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31. 发明授权

US4428938A Peptides affecting the immune regulation and a process for their preparation 失效
标题翻译：影响免疫调节的肽及其制备方法
公开(公告)号：US4428938A
公开(公告)日：1984-01-31
申请号：US387655
申请日：1982-06-11
申请人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Istvan Schon , Laszlo Denes , Julia Ember , Gyorgy Hajos , Laszlo Szporny , Bela Szende
发明人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Istvan Schon , Laszlo Denes , Julia Ember , Gyorgy Hajos , Laszlo Szporny , Bela Szende
IPC分类号： C07K5/08 , A61K38/00 , A61K38/07 , A61K38/22 , A61P37/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07K1/113 , C07K5/09 , C07K5/10 , C07K5/103 , C07K5/11 , C07K5/117 , C07K7/06 , C07K14/575 , C07K14/66 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0815 , C07K14/66 , C07K5/1008 , C07K5/1019 , C07K5/1024 , Y10S930/18
摘要： Peptides affecting the immune regulation selected from the following group:Arg-Lys-AspArg-Lys-Asp-ValArg-Lys-Asn-ValArg-Lys-Asu-ValArg-Lys-Ala-ValArg-Lys-Asp-AlaArg-Lys-Asp-IleArg-Lys-Glu-ValArg-Ala-Asp-ValArg-Asp-Lys-ValAla-Lys-Asp-ValLys-Arg-Asp-ValGlp-Arg-Lys-AspGlp-Arg-Lys-Asp-ValGlp-Arg-Lys-Asp-Val-Tyr and salts, amides lower alkyl esters and protected derivatives thereof.
摘要翻译： Arg-Lys-Asp Arg-Lys-Asp-Val Arg-Lys-Asn-Val Arg-Lys-Asu-Val Arg-Lys-Ala-Val Arg-Lys-Asp- Ala Arg-Lys-Asp-Ile Arg-Lys-Glu-Val Arg-Ala-Asp-Val Arg-Asp-Lys-Val Ala-Lys-Asp-Val Lys-Arg-Asp-Val Glp-Arg-Lys-Asp Glp-Arg-Lys-Asp-Val Glp-Arg-Lys-Asp-Val-Tyr和其盐，酰胺低级烷基酯及其被保护的衍生物。

32. 发明授权

US4330532A Angiotensin-II analogues with antagonizing effects, containing an .alpha.-hydroxycarboxylic acid residue in position 8, and a process for the preparation thereof 失效
标题翻译：在8位含有α-羟基羧酸残基的具有拮抗作用的血管紧张素-II类似物及其制备方法
公开(公告)号：US4330532A
公开(公告)日：1982-05-18
申请号：US222765
申请日：1981-01-06
申请人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
发明人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
IPC分类号： C07K7/06 , A61K38/08 , A61K38/55 , A61P43/00 , C07K7/14 , A61K37/00 , C07C103/52
CPC分类号： C07K7/14 , Y02P20/55
摘要： New angiotensin-II analogues of the general formula (I),X-Arg-Val-Tyr-Ile-His-Pro-Y-OA (I)whereinX stands for the acyl group of an N-methylamino acid, or the acyl group of an aliphatic .alpha.-aminooxy- or .alpha.-hydroxycarboxylic acid,Y is the residue of an aliphatic .alpha.-hydroxycarboxylic acid, andA is hydrogen or a C.sub.1-5 alkyl group,are prepared by removing the protecting groups of a protected octapeptide derivative of the general formula (II) or (III),B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OF (II)B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OA (III)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andF is a group for the protection of the terminal carboxy group, resistant to the effect of mild acids but removable by catalytic hydrogenolysis or upon treatment with a stronger acid.The new compounds of the invention can be applied to diagnose and differentiate hypertensions of various origin, and in the therapy to suppress hypertensions of renal origin, in the treatment of hypertensive crises, secondary cardiac insufficiency, etc.
摘要翻译：通式（I）的新型血管紧张素-II类似物，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X表示N-甲基氨基酸的酰基，或酰基脂肪族α-氨基氧基或α-羟基羧酸的基团，Y是脂肪族α-羟基羧酸的残基，A是氢或C 1-5烷基，是通过除去保护的八肽衍生物的保护基来制备的的通式（II）或（III）的BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OF（II）BX-Arg（C）-Val- Tyr（D）-Ile-His（E）-Pro-Y-OA（III）其中B是通过酸解或催化氢化除去的基团，C是用于临时保护Arg部分上胍基的基团，D 是用于临时保护Tyr部分上的芳族羟基的基团，E是His部分上咪唑基的临时保护基团，F是保护末端羧基的基团，耐受温和酸的作用b 通过催化氢解或用较强酸处理可以除去。本发明的新化合物可用于诊断和鉴别各种起因的高血压，以及用于抑制肾源性高血压，治疗高血压危象，继发性心脏功能不全等的治疗。

