公开(公告)号：US4963558A

公开(公告)日：1990-10-16

申请号：US447319

申请日：1989-12-07

申请人： Terrence M. Hotten ,  Graham H. Timms ,  David E. Tupper

发明人： Terrence M. Hotten ,  Graham H. Timms ,  David E. Tupper

IPC分类号： A61K31/47 ,  A61P1/08 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/26 ,  C07D471/04

CPC分类号： C07D471/04

摘要： Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, C.sub.3-9 cycloalkyl, optionally substituted phenyl, or --SR.sup.4 where R.sup.4 is C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, or C.sub.3-9 cycloalkyl, R.sup.3 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, c.sub.3-9 cycloalkyl, or optionally phenyl, and either X and Y are both hydrogen or together are .dbd.O; and acid addition salts thereof. These compounds show useful effects on the central nervous system.

公开(公告)号：US5258378A

公开(公告)日：1993-11-02

申请号：US794283

申请日：1991-11-19

申请人： Barry P. Clark ,  Graham H. Timms ,  David E. Tupper

发明人： Barry P. Clark ,  Graham H. Timms ,  David E. Tupper

IPC分类号： A61K31/55 ,  A61P25/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention relates to a compound of formula (I) ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halo, hydroxy, nitro, C.sub.1-4 alkylcarbonyl, hydroxy-C.sub.1-4 alkyl, R.sup.3 is hydrogen or optionally substituted phenylsulphonyl, R.sup.4 is optionally substituted phenyl, benzofuranyl or dihydrobenzofuranyl, and R.sup.5 is hydrogen or C.sub.1-4 alkyl; and salts thereof. These compounds are useful dopaminergic agents.

公开(公告)号：US4720498A

公开(公告)日：1988-01-19

申请号：US791856

申请日：1985-10-28

申请人： Graham H. Timms ,  David E. Tupper

发明人： Graham H. Timms ,  David E. Tupper

IPC分类号： A61K31/48 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  C07D457/02

CPC分类号： C07D457/02

摘要： There is described a compound of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-4 alkyl, R.sup.2 is hydrogen, C.sub.1-4 alkyl, hydroxy C.sub.1-4 alkyl, C.sub.1-4 alkoxy C.sub.1-4 alkyl, HSC.sub.1-4 alkyl, C.sub.1-4 alkyl-S-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, optionally substituted arylthio or optionally substituted aralkylthio, and R.sup.3 is hydrogen, C.sub.1-4 alkyl, optionally substituted aryl or optionally substituted aralkyl; and salts thereof. The compounds show useful effects on the central nervous system.

摘要翻译： 描述了式（I）的化合物，其中R 1是氢或C 1-4烷基，R 2是氢，C 1-4烷基，羟基C 1-4烷基，C 1-4烷氧基C 1-4烷基，HSCl 1-4烷基，C 1-4烷基-S-C 1-4烷基，C 1-4烷硫基，任选取代的芳硫基或任选取代的芳烷硫基，R 3是氢，C 1-4烷基，任选取代的芳基或任选取代的芳烷基; 及其盐。 这些化合物对中枢神经系统有效。

公开(公告)号：US4705807A

公开(公告)日：1987-11-10

申请号：US448549

申请日：1982-12-10

申请人： David C. Horwell ,  Graham H. Timms

发明人： David C. Horwell ,  Graham H. Timms

IPC分类号： A61K31/13 ,  A61K31/135 ,  C07C67/00 ,  C07C209/00 ,  C07C209/26 ,  C07C209/28 ,  C07C209/50 ,  C07C209/52 ,  C07C211/19 ,  C07C211/30 ,  C07C217/74 ,  C07C231/00 ,  C07C233/43 ,  C07D307/87 ,  A61K31/455 ,  C07C87/28

CPC分类号： C07C45/69 ,  A61K31/13 ,  C07C211/27 ,  C07C211/29 ,  C07C45/62 ,  C07C45/63

摘要： Novel amines of formula:R--(CH.sub.2).sub.n --NR.sup.1 R.sup.2where R is cis-2-phenylbicyclo[2,2,2]octane or 2-phenylbicyclo[2,2,2]oct-2-ene nucleus, n is 1 to 3, R.sup.1 is C.sub.1-3 alkyl and R.sup.2 is hydrogen or C.sub.1-3 alkyl, and acid-addition salts thereof, which are useful for the treatment of disorders of the central nervous system.

摘要翻译： 式（R-（CH2）n-NR1R2的新型胺，其中R为顺式-2-苯基双环[2,2,2]辛烷或2-苯基双环[2,2,2]辛-2-烯核，n为1 至3，R 1为C 1-3烷基，R 2为氢或C 1-3烷基，及其酸加成盐，其可用于治疗中枢神经系统疾病。

公开(公告)号：US5428065A

公开(公告)日：1995-06-27

申请号：US312600

申请日：1994-09-27

申请人： Barry P. Clark ,  Graham H. Timms

发明人： Barry P. Clark ,  Graham H. Timms

IPC分类号： A61K31/135 ,  A61K31/155 ,  A61K31/19 ,  A61K31/235 ,  A61K31/275 ,  A61P25/00 ,  A61P25/28 ,  C07C209/26 ,  C07C211/27 ,  C07C211/29 ,  C07C217/58 ,  C07C279/04 ,  C07C279/12 ,  C07C323/12 ,  C07C211/28

CPC分类号： C07C279/12 ,  C07C211/27 ,  C07C217/58 ,  C07C323/12 ,  C07C2103/26

摘要： Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.

摘要翻译： 下式的药物化合物：其中R 1至R 8各自为氢或C 1-4烷基，m，n和p各自为0,1或2，q为0,1或2， 2或3，X和Z各自为C 1-4烷基，C 1-4烷氧基，羟基，硝基，氰基，卤素，三卤代甲基，羧基，C 1-4烷氧基 - 羰基或苯基，另外z与苯环 其可以是：Y是-O-，-S-或-CH 2 - ，V是 - （CH 2）r - 或 - （CH 2）r S-，其中r是1至15，W 是氢或任选取代的苯基; 及其盐。

公开(公告)号：US4215074A

公开(公告)日：1980-07-29

申请号：US49672

申请日：1979-06-18

申请人： David C. Horwell ,  Graham H. Timms

发明人： David C. Horwell ,  Graham H. Timms

IPC分类号： A61K31/135 ,  A61K20060101 ,  A61K31/055 ,  A61K31/13 ,  A61P25/24 ,  A61P25/26 ,  C07C20060101 ,  C07C39/30 ,  C07C67/00 ,  C07C209/00 ,  C07C211/26 ,  C07C211/29 ,  C07C83/00

CPC分类号： C07C209/70 ,  C07C211/29 ,  C07B2200/07 ,  C07C2102/44

摘要： A process for preparing antidepresssant 2-phenylbicyclooctylamines of formula (I): ##STR1## where R.sup.1 and R.sup.2 represent C.sub.1-3 alkyl and Ar represents a phenyl group optionally substituted by up to two halogen atoms, by reduction of a novel enamine intermediate of formula: ##STR2## where R.sup.3 and R.sup.4 are hydrogen or taken together represent a single bond and where X is hydrogen, bromine or chlorine.

摘要翻译： 制备式（I）的抗抑郁2-苯基双环辛胺的方法：其中R 1和R 2表示C 1-3烷基，Ar表示任选被至多两个卤素原子取代的苯基，通过还原新型烯胺 中间体：其中R 3和R 4是氢或一起代表单键，其中X是氢，溴或氯。