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61. 发明专利

CA2553381A1 COMPOSITIONS FOR LOCALIZED THERAPY OF THE EYE, COMPRISING PREFERABLY TRIAMCINOLONE ACETONIDE AND HYALURONIC ACID 未知
公开(公告)号：CA2553381A1
公开(公告)日：2005-08-11
申请号：CA2553381
申请日：2005-01-14
申请人： ALLERGAN INC
发明人： HUGHES PATRICK M , OLEJNIK OREST , WHITCUP SCOTT M , BURKE JAMES A
IPC分类号： A61K9/00 , A61K9/10 , A61K9/14 , A61K31/00 , A61K47/36
摘要： Compositions, and methods of using such compositions, useful for injection into the posterior segments of human or animal eyes are provided. Such compositions include small particles of a poorly soluble therapeutic agent that facilitates formation of concentrated regions of the therapeutic agent in the retinal pigmented epithelium of an eye. The particles are formed by combining a therapeutic agent with an ophthalmically acceptable polymer component. The particles have sizes less than about 3000 nanometers, and in some cases, less than about 200 nanometers. One example of a composition includes particles of triamcinolone acetonide and hyaluronic acid have a siz e less than about 3000 nanometers.

62. 发明专利

DK1036065T3 未知
公开(公告)号：DK1036065T3
公开(公告)日：2004-08-30
申请号：DK98962883
申请日：1998-12-03
申请人： ALLERGAN INC
发明人： CHOW KEN , GIL DANIEL W , HARCOURT DALE A , GARST MICHAEL E , WHEELER LARRY A , MUNK STEPHEN A , BURKE JAMES A
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4725 , A61K31/497 , A61P5/00 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/06 , A61P43/00 , C07D233/06 , C07D233/54 , C07D233/56 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Coumpounds having adrenergic activity which are selective agonists for one or both of the alpha 2B and alpha 2C adrenoceptor receptor subtypes in preference to the alpha 2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R , wherein R is H or lower alkyl, but R is absent when the bond between X and the ring represented by formula (a) is a double bond; Y is O, N, S, (CR 2)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y CH2-, wherein Y is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R , R or R is bound to a saturated carbon atom and x is 2 when R , R or R is bound to a saturated carbon atom; R is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R2 may be oxo; R3 and R4 are, each, H, lower alkyl, hydroxy, lower alkoxy, or phenyl or, together, are -(C(R )x)z-; -Y (C(R )x)z'-; -Y (C(R )x)yY -; -(C(R )x)-Y -(C(R )x)-; -(C(R )x)-Y -(C(R )x)-(C(R )x)- and -Y -(C(R )x)-Y -(C(R )x)- wherein z is an integer of from 3 to 5, z' is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects.

64. 发明专利

AT266643T 未知
公开(公告)号：AT266643T
公开(公告)日：2004-05-15
申请号：AT98962883
申请日：1998-12-03
申请人： ALLERGAN INC
发明人： CHOW KEN , GIL DANIEL W , BURKE JAMES A , HARCOURT DALE A , GARST MICHAEL E , WHEELER LARRY A , MUNK STEPHEN A
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4725 , A61K31/497 , A61P5/00 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/06 , A61P43/00 , C07D233/06 , C07D233/54 , C07D233/56 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Coumpounds having adrenergic activity which are selective agonists for one or both of the alpha 2B and alpha 2C adrenoceptor receptor subtypes in preference to the alpha 2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R , wherein R is H or lower alkyl, but R is absent when the bond between X and the ring represented by formula (a) is a double bond; Y is O, N, S, (CR 2)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y CH2-, wherein Y is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R , R or R is bound to a saturated carbon atom and x is 2 when R , R or R is bound to a saturated carbon atom; R is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R2 may be oxo; R3 and R4 are, each, H, lower alkyl, hydroxy, lower alkoxy, or phenyl or, together, are -(C(R )x)z-; -Y (C(R )x)z'-; -Y (C(R )x)yY -; -(C(R )x)-Y -(C(R )x)-; -(C(R )x)-Y -(C(R )x)-(C(R )x)- and -Y -(C(R )x)-Y -(C(R )x)- wherein z is an integer of from 3 to 5, z' is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects.

