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1. 再颁专利

USRE41425E1 Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：USRE41425E1
公开(公告)日：2010-07-06
申请号：US12081710
申请日：2008-04-18
申请人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： C07D295/12 , A61K31/496
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
摘要： A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line represents a single bond when Z is nitrogen, and represents a single or double bond when Z is carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, are disclosed.
摘要翻译：一组具有有趣的药理学性质的新的哌嗪和哌啶化合物，其具有式（a）其中A表示具有5-7个环原子的杂环基，其中存在1-3个选自O，N和S的杂原子，R 1 是氢或氟，R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2，Z表示碳或氮，当Z是氮时，虚线表示单键并且当Z是碳时表示单键或双键，R 3和R 4独立地是氢或C 1-4 - 烷基，n具有1或2，R 5是2-吡啶基，3-吡啶基或4-吡啶基相对于具有基团Y的亚甲基桥的间位，并且任选地被（R 6）q取代，Y是苯基，呋喃基或噻吩基，该基团可以被1-3个取代基取代，羟基，卤素， CF 3，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基氨基羰基，单 - 或二-C 1-4 - 烷基氨基羰基，R 6是卤素，羟基， C 1-4 - 烷氧基或C 1-4 - 烷基，q为0,1,2或3及其盐。

2. 发明授权

US6090812A Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US6090812A
公开(公告)日：2000-07-18
申请号：US158520
申请日：1998-09-22
申请人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D295/12
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
摘要： A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) ##STR1## wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and S are present,R.sub.1 is hydrogen or fluoro,R.sub.2 is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or an oxo group, and p is 0, 1 or 2,Z represents carbon or nitrogen, and the dotted line represents a single bond when Z is nitrogen, and represents a single or double bond when Z is carbon,R.sub.3 and R.sub.4 independently are hydrogen or C.sub.1-4 -alkyl,n has the value 1 or 2,R.sub.5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R.sub.6)q,Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF.sub.3, C.sub.1-4 -alkoxy, C.sub.1-4 -alkyl, cyano aminocarbonyl, mono- or di-C.sub.1-4 -alkylaminocarbonyl,R.sub.6 is halogen, hydroxy, C.sub.1-4 -alkoxy or C.sub.1-4 -alkyl, and q is 0, 1, 2 or 3 and salts thereof, are disclosed.
摘要翻译：一组具有有趣的药理学性质的新的哌嗪和哌啶化合物，其具有式（a）其中A表示具有5-7个环原子的杂环基，其中存在1-3个选自O，N和S的杂原子，R 1 是氢或氟，R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2，Z表示碳或氮，当Z是氮时，虚线表示单键并且当Z是碳时表示单键或双键，R 3和R 4独立地是氢或C 1-4 - 烷基，n具有数值1或2，R 5是2-吡啶基，3-吡啶基或4-吡啶基相对于具有基团Y的亚甲基桥的间位，并且任选地被（R 6）q取代，Y是苯基，呋喃基或噻吩基，该基团可以被1-3个取代基取代，羟基，卤素， CF 3，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基氨基羰基，单 - 或二-C 1-4 - 烷基氨基羰基，R 6是卤素，羟基， C 1-4 - 烷氧基或C 1-4 - 烷基，q为0,1,2或3及其盐。

3. 发明授权

US06225312B1 Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US06225312B1
公开(公告)日：2001-05-01
申请号：US09155608
申请日：1999-03-04
申请人： Roelof Willem Feenstra , Cornelis Gerrit Kruse , Martinus Theodorus Maria Tulp , Wilma Kuipers , Stephen Kenneth Long
发明人： Roelof Willem Feenstra , Cornelis Gerrit Kruse , Martinus Theodorus Maria Tulp , Wilma Kuipers , Stephen Kenneth Long
IPC分类号： C07D40504
CPC分类号： C07D263/58 , C07D209/08 , C07D215/12 , C07D265/36 , C07D307/79 , C07D311/18 , C07D317/66 , C07D319/08 , C07D319/18 , C07D321/10 , C07D327/06 , C07D333/54 , C07D405/04 , C07D407/10 , C07D409/10 , C07D413/10
摘要： The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.
摘要翻译：本发明涉及具有感兴趣的药理学性质的一组新的哌嗪和哌啶化合物。已经发现式（a）的化合物其中A表示5-7个环原子的杂环基，其中存在1-3个来自O，N和S基团的杂原子; R1是氢或氟; R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2; Z表示碳或氮，当Z为氮时，虚线为单键，Z为碳时为单键或双键; R3和R4独立地是氢或C1-4烷基; n的值为1或2; R5是卤素，羟基，C1-4烷氧基或C1-4烷基，q是0,1,2或3; Y是苯基，呋喃基或噻吩基，它们可以被1-3个羟基，卤素，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基，氨基羰基，单 - 或二-C 1-4 - 烷基氨基羰基; 其盐对多巴胺D2和5-羟色胺5-HT 1A受体表现出高亲和力。

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