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11. 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。

12. 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.

13. 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。

14. 发明申请

US20070281974A1 1 H-IMIDAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS 失效
标题翻译： 1 H-咪唑衍生物作为CANNABINOID受体调节剂
公开(公告)号：US20070281974A1
公开(公告)日：2007-12-06
申请号：US11842657
申请日：2007-08-21
申请人： Josephus Lange , Cornelis Kruse , Herman Van Stuivenberg , Hiskias Keizer
发明人： Josephus Lange , Cornelis Kruse , Herman Van Stuivenberg , Hiskias Keizer
IPC分类号： A61K31/4178 , A61K31/4164 , A61K31/454 , A61P1/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P9/00
CPC分类号： C07D233/90
摘要： The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1—R4 and X have the meanings given in the specification.
摘要翻译：本发明涉及一组作为大麻素受体的调节剂的1H-咪唑衍生物，制备这些化合物的方法，可用于合成所述咪唑衍生物的新中间体，制备这些中间体的方法，药物含有这些1H-咪唑衍生物中的一种或多种作为活性成分的组合物，以及这些药物组合物用于治疗涉及大麻素受体的精神病和神经障碍的用途。化合物具有通式（I），其中R 1，R 1 -R 4和X具有说明书中给出的含义。

15. 发明申请

US20070259884A1 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：US20070259884A1
公开(公告)日：2007-11-08
申请号：US11265090
申请日：2005-11-03
申请人： Josephus Lange , Cornelis Kruse , Jacobus Tipker , Herman van Stuivenberg , Arnoldus Herremans
发明人： Josephus Lange , Cornelis Kruse , Jacobus Tipker , Herman van Stuivenberg , Arnoldus Herremans
IPC分类号： A61K31/415 , A61K31/454 , A61K31/497 , A61P25/00 , C07D231/06 , C07D401/12 , C07D403/12
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。

16. 发明申请

US20050267161A1 Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity 有权
标题翻译：四氮取代咪唑衍生物作为具有高CB1 / CB2受体亚型选择性的大麻素CB1受体调节剂
公开(公告)号：US20050267161A1
公开(公告)日：2005-12-01
申请号：US11138289
申请日：2005-05-27
申请人： Josephus Lange , Henderik Wals , Cornelis Kruse
发明人： Josephus Lange , Henderik Wals , Cornelis Kruse
IPC分类号： A61K31/4178 , A61K31/4439 , C07D233/90 , C07D43/02
CPC分类号： C07D233/90
摘要： The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB1 receptor modulators, in particular CB1 receptor antagonists or inverse agonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in 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：本发明涉及作为选择性大麻素CB 1受体调节剂的1,2,4,5-四取代的咪唑衍生物，特别是CB 1受体拮抗剂或具有高 CB 1 / CB 2受体亚型选择性，制备这些化合物的方法和可用于合成所述咪唑衍生物的新型中间体。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。本领域技术人员从本领域的说明书和一般知识中可以公开有益效果或显而易见的。本发明还涉及本发明化合物在制备用于治疗或预防疾病或病症的药物中的用途。更具体地，本发明涉及本领域技术人员从本领域技术人员的说明书和一般知识中治疗本文公开的疾病或病症的新用途。在本发明的实施方案中，本文公开的具体化合物用于制备用于治疗精神病和神经障碍的药物。化合物具有通式（I），其中符号具有说明书中给出的含义。

17. 发明申请

US20050239859A2 NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1-拮抗活性的4,5-二氢-1H-吡唑衍生物的新医学用途
公开(公告)号：US20050239859A2
公开(公告)日：2005-10-27
申请号：US10929377
申请日：2004-08-31
申请人： Jochen Antel , Gunter Krause , Josephus Lange , Cornelis Kruse , Peter-Colin Gregory , Cathaline Den Besten
发明人： Jochen Antel , Gunter Krause , Josephus Lange , Cornelis Kruse , Peter-Colin Gregory , Cathaline Den Besten
IPC分类号： A61K31/415
CPC分类号： A61K31/415
摘要： Abstract of the DisclosureThe present invention relates to a novel medical use of 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor. Said compounds are particularly suitable in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases 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.
摘要翻译：本发明摘要本发明涉及作为大麻CB 1受体的有效拮抗剂的4,5-二氢-1H-吡唑化合物的新型医疗用途。所述化合物特别适用于制备用于治疗和/或预防少年患者中CB 1受体相关疾病的药物和/或用于治疗和/或预防未成年人药物诱导的肥胖的药物就像青少年患者一样。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。

18. 发明申请

US20070135492A1 Imidazoline derivatives having CB1-antagonistic activity 失效
标题翻译：具有CB1拮抗活性的咪唑啉衍生物
公开(公告)号：US20070135492A1
公开(公告)日：2007-06-14
申请号：US11652582
申请日：2007-01-12
申请人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg
发明人： Josephus Lange , Cornelis Kruse , Herman Stuivenberg
IPC分类号： A61K31/4439 , A61K31/4178 , C07D409/02 , C07D405/02 , C07D403/02
CPC分类号： C07D233/26
摘要： The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, 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1,2,4-三取代咪唑啉衍生物，制备这些化合物的方法，可用于合成所述咪唑啉衍生物的新中间体，制备这些中间体的方法，药物组合物含有这些咪唑啉衍生物中的一种或多种作为活性成分，以及这些药物组合物用于治疗精神和神经障碍的用途。该化合物具有通式。（I）其中符号具有说明书中给出的含义。

19. 发明申请

US20050187259A1 Imidazoline derivatives having CB1-antagonistic activity 有权
标题翻译：具有CB1拮抗活性的咪唑啉衍生物
公开(公告)号：US20050187259A1
公开(公告)日：2005-08-25
申请号：US11058168
申请日：2005-02-16
申请人： Josephus Lange , Cornelis Kruse , Herman Van Stuivenberg
发明人： Josephus Lange , Cornelis Kruse , Herman Van Stuivenberg
IPC分类号： A61K31/4178 , A61K31/4439 , C07D233/26 , C07D43/02
CPC分类号： C07D233/26
摘要： The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, 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1,2,4-三取代咪唑啉衍生物，制备这些化合物的方法，可用于合成所述咪唑啉衍生物的新中间体，制备这些中间体的方法，药物组合物含有这些咪唑啉衍生物中的一种或多种作为活性成分，以及这些药物组合物用于治疗精神病和神经障碍的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

20. 发明申请

US20050124660A1 Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds 审中-公开
标题翻译：显示CB1拮抗活性的化合物的新型医疗用途和涉及所述化合物的组合治疗
公开(公告)号：US20050124660A1
公开(公告)日：2005-06-09
申请号：US10969840
申请日：2004-10-22
申请人： Jochen Antel , Peter-Colin Gregory , Harald Waldeck , Gunter Krause , Josephus Lange , Cornelis Kruse
发明人： Jochen Antel , Peter-Colin Gregory , Harald Waldeck , Gunter Krause , Josephus Lange , Cornelis Kruse
IPC分类号： A61K31/4196 , A61K31/426 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/541
CPC分类号： A61K31/4439 , A61K31/4196 , A61K31/426 , A61K31/454 , A61K31/5377 , A61K31/541
摘要： The present invention relates to a novel medical use of compounds with CB1-receptor activity selected from the group of 4,5-dihydro-1H-pyrazole derivatives, 1H-Imidazole derivatives, thiazole derivatives and/or 1H-1,2,4-triazole-3-carboxamide derivatives, as each defined in the specification, or of a prodrug thereof, a tautomer thereof or a salt thereof, in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile, as well as in adolescent, patients. Furthermore, the invention pertains to the use of said compounds with CB1-receptor activity 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. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.
摘要翻译：本发明涉及一种具有选自4,5-二氢-1H-吡唑衍生物，1H-咪唑衍生物，噻唑衍生物和/或其中之一种具有CB 1 - 1 - 受体活性的化合物的新型医疗用途在制备用于治疗和/或预防CB的药物中的1H-1,2,4-三唑-3-甲酰胺衍生物，如说明书中所定义，或其前药，其互变异构体或其盐少年患者中的受体相关疾病和/或用于治疗和/或预防青少年以及青少年患者的药物诱导的肥胖症。此外，本发明涉及具有CB 1/2受体活性的所述化合物与脂肪酶抑制剂的组合的用途。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。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。

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