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1. 发明申请

US20040266768A1 Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use 有权
标题翻译：取代的苯甲酰脲基吡啶基哌啶和吡咯烷羧酸衍生物，其制备方法及其应用
公开(公告)号：US20040266768A1
公开(公告)日：2004-12-30
申请号：US10795863
申请日：2004-03-08
申请人： Aventis Pharma Deutschland GmbH
发明人： Karl Schoenafinger , Dieter Kadereit , Elisabeth Defossa , Andreas Herling , Thomas Klabunde
IPC分类号： C07D43/04 , C07D41/04 , A61K031/505 , A61K031/501
CPC分类号： C07D401/04
摘要： The invention relates to compounds of the formula I 1 where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.
摘要翻译：本发明涉及式Ⅰ化合物，其中基团如所定义，及其生理上耐受的盐。该化合物例如可用作预防和治疗2型糖尿病的药物。

2. 发明申请

US20040259927A1 Novel substituted 2-aminoimidazoles, process for their preparation, their use as medicament or diagnostic aid 失效
标题翻译：新型取代的2-氨基咪唑，其制备方法，用作药物或诊断辅助剂
公开(公告)号：US20040259927A1
公开(公告)日：2004-12-23
申请号：US10771185
申请日：2004-02-03
申请人： Aventis Pharma Deutschland GmbH
发明人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Hans-Willi Jansen
IPC分类号： C07D233/66 , A61K031/4164
CPC分类号： C07D233/50
摘要： Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed inter alia for renal disorders such as acute or chronic renal failure, for disorders of biliary function, for respiratory disorders such as snoring or sleep apneas or for stroke. 1
摘要翻译：式I的新型取代的2-氨基咪唑，其制备方法，它们作为药物或诊断助剂的用途以及含有它们的药物。这种类型的化合物可用于预防或治疗各种疾病，并且可以特别用于肾脏疾病如急性或慢性肾衰竭，胆汁功能障碍，呼吸障碍如打鼾或睡眠呼吸暂停或中风。

3. 发明申请

US20040225109A1 Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides 有权
标题翻译：制备乙酰基 - 脒基苯丙氨酰 - 环己基甘氨酰 - 吡啶并氨酰胺的方法
公开(公告)号：US20040225109A1
公开(公告)日：2004-11-11
申请号：US10869076
申请日：2004-06-17
申请人： Aventis Pharma Deutschland GmbH
发明人： Gerhard Breipohl , Wolfgang Holla , Heiner Jendralla , Gerhard Beck
IPC分类号： C07K005/06
CPC分类号： C07K5/0821 , C07K5/06139
摘要： The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, 1 in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-null2-acetylamino-3-(4-amidinophenyl)propionylaminonull-2-cyclohexylacetic acid, which is obtained from 2-null2-acetylamino-3-(4-cyanophenyl)acryloylaminonull-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.
摘要翻译：本发明涉及一种制备式I的乙酰基 - 脒基苯脒基 - 环己基甘氨酰 - 吡啶并吡喃酰胺的方法，其中阴离子X是生理上可接受的阴离子，以及它们的类似物，它们是凝血因子Xa的有效抑制剂，可用于例如用于预防血栓形成。根据本发明的方法包括2- [2-乙酰氨基-3-（4-脒基苯基）丙酰基氨基] -2-环己基乙酸的偶联，其由2- [2-乙酰氨基-3-（4-氰基苯基）丙烯酰氨基] -2-环己基乙酸，通过不对称氢化，并将氰基转化为脒或其盐与3-（2-氨基-2-氨基甲酰基乙基）-1-甲基吡啶鎓盐或其盐。本发明还提供了该方法的起始原料和中间体，其制备方法和乙酰基 - （S）-4-脒基苯基丙氨酰 - （S） - 环己基甘氨酰 - （S） - （1-甲基-3-吡啶鎓）丙烯酰胺作为二甲苯磺酸盐。

4. 发明申请

US20040209920A1 Arylcycloalkyl-substituted alkanoic acid derivatives, processes for their preparation and their use as pharmaceuticals 有权
标题翻译：芳基环烷基取代的链烷酸衍生物，其制备方法及其作为药物的用途
公开(公告)号：US20040209920A1
公开(公告)日：2004-10-21
申请号：US10789017
申请日：2004-02-27
申请人： Aventis Pharma Deutschland GmbH
发明人： Christian Stapper , Stefanie Keil , Heiner Glombik , Eugen Falk , Jochen Goerlitzer , Dirk Gretzke , Hans-Ludwig Schaefer , Wolfgang Wendler
IPC分类号： A61K031/4439 , A61K031/422 , C07D413/02
CPC分类号： C07D263/32 , C07D413/02
摘要： Arylcycloalkyl-substituted alkanoic acid derivatives, processes for their preparation and their use as pharmaceuticals The invention relates to arylcycloalkyl-substituted alkanoic acid derivatives and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, 1 in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for the treatment and/or prevention of disorders of the fatty acid metabolism and glucose utilization disorders and also disorders in which insulin resistance is involved.
摘要翻译：芳基环烷基取代的链烷酸衍生物，其制备方法及其作为药物的用途本发明涉及芳基环烷基取代的链烷酸衍生物及其生理上可接受的盐和生理功能衍生物。描述的是式I化合物，其中基团如所定义，以及它们的生理上可接受的盐及其制备方法。该化合物例如适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病。

5. 发明申请

US20040209868A1 Substituted indoles 审中-公开
标题翻译：取代的吲哚
公开(公告)号：US20040209868A1
公开(公告)日：2004-10-21
申请号：US10842427
申请日：2004-05-11
申请人： Aventis Pharma Deutschland GmbH
发明人： Olaf Ritzeler , Hans Ulrich Stilz , Bernhard Neises , Gerhard Jaehne , Jorg Habermann
IPC分类号： A61K031/55 , A61K031/454 , A61K031/405 , C07D43/02
CPC分类号： C07D401/04 , C07D209/08 , C07D401/14
摘要： Compounds of the formula I 1 are suitable for preparing pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFnullB is involved.
摘要翻译：式I化合物适用于制备用于预防和治疗其中涉及NFκB活性升高的病症的药物。

6. 发明申请

US20040198742A1 Substituted 3-(benzoylureido) thiophene derivatives, processes for preparing them and their use 有权
标题翻译：取代的3-（苯甲酰基脲基）噻吩衍生物，其制备方法及其应用
公开(公告)号：US20040198742A1
公开(公告)日：2004-10-07
申请号：US10780344
申请日：2004-02-17
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： Karl Schoenafinger , Elisabeth Defossa , Erich Von Roedern , Dieter Kadereit , Andreas Herling , Hans-Joerg Burger , Thomas Klabunde , Karl-Ulrich Wendt
IPC分类号： C07D333/42 , A61K031/496 , A61K031/453 , A61K031/381
CPC分类号： C07D409/04 , C07D333/36 , C07D333/38 , C07D333/44 , C07D413/04
摘要： Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their use The invention relates to compounds of the formula I 1 where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.
摘要翻译：取代的3-（苯甲酰基脲基）噻吩衍生物，其制备方法及其应用本发明涉及式Ⅰ化合物，其中基团如所定义，及其生理上耐受的盐。该化合物例如可用作预防和治疗2型糖尿病的药物。

7. 发明申请

US20040127484A1 Novel bicyclic inhibitors of hormone sensitive lipase 有权
标题翻译：新型双环抑制剂激素敏感性脂肪酶
公开(公告)号：US20040127484A1
公开(公告)日：2004-07-01
申请号：US10685199
申请日：2003-10-14
申请人： Aventis Pharma Deutschland GmbH
发明人： Stefan Petry , Karl-Heinz Baringhaus , Norbert Tennagels , Guenter Mueller , Hubert Heuer
IPC分类号： A61K031/55 , C07D43/02 , A61K031/454 , A61K031/4192
CPC分类号： C07D401/06 , C07D249/18 , C07D403/06 , C07D471/10
摘要： Benzotriazoles of formula I 1 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。

8. 发明申请

US20040116494A1 Use of IkappaB-kinase inhibitors in pain therapy 有权
标题翻译： IkappaB激酶抑制剂在疼痛治疗中的应用
公开(公告)号：US20040116494A1
公开(公告)日：2004-06-17
申请号：US10642974
申请日：2003-08-18
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： Martin Michaelis , Olaf Ritzeler , Gerhard Jaehne , Karl Rudolphi , Gerd Geisslinger , Hans-Georg Schaible
IPC分类号： A61K031/4184
CPC分类号： A61K31/404 , A61K31/4184 , A61K31/4245 , A61K31/444
摘要： The present invention relates to the use of InullB-kinase Inhibitors and methods for the prophylaxis and therapy for treating pain comprising administering such compounds.
摘要翻译：本发明涉及IkappaB激酶抑制剂的用途和用于预防和治疗疼痛的方法，包括施用这些化合物。

9. 发明申请

US20040110808A1 Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的杂芳族化合物及其作为药物的用途
公开(公告)号：US20040110808A1
公开(公告)日：2004-06-10
申请号：US10634979
申请日：2003-08-05
申请人： Aventis Pharma Deutschland GmbH
发明人： Hartmut Strobel , Paulus Wohlfart , Peter Below
IPC分类号： A61K031/428 , A61K031/423 , A61K031/4184
CPC分类号： C07D215/38 , C07D235/30 , C07D263/58 , C07D277/82 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to acylamino-substituted heteroaromatic compounds of formula I, 1 wherein R1, R2, R3, R4 and R5 and X are as defined herein, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.
摘要翻译：本发明涉及式I的酰基氨基取代的杂芳族化合物，其中R 1，R 2，R 3，R 4和R 5和X如本文所定义，这种化合物，用于刺激内皮NO合成酶表达的方法，以及包括施用这些化合物的治疗方法。

10. 发明申请

US20040042981A1 Polyenecarboxylic acid derivatives, processes for preparing them, and their use 有权
标题翻译：聚烯酸衍生物，其制备方法及其应用
公开(公告)号：US20040042981A1
公开(公告)日：2004-03-04
申请号：US10608466
申请日：2003-06-27
申请人： Aventis Pharma Deutschland GmbH
发明人： Laszlo Vertesy , Michael Kurz , Joachim Wink
IPC分类号： A61K007/42 , C07C323/22 , C07C235/84
CPC分类号： C12R1/01 , C07C57/42 , C07C59/48 , C12P7/42 , C12P7/44 , C12P7/62
摘要： The present invention relates to novel compounds, termed serpentemycins, of the formula (I) 1 in which Y, R, R2, R3, R4, X, X2, X3, n, m and o are as defined in the specification, which are formed by the microorganism Actinomycetales sp. DSM 14865 during its fermentation, to chemical derivatives of the serpentemycins, to a process for preparing them, and to their use as pharmaceuticals, in particular for the treatment and prophylaxis of infectious bacterial diseases.
摘要翻译：本发明涉及其中Y，R，R2，R3，R4，X，X2，X3，n，m和o如说明书中所定义的式（I）的新化合物，称为蛇血霉素，其形成由微生物放线菌属 DSM 14865在其发酵过程中，涉及蛇血霉素的化学衍生物，其制备方法及其用作药物，特别是用于治疗和预防感染性细菌性疾病。

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