公开(公告)号：US4069241A

公开(公告)日：1978-01-17

申请号：US690361

申请日：1976-05-26

申请人： Ulrich Weiss ,  Kenner C. Rice

发明人： Ulrich Weiss ,  Kenner C. Rice

IPC分类号： C07C51/00 ,  C07C62/38 ,  C07C67/00 ,  C07C69/757 ,  C07C69/76

CPC分类号： C07C62/38

摘要： Tricyclic aromatic compounds of the formula ##STR1## including those wherein: A. R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;B. R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;C. R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;D. R.sub.1, R.sub.2, and R.sub.3 are hydrogen; andE. R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.

摘要翻译： 式“IMAGE”的三环芳族化合物包括其中：

公开(公告)号：US4150236A

公开(公告)日：1979-04-17

申请号：US817094

申请日：1977-07-19

申请人： Ulrich Weiss ,  Kenner C. Rice

发明人： Ulrich Weiss ,  Kenner C. Rice

IPC分类号： C07C51/00 ,  C07C62/38 ,  C07C67/00 ,  C07C69/757 ,  C07C69/94

CPC分类号： C07C62/38

摘要： Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(b) R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(c) R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;(d) R.sub.1, R.sub.2, and R.sub.3 are hydrogen; and(e) R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.

公开(公告)号：US4139713A

公开(公告)日：1979-02-13

申请号：US817051

申请日：1977-07-19

申请人： Ulrich Weiss ,  Kenner C. Rice

发明人： Ulrich Weiss ,  Kenner C. Rice

IPC分类号： C07C51/00 ,  C07C62/38 ,  C07C67/00 ,  C07C69/757 ,  C07C69/95

CPC分类号： C07C62/38

摘要： Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(b) R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(c) R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;(d) R.sub.1, R.sub.2, and R.sub.3 are hydrogen; and(e) R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.

公开(公告)号：US5856318A

公开(公告)日：1999-01-05

申请号：US910302

申请日：1997-08-11

申请人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

发明人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC分类号： C07D207/14 ,  C07D211/56 ,  C07D223/12 ,  C07D409/06 ,  A61K31/33 ,  A61K31/55 ,  C07D295/00 ,  C07D405/00

CPC分类号： C07D409/06 ,  C07D207/14 ,  C07D211/56 ,  C07D223/12

摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

摘要翻译： 描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。 特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。

公开(公告)号：US5679679A

公开(公告)日：1997-10-21

申请号：US348654

申请日：1994-12-02

申请人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

发明人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC分类号： A61K31/495 ,  C07D471/04 ,  C07D487/04 ,  C07D31/495 ,  C07D31/55

CPC分类号： C07D471/04 ,  A61K31/495 ,  C07D487/04

摘要： Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl; each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.11 is independently selected from the group consisting of hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; n is an integer of from three to four; m is an integer of two; A is selected from the group consisting of phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl and wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

摘要翻译： 描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。 特别感兴趣的化合物具有下式：其中：R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; R 2，R 3和R 8至R 11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; n是3至4的整数; m是2的整数; A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基，其中任何前述A基团可以进一步被一个或多个独立地选自羟基，羟基，低级烷基，低级烷氧基，卤代 ，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基; 或其药学上可接受的盐。

公开(公告)号：US5679673A

公开(公告)日：1997-10-21

申请号：US344304

申请日：1994-11-21

申请人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

发明人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC分类号： C07D453/02 ,  C07D487/08 ,  A61K31/55 ,  C07D471/08

CPC分类号： C07D487/08 ,  C07D453/02

摘要： Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.9 is selected from hydrido, loweralkyl, benzyl and haloloweralkyl; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothiophenyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

摘要翻译： 描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。 特别感兴趣的化合物具有下式：其中R，R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R10至R13各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中R8和R9各自选自氢，低级烷基，苄基和卤代低级烷基; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。

公开(公告)号：US5346908A

公开(公告)日：1994-09-13

申请号：US904354

申请日：1992-06-25

申请人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

发明人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC分类号： C07D207/14 ,  C07D211/56 ,  C07D223/12 ,  C07D409/06 ,  A61K31/55 ,  A61K31/40 ,  A61K31/445 ,  C07D211/08

CPC分类号： C07D409/06 ,  C07D207/14 ,  C07D211/56 ,  C07D223/12

摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

摘要翻译： 描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。 特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。

公开(公告)号：US5208338A

公开(公告)日：1993-05-04

申请号：US715762

申请日：1991-06-14

申请人： Brian R. de Costa ,  Michael J. Iadarola ,  Kenner C. Rice ,  Richard B. Rothman ,  Karen F. Berman

发明人： Brian R. de Costa ,  Michael J. Iadarola ,  Kenner C. Rice ,  Richard B. Rothman ,  Karen F. Berman

IPC分类号： C07D489/08 ,  G01N33/534 ,  G01N33/94

CPC分类号： G01N33/534 ,  C07D489/08 ,  G01N33/9486

摘要： The present invention is directed to radiolabeled N-substituted-6-iodo-3,14-dihydroxy-4,5.alpha.-epoxymorphinans, intermediates for producing the same, and a process for the preparation and methods of detecting opioid receptors.The radioimaging agent of the present invention has the following formula: ##STR1## wherein I is selected from the group consisting of .sup.123 I and .sup.125 I; and where R is alkyl, cycloalkylloweralkyl or allyl.

摘要翻译： 本发明涉及放射性标记的N-取代-6-碘-3,14-二羟基-4,5α-环氧吗啡喃，其制备方法及其制备方法和检测阿片受体的方法。 本发明的放射成像剂具有下式：其中I选自123I和125I的 并且其中R是烷基，环烷基低级烷基或烯丙基。

公开(公告)号：US06395900B1

公开(公告)日：2002-05-28

申请号：US09895956

申请日：2001-06-29

申请人： Andrew Coop ,  Kenner C. Rice

发明人： Andrew Coop ,  Kenner C. Rice

IPC分类号： C07D48902

CPC分类号： C07D489/02 ,  C07D489/00 ,  C07D489/08 ,  C07D489/12

摘要： The present invention provides a method for N-deprotecting an opioid compound, a method for N-deprotecting and O-demethylating an opioid compound, a method for O-demethylating an opioid compound, and a method for O-demethylating a nonpeptidic delta agonist compound or an opioid compound having a tertiary amide with no significant reaction at amide groups.

摘要翻译： 本发明提供了对阿片样物质进行N-去保护的方法，对于阿片样物质进行N-脱保护和O-脱甲基化的方法，对阿片样物质进行O-去甲基化的方法，以及将非肽δ激动剂化合物O-脱甲基化的方法 或具有在酰胺基上没有显着反应的叔酰胺的阿片样物质化合物。

公开(公告)号：US06310064B1

公开(公告)日：2001-10-30

申请号：US09347659

申请日：1999-07-06

申请人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

发明人： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC分类号： C07D47104

CPC分类号： C07D471/04 ,  A61K31/495 ,  C07D487/04

摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:

摘要翻译： 公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，例如脑缺血，精神病和抽搐。例如，感兴趣的化合物具有下式：