6,6-di-substituted Patents (Class 514/194)
  • Patent number: 8299051
    Abstract: Inhibitors of the enzyme beta-lactamase of formula (I): are provided. The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: October 30, 2012
    Assignee: Southern Methodist University
    Inventors: John D. Buynak, Anjaneyulu Sheri, Sundar Ram Reddy Pagadala
  • Patent number: 7723389
    Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Publication number: 20080318918
    Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a nonionic polymer surfactant, such as an alkyl aryl polyether alcohol (e.g., tyloxapol) to the tympanic membrane. The medicaments delivered according to the methods of the invention include antibiotic, antiviral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.
    Type: Application
    Filed: August 25, 2006
    Publication date: December 25, 2008
    Inventors: William R. Campbell, Neil E. Paulsen, Roland H. Johnson
  • Patent number: 7169771
    Abstract: The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: January 30, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Hynes, Hong Wu, Katerina Leftheris, Chunjian Liu, Jagabandhu Das, Robert V. Moquin
  • Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Patent number: 6852742
    Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: January 14, 2003
    Date of Patent: February 8, 2005
    Assignee: Vittal Mallya Scientific Research Foundation
    Inventors: Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao, Jeffrey A. Bibbs
  • Patent number: 6569679
    Abstract: The present invention provides recombinant viral vectors carrying a vector construct which directs the expression of a gene product (e.g., HSVTK) that activates a compound with little or no cytotoxicity into a toxic product. Also provided are methods of destroying or inhibiting pathogenic agents in a warm blooded animal, comprising the step of administering to the animal a viral vector such as that described above, in order to inhibit or destroy the pathogenic agent.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 2003
    Assignee: Chiron Corporation
    Inventors: Jack R. Barber, Harry E. Gruber, Douglas J. Jolly
  • Patent number: 6495539
    Abstract: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond tha
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: December 17, 2002
    Assignee: Washington University
    Inventors: Scott J. Hultgren, Fredrik Almqvist, Gabriel Soto
  • Patent number: 6436398
    Abstract: Compound of formula I: wherein R1, R2, R3, R4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: August 20, 2002
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 6403572
    Abstract: There is disclosed a process for producing an acid salt of a (Z)-2-aminothiazole compound of the formula (I): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, Y represents a halogen atom, —OSO3H or —OPO(OH)2, m indicates the valence number of an inorganic acid of the formula: HY wherein Y represents the same as defined above, and n indicates an integer of 1 or 2, which process is characterized by: reacting an acid salt of a 2-aminothiazole compound of the formula (II): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, X represents a bromine atom or an iodine atom, and the wavy line means that this compound is a mixture of the E- and Z-isomers, with the inorganic acid of the formula HY.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: June 11, 2002
    Assignees: Sumitomo Chemical Co., Ltd., Shionogi & co., Ltd.
    Inventors: Isao Kurimoto, Norihiko Hirata, Akihiko Nakamura, Yuichiro Aratake
  • Patent number: 6166014
    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: May 19, 1999
    Date of Patent: December 26, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 5994340
    Abstract: New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial .beta.-lactamases. These compounds can be used in combination with .beta.-lactam antibiotics to increase the effectiveness of the .beta.-lactam antibiotics in fighting infection caused by .beta.-lactamase producing bacteria.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: November 30, 1999
    Assignee: SynPhar Laboratories, Inc.
