Patents Examined by Margaret M. Mach
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Patent number: 5847146Abstract: N-Heteroaryl-N'-(pyrid-2-yl-sulfonyl)ureas, processes for their preparation, and their use as herbicides and plant growth regulatorsCompounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, A, n, m and w are as defined in claim 1, are suitable as herbicides for controlling harmful plants and can be prepared, inter alia, from the sulfonamides of the formula (II) ##STR2## by reacting them with carbamates R*O--CO--NR.sup.4 --A.Type: GrantFiled: March 16, 1998Date of Patent: December 8, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Schutze, Heinz Kehne, Klaus Bauer, Hermann Bieringer
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Symmetrical bis-heteroarylmethoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis
Patent number: 5843968Abstract: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d) --NR.sup.6 SO.sub.2 R.sup.Type: GrantFiled: October 27, 1997Date of Patent: December 1, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa, Andrew O. Stewart, David E. Gunn, Richard A. Craig -
Patent number: 5841001Abstract: The present invention provides an industrially advantageous process for the preparation of an optically active 2-halo-1-(substituted phenyl)ethanol useful as medicines, agricultural chemicals or as intermediates thereof; and a simple process for the preparation of an optically active substituted styrene oxide or 2-amino-1-(substituted phenyl)ethanol useful as medicines, agricultural chemicals or intermediates thereof. A 2-halo-1-(substituted phenyl)ethanol represented by the following general formula (I) is allowed to contact, in the presence of a carboxylic anhydride, with an enzyme stereoselectively catalyzing ester interchange to produce an optically active 2-halo-1-(substituted phenyl)ethanol: ##STR1## (wherein X represents a chlorine atom or a bromine atom, and R.sup.1, R.sup.2 and R.sup.3 may be the same or different and each represent a hydrogen atom, a halogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 haloalkyl group, a C.sub.Type: GrantFiled: February 28, 1997Date of Patent: November 24, 1998Assignee: Mitsubishi Chemical CorporationInventors: Ken Tanaka, Mari Yasuda, Makoto Ueda
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Patent number: 5840901Abstract: The present invention relates to a process of preparing quinacridone by oxidizing a 6,13-dihydroquinacridone salt corresponding to the quinacridone pigment with hydrogen peroxide as the oxidizing agent. The inventive process is economical and environmentally friendly and yields high performance quinacridone pigments in a high yield.Type: GrantFiled: August 13, 1997Date of Patent: November 24, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Fridolin Babler
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Patent number: 5837710Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: November 17, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: William J. Hornback, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Patent number: 5834513Abstract: Described are the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions, compositions containing these compounds, and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein, R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 --C(.dbd.X.sub.2)X.sub.3 R.sub.11, with n being an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, X.sub.2, X.sub.3, Y and Z are independently, O, NH or S.Type: GrantFiled: April 25, 1996Date of Patent: November 10, 1998Assignee: Avon Products, Inc.Inventors: Dmitri Ptchelintsev, Neil Scancarella, Robert Kalafsky
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Patent number: 5834423Abstract: The present invention is a pharmaceutical composition used as an antiviral agent, a diarrheal remedy, an antiulcer agent, an anti-inflammatory agent, an anti-allergic agent and an agent for promoting the proliferation of Bifidobacteria, characterized by containing a sialic acid derivative as an active ingredient. The method for producing a sialic acid derivative of the present invention is characterized in that an almond or apricot seed is added to an avian egg yolk, by which the desired product can easily be obtained in a high yield.Type: GrantFiled: March 15, 1996Date of Patent: November 10, 1998Assignee: Taiyo Kagaku Co., Ltd.Inventors: Mamoru Koketsu, Masakazu Nishizono, Teruhiko Nitoda, Yuko Enoki, Hiroshi Kawanami, Lekh Raj Juneja
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Patent number: 5834476Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.Type: GrantFiled: December 12, 1997Date of Patent: November 10, 1998Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hirofumi Terasawa, Akio Ejima, Satoru Ohsuki, Kouichi Uoto
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Patent number: 5834467Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: November 10, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriquez
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Patent number: 5833953Abstract: Process for the preparation of fluoridated casein micelles, in which at least 100 ppm of a soluble fluoride salt are added of a solution comprising micellar casein and the fluoridated micellar casein is isolated. Food or pharmaceutical composition for treating dental caries or plaque comprising an effective quantity of fluoridated micellar casein or its micellar subunits.Type: GrantFiled: June 14, 1996Date of Patent: November 10, 1998Assignee: Nestec S.A.Inventors: Rafael Berrocal, Jean-Richard Neeser, Pierre Tachon
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Patent number: 5834486Abstract: The invention relates to compounds of formula (I) ##STR1## wherein either R.sub.1 is hydrogen andR.sub.2 is lower alkyl lower alkenyl or lower alkynyl,m is 3 or 4 andn is 2 or 3;orR.sub.1 and R.sub.2 together are tetrainethylene,m is 3 or 4 andn is 2;or salts thereof.The compounds of formula (I) influence polyamine biosynthesis and have antiproliferative activity as well as an action against protozoans.Type: GrantFiled: September 15, 1997Date of Patent: November 10, 1998Assignee: Novartis AGInventors: Jorg Frei, Jaroslav Stanek
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Patent number: 5831125Abstract: A method of selective N-acylation of an aminodiol having a primary alcoholic hydroxyl group and a secondary alcoholic hydroxyl group, in which the objective product can be prepared in high yield and without troublesome extraction and purification operations. More particularly, a method of making a primary amide derivative represented by the following general formula (3) is disclosed: ##STR1## wherein R.sup.1 represents a linear saturated aliphatic hydrocarbon group having 11 to 19 carbon atoms, R.sup.2 represents a linear saturated or unsaturated aliphatic hydrocarbon group having 9 to 19 carbon atoms which may have a hydroxyl group at the 1-position, which includes the steps of reacting an aminodiol represented by the following general formula (1): ##STR2## wherein R.sup.1 is the same as R.sup.1 in general formula (3) with a fatty acid alkyl ester represented by the following general formula (2):R.sup.2 --COO--R.sup.3 (2)wherein R.sup.2 is the same as R.sup.2 in general formula (3) and R.sup.Type: GrantFiled: April 17, 1997Date of Patent: November 3, 1998Assignee: Takasago International CorporationInventors: Kazutoshi Sakurai, Kenya Ishida, Miharu Ogura
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Patent number: 5827891Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Patent number: 5827858Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
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Patent number: 5827859Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, John H. Tatlock
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Patent number: 5824688Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
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Patent number: 5824689Abstract: The jineol extracted from scolopendra subspinipes is represented as the following formula (I): ##STR1## The jineol is obtained from scolopendra subspinipes by extracting scolopendra subspinipes with a solvent, separating an activating portion from the extracted liquid with an organic solvent, and purifying an anticancerous activating portion from the activating portion by chromatography.The jineol derivatives prepared from the jineol extracted scolopendra subspinipes are represented as the following formula (II): ##STR2## wherein each R.sub.1 and R.sub.2, independently of each other, is a hydrogen; a lower alkyl group of C.sub.1 to C.sub.6 ; a cycloalkyl group of C.sub.5 to C.sub.7 having a substituting group; an alkyl group of C.sub.1 to C.sub.4 having a phenyl group with one to three substituting groups; a lower alkyl group of C.sub.1 to C.sub.6 having a hydroxy, an alkoxy having C.sub.1 to C.sub.5, or an aryloxy; a lower acyl group of C.sub.1 to C.sub.7 having a hydroxy, an alkoxy having C.sub.1 to C.sub.Type: GrantFiled: May 30, 1997Date of Patent: October 20, 1998Assignee: Samsung General Chemicals Co., Ltd.Inventors: Ho-Seong Lee, Young-Jun Park, Min-Hwan Kim, Seok-Shik Moon, Nam-Sun Cho, Jong-Hyun Shin, Young-Whan Suh, Jung-Ok Lee
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Patent number: 5821242Abstract: The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as hepatitis C and bovine diarrheal virus.Type: GrantFiled: June 4, 1997Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Joseph Matthew Colacino, Beverly Ann Heinz, Louis Nickolaus Jungheim, Shawn Christopher Miller, Wayne Alfred Spitzer, Joseph Chiou-chung Tang, Mark Joseph Tebbe, Frantz Victor
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Patent number: 5814651Abstract: This invention relates to 4-substituted catechol diether compounds which are selective inhibitors of phosphodiesterase (PDE) type IV. The compounds of the present invention are useful in inhibiting PDE.sub.IV and in the treatment of AIDS, asthma, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and other inflammatory diseases. This invention also relates to pharmaceutical compositions comprising the compounds hereof.Type: GrantFiled: June 10, 1997Date of Patent: September 29, 1998Assignee: Pfizer Inc.Inventors: Allen Jacob Duplantier, James Frederick Eggler, Anthony Marfat, Hiroko Masamune
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Patent number: 5814646Abstract: A method of protecting a warm-blooded mammal from the progression of Alzheimer's disease, which comprises administering an effective amount of a compound of general formula. ##STR1## in which: R.sup.1 represents an optionally substituted aromatic or heteroaromatic group;L.sup.1 and L.sup.2 each independently represents a bond or an unbranched (1-4C) alkylene group, which alkylene group may optionally bear a (1-4C) alkyl, phenyl or phenyl (1-2C) alkyl substituent;one of Y.sup.1 and Y.sup.2 represents NR.sup.3 and the other represents O, S or NR.sup.3, in which R.sup.3 represent hydrogen, hydroxyl, (1-4C) alkoxy, (1-4C) alkyl or di (1-4C) alkylamino;Z represents O or S; andR.sup.2 represents (3-8C) cycloalkyl, heterocyclyl, and optionally substituted aromatic or heteroaromatic group, or together with L.sup.2, (1-10C) alkyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 2, 1995Date of Patent: September 29, 1998Assignee: Eli Lilly and CompanyInventors: Lawrence J. Heinz, Jill A. Panetta, Michael L. Phillips, Jon K. Reel, John K. Shadle, Richard L. Simon, Celia A. Whitesitt