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公开(公告)号：US06906074B2
公开(公告)日：2005-06-14
申请号：US10370918
申请日：2003-02-20
IPC分类号： A61P29/00 , C07D241/04 , C07D241/08 , C07D401/06 , C07D403/04 , C07D403/06 , A61K31/50 , A61K31/501
CPC分类号： C07D401/06 , C07D241/04 , C07D241/08 , C07D403/04 , C07D403/06
摘要： A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl , mesyl, t-butoxycarbonyl, or a lower alkyl which may be optionally substituted, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. The derivative may be used as a tachykinin antagonist in the treatment of diseases of the digestive system, nervous system and respiratory system, inflammation, allergy, carcinoid syndrome, chronic pain, headache, Crohn disease, depression and vomiting.
摘要翻译： 由式（I）表示的2-苯基哌嗪衍生物或其药学上可接受的盐，水合物或络合物：其中X 1和X 3中的每一个为氧或两个 氢原子，X 2 O，NH，NCH 3或CH 2，n是0或1的整数，R 1， R 1是氢或低级烷基，R 2是氢，氰基，四唑基，氨基三唑基，甲磺酰基，叔丁氧基羰基或可任意取代的低级烷基，R 3 R 4和R 5中的每一个是氢，低级烷氧基或三氟甲基，虚线表示一个 单键或双键。 该衍生物可用作速激肽拮抗剂治疗消化系统疾病，神经系统和呼吸系统，炎症，变态反应，类癌综合征，慢性疼痛，头痛，克罗恩病，抑郁症和呕吐。
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公开(公告)号：US20100004456A1
公开(公告)日：2010-01-07
申请号：US12311215
申请日：2007-09-27
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
摘要翻译： 本发明提供一种化合物，具有优异的组胺受体拮抗作用的氧杂环丁衍生物，其可用作抗组胺药。 本发明的oxepin衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使经口给予该化合物的小鼠进行脑内受体结合试验，也显示低脑内迁移，使得该化合物具有优选的减轻中枢神经系统副作用的性质，例如 作为嗜睡 本发明的oxepin衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药如睡意觉是非常有用的。
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公开(公告)号：US08653285B2
公开(公告)日：2014-02-18
申请号：US13055780
申请日：2009-07-31
IPC分类号： C07D313/08 , C07D333/50 , A61K31/38 , A61K31/335
CPC分类号： C07D495/04 , C07D333/78
摘要： An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
摘要翻译： 描述了具有优异的组胺受体拮抗作用的氨基亚丙基衍生物，可用作药物组合物的化合物，特别是作为活性成分，在中枢神经系统中具有缓解的副作用。 在氨基亚丙基衍生物中，R 1和R 2可以相同或不同，代表氢，取代的羰基，取代的羰基烷基和丙烯酸，不包括两者均为氢的情况; R3和R4可以相同或不同，代表氢，可被苯基取代的烷基等; A代表未取代或氧代; B代表碳或氧; X和Y中的一个代表碳，另一个代表硫，虚线部分代表单键或双键，波浪线代表顺式和/或反式。
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公开(公告)号：US08222419B2
公开(公告)日：2012-07-17
申请号：US12311215
申请日：2007-09-27
IPC分类号： C07D401/00
CPC分类号： C07D405/04
摘要： The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
摘要翻译： 本发明提供一种化合物，具有优异的组胺受体拮抗作用的氧杂环丁衍生物，其可用作抗组胺药。 本发明的oxepin衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使经口给予该化合物的小鼠进行脑内受体结合试验，也显示低脑内迁移，使得该化合物具有优选的减轻中枢神经系统副作用的性质，例如 作为嗜睡 本发明的oxepin衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药如睡意觉是非常有用的。
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公开(公告)号：US20110124856A1
公开(公告)日：2011-05-26
申请号：US13055780
申请日：2009-07-31
IPC分类号： C07D279/12 , C07C211/32 , C07D209/56 , C07C57/50 , C07D265/30 , C07D211/08
CPC分类号： C07D495/04 , C07D333/78
摘要： An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
摘要翻译： 描述了具有优异的组胺受体拮抗作用的氨基亚丙基衍生物，可用作药物组合物的化合物，特别是作为活性成分，在中枢神经系统中具有缓解的副作用。 在氨基亚丙基衍生物中，R 1和R 2可以相同或不同，代表氢，取代的羰基，取代的羰基烷基和丙烯酸，不包括两者均为氢的情况; R3和R4可以相同或不同，代表氢，可被苯基取代的烷基等; A代表未取代或氧代; B代表碳或氧; X和Y中的一个代表碳，另一个代表硫，虚线部分代表单键或双键，波浪线代表顺式和/或反式。
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公开(公告)号：US20080262230A1
公开(公告)日：2008-10-23
申请号：US11887072
申请日：2006-03-29
IPC分类号： C07D241/06 , C07D211/32 , C07D211/82 , C07D215/14 , C07C211/27 , C07D317/26 , C07D207/333
CPC分类号： C07D317/22 , C07C233/18 , C07C233/73 , C07C235/48 , C07C237/08 , C07C237/24 , C07C237/32 , C07C271/16 , C07C271/22 , C07C271/24 , C07C271/28 , C07C271/48 , C07C2601/14 , C07D207/06 , C07D211/14 , C07D211/62 , C07D213/20 , C07D213/56 , C07D213/89 , C07D215/50 , C07D241/24
摘要： Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.
