专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06476060B2 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
标题翻译：具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US06476060B2
公开(公告)日：2002-11-05
申请号：US09814694
申请日：2001-03-23
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Bernard J. Van Vliet
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Bernard J. Van Vliet
IPC分类号： A61K31415
CPC分类号： C07D231/06 , C07D231/08 , C07D401/04 , C07D409/04
摘要： The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor. The compounds have the formula (I) wherein R and R1 are the same or different and represent unsubstituted or substituted phenyl, thienyl, or pyridyl, or naphthyl. naphthyl R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v) as defined herein, Bb represents sulfonyl or carbonyl, and R3 represents benzyl, phenyl, thienyl or pyridyl, each of which is unsubstituted or substituted, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphthyl.
摘要翻译：本发明涉及新的4,5-二氢-1H-吡唑化合物，其可以是大麻CB1-受体的有效拮抗剂。化合物具有式（I），其中R和R 1相同或不同，代表未取代或取代的苯基，噻吩基或吡啶基或萘基。萘基R 2表示氢，羟基，C 1-3 - 烷氧基，乙酰氧基或丙酰氧基，A a表示如本文所定义的基团（ⅰ），（ⅱ），（ⅲ），（ⅳ）或（Ⅴ）中的一个，Bb表示磺酰基或羰基，R 3表示苄基，苯基，噻吩基或吡啶基，其各自为未取代或取代的，或R3表示C1-8支链或非支链烷基或C3-8环烷基，或R3表示萘基。

2. 发明授权

US07456182B2 Phenylpiperazines 有权
标题翻译：苯基哌嗪
公开(公告)号：US07456182B2
公开(公告)日：2008-11-25
申请号：US11450323
申请日：2006-06-12
申请人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： A61K31/496 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统如焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

3. 发明授权

US06391896B1 3-Tetrahydropyridin-4-yl indoles for treatment of psychotic disorders 有权
标题翻译： 3-四氢吡啶-4-基吲哚用于治疗精神病
公开(公告)号：US06391896B1
公开(公告)日：2002-05-21
申请号：US09807408
申请日：2001-07-03
申请人： Roelof Van Hes , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： C07D40106
CPC分类号： C07D401/14
摘要： The invention is related to the following compounds: wherein all variables are as defined in the specification. The compounds are useful for treating psychotic disorders.
摘要翻译：本发明涉及以下化合物：其中所有变量如说明书中所定义。这些化合物可用于治疗精神病。

4. 发明授权

US07605162B2 Phenylpiperazine 失效
标题翻译：苯基哌嗪
公开(公告)号：US07605162B2
公开(公告)日：2009-10-20
申请号：US12258591
申请日：2008-10-27
申请人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： A61K31/496 , C07D403/12
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D2受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统中的干扰相关的病症的能力，例如作为焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R5和R6独立地是氢或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）p - 其中p具有3-5，R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或R6 + R7（吲哚基的第7位的R7）表示基团 - （CH 2）q，其中q具有2-4，及其盐。

5. 发明授权

US06335326B1 Benzisoxazole derivatives having d4-antagonistic activity 有权
标题翻译：具有d4拮抗活性的苯并异恶唑衍生物
公开(公告)号：US06335326B1
公开(公告)日：2002-01-01
申请号：US09601795
申请日：2000-10-23
申请人： Jacobus A. J. Den Hartog , Gerben M. Visser , Bartholomeus J. Van Steen , Martinus T. M. Tulp , Eric Ronken , Cornelis G. Kruse , Josephus H. M. Lange
发明人： Jacobus A. J. Den Hartog , Gerben M. Visser , Bartholomeus J. Van Steen , Martinus T. M. Tulp , Eric Ronken , Cornelis G. Kruse , Josephus H. M. Lange
IPC分类号： A01N4346
CPC分类号： C07D413/14
摘要： The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2, or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group —CH2—(CRH)p— wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.
摘要翻译：本发明涉及一组新的苯并异恶唑衍生物，其是多巴胺D4受体的有效和选择性拮抗剂。化合物具有通式（I），其中（R1）n表示0,1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，或二烷基（C1-2） - 氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单 - 或二烷基（C1-2） - 氨基，X是O，S，NH或 NCH 3，Y表示CH 2或（CH 2）2，（R 2）m表示0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）m是亚甲基桥或乙基桥，A是-CH 2 - （CRH）p - 基团，其中R是氢或甲基，p是0或1，B表示2-或3-吲哚基或2-苯并咪唑基，该基团可以在碳上被取代， 1或2个C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基，一或二烷基（C 1-2）氨基，磺酰基 - （C 1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单或二烷基（C 1-2） - 氨基。

