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1.发明授权1,12-disubstituted octahydroindolo[2,3-]quinolizine derivatives, pharmaceutical compositions 失效1,12-二取代八氢吲哚并[2,3-]喹嗪衍生物，药物组合物
公开(公告)号：US4843080A
公开(公告)日：1989-06-27
申请号：US853353
申请日：1986-04-17
申请人： Csaba Szantay , Ferenc Soti , Maria Incze , Zsuzsanna Balogh nee Kardos , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Lilla Forgacs , Csaba Kuthi , Laszlo Szporny
发明人： Csaba Szantay , Ferenc Soti , Maria Incze , Zsuzsanna Balogh nee Kardos , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Lilla Forgacs , Csaba Kuthi , Laszlo Szporny
IPC分类号： A61K31/435 , A61P9/08 , C07D209/14 , C07D209/16 , C07D401/06 , C07D471/14
CPC分类号： C07D401/06 , C07D209/16 , C07D471/14
摘要： The invention relates to new racemic and optically active 1,12b-disubstituted octahydroindolo[2,3-a]quinolizine derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl,R.sup.3 and R.sup.5 are the same or different and represent hydrogen, alkyl having from 1 to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety,R.sup.4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, andR.sup.6 is an electron attracting substitutent, and cis and trans isomers and acid addition salts thereof.The compounds are pharmaceutically active, in particular show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.
摘要翻译： 本发明涉及式（I）的新的外消旋和旋光活性的1,12b-二取代八氢吲哚并[2,3-a]喹嗪衍生物其中R 1和R 2相同或不同并代表氢，卤素 ，硝基，具有1至6个碳原子的烷基，具有1至6个碳原子的烷氧基或羟基，R 3和R 5相同或不同，表示氢，具有1至6个碳原子的烷基或具有1至6个碳原子的芳烷基 烷基部分中的碳原子，R4是具有1至6个碳原子的烷基，在烷基部分具有1至6个碳原子的芳基或芳烷基，R6是吸电子取代基，顺式和反式异构体和酸加成盐 其中。 这些化合物是药学活性的，特别是显示出优异的心血管，例如。 选择性外周血管扩张活动。 这些化合物中的一些是制备其它药学活性化合物的有价值的中间体。
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2.发明授权Octahydroindolo[2,3-a]quinolizin-1-yl-alkanecarboxylic acid amines and their therapeutically useful acid addition salts, pharmaceutical compositions containing them and process for preparing same 失效八氢吲哚并[2,3-a]喹嗪酮-1-基 - 链烷羧酸胺及其治疗上有用的酸加成盐，含有它们的药物组合物及其制备方法
公开(公告)号：US4782052A
公开(公告)日：1988-11-01
申请号：US783911
申请日：1985-10-03
申请人： Ferenc Soti , Csaba Szantay , Maria Incze , Zsuzsanna Balogh nee Kardos , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos , Csaba Kuthi
发明人： Ferenc Soti , Csaba Szantay , Maria Incze , Zsuzsanna Balogh nee Kardos , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos , Csaba Kuthi
IPC分类号： C07D487/14 , A61K31/404 , A61K31/435 , A61K31/4375 , A61K31/454 , A61K31/475 , A61P1/04 , A61P9/06 , A61P9/08 , A61P21/02 , C07D209/04 , C07D221/00 , C07D471/14 , C07D471/22 , A61K31/55 , A61K31/535 , C07D471/04
CPC分类号： C07D471/14
摘要： The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds. The compounds of the formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.
摘要翻译： 本发明涉及式（I）的新的1,2,3,4,6,7,12,12b-八氢吲哚并[2,3-a]喹嗪-1-基 - 烷脒酰胺，
（I）其中R1和R2独立地代表氢或卤素原子，或羟基，硝基或C1-4烷氧基; R3和R4独立地表示氢原子或C1-4烷基; R5和R6独立地表示氢原子，C1-8烷基，C3-8烯基或环烷基，芳基或芳烷基，含氧，氮或硫原子的杂芳基或杂芳烷基，所有这些基团都可以被取代; 或R 5和R 6共同形成任选取代的C 2-8α，ω-亚烷基，其中一个碳原子可任选地被氧或氮原子代替; 和G表示C 1-4直链亚烷基，以及它们的治疗上合适的酸加成盐和含有这些化合物的药物组合物。 式（I）化合物具有有价值的治疗特性，即血管舒张，解痉，抗心律失常和胃肠保护作用。 胃肠保护作用尤其重要。 -
3.发明授权Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same 失效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。
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4.发明授权Nicotine compounds and analogs thereof, synthetic methods of making compounds, and methods of use 有权尼古丁化合物及其类似物，制备化合物的合成方法和使用方法公开(公告)号：US09440948B2
公开(公告)日：2016-09-13
申请号：US13819067
申请日：2011-09-02
申请人： William Reade Kem , Ferenc Soti , Anne Rouchaud , Hong Xing , Jon Lindstrom , Kristin Marie Andrud
发明人： William Reade Kem , Ferenc Soti , Anne Rouchaud , Hong Xing , Jon Lindstrom , Kristin Marie Andrud
IPC分类号： A61K31/465 , C07D401/04 , C07D401/12
CPC分类号： C07D401/04 , C07D401/12
摘要： Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2′substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2, compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2′substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.
