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1.发明授权Substituted dodecahydrotripheylenes, and decahydropyrrolo[1,2-f]phenanthridines as CNS agents 失效取代的十二氢二苯乙烯和十氢吡咯并[1,2-f]菲啶作为CNS剂
公开(公告)号：US4642373A
公开(公告)日：1987-02-10
申请号：US628543
申请日：1984-07-06
IPC分类号： C07C29/09 , C07C29/10 , C07C29/44 , C07C29/56 , C07C33/20 , C07C43/174 , C07C43/178 , C07C59/72 , C07C69/616 , C07C205/32 , C07C205/33 , C07D207/08 , C07D211/34 , C07D215/22 , C07D215/233 , C07D455/03 , C07D455/04 , C07D471/04
CPC分类号： C07D207/08 , C07C205/32 , C07C205/33 , C07C29/095 , C07C29/10 , C07C29/44 , C07C29/56 , C07C309/00 , C07C33/20 , C07C43/174 , C07C43/1782 , C07C59/72 , C07D211/34 , C07D215/233 , C07D455/00 , C07D455/04 , C07D471/04 , C12C11/02 , C07B2200/07
摘要： 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.
摘要翻译： 1,2,3,4,4a，4b，5,6,7,8,8a，12b-十二氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基或烷氧基烷基）三苯 ，2,3,3a，3b，4,5,6,7,7a，11b-十氢-6-（氧代，羟基或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基） [1] - 菲，2,3,4,4a，4b，5,6,7,8,8a-十氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基，烷氧基烷基 ，芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基）-1H-吡啶并[1,2-f]菲啶，以及1,2,3,3a，3b，4,5,6,7,7a-十氢-6-（氧代， 羟基或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基）吡咯并[1,2-f]菲啶和衍生物作为中枢神经系统活性剂或作为具有这种活性的化合物的中间体是有价值的。
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2.发明授权Substituted hexahydrobenzo[e]indene and octahydrophenanthrene CNS agents and pharmaceutical compositions thereof 失效取代的六氢苯并[e]茚和八氢菲CNS剂及其药物组合物
公开(公告)号：US4576964A
公开(公告)日：1986-03-18
申请号：US618151
申请日：1984-06-07
IPC分类号： C07C33/20 , C07C205/33 , C07D207/08 , C07D211/34 , C07D307/10 , C07D307/16 , C07D309/04 , C07D311/78 , C07D455/04 , C07D471/04 , A61K31/22 , C07C43/10 , C07C43/205
CPC分类号： C07D207/08 , C07C205/33 , C07C309/00 , C07C33/20 , C07D211/34 , C07D307/10 , C07D307/16 , C07D309/04 , C07D311/78 , C07D455/04 , C07D471/04 , C07C2103/26
摘要： Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.
摘要翻译： 式（I）的三环苯并稠合化合物及其药学上可接受的阳离子和酸加成盐，其中n为0,1或2，t为1或2; M是CH或N，R 1是H或某些酰基; Q是CO2R4，COR5，C（OR7）R5R6，CN，CONR9R10，CH2NR9R10，CH2NHCOR11，CH2NHSO2R12，5-四唑基，或当n为1时，Q和OR1一起形成内酯或其某些还原的衍生物; Z是某些烷基，烷氧基，烷氧基烷基，芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基，是有价值的中枢神经系统活性剂，其使用方法，含有它们的药物组合物及其某些中间体。
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公开(公告)号：US4863934A
公开(公告)日：1989-09-05
申请号：US278634
申请日：1988-12-01
IPC分类号： C07C37/055 , C07C39/08 , C07C43/23 , C07C61/39 , C07D311/22 , C07D311/58 , C07D405/12 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
CPC分类号： C07D405/12 , C07C255/00 , C07C37/055 , C07C41/30 , C07C61/39 , C07D311/22 , C07D311/58 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