33. 发明授权

US5510345A Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：生物活性白蛋白衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5510345A
公开(公告)日：1996-04-23
申请号：US351447
申请日：1994-12-08
申请人： Zoltan Tuba , Sandor Maho , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Csaba Szantay , Ferenc Soti , Zsuzsa Baloghne Kardos , Maria Incze , Gabor Balogh , Maria Gazdag
发明人： Zoltan Tuba , Sandor Maho , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Csaba Szantay , Ferenc Soti , Zsuzsa Baloghne Kardos , Maria Incze , Gabor Balogh , Maria Gazdag
IPC分类号： C07D471/00 , A61K31/495 , A61K31/505 , A61K31/55 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/28 , C07D239/00 , C07D295/00 , C07D461/00 , C07D401/14 , C07D403/14
CPC分类号： C07D461/00
摘要： The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).
摘要翻译： PCT No.PCT / Hu93 / 00036 Sec。 371日期1994年12月8日第 102（e）日期1994年12月8日PCT提交1993年6月8日PCT公布。出版物WO93 / 25550 本发明涉及式（I）的新颖白蛋白衍生物：其中R 1和R 2以及R 3和R 4彼此独立地代表氢，C 2-6烷基，C 2-6烯基; 或含有1〜3个环的C 3〜10环亚烷基，后者可以被C 1-6烷基或C 2-6烯基取代; 或R 1和R 2和/或R 3和R 4与相邻的氮原子以及任选的另外的氧或氮原子一起形成可被C 1-6烷基取代的4-至6-元饱和或不饱和的环状基团或C 2-6烯基; X，Y和Z中的两个是氮，而第三个是次甲基; n为1或2; W表示氧或两个氢原子; 波浪线表示α - /α - ，α - /β - 或β - / - - - 立体位置，以及它们的酸加成盐和溶剂合物。本发明还涉及含有上述化合物的药物组合物以及制备式（I）化合物的方法。式（I）化合物具有抗氧化作用，因此它们可用于抑制哺乳动物（包括人）中发生的脂质的过氧化反应。

34. 发明授权

US5157038A 2-oxo-1-oxa-8 azaspiro[4,5]decane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： 2-OXO-1-OXA-8 AZASPIRO（4,5）癸烷衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5157038A
公开(公告)日：1992-10-20
申请号：US566274
申请日：1990-08-10
申请人： Edit Toth , Jozsef Torley , Bela Hegedus , Laszlo Szporny , Bela Kiss , Eva Palosi , Dora Groo , Istvan Laszlovszky , Erzsebet Lapis , Ferenc Auth , Laszlo Gaal
发明人： Edit Toth , Jozsef Torley , Bela Hegedus , Laszlo Szporny , Bela Kiss , Eva Palosi , Dora Groo , Istvan Laszlovszky , Erzsebet Lapis , Ferenc Auth , Laszlo Gaal
IPC分类号： A61K31/42 , A61K31/445 , A61K31/4465 , A61P3/00 , A61P25/00 , A61P43/00 , C07D211/48 , C07D491/10 , C07D491/107 , C07D491/113 , C07D493/10 , C07D498/10
CPC分类号： C07D491/10
摘要： The invention relates to novel 2-oxo-1-oxa-8-azaspiro[4,5]decane derivatives of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen; a C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the two latter two substituents optionally substituted on their aromatic moiety by one or more, same or different halogen, one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl group; or a tosyl group;R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group wherein R is as defined above, one of R.sup.1 and R.sup.2 m may represent a hydroxyl group and the other one is a methyl group; andR.sup.3 means hydrogen, benzyl, (C.sub.1-4 alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin-1-ylcarbonyl, 4-(2-hydroxethyl)piperazin-1-ylcarbonyl, 2-chloro-3-nicotinoylcarbamoyl or C.sub.1-6 alkylcarbamoyl group,as well as their acid addition and quaternary ammonium salts.

