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1. 发明授权

US5478825A 5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives 失效
标题翻译： 5-（取代氨基）-1,2,4-三唑并（1,5-A）嘧啶衍生物
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。

2. 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。

3. 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。

4. 发明授权

US4873249A Pharmaceutical composition 失效
标题翻译：药物组成
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。

5. 发明授权

US4871728A Pharmaceutical composition comprising an organic zinc complex and a process for preparing the active substance 失效
标题翻译：包含有机锌络合物的药物组合物和制备活性物质的方法
公开(公告)号：US4871728A
公开(公告)日：1989-10-03
申请号：US232162
申请日：1988-08-12
申请人： Gyula Sebestyen , Istvan Simonyi , Gizelle Miholics , Marta Kovacs , Frigyes Gorgenyi , Marton Fekete , Pal Vago , Istvan Seres , Janos Egri , Maria Szeli
发明人： Gyula Sebestyen , Istvan Simonyi , Gizelle Miholics , Marta Kovacs , Frigyes Gorgenyi , Marton Fekete , Pal Vago , Istvan Seres , Janos Egri , Maria Szeli
IPC分类号： A61K31/555 , A61P31/04 , A61P31/10 , C07D215/30
CPC分类号： C07D215/30
摘要： The invention refers to a novel pharmaceutical composition having especially antimycotic activity and comprising the zinc complex of 5-chloro-7-iodo-8-hydroxyquinoline of formula (I) ##STR1## and one or more pharmaceutically acceptable carriers. The pharmaceutical composition of the invention can be used for the effective treatment of mycotic infections on the skin surface, mucous membranes or nails.The complex of formula (I) is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8-hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product precipitated.
摘要翻译：本发明涉及具有特异性抗真菌活性的新型药物组合物，其包含式（I）的5-氯-7-碘-8-羟基喹啉与一种或多种药学上可接受的载体的锌络合物。本发明的药物组合物可用于有效治疗皮肤表面，粘膜或指甲上的霉菌感染。式（I）的络合物通过使5-氯-7-碘-8-羟基喹啉的碱金属盐溶液与含有过量的无机或有机锌盐的溶液或具有较低的稳定常数比式（I）的络合物和分离产物沉淀。

6. 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。

7. 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。

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

US5240918A 2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
标题翻译： 2-（取代的亚氨基） - 噻唑啉及其制备方法
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。

10. 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。

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