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1. 发明授权

US08084473B2 Heterocyclic compounds with affinity to muscarinic receptors 有权
标题翻译：对毒蕈碱受体具有亲和力的杂环化合物
公开(公告)号：US08084473B2
公开(公告)日：2011-12-27
申请号：US12108275
申请日：2008-04-23
申请人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Jan H. Reinders , Louise Terwel, legal representative
发明人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Jan H. Reinders
IPC分类号： C07D413/00 , C07D401/00 , A01N43/40 , A61K31/44
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 the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof.
摘要翻译：本发明涉及式（I）的杂环化合物或其药学上可接受的盐，溶剂化物或水合物。

2. 发明授权

US08252930B2 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：US08252930B2
公开(公告)日：2012-08-28
申请号：US12940271
申请日：2010-11-05
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。

3. 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。

4. 发明授权

US08586606B2 Heterocyclic compounds with affinity to muscarinic receptors 有权
标题翻译：对毒蕈碱受体具有亲和力的杂环化合物
公开(公告)号：US08586606B2
公开(公告)日：2013-11-19
申请号：US13300800
申请日：2011-11-21
申请人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Louise Terwel
发明人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Jan H. Reinders
IPC分类号： A01N43/90 , A61K31/44 , C07D453/02
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。

5. 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。

6. 发明申请

US20090018160A1 Heterocyclic Compounds with Affinity to Muscarinic Receptors 有权
公开(公告)号：US20090018160A1
公开(公告)日：2009-01-15
申请号：US12108275
申请日：2008-04-23
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： C07D401/04 , A61K31/4439 , C07D413/04 , C07D451/02 , C07D453/02 , A61K31/439 , A61K31/46 , A61P25/00 , C07F7/02
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 the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof wherein the heterocycle comprises two double bonds which may be present at several positions, and which are represented by the dashed lines (---); the heterocycle contains two heteroatoms, W is N or NH; Y is CH, O or NH, wherein if Y is O, X1 is CH and X2 is C-Z-R2 or C—R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, wherein if X1 is CH or N, X2 is C-Z-R2 or C—R3, and if X2 is CH or N, X1 is C-Z-R2 or C—R3, wherein Z is NH or S; R1 is chosen from structures (a), (b) and (c): R2 is chosen from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; and R3 is chosen from (C4-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; and optionally, when R2 is an unbranched (C2-C8)alkyl, R2 links to formula (Ia) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, through the X1a or X2a of formula (Ia), wherein if X1 is CH or N, X1a is CH or N and X2a is C-Za-, or if X1 is C-Z-R2, X1a is C-Za- and X2a is CH or N, wherein X1a or X2a having Za links to R2; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I). The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.

7. 发明申请

US20110046171A1 ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 有权
标题翻译：作为5-HT6拮抗剂的芳基磺酰基吡唑烷酮衍生物
公开(公告)号：US20110046171A1
公开(公告)日：2011-02-24
申请号：US12933182
申请日：2009-03-17
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A.M. Rensink , Jennifer Venhorst , Martina A.W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A.M. Rensink , Jennifer Venhorst , Martina A.W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
IPC分类号： A61K31/438 , C07D231/54 , C07D231/06 , C07D491/10 , C07D403/12 , C07D471/10 , A61K31/415 , A61K31/416 , A61K31/4162 , A61K31/4155 , A61P25/16 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/06 , A61P25/28 , A61P25/00 , A61P25/20 , A61P3/00 , A61P3/04 , A61P25/30 , A61P1/00 , A61P3/10
CPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4162 , A61K31/435 , A61K31/635 , A61K45/06 , C07D231/00 , C07D231/54 , C07D403/12 , C07D471/10 , C07D491/10 , C07D491/107
摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

8. 发明申请

US20090005395A1 SILDENAFIL N-OXIDE AS PRODRUG 审中-公开
标题翻译： SILDENAFIL N-OXIDE作为PRODRUG
公开(公告)号：US20090005395A1
公开(公告)日：2009-01-01
申请号：US12143915
申请日：2008-06-23
申请人： Lechoslaw A. Turski , Axel Stoit , Cornelis G. Kruse , Sander Vader , Martinus Th.M. Tulp
发明人： Lechoslaw A. Turski , Axel Stoit , Cornelis G. Kruse , Sander Vader , Martinus Th.M. Tulp
IPC分类号： A61K31/519 , C07D487/04 , A61P15/10 , A61P9/12
CPC分类号： C07D487/04
摘要： Embodiments of the present invention relate to a compound of formula (1A) or a pharmacologically acceptable salt, hydrate, or solvate thereof. Other embodiments of the present invention relate to a pharmaceutical composition containing this compound, to methods for preparing this compound, and to methods for preparing compositions containing this compound. Yet other embodiments of the invention relate to uses of this compound, and compositions containing it, for the manufacture of medicaments and pharmaceutical compositions for treating erectile dysfunction or pulmonary arterial hypertension.
摘要翻译：本发明的实施方案涉及式（1A）化合物或其药理学上可接受的盐，水合物或溶剂化物。本发明的其它实施方案涉及含有该化合物的药物组合物，该化合物的制备方法以及含有该化合物的组合物的制备方法。本发明的其它实施方案涉及该化合物及其含有组合物用于制备用于治疗勃起功能障碍或肺动脉高压的药物和药物组合物的用途。

9. 发明授权

US08563723B2 Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists 有权
标题翻译：芳基磺酰基吡唑啉甲脒衍生物作为5-HT6拮抗剂
公开(公告)号：US08563723B2
公开(公告)日：2013-10-22
申请号：US12933182
申请日：2009-03-17
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A. M. Rensink , Jennifer Venhorst , Martina A. W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A. M. Rensink , Jennifer Venhorst , Martina A. W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
IPC分类号： C07D231/06 , C07D231/54 , C07D403/12 , C07D471/10 , C07D491/10
CPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4162 , A61K31/435 , A61K31/635 , A61K45/06 , C07D231/00 , C07D231/54 , C07D403/12 , C07D471/10 , C07D491/10 , C07D491/107
摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

10. 发明授权

US08101619B2 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：US08101619B2
公开(公告)日：2012-01-24
申请号：US11294603
申请日：2005-12-06
申请人： Roelof W. Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria L. Pras-Raves , Andrew C. McCreary , Bernard J. Van Vliet , Mayke B. Hesselink , Cornelis G. Kruse , Gustaaf J. M. Van Scharrenburg
发明人： Roelof W. Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria L. Pras-Raves , Andrew C. McCreary , Bernard J. Van Vliet , Mayke B. Hesselink , Cornelis G. Kruse , Gustaaf J. M. Van Scharrenburg
IPC分类号： A61K31/496 , C07D263/58
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。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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