公开(公告)号：US4749559A

公开(公告)日：1988-06-07

申请号：US869714

申请日：1986-06-02

Applicant: John W. Kebabian

Inventor： John W. Kebabian

IPC: A61K51/04 ,  A61K49/00 ,  A61K39/00 ,  A61K43/00

CPC classification number: A61K51/047 ,  A61K2123/00

Abstract: The present invention discloses a method of detecting melanin containing matter comprising reacting melanin containing matter with an enantiomer of 2, 3, 4, 5-tetrahydro-3-methyl-5 phenyl-1H-3-benzazepin-7-ol and determining the binding of said enantiomer with melanin. The invention also describes a method of delivering cytotoxic level of gamma radiation to pigmented melanoma comprising administering to a body carrying pigmented melanoma a cytotoxically effective radiation dosage of .sup.125 I-enantiomer of 2, 3, 4, 5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-ol having specific binding affinity for said melanoma. Other applications of the invention have also been described.

Abstract translation: 本发明公开了一种检测含黑色物质的方法，包括使含黑色素的物质与2,3,4,5-四氢-3-甲基-5-苯基-1H-苯并吖庚因-7-醇的对映异构体反应并测定结合 的所述对映体与黑色素。 本发明还描述了向着色黑素瘤递送细胞毒性水平的γ辐射的方法，其包括对携带着色黑素瘤的身体施用2,3,4,5-四氢-3-甲基-5-吡喃半乳糖苷的125I-对映异构体的细胞毒性有效辐射剂量， 对所述黑素瘤具有特异性结合亲和力的苯基-1H-3-苯并氮杂-7-醇。 还描述了本发明的其它应用。

公开(公告)号：US4994486A

公开(公告)日：1991-02-19

申请号：US456011

申请日：1989-12-22

Applicant: Robert W. Schoenleber ,  John W. Kebabian ,  Michael P. DeNinno ,  Michael R. Michaelides ,  Sheela A. Thomas

Inventor： Robert W. Schoenleber ,  John W. Kebabian ,  Michael P. DeNinno ,  Michael R. Michaelides ,  Sheela A. Thomas

IPC: A61K38/00 ,  C07C41/02 ,  C07C215/64 ,  C07C217/74 ,  C07C219/28 ,  C07C233/18 ,  C07C237/08 ,  C07C271/16 ,  C07C271/44 ,  C07C309/65 ,  C07C323/60 ,  C07D207/08 ,  C07D209/62 ,  C07D221/10 ,  C07D221/20 ,  C07D311/76 ,  C07D311/78 ,  C07D311/96 ,  C07D313/08 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D493/10 ,  C07K5/06

CPC classification number: C07D207/08 ,  C07C215/64 ,  C07C217/74 ,  C07C219/28 ,  C07C233/18 ,  C07C237/08 ,  C07C271/16 ,  C07C271/44 ,  C07C309/65 ,  C07C323/60 ,  C07D209/62 ,  C07D221/10 ,  C07D221/20 ,  C07D311/76 ,  C07D311/78 ,  C07D311/96 ,  C07D313/08 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D493/10 ,  C07K5/06026 ,  A61K38/00 ,  C07C2101/14 ,  C07C2102/10 ,  C07C2102/28 ,  C07C2103/28 ,  C07C2103/74 ,  C07C2103/93

Abstract: Novel compounds of Formula (I): ##STR1## or pharmaceutically acceptable salts, esters and amides thereof, wherein A is O, C, CH or CH.sub.2, n is 0 or 1, and the dotted line is a single bond when A is O or CH.sub.2 and a double bond when A is CH or when n=0, A is C andR.sub.6 and A taken together form a nitrogen-containing heterocycle;R is hydrogen, lower alkyl or a readily cleavable group;R.sub.1 is selected from hydrogen, halogen, lower alkyl, haloalkyl and lower alkoxy;R.sub.2 is selected from hydrogen, halogen, lower alkyl and haloalkyl or, taken together with R.sub.8, forms a fused ring;R.sub.3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl or, taken together with R.sub.4, forms a spirocycloalkyl or, taken together with R.sub.5, forms a fused cycloalkyl;R.sub.4 is hydrogen or alkyl or, taken together with R.sub.3, forms a spirocycloalkyl;R.sub.5 is hydrogen or alkyl or, taken together with R.sub.3, forms a fused cycloalkyl;R.sub.6 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or arylalkyl or, taken together with A when A is C and when n is 0, forms a fused nitrogen-containing heterocycle or, taken together with R.sub.7 or R.sub.8, forms a nitrogen-containing heterocycle;R.sub.7 is hydrogen or alkyl or, taken together with R.sub.6 or R.sub.8, forms a nitrogen-containing heterocycle;R.sub.8 is hydrogen or alkyl or, taken together with R.sub.6 or R.sub.7, forms a nitrogen-containing heterocycle or, taken together with R.sub.2, forms a fused ring, with the proviso that R.sub.3 and R.sub.4 cannot simultaneously both be hydrogen, are selective dopaminergic agents and are useful for treating disorders characterized by abnormal dopaminergic activity in the central or the peripheral nervous system, for example, neurological disorders such as psychoses, Parkinson's Disease, certain cardiovascular disorders and addictive behavior disorders.

