Oxy, Not Bonded Directly To A Ring, In Same Side Chain As Carboxyl, Or Salt Thereof Patents (Class 562/470)
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Patent number: 6342525Abstract: Benzenoid HETE derivatives and methods of their use for treating dry eye are disclosed.Type: GrantFiled: October 23, 2000Date of Patent: January 29, 2002Assignee: Alcon Universal Ltd.Inventors: Peter G. Klimko, David R. Pierce
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Patent number: 6337306Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.Type: GrantFiled: November 5, 1999Date of Patent: January 8, 2002Assignee: Rhone-Poulenc AgroInventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
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Patent number: 6288120Abstract: Prostaglandin agonists of formula (I), in which, for example, A is a sulphonyl or acyl group, B is N or CH, M contains a ring and K and Q are linking groups, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: June 11, 1999Date of Patent: September 11, 2001Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6274385Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.Type: GrantFiled: August 9, 1999Date of Patent: August 14, 2001Assignee: Abbott LaboratoriesInventors: Jill Edie Hochlowski, Thomas J. Sowin, Daniel W. Norbeck, Anne-Laure Marie Grillot, Rolf E. Swenson
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Patent number: 6242635Abstract: A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.Type: GrantFiled: September 18, 1998Date of Patent: June 5, 2001Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
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Patent number: 6232344Abstract: 13-Oxa analogs of certain prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: May 21, 1999Date of Patent: May 15, 2001Assignee: Alcon Laboratories, Inc.Inventors: Zixia Feng, Mark R. Hellberg
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Patent number: 6180823Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.Type: GrantFiled: November 6, 1998Date of Patent: January 30, 2001Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Paul T. Grover
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Patent number: 6162947Abstract: A novel a process for the preparation of the chelating agent of formula (I) ##STR1## 4-carboxy-5,8,11-tris(carboxymethyl)-1-phenyl-2-oxa-5,8,11-triazatridecan- 13-oic acid, commonly named BOPTA.Type: GrantFiled: July 8, 1999Date of Patent: December 19, 2000Assignee: Dibra S.p.A.Inventors: Marina Ausonio, Carlo Distaso, Giuseppe Gerardo Elia, Alessandro Lesignoli, Rodolfo Piva, Carlo Secchi, Carlo Felice Viscardi
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Patent number: 6156891Abstract: Carboxylic acids of formula (1): ##STR1## wherein R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): ##STR2## The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): ##STR3## wherein R.sup.3 and Q are as defined above, with malonic acid derivatives of formula (6):R.sup.2 CH(COOH).sub.2wherein R.sup.2 is as defined above in the presence of a base.Type: GrantFiled: April 9, 1999Date of Patent: December 5, 2000Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6136852Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.Type: GrantFiled: March 8, 1999Date of Patent: October 24, 2000Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
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Patent number: 6107338Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Haiyan George Dai, Cynthia Jean Miley, Biswanath De
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Patent number: 6087526Abstract: Provided is an industrially useful process for producing an optically active 2-hydroxy-4-arylbutyric acid or its ester. An optically active acyloxysuccinic anhydride is reacted with an aromatic compound in the presence of a Lewis acid to produce an optically active 2-acyloxy-4-oxo-4-arylbutyric acid. The 2-acyloxy-4-oxo-4-arylbutyric acid is converted to an optically active 2-acyloxy-4-arylbutyric acid through catalytic reduction. The 2-acyloxy-4-arylbutyric acid is hydrolyzed in the presence of an acid or an alkali to produce an optically active 2-hydroxy-4-arylbutyric acid. The 2-hydroxy-4-arylbutyric acid is reacted with an alcohol in the presence of an acid to produce an optically active 2-hydroxy-4-arylbutyric acid ester.Type: GrantFiled: June 29, 1999Date of Patent: July 11, 2000Assignee: Ajinomoto Co., Inc.Inventors: Masahiko Kurauchi, Yoshimasa Hagiwara, Hiroyuki Matsueda, Takashi Nakano, Kunisuke Izawa
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Patent number: 6083982Abstract: Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.Type: GrantFiled: April 9, 1998Date of Patent: July 4, 2000Assignee: Loma Linda University MedicalInventors: William J. Wechter, David E. Murray, Darko Kantoci, Barry H. Levine, Elaine J. Benaksas
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Patent number: 6066763Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.Type: GrantFiled: August 25, 1998Date of Patent: May 23, 2000Assignee: Nippon Soda Co., Ltd.Inventor: Koichi Hayakawa
