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11. 发明申请

US20050171179A1 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
标题翻译：具有CB1拮抗活性的1,3,5-三取代的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US20050171179A1
公开(公告)日：2005-08-04
申请号：US11033683
申请日：2005-01-13
申请人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg
发明人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg
IPC分类号： C07D231/06 , A61K31/415
CPC分类号： C07D231/06
摘要： The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives as CB1 antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及作为CB 1拮抗剂的1,3,5-三取代的4,5-二氢-1H-吡唑衍生物，用于制备这些化合物的方法和用于合成的新中间体的所述吡唑衍生物。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

12. 发明申请

US20050143441A1 Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 审中-公开
标题翻译：涉及具有CB1拮抗作用的4,5-二氢-1H-吡唑衍生物的肥胖症的新型医疗联合治疗
公开(公告)号：US20050143441A1
公开(公告)日：2005-06-30
申请号：US11005486
申请日：2004-12-07
申请人： Jochen Antel , Gunter Krause , Peter-Colin Gregory , Michael Wurl , Harald Waldeck , Josephus Lange , Cornelis Kruse
发明人： Jochen Antel , Gunter Krause , Peter-Colin Gregory , Michael Wurl , Harald Waldeck , Josephus Lange , Cornelis Kruse
IPC分类号： A61K31/365 , A61K31/4152
CPC分类号： A61K31/4152 , A61K31/365 , A61K2300/00
摘要： The present invention relates to a novel medical use of e.g. 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor in combination with lipase inhibitors. Said compounds are particularly suitable in combination with lipase inhibitors in the manufacture of medicaments for the treatment and/or prophylaxis of obesity in adolescent or in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile as well as in adolescent patients. The compounds have the general formula (I) wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.
摘要翻译：本发明涉及一种新的医疗用途。 4,5-二氢-1H-吡唑化合物，其是大麻CB 1 - 受体与脂肪酶抑制剂组合的有效拮抗剂。所述化合物在制备用于治疗和/或预防青少年或青少年患者肥胖症的药物和/或用于治疗和/或预防青少年药物诱导的肥胖症以及青少年患者。化合物具有通式（I），其中基团Bb表示磺酰基或羰基，取代基R 1，R 1，R 2和R 3， SUB>，并且组Aa如说明书所示定义。优选的脂肪酶抑制剂是奥利司他，胰蛋白酶，ATL-962和/或脂抑素。

13. 发明申请

US20050065189A1 Thiazole derivatives as cannabinoid receptor modulators 审中-公开
标题翻译：噻唑衍生物作为大麻素受体调节剂
公开(公告)号：US20050065189A1
公开(公告)日：2005-03-24
申请号：US10942021
申请日：2004-09-16
申请人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg , Leonardus Sliedregt
发明人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg , Leonardus Sliedregt
IPC分类号： A61K31/427 , A61K31/4439 , A61P25/00 , C07D277/24 , C07D277/38 , C07D277/56 , C07D417/12 , C07D417/02
CPC分类号： A61K31/427 , A61K31/4439 , C07D277/24 , C07D277/56 , C07D417/12
摘要： The present invention relates to a group of thiazole derivatives, to methods for the preparation of these compounds, to pharmaceutical compositions containing at least one these compounds as active ingredient, as well to the use of these compositions for the treatment of psychiatric and neurological disorders and other diseases involving cannabinoid CB neurotransmission. The thiazole derivatives of the invention are either cannabinoid (CB) receptor antagonists, CB receptor agonists, CB receptor inverse agonists or CB receptor partial agonists. The compounds have the general formula (I) wherein R, R1 and X have the meanings given in the specification.
摘要翻译：本发明涉及一组噻唑衍生物，制备这些化合物的方法，含有至少一种这些化合物作为活性成分的药物组合物，以及这些组合物用于治疗精神和神经障碍的用途，以及其他涉及大麻素CB神经传递的疾病。本发明的噻唑衍生物是大麻素（CB）受体拮抗剂，CB受体激动剂，CB受体反向激动剂或CB受体部分激动剂。所述化合物具有通式（I），其中R，R 1和X具有说明书中给出的含义。

14. 发明申请

US20060293313A1 New phenylpiperazines 有权
标题翻译：新的苯基哌嗪
公开(公告)号：US20060293313A1
公开(公告)日：2006-12-28
申请号：US11450323
申请日：2006-06-12
申请人： Roelof Hes , Johannes Van der Heijden , Cornelis Kruse , Tipker Jacobus , Martinus Tulp , Gerben Visser , Bernard Van Vliet
发明人： Roelof Hes , Johannes Van der Heijden , Cornelis Kruse , Tipker Jacobus , Martinus Tulp , Gerben Visser , Bernard Van Vliet
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/496 , C07D417/14 , C07D413/14 , C07D405/14 , C07D403/14
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。

15. 发明申请

US20060122206A1 Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
标题翻译：具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚
公开(公告)号：US20060122206A1
公开(公告)日：2006-06-08
申请号：US11294657
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

16. 发明授权

US4874770A Aryl-substituted (N-piperidinyl)methyl- and (N-piperidinyl) methylazoles having antipsychotic properties 失效
标题翻译：具有抗精神病性质的芳基取代的（N-哌啶基）甲基和（N-哌啶基）甲基唑
公开(公告)号：US4874770A
公开(公告)日：1989-10-17
申请号：US214310
申请日：1988-07-01
申请人： Ineke Van Wijngaarden , Cornelis Kruse , Johannes A. M. Van Der Heyden , Martinus T. M. Tulp
发明人： Ineke Van Wijngaarden , Cornelis Kruse , Johannes A. M. Van Der Heyden , Martinus T. M. Tulp
IPC分类号： C07D319/00 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61P25/18 , A61P25/20 , C07D207/32 , C07D207/335 , C07D231/12 , C07D321/00 , C07D401/06 , C07D403/06 , C07D405/12
CPC分类号： C07D207/335 , C07D231/12 , C07D401/06 , C07D403/06
摘要： The invention relates to new aryl-substituted (N-piperidinyl)methyl- and (N-piperazinyl)methylazoles having interesting pharmacological, notably antipsychotic, properties.The compounds may be prepared in a manner known for the synthesis of analogous compounds and be processed to compositions according to known methods.

17. 发明申请

US20070066634A2 TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 有权
标题翻译：具有多巴胺D2受体和丝氨酸蛋白酶重复位点的亲和力组合的四氢吡啶并[4-YL]吲哚
公开(公告)号：US20070066634A2
公开(公告)日：2007-03-22
申请号：US11294657
申请日：2005-12-06
申请人： Roelof van Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof van Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6- membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5-或6-元环，其可以被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

18. 发明申请

US20060247256A1 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 审中-公开
标题翻译：具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物
公开(公告)号：US20060247256A1
公开(公告)日：2006-11-02
申请号：US11294615
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：其中符号具有说明书中给出的含义。

19. 发明申请

US20060122247A1 Aryloxyethylamine and phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 审中-公开
标题翻译：具有部分多巴胺-D2受体激动和5-羟色胺再摄取抑制的组合的芳氧基乙胺和苯基哌嗪衍生物
公开(公告)号：US20060122247A1
公开(公告)日：2006-06-08
申请号：US11294658
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Scharrenburg
IPC分类号： A61K31/423 , C07D413/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): Z-T-Ar (1) wherein: Z is a fragment of the general formula (2): and wherein the other symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用模式的新型芳氧基乙胺衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：<？in-line-formula description =“In-line Formulas”end =“lead”？> ZT-Ar（1）<？in-line-formula description =“In- 其中：Z为通式（2）的片段：其他符号具有本说明书中给出的含义，其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药学上可接受的盐，水合物和溶剂化物。

20. 发明申请

US20060122190A1 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 有权
标题翻译：具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物
公开(公告)号：US20060122190A1
公开(公告)日：2006-06-08
申请号：US11294603
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。所述化合物具有通式（1）：其中符号具有说明书中给出的含义及其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物的药理学上可接受的盐，水合物和溶剂化物，其互变异构体，立体异构体和N-氧化物。

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