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：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：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：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。

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：US5064826A

公开(公告)日：1991-11-12

申请号：US487412

申请日：1990-03-02

申请人： Klara Reiter nee Esses ,  Jozsef Reiter ,  Zoltan Budai ,  Endre Rivo ,  Peter Trinka ,  Lujza Petocz ,  Gabor Gigler ,  Istvan Gyertyan ,  Istvan Gacsalyi

发明人： Klara Reiter nee Esses ,  Jozsef Reiter ,  Zoltan Budai ,  Endre Rivo ,  Peter Trinka ,  Lujza Petocz ,  Gabor Gigler ,  Istvan Gyertyan ,  Istvan Gacsalyi

IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  A61P29/00 ,  C07D249/14 ,  C07D495/14

CPC分类号： C07D495/14

摘要： This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.

摘要翻译： 本发明涉及式（Ia）和（Ib）的新型三唑并嘧啶衍生物，其中Q表示氢，任选被C 1-4烷基取代并含有一个或多个氧和/ 或氮原子或式-SR1的基团，其中R 1是烷基或芳烷基，或式-NR 2 R 3基团，其中R 2和R 3独立地是氢，烷基，烯基，环烷基，芳烷基，芳基或杂环基，m和n是 独立地0,1,2,3或4，条件是如果m代表0，则n不同于0，并且如果n和m都是1或m代表0并且n是2，则Q不同 甲硫基或吗啉代基，它们的混合物或药学上可接受的盐。 此外，本发明涉及一种制备这些化合物的方法。 式（Ia）和（Ib）的化合物能够抑制由丁苯那嗪引起的下垂并具有止痛活性。

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：US5473072A

公开(公告)日：1995-12-05

申请号：US274848

申请日：1994-07-14

申请人： Tibor Mezei ,  Gabor Blasko ,  Zoltan Budai ,  Margit Csorgo ,  Eva Furdyga ,  Imre Klebovich ,  Laszlo Koncz ,  Ilona Sztruhar ,  Attila Mandi ,  Kalman Nagy ,  Klara Reiter nee Esses ,  Gyula Simig ,  Judit Szego ,  Gyongyi Vereczkey nee Donath

发明人： Tibor Mezei ,  Gabor Blasko ,  Zoltan Budai ,  Margit Csorgo ,  Eva Furdyga ,  Imre Klebovich ,  Laszlo Koncz ,  Ilona Sztruhar ,  Attila Mandi ,  Kalman Nagy ,  Klara Reiter nee Esses ,  Gyula Simig ,  Judit Szego ,  Gyongyi Vereczkey nee Donath

IPC分类号： C07D401/14 ,  A61K31/445 ,  A61K31/505 ,  A61P25/20 ,  B01J23/44 ,  B01J25/02 ,  C07B61/00 ,  C07D221/20 ,  C07D239/00 ,  C07D241/00 ,  C07D295/00 ,  C07D401/12 ,  C07D403/04

CPC分类号： C07D401/12

摘要： Process for the preparation of 8 -[4 -[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione (buspiron) of the Formula I ##STR1## and the hydrochlorides thereof having high purity by continuously adding a solution of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-but-2 -inyl]-8-aza-spiro[4.5]decane-7,9-dione of the formula II ##STR2## formed with an inert organic solvent having a concentration of at least 40% by weight to a suspension of a hydrogenation catalyst in an inert organic solvent and optionally converting the 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione thus obtained into the hydrochloride thereof.

摘要翻译： 制备8- [4- [嘧啶-2-基] - 哌嗪-1-基] - 丁基] -8-氮杂 - 螺[4.5]癸烷-7,9-二酮（buspiron）的方法 通过连续加入8- [4- [4-（嘧啶-2-基） - 哌嗪-1-基] - 丁-2-炔基的溶液，使式I（I）化合物及其盐酸盐具有高纯度 ] -8-氮杂 - 螺[4.5]癸烷-7,9-二酮，其具有浓度为至少40重量％的惰性有机溶剂与氢化催化剂的悬浮液形成的式II（II） 在惰性有机溶剂中并任选地将8- [4- [4-（嘧啶-2-基） - 哌嗪-1-基] - 丁基] -8-氮杂 - 螺[4.5]癸烷-7,9-二酮 从而得到其盐酸盐。

公开(公告)号：US5221673A

公开(公告)日：1993-06-22

申请号：US802235

申请日：1991-12-04

申请人： Zoltan Budai ,  Tibor Mezei ,  Klara Reiter nee Esses ,  Lajos Fekete ,  Karoly Magyar ,  Attila Nagy ,  Laszlo Puskas

发明人： Zoltan Budai ,  Tibor Mezei ,  Klara Reiter nee Esses ,  Lajos Fekete ,  Karoly Magyar ,  Attila Nagy ,  Laszlo Puskas

IPC分类号： A23K1/16 ,  A23K1/18 ,  C07D295/18

CPC分类号： A23K50/30 ,  A23K20/137

摘要： This invention relates to fodder compositions, particularly feed additives, premixes and ready-for-use fodders, and a method for increasing weight-gain and improving fodder utilization of dimestic animals.The compositions according to the invention comprise as active ingredient a compound of the general formula (I), ##STR1## wherein R.sup.1 represents methoxy or hydrogen andR stands for methyl; orR and R.sup.1 each denotes hydrogen; orR.sup.1 stands for hydrogen and R represents ethyl.The compounds of the general formula (I) known from the literature exhibit useful weight-gain increasing and fodder-utilization improving effects and can be used in animal husbandry.

公开(公告)号：US5652270A

公开(公告)日：1997-07-29

申请号：US664804

申请日：1996-06-17

申请人： Zoltan Budai ,  Istvan Gacsalyi ,  Gabor Szenasi ,  Tibor Mezei ,  Aniko Kovacs ,  Gabor Blasko ,  Katalin Szemeredi ,  Gyula Simig ,  Lujza Petocz ,  Klara Reiter nee Esses

发明人： Zoltan Budai ,  Istvan Gacsalyi ,  Gabor Szenasi ,  Tibor Mezei ,  Aniko Kovacs ,  Gabor Blasko ,  Katalin Szemeredi ,  Gyula Simig ,  Lujza Petocz ,  Klara Reiter nee Esses

IPC分类号： A61K31/135 ,  A61K31/54 ,  A61K31/445 ,  A61K31/495

CPC分类号： A61K31/135

摘要： The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.

摘要翻译： 本发明涉及药物组合物，其制备方法和双环庚烷衍生物的新型医疗用途。 本发明的药物组合物包含本说明书中所述的式I的双环庚烷衍生物。 本发明的药物组合物适用于治疗与缩胆囊素系统的影响相关的疾病和病症，特别是用于防止胆囊的痉挛性收缩。