摘要： Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译： 式（I'）的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐，其中M为O，CH 2或NR 6; R6是氢，甲酰基，苄氧羰基或某些烷氧基烷基，烷酰基，烷基，芳烷基或芳烷基羰基; A'为：（1）其中A和B之一为氢，使得当A为氢时，B为C（R2R3）（CH2）fQ且f为1或2; 当B为氢时，A为C（R2R3）（CH2）fQ，f为0或1，当A和OR1一起形成内酯或其某些衍生物时; （2）A'是
（3）A'是Q3; Q是CO 2 R 7，COR 8，C（OH）R 8 R 9，CN，CONR 12 R 13，CH 2 NR 12 R 13，CH 2 NHCOR 14，CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN，COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢，苄基或某些酰基; R4是氢，某些烷基或某些芳烷基; R5是氢或某些烷基; Z是（C1-C9）亚烷基，任选地被O，S，SO或SO 2中断; W是氢，甲基，某些芳基或环烷基; 因此在哺乳动物中作为止痛剂，镇定剂，止吐剂，利尿剂，抗惊厥药，止泻药，镇咳药，在治疗青光眼中有用。 -
公开(公告)号：US4486428A
公开(公告)日：1984-12-04
申请号：US457171
申请日：1983-01-13
IPC分类号： C07C69/157 , A61K31/05 , A61K31/085 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/425 , A61K31/44 , A61K31/443 , A61P1/08 , A61P1/12 , A61P25/04 , A61P29/00 , C07C43/23 , C07C61/39 , C07C67/00 , C07C69/738 , C07C233/16 , C07C233/18 , C07C235/32 , C07C235/34 , C07C253/00 , C07C255/40 , C07C275/50 , C07D311/04 , C07D311/22 , C07D311/58 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D491/10 , C07D491/20 , C07D493/06 , C07D493/10
CPC分类号： C07D405/12 , C07C255/00 , C07C43/23 , C07C61/39 , C07D311/22 , C07D311/58 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
摘要： Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译： 式（I'）的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐，其中M为O，CH 2或NR 6; R6是氢，甲酰基，苄氧羰基或某些烷氧基烷基，烷酰基，烷基，芳烷基或芳烷基羰基; A'为：（1）其中A和B之一为氢，使得当A为氢时，B为C（R2R3）（CH2）fQ且f为1或2; 当B为氢时，A为C（R2R3）（CH2）fQ，f为0或1，当A和OR1一起形成内酯或其某些衍生物时; （2）A'是
（3）A'是Q3; Q是CO 2 R 7，COR 8，C（OH）R 8 R 9，CN，CONR 12 R 13，CH 2 NR 12 R 13，CH 2 NHCOR 14，CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN，COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢，苄基或某些酰基; R4是氢，某些烷基或某些芳烷基; R5是氢或某些烷基; Z是（C1-C9）亚烷基，任选地被O，S，SO或SO 2中断; W是氢，甲基，某些芳基或环烷基; 因此在哺乳动物中作为止痛剂，镇定剂，止吐剂，利尿剂，抗惊厥药，止泻药，镇咳药，在治疗青光眼中有用。 -
5.发明授权Bicyclic benzo fused pyran compounds used for nausea treatment and prevention 失效用于恶心治疗和预防的双环苯并稠合吡喃化合物
公开(公告)号：US4870084A
公开(公告)日：1989-09-26
申请号：US278635
申请日：1988-12-01
IPC分类号： C07C37/055 , C07C39/08 , C07C43/23 , C07C61/39 , C07D311/22 , C07D311/58 , C07D405/12 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
CPC分类号： C07D405/12 , C07C255/00 , C07C37/055 , C07C41/30 , C07C61/39 , C07D311/22 , C07D311/58 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
摘要： Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9) alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译： 式（I'）的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐，其中M为O，CH 2或NR 6; R6是氢，甲酰基，苄氧羰基或某些烷氧基烷基，烷酰基，烷基，芳烷基或芳烷基羰基; A'为：（1）其中A和B之一为氢，使得当A为氢时，B为C（R2R3）（CH2）fQ且f为1或2; 当B为氢时，A为C（R2R3）（CH2）fQ，f为0或1，当A和OR1一起形成内酯或其某些衍生物时; （2）A'是
