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1. 发明授权

US4820734A Phenethylamine derivatives 失效
标题翻译：苯乙胺衍生物
公开(公告)号：US4820734A
公开(公告)日：1989-04-11
申请号：US117190
申请日：1987-11-04
申请人： Karl Bernauer , Hans Bruderer
发明人： Karl Bernauer , Hans Bruderer
IPC分类号： A61K31/135 , C07C205/26 , C07C205/57
CPC分类号： C07C205/57 , C07C205/26 , C07C205/45
摘要： The novel phenethylamine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R.sup.1 and R.sup.2 is different from hydrogen, R.sup.3 and R.sup.4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group --CO-- or --CHOH--, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.
摘要翻译：通式为其中R1和R2各自表示氢，卤素，三氟甲基，低级烷氧基，低级烷基，羟基或硝基的新型苯乙胺衍生物，条件是R 1和R 2中的至少一个不同于氢， R3和R4各自表示低级烷基，n表示数字1,2,3或4，B表示基团-CO-或-CHOH-，其药学上可接受的酸加成盐具有有趣的止痛和抗抑郁药性质。这些物质可以根据本身已知的各种方法制造，并且可以用作药物制剂形式的药物。

2. 发明授权

US4317914A Oxazolines 失效
标题翻译：恶唑啉
公开(公告)号：US4317914A
公开(公告)日：1982-03-02
申请号：US215965
申请日：1980-12-12
申请人： Karl Bernauer , Karlheinz Pfoertner
发明人： Karl Bernauer , Karlheinz Pfoertner
IPC分类号： C07D263/10 , A61K31/42
CPC分类号： C07D263/10 , Y10S514/866
摘要： Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are hydrogen, halogen or lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen or C.sub.1-3 alkyl; R.sup.8 is hydrogen, lower alkyl or formyl; R.sup.9 and R.sup.10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R.sup.7 and R.sup.8 are lower alkyl, n is 0 (zero) or 1,prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.
摘要翻译：式Ⅰ的化合物，其中R 1和R 2独立地是氢，卤素或低级烷基; R3，R4，R5，R6和R7独立地是氢或C1-3烷基; R8是氢，低级烷基或甲酰基; R9和R10独立地是甲基或三氟甲基; 并且n是0（零），或者当R7和R8都是低级烷基时，n是0（零）或1，特别是由可以被N-烷基取代的对氨基二苯甲醛制备。式I化合物是口服活性抗糖尿病药。

3. 发明授权

US5705703A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5705703A
公开(公告)日：1998-01-06
申请号：US784554
申请日：1997-01-21
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04 , C07C205/20
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中R a，R b和R c具有本文给出的含义。描述了其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐，并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-腺苷甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外源儿茶酚胺和具有儿茶酚结构的外源性治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物：形成本发明一部分的化合物可以根据已知方法制备。

4. 发明授权

US5236952A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5236952A
公开(公告)日：1993-08-17
申请号：US686210
申请日：1991-04-16
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中Ra，Rb和Rc具有本文给出的含义，其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐被描述并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-邻苯二甲酰甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外来儿茶酚胺和具有儿茶酚结构的非常给予的治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物; 构成本发明一部分的化合物可以根据已知方法制备。

5. 发明授权

US4360530A 5-[p-(Substituted)phenyl]-2,2-dialkyl-4-phenyl-3-oxazoline 失效
标题翻译： 5- [对 - （取代）苯基] -2,2-二烷基-4-苯基-3-恶唑啉
公开(公告)号：US4360530A
公开(公告)日：1982-11-23
申请号：US320262
申请日：1981-11-12
申请人： Karl Bernauer , Karlheinz Pfoertner
发明人： Karl Bernauer , Karlheinz Pfoertner
IPC分类号： C07D263/10 , A61K31/42
CPC分类号： C07D263/10 , Y10S514/866
摘要： Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are hydrogen, halogen or lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; R.sup.8 is hydrogen, lower alkyl or formyl; R.sup.9 and R.sup.10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R.sup.7 and R.sup.8 are lower alkyl, n is 0 (zero) or 1, prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.
摘要翻译：式Ⅰ的化合物，其中R 1和R 2独立地是氢，卤素或低级烷基; R3，R4，R5，R6和R7独立地是氢或低级烷基; R8是氢，低级烷基或甲酰基; R9和R10独立地是甲基或三氟甲基; 并且n是0（零），或者当R7和R8都是低级烷基时，n是0（零）或1，特别是由可以被N-烷基取代的对氨基二苯甲醛制备。式I化合物是口服活性抗糖尿病药。

6. 发明授权

US4234736A Antiandrogenic and schistosomicidal imidazolidine derivatives 失效
标题翻译：抗雄激素和血吸虫咪唑烷衍生物
公开(公告)号：US4234736A
公开(公告)日：1980-11-18
申请号：US954071
申请日：1978-10-24
申请人： Karl Bernauer , Helmut Link , Harro Stohler
发明人： Karl Bernauer , Helmut Link , Harro Stohler
IPC分类号： A61K31/215 , A61K31/22 , A61K31/24 , A61P5/00 , A61P33/00 , C07C67/00 , C07C239/00 , C07C275/42 , C07D233/66 , C07D233/72 , C07D233/88
CPC分类号： C07D233/72 , A61K31/24 , C07D233/88
摘要： Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
摘要翻译：咪唑烷衍生物及其制备方法，具有抗雄激素和血吸虫病活性。

7. 发明授权

US3935246A Naphthoquinones 失效
标题翻译：萘醌
公开(公告)号：US3935246A
公开(公告)日：1976-01-27
申请号：US533902
申请日：1974-12-18
申请人： Karl Bernauer , Erika Bohni , Janos Borgulya
发明人： Karl Bernauer , Erika Bohni , Janos Borgulya
IPC分类号： C07C225/30 , A61K31/12 , A61K31/13 , A61K31/135 , C07C97/22
CPC分类号： C07C46/00
摘要： Compounds represented by the formula ##SPC1##WhereinR is a cyclopentyl or cycloheptyl andR.sub.1 is a hydrogen, halogen or lower alkoxy,Processes for their production and novel intermediates as well as therapeutic preparations containing the compounds as the active ingredient for amoebicidal or bacteriostatic treatment are disclosed.
摘要翻译：由式WHEREIN R表示的化合物是环戊基或环庚基，R 1是氢，卤素或低级烷氧基，其生产和新型中间体的方法以及含有化合物作为活性成分用于抗坏血酸或杀真菌治疗的治疗方法也被公开。

8. 发明授权

US5389653A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5389653A
公开(公告)日：1995-02-14
申请号：US048685
申请日：1993-04-16
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中Ra，Rb和Rc具有本文给出的含义，其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐被描述并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-腺苷甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外源儿茶酚胺和具有儿茶酚结构的外源性治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物; 构成本发明一部分的化合物可以根据已知方法制备。

9. 发明授权

US4407814A Imidazolidine derivatives 失效
标题翻译：咪唑烷衍生物
公开(公告)号：US4407814A
公开(公告)日：1983-10-04
申请号：US330364
申请日：1981-12-14
申请人： Karl Bernauer , Helmut Link , Harro Stohler
发明人： Karl Bernauer , Helmut Link , Harro Stohler
IPC分类号： A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88
CPC分类号： C07D233/88 , C07D233/72
摘要： Imidazolidine derivatives of the formula ##STR1## wherein X is oxygen or imino and R is one of the groups ##STR2## their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
摘要翻译：描述了其中X是氧或亚氨基并且R是其中之一的组合物，其用作抗雄激素或血吸虫病活性剂以及相应的药物制剂的式Ⅰ的咪唑烷衍生物。

10. 发明授权

US4230623A Pyrrolidine derivatives 失效
标题翻译：吡咯烷衍生物
公开(公告)号：US4230623A
公开(公告)日：1980-10-28
申请号：US960352
申请日：1978-11-13
申请人： Karl Bernauer , Karlheinz Pfoertner , Fernand Schneider , Hans Schmid, deceased , by Mary Margrith Baumann-Schmid, heir , by Maria Albertine Schmid-Suter, heir , by Jeannette Martha Wawrla-Schmid, heir , by Ernst Georges Schmid-Gautschi, heir
发明人： Karl Bernauer , Karlheinz Pfoertner , Fernand Schneider , Hans Schmid, deceased , by Mary Margrith Baumann-Schmid, heir , by Maria Albertine Schmid-Suter, heir , by Jeannette Martha Wawrla-Schmid, heir , by Ernst Georges Schmid-Gautschi, heir
IPC分类号： C07D207/09 , C07D207/44
CPC分类号： C07D207/09
摘要： Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter described, prepared inter alia from the corresponding pyrrolines, are described. The compounds are useful as analgesic agents.
摘要翻译：描述了其中R 1，R 2，R 3和R 4如下文所述的式ⅩⅥ的吡咯烷衍生物，特别是由相应的吡咯烷制备。该化合物可用作止痛剂。

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