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41. 发明授权

US4981966A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US4981966A
公开(公告)日：1991-01-01
申请号：US295439
申请日：1989-01-10
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D401/10 , A61K31/47 , A61P31/04 , C07D215/56 , C07D295/067 , C07D295/155 , C07F5/02 , C07F5/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.
摘要翻译：本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或对于包含7-11个碳原子的芳族酰氧基）与式VI的胺VI，（其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。式I的化合物是已知的抗菌剂。本发明方法的优点在于使得所需的式I化合物可以简单的方式得到，产率高，反应时间短。

42. 发明授权

US4588526A Bronchodilatory azepino(1,2-A)pyrimidine derivatives and acid addition salts thereof and bronchodilating pharmaceutical compositions containing same 失效
标题翻译：支气管佐剂（1,2-A）嘧啶衍生物及其酸加成盐和含有其的支气管扩张药物组合物
公开(公告)号：US4588526A
公开(公告)日：1986-05-13
申请号：US550937
申请日：1983-11-10
申请人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
发明人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
IPC分类号： A61K31/519 , A61K31/55 , A61P11/08 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.
摘要翻译：本发明涉及通式为其中p = 1,2及其酸加成盐的通式为其中的氮杂[1,2-a]嘧啶衍生物及其酸加成盐，其可通过（a）使式图像II与具有通式III的化合物，其中p如上所定义，R 7是含有2至5个碳原子的烷氧基羰基或甲酰胺基，或（b）使通式为IV的化合物其中R8为含有1至4个碳原子的烷基与通式为其中R 7如上所定义的化合物反应，如果需要，将通式I的化合物转化为其酸加成盐或使其不含盐。新化合物显示支气管扩张活性。

43. 发明申请

US20070249669A1 CRYSTALLINE 2-AMINO-3-CYANOQUINOLINE DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：晶体2-氨基-3-氰基喹啉衍生物及其制备方法及含有它们的药物组合物
公开(公告)号：US20070249669A1
公开(公告)日：2007-10-25
申请号：US11550598
申请日：2006-10-18
申请人： Zoltan Finta , Istvan Hermecz , Gergely Heja , Agnes Horvath , Gyulane Kiss , Miklos Morvai , Benjamin Podanyi , Judit Sipos , Anna Szabo , Arpadne Vasvari , Erika Varkonyine Schlovicsko
发明人： Zoltan Finta , Istvan Hermecz , Gergely Heja , Agnes Horvath , Gyulane Kiss , Miklos Morvai , Benjamin Podanyi , Judit Sipos , Anna Szabo , Arpadne Vasvari , Erika Varkonyine Schlovicsko
IPC分类号： C07D215/38
CPC分类号： C07D405/12 , C07D215/54 , C07D405/14 , C07D409/12
摘要： The invention relates to the crystalline and amorphous forms of the desmotrope of general formula IB and its salts and solvates, and their preparation.
摘要翻译：本发明涉及通式IB及其盐和溶剂合物的去结晶形式的结晶和无定形形式及其制备方法。

44. 发明授权

US06482959B1 Process for the stereoselective reduction of &agr;,&bgr;-unsaturated ketones 有权
标题翻译： α，β-不饱和酮立体选择性还原的方法
公开(公告)号：US06482959B1
公开(公告)日：2002-11-19
申请号：US09091481
申请日：2000-06-27
申请人： Kardos Zsuzsanna Baloghne , Nandor Benno , Povarny Magdonla Beresne , Gyula Dalmadi , Katalin Ebinger , Laszlo Forro , Geza Galambos , Felix Hajdu , Istvan Hermecz , Geza Lukacs , Karoly Mozsolits , Szigeti Katalin Polikne , Judit Sebestyen , Tobor Szabo , Zoltan Szeverenyi , Ervin Vajda , Gabor Vankai , Pal Vofely
发明人： Kardos Zsuzsanna Baloghne , Nandor Benno , Povarny Magdonla Beresne , Gyula Dalmadi , Katalin Ebinger , Laszlo Forro , Geza Galambos , Felix Hajdu , Istvan Hermecz , Geza Lukacs , Karoly Mozsolits , Szigeti Katalin Polikne , Judit Sebestyen , Tobor Szabo , Zoltan Szeverenyi , Ervin Vajda , Gabor Vankai , Pal Vofely
IPC分类号： C07D30700
CPC分类号： C07D307/83
摘要： A process for the preparation of &agr;,&bgr;-unsaturated alcohols of general formula (I), wherein R means an alkyl group of 1-4 carbon atoms, or benzoyloxy group optionally substituted with a phenyl group; R1 means a hydrogen atom or an alkyl group of 1-4 carbon atoms, R2 means a hydrogen atom or an alkyl group of 1-4 carbon atoms; R3 means an alkyl group of 1-6 carbon atoms optionally substituted by phenyl group or cycloalkyl group of 5-7 carbon atoms; or a phenoxy group optionally substituted by a halogen atom, or a cycloalkyl group of 5-7 carbon atoms; R4 means a hydrogen atom or a halogen atom whereby at &agr;,&bgr;-unsaturated ketones of general formula (II) wherein the meanings of R, R1, R2, R3, and R4 are as given above—is diastereoselectively reduced with a borohydride type compound in an aprotic solvent, in the presence of an inorganic substance dissolublein the reaction mixture and having particle size from 0.01 micrometer to 10000 micrometer and optionally from the resulting mixture of epimeric &agr;,&bgr;-unsaturated alcohols of general formula (I) and (III) meanings of R, R1, R2, R3, and R4 are as given above—the &agr;,&bgr;-unsaturated alcohol of general formula (I) is separated by methods known.
摘要翻译：一种制备通式（I）的α，β-不饱和醇的方法，其中R表示1-4个碳原子的烷基或任选被苯基取代的苯甲酰氧基; R1表示氢原子或烷基 1-4个碳原子，R2表示氢原子或1-4个碳原子的烷基; R3表示1-6个碳原子的烷基，任选被5-7个碳原子的苯基或环烷基取代; 或任选被卤素原子取代的苯氧基或5-7个碳原子的环烷基; R4表示氢原子或卤素原子，在通式（II）的α，β-不饱和酮处，其中R，R 1的主题 R 2，R 3和R 4如上所述，在非质子传递溶剂中在硼氢化物型化合物的存在下，在反应混合物中溶解且粒径为0.01微米至10000微米的无机物质，并且任选地由通式（I）和（III）的差向异构α，β-不饱和醇的混合物，R，R 1，R 2，R 3和R 4的含义如上所述，通式（I）的α，β-不饱和醇，通过已知的方法分离。

