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41. 发明授权

US4285865A Process for the preparation of halogenated 15-hydroxy-E-homoeburnane compounds 失效
标题翻译：制备卤代的15-羟基-E-高硼烷化合物的方法
公开(公告)号：US4285865A
公开(公告)日：1981-08-25
申请号：US175385
申请日：1980-08-05
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
IPC分类号： C07D461/00 , A61K31/4375 , A61P9/08 , C07D471/22 , C07D487/14 , C07D487/16
CPC分类号： C07D471/22
摘要： The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the general formula (Ia) and/or (Ib), ##STR1## wherin R is a C.sub.1-6 alkyl group and X is halogen, and acid addition salts thereof. These compounds are biologically active, furthermore they can be applied as intermediates in the synthesis of other pharmaceutically active substances.The compounds of the general formulae (Ia) and (Ib) are prepared by halogenating the respective racemic or optically active 15-hydroxy-E-homoeburnane derivative of the general formula (II), wherein R is as defined above. ##STR2##
摘要翻译：本发明涉及通式（Ia）和/或（Ib）的新的外消旋或光学活性的卤代的羟基 - 均聚乙二醇衍生物，其中R是 C 1-6烷基，X为卤素，及其酸加成盐。这些化合物是生物活性的，此外它们可以作为其它药物活性物质合成中的中间体使用。通式（Ia）和（Ib）的化合物通过卤化通式（II）的各自的外消旋或光学活性的15-羟基-E-高硼烷衍生物而制备，其中R定义如上。（二）

42. 发明授权

US6103724A 2-methoxyphenylpiperazine derivatives 失效
标题翻译： 2-甲氧基苯基哌嗪衍生物
公开(公告)号：US6103724A
公开(公告)日：2000-08-15
申请号：US284313
申请日：1999-04-27
申请人： Istvan Laszlovszky , Gyorgy Domany , Tibor Acs , Gyorgy Ferenczy , Csaba Szantay , Eszter Thuroczyne Kalman , Erzsebet Lapis , Ferenc Trischler , Bela Hegedus , Feranc Auth , Monika Csejtei , Egon Karpati , Bela Kiss , Judit Laszy , Margit Pellioniszne Paroczai , Adam Sarkadi , Sandor Szabo
发明人： Istvan Laszlovszky , Gyorgy Domany , Tibor Acs , Gyorgy Ferenczy , Csaba Szantay , Eszter Thuroczyne Kalman , Erzsebet Lapis , Ferenc Trischler , Bela Hegedus , Feranc Auth , Monika Csejtei , Egon Karpati , Bela Kiss , Judit Laszy , Margit Pellioniszne Paroczai , Adam Sarkadi , Sandor Szabo
IPC分类号： C07D241/00 , A61K31/496 , A61K31/519 , A61K31/542 , A61P25/18 , A61P25/22 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention relates to fused heterocyclic compounds with ring junction nitrogen atom of the formula: ##STR1## wherein Q stands for 2-indolizinyl, 2-imidazo[1,2-a]pyridinyl, 2-imidazo[1,2-a]pyrimidinyl, 6-(2,3-dihydroimidazo[2,1-b]thiazol)-yl or 6-imidazo[2,1-b]thiazolyl group; and n is an integer from 2 to 4, as well as therapeutically useful salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions. The compounds of formula (I) exhibit mainly antipsychotic effects so the invention relates also to a method of treatment of schizophrenia, organic mental disorders, affective disorders, anxiety and personality disorders.
摘要翻译： PCT No.PCT / HU97 / 00069 Sec。一九九九年四月二十七日 102（e）1999年4月27日PCT PCT 1997年10月22日PCT公布。第WO98 / 18797号公报日期：1998年5月7日本发明涉及具有下列通式的环连氮原子的稠合杂环化合物：其中Q代表2-中氮茚基，2-咪唑并[1,2-a]吡啶基，2-咪唑并[1,2-a] 嘧啶基，6-（2,3-二氢咪唑并[2,1-b]噻唑）基或6-咪唑并[2,1-b]噻唑基; 且n为2至4的整数，以及其治疗上有用的盐。本发明还涉及含有这些化合物的药物组合物以及制备上述化合物和组合物的方法。式（I）化合物主要表现为抗精神病作用，因此本发明还涉及治疗精神分裂症，有机精神障碍，情感障碍，焦虑和人格障碍的方法。