35. 发明授权

US5118687A 1-oxa-2-oxo-8-azaspiro(4,5)decane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： 1-OXA-2-OXO-8-AZASPIRO（4,5）十二烷衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5118687A
公开(公告)日：1992-06-02
申请号：US566275
申请日：1990-08-10
申请人： Edit Toth , Jozsef Torley , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Katalin Csomor , Mihaly Bodo , Judit Laszy , Zsolt Szentirmay
发明人： Edit Toth , Jozsef Torley , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Katalin Csomor , Mihaly Bodo , Judit Laszy , Zsolt Szentirmay
IPC分类号： A61K31/33 , A61K31/335 , A61K31/42 , A61K31/435 , A61K31/445 , A61P3/00 , A61P9/00 , A61P9/10 , A61P25/28 , C07D221/00 , C07D263/00 , C07D317/00 , C07D491/10 , C07D491/107 , C07D491/113 , C07D493/10 , C07D498/10
CPC分类号： C07D491/10
摘要： The invention relates to novel compounds 1-oxa-2-oxo-8- of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, a C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.10-4 alkyl group, the latter two groups are optionally substituted on their aromatic moiety by one or more, same or different halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group, wherein R is as defined above, one of R.sup.1 and R.sup.2 may represent a hydroxyl group whereas the other is a methyl group;R.sup.3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy or hydroxyl group(s);R.sup.4 means hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl or trihalomethyl group(s); andn is 1, 2 or 3as well as their acid addition and quaternary ammonium salts.

36. 发明授权

US4677109A 1-(6-(2'-substiuted-5', 6', 7', 8'-tetrahydro-4',-oxo-quinazolino))-3-4-dihydro-6,7-disubstituted-isoqui noline derivatives and pharmaceutical compostions containing them 失效
标题翻译： 1-（6-（2'-取代 - 5'，6'，7'，8'-四氢-4' - 氧代 - 喹唑啉））-3,4-二氢-6,7-二取代 - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4677109A
公开(公告)日：1987-06-30
申请号：US721807
申请日：1985-04-10
申请人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/505 , A61K31/535 , A61P25/04 , A61P25/08 , A61P29/00 , A61P39/02 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hdyroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is alky having from 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an optionally substiutted heterocyclic group,and acid addition and quaternary salts thereof.Compounds of the formula (I) are pharmaceutically active, in particular show spasmolytic, analgesic, antipyretic activity and have a protecting effect in acute alcoholic intoxication.
摘要翻译：本发明涉及新的1- [6-（2'-取代-5'，6'，7'，8'-四氢-4'-氧代 - 喹唑啉基）] - 3,4-二氢-6,7-二取代（I）的异喹啉衍生物其中R 1和R 2各自独立地表示具有1至6个碳原子的羟基或烷氧基，R 3是具有1至6个碳原子的烷基，任选取代的苯基，任选地在烷基部分或任选取代的杂环基中具有1至4个碳原子的取代烷基苯基，及其酸加成和季盐。式（I）的化合物是药学活性的，特别是显示解痉，镇痛，解热活性，并且在急性酒精中毒中具有保护作用。

37. 发明授权

US4668688A N-substituted isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： N-取代的异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4668688A
公开(公告)日：1987-05-26
申请号：US664770
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/47 , A61K31/472 , A61P1/04 , A61P25/04 , A61P29/00 , A61P37/06 , C07D217/16
CPC分类号： C07D217/16
摘要： The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的N-取代双（羟甲基） - 甲基 - 异喹啉衍生物，其中R1和R2代表羟基或具有1-6个碳原子的烷氧基，虚线是在1,2-位上的任选的双键，R3是具有1至6个碳原子的烷基或在烷基部分含有1至4个碳原子的芳烷基，或 - 如果1,2-二烷基中存在单键，位置 - 表示如果R 4是具有1至5个碳原子的烷基，具有1至4个碳原子的烷氧基，羟基，苯基或取代的苯基，其中X是氧的式“IMAGE”的基团; 如果R 4是-NH 2，-NH-C 1-4 - 烷基，-NH-C 3-6 - 环烷基，-NH-苯基或-NH-C 1-4 - 烷基 - 苯基，则X是氧或硫; 并且R 5和R 6独立地代表氢，具有1至4个碳原子的烷基或苯基，条件是它们中的至少一个不是苯基，及其盐。用于制备这些化合物和药物组合物的方法也在本发明的范围内。

