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1. 发明申请

US20080311179A1 SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 有权
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑和磺酰基吡唑烷酮衍生物
公开(公告)号：US20080311179A1
公开(公告)日：2008-12-18
申请号：US11859323
申请日：2007-09-21
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
IPC分类号： A61K9/12 , C07D403/12 , C07D409/12 , C07D413/14 , A61K9/48 , A61P3/00 , A61P1/00 , A61P25/00 , A61K9/70 , A61K31/4155 , A61K31/4245
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns compounds of the general formula (1). and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from 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.
摘要翻译：本发明涉及通式（1）的化合物。及其衍生物，其为5-HT 6受体的拮抗剂，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，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，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，注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征肠综合征，肥胖症和2型糖尿病。

2. 发明授权

US07381729B2 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo [2,3D] pyrimidine hydrogen mesylate, its polymorphic forms, and methods for making same 有权
标题翻译： 4-（4-反 - 羟基环己基）氨基-2-苯基-7H-吡咯并[2,3d]嘧啶氢甲磺酸盐，其多晶型物及其制备方法
公开(公告)号：US07381729B2
公开(公告)日：2008-06-03
申请号：US10828650
申请日：2004-04-21
申请人： Axel Pahl , Timo Heinrich , Emil Finner , Bernd-Martin Luitjens , Jan Zorgdrager , Pieter C. Verveer
发明人： Axel Pahl , Timo Heinrich , Emil Finner , Bernd-Martin Luitjens , Jan Zorgdrager , Pieter C. Verveer
IPC分类号： C07D487/04 , A61K31/519 , A61P9/04 , A61P13/12 , A61P9/12
CPC分类号： C07D487/04
摘要： The present invention relates to the novel compound 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo[2,3d]pyrimidine hydrogen mesylate, the polymorphic α and β forms thereof, and a method for the production of said compounds.
摘要翻译：本发明涉及新化合物4-（4-反 - 羟基环己基）氨基-2-苯基-7H-吡咯并[2,3d]嘧啶氢甲磺酸盐，其多晶型α和β形式，以及制备所述化合物。

3. 发明授权

US07030241B2 Mesylates of piperazine derivatives and process for their preparation 失效
标题翻译：哌嗪衍生物的甲磺酸酯及其制备方法
公开(公告)号：US07030241B2
公开(公告)日：2006-04-18
申请号：US10468098
申请日：2002-02-14
申请人： Marcel P. M. van Aar , Stefanus J. Schouten , Jan Zorgdrager , Michiel C. Heslinga
发明人： Marcel P. M. van Aar , Stefanus J. Schouten , Jan Zorgdrager , Michiel C. Heslinga
IPC分类号： C07D403/00 , C07D401/00 , C07D405/00 , C07D409/00
CPC分类号： C07D263/58
摘要： The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3–7C) methyl, benzyl or m-phenyl benzyl
摘要翻译：本发明涉及一组哌嗪衍生物的甲磺酸盐，以及以高产率和高纯度经济地制备这些甲磺酸盐的方法。根据本发明的方法，在单个反应步骤中合并哌嗪环和甲磺酸酯形成。本发明涉及式（I）化合物的甲磺酸酯，其中X为双环杂环苯基，Y为甲基，乙基（任选被氟取代），环烷基（3-7C）甲基，苄基或间苯基苄基

4. 发明授权

US08722887B2 Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-HT6 antagonists 有权
标题翻译：磺酰基吡唑和磺酰吡唑啉甲脒衍生物作为5-HT6拮抗剂
公开(公告)号：US08722887B2
公开(公告)日：2014-05-13
申请号：US12706279
申请日：2010-02-16
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A. W. Van Der Neut , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A. W. Van Der Neut , Cornelis G. Kruse
IPC分类号： C07D231/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/10
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from 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.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的通式（1）的化合物及其衍生物，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，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，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，注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征肠综合征，肥胖症和2型糖尿病。

