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31. 发明授权

US4983633A Amide compounds, process for preparing the same, and composition for activating gastric motor function containing the same 失效
标题翻译：酰胺化合物，其制备方法和用于激活含有其的运动功能的组合物
公开(公告)号：US4983633A
公开(公告)日：1991-01-08
申请号：US241028
申请日：1988-09-02
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
IPC分类号： A61K31/165 , C07C233/12 , C07C233/73 , C07C235/48 , C07C311/15 , C07D295/08 , C07D295/092 , C07D317/68
CPC分类号： C07D295/088 , C07C255/00 , C07D317/68
摘要： Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.5 may be combined together with nitrogen to form 1-pyrrolidinyl or piperidino, and pharmacologically-acceptable acid-addition salts thereof, which exhibit excellent effects in the activation of gastric motor function, a process for preparation pharmaceutical compositons thereof, as well as a method for the treatment of a subject suffering from an ailment associated with inadequate gastric motor function by administrating such a compound to the said subject, are all disclosed.

32. 发明授权

US4948812A 1-phenoxy-3-amino-2-propanols use thereof 失效
标题翻译： 1-苯氧基-3-氨基-2-丙醇的用途
公开(公告)号：US4948812A
公开(公告)日：1990-08-14
申请号：US125308
申请日：1987-11-25
申请人： Herbert Koppe , Franz Esser , Walter Kobinge , Christian Lillie
发明人： Herbert Koppe , Franz Esser , Walter Kobinge , Christian Lillie
IPC分类号： C07D317/68 , A61K31/165 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/06 , A61P9/12 , C07C67/00 , C07C231/00 , C07C231/12 , C07C233/75 , C07C235/00 , C07C235/20 , C07C235/56 , C07C253/00 , C07C255/60 , C07C275/34 , C07C301/00 , C07C303/40 , C07C311/16 , C07D211/14 , C07D213/82 , C07D295/08 , C07D295/092
CPC分类号： C07D213/82 , C07C275/34 , C07D295/088
摘要： Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.
摘要翻译：式（I）化合物（取代基R 1，R 2，R 3，R 4和R 5在说明书中说明）可以通过常规方法制备。由于其有利的活性，化合物可有利地用于治疗某些心脏和循环障碍。

33. 发明授权

US4937360A N-substituted amide derivatives useful for treating liver diseases 失效
标题翻译：用于治疗肝脏疾病的N-取代酰胺衍生物
公开(公告)号：US4937360A
公开(公告)日：1990-06-26
申请号：US373338
申请日：1989-06-28
申请人： Geng-tao Liu , Liang Huang , Er-chang Rao , Jin Zhou , Yan Li , Katsuo Hatayama , Tatsuhiko Sano , Kensei Yoshikawa , Shohei Higuchi , Iwao Arai
发明人： Geng-tao Liu , Liang Huang , Er-chang Rao , Jin Zhou , Yan Li , Katsuo Hatayama , Tatsuhiko Sano , Kensei Yoshikawa , Shohei Higuchi , Iwao Arai
IPC分类号： A61K31/357 , A61K31/36 , A61P1/16 , C07D317/58 , C07D317/68
CPC分类号： C07D317/58
摘要： N-substituted amide derivative represented by the formula ##STR1## wherein A is --CH(OH)-- or --C(.dbd.O)--, R.sup.1 is a hydrogen atom or anlkyl group having 1 to 3 carbon atoms, and R.sup.2 is an alkyl group having 1 to 6 carbon atoms, are disclosed. These compounds are useful for prevention and therapy for liver diseases.

34. 发明授权

US4835178A Methylendioxyphenathrene and stilben derivatives, process for the preparation thereof, pharmaceutical compositions using these, and therapeutic applications 失效
标题翻译：甲基二氧苯并噻吩和芪衍生物，其制备方法，使用它们的药物组合物和治疗应用
公开(公告)号：US4835178A
公开(公告)日：1989-05-30
申请号：US171695
申请日：1988-03-22
申请人： Klaus Gorler , Gunter Krumbiegel , Michael Hanack , Lakshmina R. Subramanian
发明人： Klaus Gorler , Gunter Krumbiegel , Michael Hanack , Lakshmina R. Subramanian
IPC分类号： C07D317/64 , A61K31/335 , A61K31/357 , A61K31/36 , A61P31/00 , A61P31/12 , A61P37/04 , C07D317/68 , C07D317/70
CPC分类号： C07D317/70 , C07D317/68
摘要： The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methoxy or ethoxy radical and R.sub.2 and R.sub.3 are hydrogen atoms or R.sub.2 and R.sub.3 together represent an aromatic carbon-carbon bond and R.sub.1 is a hydrogen atom, a hydroxyl group or an ethoxy radical; and the pharmaceutically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them, as well as their use in therapy.
摘要翻译：本发明提供以下通式的化合物：其中R 1是氢原子或甲氧基或乙氧基，R 2和R 3是氢原子或R 2和R 3一起代表芳族碳 - 碳键，R 1是氢原子，羟基或乙氧基; 及其药学上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物，以及它们在治疗中的用途。

35. 发明授权

US4545942A Amino-acid derivatives, their preparation and their use as pharmaceuticals 失效
标题翻译：氨基酸衍生物，其制备及其作为药物的用途
公开(公告)号：US4545942A
公开(公告)日：1985-10-08
申请号：US597817
申请日：1984-04-09
申请人： Mitsuo Nagano , Koichi Hirai , Kouichi Kitamura , Kenkichi Shinkai , Hiroshi Yasuda
发明人： Mitsuo Nagano , Koichi Hirai , Kouichi Kitamura , Kenkichi Shinkai , Hiroshi Yasuda
IPC分类号： A61K31/275 , A61K20060101 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61P35/00 , A61P37/04 , C07C20060101 , C07C67/00 , C07C253/00 , C07C255/24 , C07C255/26 , C07C255/29 , C07C255/32 , C07C255/44 , C07C255/56 , C07C255/66 , C07D317/68 , C07C121/78
CPC分类号： C07C255/00
摘要： New compounds useful as immunoregulatory and antineoplastic agents are amino-acid derivatives of formula: ##STR1## wherein: n is an integer from 1 to 5;R.sup.1 is a hydrogen atom, an alkyl group, a haloalkyl group, a halogen atom, a mercapto group, an alkylmercapto group, a hydroxy group, an alkoxy group, an acyloxy group, a carboxyl group, an alkoxycarbonyl group, an amino group, an alkyl-substituted amino group, an aryl-substituted amino group, an acylamino group, a haloalkoxycarbonylamino group, an alkanesulphonyl group, a nitro group or a cyano group (and, when n is an integer from 2 to 5, the radicals R.sup.1 may be the same or different);R.sup.2 and R.sup.3 may be the same or different and each is a hydrogen atom or an alkyl group;R.sup.4 is a hydrogen atom, an alkyl group, a cyano group, a cyanoalkyl group, a hydroxyalkyl group, an alkoxycarbonyl group, a carboxyl group, an aryl group, an aralkyl group, a mercaptoalkyl group, an alkylthioalkyl group, or a thioalkyl group (the free bond of the sulphur in said thioalkyl group being joined to the sulphur of another moiety of the same formula); andA is a hydroxy group, an alkoxy group, an amino group, an alkyl-substituted amino group (optionally halogen- or carbamoyl- substituted in the alkyl moiety), a hydrazino group, an alkyl- or aryl- substituted hydrazino group, a hydroxylamino group, an alkoxyamino group or an aralkyloxyamino group;and the pharmaceutically acceptable salts thereof.
摘要翻译：可用作免疫调节和抗肿瘤剂的新化合物是下式的氨基酸衍生物：其中：n是1至5的整数; R1是氢原子，烷基，卤代烷基，卤素原子，巯基，烷基巯基，羟基，烷氧基，酰氧基，羧基，烷氧基羰基，氨基，烷基取代的氨基，芳基取代的氨基，酰氨基，卤代烷氧基羰基氨基，链烷磺酰基，硝基或氰基（当n为2至5的整数时，基团R 1可以相同或不同）; R2和R3可以相同或不同，各自为氢原子或烷基; R4是氢原子，烷基，氰基，氰基烷基，羟基烷基，烷氧基羰基，羧基，芳基，芳烷基，巯基烷基，烷硫基烷基或硫代烷基（所述硫代烷基中的硫的游离键与相同式的另一部分的硫连接）; 并且A是羟基，烷氧基，氨基，烷基取代的氨基（在烷基部分中任选被卤素取代或氨基甲酰基取代），肼基，烷基或芳基取代的肼基，羟基氨基，烷氧基氨基或芳烷氧基氨基; 及其药学上可接受的盐。

36. 发明授权

US4490388A Amidine compound and anticomplement agent comprising same 失效
标题翻译：脒化合物和包含其的抗补体剂
公开(公告)号：US4490388A
公开(公告)日：1984-12-25
申请号：US350964
申请日：1982-02-22
申请人： Setsuro Fujii , Takuo Aoyama , Yojiro Sakurai , Toyoo Nakayama , Shigeki Nunomura , Takashi Yaegashi , Toshiyuki Okutome
发明人： Setsuro Fujii , Takuo Aoyama , Yojiro Sakurai , Toyoo Nakayama , Shigeki Nunomura , Takashi Yaegashi , Toshiyuki Okutome
IPC分类号： C07C271/22 , C07C279/18 , C07D317/60 , C07D317/68 , C07C101/00 , A61K31/215
CPC分类号： C07D317/68 , C07C271/22 , C07C279/18 , C07D317/60
摘要： Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with 4-(.beta.-amidinoethenyl)phenol represented by the formula (III) ##STR2## and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
摘要翻译：由式（I）表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白酶，抗血纤维蛋白酶，抗激肽释放酶和抗凝血酶剂。具有强大的抗Cl（Cl＆upbar＆r，Cl＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过由式（II）R1-COOH（II）表示的羧酸化合物与由式（III）表示的4-（β-脒基乙烯基）苯酚（III）进行常规酯化而制备，如果必需的，可以转化成其药学上可接受的酸加成盐。

37. 发明授权

US4454338A Amidine compound 失效
标题翻译：脒化合物
公开(公告)号：US4454338A
公开(公告)日：1984-06-12
申请号：US300534
申请日：1981-09-09
申请人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
发明人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
IPC分类号： C07C249/02 , A61K31/155 , C07C257/18 , C07C279/18 , C07D317/68 , C07C101/00 , C07C101/48
CPC分类号： C07D317/68 , C07C279/18
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceuticlly acceptable acid addition salts thereof.
摘要翻译：由式＆lt; IMAGE＆gt;表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白胨，抗血浆素，抗激肽释放酶和抗凝血酶剂。具有强大的抗C1（C1＆upbar＆r，C1＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过将式（ⅩⅧ）代表的羧酸化合物与6-脒基-2-萘酚进行常规的酯化反应来制备，如果需要，可以将其转化成其药学上可接受的酸加成盐。

38. 发明授权

US4414214A Benzodioxole derivatives and pharmaceutical use thereof 失效
标题翻译：苯并二恶醇衍生物及其药物用途
公开(公告)号：US4414214A
公开(公告)日：1983-11-08
申请号：US369873
申请日：1982-04-19
申请人： Ernst Habicht , Paul Zbinden
发明人： Ernst Habicht , Paul Zbinden
IPC分类号： A61K31/357 , A61K31/36 , A61P7/10 , C07C45/46 , C07C45/67 , C07C45/68 , C07C49/84 , C07D317/46 , A61K31/335 , C07D317/68
CPC分类号： C07D317/46 , C07C45/46 , C07C45/673 , C07C45/68 , C07C49/84 , Y10S514/869 , Y10S514/87
摘要： The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an alkylene or alkylidene radical having a maximum of 5 carbon atoms, n represents 0 or 1, R.sub.2 and R.sub.3 each represents, independently of the other, hydrogen, lower alkyl, lower alkoxy or halogen, and A represents the radical O--R.sub.4, wherein R.sub.4 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.5 and R.sub.6 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.5 and R.sub.6 are bonded to one another and, together with the adjacent nitrogen atom, represent unsubstituted or lower alkyl-substituted tetra- or hexa-methyleneimino or 4-morpholinyl, to salts of compounds of the formula I in which A represents OR.sub.4 wherein R.sub.4 is hydrogen, with bases, and to acid addition salts of compounds of the formula I in which the radical R.sub.1 has a basic character, and to pharmaceutical compositions that contain them. The novel substances exhibit diuretic and, in addition, uricosuric activity and may be administered, according to the invention, preferably in the form of appropriate pharmaceutical compositions, to mammals for the treatment of oedema and hypertension.
摘要翻译：本发明涉及式I（I）的新的苯并间二氧杂环戊烯衍生物，其中R 1表示未取代或取代的芳族或杂芳族基团，alk表示具有最多5个碳原子的亚烷基或亚烷基，n表示0或 1，R 2和R 3各自独立地表示氢，低级烷基，低级烷氧基或卤素，A表示基团O-R 4，其中R 4表示氢或未取代或取代的脂族或芳脂族烃基，或A 表示其中R 5和R 6各自独立地表示氢或低级烷基或R 5和R 6彼此键合并且与相邻的氮原子一起代表未取代或低级烷基取代的基团四或六亚甲基亚氨基或4-吗啉基的化合物与式I化合物的盐，其中A表示OR4，其中R4是氢，具有碱，以及f的化合物的酸加成盐其中基团R1具有基本特征的Ormula I，以及含有它们的药物组合物。该新物质显示利尿剂，另外还包含尿酸活性，并且根据本发明可以优选以适当的药物组合物的形式给哺乳动物用于治疗水肿和高血压。

39. 发明授权

US4402981A N.sub.1 -Acyl-N.sub.2 -phenyl-diaminopropanols and pharmaceutical compositions thereof and processes for their preparation 失效
标题翻译： N，N-酰基-N-苯基 - 二氨基丙醇及其药物组合物及其制备方法
公开(公告)号：US4402981A
公开(公告)日：1983-09-06
申请号：US243746
申请日：1981-03-16
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
IPC分类号： C07C233/35 , A61K9/28 , A61K9/48 , A61K31/16 , A61K31/165 , A61K31/245 , A61P1/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/36 , C07C233/62 , C07D213/81 , C07D213/82 , C07D303/36 , C07D307/30 , C07D307/68 , C07D317/68 , C07D319/18 , C07C103/38 , C07C103/78
CPC分类号： C07D213/81 , C07D303/36 , C07D307/68 , C07D317/68 , C07D319/18 , Y10S514/926 , Y10S514/927
摘要： N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which possess ulcer-inhibiting activities.Further disclosed are pharmaceutical compositions which are effective in the treatment and prophylaxis of ulcers and which comprise as a pharmacologically active ulcus-inhibiting ingredient N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent.Further disclosed are processes for the preparation of the N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.
摘要翻译：公开了具有溃疡抑制活性的N 1 - 酰基-N 2 - 苯基-1,3-二氨基丙-2-醇。进一步公开的是有效治疗和预防溃疡的药物组合物，其包含作为药理学活性的抑制溃疡的成分N1-酰基-N-苯基-1,3-二氨基丙-2-醇，或其药学上可接受的酸加成其盐和药学上可接受的稀释剂。进一步公开了制备N1酰基-N-苯基-1,3-二氨基丙-2-醇的方法。

40. 发明授权

US4235926A Insecticidal esters 失效
标题翻译：杀虫剂
公开(公告)号：US4235926A
公开(公告)日：1980-11-25
申请号：US969862
申请日：1978-12-15
申请人： George Holan , David F. O'Keefe
发明人： George Holan , David F. O'Keefe
IPC分类号： C07C69/74 , A01N33/20 , A01N37/08 , A01N37/10 , A01N37/34 , A01N37/38 , A01N37/48 , A01N43/08 , A01N43/30 , C07C51/00 , C07C61/15 , C07C61/39 , C07C61/40 , C07C62/12 , C07C62/34 , C07C67/00 , C07C69/753 , C07C69/757 , C07C201/00 , C07C205/55 , C07C253/00 , C07C255/38 , C07C313/00 , C07C323/62 , C07D307/42 , C07D317/60 , C07D317/68 , A01N43/16 , C07D317/44
CPC分类号： A01N37/48 , A01N37/08 , A01N37/10 , A01N37/34 , A01N37/38 , A01N43/08 , A01N43/30 , C07C61/15 , C07C61/40 , C07C62/12 , C07C62/34 , C07C69/753 , C07C69/757 , C07D317/60
摘要： Compounds of the general formula I ##STR1## wherein R.sup.1 is hydrogen or a methoxy, ethoxy, propoxy, butoxy, tetrafluoroethoxy, methylthio, ethylthio, propylthio, fluoro, chloro, bromo, methyl, ethyl, or nitro group, and R.sup.2 is hydrogen or a methyl group, or R.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 is hydrogen, or a lower alkyl group, or one of the following groups (a) to (f):(a) 3-phenoxybenzyl(b) 2-benzyl-4-furylmethyl(c) .alpha.-cyano-3-phenoxybenzyl(d) 3,4-methylenedioxybenzyl(e) .alpha.-ethynyl-3-phenoxybenzyl(f) .alpha.-cyano-3-(4'-chlorophenoxy)-benzyland Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4, Y.sup.5 and Y.sup.6 are the same or different groups and each is hydrogen or a fluoro, bromo or chloro group, with the proviso that when R.sup.1 is hydrogen, fluoro, chloro, bromo or methyl and R.sup.2 is hydrogen, then one of Y.sup.1 to Y.sup.6 is other than hydrogen.The compounds in which R.sup.3 is one of groups (a) to (f) are insecticides.
摘要翻译：通式I的化合物其中R 1是氢或甲氧基，乙氧基，丙氧基，丁氧基，四氟乙氧基，甲硫基，乙硫基，丙硫基，氟，氯，溴，甲基，乙基或硝基，R 2是氢或甲基或R1和R2一起形成亚甲二氧基; R3是氢或低级烷基，或下列基团之一（a）至（f）：（a）3-苯氧基苄基（b）2-苄基-4-呋喃基甲基（c）α-氰基-3-苯氧基苄基（d）（e）α-乙炔基-3-苯氧基苄基（f）α-氰基-3-（4'-氯苯氧基） - 苄基和Y1，Y2，Y3，Y4，Y5和Y6的3,4-亚甲二氧基苄基是相同的或不同的基团，并且各自为氢或氟，溴或氯基团，条件是当R 1为氢，氟，氯，溴或甲基且R 2为氢时，则Y 1至Y 6中的一个不是氢。 R3（a）〜（f）中的一种化合物是杀虫剂。

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