Patents Assigned to Eli Lilly and Company Limited
-
Patent number: 6329366Abstract: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.Type: GrantFiled: November 18, 1999Date of Patent: December 11, 2001Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles
-
Patent number: 6166040Abstract: Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.Type: GrantFiled: May 11, 1999Date of Patent: December 26, 2000Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles, William Martin Owton, Colin William Smith
-
Patent number: 6075039Abstract: A pharmaceutical compound of the formula ##STR1## in which X is --CR'R"-- or --C(O)-- where R' and R" are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, Y is oxygen or sulphur, R.sup.1, R.sup.2 and R.sup.7 are each selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, nitro, cyano, amino, phenyl, phenoxy, benzyl, benzyloxy, acylamino, C.sub.1-4 alkylsulphonylamino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, carboxamido, sulphonamido, hydroxy, methylenedioxy, carboxy, and heteroaryl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, n, m and p are each 0, 1, 2 or 3;or a salt or ester thereof.Type: GrantFiled: June 24, 1997Date of Patent: June 13, 2000Assignee: Eli Lilly and Company LimitedInventors: Peter Thaddeus Gallagher, Martin Victor Miles, William Martin Owton, Colin William Smith
-
Patent number: 6054448Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
-
Patent number: 6034078Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.Type: GrantFiled: July 1, 1997Date of Patent: March 7, 2000Assignees: Eli Lilly and Company Limited, Eli Lilly and CompanyInventors: John Fairhurst, Terrence Michael Hotten, David Edward Tupper, David Taiwai Wong
-
Patent number: 6008216Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.Type: GrantFiled: July 24, 1998Date of Patent: December 28, 1999Assignee: Eli Lilly And Company and LimitedInventors: Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
-
Patent number: 5929072Abstract: A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form an alkylene link of formula --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group,R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,the dotted line represents an optional double bond, andthe fluorine atom is attached at the 6 or 7-position;and salts and esters thereof.Type: GrantFiled: August 21, 1998Date of Patent: July 27, 1999Assignee: Eli Lilly and Company LimitedInventor: John Fairhurst
-
Patent number: 5906985Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.Type: GrantFiled: August 21, 1997Date of Patent: May 25, 1999Assignees: Eli Lilly and Company Limited, Lilly, S.A.Inventors: Stephen Richard Baker, Almudena Rubio Esteban, John Goldsworthy, Concepcion Pedregal Tercero
-
Patent number: 5891899Abstract: A pharmaceutical compound of the formula: ##STR1## in which A is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OPO(OH)OR'B is a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylene,R.sup.1 is hydrogen, hydroxyl, halo or group of the formula A--B--,X is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, C.sub.2-6 alkynylene or C.sub.1-6 alkylene linked through --O--, --S-- or --NR"-- to Y, where R" is hydrogen or C.sub.1-6 alkyl,andY is (1) ##STR2## where p is and Z is ##STR3## or (2) ##STR4## and salts and esters thereof.Type: GrantFiled: December 15, 1997Date of Patent: April 6, 1999Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
-
Patent number: 5863947Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.Type: GrantFiled: May 9, 1997Date of Patent: January 26, 1999Assignee: Eli Lilly and Company LimitedInventors: Stephen Richard Baker, Barry Peter Clark, John Goldsworthy, John Richard Harris
-
Patent number: 5817657Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders relating to the use of psychoactive substances.Type: GrantFiled: November 13, 1996Date of Patent: October 6, 1998Assignees: Eli Lilly and Company, Eli Lilly and Company LimitedInventors: Charles M. Beasley, Jr., Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
-
Patent number: 5817656Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of mental disorders.Type: GrantFiled: November 13, 1996Date of Patent: October 6, 1998Assignees: Eli Lilly and Company, Eli Lilly and Company LimitedInventors: Charles M. Beasley, Jr., Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
-
Patent number: 5817655Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno -?2,3-b!?1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.Type: GrantFiled: November 13, 1996Date of Patent: October 6, 1998Assignees: Eli Lilly and Company, Eli Lilly and Company LimitedInventors: Jiban Kumar Chakrabarti, Terrence Micharl Hotten, David Edward Tupper
-
Patent number: 5773448Abstract: A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.Type: GrantFiled: April 14, 1997Date of Patent: June 30, 1998Assignee: Eli Lilly and Company LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith