Patents Represented by Attorney Robert A. Conrad
  • Patent number: 4845200
    Abstract: A conjugate comprising a vinca moiety convalently linked at the 4-position via a group of the formula --OCOXCO-- where X represents a single chemical bond or an optionally substituted C.sub.1-10 chain, to an immunoglobulin or an immunoglobulin fragment.The conjugates are useful in the treatment of cancer.
    Type: Grant
    Filed: June 23, 1986
    Date of Patent: July 4, 1989
    Assignee: Lilly Industries Limited
    Inventors: George J. Cullinan, George F. Rowland, Robin G. Simmonds
  • Patent number: 4845128
    Abstract: This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations.
    Type: Grant
    Filed: May 2, 1985
    Date of Patent: July 4, 1989
    Assignee: Eli Lilly and Company
    Inventors: Richard W. Harper, Gerald A. Poore, Brent J. Rieder
  • Patent number: 4845227
    Abstract: This invention provides azole derivatives, their pharmaceutical formulations, and their use in methods of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals.
    Type: Grant
    Filed: August 15, 1988
    Date of Patent: July 4, 1989
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. Hirsch, Charles D. Jones
  • Patent number: 4845110
    Abstract: There are provided anti-allergic pharmaceutical compounds of formula: ##STR1## in which n is 0, 1 or 2; R.sup.1 is a hydrocarbyl group containing 6 to 30 carbon atoms and optionally substituted with an optionally substituted phenyl group; R.sup.2 is (i) optionally optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.10 is hydrogen or C.sub.1-4 alkyl; and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: July 4, 1989
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, Alec Todd
  • Patent number: 4835159
    Abstract: The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists.
    Type: Grant
    Filed: August 24, 1988
    Date of Patent: May 30, 1989
    Assignee: Eli Lilly and Company
    Inventors: William L. Garbrecht, Gifford P. Marzoni, Pawel Fludzinski
  • Patent number: 4835181
    Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
    Type: Grant
    Filed: February 18, 1987
    Date of Patent: May 30, 1989
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson
  • Patent number: 4831145
    Abstract: This invention provides a process for preparing trans 2-aminopyrimido[4,5-g]quinolines employing novel intermediates.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: May 16, 1989
    Assignee: Eli Lilly and Company
    Inventors: Leland O. Weigel, Gilbert S. Staten
  • Patent number: 4820722
    Abstract: The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C.sub.4, D.sub.4 and E.sub.4 in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive amounts of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: F. Patrick Carr, Robert D. Dillard, Winston S. Marshall, Doris E. McCullough
  • Patent number: 4820723
    Abstract: The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive release or production of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof. Such conditions include an immediate hypersensitivity reaction of the type represented by asthma, or by shock or other adverse cardiovascular effects.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, Sandra K. Sigmund, Celia A. Whitesitt
  • Patent number: 4820713
    Abstract: Ketoalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: April 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: Gifford P. Marzoni, William L. Garbrecht
  • Patent number: 4801712
    Abstract: D-2-Alkyl(or phenyl)thio-6-n-alkylergolines or .+-.-2-alkyl(or phenyl)thio-4-dialkylaminotetrahydrobenz[c,d]indoles, dopamine D-1 antagonists.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: January 31, 1989
    Assignee: Eli Lilly and Company
    Inventors: Bennett C. Laguzza, Cynthia L. Nichols, Nicholas J. Bach
  • Patent number: 4801594
    Abstract: This invention provides azole derivatives, their pharmaceutical formulations, and their use in methods of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: January 31, 1989
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. Hirsch, Charles D. Jones
  • Patent number: 4801688
    Abstract: Immunoglobulin conjugates formed by reaction of an antineoplastic indole-dihydroindole vinca alkaloid containing a hydrazine group attached at C-3 or C-4 with an oxidized glycoprotein containing aldehyde groups.
    Type: Grant
    Filed: October 7, 1987
    Date of Patent: January 31, 1989
    Assignee: Eli Lilly and Company
    Inventors: Bennett C. Laguzza, Cynthia L. Nichols
  • Patent number: 4801735
    Abstract: Compounds are described of the following formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, at least one of R.sup.1 and R.sup.2 being C.sub.1-12 alkyl or C.sub.2-12 alkenyl; X.sup.1 and X.sup.2 are each hydrogen or a protecting group; and Y is(a) --(CH.dbd.CH).sub.n Z in which n is 1, 2 or 3 and Z is --CHO, --CH.sub.2 OH, --COR.sup.3, --(CH.sub.2).sub.m --COR.sup.3 or --(CH.sub.2).sub.p CH.dbd.CH(CH.sub.2).sub.q --COR.sup.3 in which m is an integer of 1 to 12, p is an integer of 1 to 4, q is an integer of 1 to 10 and R.sup.3 is (i) --OH or (ii) --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl, or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(b) --CH.dbd.NR.sup.6 in which R.sup.6 is (i) --OH, (ii) C.sub.1-12 alkyl optionally substituted by --OH, --COOH or --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.
    Type: Grant
    Filed: November 25, 1985
    Date of Patent: January 31, 1989
    Assignee: Lilly Industries Limited
    Inventors: Mark A. W. Finch, John R. Harris
  • Patent number: 4782063
    Abstract: The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: November 1, 1988
    Assignee: Eli Lilly and Company
    Inventors: William L. Garbrecht, Gifford P. Marzoni, Pawel Fludzinski
  • Patent number: 4777299
    Abstract: 1,3-Dialkylbenzenes are acylated and deprotected in a mixture of acetic or propionic acid and hydrobromic acid. The dihydroxyphenones thus produced are intermediates in the synthesis of leukotriene antagonists.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 11, 1988
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, Sandra K. Sigmund, Celia A. Whitesitt
  • Patent number: 4777298
    Abstract: Resorcinol is acylated in a mixture of acetic or propionic acid and hydrobromic acid. The dihydroxy acylbenzenes thus produced are intermediates in the synthesis of leukotriene antagonists.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 11, 1988
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, Sandra K. Sigmund, Celia A. Whitesitt
  • Patent number: 4774251
    Abstract: This invention provides a method of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals by administering certain amine derivatives.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: September 27, 1988
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. Hirsch, Harold M. Taylor
  • Patent number: 4769482
    Abstract: This invention provides novel alkane derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: September 6, 1988
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, John P. Verge
  • Patent number: 4767770
    Abstract: This invention provides a method of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals by administering certain amine derivatives. Pharmaceutical formulations of the compounds are also provided.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: August 30, 1988
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. Hirsch, Harold M. Taylor