Patents Represented by Attorney, Agent or Law Firm Paul R. Cantrell
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Patent number: 5614525Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control off parasites in vertebrate animals.Type: GrantFiled: May 4, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5614639Abstract: The present invention provides processes for preparing 2-substituted benzo[b]thiophene compounds, some of which are useful as intermediates for preparing pharmaceutically-active compounds and others which are useful, inter alia, for the treatment of osteoporosis in postmenopausal women.Type: GrantFiled: March 31, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventors: Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
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Patent number: 5607850Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides said phthalyl amidase, means for producing it by culturing the natural organism from which the activity was identified, and methods for using said phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides.Type: GrantFiled: May 22, 1995Date of Patent: March 4, 1997Assignee: Eli Lilly and CompanyInventors: Barbara S. Briggs, Milton J. Zmijewski, Jr.
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Patent number: 5596122Abstract: The present invention is directed to disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: April 25, 1995Date of Patent: January 21, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5578713Abstract: The disclosure relates to a new process for the synthesis of the macrolide antibiotic dirithromycin in crystalline form. The process is carried out in a single reaction vessel whereby an acetal dissolved in acetonitrile, in the presence of an acid catalyst, is hydrolyzed to the related hemiacetal which then reacts directly with erythromycylamine to form crystalline dirithromycin.Type: GrantFiled: July 20, 1993Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventor: John M. McGill, III
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Patent number: 5574020Abstract: An aqueous, injectable, sustained release tilmicosin formulation comprises 250-350 mg/ml of tilmicosin and 250 mg/ml of propylene glycol, and has a pH adjusted to 6.Type: GrantFiled: January 13, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: Paul R. Klink, Thomas D. Thomson
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Patent number: 5567828Abstract: The present invention provides compounds with nitrogen-containing non-basic side chains of formula II ##STR1## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo;W is CHOH, C(O), or CH.sub.2 ;Y is (CH.sub.2).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);V is S, 0, or CH.sub.2 CH.sub.2 ;n is 1, 2, or 3; andAr is optionally substituted phenyl.The present invention also provides pharmaceutical compositions containing compounds of formula II, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.Type: GrantFiled: June 7, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventor: Jeffrey A. Dodge
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Patent number: 5559006Abstract: "A method for selectively deactivating catalase while retaining D-amino acid oxidase activity is disclosed. The catalase and oxidase are both present in whole cells or a cell-free extract. The method comprises combining the whole cells or the cell-free extract with a basic solution at a pH between about 11 and about 12. The catalase activity is eliminated and the oxidase activity is unaffected. This results in the production of a solution which contains oxidase activity but no catalase activity. The whole cells and cell-free extract are preferably from Triginopsis variabilis.Type: GrantFiled: February 22, 1995Date of Patent: September 24, 1996Assignee: Eli Lilly and CompanyInventor: Jeffrey T. Vicenzi
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Patent number: 5552386Abstract: New polyether antibiotic A82810, its acyl and alkyl ester, acyl ester and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A82810 by culture of Actinomodura fibrosa sp. nov. NRRL 18348 and synergistic compositions of the A82810 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and metichlorpindol are also provided.Type: GrantFiled: April 2, 1993Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventors: Robert L. Hamill, Raymond C. Yao
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Patent number: 5543497Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides DNA compounds encoding the phthalyl amidase enzyme and methods for expressing such compounds. The present invention also provides recombinant DNA vectors encoding phthalyl amidase and host cells transformed with these DNA vectors.Type: GrantFiled: May 22, 1995Date of Patent: August 6, 1996Assignee: Eli Lilly and CompanyInventors: Stephen W. Queener, Joseph M. Zock
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Removal of phthalyl groups from amides and esters using an amidase isolated from Xanthobacter Agilis
Patent number: 5532149Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides a phthalyl amidase, a method for producing it by culturing the natural organism from which the activity was identified, and methods for using the phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides. The enzyme is isolated from Xanthobacter agilis.Type: GrantFiled: May 22, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: Barbara S. Briggs, Milton J. Zmijewski, Jr. -
Patent number: 5532161Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides 2 phthalyl amidase, 2 method for producing it by culturing the natural organism from which the activity was identified, and methods for using the phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides. The ezyme is isolated from Xanthobacter agilis.Type: GrantFiled: May 22, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: Barbara S. Briggs, Milton J. Zmijewski, Jr.