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Patent number: 6005125Abstract: A universal linker for solid-phase nucleic acid synthesis that is cleaved under conditions orthogonal to those used during the synthesis and deprotection of nucleic acids such as dsDNA or RNA fragments is disclosed. The invention includes compounds of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of OH, OR.sub.2 and an amino functionalized support and n is an integer ranging from about 1 to about 1000 or more preferably from about 1 to about 100 or greater and R.sub.2 is an alkyl (C.sub.1-20) or greater.Type: GrantFiled: May 6, 1997Date of Patent: December 21, 1999Assignee: Rutgers the State University of New JerseyInventors: Xiaohu Zhang, Roger A. Jones
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Patent number: 5998642Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.Type: GrantFiled: December 15, 1997Date of Patent: December 7, 1999Assignee: Washington UniversityInventors: Jeffrey I. Gordon, George W. Gokel, Paul T. Englund
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Patent number: 5990342Abstract: A surfactant, an emusifier for emulsion polymerization, a dispersant for suspension polymerization and a modifier for modification of resin properties are disclosed, each of these agents being comprised of a novel compound having a dibasic carboxyl group. The compound is represented by Formula (1)[X--O--(R.sup.1 O).sub.m --OC--R.sup.2 --COO].sub.y M (1)where M is a hydrogen atom, a metal atom or a quaternary nitrogen-containing group, y is equal to the valence of M, R.sup.1 is at least one hydrocarbon group, R.sup.2 is a moiety of a dibasic acid or a moiety of its anhydride, m is 0 or an integer of 1 to 1,000, and X is a hydrocarbon group having at least one polymerizable double bond of carbon--ncarbon which may contain an oxygen atom and a fluorine atom.Type: GrantFiled: July 16, 1996Date of Patent: November 23, 1999Assignee: Asahi Denka Kogyo K.K.Inventors: Masahide Tsuzuki, Kaoru Komiya
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Patent number: 5959139Abstract: Provided is an industrially useful process for producing an optically active 2-hydroxy-4-arylbutyric acid or its ester. An optically active acyloxysuccinic anhydride is reacted with an aromatic compound in the presence of a Lewis acid to produce an optically active 2-acyloxy-4-oxo-4-arylbutyric acid. The 2-acyloxy-4-oxo-4-arylbutyric acid is converted to an optically active 2-acyloxy-4-arylbutyric acid through catalytic reduction. The 2-acyloxy-4-arylbutyric acid is hydrolyzed in the presence of an acid or an alkali to produce an optically active 2-hydroxy-4-arylbutyric acid. The 2-hydroxy-4-arylbutyric acid is reacted with an alcohol in the presence of an acid to produce an optically active 2-hydroxy-4-arylbutyric acid ester.Type: GrantFiled: August 16, 1996Date of Patent: September 28, 1999Assignee: Ajinomoto Co., Inc.Inventors: Masahiko Kurauchi, Yoshimasa Hagiwara, Hiroyuki Matsueda, Takashi Nakano, Kunisuke Izawa
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Patent number: 5919970Abstract: Compounds of the formulaY.sub.3 (R.sub.4)--X--Y.sub.1 (R.sub.1 R.sub.2)--Z--Y.sub.2 (R.sub.2)--A--Bwhere the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.Type: GrantFiled: April 24, 1997Date of Patent: July 6, 1999Assignee: Allergan Sales, Inc.Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
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Patent number: 5919464Abstract: Biomodulators, which regulate cellular differentiation and proliferation, as well as methods of use thereof, e.g., for treating various conditions, e.g., cancer, senescence, immunological disorders and vascular disease; for stimulating normal tissue architecture after injury; for vaccination; for stimulating the production of biologically important molecules by cells or organs in culture; for maintaining organs or tissues outside of a body after removal from the body and prior to transplantation; and for producing of vascular grafts for transplantation; are provided.Type: GrantFiled: September 23, 1993Date of Patent: July 6, 1999Assignee: University of New MexicoInventors: Paul L. Mann, Eugene Mash
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Patent number: 5914429Abstract: In an industrial process for the manufacture of sodium orthohydroxymandelate by condensation of phenol in an inert atmosphere with glyoxylic acid in aqueous solution, in the presence of a tertiary amine and of catalytic quantities of a trivalent metal cation at a temperature below 100.degree. C., carried out continuously in at least two reactors (R1 . . .Type: GrantFiled: March 2, 1998Date of Patent: June 22, 1999Assignee: Clariant (France) S. A.Inventor: Christian Sidot
