公开(公告)号：US4143149A

公开(公告)日：1979-03-06

申请号：US790648

申请日：1977-04-25

申请人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Bartsch ,  Egon Roesch

发明人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Bartsch ,  Egon Roesch

IPC分类号： A61K31/415 ,  A61P9/00 ,  A61P25/02 ,  C07D231/56

CPC分类号： C07D231/56

摘要： New indazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; andR.sub.2 is straight-chain or branched lower alkyl which can be substituted by lower alkylthio;And the pharmacologically compatible salts thereof; are outstandingly effective adrenergic .beta.-receptor inhibitors and useful in the treatment or prevention of a recurrence of cardiac and circulatory diseases.

公开(公告)号：US4517183A

公开(公告)日：1985-05-14

申请号：US495548

申请日：1983-05-17

申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

CPC分类号： C07D203/22 ,  Y10S514/885

摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

公开(公告)号：US4330549A

公开(公告)日：1982-05-18

申请号：US104205

申请日：1979-12-17

申请人： Walter-Gunar Friebe ,  Werner Winter ,  Max Thiel ,  Androniki Roesch ,  Otto-Henning Wilhelms

发明人： Walter-Gunar Friebe ,  Werner Winter ,  Max Thiel ,  Androniki Roesch ,  Otto-Henning Wilhelms

IPC分类号： C07D409/14 ,  A61K31/085 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4468 ,  A61K31/4709 ,  A61P9/12 ,  A61P37/00 ,  A61P37/08 ,  C07D215/02 ,  C07D233/60 ,  C07D311/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/14 ,  A61K31/445 ,  C07D311/16

CPC分类号： C07D401/12 ,  Y10S514/826

摘要： The present invention provides aryl ether derivatives of the general formula: ##STR1## wherein A is an oxygen atom or the group >N--R.sub.1, R.sub.1 being a hydrogen atom or a lower alkyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.4 is a hydrogen atom or a hydroxyl group, R.sub.5 is a hydrogen atom or an acyl radical, R.sub.7 is a hydrogen atom, a lower alkyl radical or a lower alkanoyl radical and R.sub.8 is a hydrogen atom, a lower alkyl radical, a lower alkoxy radical or a hydroxyl group; and the pharmacologically acceptable salts thereof.The present invention also provides a process for the preparation of these compounds and pharmaceutical compositions containing them. It is also concerned with the use of these compounds for combating allergic diseases.

摘要翻译： 本发明提供以下通式的芳醚衍生物：其中A为氧原子或基团> N-R 1，R 1为氢原子或低级烷基，R 2和R 3可以相同或为 不同的是氢原子或低级烷基，R4是氢原子或羟基，R5是氢原子或酰基，R7是氢原子，低级烷基或低级烷酰基，R8是氢 原子，低级烷基，低级烷氧基或羟基; 及其药理学上可接受的盐。 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。 还关注这些化合物用于防治过敏性疾病。

公开(公告)号：US4212866A

公开(公告)日：1980-07-15

申请号：US006050

申请日：1979-01-24

申请人： Walter-Gunar Friebe ,  Max Thiel ,  Androniki Roesch ,  Otto-Henning Wilhelms ,  Wolfgang Schaumann

发明人： Walter-Gunar Friebe ,  Max Thiel ,  Androniki Roesch ,  Otto-Henning Wilhelms ,  Wolfgang Schaumann

IPC分类号： A61K31/52 ,  A61P29/00 ,  A61P37/08 ,  C07D211/58 ,  C07D473/34 ,  C07D473/00

CPC分类号： C07D473/34 ,  C07D211/58 ,  Y10S514/826

摘要： Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R.sub.1 and the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom or an acyl radical,or salts thereof with pharmacologically acceptable acids, characterized by anti-allergic, anti-inflammatory and anti-oedematous activity.

摘要翻译： 新颖的式[IMAGE]的9- [3-（4-氨基 - 哌啶子基） - 丙基] - 腺嘌呤衍生物，其中R1是氢原子或低级烷基，R2是氢原子，芳基，低级烷基 基团，羟基低级烷基或与R 1和它们所连接的氮原子一起形成杂环，并且R 3是氢原子或酰基，或其与药理学上可接受的酸的盐，其特征在于抗过敏 ，抗炎和抗水肿活性。

公开(公告)号：US4053624A

公开(公告)日：1977-10-11

申请号：US573214

申请日：1975-04-30

申请人： Manfred Hubner ,  Ruth Heerdt ,  Felix Schmidt ,  Max Thiel

发明人： Manfred Hubner ,  Ruth Heerdt ,  Felix Schmidt ,  Max Thiel

IPC分类号： C07D209/12 ,  A61K31/40

CPC分类号： C07D209/12 ,  Y10S514/866

摘要： New indole-2-carbaldehyde compounds of the formula ##STR1## wherein R.sub.1 is lower alkylR.sub.2 is hydrogen, halogen, or lower alkyl or alkoxy,With the proviso that when R.sub.2 is halogen or ethyl,R.sub.1 can also be hydrogenAnd the physiologically compatible derivatives thereof, are outstandingly effective in lowering excessive blood sugar in mammals.

公开(公告)号：US4348401A

公开(公告)日：1982-09-07

申请号：US185839

申请日：1980-09-10

申请人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Schaumann ,  Otto-Henning Wilhelms

发明人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Schaumann ,  Otto-Henning Wilhelms

IPC分类号： A61K31/4427 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61P11/14 ,  A61P37/00 ,  C07D211/22 ,  C07D211/58 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/455 ,  C07D403/12 ,  C07D407/12

CPC分类号： C07D211/58 ,  C07D211/22 ,  Y10S514/87

摘要： An N-phenoxyalkylpiperidine derivative of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, an acyl radical or an optionally substituted aryl radical, R.sub.2 is a hydroxymethyl radical, a cyano group, an amidino group, an amidino group substituted by hydroxyl, a 1H tetrazol-5-yl radical or a --CO--R.sub.3 radical, R.sub.3 is a hydroxyl group, a lower alkoxy radical, an amino group, or an amino group substituted by a 1H-tetrazol-5-yl radical, X is an imino group or an oxymethyl radical, A is an alkylene radical containing 2 to 4 carbon atoms, and B is a valency bond or a 4-hydroxypyrimidin-2,5-diyl radical; or a pharmacologically acceptable salt thereof. The compounds exhibit anti-histaminic, anti-oedematous and anti-phlogistic activity.

摘要翻译： 其中R 1是氢原子，酰基或任意取代的芳基，R 2是羟甲基，氰基，脒基，被羟基取代的脒基， 1H-四唑-5-基或-CO-R 3基团，R 3是羟基，低级烷氧基，氨基或被1H-四唑-5-基取代的氨基，X是亚氨基 基团或氧甲基，A是含有2至4个碳原子的亚烷基，B是价键或4-羟基嘧啶-2,5-二基; 或其药理学上可接受的盐。 该化合物表现出抗组胺，抗氧化和抗病毒活性。

公开(公告)号：US4258058A

公开(公告)日：1981-03-24

申请号：US15536

申请日：1979-02-26

申请人： Ernst-Christian Witte ,  Hans P. Wolff ,  Max Thiel ,  Karlheinz Stegmeier ,  Egon Roesch

发明人： Ernst-Christian Witte ,  Hans P. Wolff ,  Max Thiel ,  Karlheinz Stegmeier ,  Egon Roesch

IPC分类号： A61K31/19 ,  A61K31/165 ,  A61K31/195 ,  A61K31/22 ,  A61P3/06 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C303/40 ,  C07C311/03 ,  C07C311/04 ,  C07C311/06 ,  C07C311/14 ,  C07C311/16 ,  C07C311/17 ,  C07C311/29 ,  C07D209/48 ,  C07C143/78 ,  A61K31/24

CPC分类号： C07D209/48

摘要： Phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein R is hydrogen or lower alkylR.sub.1 is alkyl or aryl, aralkyl or aralkenyl radical, the aryl moiety of which can be substituted one or more times by halogen, hydroxyl, trifluoromethyl or lower alkyl, alkoxy or acylR.sub.2 and R.sub.3 are individually selected from hydrogen or lower alkyl, andn is 0, 1, 2 or 3and the physiologically acceptable salts, esters and amides thereof; are outstandingly effective in inhibiting thrombocyte aggregation.

摘要翻译： 其中R为氢或低级烷基R 1的苯氧基烷基羧酸化合物为烷基或芳基，芳烷基或芳烯基，其芳基部分可被卤素，羟基，三氟甲基或低级烷基烷氧基取代一次或多次 或酰基R2和R3分别选自氢或低级烷基，n为0,1,2或3及其生理上可接受的盐，酯和酰胺; 在抑制血小板聚集方面效果显着。

公开(公告)号：US4153728A

公开(公告)日：1979-05-08

申请号：US733542

申请日：1976-10-18

申请人： Hans P. Wolff ,  Ernst-Christian Witte ,  Max Thiel ,  Harald Stork ,  Egon Roesch

发明人： Hans P. Wolff ,  Ernst-Christian Witte ,  Max Thiel ,  Harald Stork ,  Egon Roesch

IPC分类号： A61K31/215 ,  A61K20060101 ,  A61K31/16 ,  A61K31/19 ,  A61K31/22 ,  A61P3/06 ,  A61P7/02 ,  C07C20060101 ,  C07C51/00 ,  C07C59/68 ,  C07C67/00 ,  C07C69/734 ,  C07C69/76 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C235/34 ,  C07C235/48 ,  C07C101/42 ,  A01N9/20

CPC分类号： C07C2101/14 ,  Y10S514/824

摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms;N is 1 or 2 andR.sub.1, r.sub.2 and R.sub.3 are hydrogen or lower alkyl; and the pharmacologically compatible salts thereof; have been found to be outstandingly effective in lowering the serum lipid level and the cholesterol level in mammals without inducing undesired side effects and to possess excellent thrombocyte-aggregation inhibiting activity.

摘要翻译： 式（I）的新型苯氧基烷基羧酸化合物，其中B是含有至多3个碳原子的价键或直链或支链，饱和或不饱和的烃基; N 1 OR 2，R 1，R 2和R 3为氢或低级烷基; 和其药理学上相容的盐; 已被发现在降低哺乳动物血清脂质水平和胆固醇水平而没有诱导不期望的副作用并且具有优异的血小板聚集抑制活性方面是非常有效的。

公开(公告)号：US3996361A

公开(公告)日：1976-12-07

申请号：US531420

申请日：1974-12-10

申请人： Walter-Gunar Friebe ,  Max Thiel ,  Werner Winter ,  Androniki Roesch ,  Wolfgang Schaumann

发明人： Walter-Gunar Friebe ,  Max Thiel ,  Werner Winter ,  Androniki Roesch ,  Wolfgang Schaumann

IPC分类号： C07D473/34 ,  A61K31/395 ,  A61K31/50 ,  A61K31/52 ,  C07D20060101 ,  C07D241/04 ,  C07D295/04 ,  C07D295/12 ,  C07D295/13 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D473/00 ,  C07D475/06

CPC分类号： Y10S514/826

摘要： A N.sup.6 -substituted-9-[3-(4-phenyl-piperazino)-propyl]-adenine of the formula ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl radical, andR.sub.2 is a lower alkyl radical, a lower alkyl radical substituted by at least one of phenyl and hydroxyl, a lower alkenyl radical, a cycloalkyl radical or an aryl radical, orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a piperidine, pyrrolidine or morpholine ring, andR.sub.3 is hydrogen, halogen, a lower alkyl radical or a lower alkoxy radical,Or a salt thereof with a pharmacologically compatible acid, which compounds are characterized by marked anti-edematous activity as well as by activity in reducing capillary permeability.

摘要翻译： 式（I）的N6-取代-9- [3-（4-苯基 - 哌嗪子基） - 丙基] - 腺嘌呤，其中R 1是氢或低级烷基，R 2是低级烷基， 被苯基和羟基中的至少一个取代的低级烷基，低级烯基，环烷基或芳基，或者R 1和R 2与它们所连接的氮原子一起形成哌啶，吡咯烷或吗啉环，以及 R3是氢，卤素，低级烷基或低级烷氧基，或其盐与药理学上相容的酸，其化合物由标记的抗病毒活性表征，以及活性降低毛细管渗透性。

公开(公告)号：US3982012A

公开(公告)日：1976-09-21

申请号：US585645

申请日：1975-06-10

申请人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Bartsch ,  Wolfgang Schaumann

发明人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Wolfgang Bartsch ,  Wolfgang Schaumann

IPC分类号： C07D235/06 ,  A61K31/4184 ,  C07D235/08

CPC分类号： C07D235/08

摘要： New 4-hydroxy-benzimidazole compounds of the formula: ##EQU1## wherein R.sub.1 is straight-chained or branched alkyl andR.sub.2 is hydrogen atom or lower alkylAnd the pharmacologically compatible salts thereof; are outstandingly effective in the treatment and prophylaxis of cardiac and circulatory diseases, and provide substantially greater margins of safety than prior art adrenergic .beta.-receptor inhibitors.

摘要翻译： 新的下式的4-羟基 - 苯并咪唑化合物：OH | O-CH 2 -CH-CH 2 -NH-R 1（I）其中R 1是直链或支链烷基，R 2是氢原子或低级烷基，并且其药理学上可兼容的盐 ; 在治疗和预防心脏病和循环系统疾病方面非常有效，并且提供比现有抗生素β受体抑制剂更安全的重要安全标志。