65. 发明专利

CZ20032471A3 Compounds exhibiting activity specifically aimed at alpha 2B or 2B/2C adrenergic receptors and treatment methods 未知
公开(公告)号：CZ20032471A3
公开(公告)日：2004-02-18
申请号：CZ20032471
申请日：2002-03-13
申请人： ALLERGAN INC
发明人： CHOW KEN , GIL DANIEL W , BURKE JAMES A , HARCOURT DALE A , GARST MICHAEL E , WHEELER LARRY A , MUNK STEPHEN A , GOMEZ DARIO G
IPC分类号： C07D233/58 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/435 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/538 , A61P1/12 , A61P7/12 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/54 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.

66. 发明专利

AT200222T 未知
公开(公告)号：AT200222T
公开(公告)日：2001-04-15
申请号：AT93903433
申请日：1993-01-12
申请人： ALLERGAN INC
发明人： GLUCHOWSKI CHARLES , GARST MICHAEL E , BURKE JAMES A , WHEELER LARRY A
IPC分类号： C07D403/12 , A61K31/495 , A61P7/10 , A61P9/08 , A61P9/10 , A61P27/02 , A61K31/415
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R2s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R3s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R5, R6 and R7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.

67. 发明专利

AU688380B2 Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 未知
公开(公告)号：AU688380B2
公开(公告)日：1998-03-12
申请号：AU7798894
申请日：1994-09-19
申请人： ALLERGAN INC
发明人： BURKE JAMES A , GARST MICHAEL E , WHEELER LARRY A
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having formula (I), and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, reduction of at least one effect of an inflammatory disorder, increase in renal fluid flow, and alteration in the rate of fluid transport in the gastrointestinal tract.

68. 发明专利

AU5678596A Aryl-imidazolines and aryl-imidazoles useful as alpha-2 adre nergic agonists without cardiovascular side effects 未知
公开(公告)号：AU5678596A
公开(公告)日：1996-11-29
申请号：AU5678596
申请日：1996-05-09
申请人： ALLERGAN INC
发明人： MUNK STEPHEN A , BURKE JAMES A , LAI RONALD K
IPC分类号： C07D403/12 , A61K31/495 , A61K31/498 , A61K31/535 , A61K31/538 , A61P1/12 , A61P9/00 , A61P27/02 , A61P27/06 , A61P27/16 , C07D413/12
摘要： Methods are disclosed for treating a mammal with a condition that responds to alpha -2 agonist treatment without causing cardiovascular side effects using compounds of formula (II) wherein R1 is H, alkyl of 1 to 4 carbon atoms or a halogen atom, X is O or NH and A is H or an oxo group and wherein said compound does not cause a concomitant reduction in blood pressure of said mammal.

69. 发明专利

AU670064B2 Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 未知
公开(公告)号：AU670064B2
公开(公告)日：1996-07-04
申请号：AU3470093
申请日：1993-01-12
申请人： ALLERGAN INC
发明人： GLUCHOWSKI CHARLES , GARST MICHAEL E , BURKE JAMES A , WHEELER LARRY A
IPC分类号： C07D403/12 , A61K31/495 , A61P7/10 , A61P9/08 , A61P9/10 , A61P27/02
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R2s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R3s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R5, R6 and R7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.

70. 发明专利

AU7798894A Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 未知
公开(公告)号：AU7798894A
公开(公告)日：1995-05-04
申请号：AU7798894
申请日：1994-09-19
申请人： ALLERGAN INC
发明人： BURKE JAMES A , GARST MICHAEL E , WHEELER LARRY A
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having formula (I), and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, reduction of at least one effect of an inflammatory disorder, increase in renal fluid flow, and alteration in the rate of fluid transport in the gastrointestinal tract.

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