公开(公告)号：US5912245A

公开(公告)日：1999-06-15

申请号：US737273

申请日：1997-02-14

申请人： Endre Rivo ,  Szilveszter E. Vizi ,  Gabor Makara ,  Jozsef Reiter ,  Gabor Blasko ,  Gyula Simig ,  Laszlo Gaal ,  Marton Fekete

发明人： Endre Rivo ,  Szilveszter E. Vizi ,  Gabor Makara ,  Jozsef Reiter ,  Gabor Blasko ,  Gyula Simig ,  Laszlo Gaal ,  Marton Fekete

IPC分类号： A61K31/495 ,  A61P21/02 ,  A61P25/00 ,  A61P25/08 ,  C07D241/44 ,  C07D413/00 ,  A61K31/535 ,  C07D401/12

CPC分类号： C07D241/44

摘要： The present invention is directed to an acid amide of the formula ##STR1## wherein R.sup.1 represents hydrogen or nitro,R.sup.2 and R.sup.3 stand for, independently from each other, hydrogen, lower alkyl or lower alkenyl each optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated hetero-ring selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino; orR.sup.2 and R.sup.3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino, said heterocyclic group optionally carrying a hydroxy or a hydroxy-lower alkyl group; or apharmaceutically acceptable salt thereof; process of making and pharmaceutical compositions and methods of treating.

摘要翻译： PCT No.PCT / HU95 / 00015 Sec。 371日期1997年2月14日 102（e）日期1997年2月14日PCT提交1995年5月15日PCT公布。 公开号WO95 / 31443 日期：1995年11月23日本发明涉及下式的酰胺，其中R 1表示氢或硝基，R 2和R 3彼此独立地表示氢，低级烷基或低级烯基，各自任选地带有选自 由卤素，羟基，低级烷氧基，二（低级烷基）氨基，苯基 - 低级烷氧基羰基和选自哌啶子基，吡咯烷子基，哌嗪基和吗啉代的5-至6-元饱和杂环组成的基团。 或R 2和R 3与相邻的氮原子一起形成选自哌啶子基，吡咯烷子基，哌嗪子基和吗啉代的6元饱和杂环基，所述杂环基任选地带有羟基或羟基 - 低级烷基; 或其药学上可接受的盐; 制备方法和药物组合物和治疗方法。

公开(公告)号：US4831029A

公开(公告)日：1989-05-16

申请号：US116870

申请日：1987-11-05

申请人： Jozsef Reiter ,  Endre Rivo ,  Klara Reiter nee Esess ,  Marton Fekete ,  Frigyes Gogenyi ,  Lujza Petocz ,  Istvan Gacsalyi ,  Istvan Gyertyan

发明人： Jozsef Reiter ,  Endre Rivo ,  Klara Reiter nee Esess ,  Marton Fekete ,  Frigyes Gogenyi ,  Lujza Petocz ,  Istvan Gacsalyi ,  Istvan Gyertyan

IPC分类号： A61K31/505 ,  A61P23/02 ,  A61P25/02 ,  A61P25/20 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D487/14

摘要： The invention relates to condensed cyclic triazole derivatives of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof. The compounds of the general Formula I possess useful sedative and tranquillant properties and exhibit particularly spasmolytic, motility inhibiting, and narcosis potentiating, yohimbine potentiating and local anaesthetic and also weak reserpine ptosis inhibiting effect.

摘要翻译： 本发明涉及通式I（I）的缩合环状三唑衍生物及其药学上可接受的盐。 通式I的化合物具有有用的镇静和镇静特性，并且显示出特别的解痉，运动性抑制和麻醉增强，育亨宾加强和局部麻醉以及弱的利血平下垂抑制作用。

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。

公开(公告)号：US5597822A

公开(公告)日：1997-01-28

申请号：US443487

申请日：1995-05-18

申请人： Eniko Szirt nee Kislelly ,  Zoltan Budai ,  Tibor Mezei ,  Gabor Blasko ,  Klara Kazo nee Daroczi ,  Andras Egyed ,  Gabor Gigler ,  Marton Fekete ,  Klara Reiter nee Esses ,  Gyula Simig ,  Katalin Szemeredi

发明人： Eniko Szirt nee Kislelly ,  Zoltan Budai ,  Tibor Mezei ,  Gabor Blasko ,  Klara Kazo nee Daroczi ,  Andras Egyed ,  Gabor Gigler ,  Marton Fekete ,  Klara Reiter nee Esses ,  Gyula Simig ,  Katalin Szemeredi

IPC分类号： A61K31/15 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505

CPC分类号： A61K31/15 ,  A61K31/495

摘要： The invention refers to pharmaceutical compositions for the prevention and/or treatment of gastrointestinal diseases connected with infections caused by Helicobacter pylori and a method for the treatment of such diseases.The pharmaceutical composition of the invention comprises as active ingredient a cyclic ketone derivative of the formula I ##STR1## wherein and R.sup.1 mean independently hydrogen or halo;R.sup.0 stands for hydrogen or a C.sub.1-4 alkoxy group;R.sup.2 and R.sup.3 independently represent hydrogen; a straight or branched chain C.sub.1-8 alkyl optionally substituted by a dimethylamino group; a C.sub.2-6 alkenyl or a C.sub.3-7 cycloalkyl group; orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 6-membered heterocyclic group containing an additional nitrogen atom that may bear a phenyl group optionally substituted by a C.sub.1-4 alkoxy group;or its stereoisomer or optical isomer or a possible mixture thereof, or a pharmaceutically acceptable acid addition salt or quaternary ammonium salt thereof in admixture with carrier(s) commonly used in pharmaceutical compositions.

