Patents Represented by Attorney Arthur R. Whale
  • Patent number: 4450270
    Abstract: Broad spectrum cephalosporin betaine antibiotics represented by the formula ##STR1## wherein Q is an oximino-substituted pyridinium, quinolinium or isoquinolinium group of the formulas ##STR2## wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.3 alkyl; and R' is an amino-substituted 5- or 6-membered heterocyclic, e.g., 2-aminothiazol-4-yl; and R" is C.sub.1 -C.sub.4 alkyl, an N-substituted carbamoyl group, or a carboxy-substituted alkyl or cycloalkyl group; have potent activity vs. G.sup.- organisms. Pharmaceutical formulations and a method for treating infectious disease with above compounds are provided.
    Type: Grant
    Filed: June 3, 1983
    Date of Patent: May 22, 1984
    Assignee: Eli Lilly and Company
    Inventor: William H. W. Lunn
  • Patent number: 4448990
    Abstract: o-Hydroxy tetralin carboxamides, substituted with an amino group in the aliphatic ring, are dopamine agonists.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: May 15, 1984
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Edmund C. Kornfeld, Robert D. Titus
  • Patent number: 4448717
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in whichR is hydrogen, methyl, ethyl, cyclopropylmethyl, or allyl;A is a residue of a D-amino acid selected from the group consisting of Ala, Abu, Nva, Val, Nle, Leu, Ile, Gly(Al), Gly(Cp), Met, Cys(Me), Met(O), Cys(Me) (O), Ser, Ser(Me), Thr, and Hse;R.sub.1 is hydrogen, C.sub.1 -C.sub.3 primary alkyl, cyclopropylmethyl, allyl, ethylthiomethyl, 2-fluoroethyl, or propargyl;X is fluoro, bromo, iodo, chloro, hydroxy, C.sub.1 -C.sub.3 alkyl, trifluoromethyl, or C.sub.1 -C.sub.2 alkoxy; andZ is methyl or ethyl; are useful analgesic agents.
    Type: Grant
    Filed: November 12, 1982
    Date of Patent: May 15, 1984
    Assignee: Eli Lilly and Company
    Inventor: Robert T. Shuman
  • Patent number: 4448787
    Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or R.sup.6, where R.sup.5 is hydrogen or C.sub.1-8 alkyl and R.sup.6 is phenyl or naphthyl, the phenyl or naphthyl group being optionally substituted by one or more group selected from halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, benzyloxy, nitro, trifluoromethyl, carboxyl, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N(R.sup.5).sub.2, NHCOR.sup.5 and SR.sup.5 ; R.sup.2 is R.sup.6 or --CH.dbd.CH--R.sup.6 when R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano or 5-tetrazolyl, or R.sup.2 is --CH.dbd.CH--R.sup.6 when R.sup.1 is R.sup.6 ; R.sup.3 is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy or --OCH.sub.2 R.sup.6 ; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. The compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.
    Type: Grant
    Filed: September 17, 1981
    Date of Patent: May 15, 1984
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, William J. Ross, Alec Todd
  • Patent number: 4448730
    Abstract: Di, tri and tetrahydroxybenzohydroxamic acids, amides and the corresponding di, tri and tetrahydroxy substituted phenylalkanohydroxamic acids, amides and phenyl esters, ribonucleotide reductase inhibitors.
    Type: Grant
    Filed: April 20, 1982
    Date of Patent: May 15, 1984
    Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
  • Patent number: 4443436
    Abstract: C-20-Modified derivatives of the macrolide antibiotics tylosin, desmycosin, macrocin, lactenocin, 2"'-O-demethylmacrocin and 2"-O-demethyllactenocin inhibit pathogenic bacteria, especially gram-positive bacteria, Pasteurella species, and Mycoplasma species and pharmaceutical compositions thereof.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: April 17, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, John E. Toth
  • Patent number: 4442032
    Abstract: Compounds of formula (I) ##STR1## in which n is 1 or 2, R.sup.1 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, halo or hydroxy, m is 0, 1 or 2, R.sup.2 is an immunogenic determinant and x is 1 or 2, provided that when n is 1, x is 1 or 2 and there is one diazo moiety at the 3-position or two diazo moieties at the 3- and 5-positions, with respect to the isothiocyanate group, and the hydroxy group is at the 4-position; and provided that when n is 2, x is 1 and the diazo moiety is at the 4-position and the hydroxy groups are at the 3- and 5-positions, are described. The compounds are useful in the preparation of immunoglobulin conjugates for employment in diagnostic techniques.
    Type: Grant
    Filed: November 27, 1981
    Date of Patent: April 10, 1984
    Assignee: Lilly Industries Limited
    Inventor: Robin G. Simmonds
  • Patent number: 4440857
    Abstract: A new microorganism, Streptomyces fradiae NRRL 12201, which produces mycarosyltylactone (5-O-mycarosyl-20-dihydro-20,23-dideoxytylonolide) and a process for preparing tylactone (20-dihydro-20,23-dideoxytylonolide) and mycarosyltylactone by submerged aerobic fermentation of this microorganism, or a mycarosyltylactone-producing mutant or recombinant thereof, are provided.
    Type: Grant
    Filed: March 18, 1982
    Date of Patent: April 3, 1984
    Assignee: Eli Lilly and Company
    Inventors: Eugene T. Seno, Richard H. Baltz
  • Patent number: 4440759
    Abstract: 20-Amino derivatives of tylosin and desmycosin are active against bacteria and Mycoplasma.
    Type: Grant
    Filed: February 24, 1983
    Date of Patent: April 3, 1984
    Inventors: Satoshi Omura, Akira Nakagawa
  • Patent number: 4436549
    Abstract: N-(1,3,4-Thiadiazin-2-yl)-2,6-dialkoxybenzamide derivatives useful as herbicides.
    Type: Grant
    Filed: October 28, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Thomas D. Thibault
  • Patent number: 4436815
    Abstract: An improved method for stabilizing and selecting host cells containing recombinant DNA which expresses a functional polypeptide and the novel organisms and cloning vectors for the practice thereof.
    Type: Grant
    Filed: November 27, 1981
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventors: Charles L. Hershberger, Paul R. Rosteck, Jr.
  • Patent number: 4436734
    Abstract: The antibiotic, avilamycin, is useful in the treatment or prevention of swine dysentery.
    Type: Grant
    Filed: January 17, 1983
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Earl E. Ose
  • Patent number: 4436596
    Abstract: N-substituted-2-(R)-(sulfinic acid)-3-(S)-(acylamino)-4-oxo-azetidines, which are useful as intermediates in 1-oxa .beta.-lactam antibiotics, are synthesized by electrolytic reduction of 7-(S)-acylamino-3-hydroxymethyl-3-cephem-4-carboxylic acid compounds.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: David A. Hall
  • Patent number: 4436912
    Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)]acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: William J. Wheeler
  • Patent number: 4436733
    Abstract: 4"- and 3-Ester derivatives of 23-demycinosyltylosin (DMT) and 23-de(mycinosyloxy)tylosin (DMOT) of the formula: ##STR1## wherein R is hydrogen, optionally substituted C.sub.1 -C.sub.5 -alkanoyl or optionally substituted benzoyl, phenylacetyl or phenoxyacetyl; R.sup.1 is hydrogen, optionally substituted C.sub.1 -C.sub.5 -alkanoyl or optionally substituted benzoyl, phenylacetyl, or phenylpropionyl; R.sup.2 is hydrogen, optionally substituted C.sub.1 -C.sub.5 -alkanoyl, or optionally substituted benzoyl, phenylacetyl, phenylpropionyl, phenoxyacetyl or phenylthioacetyl; R.sup.3 is hydrogen or R.sup.4 O--; and R.sup.4 is hydrogen or a specified acyl group provided that one of R or R.sup.2 must be other than hydrogen and that, when R.sup.1 is hydrogen, R.sup.3 is hydrogen or --OH and R.sup.2 is acetyl, R cannot be hydrogen, acetyl, n-butyryl or isovaleryl and, when R and R.sup.1 are hydrogen and R.sup.3 is hydrogen or --OH, R.sup.
    Type: Grant
    Filed: March 3, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Herbert A. Kirst
  • Patent number: 4436739
    Abstract: Substituted 1-thia-3-aza-4-ones having utility as plant fungicides, herbicides and terrestrial and aquatic plant growth regulators, together with methods for the use thereof and compositions containing the compounds.
    Type: Grant
    Filed: December 4, 1981
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: Eriks V. Krumkalns
  • Patent number: 4434288
    Abstract: This invention concerns a process for preparing 2-amino-1,5(6)-substituted-benzimidazole compounds by reacting a 1-unsubstituted-2-amino-5(6)-substituted-benzimidazole compound with a sulfonyl chloride or a haloalkyl isothiocyanate in the presence of an alkali metal hydroxide or carbonate, water, and a water-miscible nonhydroxylic solvent.
    Type: Grant
    Filed: April 8, 1982
    Date of Patent: February 28, 1984
    Assignee: Eli Lilly and Company
    Inventor: James H. Wikel, II
  • Patent number: 4431809
    Abstract: Antibiotic A-33853 is produced by submerged, aerobic fermentation of a new Streptomyces sp. NRRL 12068. The antibiotic and the diacetyl and triacetyl derivatives thereof disclosed herein have shown antibacterial activity against Staphylococcus and Streptococcus species which are penicillin resistant. In addition, the antibiotic and its tetraacetyl derivative have shown antiviral and antitrichomonal activity in vitro.
    Type: Grant
    Filed: May 7, 1982
    Date of Patent: February 14, 1984
    Assignee: Eli Lilly and Company
    Inventors: Marvin M. Hoehn, Karl H. Michel
  • Patent number: 4431803
    Abstract: 7-Epi-3-exomethylenecephams are useful intermediates for synthesis of antibiotics.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: February 14, 1984
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Janice L. Pfeil
  • Patent number: 4431589
    Abstract: These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.
    Type: Grant
    Filed: December 3, 1981
    Date of Patent: February 14, 1984
    Assignee: Lilly House
    Inventors: Jiban K. Chakrabarti, Terrence M. Hotten, David J. Steggles