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21. 发明授权

US06369088B2 Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use as pharmaceuticals 有权
标题翻译：取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其作为药物的用途
公开(公告)号：US06369088B2
公开(公告)日：2002-04-09
申请号：US09799082
申请日：2001-03-06
申请人： Karl Schoenafinger , Stefan Petry , Guenter Mueller , Karl-Heinz Baringhaus
发明人： Karl Schoenafinger , Stefan Petry , Guenter Mueller , Karl-Heinz Baringhaus
IPC分类号： C07D271113
CPC分类号： C07D271/113 , C07D413/10 , C07D413/12
摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, in which R1 is substituted C1-C6-alkyl and C3-C9-cycloalkyl, R2, R3, R4 and R5 are hydrogen, halogen, nitro, C1-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O—C3—C8-cycloalkyl, or 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with the proviso that R2, R3, R4 and R5 are not simultaneously hydrogen, and at least one of the radicals R2, R3, R4 or R5 is the radical 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, wherein R6=hydrogen, C1-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A=a single bond, COn, SOn or CONH, n=1 or 2, R7=hydrogen, substituted C1-C18-alkyl, C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, biphenylyl, biphenylyl-C1-C4-alkyl, indanyl, or the group Het-(CH2)r—, wherein r=0, 1, 2 or 3 and Het=a saturated or unsaturated 5-7-membered heterocycle, which may be optionally benzo-fused and optionally substituted, and proceses for their preparation. The compounds of formula 1 show an inhibitory effect on hormone-sensitive lipase, HSL.
摘要翻译：描述了式1的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，其中R 1是取代的C 1 -C 6 - 烷基和C 3 -C 9 - 环烷基，R 2，R 3，R 4和 R 5是氢，卤素，硝基，C 1 -C 4 - 烷基，C 1 -C 9 - 烷氧基，取代的C 6 -C 10 - 芳基-C 1 -C 4 - 烷氧基，C 6 -C 10 - 芳氧基，C 6 -C 10 - 芳基，C 3 -C 8 - 或O-C 3 -C 8 - 环烷基或2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，条件是R2，R3，R4和R5不同时为氢，并且基团R 2，R 3，R 4或R 5中的至少一个是基团2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，其中R6 =氢，C1-C4- 烷基或取代的C 6 -C 10 - 芳基-C 1 -C 4烷基，A =单键，COn，SO n或CONH，n = 1或2，R 7 =氢，取代的C 1 -C 18烷基，C 2 -C 18 - 烯基， C 6 -C 10 - 芳基-C 1 -C 4烷基，C 5 -C 8 - 环烷基-C 1 -C 4烷基，C 5 -C 8 - 环烷基，C 6 -C 10 - 芳基-C 2 -C 6 - 烯基，C 6 -C 10 - 芳基，联苯基，联苯基-C 1 -C 4烷基，二氢化茚基或Het-（CH 3）

22. 发明授权

US5726305A Substituted quinoline-2-carboxamides, their preparation and their use as pharmaceuticals, and intermediates 失效
公开(公告)号：US5726305A
公开(公告)日：1998-03-10
申请号：US675155
申请日：1996-07-03
申请人： Klaus Weidmann , Karl-Heinz Baringhaus , Georg Tschank , Martin Bickel
发明人： Klaus Weidmann , Karl-Heinz Baringhaus , Georg Tschank , Martin Bickel
IPC分类号： A61K31/47 , A61P1/16 , A61P11/00 , A61P17/00 , A61P37/00 , A61P43/00 , C07D215/48 , C07D215/60 , C07K5/078 , C07D215/14 , C07D215/20
CPC分类号： C07K5/06139 , C07D215/48
摘要： The invention relates to substituted quinoline-2-carboxylic acid amides of the formula I ##STR1## their preparation and their use, and intermediates which are formed in the preparation of the compounds of the formula I. The compounds according to the invention are used as inhibitors of prolyl 4-hydroxylase and as pharmaceuticals (medicaments) for treatment of fibrotic diseases.

23. 发明授权

US08933024B2 Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases 有权
标题翻译：偶氮吡啶-3-酮衍生物作为脂肪酶和磷脂酶的抑制剂
公开(公告)号：US08933024B2
公开(公告)日：2015-01-13
申请号：US13805289
申请日：2011-06-17
申请人： Stefan Petry , Norbert Tennagels , Karl-Heinz Baringhaus
发明人： Stefan Petry , Norbert Tennagels , Karl-Heinz Baringhaus
IPC分类号： A61K38/28 , A61P5/50 , C07D513/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/5383
CPC分类号： C07D513/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K45/06
摘要： The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
摘要翻译：本发明涉及具有本说明书中规定的含义的通式（I）的苯并吡喃-3-酮衍生物及其药学上可用的盐及其作为药物物质的用途。

24. 发明申请

US20090215824A1 INDAZOLE DERIVATIVES AS INHIBITORS OF HORMONE SENSITIVE LIPASE 有权
标题翻译：作为HORMONE敏感性脂质体的抑制剂的吲哚衍生物
公开(公告)号：US20090215824A1
公开(公告)日：2009-08-27
申请号：US12431010
申请日：2009-04-28
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Karl-Heinz Baringhaus
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Karl-Heinz Baringhaus
IPC分类号： A61K31/454 , C07D401/04
CPC分类号： C07D413/12 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D495/04
摘要： The present invention relates to indazole derivatives of the general formulae I or II having the meanings indicated in the description, to the pharmaceutically useful salts thereof and the use thereof as drugs.
摘要翻译：本发明涉及具有本说明书所示含义的通式I或II的吲唑衍生物，其药学上可用的盐及其作为药物的用途。

25. 发明申请

US20090030011A1 TRIAZOLOPYRIDINE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES 有权
标题翻译：作为药物和磷脂的抑制剂的三唑吡啶衍生物
公开(公告)号：US20090030011A1
公开(公告)日：2009-01-29
申请号：US12099922
申请日：2008-04-09
申请人： Stefan Petry , Gerhard Zoller , Gunter Muller , Karl-Heinz Baringhaus , Hubert Heuer
发明人： Stefan Petry , Gerhard Zoller , Gunter Muller , Karl-Heinz Baringhaus , Hubert Heuer
IPC分类号： A61K31/437 , A61P3/00 , C07D471/04 , A61K31/4725 , A61K31/4709 , A61K31/4545 , A61K31/496
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to triazolopyridine derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.
摘要翻译：本发明涉及通式（I）的三唑并吡啶衍生物，其定义如本说明书中引用的其药学上可应用的盐及其作为药物的用途。

26. 发明授权

US07453000B2 Substituted oxazolobenzoisothiazole dioxide derivatives method for production and use thereof 有权
标题翻译：取代的氧杂二氮杂异噻唑二氧化物衍生物的制备方法及其用途
公开(公告)号：US07453000B2
公开(公告)日：2008-11-18
申请号：US11560602
申请日：2006-11-16
申请人： Stefan Petry , Norbert Tennagels , Reinhard Kirsch , Karl-Heinz Baringhaus
发明人： Stefan Petry , Norbert Tennagels , Reinhard Kirsch , Karl-Heinz Baringhaus
IPC分类号： C07D275/04 , A01N43/80
CPC分类号： C07D417/14 , C07D417/12
摘要： The invention relates to compounds of formula (I), where the groups have the meanings set forth herein and the physiologically-acceptable salts thereof. The compounds are suitable as medicaments for lowering blood sugar levels and for prevention and treatment of diabetes.
摘要翻译：本发明涉及式（I）化合物，其中基团具有本文所述的含义及其生理上可接受的盐。该化合物适用于降低血糖水平和预防和治疗糖尿病的药物。

27. 发明申请

US20080032984A1 Pyrimido[5,4-e][1,2,4]triazine-5,7-diones, processes for preparing them and their use 有权
标题翻译：嘧啶并[5,4-e] [1,2,4]三嗪-5,7-二酮，其制备方法及其应用
公开(公告)号：US20080032984A1
公开(公告)日：2008-02-07
申请号：US11770106
申请日：2007-06-28
申请人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller
发明人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller
IPC分类号： A61K31/53 , A61P3/10 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives. The invention therefore relates to compounds of the formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are suitable for use as antidiabetics, for example.
摘要翻译：本发明涉及嘧啶并[5,4-e] [1,2,4]三嗪-5,7-二酮，其药用盐和生理功能衍生物。因此，本发明涉及式I化合物，其中基团具有给定的含义，以及它们的生理上耐受的盐及其制备方法。该化合物例如适用于抗糖尿病药。

28. 发明申请

US20070191441A1 DIPHENYLAMINE-SUBSTITUTED SALICYLTHIAZOLE DERIVATIVES AND RELATED COMPOUNDS AS PHOSPHOTYROSINE PHOSPHATASE 1B (PTB1B) INHIBITORS FOR USING AS BLOOD-SUGAR DECREASING ACTIVE INGREDIENTS FOR TREATING DIABETES 有权
标题翻译：二苯胺取代的三甲基噻唑衍生物及相关化合物作为磷酸二氢吡啶磷酸酯1B（PTB1B）抑制剂，用于治疗糖尿病的血糖减少活性成分
公开(公告)号：US20070191441A1
公开(公告)日：2007-08-16
申请号：US11609463
申请日：2006-12-12
申请人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller , Reinhard Kirsch
发明人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller , Reinhard Kirsch
IPC分类号： A61K31/426
CPC分类号： C07D277/42 , C07D277/46
摘要： The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood glucose levels.
摘要翻译：因此，本发明涉及式I化合物，其中变量如说明书中所定义，含有它们的药物组合物及其用于治疗降低血糖水平的用途。

29. 发明授权

US07208504B2 Bicyclic inhibitors of hormone sensitive lipase 有权
标题翻译：激素敏感脂肪酶双环抑制剂
公开(公告)号：US07208504B2
公开(公告)日：2007-04-24
申请号：US10685199
申请日：2003-10-14
申请人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller , Hubert Heuer
发明人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller , Hubert Heuer
IPC分类号： A61K31/445 , A61K31/4192 , C07D211/14 , C07D249/18
CPC分类号： C07D401/06 , C07D249/18 , C07D403/06 , C07D471/10
摘要： Benzotriazoles of formula I in which R1 to R8 have the abovementioned meanings and process for their preparation are described. The compounds show an inhibitory effect on hormone-sensitive lipase.
摘要翻译：描述其中R1至R8具有上述含义的式I的苯并三唑及其制备方法。这些化合物对激素敏感性脂肪酶具有抑制作用。

30. 发明申请

US20050197348A1 Indazole derivatives as inhibitors of hormone sensitive lipase 有权
标题翻译：吲唑衍生物作为激素敏感性脂肪酶的抑制剂
公开(公告)号：US20050197348A1
公开(公告)日：2005-09-08
申请号：US11042565
申请日：2005-01-25
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Karl-Heinz Baringhaus
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Karl-Heinz Baringhaus
IPC分类号： A61K31/416 , C07D231/56 , A61K31/519 , A61K31/454 , A61K31/4745 , C07D471/02 , C07D487/02
CPC分类号： C07D413/12 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D495/04
摘要： The present invention relates to indazole derivatives of the general formulae I or II having the meanings indicated in the description, to the pharmaceutically useful salts thereof and the use thereof as drugs.
摘要翻译：本发明涉及具有本说明书中所述含义的通式I或II的吲唑衍生物及其药学上可用的盐及其作为药物的用途。

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