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1. 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。

2. 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。

3. 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。

4. 发明授权

US5486528A Basic ethers and process for the preparation thereof 失效
标题翻译：碱性醚及其制备方法
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。

5. 发明授权

US5597822A Pharmaceutical compositions for the prevention and/or treatment a gastrointestinal diseases 失效
标题翻译：用于预防和/或治疗胃肠道疾病的药物组合物
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。

6. 发明授权

US5652270A Pharmaceutical compositions containing bicycloheptane ether amines and a process for the preparation thereof 失效
标题翻译：含有双环庚烷醚胺的药物组合物及其制备方法
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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US4077999A Novel oxime ethers 失效
标题翻译：新型肟醚
公开(公告)号：US4077999A
公开(公告)日：1978-03-07
申请号：US749399
申请日：1976-12-10
申请人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Eniko Szirt nee Kiszelly , Ibolya Kosoczky , Lujza E. Petocz
发明人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Eniko Szirt nee Kiszelly , Ibolya Kosoczky , Lujza E. Petocz
IPC分类号： C07C251/58 , C07D295/088 , C07C131/02 , C07C131/04
CPC分类号： C07D295/088 , C07C251/58 , C07C2101/08 , C07C2101/16 , C07C2101/18
摘要： The invention relates to novel oxime ethers of the formula I ##STR1## wherein R stands for a phenyl group which may be substituted by a halogen atom or by one or more C.sub.1 -C.sub.4 alkoxy, hydroxyl, nitro or di(C.sub.1 -C.sub.3 alkyl)amino groups,R.sup.1 and R.sup.2 denote each a hydrogen atom or together a valence bond,A denotes a C.sub.2 -C.sub.4 straight or branched-chain alkylene group,N denotes an integer from 3 to 10, andR.sup.3 and R.sup.4 denote a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, furthermore to acid addition salts and quaternary ammonium salts thereof. These new compounds are biologically active, and possess primarily local analgesic, spasmolytic, nicotine-lethality inhibiting, tetrabenazine-antagonistic and tetra-cor-spasm inhibiting effects.
摘要翻译：本发明涉及式I（I）的新型肟醚，其中R代表可被卤素原子取代的苯基或一个或多个C 1 -C 4烷氧基，羟基，硝基或二（C1- C 3烷基）氨基，R 1和R 2各自表示氢原子或价键一起，A表示C 2 -C 4直链或支链亚烷基，N DENOTES AN INTEGER为3〜10，R 3和R 4表示氢原子或C1-C4烷基，此外还涉及其酸加成盐和季铵盐。这些新化合物具有生物活性，主要具有局部镇痛，解痉，尼古丁致死抑制，四苯并嗪拮抗和四痉挛抑制作用。

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