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51. 发明申请

US20080146524A1 Selective inhibitors of neurotensin degrading enzymes 审中-公开
标题翻译：神经降压素降解酶的选择性抑制剂
公开(公告)号：US20080146524A1
公开(公告)日：2008-06-19
申请号：US12000273
申请日：2007-12-11
申请人： Pieter Smid , Roelof W. Feenstra , Cornelis G. Kruse
发明人： Pieter Smid , Roelof W. Feenstra , Cornelis G. Kruse
IPC分类号： A61K31/675 , A61P1/00 , A61P25/18 , A61P25/24 , A61P25/28 , A61P9/12 , C07F9/572 , C12N9/99
CPC分类号： C07K5/06 , A61K38/00 , C07F9/301 , C07F9/306 , C07F9/572 , C07F9/6539 , C07K5/06008 , C07K5/06026 , C07K5/06034 , C07K5/06139 , C07K5/06165
摘要： Embodiments of this invention relate to compounds that are selective inhibitors of neurotensin degrading enzymes, to pharmaceutical compositions containing these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions containing these compounds. The invention also relates to the use of such compounds and compositions for regulating blood pressure or gastric emptying, or treating Parkinson's disease, anxiety, depression, or psychosis. The compounds have the formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明的实施方案涉及作为神经降压素降解酶的选择性抑制剂的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，用于制备用于合成这些化合物的新中间体的方法，以及制备含有这些化合物的组合物的方法化合物。本发明还涉及这些化合物和组合物用于调节血压或胃排空或治疗帕金森病，焦虑，抑郁或精神病的用途。化合物具有式（1），其中符号具有说明书中给出的含义。

52. 发明授权

US07342032B2 Thiazole derivatives having CB1-antagonistic, agonistic or partial agonistic activity 有权
标题翻译：具有CB1拮抗，激动或部分激动活性的噻唑衍生物
公开(公告)号：US07342032B2
公开(公告)日：2008-03-11
申请号：US10490546
申请日：2003-03-17
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Arnoldus H. J. Herremans , Herman H. van Stuivenberg , Jessica A. R. Dijksman , Andrew C. McCreary
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Arnoldus H. J. Herremans , Herman H. van Stuivenberg , Jessica A. R. Dijksman , Andrew C. McCreary
IPC分类号： A61K31/426 , C07D277/56
CPC分类号： C07D417/12 , C07D277/56
摘要： Computer game systems respond to the spatial state of a pointing device. Changes in the spatial state of a hand held or mobile unit, or plurality of units drive a game scheme maintained in a computer. Position and attitude of the mobile device cause program branching functions which are bases upon a game rule set. In example, a game scheme executed on a computing apparatus may be incorporated into a mobile telephone having a GPS and electronic compass. Physical states relating to position and pointing attitude of the telephone as described in part by position or attitude parameters, drives computer programming code to takes actions which depend on measured position and attitude values thus making computer games for mobile users are made highly interactive. User gestures including simple pointing actions allow a user to express desires to a computer in an express and direct fashion. These games have many features which cannot be found in more traditional handheld computer games which do not take into consideration the spatial state of an object controlled by a player-user
摘要翻译：本发明涉及作为大麻素CB1受体的有效拮抗剂，激动剂或部分激动剂的噻唑衍生物。这些化合物具有通式（I），其中R和R 1 -R 4具有说明书中给出的含义

53. 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

54. 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。

55. 发明授权

US08461184B2 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：US08461184B2
公开(公告)日：2013-06-11
申请号：US12844156
申请日：2010-07-27
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Bernard J. Vliet Van
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Bernard J. Vliet Van
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。

56. 发明申请

US20120095039A1 HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS 有权
标题翻译：具有对肌肉受体的亲和性的杂环化合物
公开(公告)号：US20120095039A1
公开(公告)日：2012-04-19
申请号：US13300800
申请日：2011-11-21
申请人： Axel Stoit , Hein K.A.C. Coolen , Cornelis G. Kruse , Jan H. Reinders , Louise Terwel
发明人： Axel Stoit , Hein K.A.C. Coolen , Cornelis G. Kruse , Jan H. Reinders , Louise Terwel
IPC分类号： A61K31/439 , A61K31/46 , C07D413/04 , A61P25/18 , C07D401/04 , C07F7/02 , C07D487/08 , A61P25/00
CPC分类号： C07D471/08 , A61K31/439 , A61K45/06 , C07D401/04 , C07D403/04 , C07D413/04 , C07F7/1804
摘要： The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.
摘要翻译：本发明涉及对毒蕈碱受体具有亲和力的式（I）的杂环化合物，含有这些化合物的药物组合物，以及该化合物用于制备治疗，减轻或预防毒蕈碱受体介导的疾病的药物的用途，条件。

57. 发明授权

US07964728B2 Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition 有权
标题翻译：具有部分烟碱乙酰胆碱受体激动和多巴胺再吸收抑制的组合的阿维醇衍生物
公开(公告)号：US07964728B2
公开(公告)日：2011-06-21
申请号：US11773111
申请日：2007-07-03
申请人： Axel Stoit , Hein K. A. C. Coolen , Martina A. W. Van Der Neut , Cornelis G. Kruse
发明人： Axel Stoit , Hein K. A. C. Coolen , Martina A. W. Van Der Neut , Cornelis G. Kruse
IPC分类号： C07D471/02
CPC分类号： C07D471/04 , C07D519/00
摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
摘要翻译：描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过这些受体的操纵来治疗。

58. 发明授权

US07745476B2 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：US07745476B2
公开(公告)日：2010-06-29
申请号：US11033683
申请日：2005-01-13
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Herman H. Van Stuivenberg
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Herman H. Van Stuivenberg
IPC分类号： A61K31/415 , C07D231/06
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CB1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所述吡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。化合物具有通式（I），其中符号具有说明书中给出的含义。

59. 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。

60. 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。

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