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Patent number: 5910606Abstract: .alpha., .beta.-Unsaturated acids of the formula ##STR1## wherein R.sup.1 signifies C.sub.1 -C.sub.5 -alkyl and Ar signifies an aryl group which is optionally substituted by one or more substituents selected from the group consisting of halogen, phenyl, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, perfluorinated C.sub.1 -C.sub.5 -alkyl or perfluorinated C.sub.1 -C.sub.5 -alkoxy can be obtained from new or known compounds of the formula ##STR2## Compounds I can be converted by asymmetric hydrogenation into corresponding optically active saturated acids.Type: GrantFiled: January 10, 1997Date of Patent: June 8, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Foricher, Rudolf Schmid
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Patent number: 5877214Abstract: The present invention is directed to the certain polyaryl-poly(ethylene glycol) compounds ("polyaryl-PEG" compounds) which are useful as soluble polyvalent supports in the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.Type: GrantFiled: September 4, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventor: Ronald M. Kim
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Patent number: 5859295Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.Type: GrantFiled: June 18, 1996Date of Patent: January 12, 1999Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Gerald A. Rosenthal
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Patent number: 5856560Abstract: A process and intermediates for preparing .alpha.Type: GrantFiled: December 10, 1996Date of Patent: January 5, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Heinz Isak, Horst Wingert, Hubert Sauter, Michael Keil, Markus Nett, Remy Benoit, Ruth Muller
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Patent number: 5783602Abstract: The invention relates to leukotriene-B.sub.4 derivatives of general formula I, ##STR1## in which R.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3 COOR.sub.4 CONR.sub.5 R.sub.6, andR.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,X and Y mean a direct bond, whereby the resulting olefin can be E- or Z-configured or X represents a fluorine atom in .alpha.- or .beta.-position, and Y means a hydrogen atom in .beta.-position.Type: GrantFiled: December 4, 1996Date of Patent: July 21, 1998Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
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Patent number: 5780624Abstract: A process for preparing oxime ethers of the general formula I ##STR1## where R.sup.1 is a C-organic radical,R.sup.2 is hydrogen, alkoxy, cyano, nitro, SOR.sup.4, SO.sub.2 R.sup.4, CO.sub.2 -alkyl, P(O)(OR.sup.4).sub.2 or a C-organic radical, andR.sup.3 and R.sup.4 are unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, entails converting an oxime of the general formula II ##STR2## where the substituents R.sup.1 and R.sup.2 have the abovementioned meanings, in the presence or absence of an organic diluent, with a base into the corresponding salt, and reacting the latter with a dialkyl carbonate of the general formula III ##STR3## where R.sup.3 has the abovementioned meanings.Type: GrantFiled: May 20, 1997Date of Patent: July 14, 1998Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Michael Keil
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Patent number: 5750775Abstract: A crystallized sodium orthohydroxymandelate-phenol-water complex, its preparation process in which phenol (P.sub.2) is introduced into an aqueous solution S at a pH comprised between 7 and 9.5 in order to obtain the expected product which is crystallized, the aqueous solution S being such as that resulting from the reaction of phenol (P.sub.1) with glyoxylic acid in the presence of a tertiary amine and of a trivalent cation, then treatment using a solution of an alkaline hydroxide, use of this complex for the preparation of sodium orthohydroxymandelate (NaOHM), preparation process for the latter from the starting complex.Type: GrantFiled: September 18, 1996Date of Patent: May 12, 1998Assignee: Societe Francaise HoechstInventors: Christian Sidot, Michel Tarlier
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Patent number: 5712266Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.Type: GrantFiled: May 30, 1995Date of Patent: January 27, 1998Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
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Patent number: 5703017Abstract: 3-(Het)arylcarboxylic acid derivatives of the formula I ##STR1## where R is formyl, CO.sub.2 H or a radical hydrolyzable to COOH and the other substituents have the following meanings:R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms an alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen;R.sup.4 is phenyl or naphthyl, each of which is unsubstituted or substituted or an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl or phenyl;R.sup.6 is C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.Type: GrantFiled: October 19, 1995Date of Patent: December 30, 1997Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Bratz, Hans Theobald, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Wilhelm Rademacher
