公开(公告)号：EP1104407B1

公开(公告)日：2004-12-01

申请号：EP00939699.5

申请日：2000-06-08

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： C07D233/54 ,  A61K31/33 ,  A61P43/00 ,  C07D409/06 ,  C07D263/28 ,  C07D413/12 ,  C07D233/84 ,  C07D233/10 ,  C07D405/06 ,  C07D401/06 ,  C07D403/06 ,  C07D495/04

CPC分类号： C07D233/56 ,  C07D233/10 ,  C07D233/64 ,  C07D233/84 ,  C07D263/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D495/04

摘要： Compounds having adrenergic activity which are a selective agonists for one or both of the α2B and α2C adrenoceptor receptor subtypes in prefrence to the α2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S.

公开(公告)号：EP1370533A2

公开(公告)日：2003-12-17

申请号：EP02723489.7

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： C07D233/54 ,  A61K31/4164 ,  A61P43/00 ,  C07D405/06 ,  C07D409/06 ,  C07D401/06

CPC分类号： C07D233/56 ,  C07D233/06 ,  C07D233/10 ,  C07D233/64 ,  C07D233/84 ,  C07D263/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D495/04

摘要： A compound having a structure selected from the group consisting of: in which each x is independently (1) or (2); Y is selected from the group consisting of O;S;N;-(C(R7)z)s-where each R7 IS independently as previously defined fir R1, each z is independently 1-2, and s is 1-3;CH=; -CH=CH ;or Y1CH2_where Y1 is O, N, or S; and the dotted lines are optional double bonds, with the pviso that if the ring including Y is a cyclohexane ring or a heterocyclic 5 member ring said ring is not fully unsaturated, and that if Y is O,N or S, the ring including Y contains at least one said double bond, said compound further having selective agonist activity at the α2B or α2B/α2C adrenergic receptor subtype(s) over the α2A adrenergic receptor subtype, and all pharmacologically acceptable salts, esters, stereoisomers and racemic mixtures thereof.

公开(公告)号：EP1370533B1

公开(公告)日：2015-05-06

申请号：EP02723489.7

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： C07D233/54 ,  A61K31/4164 ,  A61P43/00 ,  C07D405/06 ,  C07D409/06 ,  C07D401/06 ,  C07D233/06 ,  C07D233/10 ,  C07D233/56 ,  C07D233/64 ,  C07D233/84 ,  C07D403/06 ,  C07D413/12 ,  C07D263/28 ,  C07D495/04

CPC分类号： C07D233/56 ,  C07D233/06 ,  C07D233/10 ,  C07D233/64 ,  C07D233/84 ,  C07D263/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D495/04

公开(公告)号：EP1036065B1

公开(公告)日：2004-05-12

申请号：EP98962883.9

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： C07D233/56 ,  A61K31/415 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D405/06 ,  C07D233/84 ,  C07D413/12 ,  C07D495/04

CPC分类号： C07D233/56 ,  C07D233/06 ,  C07D233/64 ,  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 α2B and α2C adrenoceptor receptor subtypes in preference to the α2A 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)R1, wherein R1 is H or lower alkyl, but R1 is absent when the bond between X and the ring represented by formula (a) is a double bond; Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R?2, R3 or R4¿ is bound to a saturated carbon atom and x is 2 when R?2, R3 or R4¿ is bound to a saturated carbon atom; R2 is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R¿2? may be oxo; R3 and R4 are, each, H, lower alkyl, hydroxy, lower alkoxy, or phenyl or, together, are -(C(R?2¿)x)z-; -Y1(C(R2)x)z'-; -Y?1(C(R2)x)yY1¿-; -(C(R?2)x)-Y1-(C(R2¿)x)-; -(C(R?2)x)-Y1-(C(R2¿)x)-(C(R2)x)- and -Y?1-(C(R2)x)-Y1-(C(R2¿)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.