The Five-membered Ring Contains An Additional Hetero Atom Patents (Class 540/303)
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Publication number: 20100010214
    Abstract: A lyophilized preparation comprising (1R,5S,6S)-6-[(1R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3S)-3-(2-guanidinoacetylamino)pyrrolidin-1-ylcarbonyl]-1-methylpyrrolidin-4-ylthio]-1-carbapen-2-em-3-carboxylic acid or a pharmacologically acceptable salt thereof as a carbapenem compound, which has a 1-alkylpyrrolidine structure and possesses a superior antimicrobial activity, and sodium chloride.
    Type: Application
    Filed: August 28, 2007
    Publication date: January 14, 2010
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Takayuki Kikuchi, Fumihiro Kihara, Masahiko Suzuki
  • Publication number: 20040077622
    Abstract: The present invention provides a compound of formula 1, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: May 1, 2003
    Publication date: April 22, 2004
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Publication number: 20040067929
    Abstract: An oxapenem compound which is, or is capable of forming, a zwitterion of formula Ia or Ib: (Ia), (Ib) wherein R is a C1-C8 branched or straight chain alkyl group which includes a protonated basic substituent. The compounds find particular use as high bioavailability &bgr;-lactamase inhibitors.
    Type: Application
    Filed: July 24, 2003
    Publication date: April 8, 2004
    Inventors: Hans Rudolf Pfaendler, Iain Nelson Simpson
  • Patent number: 5132300
    Abstract: Novel beta lactam compounds having potent elastrase inhibition activity are disclosed. These compounds are characterized by the general structural formulae I, II, and III: ##STR1## These compounds are further characterized such that X and Y are each --S-- or --CH.sub.2 --, with at least one of X and Y being --S--, or alternatively, X is --SO-- or --SO.sub.2 -- and Y is --CH.sub.2 --; R.sup.1 is hydrogen, tri(lower alkyl)silyl, --COOR" or --CONHR"', wherein R" and R"' are each lower alkyl or phenyl(lower alkyl), and may be the same or different; R.sup.3 is hydrogen, lower alkyl or (lower alkyl)oxy; one of B and D is (lower alkyl)oxycarbonyl, (lower alkenyl)oxycarbonyl, allyloxycarbonyl or phenyl(lower alkyl)oxycarbonyl; and the other of B and D is hydrogen or lower alkyl.The compounds are useful as anti-inflammatory agents, particularly in the treatment of adult respiratory distress syndrome and rheumatoid arthritis.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: July 21, 1992
    Assignee: Pfizer Inc.
    Inventors: Robert A. Volkmann, V. John Jasys, Michael S. Kellogg
  • Patent number: 5086170
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and hydroxyalkyl of 1 to 5 carbon atoms and amino, n is an integer from 1 to 3, X and X.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the carbon atom to which they are attached are ##STR2## Y is --O-- or --S--, R.sub.3 is alkyl of 1 to 3 carbon atoms or aryl of 6 to 8 carbon atoms, ##STR3## is selected from the group consisting of ##STR4## R.sub.4 and R.sub.5 are individually aryl unsubstituted or substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkyl and alkoxy of 1 to 3 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof with acids and bases having cyclooxygenase inhibiting and antibiotic acitvity.
    Type: Grant
    Filed: December 24, 1990
    Date of Patent: February 4, 1992
    Assignee: Roussel Uclaf
    Inventors: Abdul B. N. Luheshi, Robert K. Smalley, Peter D. Kennewell, Robert Westwood
  • Patent number: 5059596
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and hydroxyalkyl of 1 to 5 carbon atoms and amino, n is an integer from 1 to 3, X and X.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the carbon atom to which they are attached are >C.dbd.O Y is --O-- or --S--, R.sub.3 is alkyl of 1 to 3 carbon atoms or aryl of 6 to 8 carbon atoms, ##STR2## is selected from the group consisting of ##STR3## R.sub.4 and R.sub.5 are individually aryl unsubstituted or substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkyl and alkoxy of 1 to 3 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof with acids and bases having cyclooxygenase inhibiting and antibiotic activity.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: October 22, 1991
    Assignee: Roussel Uclaf
    Inventors: Abdul B. N. Luheshi, Robert K. Smalley, Peter D. Kennewell, Robert Westwood
  • Patent number: 4728645
    Abstract: Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.
    Type: Grant
    Filed: February 4, 1986
    Date of Patent: March 1, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Leslie J. Browne
  • Patent number: RE32465
    Abstract: Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.
    Type: Grant
    Filed: May 29, 1985
    Date of Patent: July 28, 1987
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Frank Hon