Oxy, Aldehyde Or Ketone Group In Acid Moiety Patents (Class 560/170)
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Patent number: 6388041Abstract: Disclosed are polyoxyethylene derivatives having different functional groups at both ends of the molecule represented by the following formula (I) and a process for producing the derivatives by anionic living polymerization. The present invention provides polymers which are especially suitable for use as medical materials. wherein A′ and B′ are organosilyl type amino-protecting groups, R is a hydrogen atom or a C1-6 alkyl group, and Y is a hydrogen atom, an alkali metal or a certain functional group.Type: GrantFiled: November 7, 2000Date of Patent: May 14, 2002Assignee: Nano Carrier Co LtdInventors: Kazunori Kataoka, Masao Kato, Yukio Nagasaki, Takahisa Hayashida, Michihiro Iijima, Teruo Okano
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Publication number: 20020035283Abstract: A novel process in which an optically active alcohol compound having a desired absolute configuration and a high optical purity can be obtained by asymmetrically hydrogenating a &bgr;-keto acid compound through a simple operation. An optically active alcohol represented by general formula (III) as defined is obtained by asymmetrically hydrogenating a &bgr;-keto ester compound represented by general formula (I) as defined in the presence of at least one ruthenium complex having as a ligand an optically active tertiary diphosphine compound represented by general formula (II) as defined.Type: ApplicationFiled: July 23, 2001Publication date: March 21, 2002Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Takao Saito, Tohru Yokozawa, Kazuhiko Matsumura, Noboru Sayo
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Patent number: 6355618Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: April 7, 2000Date of Patent: March 12, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
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Patent number: 6346547Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent sType: GrantFiled: February 8, 2000Date of Patent: February 12, 2002Assignee: Checkpoint, Genetics, Inc.Inventor: Nathan Tzodikov
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Patent number: 6303569Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: August 21, 1998Date of Patent: October 16, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri
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Patent number: 6281379Abstract: This invention to provide a process for producing an optically active threo-phenylnorstatin derivative which does not require a toxic cyanating agent or a costly reagent, or a complicated procedure, and can be practiced on a commercial scale. This invention is directed to a process for producing a &bgr;-amino-&agr;-hydroxy acid derivative which comprises treating either a &ggr;-amino-&bgr;-keto sulfoxide derivative with a halogenating agent to produce a &ggr;-amino-&agr;-halo-&bgr;-keto sulfoxide derivative, treating the same with an acid and an alcohol to produce a &bgr;-amino-&agr;-keto ester derivative or &bgr;-amino-&agr;-keto acid derivative, and followed by reducing.Type: GrantFiled: May 26, 2000Date of Patent: August 28, 2001Assignee: Kaneka CorporationInventors: Akio Fujii, Masanobu Sugawara, Kenji Inoue
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Patent number: 6245810Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. wherein y is 0 or 1; R1 represents an unsubstituted C1-C8 alkyl group or others; R2 represents a hydrogen atom, a C1-C5 alkyl group or others; R3 represents a hydrogen atom, a C1-C8 alkyl group or others; R4 represents a hydrogen atom, a C1-C3 alkyl group or others; R5 represents a group —OR42, a group or others.Type: GrantFiled: June 30, 1998Date of Patent: June 12, 2001Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Ishizuka, Masaji Kawazu, Toshiaki Katsumi, Yoshihide Fuse, Kenji Maeda, Tomio Takeuchi
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Patent number: 6245922Abstract: A photoactive compound that is the reaction product of an alkenyl azlactone compound and a nucleophilic aromatic ketone is described. Mer units derived from this compound can be used, for example, to crosslink via a hydrogen abstracting mechanism acrylic polymers in which they are incorporated.Type: GrantFiled: November 19, 1996Date of Patent: June 12, 2001Assignee: 3M Innovative Properties CompanyInventors: Steven M. Heilmann, Gaddam N. Babu, Larry R. Krepski, Howell K. Smith, II, Daniel E. Mickus
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Patent number: 6207828Abstract: This invention provides a convenient, new, one step process for the preparation of 2-(trihaloacetyl)-3-(substituted amino)-2-propenoates and related derivatives thereof by reaction of carbonyl compounds substituted with a trihaloacetyl group with an acetal in the presence of an organic acid. The resulting propenoates are useful as intermediates for the construction of trihalomethyl substituted heterocyclic compounds for use in pharmaceutical and agricultural applications.Type: GrantFiled: November 4, 1999Date of Patent: March 27, 2001Assignee: Rolm and Haas CompanyInventor: Peter Osei-Gyimah
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Patent number: 6203808Abstract: The present application relates to novel ceramide compounds to their process of preparation and to their use in cosmetics or in pharmaceuticals, in particular for treating and caring for the skin, hair, nails and eyelashes.Type: GrantFiled: December 21, 1999Date of Patent: March 20, 2001Assignee: L'OrealInventors: Rémy Tuloup, Michel Philippe
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Patent number: 6197996Abstract: A process for preparing an optically active carnitine ester represented by formula (I): wherein R represents a lower alkyl group; and X represents a halogen atom, is disclosed, comprises asymmetrically hydrogenating a &ggr;-trimethylammonium-3-oxobutanoic ester halide represented by formula (II): wherein R and X are as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst. An optically active carnitine ester of any desired isomerism can be obtained through simple operation in high yield at high optical purity. The substrate used is easily available.Type: GrantFiled: October 22, 1993Date of Patent: March 6, 2001Assignee: Takasago International CorporationInventors: Takanao Taketomi, Toshiaki Sakaguchi, Hidenori Kumobayashi
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Patent number: 6180667Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: March 28, 1997Date of Patent: January 30, 2001Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria Ornella Tinti, Nazareno Scafetta
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Patent number: 6180818Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).Type: GrantFiled: November 3, 1999Date of Patent: January 30, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
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Patent number: 6150537Abstract: The invention relates to a method for preparing an ester, by admixing a compound having the structure I or IV: ##STR1## with a base and an alcohol to produce an ester, wherein the alcohol is a precursor to Taxol and its analogs. The present invention also relates to compounds having the structure I and IV and methods of making them therefor. The invention also relates to the esterification of an alcohol by adding an alkoxide to a compound having the structure VII: ##STR2## The invention further relates to compounds having the structure I, IV, and VII and methods of making them therefor. The invention further relates to alcohols, and in particular, alcohols that are synthetic precursors to Taxol and analogs thereof.Type: GrantFiled: December 12, 1997Date of Patent: November 21, 2000Assignee: Emory UniversityInventors: Dennis C. Liotta, Hariharan Venkatesan, Laura Captain, Michael V. Voronkov, James P. Snyder, Marcus A. Schestopol
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Patent number: 6121487Abstract: The present invention is relative to a chemical method of producing compounds of the general formula (I) ##STR1## starting from compounds of the general formula (II) and (III) ##STR2## under radical conditions. Products I are used as intermediates in the synthesis of bioactive substances.Type: GrantFiled: July 28, 1999Date of Patent: September 19, 2000Assignee: Degussa-Huls AktiengesellschaftInventors: Annegret Vogt, Hans-Josef Altenbach, Michael Kirschbaum, Michael-Gottfried Hahn, Mike Siegfried Paul Matthaus, Andreas Rainer Hermann
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Patent number: 6110970Abstract: This invention relates to nitrogen-containing oxyalkylene diester compositions for treating disease conditions including cancer and other proliferative diseases. The nitrogen-containing oxyalkylene diesters are represented by the formula ##STR1## where the nitrogen-containing group is R.sub.3 and includes particular alkyl, alkenyl, cycloalkyl, aryl, aralkyl, heterocycloalkyl or heteroaryl groups, which have nitrogen-containing substituents, such as amines, amides, or nitrogen heteroatoms.Type: GrantFiled: March 11, 1997Date of Patent: August 29, 2000Assignees: Beacon Laboratories, Inc., Mor Research Applications, Ltd., Bar-Ilan UniversityInventors: Abraham Nudelman, Ada Rephaeli
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Patent number: 6107286Abstract: Cationic lipids of general formula (I), wherein m is an integer from 2 to 6 inclusive; n is an integer from 1 to 9 inclusive, preferably 1-5, where, when n is 2-9, a single R grouping other than hydrogen is present in the general formula, and m has variable or identical values within the groupings (a) or --(CH.sub.2).sub.m ; R is a hydrogen atom or a radical of general formula (II), wherein X or X.sup.1, which are the same or different, are an oxygen atom, a methylene grouping --(CH.sub.2).sub.q -- where q is 0, 1, 2 or 3, or an amino grouping --NH-- or NR.sup.1 --, where R is a C.sub.1-4 alkyl grouping; Y and Y.sup.1, which are the same or different, are a hydrogen atom or an optionally substituted C.sub.1-4 alkyl radical, and p is 0-5; and R.sub.6 is a cholesterol derivative or an alkylamino grouping --NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are, independently of each other, a straight or branched, saturated or unsaturated C.sub.12-22 aliphatic radical.Type: GrantFiled: June 4, 1997Date of Patent: August 22, 2000Assignee: Rhone-Poulenc Rorer S.A.Inventors: Gerardo Byk, Daniel Scherman, Catherine Dubertret
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Patent number: 6077972Abstract: The present application relates to novel ceramide compounds to their process of preparation and to their use in cosmetics or in pharmaceuticals, in particular for treating and caring for the skin, hair, nails and eyelashes.Type: GrantFiled: November 4, 1998Date of Patent: June 20, 2000Assignee: L'OrealInventors: Remy Tuloup, Michel Philippe
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Patent number: 6063955Abstract: A method for producing an optically active erythro-3-amino-2-hydroxybutyric ester as an important intermediate of pharmaceutical agents, specifically HIV protease inhibitor, in high purity and in high yield. The method includes producing an optically active erythro-3-amino-2-hydroxybutyric ester by oxidizing the hydroxyl group at the 2-position of an optically active 3-amino-2-hydroxybutyric ester, optically active at the 3-position, as represented by formula (I): ##STR1## (wherein R.sup.1 represents a phenyl group or a cyclohexyl group; R.sup.2 represents a protective group and R.sup.3 represents an unsubstituted or substituted alkyl residue; the steric configuration of *1 represents S configuration or R configuration), and then reducing erythro-selectively the resulting product by using aluminum alkoxide.Type: GrantFiled: February 3, 1999Date of Patent: May 16, 2000Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hisao Satoh, Kenichi Yamamoto
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Patent number: 6008403Abstract: A method for producing an optically active amino acid or derivative thereof having a high optical purity from an optically active amino acid comprising optical isomers or derivative thereof, which comprises any one of processes (A), (B), and (C), wherein the process (A) comprises the steps: (1) previously preparing an optically active amino acid or derivative thereof having an optical purity higher than a convergent value of a mutual solubility of the optical isomers and (2) crystallizing the optically active amino acid or the derivative thereof that exists in excess, said convergent value being a ratio of the desired optical isomer in the optical isomers dissolved in a mother liquor in which crystals of a racemate and an optically active compound coexist at equilibrium (the optical purity in a mother liquor). The processes (B) and (C) are described in the specification.Type: GrantFiled: September 26, 1997Date of Patent: December 28, 1999Assignee: Tosoh CorporationInventors: Kimio Katsuura, Shigeaki Irino, Akira Tokuda
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Patent number: 5990341Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.Type: GrantFiled: December 24, 1996Date of Patent: November 23, 1999Assignee: Emory UniversityInventors: Dennis C. Liotta, Bharat Ramkrishna Lagu
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Patent number: 5977401Abstract: The present invention relates to a novel intermediate compound for preparing optionally substituted 1,2,4-triazolinones and a process for preparing that intermediate compound.Type: GrantFiled: April 14, 1999Date of Patent: November 2, 1999Assignee: BayeraktiengesellschaftInventor: Heinz-Jurgen Wroblowsky
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Patent number: 5965119Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: B is a leaving group or a residue of an amine-containing target moiety;G is ##STR2## or CH.sub.2 ; Y.sub.1-2 are independently O or S;M is X or Q; where X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2);R.sub.1, R.sub.4, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.13 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls, substituted C.sub.1-6 heteroalkyls;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.Type: GrantFiled: December 30, 1997Date of Patent: October 12, 1999Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 5935988Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.Type: GrantFiled: July 12, 1996Date of Patent: August 10, 1999Assignee: Bayer AktiengesellschaftInventors: Michael Matzke, Hans-Christian Militzer, Joachim Mittendorf, Franz Kunisch, Axel Schmidt, Wolfgang Schonfeld, Karl Ziegelbauer
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Patent number: 5902887Abstract: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.Type: GrantFiled: April 14, 1998Date of Patent: May 11, 1999Assignee: Ajinomoto Co., Inc.Inventors: Yutaka Honda, Satoshi Katayama, Kunisuke Izawa, Masakazu Nakazawa, Takayuki Suzuki, Naoko Kanno
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Patent number: 5886213Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.Type: GrantFiled: August 22, 1997Date of Patent: March 23, 1999Assignee: Gilead Sciences, Inc.Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. Kelly, Matthew A. Williams, Lijun Zhang
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Patent number: 5866712Abstract: A novel peroxide composition of Structure A, ##STR1## and use of the novel oxalic acid peroxide composition of Structure A as an initiator; a) for curing of unsaturated polyester resins, b) for polymerizing ethylenically unsaturated monomers, c) for crosslinking of polyolefins, d) for curing of elastomers, e) for modifying polyolefins, f) for grafting of vinyl monomers onto polymer backbones and g) for compatibilizing blends of two or more incompatible polymers are disclosed.Type: GrantFiled: October 10, 1997Date of Patent: February 2, 1999Assignee: ELF Atochem North America, Inc.Inventors: Jose Sanchez, Daryl L. Stein
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Patent number: 5831091Abstract: An N-?2-(1-hydroxyethyl)-3-oxopropyl!amine compound of the formula ?III!: ##STR1## wherein Ring B represents a benzene ring which may be substituted; W represents oxygen atom or sulfur atom; Y represents oxygen atom, sulfur atom or N R.sup.0, R.sup.0 represents hydrogen atom or a substituent; Z represents a substituted methylene group which contains at least one chiral center; R.sup.5 represents an aralkyloxycarbonyl group or an alkoxycarbonyl group; R.sup.6 represents hydrogen atom, an aralkyl group, an acyloxy group, a tri-substituted silyloxy group or an alkoxy group; or both of R.sup.5 and R.sup.6 bond at their termini and combine with the adjacent nitrogen atom to form phthalimido group, and a process thereof are disclosed. Said compound ?III! is useful as a starting compound of .beta.-lactam antibacterial agents.Type: GrantFiled: November 5, 1996Date of Patent: November 3, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hiroshi Ohmizu, Masahiko Seki
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Patent number: 5801270Abstract: The present invention relates to an amine derivative represented by the following general formula (1): ##STR1## wherein R.sup.2 and R.sup.3 mean individually an alkyl or alkenyl group which may have --OH and has 1-24 carbon atoms, A denotes an alkylene or alkenylene group which may have at least one --OH, --COOH or --SO.sub.3 H and has 1-6 carbon atoms, Y.sup.1 is --COOH, --SO.sub.3 H or --OSO.sub.3 H, Y.sup.2 means --OH, --OSO.sub.3 H or --OCO--A--COOH, n stands for a number of 0 or 1, and p is an integer of 1-8, or a salt or quaternized product thereof, and a detergent composition containing such a compound. This compound is low in irritativeness to the skin and hair and excellent in foamability, and can give a pleasant feeling to the user's skin and the like.Type: GrantFiled: June 13, 1996Date of Patent: September 1, 1998Assignee: Kao CorporationInventors: Mitsuru Uno, Tomohito Kitsuki, Katsumi Kita, Yoshiaki Fujikura, Akiko Okutsu
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Patent number: 5801197Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.Type: GrantFiled: May 13, 1996Date of Patent: September 1, 1998Assignee: GPI Nil Holdings, Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 5798387Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. ##STR1## wherein y is 0 or 1; R.sup.1 represents an unsubstituted C.sub.1 -C.sub.8 alkyl group or others;R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or others;R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or others;R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group or others;R.sup.5 represents a group --OR.sup.42, a group ##STR2## or others.Type: GrantFiled: November 25, 1996Date of Patent: August 25, 1998Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Ishizuka, Masaji Kawazu, Toshiaki Katsumi, Yoshihide Fuse, Kenji Maeda, Tomio Takeuchi
