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1. 发明授权

US4704464A Tumor retarding (1-benzyl-ethylenediamine)-platin (II)-complexes 失效
标题翻译：肿瘤抑制（1-苄基 - 乙二胺） - 铂（II） - 复合物
公开(公告)号：US4704464A
公开(公告)日：1987-11-03
申请号：US831911
申请日：1986-02-21
申请人： Henri Brunner , Helmut Schonenberger , Manfred Schmidt , Ulrich Holzinger , Gerfried Unger , Jurgen Engel
发明人： Henri Brunner , Helmut Schonenberger , Manfred Schmidt , Ulrich Holzinger , Gerfried Unger , Jurgen Engel
IPC分类号： A61K31/28 , A61K31/555 , A61P35/00 , C07F15/00
CPC分类号： C07F15/0093
摘要： There are described (1-benzylethylenediamine)-platin(II)-complexes of the general formula: ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a benzyl group, or a phenylethyl group, and B is a thienyl radical, an indolyl radical, an imidazolyl radical, or a phenyl radical substituted by the radicals R.sub.5, R.sub.6, an R.sub.7 which are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, phenoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, C.sub.1 -C.sub.6 -alkanesulfonyloxy, carboxy, C.sub.1 -C.sub.6 -carbalkoxy, cyano, aminocarboxyl, aminocarbonyl, which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkylcarbonyl, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, (C.sub.1 -C.sub.6 -alkyl).sub.3 N.sup.+, C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkanesulfonylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanesulfonylamino, aminosulfonyl, aminosulfonyl which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkoxysulfonyl (--SO.sub.2 --O--C.sub.1 --C.sub.6 -alkyl), sulfo (--SO.sub.3 H) or C.sub.1 -C.sub.6 -alkanesulfonyl and two of these groups can be the methylenedioxy group and X is the equivalent of a physiologically compatible anion, as well as optionally their salts with physiologically compatible cations and anions and process of their production.
摘要翻译：描述了通式如下的（1-苯乙二胺） - 铂（II） - 复合物：其中基团R 1，R 2，R 3和R 4相同或不同，为氢，C 1 -C 6 - 烷基，苄基或苯基乙基，B是噻吩基，吲哚基，咪唑基或被基团R5，R6，R7相同或不同并且为氢的卤素取代的苯基，卤素，三卤代甲基，C 1 -C 6烷基，羟基，C 1 -C 6 - 烷氧基，苯氧基，苄氧基，C 1 -C 6 - 烷酰氧基，苯甲酰氧基，C 1 -C 6烷基磺酰氧基，羧基，C 1 -C 6烷氧基，氰基，氨基羰基，氨基羰基含有一个或两个C 1 -C 6烷基，C 1 -C 6烷基羰基，硝基，氨基，C 1 -C 6烷基氨基，二-C 1 -C 6烷基氨基，（C 1 -C 6烷基）3 N +，C 1 -C 6烷酰基氨基，含有一个或两个C 1 -C 6烷基的C 1 -C 6烷基-C 1 -C 6烷酰基氨基，C 1 -C 6烷基磺酰基氨基，C 1 -C 6烷基-C 1 -C 6烷基磺酰基氨基，氨基磺酰基，氨基磺酰基，C 1 -C 6烷氧基磺酰基（-SO 2 -O-C 1 -C 6-a 烷基），磺基（-SO 3 H）或C 1 -C 6 - 烷基磺酰基，并且这些基团中的两个可以是亚甲二氧基，X是生理上相容的阴离子的当量，以及任选的与生理上相容的阳离子和阴离子的盐以及他们的生产。

2. 发明授权

US4704387A N-benzyl, phenethyl, methoxyethyl or allyl substituted benzylphthalazinones having antiallergic and antihistamine action 失效
标题翻译：具有抗过敏和抗组胺作用的N-苄基，苯乙基，甲氧基乙基或烯丙基取代的苄基酞嗪酮
公开(公告)号：US4704387A
公开(公告)日：1987-11-03
申请号：US764995
申请日：1985-08-12
申请人： Jurgen Engel , Gerhard Scheffler
发明人： Jurgen Engel , Gerhard Scheffler
IPC分类号： C07D403/06 , A61K31/55 , A61P37/08 , C07D237/00 , C07D403/04 , C07D223/12 , C07D237/32
CPC分类号： C07D403/04
摘要： Compounds of the formula ##STR1## wherein R is a benzyl group, a phenylethyl group, a methoxyethyl group or an allyl group having an antiallergic activity.
摘要翻译：其中R为苄基，苯基乙基，甲氧基乙基或具有抗过敏活性的烯丙基的式Ⅰ化合物。

3. 发明授权

US4065501A Basic enol ether and acid addition salts thereof 失效
标题翻译：碱性烯醇醚及其酸加成盐
公开(公告)号：US4065501A
公开(公告)日：1977-12-27
申请号：US557535
申请日：1975-03-12
申请人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
发明人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
IPC分类号： A61K31/135 , A61K31/075 , A61K31/13 , A61P9/08 , C07C67/00 , C07C213/00 , C07C217/08 , C07C217/10 , C07C217/12 , C07D213/30 , C07D295/088 , C07D295/092 , C07D333/16 , C07C91/16
CPC分类号： C07D295/088 , C07D333/16
摘要： The present invention is related to new basic enol ethers having the general formula ##STR1## and to the pharmacologically acceptable acid addition salts thereof. The invention is further related to process for the treatment of spasmodic conditions in humans by administering a compound of the above general formula or a pharmacologically acceptable acid addition salt thereof to a human suffering from such conditions.
摘要翻译：本发明涉及具有通式“IMAGE”的新的碱性烯醇醚及其药学上可接受的酸加成盐。本发明还涉及通过向患有这些病症的人施用上述通式的化合物或其药理学上可接受的酸加成盐来治疗人的痉挛状况的方法。

4. 发明授权

US4124716A Process for the treatment of spasmodic conditions in humans 失效
标题翻译：治疗人体痉挛状况的方法
公开(公告)号：US4124716A
公开(公告)日：1978-11-07
申请号：US842092
申请日：1977-10-14
申请人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
发明人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
IPC分类号： C07D295/088 , C07D333/16 , A61K27/00 , A61K31/135 , A61K31/40 , A61K31/445
CPC分类号： C07D295/088 , C07D333/16
摘要： Process for the treatment of spasmodic conditions in humans by administering a compound of the general formula ##STR1## or a pharmacologically acceptable acid addition salt thereof to a human suffering from such conditions.
摘要翻译：通过向患有这些病症的人施用通式为“IMAGE”的化合物或其药学上可接受的酸加成盐来治疗人类痉挛状况的方法。

5. 发明授权

US4239761A Basically substituted ureas and processes for the treatment of virus diseases 失效
标题翻译：用于治疗病毒性疾病的基本取代的脲和方法
公开(公告)号：US4239761A
公开(公告)日：1980-12-16
申请号：US69335
申请日：1979-08-23
申请人： Rolf Rebling , Gerhard Scheffler , Klaus Pressler , Klaus D. Schenk
发明人： Rolf Rebling , Gerhard Scheffler , Klaus Pressler , Klaus D. Schenk
IPC分类号： C07D295/12 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P1/00 , A61P11/00 , A61P25/00 , A61P31/12 , C07D295/13 , C07D295/20 , C07D295/215 , C07D295/22 , C07D295/26 , C07D295/10 , C07D295/16
CPC分类号： C07D295/215 , C07D295/13 , C07D295/26 , Y10S514/849 , Y10S514/888 , Y10S514/894 , Y10S514/915 , Y10S514/934
摘要： The present invention is related to new basically substituted ureas having the general Formula I ##STR1## and the pharmaceutically acceptable acid addition salts thereof which produce an improved antiviral activity against DNS- and RNS-viruses. The invention is further related to the treatment of humans or animals suffering from diseases caused by viruses by administering compositions containing such ureas or salts thereof as active agent.
摘要翻译：本发明涉及具有通用式I的新基本取代的脲和其药学上可接受的酸加成盐，其产生针对DNS-和RNS-病毒的改进的抗病毒活性。本发明还涉及通过施用含有这种脲或其盐作为活性剂的组合物治疗患有由病毒引起的疾病的人或动物。

6. 发明授权

US4220660A Process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents 失效
标题翻译：用于治疗由细胞活性的活性烷化剂引起的不希望的尿毒性副作用的人的治疗方法
公开(公告)号：US4220660A
公开(公告)日：1980-09-02
申请号：US967000
申请日：1978-12-06
申请人： Norbert Brock
发明人： Norbert Brock
IPC分类号： A61K31/185 , A61K31/675 , A61P35/00 , A61P39/02
CPC分类号： A61K31/675 , A61K31/185
摘要： The invention is related to a process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents administered to them against malign tumors, comprising administering a pharmacologically acceptable salt of a mercapto alkane sulfonic acid having the general formulaHS--alk--SO.sub.3 4to the human treated with the cytostatically active alkylating agent, in an amount ranging from 20% of the weight of the alkylating agent to the highest tolerated dosage of the salt of the mercapto alkane sulfonic acid, simultaneously or separately in combination with the alkylating agent.
摘要翻译：本发明涉及一种治疗患有由恶性肿瘤施用的细胞活性的烷化剂引起的不利的尿毒性副作用的人的方法，包括给予具有通式HS-alk的巯基烷烃磺酸的药学上可接受的盐 -SO34至用细胞活性的烷化剂处理的人，其量为烷基化剂重量的20％至巯基烷烃磺酸的盐的最高耐受剂量，同时或分开地与烷基化代理商

7. 发明授权

US4218471A Process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents 失效
标题翻译：用于治疗由细胞活性的活性烷化剂引起的不希望的尿毒性副作用的人的治疗方法
公开(公告)号：US4218471A
公开(公告)日：1980-08-19
申请号：US9625
申请日：1979-02-06
申请人： Norbert Brock , Jurij Stekar
发明人： Norbert Brock , Jurij Stekar
IPC分类号： A61K31/185 , A61K31/675 , A61P35/00 , C07C67/00 , C07C313/00
CPC分类号： A61K31/185 , A61K31/675
摘要： The invention is related to a process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents administered to them against malign tumors, comprising administering a pharmacologically acceptable salt of a dithiodi-(alkane sulfonic acid) having the general formula ##STR1## to the human treated with the cytostatically active alkylating agent, in an amount ranging from 20% of the weight of the alkylating agent to the highest tolerated dosage of the salt of the dithiodi-(alkane sulfonic acid), simultaneously or separately in combination with the alkylating agent.
摘要翻译：本发明涉及一种用于治疗患有由恶性肿瘤施用的细胞活性的烷化剂引起的不利的尿毒性副作用的人的方法，包括给予具有通式（II）的二硫代（烷烃磺酸）的药学上可接受的盐对于用细胞活性活性烷化剂处理的人，其量为烷基化剂重量的20％至二硫代（烷烃磺酸）的盐的最高耐受剂量，同时或分开地与烷基化剂组合。

8. 发明授权

US4730068A Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes 失效
标题翻译：抗肿瘤剂（1,2-二苯基 - 乙二胺） - 铂（II） - 复合物
公开(公告)号：US4730068A
公开(公告)日：1988-03-08
申请号：US831913
申请日：1986-02-21
申请人： Helmut Schonenberger , Erwin von Angerer , Johann Karl , Margaretha Jennerwein , Jurgen Engel
发明人： Helmut Schonenberger , Erwin von Angerer , Johann Karl , Margaretha Jennerwein , Jurgen Engel
IPC分类号： A61K31/28 , A61P35/00 , C07C45/29 , C07C45/51 , C07C45/56 , C07C47/575 , C07F15/00
CPC分类号： C07F15/0093 , C07C45/298 , C07C45/515 , C07C45/562 , C07C47/575
摘要： There are disclosed antitumor active 1,2-diphenyl-ethylenediamine)-platinum(II)-complex of the general formula ##STR1## wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl and R.sub.2 is either (1) a halogen atom and the groups R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydrogen C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, or R.sub.2 is (2) a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group in the 4-position or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and if R.sub.2 is (2) then the groups R.sub.1 and R.sub.3 which are the same or differnt are in the 2 and 6 positions of the phenyl group and are halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, a C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alklanoyloxy group or a halo or C.sub.1 -C.sub.5 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, with the proviso that R.sub.1 can also be hydrogen and the groups R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy group or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and X is the equivalent of a physiologically compatible anion and process of their production.
摘要翻译：公开了具有通式“IMAGE”I的抗肿瘤活性的1,2-二苯基 - 乙二胺） - 铂（II） - 复合物，其中R 7是氢或C 1 -C 6 - 烷基，R 2是（1）卤素原子，基团R 1，R 3，R 4，R 5和R 6相同或不同，为氢，卤素，三卤甲基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，或R 2为（2）羟基，C 1 -C 6 - 烷氧基，C 4 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧取代 C 2 -C 6 - 烷酰氧基，如果R 2为（2），则相同或不同的基团R 1和R 3为苯基的2和6位，为卤素，三卤代甲基，C 1 -C 6烷基，羟基， C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 5 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，条件是R 1也可以是氢，基团R 4，R 5和R 6是相同或不同的氢，卤素，三卤代甲基，C 1 -C 6 - 烷基，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，X等同于生理上相容的阴离子及其生产方法。

9. 发明授权

US4623742A Oxazaphosphorin-4-thio-alkanesulphonic acids, and neutral salts thereof 失效
标题翻译：氧氮杂磷素-4-硫代烷基磺酸及其中性盐
公开(公告)号：US4623742A
公开(公告)日：1986-11-18
申请号：US683374
申请日：1984-12-19
申请人： Gerhard Scheffler , Ulf Niemeyer , Norbert Brock , Jorg Pohl
发明人： Gerhard Scheffler , Ulf Niemeyer , Norbert Brock , Jorg Pohl
IPC分类号： C07F9/24 , A61K31/675 , A61P35/00 , C07F9/6584 , C07F9/21
CPC分类号： C07F9/65846
摘要： This invention relates to new oxazaphosphorin-4-thio-alkanesulphonic acids and to the neutral salts thereof corresponding to the general formula I ##STR1## and to methods to use such compounds to control cancer diseases and to produce immunosuppression in humans and animals.
摘要翻译：本发明涉及新的恶唑磷蛋白-4-硫代烷基磺酸及其对应于通式Ⅰ“IMAGE”的中性盐，以及使用这些化合物来控制癌症疾病并在人和动物中产生免疫抑制的方法。

10. 发明授权

US4618692A 4-carbamoyloxy-oxazaphosphorins 失效
标题翻译： 4-氨基甲酰氧基 - 恶唑磷
公开(公告)号：US4618692A
公开(公告)日：1986-10-21
申请号：US579570
申请日：1984-02-13
申请人： Gerhard Scheffler , Ulf Niemeyer , Norbert Brock , Jorg Pohl
发明人： Gerhard Scheffler , Ulf Niemeyer , Norbert Brock , Jorg Pohl
IPC分类号： C07F9/6584 , C07F9/24 , C07F9/65
CPC分类号： C07F9/65846
摘要： The present invention relates to new 4-carbamoyloxy-oxazaphosphorins of the general Formula I ##STR1## as well as to a method for the treatment of malign tumor diseases in humans using such compounds as active agent.
摘要翻译：本发明涉及通式Ⅰ“IMAGE”I的新的4-氨基甲酰氧基 - 恶唑磷酸，以及使用这些化合物作为活性剂治疗人类恶性肿瘤疾病的方法。

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