Ring In Alcohol Moiety Patents (Class 560/32)
  • Patent number: 6803378
    Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: October 12, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
  • Patent number: 6759511
    Abstract: The present invention relates to a carbonic acid ester compound of the following formula (1): in which X, Y, and Ar are defined in the specification, which can be easily combined with the amino group of an amino acid or removed therefrom under mild conditions, whereby the amino group can be effectively protected during peptide syntheses, process for preparing the same, and use of the same. Since the amino acid derivatives thus protected have high thermal and chemical stabilities and good solubility for organic solvents, peptides can be synthesized at a low cost with a high yield.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: July 6, 2004
    Assignee: Hanchem Co., Ltd.
    Inventors: Hogyu Han, Nakcheol Jeong, SangJo Lee, Jin Gab Oh, Hosung Yu
  • Patent number: 6727098
    Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: April 27, 2004
    Assignee: Kanazawa University
    Inventors: Tomihisa Ohta, Shinzo Hosoi
  • Patent number: 6642406
    Abstract: N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is produced by hydrogenation of a mixture of 3,3-dimethylbutyraldehyde and a precursor of L-&agr;-aspartyl-L-phenylalanine 1-methyl ester. In particular, N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is produced using an acid salt of L-&agr;-aspartyl-L-phenylalanine 1-methyl ester or N-protected L-&agr;-aspartyl-L-phenylalanine 1-methyl ester. The production method is efficient and low cost, as compared with conventional N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester synthesis.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: November 4, 2003
    Assignee: The NutraSweet Company
    Inventors: Indra Prakash, Zhi Guo, Steve Schroeder, Kurt L. Wachholder
  • Publication number: 20030199698
    Abstract: Novel compounds of the formula I 1
    Type: Application
    Filed: May 16, 2003
    Publication date: October 23, 2003
    Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
  • Patent number: 6635621
    Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: October 21, 2003
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Rajeshwar Singh, Nian Zhou, Andhe V. N. Reddy, George Thomas, Qizhu Ding, Jadwiga Kaleta, Ronald George Micetich, Mark Whittaker
  • Patent number: 6620961
    Abstract: Biarylalkylenecarbamic acid derivative represented by general formula (I): [wherein Q is a phenyl group which may be substituted or the like, X is a halogen atom, a (C1-C6) alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a (C1-C6) alkyl group or the like, R2 is a hydrogen atom, a (C1-C6) alkyl group or the like, A is a (C1-C7) alkylene group which may be branched, and G is an oxygen atom, a sulfur atom or a group —NR— (wherein R3 is a hydrogen atom or a (C1-C4) alkyl group)] and agricultural and horticultural fungicides. The agricultural and horticultural fungicides of the present invention are useful as agricultural and horticultural fungicides because they have high preventive effects on cucumber downy mildew, apple scab, wheat powdery mildew, rice blast, cucumber gray mold and rice sheath blight without damaging crops, and are excellent in residual effectiveness and rain-resistance.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: September 16, 2003
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co. Ltd.
    Inventors: Kazuhiro Ikegaya, Masami Ozaki, Takahiro Kawashima, Ichiro Miura, Norimichi Muramatsu
  • Publication number: 20030166961
    Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.
    Type: Application
    Filed: January 27, 2003
    Publication date: September 4, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Akinori Fujita, Naoto Yanagihara, Yohsuke Takeuchi, Daisuke Arioka, Kimi Ikeda, Sachiko Arai
  • Patent number: 6541653
    Abstract: The process disclosed herein satisfies the need in the art for an industrially viable oxidative carbonylation catalytic system, and is capable of producing carbamates at a significantly higher rate than those processes reported in journal and patent literature. This reaction process takes place via a reaction mechanism that does not involve drastic conditions. Specifically, the catalytic system of the present invention employs Group VIII metal catalysts and/or copper-based catalysts with halide promoters to produce carbamates through heterogeneous oxidative carbonylation at atmospheric pressure and relatively non-drastic temperatures in a gas-solid carbonylation process.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: April 1, 2003
    Inventors: Steven S. C. Chuang, Yawu Chi, Bei Chen, Pisanu Toochinda
  • Patent number: 6528678
    Abstract: A phosgene-free method for preparing a carbamate from a compound containing an amine group involves reacting the compound with an alkylating agent in the presence of carbon dioxide and cesium carbonate. A reaction can take place under standard pressure and temperature conditions and produces carbamates in a high yield with low by-product formation.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: March 4, 2003
    Assignee: Pharmacia& Upjohn Company
    Inventor: Byung H. Lee
  • Publication number: 20020188020
    Abstract: This invention is directed to compounds of the following formula: 1
    Type: Application
    Filed: August 31, 2001
    Publication date: December 12, 2002
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B.H. Youdim
  • Patent number: 6486342
    Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: November 26, 2002
    Assignee: Virginia Commonwealth University
    Inventors: Donald J. Abraham, Gajanan S. Joshi, Stephen J. Hoffman, Melissa Grella, Richmond Danso-Danquah, Amal Yousseff, Martin Safo, Sanjeev Kulkarni
  • Patent number: 6455585
    Abstract: New esters derived from substituted phenyl-cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: September 24, 2002
    Assignee: Vita Invest, S.A.
    Inventors: Juan Carlos Del Castillo Nieto, Joan Huguet Clotet, Elisabet De Ramon Amat, Maria Chalaux Freixa, Marisabel Mourelle Mancini
  • Patent number: 6416686
    Abstract: Polyisocyanates are prepared by a process which comprises (i) preparation of an addition product (A) which contains one group which is reactive toward isocyanate and one isocyanate group by reacting (a) a diisocyanate I with (b) compounds containing two groups which are reactive toward isocyanate, where at least one of the components (a) or (b) has functional groups having differing reactivities toward the functional groups of the other component, (ii) if desired, intermolecular addition reaction of the addition product (A) to form a polyaddition product (P) which contains one group which is reactive toward isocyanate and one isocyanate group and (iii) reaction of the addition product (A) and/or the polyaddition product (P) with a diisocyanate or polyisocyanate II which is different from diisocyanate I.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: July 9, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Bruchmann, Hans Renz, Rainer Königer, Ulrike Ehe, Ulrich Treuling, Rudolf Müller-Mall
  • Patent number: 6414158
    Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bayer AKtiengesellschaft
    Inventors: Hubert Dyker, Andrew Plant, Jürgen Scherkenbeck, Christoph Erdelen, Achim Harder
  • Patent number: 6350305
    Abstract: A polymeric furanone magenta colorant is disclosed that contains a furanone magenta chromophore having a furanone adduct, the adduct containing at least one alkoxylated phenyl radical, the chromophore further being derived from at least one aromatic aldehyde having a para-nitrogen and containing electron donating groups selected from the group consisting of alkyls, cycloalkyls, and oligomers or polymers derived from alkyleneoxy or aryleneoxy moieties. The colorant can be utilized in resins, waxes and inks.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: February 26, 2002
    Assignee: Xerox Corporation
    Inventors: Clifford R. King, Jeffery H. Banning
  • Patent number: 6344558
    Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: February 5, 2002
    Assignee: Gruenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: 6335459
    Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor agonists, and which are represented by Formula I: wherein R1, R2, R3, R4, R5, A, and B are as defined in the specification, and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: January 1, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Daniel Lee Severance
  • Patent number: 6306873
    Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: October 23, 2001
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
  • Patent number: 6303650
    Abstract: This invention is directed to compounds of the following formula wherein when a is O, b is 1 or 2; when a is 1, b is 1, m is from 0-3 X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADC), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: October 16, 2001
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation, Ltd., Teva Pharmaceutical Industries, Ltd.
    Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B. H. Youdim
  • Patent number: 6248737
    Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 19, 2001
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: 6235929
    Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.
    Type: Grant
    Filed: December 27, 1996
    Date of Patent: May 22, 2001
    Assignee: Georgia Tech Research Corporation
    Inventor: James C Powers
  • Patent number: 6194458
    Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.
    Type: Grant
    Filed: October 21, 1999
    Date of Patent: February 27, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
  • Patent number: 6180374
    Abstract: Azlactone (3), or the opposite enantiomer thereof, undergoes biotransformation, using suitable enzymatic activity, in the presence of a compound YH to form a N-acyl-amino acid (2), wherein R1, R2 and R3 are each not hydrogen and are independently selected from groups containing up to 20 carbon atoms, optionally with any combination of R1, R2 and R3 being joined together to form at least one ring, X is selected from groups containing up to 20 carbon atoms, and Y is selected from the group consisting of —OH, -Oalkyl and -Nalkyl. Amino acid (1), or the opposite enantiomer thereof, can be prepared in high enantiomeric excess from N-acyl amino acid (2), by converting Y to OH.
    Type: Grant
    Filed: August 10, 1998
    Date of Patent: January 30, 2001
    Assignee: Chirotech Technology, Inc.
    Inventors: Nicholas Turner, James Winterman, Raymond McCague
  • Patent number: 6174885
    Abstract: A [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is—(CH2)n-NR2R3; Z is —O—, —OCO—, —OCONR6— or —NR6—; R2 and R3 individually represent a hydrogen, lower alkyl, phenyl or benzyl group, or together represent a heterocycle having 3-7 members; —NR5—(CH2)n-NR2R3 or —NR6—(CH2)n-NR2R3 may be Group W, and —OCONR6—(CH2)n-NR2R3 may be —OCO—W, wherein W is a formula of: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, lower alkyl, phenyl or benzyl group; R4 is a halogen, lower alkyl, lower acyl, nitro, cyano, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, lower alkylamino, lower acylamino, lower alkoxy or lower acyloxy group; each of R5 and R6 is a hydrogen, low
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: January 16, 2001
    Assignee: Shiseido Co., Ltd.
