Patents Represented by Attorney Nancy J. Harrison
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Patent number: 4293483Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is an N-alkanoyl amino acyl group of the formula ##STR2## wherein: W is a divalent aminoacyl radical of the formula: ##STR3## wherein A is C.sub.1 -C.sub.10 alkylene or C.sub.5 -C.sub.6 cycloalkylene; ##STR4## wherein R.sup.3 is hydroxymethyl, hydroxyethyl, mercaptomethyl, mercaptoethyl, methylthioethyl, 2-thienyl, 3-indole-methyl, phenyl, benzyl, or substituted phenyl or substituted benzyl in which the benzene ring thereof is substituted with chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkylthio, carbamyl, or C.sub.1 -C.sub.3 alkylcarbamyl; ##STR5## wherein X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl, or C.sub.1 -C.sub.3 alkylcarbamyl; ##STR6## wherein X.sup.1 is chloro, bromo, or iodo; ##STR7## wherein B is a divalent radical of the formula: --(CH.sub.2).sub.n --, wherein n is an integer from 1 to 3; --CH.dbd.CH--; --CH.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4293488Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is an N-alkanoyl amino acyl group of the formula ##STR2## wherein: W is a divalent aminoacyl radical of the formula: ##STR3## wherein A is C.sub.1 -C.sub.10 alkylene or C.sub.5 -C.sub.6 cycloalkylene; ##STR4## wherein R.sup.3 is hydroxymethyl, hydroxyethyl, mercaptomethyl, mercaptoethyl, methylthioethyl, 2-thienyl, 3-indolemethyl, phenyl, benzyl, or substituted phenyl or substituted benzyl in which the benzene ring thereof is substituted with chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkylthio, carbamyl, or C.sub.1 -C.sub.3 alkylcarbamyl; ##STR5## wherein X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl, or C.sub.1 -C.sub.3 alkylcarbamyl; ##STR6## wherein X.sup.1 is chloro, bromo, or iodo; ##STR7## wherein B is a divalent radical of the formula: --(CH.sub.2).sub.n --, wherein n is an integer from 1 to 3; ##STR8## and R.sup.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4293486Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## wherein A is divalent oxygen, sulfur, sulfinyl, or sulfonyl; A.sup.1 is divalent oxygen, sulfur, sulfinyl, sulfonyl or --NH--; X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl or C.sub.1 -C.sub.3 alkylcarbamyl; X.sup.1 is chloro, bromo, or iodo; R.sup.2 is hydrogen, C.sub.1 -C.sub.18 alkyl or C.sub.2 -C.sub.18 alkenyl; W is C.sub.1 -C.sub.10 alkylene or C.sub.2 -C.sub.10 alkenylene; m, n and p are 0 or 1, but if m=0, n must=0; provided: that the sum of the carbon atom in the R.sup.2 and W groups must be greater than 4 but cannot exceed 21; that when X is mercapto, A and A.sup.1 cannot be sulfinyl or sulfonyl; and that when A and A.sup.1 are sulfinyl or sulfonyl, they must be in equal oxidation states.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4293484Abstract: Compounds of the formula ##STR1## wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl and R.sup.1 is a group of the formula: ##STR2## wherein A is divalent oxygen, sulfur, sulfinyl, or sulfonyl; A.sup.1 is divalent oxygen, sulfur, sulfinyl, sulfonyl or --NH--; X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl or C.sub.1 -C.sub.3 alkylcarbamyl; X.sup.1 is chloro, bromo or iodo; R.sup.2 is hydrogen, C.sub.1 -C.sub.18 alkyl or C.sub.2 -C.sub.18 alkenyl; W is C.sub.1 -C.sub.10 alkylene or C.sub.2 -C.sub.10 alkenylene; m, n and p are 0 or 1, but if m=0, n must =0; provided: that the sum of the carbon atoms in the R.sup.2 and W groups must be greater than 4 but cannot exceed 21; that when X is mercapto, A and A.sup.1 cannot be sulfinyl or sulfonyl; and that when A and A.sup.1 are sulfinyl or sulfonyl, they must be in equal oxidation states.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4293489Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## wherein A is divalent oxygen, sulfur, sulfinyl, or sulfonyl; A.sup.1 is divalent oxygen, sulfur, sulfinyl, sulfonyl or --NH--; X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 --C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl or C.sub.1 -C.sub.3 alkylcarbamyl; X.sup.1 is chloro, bromo or iodo; R.sup.2 is hydrogen, C.sub.1 -C.sub.18 alkyl or C.sub.2 -C.sub.18 alkenyl; W is C.sub.1 -C.sub.10 alkylene or C.sub.2 -C.sub.10 alkenylene; m, n and p are 0 or 1, but if m=0, n must=0; provided: that the sum of the carbon atoms in the R.sup.2 and W groups must be greater than 4 but cannot exceed 21; that when X is mercapto. A and A.sup.1 cannot be sulfinyl or sulfonyl; and that when A and A.sup.1 are sulfinyl or sulfonyl, they must be in equal oxidation states.