摘要翻译： 本发明涉及用于预防和/或治疗与由幽门螺杆菌引起的感染有关的胃肠道疾病的药物组合物和治疗这些疾病的方法。 本发明的药物组合物包含作为活性成分的式I（I）的环酮衍生物，其中R 1独立地表示氢或卤素; R0表示氢或C1-4烷氧基; R2和R3独立地表示氢; 任选被二甲基氨基取代的直链或支链C 1-8烷基; C 2-6烯基或C 3-7环烷基; 或者R 2和R 3与相邻的氮原子一起形成含有另外的氮原子的6元杂环基，其可以具有任选被C 1-4烷氧基取代的苯基; 或其立体异构体或光学异构体或其可能的混合物，或其药学上可接受的酸加成盐或季铵盐与药物组合物中通常使用的载体混合。

公开(公告)号：US5486528A

公开(公告)日：1996-01-23

申请号：US226089

申请日：1994-04-11

申请人： Judit Bajnogel ,  Gabor Blasko ,  Zoltan Budai ,  Eva Schmidt ,  Andras Egyed ,  Marton Fekete ,  Istvan Gacsalyi ,  Istvan Gyertyan ,  Tibor Mezei ,  Kalara Reiter nee Esses ,  Gyula Simig ,  Katalin Szemeredi ,  Enik Szirt nee Kiszelly

发明人： Judit Bajnogel ,  Gabor Blasko ,  Zoltan Budai ,  Eva Schmidt ,  Andras Egyed ,  Marton Fekete ,  Istvan Gacsalyi ,  Istvan Gyertyan ,  Tibor Mezei ,  Kalara Reiter nee Esses ,  Gyula Simig ,  Katalin Szemeredi ,  Enik Szirt nee Kiszelly

IPC分类号： A61K31/135 ,  A61K31/15 ,  A61K31/357 ,  A61K31/36 ,  A61K31/395 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/495 ,  A61P1/04 ,  A61P25/20 ,  C07C251/32 ,  C07C251/58 ,  C07D207/08 ,  C07D213/30 ,  C07D295/00 ,  C07D295/08 ,  C07D295/088 ,  C07D317/58 ,  C07D405/12 ,  C07C251/48

CPC分类号： C07D207/08 ,  C07C251/58 ,  C07D295/088 ,  C07C2101/02 ,  C07C2101/14

摘要： Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.

摘要翻译： 新型通式（I）的基本醚，其中R 1和R 2独立地为氢，卤素或C 1-4烷氧基，或一起它们代表3,4-亚甲二氧基，R代表C1-8烷基 ，R3代表氢，C1-4烷基或羟基，A是价键或亚甲基，R4和R5独立地是氢，C1-12烷基或C1-12烯基，或R4和R5与相邻的氮原子1一起形成 吡咯烷基，1-哌啶基，吗啉代或1-哌嗪基，立体和旋光异构体及其可能的混合物，其酸加成盐和季铵衍生物。 碱性醚具有抗溃疡和抗焦虑作用。

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。

公开(公告)号：US5478825A

公开(公告)日：1995-12-26

申请号：US261214

申请日：1994-06-15

申请人： Jozsef Reiter ,  Gabor Berecz ,  Gizella Zsila ,  Lujza Pet cz ,  Gabor Gigler ,  Marton Fekete ,  Maria Szecsey nee Heged s ,  Enik Szirt nee Kiszelly ,  Ludmila Rohacs nee Zamkovaja ,  Frigyes Gorgenyi ,  Margit Csorg

发明人： Jozsef Reiter ,  Gabor Berecz ,  Gizella Zsila ,  Lujza Pet cz ,  Gabor Gigler ,  Marton Fekete ,  Maria Szecsey nee Heged s ,  Enik Szirt nee Kiszelly ,  Ludmila Rohacs nee Zamkovaja ,  Frigyes Gorgenyi ,  Margit Csorg

IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D495/14 ,  A61K31/535 ,  A61K31/505

CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D495/14

摘要： The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.9 is alkyl substituted by alkoxy-carbonyl and possess inotropic and antianginal effects, complemented by antiinflammatory, ulcus, and gastric acid secretion inhibiting, and by weaker tranquillant, spasmolytic, and analgesic properties.

摘要翻译： 所公开的化合物具有式“IMAGE”，其中Q为6元饱和杂环基团或S（O）pR 3基团，其中p为0,1或2，R 3为烷基，烯基或苯基，其中 可以具有卤素或硝基取代基，或任选取代的苯基; 或NR4R5，其中R4和R5是氢，烷基，烯基，苯基 - 烷基或二 - 烷基 - 氨基 - 烷基; 或者一起形成基团（CH 2）n -Y-（CH 2）m，其中Y是CH 2或NR 6，其中R 6是苯基 - 烷基，n和m是0或1至5; Z是NR7R8，其中R7和R8各自是氢，烯基，环烷基，金刚烷基或苯基 - 烷基，其可以具有一个或多个取代基或一起形成（CH 2）j W-（CH 2）k的基团，其中j和k 各自为1至3，W为氧，CH 2，CHOH或NR 10，其中R 10为氢，烷氧基羰基或烷基，后者可以被取代。 - 或SR9，其中R9是被烷氧基 - 羰基取代的烷基，并且具有各向同性和抗心绞痛作用，由抗炎，溃疡和胃酸分泌抑制以及较弱的镇静剂，解痉药和镇痛药物补充。

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.

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：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.