公开(公告)号：US4358451A

公开(公告)日：1982-11-09

申请号：US112238

申请日：1980-01-15

申请人： Gabor I. Koletar ,  Jonathan R. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

发明人： Gabor I. Koletar ,  Jonathan R. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

IPC分类号： A61K31/435 ,  A61K31/505 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D471/04 ,  C07D471/14

CPC分类号： C07D471/04 ,  C07D471/14

摘要： Pyrimido- and imidazo-pyridoindole derivatives, in the form of racemates or optically active isomers, of formula: ##STR1## in which n=0 or 1, R.sub.1 =H, Hal, alkyl or alkoxy or CF.sub.3, R.sub.2 =H, alkyl, cycloalkyl-alkyl, cycloalkyl, N,N-dialkylaminoalkyl or phenyl, R.sub.3 =H or alkyl and R.sub.4 =H, alkyl or benzyl are useful as anti-anoxia or psychotropic agents in therapy. They are prepared by cyclizing a compound of formula: ##STR2## wherein R.sub.5 is alkyl, by heating it in an acidic medium, such as ethanolic hydrogen chloride.

摘要翻译： 嘧啶并咪唑并 - 吡啶并吲哚衍生物，其为n = 0或1，R1 = H，Hal，烷基或烷氧基或CF3，R2 = H的式（I）的外消旋体或光学活性异构体 烷基，环烷基 - 烷基，环烷基，N，N-二烷基氨基烷基或苯基，R3 = H或烷基，R4 = H，烷基或苄基可用作治疗中的抗缺氧或精神药物。 它们通过在酸性介质如氯化氢乙醇中加热而使其中R 5为烷基的式（II）化合物环化来制备。

公开(公告)号：US4336256A

公开(公告)日：1982-06-22

申请号：US184070

申请日：1980-09-04

申请人： Gabor I. Koletar ,  Jonathan B. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

发明人： Gabor I. Koletar ,  Jonathan B. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

IPC分类号： A61K31/435 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D471/04

CPC分类号： C07D471/04 ,  Y10S514/923

摘要： Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk--O--, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

摘要翻译： 式（I）的吡啶并吲哚衍生物n = 0或1; R1 = H，Hal，alk，alk-O-，CF3; R2 = -COOalk; -CONHR5（R5 = H或各种取代基）; R3 = H，alk，-COOalk; R4 = H，Ac，alk，-CONHR6（R6 = H或各种取代基），除了某些已知化合物之外，酸加成盐可用于治疗缺氧和抑郁症以及精神药物治疗。 它们由色胺或其衍生物通过与丙酮酸酯或3-乙氧基羰基-1,2-二氧代-1-乙氧基丙烷的反应制备，以形成其中R 4为H且R 2为-COOalk的化合物。 这些化合物与胺，异氰酸酯或通常的N-酰化或N-烷基化试剂反应以制备其它化合物。

公开(公告)号：US4277476A

公开(公告)日：1981-07-07

申请号：US60857

申请日：1979-07-26

申请人： Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Jonathan Frost ,  Gabor I. Koletar

发明人： Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Jonathan Frost ,  Gabor I. Koletar

IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  A01N43/48 ,  A61K31/495

CPC分类号： C07D471/04 ,  C07D471/14

摘要： Derivatives of fluorenes and fluoranthenes, in the form of racemates or of enantiomers, of the formula (I) ##STR1## in which n is 1 or 2, R.sub.1 is a hydrogen or halogen atom or an alkyl or alkoxy radical, R.sub.2 is a hydrogen atom or an alkyl, cycloalkyl, cycloalkylalkyl, benzyl, halogenobenzyl, alkylbenzyl, alkoxybenzyl, acyl, alkoxycarbonyl or alkylaminocarbonyl radical, R.sub.3 is a hydrogen atom or an alkyl radical, R.sub.4 is a hydrogen atom or an alkyl, acyl or aroyl radical, the alkyl and alkoxy radicals or parts of radicals having from 1 to 4 carbon atoms and pharmaceutically acceptable acid addition salts thereof, are therapeutically valuable as anti-anoxia and psychotropic agents.

摘要翻译： 式（I）其中n为1或2的式（I）的外消旋物或对映异构体的芴和荧蒽衍生物，R1为氢或卤素原子或烷基或烷氧基，R2 是氢原子或烷基，环烷基，环烷基烷基，苄基，卤代苄基，烷基苄基，烷氧基苄基，酰基，烷氧基羰基或烷基氨基羰基，R3是氢原子或烷基，R4是氢原子或烷基，酰基或芳酰基 ，烷基和烷氧基或具有1至4个碳原子的基团部分及其药学上可接受的酸加成盐作为抗缺氧和精神药物具有治疗价值。