5. 发明申请

US20070275977A1 N-OXIDES OF PYRIDYLMETHYL -PIPERAZINE AND -PIPERIDINE DERIVATIVES 审中-公开
标题翻译：吡咯并吡啶和哌啶衍生物的N-氧化物
公开(公告)号：US20070275977A1
公开(公告)日：2007-11-29
申请号：US11743049
申请日：2007-05-01
申请人： Marcel Van Aar , Peter Van Amsterdam , Gerrit Barf , Johan Bakker , Cathaline Den Besten , Arnoldus Herremans , Jan Zorgdrager
发明人： Marcel Van Aar , Peter Van Amsterdam , Gerrit Barf , Johan Bakker , Cathaline Den Besten , Arnoldus Herremans , Jan Zorgdrager
IPC分类号： A61K31/496 , C07D405/14
CPC分类号： C07D405/12
摘要： N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives are provided as alternatives to or as “prodrugs” of their respective parent compounds, as well as pharmaceutical compositions containing these N-oxides, methods for preparing them, and compositions comprising them. The N-oxides have the formula (a) wherein the substituents have the meanings given in the description, and wherein the oxidized nitrogen atom can be the nitrogen atom in the pyridyl ring of R5, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or both the nitrogen atom connected to R5 via a methylene group, and the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates, and solvates thereof. In addition, the N-oxides and compositions can be used as medicaments useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems.
摘要翻译：提供某些吡啶基甲基哌嗪和哌啶衍生物的N-氧化物作为其各自母体化合物的“前体药物”的替代物或含有这些N-氧化物的药物组合物，其制备方法和包含它们的组合物。 N-氧化物具有式（a），其中取代基具有本说明书中给出的含义，其中氧化的氮原子可以是R 5的吡啶环中的氮原子，或氮哌啶环中的一个原子（当Z为碳时）或哌嗪环中的氮原子之一（当Z为氮时），或通过亚甲基与R 5连接的氮原子，和R 5的吡啶环中的氮原子，以及互变异构体，立体异构体，药理学上可接受的盐，水合物和溶剂化物。此外，N-氧化物和组合物可以用作治疗由多巴胺能或血清素能系统中的紊乱引起的中枢神经系统的情感或疾病的药物。

6. 发明授权

US6075015A Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：US6075015A
公开(公告)日：2000-06-13
申请号：US863947
申请日：1997-05-27
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： Vitamin D.sub.3 analogues of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is (C.sub.1 -C.sub.3)alkyl, hydroxy(C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.2)alkoxymethyl, (C.sub.2 -C.sub.3)alkenyl, or (C.sub.2 -C.sub.3)alkynyl, R.sub.3 is a branched or unbranched, saturated or unsaturated aliphatic 3- to 5- membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy, R.sub.4 is sec. or tert. (C.sub.3 -C.sub.6)alkyl or (C.sub.3 -C.sub.6)cycloalkyl, A and B are each individually hydrogen or methyl, or A and B together from methylene. The compounds of the present invention exhibit pharmacotherapeutic activities, including in particular, the treatment of osteoporosis, renal osteodystrophy, osteomalacia, skin disorders such as psoriasis and other hyperproliferative skin diseases, eczema and dermatitis, nmyopathy, leukemia, breast and colon cancer, osteosarcomas, squamous cell carcinomas, melanoma, certain immunological disorders, and transplant rejections. Several methods of synthesis, including reaction of an ester compound of general formula (IX) with an inorganometallic compound of formula (III) followed by deprotection or, alternatively, first finalization of the C.sub.17 -side chain are also disclosed.
摘要翻译：式（I）的维生素D3类似物：其中R1是氢或羟基，R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基，（C2-C3）烯基或（ C 2 -C 3）炔基，R 3是支链或非支链的饱和或不饱和的脂族3-至5-元烃基或氧杂烃双基，在主链中具有至少3个原子，并且任选地被一个或多个选自环氧基，氟和羟基，R4是秒。或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基，A和B各自独立地为氢或甲基，或A和B一起为亚甲基。本发明的化合物具有药物治疗活性，特别包括治疗骨质疏松症，肾性骨营养不良，骨软化症，皮肤疾病如牛皮癣和其它过度增生性皮肤病，湿疹和皮炎，纳米病，白血病，乳腺和结肠癌，骨肉瘤，鳞状细胞癌，黑素瘤，某些免疫性疾病和移植排斥。还公开了几种合成方法，包括通式（IX）的酯化合物与式（III）的无机金属化合物反应，然后进行脱保护，或者也可以首先终止C17-侧链。

7. 发明授权

US5449668A Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：US5449668A
公开(公告)日：1995-09-12
申请号：US70998
申请日：1993-06-04
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/24 , A61K31/205
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及通式（I）的新的维生素D化合物，其中：R1是氢原子或羟基; R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基或（C2-C3）烯基或炔基; R3是在主链中具有至少3个原子且任选地被一个或多个选自环氧基，氟和羟基的取代基取代的支化或非支化的饱和或不饱和脂族3-至5-元烃或二烃基双基。 R4是秒或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基; A和B各自为氢原子或甲基，或A和B一起形成亚甲基。本发明还涉及这些化合物的制备方法及其在药物治疗和化妆品中的应用。

8. 再颁专利

USRE36854E Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：USRE36854E
公开(公告)日：2000-09-05
申请号：US931073
申请日：1997-09-15
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/205 , A61K31/59
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及以下通式的新的维生素D化合物：其中：R1是氢原子或羟基; R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基或（C2-C3）烯基或炔基; R3是在主链中具有至少3个原子且任选地被一个或多个选自环氧基，氟和羟基的取代基取代的支化或非支化的饱和或不饱和脂族3-至5-元烃或二烃基双基。 R4是秒或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基; A和B各自为氢原子或甲基，或A和B一起形成亚甲基。本发明还涉及这些化合物的制备方法及其在药物治疗和化妆品中的应用。

9. 发明授权

US06072062A Synthesis of C.sub.18 -modified vitamin D compounds and compounds resulting therefrom 失效
标题翻译： C18改性维生素D化合物的合成及由此产生的化合物
公开(公告)号：US06072062A
公开(公告)日：2000-06-06
申请号：US799346
申请日：1997-02-13
申请人： Maria J. Valles , Jose L. Mascarenas , Antonio Mourino , Sebastianus J. Halkes , Jan Zorgdrager
发明人： Maria J. Valles , Jose L. Mascarenas , Antonio Mourino , Sebastianus J. Halkes , Jan Zorgdrager
IPC分类号： A61K31/59 , A61P3/02 , C07C29/143 , C07C35/32 , C07C43/305 , C07C43/315 , C07C401/00 , C07D305/14 , C07D307/93 , C07D307/94 , C07D311/94 , C07D317/20 , C07D407/04 , C07F7/18 , C07F9/53
CPC分类号： C07D407/04 , C07C401/00 , C07C43/315 , C07D307/93 , C07D307/94 , C07D311/94 , C07D317/20 , C07F7/1856 , C07F9/532 , C07C2101/14 , C07C2102/24
摘要： The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate. The vitamin D compound is of the general formula ##STR1##
摘要翻译：本发明涉及在18位被烷基，羟基，烷氧基，烯基，炔基，氟化烷基或氟化烯基取代的新的维生素D化合物。本发明还涉及一种制备所述维生素D化合物以及内酯和氢化茚中间体的方法。维生素D化合物为通式

10. 发明申请

US20100145042A1 SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 有权
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑和磺酰基吡唑烷酮衍生物
公开(公告)号：US20100145042A1
公开(公告)日：2010-06-10
申请号：US12706279
申请日：2010-02-16
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
IPC分类号： C07D413/12 , C07D403/12 , C07D471/10 , C07D401/12 , C07D417/12 , C07D231/06
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from 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.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的通式（1）的化合物及其衍生物，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，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，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，注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征肠综合征，肥胖症和2型糖尿病。

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