6. 发明授权

US07786144B2 Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 有权
标题翻译：含硫吡唑衍生物作为选择性大麻素CB1受体拮抗剂
公开(公告)号：US07786144B2
公开(公告)日：2010-08-31
申请号：US11754544
申请日：2007-05-29
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
IPC分类号： A61K31/4155 , A61K31/4453 , C07D231/10 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB1 / CB2受体亚型选择性的选择性大麻素CB1受体拮抗剂，用于制备这些化合物的方法，可用于合成的新中间体这些吡唑衍生物，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗精神和神经障碍的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

7. 发明申请

US20090143406A1 New Phenylpiperazine 失效
标题翻译：新苯基哌嗪
公开(公告)号：US20090143406A1
公开(公告)日：2009-06-04
申请号：US12258591
申请日：2008-10-27
申请人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T.M Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T.M Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： A61K31/496 , C07D403/04
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D2受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统中的干扰相关的病症的能力，例如作为焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R5和R6独立地是氢或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）p - 其中p具有3-5，R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或R6 + R7（吲哚基的第7位的R7）表示基团 - （CH 2）q，其中q具有2-4，及其盐。

8. 发明授权

US06974810B2 4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity 失效
标题翻译：具有强的CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US06974810B2
公开(公告)日：2005-12-13
申请号：US10472529
申请日：2002-09-17
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Herman H. van Stuivenberg , Arnoldus H. J. Herremans
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Herman H. van Stuivenberg , Arnoldus H. J. Herremans
IPC分类号： C08K5/09 , A61K31/194 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P1/04 , A61P1/08 , A61P1/12 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07D231/06 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/04 , C07D413/06
CPC分类号： C07D231/06 , C07D401/04 , C07D401/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱相关的疾病的有效大麻素（CB 1）受体拮抗剂。化合物具有通式（Ia）或（Ib），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物

9. 发明授权

US07608718B2 4,5-dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity 失效
标题翻译：具有强的CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US07608718B2
公开(公告)日：2009-10-27
申请号：US11265090
申请日：2005-11-03
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Herman H. van Stuivenberg , Arnoldus H. J. Herremans
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Herman H. van Stuivenberg , Arnoldus H. J. Herremans
IPC分类号： A61K31/454 , C07D401/12
CPC分类号： C07D231/06 , C07D401/04 , C07D401/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱有关的疾病的有效大麻素（CB1）受体拮抗剂。化合物具有通式（Ia）或（Ib），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。

10. 发明授权

US07528162B2 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
标题翻译：具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US07528162B2
公开(公告)日：2009-05-05
申请号：US10490291
申请日：2002-09-17
申请人： Cornelis G. Kruse , Josephus H. M. Lange , Jacobus Tipker , Arnoldus H. J. Herremans , Herman H. Van Stuivenberg
发明人： Cornelis G. Kruse , Josephus H. M. Lange , Jacobus Tipker , Arnoldus H. J. Herremans , Herman H. Van Stuivenberg
IPC分类号： A61K31/415 , C07D401/12
CPC分类号： C07D231/06 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱有关的疾病的有效大麻素（CB1）受体拮抗剂。化合物具有通式（I），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式