（3）A'是Q3; Q是CO 2 R 7，COR 8，C（OH）R 8 R 9，CN，CONR 12 R 13，CH 2 NR 12 R 13，CH 2 NHCOR 14，CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN，COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢，苄基或某些酰基; R4是氢，某些烷基或某些芳烷基; R5是氢或某些烷基; Z是（C1-C9）亚烷基，任选地被O，S，SO或SO 2中断; W是氢，甲基，某些芳基或环烷基; 因此在哺乳动物中作为止痛剂，镇定剂，止吐剂，利尿剂，抗惊厥药，止泻药，镇咳药，在治疗青光眼中有用。 -
公开(公告)号：US4680404A
公开(公告)日：1987-07-14
申请号：US639151
申请日：1984-08-09
IPC分类号： C07C37/055 , C07C39/08 , C07C43/23 , C07C61/39 , C07D311/22 , C07D311/58 , C07D405/12 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10 , C07D311/20 , C07D405/04
CPC分类号： C07D405/12 , C07C255/00 , C07C37/055 , C07C41/30 , C07C61/39 , C07D311/22 , C07D311/58 , C07D407/12 , C07D417/12 , C07D491/10 , C07D493/06 , C07D493/10
摘要： Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 and Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, Antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译： 式（I'）的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐，其中M为O，CH 2或NR 6; R6是氢，甲酰基，苄氧羰基或某些烷氧基烷基，烷酰基，烷基，芳烷基或芳烷基羰基; A'为：（1）其中A和B之一为氢，使得当A为氢时，B为C（R2R3）（CH2）fQ且f为1或2; 当B为氢时，A为C（R2R3）（CH2）fQ，f为0或1，当A和OR1一起形成内酯或其某些衍生物时; （2）A'是
（3）A'是Q3; Q是CO 2 R 7，COR 8，C（OH）R 8 R 9，CN，CONR 12 R 13，CH 2 NR 12 R 13，CH 2 NHCOR 14，CH 2 NHSO 2 R 17或5-四唑基; Q3是5-四唑基，CH 2 CONHCOR 7，COOH或其某些酯，酰胺，羧酰亚氨基或磺酰亚氨基衍生物，CONHOH，CONHCONH 2或COCH 2 Q 4和Q 4是CN或COOH或其某些酯; R1是氢，苄基或某些酰基; R4是氢，某些烷基或某些芳烷基; R5是氢或某些烷基; Z是（C 1 -C 9）亚烷基，任选地被O，S，SO或SO 2中断; W是氢，甲基，某些芳基或环烷基; 因此，在哺乳动物中作为止痛剂，镇静剂，止吐剂，利尿剂，抗惊厥药，止泻药，镇咳药，在治疗青光眼中有用。 -
7.发明授权Substituted hexahydropyrrolo[1,2-a]-quinolines, hexahydro-1H-pyrido[1,2-a]- q 失效取代的六氢吡咯并[1,2-a] - 喹啉，六氢-1H-吡啶并[1,2-a] - 喹啉和含有它们的药物组合物
公开(公告)号：US4476131A
公开(公告)日：1984-10-09
申请号：US358569
申请日：1982-03-16
IPC分类号： A61K31/35 , A61K31/05 , A61K31/085 , A61K31/135 , A61K31/335 , A61K31/352 , A61K31/47 , A61P1/08 , A61P1/12 , A61P1/16 , A61P7/10 , A61P11/14 , A61P25/00 , A61P25/04 , A61P25/18 , A61P27/02 , C07C13/60 , C07C27/00 , C07C33/20 , C07C35/22 , C07C39/17 , C07C39/225 , C07C43/178 , C07C43/23 , C07C45/00 , C07C49/755 , C07C67/00 , C07C69/675 , C07C205/33 , C07C213/00 , C07C215/46 , C07C215/64 , C07C217/48 , C07C217/54 , C07C219/28 , C07C229/06 , C07C233/18 , C07C235/32 , C07C235/40 , C07C255/36 , C07C255/37 , C07C255/38 , C07C255/47 , C07C301/00 , C07C311/00 , C07D207/08 , C07D211/34 , C07D307/10 , C07D307/16 , C07D309/04 , C07D311/02 , C07D311/78 , C07D311/92 , C07D455/04 , C07D455/06 , C07D471/04 , C07D491/00 , C07D491/147 , C07D491/16 , C07D495/04 , C07D487/14
CPC分类号： C07D207/08 , C07C205/33 , C07C309/00 , C07C33/20 , C07D211/34 , C07D307/10 , C07D307/16 , C07D309/04 , C07D311/78 , C07D455/04 , C07D471/04 , C07C2103/26
摘要： Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.