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Patent number: 5698711Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: Rhone-Poulenc Rorer LimitedInventor: Malcolm Norman Palfreyman
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Patent number: 5684168Abstract: .beta.-phenylisiserine-(2R,3S), salts and preparation thereof through the action of ammonia on .beta.-phenylglycidic-(2R,3R) acid and its use in the preparation of taxane derivatives of general formula: ##STR1## wherein R is hydrogen or --COCH.sub.3 ;and R.sub.1 is phenyl or --O--C(CH.sub.3).sub.3.Type: GrantFiled: April 10, 1995Date of Patent: November 4, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Pierre Duchesne, Max Ferraro
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Patent number: 5684186Abstract: A process for producing a phenyllactic acid derivative comprises hydrogenating a phenylpyruvic acid derivative in the presence of a catalyst containing at least one element selected from the Group VIII elements of the periodic table. The process provides a phenyllactic acid derivative useful as an intermediate in the production of pharmaceuticals and agricultural chemicals. The process uses as a starting material a phenylpyruvic acid derivative which is easily synthesized. The process is simpler in operation and provides a higher yield than conventional processes.Type: GrantFiled: August 4, 1995Date of Patent: November 4, 1997Assignee: Nitto Chemical Industry Co., Ltd.Inventors: Hikari Morita, Hiroyuki Mori
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Patent number: 5679740Abstract: Mechanically stable, self-inverting water-in-oil polymer emulsions for use in industrial water treatment, waste water treatment, sludge conditioning, ore dressing, papermaking, secondary and tertiary oil recovery containing carboxylated ethoxylated phenols and alcohols are provided.Type: GrantFiled: June 13, 1996Date of Patent: October 21, 1997Assignee: Cytec Technology Corp.Inventor: Howard Ivan Heitner
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Patent number: 5650533Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.Type: GrantFiled: June 2, 1995Date of Patent: July 22, 1997Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
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Patent number: 5648387Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.Type: GrantFiled: March 24, 1995Date of Patent: July 15, 1997Assignee: Warner-Lambert CompanyInventors: Charles Larry Bisgaier, Paul Leroy Creger, Alan Robert Saltiel, Sherrie Rae Tafuri
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Patent number: 5635608Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.Type: GrantFiled: November 8, 1994Date of Patent: June 3, 1997Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Kyle R. Gee
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Patent number: 5614634Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
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Patent number: 5602273Abstract: A release tag reagent suitable for use in the chemical analysis of a substance to be detected comprises signal, release, and reactivity groups. A class of release tag compounds that are cleaved to release as signal groups very stable electrophoric ketones which are sufficiently volatile for determination in the gas phase of an analytical reaction mixture is disclosed.Type: GrantFiled: February 8, 1996Date of Patent: February 11, 1997Assignee: Northeastern UniversityInventors: Roger W. Giese, Samy Abdel-Baky, Linxiao Xu
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5583132Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: February 2, 1995Date of Patent: December 10, 1996Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5563161Abstract: Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; R.sup.1 is H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; COR.sup.a ; COOR.sup.a ; COHet; COC.sub.1-6 alkylhalo; COC.sub.1-6 alkylNR.sup.a R.sup.b ; CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b ; CONR.sup.a R.sup.b ; or SO.sub.2 R.sup.a ; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-3 alkyl substituted by optionally substituted phenyl; R.sup.4 and R.sup.5 are each H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.Type: GrantFiled: March 10, 1995Date of Patent: October 8, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian T. Huscroft, Graeme I. Stevenson, Brain J. Williams
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Patent number: 5530145Abstract: Novel anticholesteremic compounds capable of reducing blood cholesterol levels. Also included in this invention are (i) intermediates from which the abovementioned anticholesteremic compounds can be prepared, and (ii) methods for preparing both the intermediates and the anticholesteremic compounds.Type: GrantFiled: December 6, 1994Date of Patent: June 25, 1996Assignee: Syn-Tech Chem & Pharm Co., Ltd.Inventors: Hui-Po Wang, On Lee, Chin-Tsai Fan
