. Gupta
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Patent number: 6258931Abstract: The invention relates to a method and reagent for the synthesis of peptides containing deoxyhypusine, the reagent having the formula: wherein: Q1 and Q2 may be the same or different and are amino protective groups, and Q3 is an amino protective group which is orthogonal to Q1 and Q2. The invention also relates to peptides of formula S-deoxyHpu-T (2) that may be synthesized using the reagent of the invention, wherein deoxyHpu is the deoxyhypusine residue, S and T are each independently peptide residues from zero to 12 amino acids in length.Type: GrantFiled: August 19, 1998Date of Patent: July 10, 2001Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 6251939Abstract: The present invention provides novel carbamate-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof, wherein (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an integer from 1 to 8; (d) X is an anion or polyanion; and (e) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions, and a kit for preparing the same.Type: GrantFiled: June 5, 1996Date of Patent: June 26, 2001Assignee: Promega Biosciences, Inc.Inventors: David Aaron Schwartz, Bob Dale Brown, Brian Patrick Dwyer
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Patent number: 6251382Abstract: Polymeric compounds of the formula: (D)n—M—(R1)m (I) wherein (m) and (n) independently selected positive integers, preferably from about 1 to about 6 each; D is a residue of a biologically active moiety; M is a multifunctional linker/spacer moiety; and R1 is a polymer residue are disclosed. Methods of preparing the same and methods of treatment using the same are also included as part of the present invention.Type: GrantFiled: April 15, 1999Date of Patent: June 26, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Anthony J. Martinez, Yun H. Choe, Annapurna Pendri
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Patent number: 6235929Abstract: A novel class of tripeptide &agr;-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 M1—AA—AA—AA—CO—NR3R4.Type: GrantFiled: December 27, 1996Date of Patent: May 22, 2001Assignee: Georgia Tech Research CorporationInventor: James C Powers
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Patent number: 6221116Abstract: Aminocarbamates of polyalkylphenoxyalkanols having the formula: wherein R is a polyalkyl group having an average molecular weight in the range of about 600 to 5,000; R1 and R2 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; and A is a polyamine moiety having at least one basic nitrogen atom, wherein the polyamine is connected to the carbonyl group through one of its nitrogen atoms to form a carbamate linkage. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: September 27, 1996Date of Patent: April 24, 2001Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 6207173Abstract: Lysine derivatives, salts of the derivatives, their optical isomers of D or L configuration, or their mixtures, the derivatives containing an Ne-alkoxy or Ne-alkenoxycarbonyl group and having the formula: in which: R represents a linear or branched C13-C24 alkyl radical or alkenyl radicals, are used in cosmetic, pharmaceutical, hygiene or food compositions, particularly compact compositions.Type: GrantFiled: April 23, 1999Date of Patent: March 27, 2001Assignee: L'OrealInventors: Michel Philippe, Thierry Bordier
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Patent number: 6187938Abstract: The invention relates to amino acid derivatives of general formula (I), wherein R1 is H or CH3, X is H or NR2R3, wherein R2 is H, CH3, COH or COCH3 and R3 is H, CH3 or COO—Z wherein Z is R2R3 NH+CHR1(CH2)nCOO(CH2)mCH2Y; Y is H, CH3 or NHR4, wherein R4 a COO—NH3+CH2(CH2)mOOC(CH2)nCH3, the meaning of group (CH2)m being selected from alkyls, secondary alkyls, monocycloalkyls, bicycloalkyls and tricycloalkyls having from 4 to 15 carbon atoms and n having a value of from 3 to 14.Type: GrantFiled: December 21, 1999Date of Patent: February 13, 2001Assignee: Bochemie, s.r.o.Inventors: Alexandr Hrabálek, Pavel Dole{haeck over (z)}al, Old{haeck over (r)}ich Farsa, Ale{haeck over (s)} Krebs, Ale{haeck over (s)} Kroutil, Martin Roman, Zde{haeck over (n)}ka {haeck over (S)}klubalová