摘要翻译： 公开了一种具有优异的速激肽受体拮抗作用的新型苄氧基丙胺衍生物。 该化合物在使用豚鼠口服给予该化合物的血液动力学试验中表现出良好的血液转运和长血半衰期，并且在动物血浆中稳定。 当以一定剂量口服给豚鼠时，该化合物还显示出对中枢神经系统的高转移。 因此，苄氧基丙胺衍生物作为新的抗速激肽剂非常有用。
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公开(公告)号：US07939552B2
公开(公告)日：2011-05-10
申请号：US11887072
申请日：2006-03-29
IPC分类号： A61K31/445 , A61K31/165 , A61K31/44 , C07D213/81 , C07D211/30 , C07D211/82 , C07C233/00
CPC分类号： C07D317/22 , C07C233/18 , C07C233/73 , C07C235/48 , C07C237/08 , C07C237/24 , C07C237/32 , C07C271/16 , C07C271/22 , C07C271/24 , C07C271/28 , C07C271/48 , C07C2601/14 , C07D207/06 , C07D211/14 , C07D211/62 , C07D213/20 , C07D213/56 , C07D213/89 , C07D215/50 , C07D241/24
摘要： Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.
摘要翻译： 公开了一种具有优异的速激肽受体拮抗作用的新型苄氧基丙胺衍生物。 该化合物在使用豚鼠口服给予该化合物的血液动力学试验中表现出良好的血液转运和长血半衰期，并且在动物血浆中稳定。 当以一定剂量口服给豚鼠时，该化合物还显示出对中枢神经系统的高转移。 因此，苄氧基丙胺衍生物作为新的抗速激肽剂非常有用。
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公开(公告)号：US08377967B2
公开(公告)日：2013-02-19
申请号：US12864878
申请日：2008-11-20
IPC分类号： A61K31/4535 , C07D409/02 , A61P37/08
CPC分类号： C07D495/04 , C07D409/04 , C07D497/04
摘要： The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
摘要翻译： 本发明提供了具有优异的组胺受体拮抗作用的化合物哌啶衍生物，其可用作药物组合物，特别是抗组胺药的活性成分。 本发明的哌啶衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使在小鼠口服给药化合物的脑受体结合试验中也显示低脑转移，因此该化合物具有减轻中枢神经系统中的副作用的优选性质，例如嗜睡。 本发明的哌啶衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药例如嗜睡是非常有用的。
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公开(公告)号：US20100331365A1
公开(公告)日：2010-12-30
申请号：US12864878
申请日：2008-11-20
IPC分类号： A61K31/4535 , C07D409/02 , A61P37/08
CPC分类号： C07D495/04 , C07D409/04 , C07D497/04
摘要： The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.
摘要翻译： 本发明提供了具有优异的组胺受体拮抗作用的化合物哌啶衍生物，其可用作药物组合物，特别是抗组胺药的活性成分。 本发明的哌啶衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使在小鼠口服给药化合物的脑受体结合试验中也显示低脑转移，因此该化合物具有减轻中枢神经系统中的副作用的优选性质，例如嗜睡。 本发明的哌啶衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药例如嗜睡是非常有用的。
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公开(公告)号：US20120123127A1
公开(公告)日：2012-05-17
申请号：US13383441
申请日：2010-07-26
IPC分类号： C07D409/08
CPC分类号： C07D409/04
摘要： Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
摘要翻译： 公开了可用作抗组胺剂等的有效成分的噻哆烷 - 丙酸衍生物的制造方法。 根据本发明的制造方法，可以制备噻吩并薁类骨架的2位用丙酸取代的噻吩并薁 - 丙酸衍生物。 由此合成的硫代苯并薁丙酸衍生物对组胺H1受体和低脑内转移具有优异的拮抗作用，因此可用作药物组合物如抗组胺剂的活性成分。
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