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1. 发明授权

US5523303A Trisubstituted cycloalkane derivatives and process for the preparation thereof 失效
标题翻译：三取代环烷烃衍生物及其制备方法
公开(公告)号：US5523303A
公开(公告)日：1996-06-04
申请号：US226051
申请日：1994-04-11
申请人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
发明人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P1/04 , C07C249/12 , C07C251/58 , C07D295/08 , C07D295/088 , C07D317/58
CPC分类号： C07D295/088 , C07C251/58 , C07C2101/08 , C07C2101/14 , C07C2101/18 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.1-4 alkoxy, or together represent a 3,4-methylenedioxy group,n is an integer from 2 to 5,A represents a valency bond or a --CH.sub.2 -- group.The compounds exert a valuable antiulcer effect, so they can be used to advantage in the therapy.
摘要翻译：本发明涉及新颖的药学活性三取代环烷烃衍生物，其制备方法和包含其的药物组合物。本发明还包括所述环烷烃衍生物用于治疗疾病和制备适于治疗疾病的药物组合物的用途。根据本发明的化合物的特征在于通式（I），其中R表示氢，C 1-4烷基或羟基，R 1表示C 1-12烷基，R 2和R 3各自表示氢，C 1 -12烷基或C2-12烯基，或R2和R3与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4-至7-元环，后者可以携带苯基，苄基或C1 -4-烷基取代基，R4和R5各自代表氢，卤素或C1-4烷氧基，或一起代表3,4-亚甲二氧基，n是2至5的整数，A表示价键或-CH 2 - 组。这些化合物具有有价值的抗溃疡作用，因此可用于治疗。

2. 发明授权

US5135928A Triazolo derivatives and process for their preparation 失效
标题翻译： TRIAZOLO衍生物及其制备方法
公开(公告)号：US5135928A
公开(公告)日：1992-08-04
申请号：US604486
申请日：1990-10-25
申请人： Jozsef Reiter , Jozsef Barkoczy , Lujza Petocz , Frigyes Gorgenyi , Marton Fekete , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan , Klara Reiter nee Esses
发明人： Jozsef Reiter , Jozsef Barkoczy , Lujza Petocz , Frigyes Gorgenyi , Marton Fekete , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan , Klara Reiter nee Esses
IPC分类号： A61K31/41 , A61K31/50 , A61K31/535 , A61K31/55 , A61P9/08 , A61P9/10 , A61P29/00 , C07D249/14 , C07D403/04 , C07D405/12 , C07D413/04 , C07D487/04
CPC分类号： C07D405/12 , C07D249/14 , C07D487/04
摘要： This invention relates to novel triazolo derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said triazolo derivatives for the treatment of diseases and also for the preparation of pharmaceutical compositions suitable for the treatment of the said diseases.The new triazolo derivatives of the general formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s); or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl); or q represents a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chain C.sub.1-12 alkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-4 alkyl);R.sup.4 and R.sup.7 each represent hydrogen, C.sub.1-6 alkyl or phenyl-(C.sub.1-4 alkyl) optionally bearing one or more halogen substituent(s);R.sup.5 and R.sup.6 each stand for C.sub.1-4 alkyl optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a heterocyclic group or a phenyl group optionally bearing one or more halogen, hydroxyl, cyano, nitro, alkyl, methylene dioxy and carbamoylmethoxy, di-(C.sub.1-4 alkyl)-amino or C.sub.1-4 alkoxy substituent(s) which latter may carry a di-(C.sub.1-4 alkyl)-amino group; furthermore one of R.sup.5 and R.sup.6 may represent hydrogen, orR.sup.5 and R.sup.6 together stand for C.sub.4-15 alkylene, or together with the adjacent carbon atom they are attached to form a heterocyclic group bearing a phenyl(C.sub.1-4 alkyl) substituent,possess valuable antianginal and tranquillant/sedative properties and are useful in therapy.

3. 发明授权

US4965259A Dioxazocine derivatives compositions and methods containing them having antidepressive, spasmolytic, anticonvulsive, and antiarrhythmic properties 失效
标题翻译：二恶唑辛衍生物组合物和含有它们的方法具有抗抑郁，解痉，抗惊厥和抗心律失常性质
公开(公告)号：US4965259A
公开(公告)日：1990-10-23
申请号：US292450
申请日：1988-12-30
申请人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Marton Fekete , Maria Szecsey nee Hegedus , Gabor Gigler , Istvan Gacsalyi
发明人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Marton Fekete , Maria Szecsey nee Hegedus , Gabor Gigler , Istvan Gacsalyi
IPC分类号： A61K31/357 , A61K31/395 , A61P9/06 , A61P21/02 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , C07D273/00 , C07D273/01
CPC分类号： C07D273/00
摘要： Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,R.sub.2 represents alkyl having from 1 to 4 carbon atoms, andn is equal to 0 or 1,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.Two different reactions are described for making these compounds. They can be formulated into pharmaceutical compositions in the usual manner and exhibit central nervous system affecting activities.
摘要翻译：二恶唑辛衍生物及其制备方法和含有它们的组合物，所述衍生物由式I（I）表示，其中R 1表示氢或具有1至4个碳原子的烷基，R 2表示具有1至4个碳原子的烷基，以及 n等于0或1，并且其药学上可接受的酸加成盐与无机或有机酸形成。描述了制备这些化合物的两种不同的反应。它们可以以通常的方式配制成药物组合物，并显示中枢神经系统影响活性。

4. 发明授权

US4939142A Substituted styrene derivatives 失效
标题翻译：取代苯乙烯衍生物
公开(公告)号：US4939142A
公开(公告)日：1990-07-03
申请号：US301944
申请日：1989-01-26
申请人： Zoltan Budai , Lujza Petocz , Tibor Mezei , Eniko Szirt nee Kiszelly , Maria Szecsey nee Hegedus , Gabor Gigler , Klara Reiter nee Esses , Aranka Lay nee Konya , Eva Furdyga , Istvan Gertyan , Istvan Gacsalyi
发明人： Zoltan Budai , Lujza Petocz , Tibor Mezei , Eniko Szirt nee Kiszelly , Maria Szecsey nee Hegedus , Gabor Gigler , Klara Reiter nee Esses , Aranka Lay nee Konya , Eva Furdyga , Istvan Gertyan , Istvan Gacsalyi
IPC分类号： A61K31/15 , A61K31/357 , A61K31/36 , A61K31/40 , A61P1/04 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C249/04 , C07C249/08 , C07C251/44 , C07C251/58 , C07D295/08 , C07D295/088 , C07D317/58
CPC分类号： C07D295/088 , C07C251/44 , C07C2101/16
摘要： The new compounds of the general Formula I ##STR1## (wherein A stands for a C.sub.2-4 straight or branched chain alkylene group;R.sup.1 and R.sup.2 may be same or different and each stands for hydrogen, halogen, lower alkyl or lower alkoxy; orR.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 and R.sup.4 may be the same or different and each stands for C.sub.1.ident. alkyl or C.sub.3.notident. cycloalkyl orR.sup.3 and R.sup.4 together with the nitrogen atom, they are attached to, form a 4-7 membered ring which may contain as additional ring member an oxygen or sulfur atom or a further nitrogen atom and the latter nitrogen atom may optionally bear a C.sub.1-3 alkyl or benzyl substituent)and pharmaceutically acceptable acid addition salts and quaternary ammonium salts thereof possess valuable therapeutical properties and exert particularly useful transquillant-sedative, antidepressant, antiepileptic, antiparkinson, analgesic, local anaesthetic, gastric acid secretion inhibiting and/or antianginal effect.The new compounds of the general Formula I may be prepared by methods known per se.
摘要翻译：通式I的新化合物（I）（其中A代表C2-4直链或支链亚烷基; R1和R2可以相同或不同，代表氢，卤素，低级烷基或低级）烷氧基;或R 1和R 2一起形成亚甲二氧基; R 3和R 4可以相同或不同，并且各自代表C 1 =烷基或C 3或C 6的环烷基或R 3和R 4与氮原子一起形成4个 -7元环，其可以含有氧或硫原子或另外的氮原子作为附加的环成员，后一个氮原子可以任选地带有C 1-3烷基或苄基取代基）及其药学上可接受的酸加成盐和季铵盐具有有价值的治疗性质，并且发挥特别有用的抗惊孕药，抗抑郁药，抗癫痫药，抗帕金森，止痛剂，局部麻醉剂，胃酸分泌抑制和/或抗心绞痛作用。通式I的新化合物可以通过本身已知的方法制备。

5. 发明授权

US4303660A Pyrazolo[1,5-c]quinazoline derivatives and analgesic compositions containing them 失效
标题翻译：吡唑并[1,5-c]喹唑啉衍生物和含有它们的镇痛组合物
公开(公告)号：US4303660A
公开(公告)日：1981-12-01
申请号：US150349
申请日：1980-05-16
申请人： Edit Berenyi nee Poldermann , Eniko Szirt nee Kiszelly , Peter Gorog , Lujza Petocz , Ibolya Kosoczky , Agnes Kovacs nee Palotai , Gabriella rmos nee Lassu
发明人： Edit Berenyi nee Poldermann , Eniko Szirt nee Kiszelly , Peter Gorog , Lujza Petocz , Ibolya Kosoczky , Agnes Kovacs nee Palotai , Gabriella rmos nee Lassu
IPC分类号： A61K31/4162 , A61K31/4745 , A61K31/505 , A61K31/519 , A61P1/00 , A61P1/04 , A61P25/04 , A61P29/00 , C07D231/16 , C07D487/04
CPC分类号： C07D487/04 , C07D231/16
摘要： The invention relates to novel pyrazolo[1,5-c]quinazoline derivatives of the general formula I ##STR1## wherein R represents a hydrogen atom, a C.sub.1-4 alkyl group or an acyl group,R.sub.1 represents a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.2-4 alkenyl group, an aralkyl group, wherein the alkyl group has 1 to 4 carbon atoms, a phenylalkenyl group, wherein the alkenyl group has 2 to 4 carbon atoms, furthermore a carboxy group or a phenyl group optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy, nitro or di(C.sub.1-4 alkyl)amino groups, orR and R.sub.1 may form together a valence bond,R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl or a phenyl group, orR.sub.1 and R.sub.2 may form together a C.sub.2-7 alkylene group,R.sub.3 represents a nitro group, an amino group, an alkylamino group, a dialkylamino group, wherein the alkyl groups have 1 to 4 carbon atoms, an alkylideneimino group, wherein the alkylidene group has 1 to 4 carbon atoms, a benzylideneimino group or an acylamino group,and pharmaceutically acceptable acid addition salts thereof.The novel compounds of the general formula I can be employed primarily as analgesic agents.
摘要翻译：本发明涉及通式I（XIX）的新颖的吡唑并[1,5-c]喹唑啉衍生物，其中R表示氢原子，C1-4烷基或酰基，R1表示氢原子， C1-12烷基，C3-8环烷基，C2-4烯基，其中烷基具有1至4个碳原子的芳烷基，苯基烯基，其中烯基具有2至4个碳原子此外，羧基或任选被一个或多个选自卤素，羟基，C 1-4烷氧基，硝基或二（C 1-4烷基）氨基的取代基取代的苯基，或R和R 1可以一起形成价键，R2表示氢原子，C1-4烷基或苯基，或R1和R2可以一起形成C2-7亚烷基，R3表示硝基，氨基，烷基氨基，二烷基氨基基团，其中烷基具有1至4个碳原子，亚烷基亚氨基，其中亚烷基具有1至4个碳 n原子，亚苄基亚氨基或酰氨基，及其药学上可接受的酸加成盐。通式I的新化合物可以主要用作止痛剂。

6. 发明授权

US5439940A Benz[e]indene derivatives 失效
标题翻译：苯并[e]茚衍生物
公开(公告)号：US5439940A
公开(公告)日：1995-08-08
申请号：US141954
申请日：1993-10-28
申请人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
发明人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/16 , A61K31/335 , A61K31/336 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/495 , A61P25/04 , A61P25/20 , A61P29/00 , C07C13/547 , C07C249/04 , C07C251/58 , C07C269/02 , C07C271/60 , C07D209/48 , C07D213/74 , C07D239/24 , C07D239/34 , C07D241/04 , C07D295/08 , C07D295/088 , C07D303/12 , C07D401/02 , C07D401/04 , C07C251/54
CPC分类号： C07D209/48 , C07C251/58 , C07C271/60 , C07D213/74 , C07D239/34 , C07D295/088 , C07D303/12 , C07C2101/02 , C07C2101/14 , C07C2103/16
摘要： The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; orA represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, whereinR.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; andR denotes hydrogen or C.sub.1-7 alkyl,stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.
摘要翻译：本发明涉及新的药学活性苯并[e]茚衍生物，其制备方法，包含其的药物组合物，进一步使用所述苯并[e]茚衍生物在某些疾病的治疗中以及在制备适于治疗所述疾病的药物组合物。根据本发明的新的苯并[e]茚衍生物对应于通式（I）其中A表示式alk-NR1R2的基团，其中alk表示任选携带羟基取代基的C 2-7亚烷基， R1和R2独立地是氢，C1-7烷基，C2-7烯基，C2-7炔基，单（C1-7）烷基氨基（C1-7）烷基，二（C1-7）烷基氨基（C1-7）烷基或 C3-7环烷基; 或R 1和R 2与它们所连接的氮原子一起形成4至7元环，任选地包含氧原子或另外的氮原子，后者可以携带苯基，苄基，吡啶基，嘧啶基或C 1-3烷基取代基，其取代基又可以具有羟基或甲氧基或卤素原子或卤代苯基; 或R 1和R 2与它们所连接的氮原子一起形成苯二甲酰亚氨基; 或A表示嘧啶基，2,3-环氧丙基或式-C（O）NHR 3的基团，其中R 3表示C 1-7烷基，C 2-7烯基或C 3-8环烷基; R表示氢或C 1-7烷基，立体异构体和旋光异构体及其可能的混合物，这些化合物的其它酸加成盐和季铵衍生物。

7. 发明授权

US5225410A Triazolyl hydrazide derivatives 失效
标题翻译：三唑氢化合物衍生物
公开(公告)号：US5225410A
公开(公告)日：1993-07-06
申请号：US604488
申请日：1990-10-25
申请人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Frigyes Gorgenyi , Marton Fekete , Eniko Szirt nee Kiszelly , Maria Szecsey nee Hegedus , Istvan Gacsalyi , Istvan Gyertyan
发明人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Frigyes Gorgenyi , Marton Fekete , Eniko Szirt nee Kiszelly , Maria Szecsey nee Hegedus , Istvan Gacsalyi , Istvan Gyertyan
IPC分类号： A61K31/41 , A61K31/50 , A61K31/55 , A61P1/04 , A61P9/08 , A61P9/10 , C07D249/14 , C07D403/04 , C07D413/04
CPC分类号： C07D249/14
摘要： This invention relates to novel triazolyl hydrazide derivatives and a process for the preparation thereof.The new triazolyl hydrazide derivatives of the general formula (I). ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group; or a group of general formula SR.sup.1, whereinR.sup.1 stands for C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl) optionally substituted by halogen, C.sub.1-4 alkyl or nitro substitute therefor substituents; or Q represents a group of the formula NR.sup.2 R.sup.3, wherein R.sup.2 and R.sup.3 each represents hydrogen, straight or branched chain C.sub.1-6 alkyl or C.sub.2-6 alkenyl;Z represents hydrogen or a group of the formula (C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, whereinX stands for oxygen or sulfur,R.sup.4, R.sup.5 and R.sup.6 each stand for hydrogen or C.sub.1-4 alkyl;R.sup.7 stands for hydrogen, C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl) optionally substituted by one or more halogen atom(s) or an amino group optionally substituted by one or two C.sub.1-4 alkyl substituents,R.sup.8 stands for hydrogen or a group of the formula --(C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, wherein X, R.sup.4, R.sup.5 and R.sup.6 are as stated above,with the proviso that if Z represents a group of the formula --(C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, R.sup.8 stands for hydrogen, and if Z represents hydrogen, R.sup.8 stands for a group of the formula (C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, and pharmaceutically acceptable acid addition salts thereof excert valuable antianginal and/or gastric ulcer inhibiting properties and are useful in therapy.

8. 发明授权

US4395413A Oxime ethers and pharmaceutical compositions containing the same 失效
标题翻译：肟醚和含有它的药物组合物
公开(公告)号：US4395413A
公开(公告)日：1983-07-26
申请号：US162674
申请日：1980-06-24
申请人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
发明人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
IPC分类号： A61K31/15 , A61K31/495 , A61P25/04 , C07C67/00 , C07C239/00 , C07C249/10 , C07C251/58 , C07D295/02 , C07D295/088 , C07D295/08
CPC分类号： C07D295/088 , Y10S514/926 , Y10S514/927
摘要： The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.N--OH group with an aminoalkyl derivative of the general formula /III/ ##STR3## wherein R, R.sup.1 and A have the same meaning as stated above andZ means a halogen atom or a H.sub.2 N--O-- group or a salt thereof in the presence of a basic condensing agent.The new compounds of the general formula /I/ possess valuable nicotine-lethality inhibiting, local anaesthetic, analgesic effects, which are, in case of certain compounds, complemented by anti-hypertensive, maximum electroshock and tetracorspasm inhibiting, ulcus inhibiting and motility inhibiting effects, and can be applied to advantage in the therapy.
摘要翻译：本发明涉及通式I I的新型肟醚及其酸加成盐和季铵衍生物，其中A表示C2-6直链或支链亚烷基链，R和R1各自表示C1 -6烷基，或者它们与相邻的氮原子一起与含有4至7个碳原子的杂环和任选的另外的杂原子（即氧，硫或氮原子）一起形成，并且所述环可以任选地被C 1-3 烷基，苯基或苄基，R2和R3各自表示氢原子或一起形成价键，R4表示C1-10烷基或C2-10烯基，n表示3至7的整数。根据本发明通过使通式/ II / IMAGE / II /的环烷烃衍生物与其中R2，R3，R4和n具有与上述相同的含义反应制备通式/ I / I，而Y表示氧或硫原子或a =具有氨基烷基衍生物的N-OH基团通式/ III / / III /其中R，R 1和A具有与上述相同的含义，Z表示在碱性缩合剂存在下的卤素原子或H 2 N-O-基或其盐。新型化合物/ I /具有有价值的尼古丁杀伤力抑制，局部麻醉，止痛作用，在某些化合物的情况下，补充有抗高血压，最大电休克和四疣抑制作用，抑制溃疡和运动抑制作用，并且可以在治疗中有利地应用。

9. 发明授权

US4727074A 2-(phenylmethylene)-1-(diaminoalkoxy) cycloalkanes and their pharmaceutical uses 失效
标题翻译： 2-（苯基亚甲基）-1-（二氨基烷氧基）环烷烃及其药物用途
公开(公告)号：US4727074A
公开(公告)日：1988-02-23
申请号：US578286
申请日：1984-02-08
申请人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
发明人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61P9/06 , A61P23/00 , A61P25/04 , C07C67/00 , C07C239/00 , C07C251/44 , C07C251/58 , C07D295/088 , A61K31/495 , A61K31/205 , C07C131/02
CPC分类号： C07D295/088
摘要： The invention relates to selected stereoisomers having the E, E or E, Z configuration and within the Formula (I) ##STR1## wherein N is 2-4, A is alkylene or 2 or 3 carbon atoms, R is phenyl or substituted phenyl and R.sup.1 and R.sup.2 are lower alkyl, or, together with the carbon to which attached, form a heterocyclic ring; and pharmaceutically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions comprising the same.The compounds of the general formula (I) can be used in therapy due to their narcosis potentiating, analgesic and antiarrhythmial effect.
摘要翻译：本发明涉及具有E，E或E，Z构型的选定的立体异构体，并且在其中N为2-4的式（I）中，A为亚烷基或2或3个碳原子，R为苯基或取代的苯基，R 1和R 2为低级烷基，或与连接的碳一起形成杂环; 及其药学上可接受的酸加成盐，其制备方法和包含其的药物组合物。通式（I）的化合物可以用于治疗，因为它们具有麻醉增效，止痛和抗心律失常作用。

10. 发明授权

US4324894A Aminoisoquinoline derivatives 失效
标题翻译：氨基异喹啉衍生物
公开(公告)号：US4324894A
公开(公告)日：1982-04-13
申请号：US138843
申请日：1980-04-10
申请人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
发明人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61P25/00 , A61P25/04 , C07D217/22 , C07D217/24 , C07D401/12 , C07D413/04 , C07D403/14
CPC分类号： C07D217/22 , C07D217/24
摘要： Novel aminoisoquinoline derivatives of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.2 represents a hydrogen atom,R.sub.3 represents a hydrogen atom,R.sub.4 represents a morpholinyl group or a piperazinyl group substituted with a pyridyl group, andpharmaceutically acceptable acid addition salts and quaternary derivatives thereof have been prepared. The novel compounds exert narcosis potentiating effects.
摘要翻译：通式（I）的新型氨基异喹啉衍生物其中R 1表示氢原子或C 1-4烷基，R 2表示氢原子，R 3表示氢原子，R 4表示吗啉基或哌嗪基已经制备了被吡啶基取代的基团，以及其药学上可接受的酸加成盐和其季衍生物。新型化合物发挥麻醉加强作用。

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