专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4851416A Berban derivatives as .alpha..sub.2 -adrenergic antagonists 失效
标题翻译： Berban衍生物作为α2-肾上腺素能拮抗剂
公开(公告)号：US4851416A
公开(公告)日：1989-07-25
申请号：US867323
申请日：1986-05-23
申请人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
发明人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
IPC分类号： C07D453/00 , A61K31/47 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/03 , C07D471/04
CPC分类号： C07D455/00
摘要： The invention relates to novel racemic or optically active berban derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group 1 to 6 carbon atoms or R.sup.1 and R.sup.2 together represent a C.sub.1-3 alkylenedioxy group;R.sup.3 and R.sup.4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 6 carbon atoms and optionally substituted by hydroxyl group, or a C.sub.2-6 alkoxycarbonyl or cyano group; andR.sup.5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C.sub.1-7 aliphatic or aromatic acyl group or C.sub.1-7 alkylsulphonyl or arylsulphonyl group, anda salt thereof, to pharmaceutical compositions containing them, to the use as well as to process for preparing the novel compounds. The compounds of the formula (I) are selective .alpha..sub.2 -adrenergic receptor-blocking substances and thus, they may be used for the treament of depressive illnesses.
摘要翻译：本发明涉及式（I）的新型外消旋或光学活性伯类衍生物，其中R 1和R 2彼此独立地表示1至6个碳原子的羟基，直链或支链烷氧基或R1和R2 一起代表C1-3亚烷基二氧基; R3和R4独立地表示独立于具有1-6个碳原子并且任选被羟基取代的另一个氢，直链或支链烷基或C 2-6烷氧羰基或氰基; 并且R 5表示氢，具有1〜6个碳原子的直链或支链烷基，C 1-7脂族或芳族酰基或C 1-7烷基磺酰基或芳基磺酰基及其盐与含有它们的药物组合物以及用于制备新化合物的方法。式（I）化合物是选择性α2-肾上腺素能受体阻断物质，因此可用于抑郁症的治疗。

2. 发明授权

US4735965A 7-oxo-PGI.sub.2 -ephedrine salts and their pharmaceutical compositions and methods 失效
标题翻译： 7-氧代-PGI2-麻黄碱盐及其药物组合物和方法
公开(公告)号：US4735965A
公开(公告)日：1988-04-05
申请号：US868772
申请日：1986-05-28
申请人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
发明人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
IPC分类号： C07C59/90 , A61K31/135 , A61K31/19 , A61K31/34 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P1/16 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07C51/00 , C07C51/41 , C07C67/00 , C07C213/00 , C07C215/40 , C07C405/00 , C07D307/935 , C07D307/937 , C07D521/00
CPC分类号： C07D307/937
摘要： The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks. Accordingly the salts of the present invention are useful in the prevention of peripheral vascular diseases, in improving circulation of extremities, in relieving the seriousness of cardiac infarction and also in the treatment and prevention of gastrointestinal ulcer and acute or chronical liver injury.
摘要翻译：本发明涉及式I的新的7-氧代-PGI-麻黄碱盐类似物，其中A代表 - （CH 2）2 - ，顺式或反式-CH = CH-或-C 3位C; R1是低级烷基或氢; B表示化学键，-CH 2 - 或-CR 2 R 3; R2代表低级烷基或氢; R3表示低级烷基或氢; X是化学键，-O-或-CH2-; R4代表C 1-6烷基，C 4-7环烷基，C 1-6氟代烷基，C 2-6烯基，C 2-6炔基，苯基，取代的苯基或杂芳基。式I的盐显示与PGI2的钠盐相同的药理学特征，它们抑制血液聚集和胃酸分泌，可用于预防心绞痛发作。因此，本发明的盐可用于预防周围血管疾病，改善四肢的循环，缓解心肌梗死的严重性，以及治疗和预防胃肠溃疡和急性或慢性肝损伤。

3. 发明授权

US4840949A Oxadiazole-alkyl-purine derivatives useful as antitussive agents 失效
标题翻译：用作镇咳剂的恶二唑 - 烷基嘌呤衍生物
公开(公告)号：US4840949A
公开(公告)日：1989-06-20
申请号：US107693
申请日：1987-10-09
申请人： Dezso Korbonits , Emil Minker , Zoltan Vargai , Gergely Heja , Gabor Kovacs , Agnes Gottsegen , Sandor Antus , Sandor Virag , Andrea Bolehovszky , Jeno Marton , Katalin Marmarosi nee Kellner , Lorand Debreczeni , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Gabor Horvath
发明人： Dezso Korbonits , Emil Minker , Zoltan Vargai , Gergely Heja , Gabor Kovacs , Agnes Gottsegen , Sandor Antus , Sandor Virag , Andrea Bolehovszky , Jeno Marton , Katalin Marmarosi nee Kellner , Lorand Debreczeni , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Gabor Horvath
IPC分类号： C07D473/04 , A61K31/52 , A61K31/522 , A61P11/04 , A61P11/14 , C07D271/06 , C07D273/02 , C07D473/06
CPC分类号： C07D473/06
摘要： The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.
摘要翻译：本发明涉及式I的新型氧化噻唑烷基嘌呤衍生物及其药学上可接受的盐，其中A代表C1-4亚烷基，R1代表C1-6烷基，羟基烷基，卤代烷基，羧基烷基，C5-6环烷基或其中基团n为整数1-3的式 - （CH 2）n -NR 2 R 3的氨基烷基; R 2和R 3各自代表氢或C 1-4烷基或与它们相连的相邻氮原子一起形成5-或6-元含氮杂环，其可以任选地包含另外的氮原子或氧原子作为杂原子; 或R 1代表苯基，羟基苯基，羧基苯基，苄基或二甲氧基苄基。式I化合物可以通过本身已知的方法制备，并且可用于作为止咳剂的治疗。

4. 发明授权

US4871849A 1-Methylamino-quinoline-carboxylic acid derivatives 失效
标题翻译： 1-甲基氨基 - 喹啉羧酸衍生物
公开(公告)号：US4871849A
公开(公告)日：1989-10-03
申请号：US105299
申请日：1987-06-24
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvavi , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvavi , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D401/02 , A61K31/47 , C07D20060101 , C07D215/00 , C07D215/56 , C07D215/58 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07F5/02
CPC分类号： C07F5/022 , C07D215/58
摘要： The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.1 and R.sup.2 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms) with a piperazine of the general Formula III ##STR3## (wherein R.sup.3 represent hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general Formula IV ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) without or after hydrolysis and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the general Formula I are known antibacterial agents.The advantage of the process of the present invention is that it enables the preparation of the compounds of the general Formula I in a simple manner, with high yields and in a short reaction time.
摘要翻译： PCT No.PCT / HU86 / 00067 Sec。 371日期1987年6月24日 102（e）1987年6月24日PCT PCT日期：1986年12月9日PCT公布。公开号WO87 / 03586 日期：1987年6月18日。本发明涉及一种制备通式I的化合物及其药学上可接受的盐（其中R代表哌嗪基或4-甲基 - 哌嗪基）的方法，其包括使通式II的化合物（其中R1和R2代表卤素;包含2-6个碳原子并任选被卤素取代的脂族酰氧基或者包含7-11个碳原子的芳香酰氧基）与哌嗪通式III III（其中R 3表示氢或甲基）或其盐，水解由此得到的通式IV的化合物（其中R，R 1和R 2如上所述），无水解后，如果需要，将由此获得的通式I的化合物转化为其盐或使其与其盐相同。通式I的化合物是已知的抗菌剂。本发明方法的优点在于它能够以高产率和短的反应时间以简单的方式制备通式I的化合物。

5. 发明授权

US4599327A Dibenzo[bd]pyran derivatives, process for the preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：二苯并[bd]吡喃衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4599327A
公开(公告)日：1986-07-08
申请号：US557629
申请日：1983-12-02
申请人： Mihaly Nogradi , Dezso Korbonits , Agnes Gottsegen , Sandor Antus , Zsuzsa Furst , Jozsef Knoll , Jozsef Szejtli , Agnes Stadler , Gabor Kovacs , Katalin Marmarosi
发明人： Mihaly Nogradi , Dezso Korbonits , Agnes Gottsegen , Sandor Antus , Zsuzsa Furst , Jozsef Knoll , Jozsef Szejtli , Agnes Stadler , Gabor Kovacs , Katalin Marmarosi
IPC分类号： A61K31/35 , A61K31/352 , A61K31/715 , A61P1/08 , A61P23/00 , A61P23/02 , A61P25/02 , A61P25/04 , C07C43/178 , C07C43/205 , C07C43/23 , C07C59/68 , C07D221/12 , C07D311/78 , C07D311/80 , C07D311/92 , C07D493/10 , C08B37/00 , C08B37/16 , A61K31/70
CPC分类号： C07D493/10 , C07C309/00 , C07C43/1782 , C07C43/1785 , C07C43/2055 , C07C43/23 , C07C59/68 , C07D221/12 , C07D311/78 , C07D311/80 , C08B37/0015
摘要： 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.
摘要翻译：式（1a）化合物的2,6-二-O-甲基-β-环糊精复合物其中R 2'代表C 1至C 12烷基或其中R 11为C 1至C 4的式烷基; R 12是氢或C 1至C 4烷基; n为0或1; p为1〜4; r为1〜4; 和R 3'和R 4'各自为C1至C4烷基，或其药学上可接受的盐，具有止痛活性。

6. 发明授权

US4450309A Process for the preparation of unsaturated geminal dihalogen compounds 失效
标题翻译：制备不饱和偕二卤化合物的方法
公开(公告)号：US4450309A
公开(公告)日：1984-05-22
申请号：US391866
申请日：1982-06-24
申请人： Rudolf Soos , Jozsef Nemes , Laszlo Vidra , Miklos Szelestei , Gabor Kovacs , Istvan Szekeley
发明人： Rudolf Soos , Jozsef Nemes , Laszlo Vidra , Miklos Szelestei , Gabor Kovacs , Istvan Szekeley
IPC分类号： C07C17/361 , B01J21/00 , B01J23/00 , B01J23/06 , B01J27/00 , C07B61/00 , C07C17/00 , C07C17/363 , C07C21/02 , C07C21/04 , C07C21/17 , C07C21/19 , C07C67/00 , C07C17/33
CPC分类号： C07C17/363
摘要： The invention relates to a new process for preparing unsaturated geminal dihalogen compounds. More particularly, the invention concerns a process for preparing compounds of the formula (I) ##STR1## wherein X is halogen,R.sup.1 is a straight or branched chained alkenyl group having 2 to 6 carbon atoms,by clearing the corresponding 1-substituted 2,2,2-trihaloethylesters.
摘要翻译：本发明涉及一种制备不饱和偕二卤化合物的新方法。更具体地，本发明涉及制备式（I）化合物的方法，其中X是卤素，R 1是具有2-6个碳原子的直链或支链链烯基，通过将相应的1-取代的2， 2,2-三卤乙基酯。

7. 发明授权

US4806645A Boric anhydrides of 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 失效
标题翻译： 6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸的硼酸酐
公开(公告)号：US4806645A
公开(公告)日：1989-02-21
申请号：US105295
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07D215/58 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I ##STR1## (wherein R and R.sup.1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms).The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline-3- carboxylic acid.The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II ##STR2## or a compound of the general Formula III ##STR3## (wherein R.sup.2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IVHBF.sub.4 /IV/or a borone trihalide of the general Formula VBX.sub.3 /V/(wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI ##STR4## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).
摘要翻译： PCT No. PCT / HU86 / 00066 Sec。 371日期1987年8月7日 102（e）日期1987年8月7日PCT申请日1986年12月9日PCT公布。公开号WO87 / 03594 日期：1987年6月18日本发明涉及通式I的新的6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸/硼酸酐，图像（I）（其中R和R1代表卤素;包含2-6个碳原子并任选被卤素取代的脂族酰氧基;或包含7-11个碳原子的芳族酰氧基）。通式I的新化合物是可用于制备抗菌剂6-氟-1-甲基氨基-7-（4-甲基 - 哌嗪子基）-4-氧代-1,4-二氢 - 喹啉线衍生物的有价值的中间体， 3-羧酸。通式I的新化合物可以通过使式II的化合物（II）或通式III的化合物（III）（其中R 2代表包含1-4个碳原子的烷基）原子）与式IV的氢氟硼酸盐HBF 4 / IV /或通式V BX 3 / V /（其中X表示氟，氯或溴）的三卤化硼硼烷或其与醚或硼烷衍生物形成的络合物通式VI（VI）（其中R 3，R 4和R 5代表包含1-5个碳原子并且任选地被卤素或包含6-10个碳原子的芳基取代的烷基）。

8. 发明授权

US4803274A Norfloxacin intermediate 失效
标题翻译：诺氟沙星中间体
公开(公告)号：US4803274A
公开(公告)日：1989-02-07
申请号：US105298
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to a process for the preparation of compounds of the Formula I ##STR1## (wherein R and R.sup.1 stand for an aliphatic acyloxy group comprising 2-5 carbon atoms and optionally substituted by halogen or for an aromatic acyloxy group comprising 7-11 carbon atoms), which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.2 stands for hydrogen or alkyl comprising 1-4 carbon atoms) with a boron derivative of the Formula III ##STR3## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for an alkyl group comprising 1-4 carbon atoms and optionally substituted by halogen or for an aryl group comprising 6-10 carbon atoms).The new compounds of the general Formula I are useful pharmaceutical intermediates.
摘要翻译： PCT No.PCT / HU86 / 00068 Sec。 371日期1987年8月7日 102（e）日期1987年8月7日PCT申请日1986年12月9日PCT公布。第WO87 / 03595号公报日本1987年6月18日。本发明涉及制备式I化合物（I）的方法（其中R和R 1代表包含2-5个碳原子并任选被卤素取代的脂族酰氧基或包含7-11个碳原子的芳族酰氧基），其包括使通式II的化合物（II）（其中R 2表示氢或包含1-4个碳原子的烷基）与式式III（III）（其中R3，R4和R5代表含有1-4个碳原子的烷基，任选被卤素取代或含有6-10个碳原子的芳基）。通式I的新化合物是有用的药物中间体。