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Patent number: 5523460Abstract: A 4-fluorobiphenyl derivative of formula (I), which is useful as a cholesterol lowering agent or a lipid lowering agent because of its strong inhibitory effect on HMG-CoA reductase), and which is also useful as an intermediate for producing the above-mentioned cholesterol lowering agent or lipid lowering agent: ##STR1## wherein A is a .omega.-oxycarbonyldihydroxybutyl group, a tetrahydropyranyl group, a .omega.-oxycarbonyl-3-oxobutyl group, a formyl group, or a cyano group; R.sup.1 is a halogen atom, an alkyl group, or a group represented by R.sup.5 O--, wherein R.sup.5 is a hydrogen atom, or an alkyl group; R.sup.2 is a hydrogen atom, an alkyl group; R.sup.3 is a hydrogen atom, or an alkyl group; R.sup.5 and R.sup.2 may form a five-membered ring or a six-membered ring in combination with the oxygen atoms to which R.sup.5 and R.sup.2 are respectively bonded, and R.sup.5 and R.sup.3 may form a five-membered ring or a six-membered ring in combination with the oxygen atom to which R.sup.5 is bonded.Type: GrantFiled: March 28, 1994Date of Patent: June 4, 1996Assignee: Fujirebio Inc.Inventors: Masakatsu Matsumoto, Nobuko Watanabe, Eiko Mori, Miwa Ishihara, Tetsuaki Yamaura, Misao Aoyama, Hiroshi Ikawa, Hisako Kobayashi
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Patent number: 5516932Abstract: The present invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen or an alkyl radical having 1 to 18 carbon atoms and optionally containing oxygen, nitrogen or halogen, the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or if two of the radicals X, Y or Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom. The invention further relates to a process for the preparation of the compounds, by reacting an aryldiazonium salt of the formula ##STR2## in which the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or, if two of the radicals X, Y and Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom and A.sup.(-) is an anion of an acid having a pK.sub.a <7, with a compound of the formula ##STR3## in which R.sup.Type: GrantFiled: January 6, 1994Date of Patent: May 14, 1996Assignee: Hoechst AktiengesellschaftInventors: Matthias Beller, Hartmut Fischer, Laurent Weisse, Klaus Forstinger, Ralf Pfirmann, Heinz Strutz
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Patent number: 5502152Abstract: Disclosed is a polyoxyalkylene derivative which is useful for a carboxyl group-containing polyurethane resin, can easily introduce a carboxyl group into a polyurethane resin skeleton, and has a low melting point or is in a liquid state at normal temperature. The polyoxyalkylene derivative is represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms; R.sub.2 represents an alkylene group having from 1 to 6 carbon atoms or an arylene group having from 6 to 8 carbon atoms; A represents an alkylene group having from 4 to 7 carbon atoms; B represents an alkylene group having from 2 to 6 carbon atoms; l represents from 0 to 2; m represents from 0.1 to 35; n represents from 0.1 to 50; and 0.5<(m+n)<50.Type: GrantFiled: January 13, 1995Date of Patent: March 26, 1996Assignee: Hodogaya Chemical Co., Ltd.Inventors: Shigeru Shimada, Susumu Jinbo, Hideyuki Isii
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Patent number: 5466833Abstract: The invention relates to a novel process for the preparation of 13,14-dihydro-15 (R)-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. isopropyl ester of the formula (I)--wherein R stands for saturated or unsaturated straight, branched or cyclic C.sub.Type: GrantFiled: October 6, 1994Date of Patent: November 14, 1995Assignees: Kabi Pharmacia AB, Chinoin Ltd.Inventors: Jozsef Ivanics, Tibor Szabo, Istvan Hermecz, Gyula Dalmadi, Jozsefne Ivanics, Gaborne Kovacs, Resul Bahram
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Patent number: 5466435Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.Type: GrantFiled: April 4, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: Edward J. Baker, Edward R Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef, John L. Toner, Robert W. Lee
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Patent number: 5453443Abstract: Compounds having the formula I: ##STR1## are inhibitors of the PLA.sub.2 s enzymes. These compounds are useful as anti-allergic, anti-asthmatic, they are also useful in treating various inflammatory diseases such as rheumatoid arthritis, osteoarthritis, bursitis, psoriasis; immunoinflammatory disorders such as contact dermatitis, irritable bowel disease and the like.Type: GrantFiled: July 20, 1994Date of Patent: September 26, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Helene Perrier, Petpiboon Prasit, Ian Street, Zhaoyin Wang
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Patent number: 5447954Abstract: Compounds of the formula ##STR1## where the substituents are defined in the specification useful in the treatment of hyperlipidemia.Type: GrantFiled: November 4, 1994Date of Patent: September 5, 1995Assignee: SmithKline Beecham p.l.c.Inventors: Andrew D. Gribble, Pieter H. E. Groot, Antony N. Shaw, Roland E. Dolle