45. 发明授权

US5294712A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US5294712A
公开(公告)日：1994-03-15
申请号：US583296
申请日：1990-09-14
申请人： Istvan Hermecz , Geza Keresturi , Lelle V. Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Keresturi , Lelle V. Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07F5/02 , C07D401/04
CPC分类号： C07D215/56 , C07F5/022
摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.
摘要翻译：本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或用于包含7-11个碳原子的芳族酰氧基）与式VI的胺（VI）（其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。式I的化合物是已知的抗菌剂。

46. 发明授权

US5284950A Process for the preparation of quinoline carboxyolic acids 失效
标题翻译：喹啉羧酸的制备方法
公开(公告)号：US5284950A
公开(公告)日：1994-02-08
申请号：US691633
申请日：1991-04-25
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07F5/02 , C07F5/04 , C07D403/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy,for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:(a) aminating the compound of the Formula (V) or a pharmaceutically acceptable salt thereof with piperazine in an inert organic solvent to yield a compound of the Formula (VII) ##STR3## or a pharmaceutically acceptable salt thereof, and (b) hydrolyzing the compound of the Formula (VII) or a pharmaceutically acceptable salt thereof, after or without isolation, to obtain the compound of the Formula (I), and if desired, converting the compound of the Formula (I) into a pharmaceutically acceptable salt thereof, or setting free the compound of the Formula (I) from its pharmaceutically acceptable salt.
摘要翻译：公开了使用式（V）的化合物或其药学上可接受的盐的方法，其中R 1和R 2各自是未被取代或被卤素取代的C 1至C 6脂族酰氧基，或各自为C7至 C11芳族酰氧基，用于防止当式（I）化合物或其药学上可接受的盐形成时，6-位的胺化，其包括以下步骤：（a）胺化化合物（VII）化合物或其药学上可接受的盐，和（b）将式（Ⅴ）化合物或其药学上可接受的盐与哌嗪在惰性有机溶剂中反应，得到式式（VII）化合物或其药学上可接受的盐在得到式（I）化合物后，如果需要，将式（I）化合物转化为其药学上可接受的盐，或设定释放式的化合物（I）的药学上可接受的盐。

47. 发明授权

US5179089A Isoquinoline compounds, compositions and use 失效
标题翻译：异喹啉化合物，组合物和用途
公开(公告)号：US5179089A
公开(公告)日：1993-01-12
申请号：US792255
申请日：1991-11-14
申请人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
发明人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC分类号： A61K31/47 , A61K31/33 , A61K31/472 , A61K31/4725 , A61P11/08 , A61P29/00 , A61P37/08 , C07D217/12 , C07D217/16 , C07D217/26
CPC分类号： C07D217/16
摘要： The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.3 means hydrogen, a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; orR.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR2## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds.The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.

48. 发明授权

US5091530A Baron chelates of quinoline carboxylic acids 失效
标题翻译：喹啉羧酸的巴伦酸
公开(公告)号：US5091530A
公开(公告)日：1992-02-25
申请号：US290105
申请日：1988-11-23
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Marie Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Marie Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/495 , A61P31/04 , C07D215/56 , C07F5/02
CPC分类号： C07D215/56
摘要： The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## /wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group/ and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## /wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms/ with a piperazine derivative of the general Formula ##STR3## /wherein R.sup.3 stands for hydrogen, methyl or ethyl/ or a salt thereof and subjecting the compound of the general Formula IV ##STR4## thus obtained /wherein R, R.sup.1 and R.sup.2 are as stated above/ to hydrolysis after or without isolation 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 present invention is that it makes the desired compounds of the general Formula I available in a simple manner, with high yields and in a short reaction time.
摘要翻译： PCT No.PCT / HU88 / 00019 Sec。 371日期1988年11月23日第 102（e）日期1988年11月23日PCT提交1988年4月8日PCT公布。公开号WO88 / 07993 1988年10月20日的日期。本发明涉及制备通式I化合物的新方法，其中R代表哌嗪基，4-甲基 - 哌嗪基或4-乙基 - 哌嗪基/ 或其药学上可接受的盐，其包括使通式II的化合物其中R 1和R 2表示卤素，含有2至6个碳原子的脂族酰氧基并且任选被卤素取代，或含有7〜11个碳原子的芳香族酰氧基/通式为其中R 3代表氢，甲基或乙基/或其盐，并通式IV的化合物 / IV /由此获得的/其中R，R 1和R 2如上所述/在分离后或不分离下进行水解，如果需要，将所得通式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。本发明的优点在于使得所需的通式Ⅰ化合物以简单的方式得到，产率高，反应时间短。

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