摘要翻译： 本公开的实施方案提供了如图1所示的化合物。 1.1（化合物A，B，C和D），2'-取代的尼古丁化合物，氮杂环丁烷化合物，醚连接的尼古丁化合物（图1.2，化合物E，F，G和H），化合物的合成方法 使用化合物A，B，C，D，2'-取代的尼古丁化合物，氮杂环丁烷化合物或醚连接的尼古丁化合物治疗病症的方法，选择性刺激α7nAChR和/或α4β2受体的方法等。
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公开(公告)号：US08093269B2
公开(公告)日：2012-01-10
申请号：US11921832
申请日：2006-06-07
申请人： William R. Kem , Ferenc Soti
发明人： William R. Kem , Ferenc Soti
IPC分类号： C07D401/04 , A61K31/44
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.
摘要翻译： 本发明涉及对α7烟碱受体具有增强的选择性的3-亚芳基 - 酰胺基化合物的设计和合成。 预期这些化合物可用于治疗各种各样的病症，包括神经变性疾病如阿尔茨海默病，神经发育疾病如精神分裂症，以及由巨噬细胞浸润介导的某些外周位置的炎症。
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6.发明授权Materials and methods for inhibiting fouling of surfaces exposed to aquatic environments 有权防止暴露于水生环境的表面结垢的材料和方法公开(公告)号：US07087106B2
公开(公告)日：2006-08-08
申请号：US10783312
申请日：2004-02-19
申请人： William Reade Kem , Ferenc Soti , Dan Rittschof
发明人： William Reade Kem , Ferenc Soti , Dan Rittschof
IPC分类号： A01N43/40 , A01N443/42
摘要： The subject invention provides materials and methods for inhibiting the biofouling of surfaces exposed to aquatic environments. In one embodiment, the subject invention provides additives for marine paints and surface treatments. The subject invention further provides repellants and selective inhibitors for aquatic and/or terrestrial crustacean pests.
摘要翻译： 本发明提供了用于抑制暴露于水生环境的表面的生物污损的材料和方法。 在一个实施方案中，本发明提供了用于船用涂料和表面处理的添加剂。 本发明还提供了用于水生和/或陆生甲壳类害虫的驱避剂和选择性抑制剂。
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7.发明申请Materials and methods for inhibiting fouling of surfaces exposed to aquatic environments 有权防止暴露于水生环境的表面结垢的材料和方法公开(公告)号：US20050159454A1
公开(公告)日：2005-07-21
申请号：US11015361
申请日：2004-12-17
申请人： William Kem , Ferenc Soti , Dan Rittschof
发明人： William Kem , Ferenc Soti , Dan Rittschof
摘要： The subject invention provides materials and methods for inhibiting the biofouling of surfaces exposed to aquatic environments. In one embodiment, the subject invention provides additives for marine paints and surface treatments. The subject invention further provides repellants and selective inhibitors for aquatic and/or terrestrial crustacean pests.
摘要翻译： 本发明提供了用于抑制暴露于水生环境的表面的生物污损的材料和方法。 在一个实施方案中，本发明提供了用于船用涂料和表面处理的添加剂。 本发明还提供了用于水生和/或陆生甲壳类害虫的驱避剂和选择性抑制剂。
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公开(公告)号：US09233109B2
公开(公告)日：2016-01-12
申请号：US13642907
申请日：2011-04-22
IPC分类号： A61K31/444 , A61K31/44 , A61K31/4995 , A61K45/06 , A61K31/445
CPC分类号： A61K31/4995 , A61K31/44 , A61K31/444 , A61K31/445 , A61K45/06 , A61K2300/00
摘要： Briefly described, embodiments of this disclosure, among others, include compositions, pharmaceutical compositions, methods of treating nicotine dependence, methods of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorder, method of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorders, and the like.
摘要翻译： 简要描述，本公开的实施方案包括组合物，药物组合物，治疗尼古丁依赖的方法，治疗吸烟的受试者和具有抑郁或其它神经精神障碍风险的方法，治疗吸烟的受试者的方法 抑郁症或其他神经精神障碍的风险等。
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公开(公告)号：US08592458B2
公开(公告)日：2013-11-26
申请号：US13328841
申请日：2011-12-16
申请人： William Reade Kem , Ferenc Soti
发明人： William Reade Kem , Ferenc Soti
IPC分类号： C07D401/14 , A61K31/44
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.
摘要翻译： 本发明涉及对α7烟碱受体具有增强的选择性的3-亚芳基 - 酰胺基化合物的设计和合成。 预期这些化合物可用于治疗各种各样的病症，包括神经变性疾病如阿尔茨海默病，神经发育疾病如精神分裂症，以及由巨噬细胞浸润介导的某些外周位置的炎症。
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公开(公告)号：US20130137697A1
公开(公告)日：2013-05-30
申请号：US13642907
申请日：2011-04-22
IPC分类号： A61K31/4995 , A61K31/444
CPC分类号： A61K31/4995 , A61K31/44 , A61K31/444 , A61K31/445 , A61K45/06 , A61K2300/00
摘要： Briefly described, embodiments of this disclosure, among others, include compositions, pharmaceutical compositions, methods of treating nicotine dependence, methods of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorder, method of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorders, and the like.
摘要翻译： 简要描述，本公开的实施方案包括组合物，药物组合物，治疗尼古丁依赖的方法，治疗吸烟的受试者和具有抑郁或其它神经精神障碍风险的方法，治疗吸烟的受试者的方法 抑郁症或其他神经精神障碍的风险等。
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