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1. 发明授权

US07297699B2 Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US07297699B2
公开(公告)日：2007-11-20
申请号：US11129465
申请日：2005-05-16
申请人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
发明人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
IPC分类号： A61K31/496 , C07D263/58 , C07D277/68
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, —Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors
摘要翻译：本发明涉及下式的一组新的哌嗪和哌啶衍生物其中Y是氢，卤素，烷基（1-3C）或CN，CF 3，OCF 3， >，SCF 3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基，X是O，S，SO或SO 2， SUB，-Z表示-C，-C或-N，R 1和R 2独立地表示氢或烷基（1-3C），Q是苄基或2 - ，3-或4-吡啶基甲基，其基团可以被一个或多个取代基取代，所述取代基可以是卤素，硝基，氰基，氨基，单或二（1-3C）烷基氨基，（1-3C）烷氧基，CF OCF 3，SCF 3，（1-4C） - 烷基，（1-3C）烷基磺酰基或羟基，及其盐和前体药物其中。已经发现，这些化合物由于（多）向多巴胺D 2受体亚家族的成员的组合以及对相关的5-羟色胺和/或去甲肾上腺素能受体的亲和力而具有令人感兴趣的药理学性质

2. 发明授权

US06911448B2 Piperazine and piperidine compounds 失效
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US06911448B2
公开(公告)日：2005-06-28
申请号：US10257677
申请日：2001-05-10
申请人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
发明人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
IPC分类号： C07D413/10 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D263/54 , C07D263/58 , C07D277/62 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/454
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors
摘要翻译：本发明涉及下式的一组新的哌嗪和哌啶衍生物其中Y是氢，卤素，烷基（1-3C）或CN，CF 3，OCF 3， >，SCF 3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基，X是O，S，SO或SO 2， Z表示-C，-C或-N，R 1和R 2独立地表示氢或烷基（1-3C），Q表示苄基或2-，3-或4-吡啶基甲基，其可以被一个或多个取代基取代为卤素，硝基，氰基，氨基，单或二（1-3C）烷基氨基，（1-3C）烷氧基，CF 3 3，OCF 3，SCF 3，（1-4C） - 烷基，（1-3C）烷基磺酰基或羟基，和盐及其前体药物。已经发现，这些化合物由于（多）向多巴胺D 2受体亚家族的成员的组合以及对相关的5-羟色胺和/或去甲肾上腺素能受体的亲和力而具有令人感兴趣的药理学性质

3. 发明授权

US06780864B1 Piperazine and piperidine compounds 失效
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US06780864B1
公开(公告)日：2004-08-24
申请号：US09831149
申请日：2001-08-14
申请人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
发明人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D277/68 , C07D401/04 , C07D413/04 , C07D417/04 , Y02P20/55
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents ═C or —N; —R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl—methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.
摘要翻译：本发明涉及一组式（I）的新的哌嗪和哌啶衍生物，其中：S1为氢，卤素，烷基（1-3C），CN，CF3，OCF3，SCF3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基; X表示NR 3，S，CH 2，O，SO或SO 2，其中R 3是H或烷基（1-3C）; 。。。 Z表示= C或-N; -R1独立地表示H或烷基（1-3C），或者R1和R2一起可以形成桥2或3个C原子; R4是氢或烷基（1-3C）; Q是甲基，乙基，被一个或多个氟原子取代的乙基，任选被一个或多个氟原子取代的环丙基甲基，及其盐和前药。已经发现这些化合物具有部分多巴胺D2受体激动和部分5-羟色胺5-HT 1A受体激动介导的活性。

4. 发明授权

US06214829B1 Piperazine compounds, their preparation, and methods of using them 有权
标题翻译：哌嗪化合物，它们的制备方法和使用它们的方法
公开(公告)号：US06214829B1
公开(公告)日：2001-04-10
申请号：US09144076
申请日：1998-08-31
申请人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： A61K31496
CPC分类号： C07D263/58 , C07D215/38 , C07D265/36 , C07D401/12 , C07D409/12
摘要： Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2 receptors and serotonine 5-HT1A receptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.
摘要翻译：新颖的哌嗪和哌啶衍生化合物具有有趣和有利的药理学性质。所述化合物具有通式（a）及其盐。这些化合物对多巴胺D2受体和5-羟色胺5-HT 1A受体具有高亲和力，使其可用于治疗中枢神经系统疾病，特别是精神分裂症。

5. 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。

6. 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。

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