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
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
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.
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.
Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
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
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
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.
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.
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.
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
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
Abstract: This invention provides a method of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals by administering certain amine derivatives.
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.
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.