38. 发明授权

US4654351A Bis(substituted methyl)-methyl-isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译：双（取代的甲基） - 甲基 - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4654351A
公开(公告)日：1987-03-31
申请号：US664849
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Gabor Motika , Attila Sohajda , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Gabor Motika , Attila Sohajda , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/47 , A61K31/472 , A61P1/04 , A61P9/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/06 , C07D217/14 , C07D217/16
CPC分类号： C07D217/16 , C07D217/14
摘要： The invention relates to new bis(substituted methyl)-methyl-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a ##STR2## group, in which R.sup.4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or --NH--phenyl,X is oxygen or sulfur,R.sup.7 is hydroxyl, halogen or an ##STR3## group, R.sup.8 is halogen, alkoxy from 1 to 4 carbon atoms or an ##STR4## group, in which X has the same meaning as defined above, andR.sup.9 independently from R.sup.4 may have the same meanings as defined for R.sup.4, or is an --NH(C.sub.1-4 -alkyl) or C.sub.3-6 -cycloalkyl group,and salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的新的双（取代的甲基） - 甲基 - 异喹啉衍生物，其中R 1和R 2表示羟基或具有1至6个碳原子的烷氧基，R 3是氢，具有烷基部分或其中R 4为具有1至5个碳原子的烷基，苯基，取代的苯基或-NH-苯基，X为氧或硫，R 7为羟基，卤素或一个基团，R 8为卤素，1至4个碳原子的烷氧基或一个基团，其中X具有与上述相同的含义，并且独立地为R 4的R 9可具有与R 4所定义相同的含义，或是-NH（C 1-4 - 烷基）或C 3-6 - 环烷基，及其盐。根据本发明的另一方面，提供了制备这些化合物的方法和含有它们的药物组合物。

39. 发明授权

US4605653A 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： 1-（羟基甲基）-1,6,7,11b-四氢-2H- 2H- [1,3]恶嗪基 - 或噻嗪并[4,3-a]异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4605653A
公开(公告)日：1986-08-12
申请号：US713533
申请日：1985-03-19
申请人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Attila Sohajda , Alajos Kalman , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Attila Sohajda , Alajos Kalman , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/535 , A61K31/54 , A61P1/12 , A61P9/08 , A61P25/08 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04
摘要： The invention relates to 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are alkoxy having from 1 to 6 carbon atoms,X is oxygen or sulfur,Y is .dbd.O, .dbd.S or an .dbd.NR.sup.3 group, whereinR.sup.3 is hydrogen, alkyl having from 1 to 6 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms or optionally substituted phenyl,and acid addition and quaternary salts thereof.
摘要翻译：本发明涉及式（I）的1-（羟甲基）-1,6,7,11b-四氢-2H，4H- [1,3]恶嗪基 - 或噻唑并〔4,3-a〕异喹啉衍生物，，其中R 1和R 2是具有1至6个碳原子的烷氧基，X是氧或硫，Y是= O，= S或= NR 3基团，其中R 3是氢，具有1至 6个碳原子，具有3至8个碳原子的环烷基或任选取代的苯基，及其酸加成盐和季盐。

40. 发明授权

US4481204A E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
标题翻译： E-Homo-eburnane衍生物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4481204A
公开(公告)日：1984-11-06
申请号：US509150
申请日：1983-06-29
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/22 , A61K31/395 , C07D459/00 , C07D461/00
CPC分类号： C07D471/22
摘要： The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.
摘要翻译：本发明涉及式/ I /，其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /，/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。新化合物是药学上活性的，例如它们的特定代表，特别是顺式的化合物显示出抗抑郁活性，而其它代表，特别是反式系列的化合物是有效的抗氧化剂。因此，式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。

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