Abstract: 17.beta.-hydroxywortmannin and certain of its analogs are inhibitors of phosphatidylinositol 3-kinase. The compounds are particularly useful for inhibiting phosphatidylinositol 3-kinase in mammals and for treating phosphatidylinositol 3-kinase-dependent conditions, especially neoplasms, in mammals.
Type:
Grant
Filed:
August 25, 1993
Date of Patent:
April 2, 1996
Assignee:
Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Jeffrey A. Dodge, Chris J. Vlahos
Abstract: This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: ##STR1## and their use as LTD.sub.4 antagonists.
Abstract: Selected acid functional 6-azaindole type derivatives effective as thromboxane synthase inhibitors having the formula (II): ##STR1## where n is an integer from zero to 3, m is an integer from zero to 2, R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.
Type:
Grant
Filed:
January 31, 1994
Date of Patent:
November 21, 1995
Assignee:
Eli Lilly and Company
Inventors:
Joseph A. Jakubowski, Alan D. Palkowitz, Sandra K. Sigmund
Abstract: Pergolide is produced from 8,9-dihydroelymoclavine by a one-pot process in which it is reacted successively with 1-iodopropane, with a sulfonyl halide, and with an alkali metal thiomethoxide without isolation of intermediate products.
Abstract: Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.
Type:
Grant
Filed:
November 1, 1994
Date of Patent:
October 31, 1995
Assignee:
Eli Lilly and Company
Inventors:
S. Richard Baker, Robert D. Dillard, Paul E. Floreancig, J. Scott Sawyer, Michael J. Sofia
Abstract: This invention provides 6-substituted-4-(amino or substituted amino)tetrahydrobenz[c,d]indole serotonin agonists useful in treating a variety of conditions associated with serotonin function.
Abstract: A compound having pharmaceutical activity, of the formula ##STR1## in which A is hydrogen or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 0 or 1 to 4, R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl and R.sup.3 is --CN, --COOH, tetrazolyl or --CONHSO.sub.2 R.sup.4 where R.sup.4 is optionally substituted phenyl, and ##STR2## where R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x, R.sup.1, R.sup.2 and R.sup.3 are as defined above, and R.sup.7 is hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 1 to 4, and R.sup.1, R.sup.2 and R.sup.3 are as defined above;provided that when A is hydrogen at least one of R.sup.5, R.sup.6 and R.sup.7is --(CR.sup.1 R.sup.2).sub.x R.sup.3, and provided that when ##STR3## A is --(CR.sup.1 R.sup.2).sub.x R.sup.3 and x is 1 to 4 then R.sup.3 is --CONHSO.sub.2 R.sup.4 ;and salts and esters thereof.
Abstract: This invention provides novel benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: This invention provides 1,2,4-trioxygenated benzene derivatives which are leukotriene B.sub.4 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 certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Type:
Grant
Filed:
December 10, 1992
Date of Patent:
June 28, 1994
Assignee:
Eli Lilly and Company
Inventors:
Robert D. Dillard, J. Scott Sawyer, Michael J. Sofia
Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.
Type:
Grant
Filed:
February 7, 1992
Date of Patent:
March 15, 1994
Assignee:
Eli Lilly and Company
Inventors:
Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
Abstract: This invention relates to N-hydroxy-N-[3-[2-(4'-halophenylthio)phenyl]prop-2-enyl]ureas, formulations containing those compounds and methods of using such compounds as 5-lipoxygenase inhibiting agents.
Type:
Grant
Filed:
April 8, 1992
Date of Patent:
February 1, 1994
Assignee:
Eli Lilly and Company
Inventors:
Gary A. Hite, Edward D. Mihelich, David W. Snyder, Tulio Suarez
Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C.sub.1-4 alkyl, aldehydo, --CH.sub.2 Z, --CH.dbd.CH--Z or --CH.sub.2 CH.sub.2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R.sup.2 is halo, nitrile, an optionally protected acid group or --CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or C.sub.1-4 alkyl substituted by --CONR.sup.7 R.sup.8 or an optionally protected acid group; R.sup.5 is ##STR2## where W is --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --O-- or --S--, R.sup.9 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl, and R.sup.10 is hydrogen, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl; R.sup.6 is hydrogen or C.sub.
Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: Novel s-triazine compounds containing at least one N,N-bis(alkoxy or hydroxyalkoxy-carbonyl-amino C.sub.2 -C.sub.10 alkyl) amino substituent function in self-condensation and as cross-linkers for compounds containing active hydrogen groups. The compositions cure to coatings with excellent properties, especially corrosion resistance, humidity resistance, abrasion resistance and flexibility. The coatings have excellent exterior durability.
Abstract: The binder composition of this invention contains a beta-hydroxy urethane functional material and a polycarboxylic acid. Coated glass fibers are prepared by contacting said fibers with the binder composition of the invention and thereafter curing the composition. This invention is also an improved method of treating glass fibers by contacting them with the improved binder composition of the invention.
Type:
Grant
Filed:
June 8, 1989
Date of Patent:
April 28, 1992
Assignee:
American Cyanamid Company
Inventors:
Gerald J. Guerro, William A. Henderson, Jr., Balwant Singh
Abstract: Novel rigid polyurethane and/or polyisocyanurate foams are disclosed which have fine cell structure, low K-factor, and flame retardance. These foams are prepared by the reaction of a polyisocyanate with heterocyclic nitrogen containing polybeta-hydroxy urethane functional polyols which act as chemically bound flame retardants. Also disclosed are novel modified poly-beta-hydroxyalkyl carbamylalkylated heterocyclic nitrogen containing polyols useful for the formation of rigid foams.
Type:
Grant
Filed:
January 14, 1991
Date of Patent:
April 7, 1992
Assignee:
American Cyanamid Company
Inventors:
Harold Porosoff, Balwant Singh, Kurt C. Frisch
Abstract: Novel beta-hydroxyalkylcarbamylmethyl aminotriazines function in self-condensation and as cross-linkers for amino resins and also compounds containing active hydrogen groups. The compositions cure to coatings with excellent properties, and they can be used as binders for fillers such as insulating glass and foundry sand.
Abstract: Novel alkylcarbamylmethyl aminotriazines self-cure and also function as crosslinkers for compounds containing active hydrogen groups. When the active hydrogen-containing compounds are hydroxylated polymers, coatings are provided with exceptional resistance to detergent and salt-spray exposure and improved abrasion resistance. The novel aminotriazines also can be combined with fillers as binders which when cured provide shaped articles of manufacture, such as insulation and foundry core molds.
Abstract: Novel triisocyanato triazines and carbamoyl triazine derivatives thereof are disclosed. These compounds will self-cure and also function as crosslinkers for compounds containing active hydrogen groups. When the active hydrogen-containing compounds are hydroxylated polymers, environmentally-resistant coatings are provided.