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Patent number: 6160160Abstract: The present invention relates to a process for preparing optionally substituted benzyl carbazates of formula (I) ##STR1## wherein each R.sup.1 independently represents C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, di(C.sub.1 -C.sub.4 -alkyl)amino, nitro, halogen, hydroxyl, the group X-R.sup.3, wherein X represents O or S and R.sup.3 represents straight-chain or branched C.sub.1 -C.sub.4 -alkyl, the group COOR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 -alkyl, the group NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 independently represent C.sub.1 -C.sub.4 -alkyl, or a C.sub.3 -C.sub.6 -cycloalkyl group that is optionally substituted by straight-chain or branched C.sub.1 -C.sub.4 -alkyl groups, andn is an integer from 0 to 5,by reacting a dialkyl carbonate with an optionally substituted benzyl alcohol in the presence of a catalyst, separating off the resulting reaction mixture from the catalyst, and subsequently reacting the separated reaction mixture with hydrazine hydrate.Type: GrantFiled: August 6, 1999Date of Patent: December 12, 2000Assignee: Bayer AktiengesellschaftInventors: Edwin Ritzer, Robert Sollner, Claus Dreisbach, Frank Jelitto
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Patent number: 6156895Abstract: An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxamide, an intermediate for an HIV protease inhibitor.Type: GrantFiled: August 4, 1999Date of Patent: December 5, 2000Assignee: Merck & Co., Inc.Inventors: Kai Rossen, Philip J. Pye, Ralph P. Volante, Paul J. Reider
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Patent number: 6150542Abstract: The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor.The compounds under consideration are compounds of the formula:X--(Z).sub.n --CO--NH--CH--(COO--Y)--CH.sub.2 CH.sub.2 CONH.sub.2I.Type: GrantFiled: April 13, 1999Date of Patent: November 21, 2000Assignee: Givaudan Roure (International) SAInventors: Gonzalo Acuna, Georg Frater, Peter Gygax
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Patent number: 6150457Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I ##STR1## wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer,X represents OR' or NHR' andR' represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I andn has a value of 2 to 6.The present invention also relates to one-component, thermoset coating compositions containing the compounds of formula I and a cross-linking component that is reactive with these compounds. Finally, the present invention relates coatings, sealants and adhesives prepared from these thermoset compositions.Type: GrantFiled: November 23, 1998Date of Patent: November 21, 2000Assignees: Bayer Corporation, Bayer AktiengesellscaftInventors: Sze-Ming Lee, Douglas A. Wicks, Eberhard Koenig, Carol L. Kinney, Karen M. Henderson
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Patent number: 6140530Abstract: This invention relates to quinidine derivatives and immunogenic conjugates and reporter conjugates prepared therefrom. The immunogenic conjugates and reporter conjugates are useful for eliciting antibodies and for performing immunoassays for quinidine. A particle agglutination immunoassay for quinidine is also provided.Type: GrantFiled: March 27, 1997Date of Patent: October 31, 2000Assignee: Dade Behring Inc.Inventor: Donald M. Simons
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Patent number: 6124345Abstract: The present invention relates to carbomoylcarboxamide oximes of the formula (I): ##STR1## or salts thereof, processes for preparing the carbomoylcarboxamide oximes, compositions containing the carbomoylcarboxamide oximes and processes for controlling harmful fungi with an effective amount of the carbomoylcarboxamide oximes.Type: GrantFiled: November 24, 1998Date of Patent: September 26, 2000Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Karl Eicken, Reinhard Kirstgen, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6114325Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.Type: GrantFiled: October 22, 1998Date of Patent: September 5, 2000Assignee: Shiseido Co., Ltd.Inventors: Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima, Koji Kobayashi
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Patent number: 6110946Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: July 1, 1998Date of Patent: August 29, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
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Patent number: 6028093Abstract: Fungicidal mixtures, comprisinga) a carbamate of the formula I ##STR1## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, and/orb) an oxime ether of the formula II, ##STR2## where the substituents have the following meanings: X is oxygen or amino;Y is CH or N;Z is oxygen, sulfur, amino or C.sub.1 -C.sub.4 -alkylaminoR' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkyl-methyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio; andc) a carbamate of the formula III(CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 CH.sub.Type: GrantFiled: October 21, 1998Date of Patent: February 22, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer, Dietrich Mappes, Joachim Leyendecker, Herbert Bayer, Ruth Muller