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Patent number: 5773543Abstract: A process for the free radical initiated polymerization of unsaturated species characterized by the use of compound of Formula (I) as chain transfer agents: ##STR1## wherein: X is selected from hydrogen; CN; optionally substituted aryl; COOH; COOR; C(O)NHR.sup.6 ; C(O)NR.sup.7 R.sup.8 ; and halogen;Q is selected from COOR.sup.1 ; CN; and C(O)NR.sup.7 R.sup.8 ;Y is selected from hydrogen; C.sub.1 to C.sub.6 alkyl; C.sub.1 to C.sub.6 alkyl substituted with one or more substituents selected from hydroxy, amino, C.sub.1 to C.sub.6 alkoxy, C.sub.1 to C.sub.6 alkoxycarbonyl, halogen, CN and optionally substituted aryl; C.sub.1 to C.sub.6 alkenyl; and C.sub.1 to C.sub.6 alkynyl;Z is selected from COOR.sup.2 ; CN; and optionally substituted aryl;R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen C.sub.1 to C.sub.4 alkyl and halogen; or R.sup.3 and R.sup.Type: GrantFiled: August 1, 1996Date of Patent: June 30, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Ezio Rizzardo, San Hoa Thang, Graeme Moad, Charles Thomas Berge
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Patent number: 5767277Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.Type: GrantFiled: January 7, 1997Date of Patent: June 16, 1998Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5756784Abstract: An amide represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are C1-C24 alkyl, etc.; B is C2-C10 alkylene, etc.; A.sup.1 and A.sup.2 are C1-C6 alkylene, etc.; Y.sup.1 and Y.sup.2 are ##STR2## wherein R.sup.3, R.sup.4, and R.sup.5 are C1-C4 alkyl, etc., and X.sup.1 is halogen; or a salt of the amide and detergent compositions containing the amide or salt are mild to the skin or hair, provide a pleasant sensation to the skin or hair, and have excellent latherability and emulsion stability. These compounds are useful as components of various detergents and cosmetic compositions, emulsifiers, and conditioners.Type: GrantFiled: May 8, 1996Date of Patent: May 26, 1998Assignee: Kao CorporationInventors: Mitsuru Uno, Tetsuya Miyajima, Tomohito Kitsuki, Katsumi Kita
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Patent number: 5756822Abstract: An acetamide derivative having the general formula (I): ##STR1## or a pharmacologically acceptable salt thereof; a synthetic intermediate of the above-mentioned acetamide derivative; a treating agent for peptic ulcer and for gastritis which comprises the above-mentioned compound having the general formula (I) as an effective ingredient, and a process for treating peptic ulcer and gastritis using the above-mentioned compound having the general formula (I), are disclosed.Type: GrantFiled: April 4, 1997Date of Patent: May 26, 1998Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Nobuo Ishiyama, Toshihiro Koyama, Mitsuo Hayashida, Katsuyuki Otsuka, Masahiro Fujii, Kunio Kimura, Yoshiyuki Hata, Nobuko Miyao
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Patent number: 5756832Abstract: Amino acid esters of the formula ##STR1## wherein m is zero or one and R.sub.3 is an acid protecting group are prepared. These amino acid esters are useful as intermediates in the preparation of fused bicyclic ring compounds.Type: GrantFiled: May 9, 1997Date of Patent: May 26, 1998Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5714517Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: August 22, 1996Date of Patent: February 3, 1998Assignee: Monsanto CompanyInventor: Peter Gerrard Ruminski
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Patent number: 5663435Abstract: Reaction products of amino-alkylenecarboxylic acids with polyoxyalkylene compounds are used as paraffin dispersants for mineral oil middle distillates.Type: GrantFiled: November 29, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Gabriele Dralle-Voss, Knut Oppenlander, Klaus Barthold, Bernd Wenderoth, Wolfgang Kasel
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Patent number: 5663348Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.Type: GrantFiled: July 19, 1995Date of Patent: September 2, 1997Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5646098Abstract: The invention relates to novel compositions comprising ene and free radical adducts of unsaturated and saturated hydrocarbons, and acyclic and cyclic vicinal polycarbonyl compounds such as diethyl ketomalonate and indantrione. The adducts are reacted with nucleophiles such as amines, electrophiles such as anhydrides and esters, and metal ions. Post-products are obtained via reaction of said products with capping reagents such as boric acid. Compositions containing said adducts, products and post-products include oleaginous substances such as fuels and lube oils.Type: GrantFiled: May 13, 1994Date of Patent: July 8, 1997Assignee: Exxon Chemical Patents IncInventor: Stanley J. Brois