43. 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。

44. 发明授权

US4659816A Process for the preparation of dimeric alkaloids 失效
标题翻译：二聚生物碱的制备方法
公开(公告)号：US4659816A
公开(公告)日：1987-04-21
申请号：US688932
申请日：1985-01-04
申请人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
发明人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： A process is disclosed for the preparation of dimeric alkaloids of formula (II) ##STR1## wherein R stands for methyl or formyl, as well as acid addition salts thereof which comprises oxidizing the vinblastine of formula (III) ##STR2## with chromium (VI) oxide or bichromate or chromic acid alcohol ester in an inert solvent, converting the compound of formula (II), wherein R stands for methyl, so obtained to the acid addition salt and optionally further oxidizing the acid addition salt obtained with an oxidizing agent as defined above and optionally converting the compound of formula (II), wherein R stands for formyl, so obtained to the acid addition salt.
摘要翻译：公开了用于制备式（II）的二聚生物碱的方法，其中R代表甲基或甲酰基，以及其酸加成盐，其包括氧化式（III）的长春花碱（IMA） III）与惰性溶剂中的重铬酸铬（VI）或重铬酸盐或铬酸醇酯反应，将得到的式（II）化合物（其中R代表甲基）转化成酸加成盐，并任选地进一步氧化酸加成盐用如上定义的氧化剂获得，并任选地将所得到的式（II）化合物（其中R代表甲酰基）转化成酸加成盐。

45. 发明授权

US4746665A Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them 失效
标题翻译：长春花碱型双吲哚的硝基衍生物和含有它们的药物组合物
公开(公告)号：US4746665A
公开(公告)日：1988-05-24
申请号：US873537
申请日：1986-06-12
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor cs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor cs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a methyl or a formyl group;R.sub.2 stands for a hydroxy or ethyl group of .beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond;R.sub.5, R.sub.6 and R.sub.7 stand for a nitro group or hydrogen atom, with the proviso that simultaneously only one of them may stand for hydrogen atom; andY stands for --N.dbd. when R.sub.5 stands for a nitro group; whereasY stands for --NH-- when R.sub.5 stands for a hydrogen atom and a valence bond exists between the C.sub.2, and C.sub.7, atoms,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
摘要翻译：本发明涉及通式（I）的新型硝基衍生物（Ⅰ），其中R1代表甲基或甲酰基; R2代表β位的羟基或乙基; R3表示α-位的乙基; R4代表氢原子; 或R3和R4一起表示氧桥或双键; R5，R6和R7代表硝基或氢原子，条件是同时只有一个可以代表氢原子; 而Y代表-N =当R5代表硝基时; 而当R5表示氢原子且Y代表-NH-时，C2和C7原子之间存在价键，以及它们的酸加成盐和含有这些化合物的药物制剂。此外，本发明涉及一种制备这些化合物和制剂的方法。通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。

46. 发明授权

US4490378A N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment 失效
标题翻译： N-去甲基-N-（烯丙氧基甲基） - 长春花碱和抗白血病和抗病毒组合物和治疗方法
公开(公告)号：US4490378A
公开(公告)日：1984-12-25
申请号：US503791
申请日：1983-06-13
申请人： Lajos Dancsi , Tibor Keve , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor cs , Csaba Szantay , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Zsuzsanna Relle nee Somfa , Janos Sugar
发明人： Lajos Dancsi , Tibor Keve , Gyorgy Fekete , Eszter Dezseri , Sandor Gorog , Tibor cs , Csaba Szantay , Lajos Szabo , Katalin Honty , Sandor Eckhardt , Ivan Hindi , Sandor Kerpel-Fronius , Zsuzsanna Relle nee Somfa , Janos Sugar
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04 , Y10S514/908
摘要： The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a --CH.sub.2 --O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl,R.sup.4 is other than ethyl.These compounds and N-desmethyl-N-(ethoxymethyl)-vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH [III]Pharmaceutical compositions containing compounds of the general formula [I] as active ingredients are also within the scope of invention.
摘要翻译：本发明涉及新的细胞生长抑制化合物，其制备方法和含有它们的药物组合物。更具体地，提供了通式为“IMAGE”/ I /的新化合物，其中R 4是β-羟基和R 3是α-乙基; 或R4是氢，R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基，其中与> Na-CH 2 -O-基团连接的碳原子具有伯或二级构型或具有3至6个碳原子的烯基或炔基，或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基，R2是乙酰基，条件是如果R3是α-乙基和R4β-羟基，R4不是乙基。这些化合物和N-去甲基-N-（乙氧基甲基） - 长春花碱可以根据本发明通过将通式为“IMAGE”/ II /的化合物的化合物与大量过量的通式R' '-OH [III]含有通式[I]化合物作为活性成分的药物组合物也在本发明的范围内。

47. 发明授权

US4342871A Benzo(a)quinolizidine derivatives 失效
标题翻译：苯并（a）喹嗪啶衍生物
公开(公告)号：US4342871A
公开(公告)日：1982-08-03
申请号：US744608
申请日：1976-11-24
申请人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
发明人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
IPC分类号： C07D455/06 , C07D491/056 , C07D491/14 , C07D455/03 , A61K31/47
CPC分类号： C07D491/14 , C07D455/06
摘要： An antiphlogistic compound of the formula (I) ##STR1## or a pharmaceutically effective salt thereof wherein R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkoxy or together form a methylenedioxy group;R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n -R.sup.7 with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen;R.sup.7 is a carboxylic group or a carboxylic acid derivative group; n=0, 1 or 2, provided that if R.sup.3, R.sup.4 and R.sup.5 are hydrogen and R.sup.7 in the group R.sup.6 is cyano or alkoxycarbonyl, and n=1, then R.sup.1 and R.sup.2 are hydrogen, C.sub.2-4 alkoxy, or together form a methylenedioxy group.
摘要翻译：式（I）的消炎化合物（I）或其药学上有效的盐，其中R 1和R 2是氢或C 1-4烷氧基或一起形成亚甲二氧基; R3，R4，R5和R6是氢或式-CH2-（CH2）n-R7的基团，条件是R3，R4，R5和R6中的至少一个不是氢; R7是羧基或羧酸衍生物基团; n = 0,1或2，条件是如果R3，R4和R5是氢，R6中的R7是氰基或烷氧基羰基，n = 1，则R1和R2是氢，C2-4烷氧基或一起形成亚甲二氧基。

48. 发明授权

US4199505A Process for the preparation of alkaloids of the leurosine type 失效
标题翻译：制备柠檬酸类生物碱的方法
公开(公告)号：US4199505A
公开(公告)日：1980-04-22
申请号：US907626
申请日：1978-05-19
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Katalin Nogradi , Karola Jovanovics , Eszter Dezseri , Lajos Dancsi , Csaba Lorincz , Bela Szarvady , Lajos Kovacs
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Katalin Nogradi , Karola Jovanovics , Eszter Dezseri , Lajos Dancsi , Csaba Lorincz , Bela Szarvady , Lajos Kovacs
IPC分类号： A61K31/407 , A61K31/475 , A61P35/00 , C07D471/20 , C07D519/04
CPC分类号： C07D519/04
摘要： A process for the preparation of alkaloids of the leurosine type having the formula I ##STR1## and the acid addition salts thereof. In the formula I R is hydrogen or methyl. The compounds prepared according to the invention are known compounds showing cytostatic activity.
摘要翻译：一种制备具有式I（I）的黎明酪型生物碱及其酸加成盐的方法。在式I中R 1是氢或甲基。根据本发明制备的化合物是显示出细胞抑制活性的已知化合物。

49. 发明授权

US4757077A Bis-indole derivatives and pharmaceutical compositions containing them 失效
标题翻译：双吲哚衍生物和含有它们的药物组合物
公开(公告)号：US4757077A
公开(公告)日：1988-07-12
申请号：US873540
申请日：1986-06-12
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
摘要翻译：本发明涉及通式（I）的新的双吲哚衍生物：其中R1代表氢原子或乙酰基; R2代表氢原子; R3表示α-位的乙基; 或R2和R3一起表示氧桥; R4表示β-位的乙基或羟基; R5代表氢原子或羟基; A表示C 1-10直链或C 3-10支链烷基，羟基 - 烷基，乙酰基 - 烷基，苄基，C 3-6烯基或炔基或C 5-7环烷基或芳族基团或含杂芳基一个氮原子或一个氧原子，X代表氧或硫原子，以及它们的酸加成盐和含有这些化合物的药物制剂。此外，本发明涉及一种制备这些化合物和制剂的方法。通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。

50. 发明授权

US4102886A Process for the preparation of benzo(a)quinolizidine derivatives 失效
标题翻译：苯并（a）喹嗪衍生物的制备方法
公开(公告)号：US4102886A
公开(公告)日：1978-07-25
申请号：US624470
申请日：1975-10-21
申请人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
发明人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
IPC分类号： C07D455/06 , C07D491/056 , C07D491/14
CPC分类号： C07D491/14 , C07D455/06
摘要： A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.10 is a cyano or alkoxycarbonyl group.
摘要翻译：一种制备式I化合物或其盐的方法，其中R 1和R 2各自代表氢或C 1-4烷氧基，或一起形成亚甲二氧基; R 3，R 4，R 5和R 6相同或不同，为氢或式-CH 2 - （CH 2）n -R 7的基团，条件是至少有一个R 3，R 4，R 5和R 6不是氢; R7是羧基或羧酸衍生物基团; N = 0.1或2，其包含用有机仲胺反应式II化合物，并使由此得到的式III的N-胺反应，其中R 8和R 9各自表示C 1-5烷基，或者与相邻的氮原子一起形成可以含有另外的杂原子的5或6元杂环与式IV的化合物CH2 = CH-（CH2）n-R10（IV），其中R10是氰基或烷氧基羰基。

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