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4293482Abstract: A-30912A nucleus, which is prepared by enzymatic deacylation of an antibiotic selected from A-30912 factor A, tetrahydro-A-30912A, and aculeacin A using an enzyme produced by the Actinoplanaceae, preferably by Actinoplanes utahensis. A-30912A nucleus and salts thereof are useful intermediates to prepare new semi-synthetic antifungal agents.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4293490Abstract: A-30912H-type nuclei of formula 1, which are prepared by enzymatic deacylation of an antibiotic having formula 2 using an enzyme produced by the Actinoplanaceae, preferably by Actinoplanes utahensis. A-30912H-type nuclei and salts thereof are useful intermediates for preparing new semi-synthetic anti-fungal agents.Type: GrantFiled: August 25, 1980Date of Patent: October 6, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4289692Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## wherein A is divalent oxygen, sulfur, sulfinyl, or sulfonyl; A.sup.1 is divalent oxygen, sulfur, sulfinyl, sulfonyl or --NH--; X is hydrogen, chloro, bromo, iodo, nitro, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, mercapto, C.sub.1 -C.sub.3 alkylthio, carbamyl or C.sub.1 -C.sub.3 alkylcarbamyl; X.sup.1 is chloro, bromo or iodo; R.sup.2 is hydrogen, C.sub.1 -C.sub.18 alkyl or C.sub.2 -C.sub.18 alkenyl; W is C.sub.1 -C.sub.10 alkylene or C.sub.2 -C.sub.10 alkenylene; m, n and p are 0 or 1, but if m=0, n must=0; provided: that the sum of the carbon atoms in the R.sup.2 and W groups must be greater than 4 but cannot exceed 21; that when X is mercapto, A and A.sup.1 cannot be sulfinyl or sulfonyl; and that when A and A.sup.1 are sulfinyl or sulfonyl, they must be in equal oxidation states.Type: GrantFiled: August 25, 1980Date of Patent: September 15, 1981Assignee: Eli Lilly and CompanyInventor: Manuel Debono
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Patent number: 4288549Abstract: The microorganism Aspergillus nidulans var. roseus NRRL 11440 and the method of producing the A-30912 antibiotics by submerged aerobic fermentation of this microorganism to give the A-42355 antibiotic complex. A-30912 factors A, B, D, and H are separated from the A-42355 complex by chromatography. The A-42355 complex and A-30912 factors A, B, D, and H are antifungal agents.Type: GrantFiled: March 3, 1980Date of Patent: September 8, 1981Assignee: Eli Lilly and CompanyInventors: LaVerne D. Boeck, Ralph E. Kastner
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Patent number: 4287302Abstract: Cultivation of Streptomyces chartreusis NRRL 11407 in the presence of antibiotic A23187 methyl ester produces 16-hydroxy A23187 methyl ester, 16-hydroxy-N-demethyl A23187 methyl ester, and N-demethyl A23187 methyl ester. Hydrolysis of the products affords the corresponding free acids which form dimeric complexes with divalent cations.Type: GrantFiled: July 30, 1980Date of Patent: September 1, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4287120Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is C.sub.6 -C.sub.24 alkyl or C.sub.6 -C.sub.24 alkenyl, have antifungal activity.Type: GrantFiled: August 25, 1980Date of Patent: September 1, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4252898Abstract: Antibiotic compounds of the formula: ##STR1## wherein R' is ##STR2## or --CH.sub.2 OH, and the non-toxic pharmaceutically acceptable acid addition salts thereof, are produced by culturing Streptomyces flocculus NRRL 11459. Techniques for isolating the compounds are also described. Cirramycin A.sub.1 and cirramycin B are coproduced.Type: GrantFiled: May 23, 1979Date of Patent: February 24, 1981Assignee: Eli Lilly and CompanyInventors: Stephen M. Nash, Kay F. Koch, Marvin M. Hoehn