    Inventors: Samarendra N. Maiti, Oludotun A. Phillips, Eduardo L. Setti, Andhe V. Narender Reddy, Ronald G. Micetich, Fusahiro Higashitani, Chieko Kunugita, Koichi Nishida, Tatsuya Uji
  • Patent number: 5538962
    Abstract: The present invention provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;Z is carboxy, sufonic acid, tetrazol-5-yl or C .sub.1-4 alkylsulfonylcarbamoyl (--CONHSO.sub.2 C.sub.1-4 alkyl);A is a phenyl or thienyl ring;and A is optionally further substituted by one or two substituents or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: July 23, 1996
    Assignee: Zeneca Limited
    Inventor: Patrice J. Siret
  • Patent number: 5384346
    Abstract: Polyvinyl butyrals (PVBs) with improved thermal stability and improved light resistance contain as stabilizers polynuclear phenols which phenolic radicals have a quaternary carbon atom in the para-position to the phenolic hydroxyl group and if desired in combination with synergistically acting, nitrogen-containing, sulfur-containing or phosphorus-containing co-stabilizers of the types a) to d). The use of the resulting films of low yellowness as interlayer films having substantially reduced yellowing for the production of laminated glasses and glass composites of silicate glass sheets is described.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: January 24, 1995
    Assignee: Hoechst AG
    Inventors: Matthas Gutweiler, Ulrich Hutten, Gerhard Pfahler, Hermann Schindler
  • Patent number: 5180719
    Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: January 19, 1993
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Ronald E. White, Thomas P. Demuth, Jr.
  • Patent number: 4877783
    Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
    Type: Grant
    Filed: January 24, 1985
    Date of Patent: October 31, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Peter H. Milner
  • Patent number: 4847247
    Abstract: Derivatives of Penicillin, their sulfoxides and sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
    Type: Grant
    Filed: October 16, 1986
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Kevan R. Thompson, Paul E. Finke, James B. Doherty
  • Patent number: 4829053
    Abstract: New aminoacid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--NR.sup.6 --(CHR.sup.7).sub.s --D Iwherein X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, R.sup.6, R.sup.7, D, n and s have the meanings defined herein and their salts, inhibit the activity of human plasma renin.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: May 9, 1989
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Peter Raddatz, Joachim Gante, Claus J. Schmitges, Klaus Otto Minck, Johannes Sombroek, Gunter Holzemann
  • Patent number: 4820701
    Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: April 11, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Robert Southgate, Colin H. Frydrych
  • Patent number: 4748163
    Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.
    Type: Grant
    Filed: February 21, 1986
    Date of Patent: May 31, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4734407
    Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: March 29, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4731360
    Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4729989
    Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: March 8, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix
  • Patent number: 4692441
    Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 8, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4684639
    Abstract: A compound having the partial structure (I) ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a group --COR.sup.5 or --CO--OR.sup.5 wherein R.sup.5 represents an optionally substituted hydrocarbon group; R.sup.3 is halogen and R.sup.4 is hydrogen, methoxy, hydroxymethyl or formamido.These compounds are suitably bicyclic .beta.-lactam antibiotics.
    Type: Grant
    Filed: July 5, 1984
    Date of Patent: August 4, 1987
    Assignee: Beecham Group
    Inventors: George Burton, Desmond J. Best
  • Patent number: 4675317
    Abstract: Disclosed are 6- and 6,6-disubstituted-2-substituted thio-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, cycloalkyl, halo, alkoxyl, alkenyl, aralkyl, aryl, heterocyclyl, heteroaryl, and heterocyclylalkyl; W is an electron withdrawing group, and, for example, is selected from: --COR.sup.5, --CN, SO.sub.2 C.sub.6 H.sub.5 ; R.sup.5 is hydrogen; substituted and unsubstituted: alkyl, aryl, aralkyl, heteroaryl, heterocyclyl, or heterocyclylalkyl; or R.sup.5 may be --OR.sup.6, --NR.sup.7 R.sup.8, and --SR.sup.9 ; wherein R.sup.6 is H; substituted and unsubstituted: alkyl, alkenyl, or a group which defines --CO.sub.2 R.sup.6 as a pharmaceutically acceptable ester wherein R.sup.6 is, for example, phthalidyl, or 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl; R.sup.7 and R.sup.
