The Additional Hetero Ring Is Six-membered Patents (Class 546/280.1)
  • Patent number: 6881742
    Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.
    Type: Grant
    Filed: October 5, 2000
    Date of Patent: April 19, 2005
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
  • Patent number: 6858732
    Abstract: Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity/coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: February 22, 2005
    Assignee: Vision-Ease Lens, Inc.
    Inventors: Xuzhi Qin, J. Thomas Ippoliti
  • Patent number: 6750233
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
  • Publication number: 20040097729
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.
    Type: Application
    Filed: December 6, 2002
    Publication date: May 20, 2004
    Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
  • Publication number: 20040097733
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: July 2, 2003
    Publication date: May 20, 2004
    Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Publication number: 20040082601
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1
    Type: Application
    Filed: October 21, 2003
    Publication date: April 29, 2004
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6696470
    Abstract: A compound of the formula: and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following: (a) hydrogen, halo, R5—, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5—, R5—O—R5—, or the like; (b) Ar—, Ar—R5—, Ar—C2-6 alkenyl, Ar—C2-6 alkynyl, Ar—O—, Ar—O—R5— or the like; (c) R5—C(O)—, —NO2, cyano, NH2—C(O)—, R5—NH—C(O)—, (R5)2—N—C(O)—, Ar—C(O)— or the like; and (d) R5—C(O)—NH—, Ar—C(O)—NH— or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R5 is optionally halo-substituted C1-6 alkyl; R3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R5—C(O)—, C2-6 alkenyl-C(O)—, C2-6 alkynyl-C(O)—, R5—C(O)—R5—, or the
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: February 24, 2004
    Assignee: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Publication number: 20030225077
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.
    Type: Application
    Filed: April 28, 2003
    Publication date: December 4, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
  • Patent number: 6645951
    Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 11, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
  • Publication number: 20030203927
    Abstract: Heterocyclic-substituted tricyclics of the formula 1
    Type: Application
    Filed: October 16, 2002
    Publication date: October 30, 2003
    Applicant: Schering Corporation
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Yan Xia
  • Publication number: 20030166932
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: January 4, 2002
    Publication date: September 4, 2003
    Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Publication number: 20030158413
    Abstract: The present invention relates to an amide compound of the formula 1
    Type: Application
    Filed: October 21, 2002
    Publication date: August 21, 2003
    Inventors: Shinichi Takanashi, Yoichiro Naito, Hiroshi Tanaka, Masayoshi Uehata, Koshiro Katayama
  • Publication number: 20030130515
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: January 2, 2003
    Publication date: July 10, 2003
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
  • Publication number: 20030078441
    Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.
    Type: Application
    Filed: September 4, 2001
    Publication date: April 24, 2003
    Inventors: Weili Zhao, Erick M. Carreira
  • Publication number: 20030050306
    Abstract: A heteroaryl derivative having the formula (I) 1
    Type: Application
    Filed: June 25, 2002
    Publication date: March 13, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Christian Krog-Jensen, Ivan Mikkelsen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
  • Patent number: 6495568
    Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: December 17, 2002
    Assignee: Warner-Lambert Company
    Inventors: Kevin Neil Dack, Gavin Alistair Whitlock
  • Patent number: 6495576
    Abstract: Compounds of formula (I) may be useful in treating diseases prevented by or ameliorated with potassium channel openers.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: December 17, 2002
    Assignee: Abbott Laboratories
    Inventors: Michael E. Kort, Robert J. Gregg, William A. Carroll, Arturo Perez Medrano, Jürgen Dinges, Fatima Z. Basha
  • Patent number: 6489344
    Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: December 3, 2002
    Assignee: Chiron Corporation
    Inventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
  • Patent number: 6458950
    Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: October 1, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuhiro Nishitani, Koji Ishikura
  • Patent number: 6458789
    Abstract: The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1 to R5 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: October 1, 2002
    Assignee: Lion Bioscience AG
    Inventors: Behrouz Forood, Brenton T. Flatt, Christophe Chassaing, Alan K. Katritzky
  • Patent number: 6440899
    Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: August 27, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 6432880
    Abstract: 2-Phenylpyridines I an their salts, wherein R1 to R17, X1-X3 are as defined in the specification. The compounds are useful as herbicides, desiccants and defoliants.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: August 13, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Olaf Menke, Markus Menges, Ingo Sagasser, Gerhard Hamprecht, Robert Reinhard, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
  • Publication number: 20020103217
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1
    Type: Application
    Filed: January 8, 2002
    Publication date: August 1, 2002
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6420375
    Abstract: To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be substituted, X is a divalent group, Y is a nitrogen atom or a methine group, Z is an ethenylene which may be substituted or ethynylene, R is a heterocyclic group which may be substituted, provided that 3,4-dihydro-6-[3-(1H-imidazol-1-yl)-1-propenyl]-2(1H)-quinolone and 2-[3-[5-ethyl-6-methyl-2-(benzyloxy)-3-pyridyl]-1-propenyl]benzoxazole are excluded.], or a salt thereof which has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating mammals suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: July 16, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Fumio Itoh, Tomohiro Kaku, Masuo Yamaoka
  • Publication number: 20020091150
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: December 10, 2001
    Publication date: July 11, 2002
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
  • Publication number: 20020082419
    Abstract: Compounds of Formula 1 1
    Type: Application
    Filed: November 5, 2001
    Publication date: June 27, 2002
    Applicant: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 6387931
    Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: May 14, 2002
    Assignee: Pfizer INC
    Inventors: Kevin Neil Dack, Gavin Alistair Whitlock
  • Patent number: 6384045
    Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: May 7, 2002
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Jean-Pierre Perchellet
  • Patent number: 6362183
    Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 26, 2002
    Assignee: G. D. Searle & Company
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Patent number: 6340676
    Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: January 22, 2002
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Zenan Li
  • Patent number: 6211379
    Abstract: The present application relates to a process for preparing compounds of the formula (I) in which R1, A, X and Z are each as defined in the description by reacting compounds of the formula (II) in which A and X are each as defined in the description with compounds of the formula (III) in which Z, R1 and M1 are each as defined in the description.
    Type: Grant
    Filed: January 20, 2000
    Date of Patent: April 3, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Seifert, Reinhard Lantzsch, Werner Lindner, Klaus Jelich
  • Patent number: 6211385
    Abstract: Compounds of Formula 1 where the symbols have the meaning disclosed in the specification are prepared by reaction of a compound of Formula 2 with an organometal reagent R—M to provide a compound of Formula 3 that is reacted with the reagent X3—Y(R2)—A—B in the presence of a catalyst to provide the compounds of Formula 1.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: April 3, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna