专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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.

3. 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。

4. 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.

5. 发明授权

US4883798A Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US4883798A
公开(公告)日：1989-11-28
申请号：US221529
申请日：1988-07-20
申请人： Lujza Petocz , Istvan Simonyi , Ivan Beck , Gabor Gigler , Marton Fekete , Eniko Szirt nee Kiszelly , Attila Mandi , Frigyes Gorgenyi , Andras Dietz , Elemer Jakfalvi , Katalin Zukovics nee Sumeg , Klara Gado , Maria Hegedus
发明人： Lujza Petocz , Istvan Simonyi , Ivan Beck , Gabor Gigler , Marton Fekete , Eniko Szirt nee Kiszelly , Attila Mandi , Frigyes Gorgenyi , Andras Dietz , Elemer Jakfalvi , Katalin Zukovics nee Sumeg , Klara Gado , Maria Hegedus
IPC分类号： A61K31/505 , A61P25/04 , A61P29/00 , A61P43/00 , C07D239/49 , C07D405/06
CPC分类号： A61K31/505
摘要： The compounds of the general Formula I ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different and each stands for hydrogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy or phenyl-(C.sub.1-3 alkoxy), or R.sup.1 and R.sup.2 together form C.sub.1-2 alkylenedioxy; with the proviso that at least one of symbols R.sup.1 and R.sup.2 is other than hydrogen and with the further proviso that R.sup.1 and R.sup.2 can not represent 3,4-dimethoxy substitution) andtheir pharmaceutically acceptable acid addition salts exhibit useful analgesic, antipyretic, anti-inflammatory, anti-anginal and antioxidant effect.
摘要翻译：通式I的化合物（I）（其中R 1和R 2可以相同或不同，各自代表氢，羟基，C 1-6烷氧基，C 1-6烷氧基-C 1-6烷氧基，C 2-6 烯基氧基或苯基 - （C1-3烷氧基），或R1和R2一起形成C1-2亚烷基二氧基;条件是符号R1和R2中的至少一个不是氢，另外条件是R1和R2不能表示 3,4-二甲氧基取代）及其药学上可接受的酸加成盐显示出有用的镇痛，解热，抗炎，抗心绞痛和抗氧化作用。

6. 发明授权

US5130487A Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
标题翻译：氨基壬酸衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5130487A
公开(公告)日：1992-07-14
申请号：US572641
申请日：1991-08-27
申请人： Zoltan Budai , Tibor Mezei , Klara Reiter nee Esses , Eniko Sziri neKiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
发明人： Zoltan Budai , Tibor Mezei , Klara Reiter nee Esses , Eniko Sziri neKiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
IPC分类号： A61K31/15 , A61K31/133 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/445 , A61K31/452 , A61K31/495 , A61K31/55 , A61P1/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P25/02 , A61P25/04 , A61P25/20 , A61P29/00 , C07C249/08 , C07C249/12 , C07C251/58 , C07D213/16 , C07D251/58 , C07D295/08 , C07D295/088 , C07D317/56
CPC分类号： C07D213/16 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkylaminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6, acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要翻译：本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C1-12烷基，或R4和R5 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，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以带有羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其是任选取代的由苯基或苄基组成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。本发明还涉及制备这些化合物的方法。本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

7. 发明授权

US5234934A Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
标题翻译：氨基丙醇衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5234934A
公开(公告)日：1993-08-10
申请号：US876091
申请日：1992-04-30
申请人： Zoltan Budai , Klara Reiter nee Esses , Eniko Sziri nee Kiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
发明人： Zoltan Budai , Klara Reiter nee Esses , Eniko Sziri nee Kiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
IPC分类号： C07C251/58 , C07D213/16 , C07D295/088
CPC分类号： C07D213/16 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要翻译：本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C 1-12烷基，或R 4 和R5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，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以携带羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其任选地是由苯基或苄基构成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。本发明还涉及制备这些化合物的方法。本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

8. 发明授权

US5276030A Triazolyl thioamide derivates 失效
标题翻译：三唑基硫代酰胺衍生物
公开(公告)号：US5276030A
公开(公告)日：1994-01-04
申请号：US755219
申请日：1991-09-09
申请人： Josef Barkoczy , Josef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
发明人： Josef Barkoczy , Josef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P13/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
CPC分类号： C07D249/14
摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##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 alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom, with the proviso that if Q represents methylthio, dimethylamino, piperidino or morpholino, Y is other than benzyl,and pharmaceutically acceptable acid additional salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spasmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要翻译：本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR1的基团，其中R 1 代表包含1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基，Y 表示具有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基）或苯氧基 - （ C 1-4烷基），其任选在苯环上被带有含氮原子的杂环基的C 1-4烷基取代，条件是如果Q表示甲硫基，二甲基氨基，哌啶子基或吗啉代，则Y不是苄基，其酸加成盐。此外，本发明涉及一种制备这些化合物的方法。根据本发明的化合物具有镇静，抗抑郁，解痉，抗炎，止痛和抗静脉作用。

9. 发明授权

US5175163A Triazolyl thioamide derivates 失效
标题翻译：三唑氧化物衍生物
公开(公告)号：US5175163A
公开(公告)日：1992-12-29
申请号：US617126
申请日：1990-11-21
申请人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
发明人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P13/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
CPC分类号： C07D249/14
摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##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 alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl optionally bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom,and pharmaceutically acceptable acid addition salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spacmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要翻译：本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR 1的基团其中R1代表包括1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基基团，Y表示任选带有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基）或在苯环上被含有含有氮原子的杂环基的C 1-4烷基任选取代的苯氧基 - （C 1-4烷基）及其药学上可接受的酸加成盐。此外，本发明涉及一种制备这些化合物的方法。根据本发明的化合物具有镇静，抗抑郁，间质，抗炎，止痛和抗静脉作用。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式