Abstract translation: 式（I）的新型化合物：其中A为O，C，CH或CH 2，n为0或1，虚线为单键， A为O或CH2，当A为CH或当n = 0时为双键，A为C且R6和A一起形成含氮杂环; R是氢，低级烷基或易裂解基团; R1选自氢，卤素，低级烷基，卤代烷基和低级烷氧基; R2选自氢，卤素，低级烷基和卤代烷基，或与R8一起形成稠环; R 3是氢，烷基，烯基，炔基，环烷基，芳基或芳烷基，或与R 4一起形成螺环烷基，或与R 5一起形成稠合环烷基; R4是氢或烷基，或与R3一起形成螺环烷基; R5是氢或烷基，或与R3一起形成稠合的环烷基; R 6是氢，烷基，烯基，炔基，环烷基或芳基烷基，或者当A是C时，与A一起，当n是0时，形成稠合含氮杂环，或者与R 7或R 8一起形成含氮 杂环 R7是氢或烷基，或与R6或R8一起形成含氮杂环; R8是氢或烷基，或与R6或R7一起形成含氮杂环，或者与R2一起形成稠合环，条件是R3和R4不能同时为氢，是选择性多巴胺能试剂， 可用于治疗以中枢或周围神经系统异常多巴胺能活性为特征的疾病，例如神经系统疾病如精神病，帕金森病，某些心血管疾病和成瘾行为障碍。

公开(公告)号：US4963568A

公开(公告)日：1990-10-16

申请号：US359448

申请日：1989-05-31

Applicant: Robert W. Schoenleber ,  John W. Kebabian ,  Yvonne C. Martin ,  Michael P. DeNinno ,  Richard J. Perner ,  David M. Stout ,  Chi-Nung W. Hsiao ,  Stanley DiDomenico, Jr. ,  John F. DeBernardis ,  Fatima Z. Basha ,  Michael D. Meyer ,  Biswanath De

Inventor： Robert W. Schoenleber ,  John W. Kebabian ,  Yvonne C. Martin ,  Michael P. DeNinno ,  Richard J. Perner ,  David M. Stout ,  Chi-Nung W. Hsiao ,  Stanley DiDomenico, Jr. ,  John F. DeBernardis ,  Fatima Z. Basha ,  Michael D. Meyer ,  Biswanath De

IPC: A61K31/13 ,  A61K31/135 ,  A61K31/16 ,  A61K31/335 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K38/00 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/30 ,  C07C41/02 ,  C07C215/48 ,  C07C215/64 ,  C07C217/56 ,  C07C217/74 ,  C07C219/28 ,  C07C233/18 ,  C07C237/08 ,  C07C271/16 ,  C07C271/44 ,  C07C309/65 ,  C07C323/60 ,  C07D207/08 ,  C07D209/08 ,  C07D209/62 ,  C07D221/06 ,  C07D221/10 ,  C07D221/20 ,  C07D311/76 ,  C07D311/78 ,  C07D311/96 ,  C07D313/08 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D493/10 ,  C07K5/06

CPC classification number: C07D207/08 ,  C07C215/64 ,  C07C217/74 ,  C07C219/28 ,  C07C233/18 ,  C07C237/08 ,  C07C271/16 ,  C07C271/44 ,  C07C309/65 ,  C07C323/60 ,  C07D209/62 ,  C07D221/10 ,  C07D221/20 ,  C07D311/76 ,  C07D311/78 ,  C07D311/96 ,  C07D313/08 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D493/10 ,  C07K5/06026 ,  A61K38/00 ,  C07C2101/14 ,  C07C2102/10 ,  C07C2102/28 ,  C07C2103/28 ,  C07C2103/74 ,  C07C2103/93

Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.

Abstract translation: 作为选择性多巴胺激动剂的新型化合物可用于治疗以异常多巴胺水平为特征的疾病，例如帕金森病，以及心血管疾病。

公开(公告)号：US5158948A

公开(公告)日：1992-10-27

申请号：US762828

申请日：1991-09-19

Applicant: Robert W. Schoenleber ,  Paul P. Ehrlich ,  John W. Kebabian ,  James R. Campbell

Inventor： Robert W. Schoenleber ,  Paul P. Ehrlich ,  John W. Kebabian ,  James R. Campbell

IPC: C07D223/14 ,  C07D223/16 ,  C07D223/32 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC classification number: C07D223/16 ,  C07D223/14 ,  C07D223/32 ,  C07D491/10 ,  C07D495/10

Abstract: Novel tetracyclic spirobenzazepine compounds of the formula ##STR1## or a pharmaceutically-acceptable salt, amide or ester thereof, which are dopamine D-1 receptor antagonists useful for treating dopamine-related neurological and psychological disorders, cognitive impairment, attention deficit disorders and addictive behavior disorders.

Abstract translation: 可用于治疗多巴胺相关神经和心理障碍，认知障碍，注意力缺陷障碍和成瘾行为的新颖的四环型螺苯并氮平化合物或其药学上可接受的盐，酰胺或酯，其为多巴胺D-1受体拮抗剂 疾病