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Patent number: 4247542Abstract: A-40104 antibiotic complex, comprising active factors A, B, C, and D, produced by submerged aerobic fermentation of Clitopilus pseudo-pinsitus. Individual factors A, B, and C have been isolated. A-40104 factor C is the known antibiotic pleuromutilin. A-40104 factors A and B are novel antibiotics related to pleuromutilin. A-40104 factor A, the major new factor, is the D-xylose acetal derivative of pleuromutilin. A-40104 factors A and B, their 19,20-dihydro derivatives and the per(C.sub.2 -C.sub.6)alkanoyl derivatives of factors A and B and of their 19,20-dihydro derivatives are active against gram-positive and gram-negative bacteria, anaerobic bacteria, and Mycoplasma.Type: GrantFiled: June 22, 1978Date of Patent: January 27, 1981Assignee: Eli Lilly and CompanyInventors: Karl H. Michel, Calvin E. Higgens
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Patent number: 4247703Abstract: Cultivation of Streptomyces chartreusis NRRL 11407 in the presence of antibiotic A23187 methyl ester produces 16-hydroxy A23187 methyl ester, 16-hydroxy-N-demethyl A23187 methyl ester, and N-demethyl A23187 methyl ester. Hydrolysis of the products affords the corresponding free acids which form dimeric complexes with divalent cations.Type: GrantFiled: December 20, 1978Date of Patent: January 27, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4237225Abstract: Tunicamycin is co-produced with antibiotic A-23187 by the cultivation of Streptomyces chartreusis NRRL 3882. Methods of recovering tunicamycin and for separating and isolating individual factors A, B, C, and D from tunicamycin complex are described.Type: GrantFiled: December 1, 1978Date of Patent: December 2, 1980Assignee: Eli Lilly and CompanyInventor: Robert L. Hamill
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Patent number: 4234684Abstract: An improved method of preparing mycophenolic acid glucoside which comprises contacting mycophenolic acid with glucose in an aqueous medium in the presence of a glucosylating enzyme selected from that produced by Streptomyces candidus NRRL 5449 and that produced by Streptomyces aureofaciens NRRL 2209 until mycophenolic acid glucoside is formed.Type: GrantFiled: December 11, 1979Date of Patent: November 18, 1980Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, John G. Whitney
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Patent number: 4228293Abstract: Iodo-A-23187 derivatives, prepared by reaction of antibiotic A-23187 with iodine monochloride, and salts thereof, which are (1) useful biochemical tools for the study of transport of ions in cellular systems and (2) useful chemical tools for removal of recovery of ions.Type: GrantFiled: October 11, 1978Date of Patent: October 14, 1980Assignee: Eli Lilly and CompanyInventors: R. Michael Molloy, Manuel Debono
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Patent number: 4227003Abstract: Bromo-A-23187 derivatives, prepared by reaction of antibiotic A-23187 with pyridinium hydrobromide perbromide and salts thereof, which are (1) useful biochemical tools for the study of transport of ions in cellular systems, and (2) useful chemical tools for removal and recovery of ions.Type: GrantFiled: October 11, 1978Date of Patent: October 7, 1980Assignee: Eli Lilly and CompanyInventors: Manuel Debono, R. Michael Molloy
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Patent number: 4227002Abstract: Halo-A-23187 derivatives, prepared by reaction of antibiotic A-23187 with an N-halo-type halogenating agent, and salts thereof, which are (1) useful biochemical tools for the study of transport of ions in cellular systems, (2) useful chemical tools for removal and recovery of ions, and (3) potential cardiotonic agents.Type: GrantFiled: October 11, 1978Date of Patent: October 7, 1980Assignee: Eli Lilly and CompanyInventors: Donner F. Babcock, Charles M. Deber, Manuel Debono, R. Michael Molloy, Douglas R. Pfeiffer
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Patent number: 4222946Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 5-membered ring containing a single heteroatom, which may be oxygen, or sulphur, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.Type: GrantFiled: January 12, 1979Date of Patent: September 16, 1980Assignee: Lilly Industries, LimitedInventors: Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann