Benzene Ring Containing Patents (Class 564/155)
  • Publication number: 20010053863
    Abstract: Allylated amide compounds are formulated into curable compositions with a free radical curing agent, and optionally, one or more fillers, for use as adhesives in the manufacture of microelectronic devices.
    Type: Application
    Filed: June 29, 2001
    Publication date: December 20, 2001
    Inventors: Rose Ann Schultz, Donald Herr, Chaodong Xiao
  • Publication number: 20010051731
    Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Application
    Filed: May 1, 2001
    Publication date: December 13, 2001
    Inventors: Fred T. Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Publication number: 20010051719
    Abstract: Novel carboxamide derivatives having CNS activity, processes for their preparation and their use as medicaments
    Type: Application
    Filed: May 4, 2001
    Publication date: December 13, 2001
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
  • Patent number: 6326398
    Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.
    Type: Grant
    Filed: February 28, 2000
    Date of Patent: December 4, 2001
    Assignee: Pfizer Inc.
    Inventors: Yuan-Ching Phoebe Chiang, Robert L. Dow
  • Patent number: 6316669
    Abstract: Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido polybiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting/cleaning contact lenses.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: November 13, 2001
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Joonsup Park, Nathaniel D. McQueen
  • Patent number: 6313122
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6310244
    Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3. A substrate of solid phase synthesis of the formula III is also disclosed.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: October 30, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
  • Patent number: 6307044
    Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
    Type: Grant
    Filed: June 10, 1999
    Date of Patent: October 23, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
  • Patent number: 6297400
    Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1,2-diaminobenzene)to yield the tetraamido macrocycle.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: October 2, 2001
    Assignee: The Clorox Company
    Inventors: James E. Deline, Michael M. Ott
  • Patent number: 6297283
    Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: October 2, 2001
    Assignee: Kowa Co., Ltd.
    Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
  • Patent number: 6291413
    Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: September 18, 2001
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Richard Dykstra
  • Patent number: 6262302
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: July 17, 2001
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
  • Patent number: 6258966
    Abstract: A chiral ligand of the formula (II) or formula (II′), was synthesized. The chiral ligand (II) or formula (II′) can chelate to metals to form a catalytic complex to catalyze the addition of trimethylsilyl cyanide to aldehydes to give optically active cyanohydrin, individually.
    Type: Grant
    Filed: October 13, 1999
    Date of Patent: July 10, 2001
    Assignee: Everlight USA, Inc.
    Inventors: Biing-Jiun Uang, Chun-Tzu Yang
  • Patent number: 6255285
    Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).
    Type: Grant
    Filed: February 15, 2000
    Date of Patent: July 3, 2001
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Ken-ichiro Kotake, Toshiro Kozono, Tsutomu Sato, Hisanori Takanashi
  • Patent number: 6242609
    Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Konica Corporation
    Inventor: Fumio Ishii
  • Patent number: 6235823
    Abstract: Disclosed are a crystalline polypropylene resin composition comprising a crystalline polyproplylene resin and a &bgr;-nucleating agent, and a method of increasing the proportion of &bgr;-form crystals in a crystalline polypropylene resin molding comprising molding the composition, the &bgr;-nucleating agent being a diamide compound.
    Type: Grant
    Filed: January 13, 1993
    Date of Patent: May 22, 2001
    Assignee: New Japan Chemical Co., Ltd.
    Inventors: Naoki Ikeda, Masafumi Yoshimura, Kazuaki Mizoguchi, Hiroshi Kitagawa, Yuji Kawashima, Kiyoshi Sadamitsu, Yasuyuki Kawahara
  • Patent number: 6204391
    Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: March 20, 2001
    Assignee: The Regents of the University of California
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
  • Patent number: 6197798
    Abstract: Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, cycloalkyl or heterocyclyl; R2, R3, R4 and R5 are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4 and R5 at adjacent positions are alkylenedioxy; R6 is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Ra is hydrogen or optionally substituted alkyl, Rb and Rc are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rb and Rc together represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rd is optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Re is op
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: March 6, 2001
    Assignee: Novartis AG
    Inventors: Cynthia A. Fink, Gary M. Ksander, Paivi J. Kukkola, Eli M. Wallace, Mahavir Prashad
  • Patent number: 6194437
    Abstract: The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: February 27, 2001
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, Martyn Clive Pritchard
  • Patent number: 6194612
    Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.
    Type: Grant
    Filed: April 7, 1998
    Date of Patent: February 27, 2001
    Assignees: The Scripps Research Institute, CombiChem, Inc.
    Inventors: Dale L. Boger, Soan Cheng, Peter L. Myers
  • Patent number: 6184249
    Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: February 6, 2001
    Assignee: Biophysica, Inc.
    Inventors: Milos Sovak, Allen L. Seligson, James Gordon Douglass, III, Brian Campion, Jason W. Brown
  • Patent number: 6162807
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: January 11, 2000
    Date of Patent: December 19, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6153652
    Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: November 28, 2000
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
  • Patent number: 6140369
    Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease or Alzheimer's which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: October 31, 2000
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William David Flitter, William A. Garland, Allan L. Wilcox, Richard E. Paylor
  • Patent number: 6130315
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: October 10, 2000
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • Patent number: 6127341
    Abstract: Compounds of the general formula I ##STR1## compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: October 3, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Jesper Lau, Bernd Peschke, Michael Ankersen, Kjeld Madsen, Nils Langeland Johansen
  • Patent number: 6121326
    Abstract: Compounds which are useful as a tachykinin antagonist are substituted alkyltetraamine derivatives which are represented by the following formula (I) or a pharmaceutically acceptable salt, a complex compound or a solvate thereof. ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is a phenyl group which may be substituted with one or more hydroxyl, lower alkoxy and/or acyloxy group(s). The compounds are useful as an anti-inflammatory agent, anti-allergic agent, analgesic, antiemetic, agent for irritable colon syndrome, agent for dermal disease, agent for vasospastic disease, agent for cerebral ischemic disease, antidepressant, antianxiety agent, agent for autoimmune disease, antispasmodic, and as a muscle relaxant, etc.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 19, 2000
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Atsushi Yamamoto, Ko Nakamura, Masanori Otsuka
  • Patent number: 6110925
    Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: August 29, 2000
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Robert M. Williams, Chenguang Yuan
  • Patent number: 6096098
    Abstract: The present invention discloses asymmetrical bleach activators for use in both solid and liquid additive, bleaching and detergent compositions. The asymmetrical bleach activators display the unique ability to form both hydrophilic and hydrophobic bleaching agents in aqueous liquors such as bleaching solutions. Thus, fabrics, hard surfaces or dishes having hydrophobic stains such as dingy and or hydrophilic stains such as beverages can be effectively cleaned or bleached using the bleach activators of the present invention.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: August 1, 2000
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Richard Dykstra, Kevin Lee Kott, Stefano Scialla
  • Patent number: 6084065
    Abstract: The present invention relates to oligopeptidic compounds having the general formula (I):K--[--A--].sub.z --[--B--].sub.w --L (I)The compounds having general formula (I) are antifungals for agricultural purposes.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: July 4, 2000
    Assignee: Isagro Spa
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Ernesto Signorini
  • Patent number: 6071957
    Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: June 6, 2000
    Assignee: The University of Tennessee Research Corporation
    Inventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
  • Patent number: 6066765
    Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.
    Type: Grant
    Filed: March 30, 1998
    Date of Patent: May 23, 2000
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
  • Patent number: 6063819
    Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.
    Type: Grant
    Filed: February 18, 1998
    Date of Patent: May 16, 2000
    Assignee: Cypros Pharmaceutical Corp.
    Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
  • 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: 6040339
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 6028192
    Abstract: The present invention relates to a process for the preparation of compounds of the formula 1 ##STR1## by reacting a secondary acid amide of the formula 2 ##STR2## with an acid chloride of the formula 3 ##STR3## in the presence of N,N-diisopropyl-N-ethylamine. R.sup.1, R.sup.2 and R.sup.3 are alkyl or alkenyl radicals, if required also aryl radicals. The compounds of the formula 1 are suitable for use as insecticides or bleach activators.
    Type: Grant
    Filed: January 27, 1998
    Date of Patent: February 22, 2000
    Assignee: Clariant GmbH
    Inventors: Johannes Becherer, Klaus Delpy, Karl-Heinz Keil, Bernhard Mees
  • Patent number: 6025328
    Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.
    Type: Grant
    Filed: February 20, 1998
    Date of Patent: February 15, 2000
    Assignee: The Regents of the University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Patent number: 6013837
    Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2)a-(X.sub.1).sub.b -Q.sub.1 -Q.sub.2 -C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radical or one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 -R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2, their preparation process and their use as pesticides.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: January 11, 2000
    Assignee: Hoechst Marion Roussel
    Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
  • Patent number: 6013673
    Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: January 11, 2000
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yuuki Nagao, Kazuhiko Torisu, Takayuki Maruyama
  • Patent number: 6005010
    Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
  • Patent number: 5977178
    Abstract: Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: November 2, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
  • Patent number: 5969184
    Abstract: The present invention is directed to the novel intermediate compounds of the formula: ##STR1## wherein, interalia, R.sub.4 is a substituted phenyl or an optionally substituted napthyl derivative.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: October 19, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry Leroy Adams, Peter William Sheldrake, Timothy Francis Gallagher, Ravi Shanker Garigipati, Paul Elliot Bender, Jeffrey Charles Boehm, Joseph Sisko, Zhi-Qiang Peng, John C. Lee
  • Patent number: 5962736
    Abstract: A logically ordered array of 10,240 different compounds, each compound prepared from the reaction product of an oxazolone, aldehyde and amine.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: October 5, 1999
    Assignee: Arqule, Inc.
    Inventors: Robert Zambias, David A. Bolten, Joseph C. Hogan, Paul Furth, David Casebier, Cheng Tu
  • Patent number: 5962530
    Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: October 5, 1999
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
  • Patent number: 5955506
    Abstract: A group of benzamide compounds are disclosed. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The pharmaceutical compositions can arrest or slow the progressive loss of function.
    Type: Grant
    Filed: February 2, 1998
    Date of Patent: September 21, 1999
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William David Flitter, William A. Garland, Allan L. Wilcox, Richard E. Paylor
  • Patent number: 5955452
    Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: September 21, 1999
    Assignee: Roche Diagnostics GmbH
    Inventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss
  • Patent number: 5935585
    Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: August 10, 1999
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, Laurence Vigne
  • Patent number: 5935979
    Abstract: The invention relates to novel substituted amino acid amides, to a process for their preparation and to their use as pesticides.
    Type: Grant
    Filed: July 16, 1997
    Date of Patent: August 10, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Gerd Hanssler, Klaus Stenzel
  • Patent number: 5929118
    Abstract: The present invention relates to novel fluorobutenic acid hydrazides of the formula (I) ##STR1## in which Y represents C.dbd.O, C.dbd.S or SO.sub.2,R.sup.1 represents hydrogen or halogen andR.sup.2 represents alkyl, halogenoalkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkenyloxy, alkoxy, cycloalkyloxy, alkylthio or respectively optionally substituted aryl, aralkyl, aralkyloxy or hetaryl,to processes for their preparation and to their use for controlling animal pests.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: July 27, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Kraatz, Wolfgang Kramer, Wolfram Andersch, Andreas Turberg, Norbert Mencke
  • Patent number: 5888481
    Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: March 30, 1999
    Assignee: AlliedSignal Inc.
    Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind