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1. 发明授权

US06407106B1 N-triazolylmethyl-piperazine compounds with neurokinin-receptor antagonist activity 有权
标题翻译： N-三唑基甲基 - 哌嗪化合物与神经激肽受体拮抗剂活性
公开(公告)号：US06407106B1
公开(公告)日：2002-06-18
申请号：US09915558
申请日：2001-07-27
申请人： Daniel Jasserand , Uwe Schoen , Holger Sann , Reinhard Brueckner , Christian Eeckhout
发明人： Daniel Jasserand , Uwe Schoen , Holger Sann , Reinhard Brueckner , Christian Eeckhout
IPC分类号： A61K315377
CPC分类号： C07D403/06 , C07D403/14
摘要： N-triazolylmethyl-piperazine compounds which exhibit neurokinin receptor antagonistic activity corresponding to the formula I: wherein R1, R2 and R3 have the meanings given in the specification; pharmaceutical compositions containing these compounds; a process for preparing these compounds, and intermediate products of this process.
摘要翻译：表现出对应于式I的神经激肽受体拮抗活性的N-三唑基甲基 - 哌嗪化合物：其中R1，R2和R3具有说明书中给出的含义; 含有这些化合物的药物组合物; 制备这些化合物的方法，以及该方法的中间产物。

2. 发明授权

US06770649B2 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds, process for their preparation and pharmaceutical compositions containing them 有权
标题翻译： 1- [1-（杂）芳基-1-全羟基烷基甲基] - 哌嗪化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06770649B2
公开(公告)日：2004-08-03
申请号：US10242678
申请日：2002-09-13
申请人： Daniel Jasserand , Ulf Preuschoff , Jochen Antel , Samuel David , Holger Sann , Reinhard Brueckner , Dania Reiche , Christian Eeckhout
发明人： Daniel Jasserand , Ulf Preuschoff , Jochen Antel , Samuel David , Holger Sann , Reinhard Brueckner , Dania Reiche , Christian Eeckhout
IPC分类号： C07D33320
CPC分类号： C07D295/092 , C07D307/52 , C07D333/20 , C07D407/04
摘要： Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R6, R7, A and Z have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as a process for the preparation of such compounds and intermediate products of this process.
摘要翻译：对通式I所示的对速激肽受体具有拮抗作用的新型1- [1-（杂）芳基-1-全羟基烷基甲基] - 哌嗪化合物，其中R 6，R 7，A和Z具有描述和含有这些化合物的药物组合物，以及这种化合物的制备方法和该方法的中间产物。

3. 发明授权

US06001833A Urea derivatives 有权
标题翻译：尿素衍生物
公开(公告)号：US06001833A
公开(公告)日：1999-12-14
申请号：US141623
申请日：1998-08-27
申请人： Daniel Jasserand , Samuel David , Jochen Antel , Reinhard Brueckner , Christian Eeckhout , Gerhard-Wilhelm Bielenberg
发明人： Daniel Jasserand , Samuel David , Jochen Antel , Reinhard Brueckner , Christian Eeckhout , Gerhard-Wilhelm Bielenberg
IPC分类号： C07D403/06 , A61K31/495 , A61K31/496 , A61P1/00 , A61P29/00 , A61P43/00 , C07D209/00 , C07D209/14 , C07D241/00 , A61K31/47
CPC分类号： C07D209/14 , Y02P20/55
摘要： Compounds of Formula I ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen or halogen andR.sup.3 is hydrogen or lower alkoxy,and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds. Pharmaceutical composition containing these compounds are suitable, for example, for treating functional and inflammatory disorders of the gastrointestinal tract.
摘要翻译：式Ⅰ化合物，其中R 1是氢或低级烷基，R 2是氢或卤素，R 3是氢或低级烷氧基，以及它们的药学上可接受的酸加成盐和含有这些化合物的药物组合物，以及制备这些化合物的方法。含有这些化合物的药物组合物适用于例如治疗胃肠道的功能性和炎症性疾病。

4. 发明授权

US06300336B1 Method of treating or inhibiting functional disturbances or illnesses of the lower intestinal tracts, particularly abdominal visceral pain which accompanies them 有权
标题翻译：治疗或抑制下肠道功能障碍或疾病的方法，特别是伴随其的腹部内脏痛
公开(公告)号：US06300336B1
公开(公告)日：2001-10-09
申请号：US09525896
申请日：2000-03-15
申请人： Christian Eeckhout , Holger Sann
发明人： Christian Eeckhout , Holger Sann
IPC分类号： A61K31505
CPC分类号： A61K31/506
摘要： The use of moxonidine or a physiologically compatible acid addition salt thereof for the treatment and/or inhibition of functional gastrointestinal disturbances or illnesses in the region of the lower intestinal tracts, particularly for the treatment and/or inhibition of abdominal visceral pain which accompanies them, and the preparation of pharmaceutical compositions suitable for this treatment are is described. The functional disturbances and illnesses of the lower intestinal tracts which can be treated according to the invention are known in particular as irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), which generally also include visceral pain as one of their symptoms.
摘要翻译：莫西尼定或其生理上相容的酸加成盐用于治疗和/或抑制下肠道区域功能性胃肠道紊乱或疾病，特别是用于治疗和/或抑制伴随其的腹部内脏痛，并描述了适用于该处理的药物组合物的制备。根据本发明可以治疗的下肠道的功能紊乱和疾病特别是已知的肠易激综合征（IBS）和炎症性肠病（IBD），其通常还包括作为其症状之一的内脏痛。

5. 发明授权

US6040303A 7-phenyl-1, 4-diazepane compounds, process for their preparation, and pharmaceutical compositions containing them 有权
标题翻译： 7-苯基-1,4-二氮杂环丁烷化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US6040303A
公开(公告)日：2000-03-21
申请号：US141312
申请日：1998-08-27
申请人： Samuel David , Jochen Antel , Reinhard Brueckner , Dieter Ziegler , Christian Eeckhout , Gerhard-Wilhelm Bielenberg , Michael Peck
发明人： Samuel David , Jochen Antel , Reinhard Brueckner , Dieter Ziegler , Christian Eeckhout , Gerhard-Wilhelm Bielenberg , Michael Peck
IPC分类号： A61K31/55 , A61P1/00 , A61P43/00 , C07D243/08
CPC分类号： C07D243/08 , Y02P20/55
摘要： Neurokinin-antagonistic compounds corresponding to formula I: ##STR1## in which R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.2 and R.sup.3 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.4 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.5 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.4 and R.sup.5 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.6 is lower alkyl, halogen or trifluoromethyl,R.sup.7 is lower alkyl, halogen or trifluoromethyl,A is a --(CH.sub.2).sub.n -- group in which n represents an integer from 1 to 3, or an --NH--(CH.sub.2).sub.m -- group in which m represents an integer from 2 to 3, andB is an alkylene chain with 1 to 3 carbon atoms optionally substituted by lower alkyl,and physiologically acceptable salts thereof and processes for the preparation of these compounds.
摘要翻译：对应于式I的神经激肽拮抗化合物：其中R1是氢或低级烷基，R2是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R3是氢，低级烷基，低级烷氧基，卤素或三氟甲基，或R2和 R3一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R4是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R5是氢，低级烷基，低级烷氧基，卤素或三氟甲基，或R4和R5一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R6是低级烷基，卤素或三氟甲基，R7是低级烷基，卤素或三氟甲基，A是 - （CH2）n - 其中n表示1至3的整数的基团，或其中m表示2至3的整数的-NH-（CH 2）m - 基团，B是具有1至3个碳原子的亚烷基链，其任选被低级烷基和其生理上可接受的盐 d制备这些化合物的方法。

6. 发明授权

US6165985A 11-acetyl-12,13-dioxabicyclo[8.2.1]-tridecenone derivatives, processes for their preparation and pharmaceutical compositions comprising them 有权
标题翻译： 11-乙酰基-12,13-二氧杂二环[8.2.1] - 十一内酯衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：US6165985A
公开(公告)日：2000-12-26
申请号：US338602
申请日：1999-06-23
申请人： Daniel Jasserand , Ulf Preuschoff , Christian Eeckhout
发明人： Daniel Jasserand , Ulf Preuschoff , Christian Eeckhout
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： Ring-contracted N-demethyl-N-isopropyl-erythromycin-A derivatives having a modified side chain and gastrointestinally effective motilin-agonistic properties and the preparation thereof are described.
摘要翻译：描述具有改性侧链和胃肠道有效的促胃动素激动性质的收缩N-去甲基-N-异丙基 - 红霉素-A衍生物及其制备。

7. 发明授权

US5418224A 4,13-dioxabicyclo[8.2.1]tridecenone compounds and pharmaceutical compositions containing them 失效
标题翻译： 4,13-二氧杂双环[8.2.1]十三酮化合物和含有它们的药物组合物
公开(公告)号：US5418224A
公开(公告)日：1995-05-23
申请号：US996083
申请日：1992-12-23
申请人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout
发明人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/14 , A61P43/00 , C07H17/08
CPC分类号： C07H17/08
摘要： Ring-contracted N-demethyl-N-isopropylerythromycin A derivatives with gastrointestinally effective motilin-agonistic properties, a method for preparing such compounds, and pharmaceutical compositions containing them.
摘要翻译：具有胃肠道有效的胃动素激动性的收缩N-去甲基-N-异丙基红霉素A衍生物，制备这些化合物的方法和含有它们的药物组合物。

8. 发明授权

US5912235A 10, 13, 15-trioxatricyclo �9.2.1.1..sup.9.6 !-pentadecan one derivatives, method for their production and pharmaceutical compositions containing them 失效
标题翻译： 10,13,15-三氧杂三环[9.2.1.1.9.6] - 十五烷一种衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5912235A
公开(公告)日：1999-06-15
申请号：US954891
申请日：1997-10-21
申请人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout , Emil Finner
发明人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout , Emil Finner
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/06 , A61P43/00 , C07H17/08 , C07H1/00
CPC分类号： C07H17/08
摘要： Ring-contracted N-demethyl-N-isopropyl-erythromycin-A-spiroacetal compounds corresponding to formula I ##STR1## having gastrointestinally effective motilin-agonistic properties and the preparation thereof.
摘要翻译：对应于具有胃肠道有效的胃动素激动性质的式I的收缩N-去甲基-N-异丙基 - 红霉素A-螺旋缩醛化合物及其制备。

9. 发明授权

US5438068A Method of treating colon disturbances with pharmaceutical compositions containing imidazol-1-yl compounds 失效
标题翻译：用含有咪唑-1-基化合物的药物组合物治疗结肠紊乱的方法
公开(公告)号：US5438068A
公开(公告)日：1995-08-01
申请号：US145164
申请日：1993-11-03
申请人： Christian Eeckhout , Ulf Preuschoff , Samuel David
发明人： Christian Eeckhout , Ulf Preuschoff , Samuel David
IPC分类号： A61K31/4184 , A61K31/415 , A61K31/4164 , A61K31/437 , A61K31/44 , A61K31/47 , A61P1/00 , A61P1/14 , C07D233/96 , C07D403/06
CPC分类号： A61K31/415 , A61K31/44
摘要： Use of imidazol-1-yl compounds of the general formula I ##STR1## wherein R.sup.1 denotes lower alkyl or hydrogen;m represents 2 or 3, andn represents 2 or 3;or a physiologically acceptable acid addition salt thereof for treating functional disturbances of the lower intestinal tract in larger mammals and humans associated with increased pain sensitivity and/or anomalies in stool passage in the colon region.
摘要翻译：使用通式I的咪唑-1-基化合物其中R 1表示低级烷基或氢; m表示2或3，n表示2或3; 或其生理上可接受的酸加成盐，用于治疗较大的哺乳动物和人类的下肠道的功能障碍，其与结肠区域的粪便通过增加的疼痛敏感性和/或异常相关。

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