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Patent number: 5646327Abstract: Substituted hydroxylamines useful in photographic processing solution can be prepared by reacting a hydroxylamine with a vinylic compound having an electron withdrawing substituent in a suitable solvent, in the absence of a neutralizing base. The resulting products can be used without isolation from the reaction solution.Type: GrantFiled: December 8, 1995Date of Patent: July 8, 1997Assignee: Eastman Kodak CompanyInventors: Elizabeth Gertrude Burns, Lynda Woedy McGarry, Gary Stephen Proehl, Lee Hamilton Latimer
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Patent number: 5631389Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.Type: GrantFiled: April 30, 1996Date of Patent: May 20, 1997Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Robert Vermeer, Van Au, Bijan Harichian
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Patent number: 5628804Abstract: A polyether esteramide reaction product effective as a fuel additive for reducing intake valve deposits and octane requirement increase, as well as controlling combustion chamber deposits, in gasoline engines is disclosed together with fuel compositions and methods of making and using the same. The polyether esteramide reaction product contains two carbonyl groups. Preferably, the polyether esteramide contains an oxalyl group. Also disclosed are compositions and methods for dispersing deposits in lubricating oil products.Type: GrantFiled: December 21, 1995Date of Patent: May 13, 1997Assignee: Ethyl CorporationInventor: John T. Loper
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Patent number: 5625085Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: July 14, 1994Date of Patent: April 29, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria O. Tinti, Nazareno Scafetta
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Patent number: 5610188Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.Type: GrantFiled: December 30, 1994Date of Patent: March 11, 1997Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
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Patent number: 5599954Abstract: Compounds represented by the following general structural formula (1) and methods for producing the compounds: ##STR1## R.sup.1 represents a group such as benzyloxycarbonyl, R.sup.2 represents a lower alkyl group, R.sup.3 represents a hydrogen atom or a protecting group, each of M.sup.1 and M.sup.2 represents a metal atom, and n represents the atomic valence of M.sup.1. Intermediates for HMG-CoA reductase inhibitors can be prepared safely and easily from these compounds.Type: GrantFiled: January 26, 1996Date of Patent: February 4, 1997Assignee: Takasago International CorporationInventors: Sigeru Mitsuhashi, Tsukasa Sotoguchi, Yoshifumi Yuasa, Hidenori Kumobayashi
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Patent number: 5599947Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.Type: GrantFiled: March 24, 1995Date of Patent: February 4, 1997Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Patent number: 5587514Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.Type: GrantFiled: November 8, 1993Date of Patent: December 24, 1996Assignee: Emory UniversityInventors: Dennis C. Liotta, Bharat R. Lagu
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Patent number: 5580481Abstract: To provide an aqueous fabric softener composition, which is excellent in softening performance, elasticity and storage stability, and a quaternary ammonium salt which is useful as a softening base of this composition and nondetrimental to the natural environment because of its excellent biodegradability, and a process for the preparation of this salt.The aqueous fabric softener composition of the present invention comprises from 8 to 40% by weight of a quaternary ammonium salt represented by the following formula (I), a quaternary ammonium salt represented by the following formula (II) or a mixture thereof, and water: ##STR1## wherein R.sup.1 and R.sup.2 represent each a C.sub.1-4 alkyl group, etc.; R.sup.3 and R.sup.4 represent each a C.sub.7-35 alkyl group, etc.; and X.sup.- represents an anion group; and ##STR2## wherein R.sup.5 and R.sup.6 represent each a C.sub.1-4 group, etc.; R.sup.7 and R.sup.8 represent each a C.sub.1-5 alkylene group, etc.; R.sup.9 and R.sup.10 represent each a C.sub.Type: GrantFiled: March 24, 1995Date of Patent: December 3, 1996Assignee: Kao CorporationInventors: Yushi Sakata, Junichi Inokoshi, Tohru Katoh, Osamu Tachizawa, Uichiro Nishimoto, Yasuki Ohtawa, Masaaki Yamamura