摘要翻译： 式（I）的三环苯并稠合化合物及其药学上可接受的阳离子和酸加成盐，其中n为0,1或2，t为1或2; M是CH或N，R 1是H或某些酰基; Q是CO2R4，COR5，C（OR7）R5R6，CN，CONR9R10，CH2NR9R10，CH2NHCOR11，CH2NHSO2R12，5-四唑基或当n为1时，Q和OR1一起形成内酯或其某些还原的衍生物; Z是某些烷基，烷氧基，烷氧基烷基，芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基，是有价值的中枢神经系统活性剂，其使用方法，含有它们的药物组合物及其某些中间体。
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8.发明授权Substituted decahydro-1H-pyrido[1,2-f]phenanthridines and decahydropyrrolo[1,2-f]phenanthridines 失效取代的十氢-1H-吡啶并[1,2-f]菲啶和十氢吡咯并[1,2-f]菲啶
公开(公告)号：US4920221A
公开(公告)日：1990-04-24
申请号：US919912
申请日：1986-10-16
IPC分类号： C07C29/09 , C07C29/10 , C07C29/44 , C07C29/56 , C07C33/20 , C07C43/174 , C07C43/178 , C07C59/72 , C07C205/32 , C07C205/33 , C07D207/08 , C07D211/34 , C07D215/22 , C07D215/233 , C07D455/03 , C07D455/04 , C07D471/04
CPC分类号： C07D207/08 , C07C205/32 , C07C205/33 , C07C29/095 , C07C29/10 , C07C29/44 , C07C29/56 , C07C309/00 , C07C33/20 , C07C43/174 , C07C43/1782 , C07C59/72 , C07D211/34 , C07D215/233 , C07D455/00 , C07D455/04 , C07D471/04 , C07B2200/07
摘要： 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.
摘要翻译： 1,2,3,4,4a，4b，5,6,7,8,8a，12b-十二氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基或烷氧基烷基）三苯 ，2,3,3a，3b，4,5,6,7,7a，11b-十氢-6-（氧代，羟基或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基）-1H-环戊二烯 [1] - 菲，2,3,4,4a，4b，5,6,7,8,8a-十氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基，烷氧基烷基 ，芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基）-1H-吡啶并[1,2-f]菲啶，以及1,2,3,3a，3b，4,5,6,7,7a-十氢-6-（氧代， 羟基或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基） - 吡咯并[1,2-f]菲啶和衍生物作为中枢神经系统活性剂或作为具有这种活性的化合物的中间体是有价值的。
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9.发明授权Substituted dodecahydrotriphenylenes, decahydro-1H-cyclopenta[1]phenanthrenes, decahydro-1H-pyrido[1,2-f]phenanthridines and decahydropyrrolo[1,2-f]phenanthridines as CNS agents 失效十氢-1H-环戊二烯并[1]菲，十氢-1H-吡啶并[1,2-f]菲啶和十氢吡咯并[1,2-f]菲啶作为CNS剂
公开(公告)号：US4473704A
公开(公告)日：1984-09-25
申请号：US358765
申请日：1982-03-16
IPC分类号： C07C69/03 , A61K31/05 , A61K31/085 , A61K31/12 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/47 , A61K31/475 , A61P1/08 , A61P1/12 , A61P7/10 , A61P11/14 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P27/02 , A61P27/06 , C07C27/00 , C07C29/09 , C07C29/10 , C07C29/44 , C07C29/56 , C07C33/20 , C07C39/17 , C07C39/42 , C07C41/00 , C07C43/14 , C07C43/174 , C07C43/178 , C07C43/20 , C07C43/23 , C07C45/00 , C07C49/703 , C07C49/727 , C07C49/753 , C07C49/755 , C07C59/72 , C07C67/00 , C07C69/017 , C07C69/035 , C07C69/157 , C07C69/78 , C07C205/32 , C07C205/33 , C07C213/00 , C07C217/74 , C07C219/26 , C07C227/00 , C07C229/06 , C07C231/00 , C07C233/23 , C07C311/07 , C07D207/08 , C07D211/34 , C07D215/22 , C07D215/233 , C07D455/03 , C07D455/04 , C07D455/06 , C07D471/04
CPC分类号： C07D207/08 , C07C205/32 , C07C205/33 , C07C29/095 , C07C29/44 , C07C29/56 , C07C309/00 , C07C33/20 , C07C43/174 , C07C43/1782 , C07C59/72 , C07D211/34 , C07D215/233 , C07D455/00 , C07D455/04 , C07D471/04 , C07B2200/07
摘要： 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.
