Patents Represented by Attorney MaCharri R. Vorndran-Jones
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Patent number: 7259175Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethylType: GrantFiled: February 13, 2003Date of Patent: August 21, 2007Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Patent number: 6686365Abstract: The present invention provides a pharmaceutical composition comprising pemetrexed; at least one antioxidant selected from the group consisting of monothioglycerol, L-cysteine, and thioglycolic acid; and a pharmaceutically acceptable excipient. The pharmaceutical formulation is suitable for liquid parenteral administration.Type: GrantFiled: October 4, 2002Date of Patent: February 3, 2004Assignee: Eli Lilly and CompanyInventors: Bernd Ulrich Riebesehl, Jens Kemken
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Patent number: 6187798Abstract: The present invention provides aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: June 1, 1999Date of Patent: February 13, 2001Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Lone Jeppesen, John S. Ward
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Patent number: 6071900Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: March 22, 1999Date of Patent: June 6, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6043258Abstract: This invention relates to the use of xanomeline for the treatment of Disruptive Behavior Disorder and Attention Deficit Hyperactivity Disorder.Type: GrantFiled: December 16, 1998Date of Patent: March 28, 2000Assignee: Eli Lilly and CompanyInventors: Franklin P Bymaster, Harlan E Shannon
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Patent number: 6030966Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: July 28, 1999Date of Patent: February 29, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 5821371Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: October 13, 1998Assignee: Eli Lilly and ComanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5736544Abstract: The present invention provides methods for binding a 5-HT.sub.2B receptor in mammals using both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT.sub.2B related conditions. Finally, the invention provides an article of manufacture.Type: GrantFiled: March 25, 1996Date of Patent: April 7, 1998Assignee: Eli Lilly and CompanyInventors: James E. Audia, Marlene L. Cohen, Jaswant S. Gidda, David L. G. Nelson
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Patent number: 5629317Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: May 19, 1995Date of Patent: May 13, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen R. Baker, Jesus E. Carrera, Carlos L. Peteira, Concepcion P. Tercero
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Patent number: 5580900Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.Type: GrantFiled: November 30, 1994Date of Patent: December 3, 1996Assignee: Lilly Industries LimitedInventors: Barry P. Clark, John R. Harris
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Patent number: 5576435Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.Type: GrantFiled: May 19, 1995Date of Patent: November 19, 1996Assignee: Eli Lilly and CompanyInventors: Anita Melikian-Badalian, Paul L. Ornstein
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Patent number: 5574028Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering to the human an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein Z is a 5-membered heterocyclic ring as defined in the disclosure.Type: GrantFiled: October 31, 1994Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5574158Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.Type: GrantFiled: February 20, 1996Date of Patent: November 12, 1996Assignee: Lilly Industries LimitedInventors: Barry P. Clark, John R. Harris
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Patent number: 5574029Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein X R.sup.43, R.sup.44, R.sup.45 and R.sup.46 are defined in the disclosure.Type: GrantFiled: May 23, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5574169Abstract: The present invention provides an enantiomerically selective process and intermediates for preparing certain 4,5-disubstituted pyrazolidinones and intermediates which are useful for treating diseases of the central nervous system.Type: GrantFiled: February 16, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: William B. Blanchard, Thomas C. Britton, David L. Varie
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Patent number: 5574053Abstract: The present invention provides a method for treating anxiety in humans using a compound of the formula ##STR1## as described in the specification which modulates a muscarinic receptor.Type: GrantFiled: May 23, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5399565Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.Type: GrantFiled: November 12, 1993Date of Patent: March 21, 1995Assignee: Eli Lilly and CompanyInventors: Beverley Greenwood, David R. Helton, J. Jeffry Howbert, Steven J. Mitan, Kurt Rasmussen
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Patent number: 5399708Abstract: The present invention provides an enantiomerically selective process and intermediates for preparing certain 4,5-disubstituted pyrazolidinones and intermediates which are useful for treating diseases of the central nervous system.Type: GrantFiled: November 12, 1993Date of Patent: March 21, 1995Assignee: Eli Lilly and CompanyInventors: William B. Blanchard, Thomas C. Britton, David L. Varie
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Patent number: 5338735Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.Type: GrantFiled: August 12, 1993Date of Patent: August 16, 1994Assignee: Lilly Industries LimitedInventors: John Fairhurst, David E. Tupper
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Patent number: 5334725Abstract: The present invention provides a novel process for preparing a 2-(aminomethyl)-4-thiazolemethanol. The compounds produced by the process of the present invention are useful for synthesizing anti-ulcer compounds such as Nizatidine.Type: GrantFiled: June 14, 1993Date of Patent: August 2, 1994Assignee: Eli Lilly and CompanyInventor: Kenneth P. Moder