    Type: Grant
    Filed: January 25, 1983
    Date of Patent: June 23, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, William J. Leanza, Ronald W. Ratcliffe, David A. Muthard
  • Patent number: 4670431
    Abstract: A compound having the partial structure (A): ##STR1## wherein n is 1 or 2.
    Type: Grant
    Filed: January 19, 1984
    Date of Patent: June 2, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Peter H. Milner
  • Patent number: 4647457
    Abstract: .beta.-lactams of the formula ##STR1## wherein R.sup.1 signifies hydrogen or a group readily cleavable by hydrolysis, A signifies the group R.sup.2 --N.dbd.C(CH.sub.3)--CH.dbd.C< or O.dbd.C(CH.sub.3)--CH.sub.2 --C(R.sup.3)<, R.sup.2 signifies hydroxy, lower alkoxy or arylamino and R.sup.3 signifies arylthio, lower alkanoylthio, lower alkoxycarbonylhydrazino or a N-containing saturated heterocycle attached via a N-atom, and pharmaceutically acceptable salts thereof, are disclosed. The compounds and their salts exhibit .beta.-lactamase inhibiting activities against .beta.-lactamases from bacteria.
    Type: Grant
    Filed: March 2, 1984
    Date of Patent: March 3, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Solange Adam-Molina
  • Patent number: 4614738
    Abstract: This invention relates to 2-(N-heterocycloaliphaticthio)penems wherein the nitrogen of the heterocyclic ring is connected to the alkyl group, and to their use as antibacterial agents.
    Type: Grant
    Filed: March 25, 1983
    Date of Patent: September 30, 1986
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
  • Patent number: 4609652
    Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
    Type: Grant
    Filed: January 24, 1985
    Date of Patent: September 2, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Peter H. Milner
  • Patent number: 4596677
    Abstract: A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl)anhydropenicillin intermediate.
    Type: Grant
    Filed: April 6, 1984
    Date of Patent: June 24, 1986
    Assignee: Bristol-Myers Company
    Inventors: Alain Martel, Jean-Paul Daris
  • Patent number: 4540689
    Abstract: A penicillin derivative having an antibacterial activity similar to a penicillin antibiotic in a living body without affecting the intestinal bacterial colonies, a process for preparing the derivative and a pharmaceutical composition in a dosage unit form containing the derivative as an active ingredient are disclosed.
    Type: Grant
    Filed: September 16, 1982
    Date of Patent: September 10, 1985
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Shigeaki Muto, Kouichi Niimura, Takao Ando, Akihiko Kanno, Takao Furusho, Chikao Yoshikumi
  • Patent number: 4537886
    Abstract: A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;X represents; ##STR2## wherein R.sup.Y is methyl or acetyl; R.sup.2 and R.sup.3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group; and R.sup.4 is hydrogen, a C.sub.1-6 alkylcarbonyl group, an aryl group, a heterocyclyl group, a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group;R.sup.5 represents, hydrogen, methoxy or --NHCHO; and Y is: ##STR3## wherein Y.sup.1 is oxygen, sulphur or --CH.sub.2 -- and Z represents hydrogen, halogen or an organic group such as C.sub.1-4 alkoxy, --CH.sub.2 Q or --CH.dbd.
    Type: Grant
    Filed: March 29, 1983
    Date of Patent: August 27, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Andrew W. Taylor, Richard T. Cook
  • Patent number: 4505915
    Abstract: This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 6-amino nitrogen moiety of the penicillin (or ring analogue thereof) nucleus represents a mono- or polycyclic N-containing heterocyclic group;X is S, SO, CH.sub.2, or O; m is 0, 1 or 2;R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkyl, heterocyclylalkenyl, aralkenyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN;R.sup.2 is H, or lower alkoxyl.
    Type: Grant
    Filed: March 16, 1981
    Date of Patent: March 19, 1985
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: RE33948
    Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing ##STR3## Z representing O, S, or NR.sup.10, and R.sup.2 represents hydrogen or a protective group.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: June 2, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger