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1. 发明授权

US06566525B1 Preparation of N-substituted-hydroxycycloalkylamine derivatives 失效
标题翻译： N-取代羟基环烷基胺衍生物的制备
公开(公告)号：US06566525B1
公开(公告)日：2003-05-20
申请号：US09787202
申请日：2001-04-07
申请人： Seong Jin Kim , Keon Il Kim , Kyoung Youl Yang
发明人： Seong Jin Kim , Keon Il Kim , Kyoung Youl Yang
IPC分类号： C07D21142
CPC分类号： C07D207/12 , C07D211/22 , C07D211/42 , Y02P20/55
摘要： A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives, that are useful intermediates for the synthesis of various organic chemicals including pharmaceutical and agrochemical compounds, represented by formula (1), by reacting a 1,2-dihydroxalkyl alcohol, represented by the following formula (2), with a thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by the following formula (3); and then cyclizing that intermediate with an amine compounds represented by the following formula (4). In the above structural formuli, * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; m is an integer of 1-3; and X is halogen. The reactant compounds as well as the compounds made according to this invention have the following substitution pattern: n=1, R2=OH, R3=H and m=1; n=1, R2=H, R3=CH2OH and m=2; n=2, R2=OH, R3=H; and m=2; and n=2, R2=H, R3=CH2OH and m=3.
摘要翻译：一种制备N-取代羟基环烷基胺衍生物的方法，其为由式（1）表示的用于合成包括药物和农药化合物在内的各种有机化学品的有用的中间体，通过使由（2）表示的亚硫酰卤，得到下式（3）表示的中间体1,2-环丙烷基烷基卤化物。然后用下式（4）表示的胺化合物环化该中间体。在上述结构式中，*表示不对称碳原子; R1是氢或氨基保护基; m为1-3的整数; X为卤素。反应物化合物以及根据本发明制备的化合物具有以下取代模式：n = 1，R 2 = OH，R 3 = H且m = 1; n = 1，R2 = H，R3 = CH2OH，m = 2; n = 2，R2 = OH，R3 = H; m = 2; n = 2，R2 = H，R3 = CH2OH，m = 3。

2. 发明授权

US06376672B1 Naphthalenylmethoxypiperidines as renin inhibitors 失效
标题翻译：萘基哌啶作为肾素抑制剂
公开(公告)号：US06376672B1
公开(公告)日：2002-04-23
申请号：US09542303
申请日：2000-04-04
申请人： Volker Breu , Hans-Peter Märki , Eric Vieira , Wolfgang Wostl
发明人： Volker Breu , Hans-Peter Märki , Eric Vieira , Wolfgang Wostl
IPC分类号： C07D21142
CPC分类号： C07D231/12 , C07D211/42 , C07D233/56 , C07D249/08
摘要： The present invention relates to compound of formula (I) wherein R1, R2 and R3 are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2和R 3如说明书和权利要求及其药学上可接受的盐所定义。这些化合物可用于治疗与再狭窄，青光眼，心肌梗塞，高血压和终末器官损害相关的疾病，例如，心功能不全和肾功能不全。

3. 发明授权

US06673931B2 Naphthalenyl piperidines as renin inhibitors 失效
标题翻译：萘基哌啶作为肾素抑制剂
公开(公告)号：US06673931B2
公开(公告)日：2004-01-06
申请号：US10023679
申请日：2001-12-18
申请人： Volker Breu , Hans-Peter Märki , Eric Vieira , Wolfgang Wostl
发明人： Volker Breu , Hans-Peter Märki , Eric Vieira , Wolfgang Wostl
IPC分类号： C07D21142
CPC分类号： C07D231/12 , C07D211/42 , C07D233/56 , C07D249/08
摘要： Piperidine derivatives, their manufacture and use as medicaments is described. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.
摘要翻译：描述了哌啶衍生物，其作为药物的制造和用途。这些化合物可用于治疗与再狭窄，青光眼，心肌梗塞，高血压和终末器官损害相关的疾病，例如，心功能不全和肾功能不全。

4. 发明授权

US06407235B1 Prodrug acid esters of [2-(4-benzyl-3-hydroxy-piperidin-1-yl)-ethansulfonyl]phenol 有权
标题翻译： [2-（4-苄基-3-羟基 - 哌啶-1-基） - 乙二磺酰基]苯酚的前药酸酯
公开(公告)号：US06407235B1
公开(公告)日：2002-06-18
申请号：US09931431
申请日：2001-08-16
申请人： Alexander Alanine , Bernd Buettelmann , Holger Fischer , Marie-Paule Heitz Neidhart , Joerg Huwyler , Georg Jaeschke , Emmanuel Pinard , René Wyler
发明人： Alexander Alanine , Bernd Buettelmann , Holger Fischer , Marie-Paule Heitz Neidhart , Joerg Huwyler , Georg Jaeschke , Emmanuel Pinard , René Wyler
IPC分类号： C07D21142
CPC分类号： C07D211/42 , C07F9/59
摘要： The invention is a compound of the formula wherein R is a) —C(O)(CH2)nC(O)OH, b) wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl, c) —P(O)(OH)2, or is d) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); and R2/R3 are hydrogen or lower alkyl; n is 1, 2, 3 or 4; or a pharmaceutically acceptable acid addition salt thereof
摘要翻译：本发明是式（I）-C（O）（CH 2）n C（O）OH，b）其中R 1是-N（R 2）（R 3）的化合物，或者是五或六元芳族或非芳香族的化合物 c）-P（O）（OH）2或isd）-C（O）（CH 2）n NHC（O）（O）（O） CH2）nN（R2）（R3）; 和R2 / R3是氢或低级烷基; n是1,2,3或4;或其药学上可接受的酸加成盐

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