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：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：US06326378B1

公开(公告)日：2001-12-04

申请号：US09622325

申请日：2000-10-05

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

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

IPC分类号： A61K31437

CPC分类号： A61K31/437

摘要： The present invention relates to the method of treating leukemia, lymphoma or inhibiting the proliferation of cells with a compound of formula I.

摘要翻译： 本发明涉及用式I化合物治疗白血病，淋巴瘤或抑制细胞增殖的方法。

公开(公告)号：US4486442A

公开(公告)日：1984-12-04

申请号：US469856

申请日：1983-02-25

申请人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Androniki Roesch nee Apostolides ,  Wolfgang Schaumann

发明人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Androniki Roesch nee Apostolides ,  Wolfgang Schaumann

IPC分类号： A61K31/443 ,  A61K31/445 ,  A61P37/08 ,  C07D307/83 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D307/83 ,  C07D405/12

摘要： The present invention provides bicyclic phenol ethers of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom or an acyl radical,X is an oxygen or sulphur atom or an --NH-- group;Y is a --CO--CHR.sub.3 -- group or a ##STR2## group; R.sub.3 is a hydrogen atom, a lower alkyl radical which can be optionally substituted by an aryl radical, or a cycloalkyl radical containing 3 to 7 carbon atoms; andR.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, lower alkyl radicals, lower alkyl radicals, alkenyl radicals containing 2 to 16 carbon atoms, which can be optionally substituted by an aryl radical, or an aryl radical; orR.sub.4 and R.sub.5, together with the carbon atom to which they are attached, form a cycloalkyl ring containing 3 to 7 carbon atoms; and thesalts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

摘要翻译： 本发明提供以下通式的双环酚醚：其中R 1为氢原子或低级烷基，R 2为氢原子或酰基，X为氧或硫原子或 - NH-基团; Y是-CO-CHR3-基团或基团; R3是氢原子，可任意被芳基取代的低级烷基或含有3至7个碳原子的环烷基; 和可以相同或不同的R 4和R 5是氢原子，低级烷基，低级烷基，含有2至16个碳原子的烯基，其可任选被芳基或芳基取代; 或R 4和R 5与它们所连接的碳原子一起形成含有3至7个碳原子的环烷基环; 其盐与药理学上可接受的酸。 本发明还提供了制备这些化合物的方法，以及含有它们的药物组合物。

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：US4704381A

公开(公告)日：1987-11-03

申请号：US701139

申请日：1985-02-13

申请人： Wolfgang Schaumann ,  Otto-Henning Wilhelms ,  Androniki Roesch ,  Wolfgang Kampe

发明人： Wolfgang Schaumann ,  Otto-Henning Wilhelms ,  Androniki Roesch ,  Wolfgang Kampe

IPC分类号： C07H19/167 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P37/08 ,  C07H19/16 ,  C07H19/06

CPC分类号： C07H19/16 ,  A61K31/70

摘要： The present invention is concerned with the use of adenosine derivatives for the treatment of allergic diseases, as well as for bronchosphatic and broncho-constrictive reactions brought about by inflammation. The above adenosine derivatives can be used alone or together with xanthine derivatives. The invention is further concerned with compositions containing compounds of adenosine derivatives and optionally compounds of xanthine derivatives together with appropriate pharmaceutical carriers.

摘要翻译： 本发明涉及腺苷衍生物用于治疗过敏性疾病以及由炎症引起的支气管和支气管收缩反应的用途。 上述腺苷衍生物可以单独使用或与黄嘌呤衍生物一起使用。 本发明还涉及含有腺苷衍生物和任选的黄嘌呤衍生物化合物与合适的药物载体的组合物。

公开(公告)号：US4076829A

公开(公告)日：1978-02-28

申请号：US626512

申请日：1975-10-28

申请人： Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

发明人： Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

IPC分类号： C07D209/43 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P25/02 ,  C07D209/08 ,  C07D209/12 ,  C07D209/32 ,  C07D209/42 ,  C07D209/14

CPC分类号： C07D209/42 ,  C07D209/08 ,  C07D209/12 ,  Y10S514/927

摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen andThe pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.

摘要翻译： 式（I）的新的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟基烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 相同或不同，代表氢或低级烷基，R2是低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R是烷硫基烷基或R1是新戊酰氧基烷基时，R2也可以是氢，并且其药学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

公开(公告)号：US4229464A

公开(公告)日：1980-10-21

申请号：US943512

申请日：1978-09-18

申请人： Wolfgang Kampe ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

发明人： Wolfgang Kampe ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

IPC分类号： C07D209/43 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P25/02 ,  C07D209/08 ,  C07D209/12 ,  C07D209/32 ,  C07D209/42 ,  C07D209/18 ,  C07D209/20

CPC分类号： C07D209/42 ,  C07D209/08 ,  C07D209/12 ,  Y10S514/927

摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.

摘要翻译： 新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏和循环系统疾病方面非常有效。

公开(公告)号：US4152446A

公开(公告)日：1979-05-01

申请号：US805558

申请日：1977-06-10

申请人： Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

发明人： Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

IPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  A61K31/40 ,  C07D209/04

CPC分类号： C07D209/42 ,  C07D209/08 ,  C07D209/12

摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof;Are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.

摘要翻译： 新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

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。