9. 发明授权

US4706711A Elastic technical hose with a foam insert 失效
标题翻译：弹性技术软管，带泡沫插件
公开(公告)号：US4706711A
公开(公告)日：1987-11-17
申请号：US775080
申请日：1985-09-12
申请人： Tibor Czvikovszky , Gabor Kovacs , Endre Lakner , Lajos Mahr , Agnes Somogyi , Sandor Mikes , Gyorgy Kegly , Istvan Muzsai , Laszlo Palotas , Nandor Pfisztner
发明人： Tibor Czvikovszky , Gabor Kovacs , Endre Lakner , Lajos Mahr , Agnes Somogyi , Sandor Mikes , Gyorgy Kegly , Istvan Muzsai , Laszlo Palotas , Nandor Pfisztner
IPC分类号： B29C70/16 , B29C70/06 , B29D23/00 , B32B1/08 , B32B5/28 , B32B7/02 , B32B7/12 , F16L11/04 , F16L11/133 , F16L55/00
CPC分类号： B29D23/001 , F16L11/04 , F16L11/133 , Y10S138/05 , Y10S138/09
摘要： A technical hose with foam insert, expediently a maritime swimming hose for drawing-off oil, as well as to the process for the production thereof. The hose according to the invention consists of the elastic cross-linked elastomer layer containing also fibre-reinforcement, of the foam layer with closed cells arranged above said layer and assuring swimming ability, as well as of the new type of outer coating sheet.The outer coating sheet is a multi-layer system, the elementary layers are previously partially cross-linked, in their cross-section inhomogenous elastomer layers, stretched longitudinally in a given case, being interconnected and connected to the foam layer, respectively, by means of thermally and/or chemically activated adhesive layers.
摘要翻译：具有泡沫插入件的技术软管，有利地是用于排出油的海上游泳软管，以及生产它的过程。根据本发明的软管由包含纤维增强的弹性交联弹性体层组成，泡沫层具有布置在所述层之上的闭孔并确保游泳能力，以及新型外涂层。外涂层是多层体系，基本层预先部分交联，在其横截面上不均匀的弹性体层，在给定情况下纵向拉伸，分别通过装置互连并连接到泡沫层的热和/或化学活化的粘合剂层。

10. 发明授权

US4565817A Theophyllinyl-alkyl-oxadiazoles, process for the preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：木脂基 - 烷基 - 恶二唑，其制备方法和含有它们的药物组合物
公开(公告)号：US4565817A
公开(公告)日：1986-01-21
申请号：US474227
申请日：1983-03-11
申请人： Dezso Korbonits , Maria Szomor nee Wundele , Gergely Heja , Ida Szvoboda nee Kanzel , Pal Kiss , Csaba Gonczi , Endre Palosi , Gabor Kovacs , Judit Kun , Emil Minker , Sandor Virag , Gyula Sebestyen , Tamas Szuts
发明人： Dezso Korbonits , Maria Szomor nee Wundele , Gergely Heja , Ida Szvoboda nee Kanzel , Pal Kiss , Csaba Gonczi , Endre Palosi , Gabor Kovacs , Judit Kun , Emil Minker , Sandor Virag , Gyula Sebestyen , Tamas Szuts
IPC分类号： C07D413/06 , A61K31/52 , A61K31/522 , A61P11/00 , A61P11/08 , A61P11/14 , A61P29/00 , A61P31/14 , C07D20060101 , C07D271/06 , C07D401/14 , C07D473/08 , C07D473/14 , C07D473/10
CPC分类号： C07D473/08
摘要： Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3 whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia ##STR4## and R.sub.1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.
摘要翻译：公开了式I的镇咳药（I）或其生理上可接受的酸加成盐，其中A代表直链或支链C 1-5亚烷基，或者R 1代表直链或支链C 1-10烷基，卤代烷基，羟基烷基，C 5-6环烷基，乙烯基，2-乙氧基乙基，羰基烷基或下式的氨基烷基其中R代表氢或甲基，n为0-3，R2代表氢或直链或支链烷基，R3 代表氢或直链或支链烷基，或者R2和R3与氮原子一起可以形成5-6元环，该环可以任选地含有氧或第二氮原子，后者任选地被甲基或 R1可以代表式为R4R5C6H3的苯基，其中R4和R5独立地表示氢，氯，羟基，甲氧基，乙氧基，甲基或氨基，或者R1可以进一步代表羟基，在这种情况下可以存在式I化合物根据式Ia（Ia）或（Ib）和R1的互变异构体形式的条件可以进一步代表苄基，2,2-二苯基乙基或甲茶素-7-基 - 甲基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式