公开(公告)号：US5240918A

公开(公告)日：1993-08-31

申请号：US857067

申请日：1992-03-24

申请人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

发明人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

IPC分类号： C07D277/18

CPC分类号： C07D277/18

摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.

摘要翻译： 本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物 适用于治疗疾病的组合物。 本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基 ，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或 二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与 进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。

公开(公告)号：US4665083A

公开(公告)日：1987-05-12

申请号：US726867

申请日：1985-04-25

申请人： Karoly Lempert ,  Gyula Hornyak ,  Ferenc Bartha ,  Gabor Doleschall ,  Jozsef Fetter ,  Jozsef Nyitrai ,  Gyula Simig ,  Karoly Zauer ,  Peter Huszthy ,  Antal Feller ,  Lujza Petocz ,  Eniko Szirt ,  Katalin Grasser ,  Edit Berenyi ,  Zsuzsanna Orr ,  Etelka Pjeczka

发明人： Karoly Lempert ,  Gyula Hornyak ,  Ferenc Bartha ,  Gabor Doleschall ,  Jozsef Fetter ,  Jozsef Nyitrai ,  Gyula Simig ,  Karoly Zauer ,  Peter Huszthy ,  Antal Feller ,  Lujza Petocz ,  Eniko Szirt ,  Katalin Grasser ,  Edit Berenyi ,  Zsuzsanna Orr ,  Etelka Pjeczka

IPC分类号： A61K31/425 ,  A61K31/426 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/24 ,  A61P25/26 ,  C07D277/12 ,  C07D277/18

CPC分类号： C07D277/18

摘要： The invention relates to novel iminothiazolidine derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.3 represent, independently from each other, hydrogen or lower alkyl group,R.sup.3 is nitro or amino group,R stands for halo, lower alkyl, haloalkyl, nitro, amino, hydroxy, lower alkoxy, carboxy or lower alkoxycarbonyl group, andn is 0, 1 or 2,and pharmaceutically acceptable acid addition salts thereof.The iminothiazolidine derivatives of the formula (I) possess valuable antidepressant, antiparkinsonic, antiepileptic and spasmolytic activities.

摘要翻译： 本发明涉及式（I）的新型亚氨基噻唑烷衍生物，其中R 1和R 3彼此独立地表示氢或低级烷基，R 3是硝基或氨基，R代表卤素，低级 烷基，卤代烷基，硝基，氨基，羟基，低级烷氧基，羧基或低级烷氧基羰基，n为0,1或2及其药学上可接受的酸加成盐。 式（I）的亚氨基噻唑烷衍生物具有有价值的抗抑郁药，抗帕金森病，抗癫痫和解痉作用。

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。

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。

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.

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。

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。

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。

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。

公开(公告)号：US4873249A

公开(公告)日：1989-10-10

申请号：US17090

申请日：1987-02-20

申请人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Katalin Sumeg nee Zukovics ,  Elemer Jakfalvi

发明人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Katalin Sumeg nee Zukovics ,  Elemer Jakfalvi

IPC分类号： C07D239/49 ,  A61K31/505 ,  A61P25/04 ,  A61P29/00

CPC分类号： A61K31/505 ,  Y10S514/825

摘要： The invention relates to pharmaceutical compositions having analgesic and/or anti-inflammatory effect comprising as active ingredient 2,4-diamino-5-(3,4-dimethoxy-benzyl)-pyrimidine or a pharmaceutically acceptable acid addition salt thereof.The pharmaceutical compositions of the present invention exhibit the desired analgesic and anti-inflammatory effect without causing undesired ulcerogenic side-effects.

摘要翻译： 本发明涉及包含作为活性成分2,4-二氨基-5-（3,4-二甲氧基 - 苄基） - 嘧啶或其药学上可接受的酸加成盐的镇痛和/或抗炎作用的药物组合物。 本发明的药物组合物显示出期望的止痛和抗炎作用，而不引起不希望的溃疡发生副作用。