    Inventors: Hirotada Fukunishi, Tsunao Magara, Koji Kobayashi
  • Patent number: 6172108
    Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z  (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptor
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: January 9, 2001
    Assignee: Adir et Compagnie
    Inventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
  • Patent number: 6169206
    Abstract: 4-(N,N-Dialkylamino)aniline compounds of the following general formula (I): wherein R1 represents an alkyl group, an aryl group or a heterocyclic group, R2 to R5 each represent a hydrogen atom or a substituent, and R2 and R3, R1 and R2, or R4 and R5 may form a ring together; a processing composition for color photography, which contains at least one of these compounds; and a color image-forming method wherein at least one of these aniline compounds is used.
    Type: Grant
    Filed: January 24, 2000
    Date of Patent: January 2, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
  • Patent number: 6143917
    Abstract: A process for producing an aryl carbamate of a high purity at a high yield by reacting a diaryl carbonate with an amine compound having one or more hydrogen atoms bonded to the N position in the presence of carboxylic acid(s) of the following general formulae (I): R.sup.1 --COOH and/or (II): R.sup.2 --COOH (wherein R.sup.1 represents an alkyl or cycloalkyl group having an .alpha.-positioned carbon atom bonded to only one hydrogen atom, an alkyl group having an .alpha.-positioned carbon atom bonded to no hydrogen atom, or an aryl or heterocyclic group, and R.sup.2 represents an alkyl group having an .alpha.-positioned carbon atom bonded to two or more hydrogen atoms).
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: November 7, 2000
    Assignee: Ube Industries, Ltd.
    Inventors: Katsumasa Harada, Ryoji Sugise, Kohichi Kashiwagi, Tsunao Matsuura
  • Patent number: 6114325
    Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: September 5, 2000
    Assignee: Shiseido Co., Ltd.
    Inventors: Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima, Koji Kobayashi
  • Patent number: 6096836
    Abstract: Disclosed herein is a curing catalyst comprising at least one compound which is a substituted or unsubstituted aromatic or heteroaromatic compound and having any one of groups (I) --O--R.sub.1, (II) --O--CY--R.sub.1, or (III) --O--CY--X--R.sub.1, the groups being directly bonded to the armoatic or heteroaromatic ring, in a number of 1 to 10 wherein R.sub.1 may be the same or different and is a substituted or unsubstituted hydrocarbon group having 1 to 20 carbon atoms, X is O or NH and Y is O or S. Furthermore, an epoxy resin composition comprising the curing catalyst is disclosed.
    Type: Grant
    Filed: March 2, 1998
    Date of Patent: August 1, 2000
    Assignee: Kabushiki Kaisha Toshiba
    Inventors: Shuzi Hayase, Yoshihiko Nakano, Shinji Murai, Yukihiro Mikogami
  • Patent number: 6080784
    Abstract: Compositions with protein kinase C-modulatory, anti-inflammatory and other activities are disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 27, 2000
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 6057269
    Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: May 2, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6043284
    Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: February 5, 1998
    Date of Patent: March 28, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
  • Patent number: 6013606
    Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: January 11, 2000
    Assignee: BASF Akteingesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Christoph-Sweder von dem Bussche-Hunnefeld, Peter Munster, Reinhard Kirstgen, Albrecht Harreus, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5985919
    Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5977398
    Abstract: A viscosity conditioner is disclosed which is comprised of a compound represented by the following formula ##STR1## where R.sup.1 to R.sup.3 each are hydrocarbyl groups which may be identical or different, m ranges from 2 to 4, and n ranges from 1 to 1,000. The specified viscosity conditioner is by nature non-ionic and excellent in leveling.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: November 2, 1999
    Assignee: Asahi Denka Kogyo K.K.
    Inventor: Kaoru Komiya
  • Patent number: 5962487
    Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: October 5, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
  • Patent number: 5955501
    Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 21, 1999
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 5854283
    Abstract: The optically pure forms of monoocarbamates of halogenated 2-phenyl-1,2-ethanediol and dicarbamates of 2-phenly-1,2-ethaniediol have been found to be effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: December 29, 1998
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Min Woo Kim, Jeonghan Park
  • Patent number: 5837873
    Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: November 17, 1998
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Lynn M. Codacovi, Steven J. Wittenberger
  • Patent number: 5831114
    Abstract: Substituted N-phenyl- and N-heteroarylalkylcarbamates of formula (I), in which Q is a group (1), (2) or (3); R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy; Z is hydrogen or halogen; or Z and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--; R.sub.1 is C.sub.1 -C.sub.5 alkyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl; X is oxygen, sulfur, --SO-- or --SO.sub.2 --, Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano; n is 0, 1 or 2; n.sub.1 is 0 or 1; and m is 0 or 1, with the proviso that m is 1 if Q is group (1) or (2); and the diastereomers and enantiomers thereof, exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: November 3, 1998
    Assignee: Novartis Finance Corporation
    Inventors: Hermann Rempfler, Fredrik Cederbaum, Felix Spindler, Willy Urs Lottenbach
  • Patent number: 5780585
    Abstract: A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 14, 1998
    Assignee: Cancer Research Campaign Technology Limited
    Inventors: Gillian Anlezark, Roger Melton, Roger Sherwood, Thomas Connors, Frank Friedlos, Michael Jarman, Richard Knox, Anthony Mauger, Caroline Joy Springer
  • Patent number: 5756817
    Abstract: The present invention relates to a racemic or enantiomerically enriched O-carbamoyl-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ph is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3, R.sup.1 and R.sup.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cyclic propyl and 5 to 7-membered aliphatic cyclic compounds, and R.sup.1 and R.sup.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: May 26, 1998
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Dong Il Han, Yong Kil Kim, Hun Woo Shin, Jeong-Han Park
  • Patent number: 5750696
    Abstract: Dioxacycloalkane compounds of the formula ?1! ##STR1## wherein A is ##STR2## wherein W is ##STR3## X is --CO-- or --SO.sub.2 --; Y is --CH.sub.2 --, --O-- or --NR.sup.25 --; and R.sup.1 is an aralkyl which may be substituted by lower alkoxy;R.sup.2 is a hydrogen atom or a lower alkyl;R.sup.3 is --(CH.sub.2)d-SR.sup.26 or ##STR4## R.sup.4 and R.sup.5 are each a hydrogen atom or a lower alkyl; and E is --C(R.sup.29)(R.sup.30)-- or --CH.sub.2 CH.sub.2 --, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula ?1! have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: May 12, 1998
    Assignee: Japan Tobacco Inc.
    Inventors: Saizo Shibata, Yasuki Yamada, Koji Ando, Kiyoshi Fukui, Ikuro Nakamura, Itsuo Uchida
  • Patent number: 5734082
    Abstract: This invention relates to a class of aminimides structurally characterized as an acyl nitrogen-nitrogen ylide such that the acyl moiety possess the structural diversity element G, the quaternary nitrogen possess structural diversity elements E and F, and the quaternary nitrogen is bonded to a hydroxyethyl substituent, which in turn is bonded to an aminomethylene moiety that possess structural diversity elements A and B from the amino group and diversity element C from the methylene substituent, as shown below, ##STR1## wherein structural diversity element A, B, C, D, E, F and G are chosen from the set of elements consisting of substituted and unsubstituted as well as branched and straight chain alkyl, aryl, alkaryl, aralkyl, carbocyclic, heterocyclic, hydrogen, amino acid, peptide, polypeptide, protein, depsipeptide, carbohydrate derivatives, nucleotide derivatives, oligonucleotide derivatives, naturally occurring or synthetic organic structural motifs, reporter elements, organic moieties containing at least
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: March 31, 1998
    Assignee: Arqule Inc.
    Inventors: Joseph C. Hogan, Jr., David Casebier, Paul S. Purth, Steve Gallion, Alan Kaplan
  • Patent number: 5728588
    Abstract: A surface of specific reactivity is formed by adsorbing a modified block polymeric surfactant of the Pluronic-type, i.e., containing pendant poly(ethylene oxide) blocks attached at an end to poly(propylene oxide) center blocks and with specifically reactive groups at the unattached ends of the poly(ethylene oxide) blocks, upon a hydrophobic surface.
    Type: Grant
    Filed: March 7, 1995
    Date of Patent: March 17, 1998
    Inventors: Karin Maria Elisabet Caldwell, Per Jan Erik Carlsson, Jenq-Thun Li
  • Patent number: 5705521
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in radiation oncology applications. The compounds are capable of acting on hemoglobin in whole blood.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: The Center for Innovative Technology
    Inventor: Donald J. Abraham
  • Patent number: 5703263
    Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: December 30, 1997
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 5698731
    Abstract: A process is described for the preparation of aromatic carbamates in which an organic carbonate in a stoichiometric quantity or in a quantity higher than the stoichiometric value is reacted with an aromatic amine operating in the presence of a carbamation catalyst, wherein this catalyst is selected from N,N-substituted carbamate complexes of zinc or copper.The process gives high yields and selectivity in the useful reaction product.
    Type: Grant
    Filed: June 27, 1996
    Date of Patent: December 16, 1997
    Assignee: Ministero dell `Universita` e della Ricerca Scientifica e Tecnologica
    Inventors: Aldo Bosetti, Pietro Cesti, Fausto Calderazzo