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Patent number: 5514778Abstract: The present invention provides a group of novel compounds that inhibit the proteolytic activity of 3C proteases which are found in picornaviruses, particularly rhinoviruses. In picornaviruses the RNA genome is translated into a single large viral polyprotein precursor. The precursor demonstrates auto-proteolytic activity, cleaving itself into mature viral gene products. Therefore, compounds of the current invention are particularly useful in treating picornaviral infections by interrupting the processing of the viral gene products into mature and infectious viral particles. The current invention also provides a novel process the preparation of compounds of the current invention. The process entails the selective reduction of an imide intermediate representing a marked improvement over processes known in the art for making peptidyl-aldehydes.Type: GrantFiled: July 1, 1993Date of Patent: May 7, 1996Assignee: Eli Lilly and CompanyInventors: Marlys Hammond, Stephen W. Kaldor
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Patent number: 5494670Abstract: In a method of treating ketosis in an animal during pregnancy or lactation, such as toxaemia of pregnancy or fat cow syndrome, the amount or activity of somatotropin in the blood is increased while administering glucose or a glucose precursor to the affected animal.Type: GrantFiled: July 21, 1993Date of Patent: February 27, 1996Assignee: Lilly Industries LimitedInventor: John D. I. Wilkinson
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Patent number: 5453504Abstract: A method for preparing a new class of protected amino intermediates is provided which utilizes reaction of an imido protected primary amine with a secondary amine. The intermediates thus provided are suitably protected for nucleophilic functionalization on the residue of the primary amine. The desired imido protected amine thus derivatized may be regenerated using acid. Further provided are methods for resolving racemic primary amines. Also provided are .beta.-lactam intermediates protected with the new amino protecting group which are useful in the preparation of .beta.-lactam antibiotics.Type: GrantFiled: September 21, 1994Date of Patent: September 26, 1995Assignee: Eli Lilly and CompanyInventor: Leland O. Weigel
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Patent number: 5453503Abstract: 7.beta.-Amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are provided via cyclization of cis-3-(substituted amino)-1-(2-substituted 2-oxoethyl)-4-substituted azetidinones. The 7.beta.-amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are useful chiral intermediates to .beta.-lactam antibiotics.Type: GrantFiled: August 9, 1993Date of Patent: September 26, 1995Assignee: Eli Lilly and CompanyInventors: James Aikins, John P. Gardner, Billy G. Jackson, John R. Rizzo, Eddie V. Tao
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Patent number: 5451522Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides DNA compounds encoding the phthalyl amidase enzyme and methods for expressing such compounds. The present invention also provides recombinant DNA vectors encoding phthalyl amidase and host cells transformed with these DNA vectors.Type: GrantFiled: July 15, 1994Date of Patent: September 19, 1995Assignee: Eli Lilly and CompanyInventors: Stephen W. Queener, Joseph M. Zock
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Patent number: 5445959Abstract: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides said phthalyl amidase, means for producing it by culturing the natural organism from which the activity was identified, and methods for using said phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides.Type: GrantFiled: July 15, 1994Date of Patent: August 29, 1995Assignee: Eli Lilly and CompanyInventors: Barbara S. Briggs, Milton J. Zmijewski, Jr.
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Patent number: 5424203Abstract: A method for selectively deactivating catalase while retaining D-amino acid oxidase activity is disclosed. The catalase and the oxidase are both present in whole cells or a cell-free extract. The method comprises combining the whole cells or the cell-free extract with a basic solution at a pH between about 11 and about 12 for a time of about 1 hour and 45 minutes to about 2 hours. The catalase activity is eliminated and the oxidase activity is uneffected. This results in the production of a solution which contains the oxidase and which has no catalase activity. The pH of the solution containing the oxidase is then lowered to provide a D-amino acid oxidase capable of enzymatic oxidation of cephalosporin C to glutaryl-7-ACA in high yields. The whole cells and cell-free extract are preferrably from Triginopsis variablilis.Type: GrantFiled: March 11, 1994Date of Patent: June 13, 1995Assignee: Eli Lilly and CompanyInventor: Jeffrey T. Vicenzi
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Patent number: 5422426Abstract: A method is disclosed for the rapid synthesis of very large numbers of peptides which can be integrated with the screening of these peptides as heterogeneous mixtures to identify the specific peptides which demonstrate biological activity using a small number of coupling steps.Type: GrantFiled: May 25, 1993Date of Patent: June 6, 1995Assignee: Eli Lilly and CompanyInventors: Richard D. DiMarchi, Paul D. Gesellchen, Rebecca A. Owens