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1. 发明授权

US06815549B2 Process for the preparation of 4-[1-hydroxy -4-[4-(hydroxydiphenylmethly)-1-piperidinyl]-butyl]-&agr;, &agr;-dimethylbenzeneacetic acid 失效
标题翻译：制备4- [1-羟基-4- [4-（羟基二苯基甲基）-1-哌啶基] - 丁基]-α，α-二甲基苯乙酸的方法
公开(公告)号：US06815549B2
公开(公告)日：2004-11-09
申请号：US10145765
申请日：2002-05-16
申请人： Graziano Castaldi , Giuseppe Barreca , Domenico Magrone
发明人： Graziano Castaldi , Giuseppe Barreca , Domenico Magrone
IPC分类号： C07D21134
CPC分类号： C07D211/22
摘要： A process for the preparation of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-&agr;,&agr;-dimethylbenzeneacetic acid (Fexofenadine) of formula
摘要翻译：制备式（I）的4- [1-羟基-4- [4-（羟基二苯基甲基）-1-哌啶基] - 丁基]-α，α-二甲基苯乙酸（非索非那定）

2. 发明授权

US06503905B1 3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives 失效
标题翻译： 3,3'-联芳基哌啶和2,2-二芳基吗啉衍生物
公开(公告)号：US06503905B1
公开(公告)日：2003-01-07
申请号：US09369841
申请日：1999-08-06
申请人： Spiros Liras , Martin P. Allen , Barbara E. Segelstein
发明人： Spiros Liras , Martin P. Allen , Barbara E. Segelstein
IPC分类号： C07D21134
CPC分类号： C07D265/30 , C07D211/20 , C07D211/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/06
摘要： The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.
摘要翻译：本发明涉及式I化合物，其中Z 1，Z 2，X，Q，R 1，R 2和R 3如说明书中所定义，含有这些化合物的药物组合物使用这些化合物来治疗神经和胃肠道疾病。

3. 发明授权

US06452011B1 Process for production of piperidine derivatives 有权
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06452011B1
公开(公告)日：2002-09-17
申请号：US09634169
申请日：2000-08-09
申请人： Thomas E. D'Ambra , Garry M. Pilling
发明人： Thomas E. D'Ambra , Garry M. Pilling
IPC分类号： C07D21134
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译：本发明涉及通过用哌啶化合物转化具有下式的区域异构体来制备哌啶衍生物化合物的方法：其中Z为异或其中m为1或4-6; Q和Y相同或不同，选自O，S和NR5; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。

4. 发明授权

US06201124B1 Process for production of piperidine derivatives 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06201124B1
公开(公告)日：2001-03-13
申请号：US08575344
申请日：1995-12-21
申请人： Thomas E. D'Ambra , Garry M. Pilling
发明人： Thomas E. D'Ambra , Garry M. Pilling
IPC分类号： C07D21134
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: and where m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译：本发明涉及通过用哌啶化合物转化具有下式的区域异构体制备哌啶衍生物化合物的方法：其中m为1至6的整数; Q和Y相同或不同，选自O，S和NR5; G1，G2和G3相同或不同，选自OR8，SR8和NR8R9; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。

5. 发明授权

US06613906B1 Crystal modification 失效
公开(公告)号：US06613906B1
公开(公告)日：2003-09-02
申请号：US09588391
申请日：2000-06-06
申请人： Julian Anthony Davies , James E. Gano
发明人： Julian Anthony Davies , James E. Gano
IPC分类号： C07D21134
CPC分类号： C07D211/22 , C07D211/34
摘要： A novel crystal form of ,&agr;-dimethyl-4-{1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}butyl}benzeneacetic acid hydrochloride, processes for its preparation and its pharmaceutical use are disclosed.

6. 发明授权

US06458958B1 Process for production of piperidine derivatives 有权
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06458958B1
公开(公告)日：2002-10-01
申请号：US09637127
申请日：2000-08-09
申请人： Thomas E. D'Ambra , Garry M. Pilling
发明人： Thomas E. D'Ambra , Garry M. Pilling
IPC分类号： C07D21134
CPC分类号： C07D211/22 , C07D211/14 , C07D211/20 , C07D211/46
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG1G2G3; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; and R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.
摘要翻译：本发明涉及一种通过用哌啶化合物转化具有下式的区域异构体制备哌啶衍生物化合物的方法：其中Z为-CG1G2G3; G1，G2和G3相同或不同，选自OR8，SR8和NR8R9; 并且R 8和R 9相同或不同，并且选自氢，烷基部分和芳基部分。

7. 发明授权

US06444824B1 Process for production of piperidine derivatives 有权
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06444824B1
公开(公告)日：2002-09-03
申请号：US09634983
申请日：2000-08-09
申请人： Thomas E. D'Ambra , Garry M. Pilling
发明人： Thomas E. D'Ambra , Garry M. Pilling
IPC分类号： C07D21134
CPC分类号： C07D211/22 , C07D211/14 , C07D211/20 , C07D211/46
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.
摘要翻译：本发明涉及通过用哌啶化合物转化具有下式的区域异构体来制备哌啶衍生物化合物的方法：其中Z是并且其中m是1或3-6; Q和Y相同或不同，选自O，S和NR5; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; 并且R 5，R 8和R 9相同或不同，并且选自氢，烷基部分和芳基部分。

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