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1. 发明授权

US08642777B2 Process for producing 3-alkoxy-2-amino-6-fluorobicyclo [3.1.0] hexane-2,6-dicarboxylic acid derivative and intermediate thereof 有权
标题翻译： 3-烷氧基-2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物及其中间体的制备方法
公开(公告)号：US08642777B2
公开(公告)日：2014-02-04
申请号：US13510428
申请日：2010-11-18
申请人： Noriaki Murase , Toshihito Kumagai , Hisaya Wada , Hisahide Tanimoto , Koumei Ohta , Yoshihiro Kimura
发明人： Noriaki Murase , Toshihito Kumagai , Hisaya Wada , Hisahide Tanimoto , Koumei Ohta , Yoshihiro Kimura
IPC分类号： C07D293/00
CPC分类号： C07D235/02 , C07C51/08 , C07C67/31 , C07C67/313 , C07C69/757 , C07C227/02 , C07C229/50 , C07C235/82 , C07C237/24 , C07C255/47 , C07C2602/18 , C07F7/1804
摘要： A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
摘要翻译：一种制备由式（I）表示的3-烷氧基-2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物或其盐的方法，其包括将式式（VI）所示的化合物或其盐与式（I）表示的化合物或其盐。

2. 发明申请

US20120238763A1 PROCESS FOR PRODUCING 3-ALKOXY-2-AMINO-6-FLUOROBICYCLO [3.1.0] HEXANE-2,6-DICARBOXYLIC ACID DERIVATIVE AND INTERMEDIATE THEREOF 有权
标题翻译：制备3-烷氧基-2-氨基-6-氟代羰基的方法[3.1.0] HEXANE-2,6-二羧酸衍生物及其中间体
公开(公告)号：US20120238763A1
公开(公告)日：2012-09-20
申请号：US13510428
申请日：2010-11-18
申请人： Noriaki Murase , Toshihito Kumagai , Hisaya Wada , Hisahide Tanimoto , Koumei Ohta , Yoshihiro Kimura
发明人： Noriaki Murase , Toshihito Kumagai , Hisaya Wada , Hisahide Tanimoto , Koumei Ohta , Yoshihiro Kimura
IPC分类号： C07C51/08 , C07C69/78 , C07F7/18 , C07D235/02 , C07C255/47 , C07C237/24 , C07C51/06 , C07C69/757 , C07C235/82
CPC分类号： C07D235/02 , C07C51/08 , C07C67/31 , C07C67/313 , C07C69/757 , C07C227/02 , C07C229/50 , C07C235/82 , C07C237/24 , C07C255/47 , C07C2602/18 , C07F7/1804
摘要： A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
摘要翻译：一种制备由式（I）表示的3-烷氧基-2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物或其盐的方法，其包括将式式（VI）所示的化合物或其盐与式（I）表示的化合物或其盐。

3. 发明授权

US5990151A Optically active substituted phenylalkylamine derivatives 失效
标题翻译：光学活性取代苯基烷基胺衍生物
公开(公告)号：US5990151A
公开(公告)日：1999-11-23
申请号：US981539
申请日：1998-05-15
申请人： Atsuro Nakazato , Toshihito Kumagai , Tomoki Miyazawa , Koumei Ohta , Yutaka Kawashima , Katsuo Hatayama, deceased
发明人： Atsuro Nakazato , Toshihito Kumagai , Tomoki Miyazawa , Koumei Ohta , Yutaka Kawashima , Katsuo Hatayama, deceased
IPC分类号： C07C217/60 , C07C217/62 , C07C271/16 , C07D333/16 , A61K31/135 , A61K31/38 , C07D333/06
CPC分类号： C07C271/16 , C07C217/60 , C07C217/62 , C07D333/16
摘要： The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases. Further, the compound of the invention is also useful for treating dependence resulted from drug abuse.
摘要翻译： PCT No.PCT / JP96 / 01613 Sec。 371日期：1998年5月15日 102（e）日期1998年5月15日PCT提交1996年6月13日PCT公布。出版物WO97 / 00238 日本1997年1月3日本发明涉及由式[1]表示的光学活性的取代的苯基烷基胺衍生物：其中A是取代或未取代的苯基或噻吩基; X 1为氢，卤素，羟基或取代或未取代的C 1-5烷氧基; R1和R2同等或不同，氢，C1-7烷基，C3-7烯基或C3-7炔基; R3是C1-10烷基，C2-10烯基或C2-10炔基; n是2至5的整数; m为1〜4的整数，或其药学上可接受的盐，以及该化合物或其盐的药物用途。本发明化合物在σ1受体拮抗作用方面优异，可用于治疗精神分裂症，抑郁症，焦虑症，脑血管疾病/老年麻醉行为，以及认知功能障碍和运动功能障碍如阿尔茨海默氏病，帕金森病和亨廷顿舞蹈病，这些疾病均为神经变性疾病。此外，本发明的化合物还可用于治疗药物滥用引起的依赖性。

4. 发明授权

US06894168B2 Carbamoyl tetrahydropyridine derivatives 失效
标题翻译：氨基甲酰四氢吡啶衍生物
公开(公告)号：US06894168B2
公开(公告)日：2005-05-17
申请号：US10347288
申请日：2003-01-21
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
IPC分类号： A61K31/519 , A61P1/00 , A61P7/10 , A61P9/10 , A61P9/12 , A61P17/02 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D473/00 , C07D487/04 , C07D211/78
CPC分类号： A61K31/519 , C07D473/00 , C07D487/04
摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7) N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译：由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1，R 2和R 2'相同或不同，各自表示氢原子，C 1 C 5 -C 15烷基等; Y 1 - （CH 2）2（R 4 S）（R 5），（R 6） CN，NN，（R 7）N-CO或NC（R 8）; X 1，X 2和X 3相同或不同，各自表示氢原子，卤素原子等; R 3，R 4，R 5和R 6相同或不同，并且各自表示氢原子或烷基; R 7表示氢原子，C 1 -C 5烷基等; 和R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐，以及其制备中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

5. 发明授权

US06852732B2 Tetrahydropyridino or piperidino heterocylic derivatives 失效
标题翻译：四氢吡啶基或哌啶子杂环衍生物
公开(公告)号：US06852732B2
公开(公告)日：2005-02-08
申请号：US10311277
申请日：2001-07-04
申请人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
发明人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
IPC分类号： A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/14 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A01N43/42
CPC分类号： C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I] has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：由式[I]表示的四氢吡啶基或哌啶子基杂环衍生物对CRF受体具有高亲和力，并且对于被认为涉及CRF的疾病有效。

6. 发明申请

US20050009874A1 Tetrahydropyridin or piperidino heterocyclic derivatives 失效
标题翻译：四氢吡啶或哌啶子基杂环衍生物
公开(公告)号：US20050009874A1
公开(公告)日：2005-01-13
申请号：US10912185
申请日：2004-08-06
申请人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
发明人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
IPC分类号： A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/14 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/454 , C07
CPC分类号： C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I]has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：由式[I]表示的四氢吡啶基或哌啶子基杂环衍生物：A-Het [I]对CRF受体具有高亲和力，并且对于CRF被认为涉及的疾病有效。

7. 发明授权

US06770676B2 Dicarboxylic acid derivatives 失效
标题翻译：二羧酸衍生物
公开(公告)号：US06770676B2
公开(公告)日：2004-08-03
申请号：US10297479
申请日：2002-12-06
申请人： Atsuro Nakazato , Toshihito Kumagai , Kosuke Kanuma , Kazunari Sakagami
发明人： Atsuro Nakazato , Toshihito Kumagai , Kosuke Kanuma , Kazunari Sakagami
IPC分类号： C07C6113
CPC分类号： C07C229/50 , C07C2602/18
摘要： The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.
摘要翻译：本发明涉及由下式表示的2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物或其药学上可接受的盐或其水合物。本发明的化合物可用作药物，特别是可用作作用于组2代谢型谷氨酸受体的调节剂，具有治疗和/或预防精神病学障碍如精神分裂症，焦虑及其相关疾病，抑郁症，双相障碍和癫痫; 和/或神经系统疾病如药物依赖性，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森病，与肌肉僵硬相关的运动障碍，脑缺血，脑衰竭，脊髓病和头部创伤。

8. 发明授权

US08044068B2 Aminopyrrolidine compound 失效
标题翻译：氨基吡咯烷化合物
公开(公告)号：US08044068B2
公开(公告)日：2011-10-25
申请号：US12296082
申请日：2007-03-30
申请人： Taketoshi Okubo , Toshihito Kumagai , Takaaki Ishii , Toshio Nakamura , Kumi Abe , Yuri Amada , Tomoko Ishizaka , Xiang-Min Sun , Yoshinori Sekiguchi , Shigetada Sasako , Takanori Shimizu , Takayuki Nagatsuka
发明人： Taketoshi Okubo , Toshihito Kumagai , Takaaki Ishii , Toshio Nakamura , Kumi Abe , Yuri Amada , Tomoko Ishizaka , Xiang-Min Sun , Yoshinori Sekiguchi , Shigetada Sasako , Takanori Shimizu , Takayuki Nagatsuka
IPC分类号： A61K31/47 , C07D453/04
CPC分类号： C07D401/12
摘要： Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.
摘要翻译：公开了由式[I]表示的氨基吡咯烷化合物或其药学上可接受的盐。化合物或盐可用作模式障碍如抑郁症，焦虑障碍，厌食症，恶病质，疼痛和药物依赖性的预防/治疗剂，其作用依赖于MC4受体拮抗作用。

9. 发明授权

US06600038B1 Carbamoyl tetrahydropyridine derivatives 失效
标题翻译：氨基甲酰四氢吡啶衍生物
公开(公告)号：US06600038B1
公开(公告)日：2003-07-29
申请号：US09914534
申请日：2001-08-30
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
IPC分类号： C07D47334
CPC分类号： A61K31/519 , C07D473/00 , C07D487/04
摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译：由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1和R 2相同或不同，各自表示氢原子，C 1 -C 5烷基等; Y1-Y2表示（R4）C = C（R5），（R6）C = N，N = N，（R7）N-CO或N = C（R8） X1，X2和X3相同或不同，各自表示氢原子，卤素原子等; R3，R4，R5和R6相同或不同，各自表示氢原子或烷基; R7表示氢原子，C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐，并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

10. 发明授权

US06380384B1 1,2-dihydro-2-oxoquinoline derivatives 失效
标题翻译： 1,2-二氢-2-氧代喹啉衍生物
公开(公告)号：US06380384B1
公开(公告)日：2002-04-30
申请号：US09829203
申请日：2001-04-10
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D215/54 , C07D241/44
摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar是吡啶基或由下式表示的基团：（其中X 3和X 4相同或不同，并且各自为氢原子，卤素原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y是氮原子，CH或C（OH），R 1和R 2相同或不同，各自相同或不同氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X 1和X 2是相同或不同，并且各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子; 或者X1和X2一起形成亚烷基二氧基，n为1〜3的整数。或其药学上可接受的盐。

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