摘要翻译： 1,2,3,4,4a，4b，5,6,7,8,8a，12b-十二氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基或烷氧基烷基）三苯 ，2,3,3a，3b，4,5,6,7,7a，11b-十氢-6-（氧代，羟基或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基） [1]菲，2,3,4,4a，4b，5,6,7,8,8a-十氢-7-（氧代，羟基或氨基）-9-羟基-11-（烷基，烷氧基，烷氧基烷基， 芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基）-1H-吡啶并[1,2-f]菲啶和1,2,3,3a，3b，4,5,6,7,7a-十氢-6-（氧代，羟基 或氨基）-8-羟基-10-（烷基，烷氧基或烷氧基烷基）吡咯并[1,2-f]菲啶和衍生物作为中枢神经系统活性剂或作为具有这种活性的化合物的中间体是有价值的。
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公开(公告)号：US4454144A
公开(公告)日：1984-06-12
申请号：US390418
申请日：1982-06-21
IPC分类号： C07D311/80 , C07D405/12 , A61K31/35 , A61K31/44 , C07D311/78 , C07D405/02
CPC分类号： C07D405/12 , C07D311/80
摘要： The present invention comprises novel compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: G is hydroxymethylene or carbonyl;R.sub.a and R.sub.b are each methyl or hydrogen;R.sub.1 is hydrogen or alkanoyl having one to five carbon atoms;R.sub.2 is hydrogen, bromo, chloro or fluoro;R.sub.3 is hydrogen, bromo, chloro, fluoro, alkyl having one to six carbon atoms, (CH.sub.2).sub.p COOR.sub.4 wherein p is an integer from 0-6 and R.sub.4 is hydrogen, methyl or ethyl, or (CH.sub.2).sub.q OH wherein q is an integer from 1-6; with the proviso that when R.sub.3 is hydrogen or alkyl, R.sub.2 is bromo, chloro or fluoro;Z is (--alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) has from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each zero or 1;X is oxygen or methylene; andW is methyl, pyridyl, piperidyl or ##STR2## wherein W.sub.1 is hydrogen, fluoro, chloro or methoxy. An analgesically producing quantity of the compound when administered to a mammal produces analgesia therein.
摘要翻译： 本发明包括式IMA的新化合物或其药学上可接受的盐，其中：G是羟基亚甲基或羰基; Ra和Rb各自为甲基或氢; R1是氢或具有1-5个碳原子的烷酰基; R2是氢，溴，氯或氟; R3是氢，溴，氯，氟，具有1-6个碳原子的烷基，（CH2）pCOOR4，其中p是0-6的整数，R4是氢，甲基或乙基，或（CH2）qOH其中q是整数 从1-6开始; 条件是当R3为氢或烷基时，R2为溴，氯或氟; Z是（-alk1）mX-（alk2）n-，其中（alk1）和（alk2）中的每一个具有1至9个碳原子，条件是（alk1）+（alk2）中的碳原子的加成不是 大于9; m和n分别为零或1; X是氧或亚甲基; W是甲基，吡啶基，哌啶基或者其中W1是氢，氟，氯或甲氧基。 给予哺乳动物的化合物的镇痛产生量在其中产生镇痛。
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