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1. 发明申请

US20100004459A1 2-PHENYLNICOTINIC ACID DERIVATIVE 审中-公开
标题翻译： 2-苯基丙酸衍生物
公开(公告)号：US20100004459A1
公开(公告)日：2010-01-07
申请号：US12448050
申请日：2007-12-12
申请人： Nobuo Menjo , Tomohiro Ookubo , Taisuke Hasegawa , Kazuhito Furukawa , Akihiro Fujita
发明人： Nobuo Menjo , Tomohiro Ookubo , Taisuke Hasegawa , Kazuhito Furukawa , Akihiro Fujita
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D401/10 , C07D413/10
摘要： The present invention is to provide the compounds useful as a treating or preventing agent for gout and hyperuricemia which are 2-phenylnicotinic acid derivatives having a uric acid lowering action due to an excellent xanthine oxidase inhibitory action. Since the 2-phenylnicotinic acid derivatives of the present invention exhibit a uric acid lowering action due to an excellent xanthine oxidase inhibitory action and also hypolipemic action, their utility is very high as a treating or preventive agent for gout and hyperuricemia which are often accompanied by hyperlipemia as a complication.
摘要翻译：本发明提供可用作痛风和高尿酸血症的治疗或预防剂的化合物，其是由于优异的黄嘌呤氧化酶抑制作用而具有尿酸降低作用的2-苯基烟酸衍生物。由于本发明的2-苯基烟酸衍生物由于优异的黄嘌呤氧化酶抑制作用和降血脂作用而显示出尿酸降低作用，因此其作为痛风和高尿酸血症的治疗或预防剂的效用非常高，通常伴随着高脂血症为并发症。

2. 发明授权

US5776942A Bronchodilating pyrido�2,3-d!pyrimidine derivatives 失效
标题翻译：支气管扩张吡啶并[2,3-d]嘧啶衍生物
公开(公告)号：US5776942A
公开(公告)日：1998-07-07
申请号：US490297
申请日：1995-06-14
申请人： Kazuhito Furukawa , Taisuke Hasegawa
发明人： Kazuhito Furukawa , Taisuke Hasegawa
IPC分类号： C07D471/04 , C07D239/00 , A61K31/505
CPC分类号： C07D471/04
摘要： A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido�2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action. It can be used as a therapy not only for allergic asthma but also for various bronchial asthmas such as endogenous asthma, exogenous asthma and dust asthma.
摘要翻译：具有支气管扩张作用的哮喘的快速作用补救剂包含至少一种由通式（A）表示的吡啶并[2,3-d]嘧啶衍生物或其药学上可接受的盐或金属络合物作为有效成分： A）其中R1和R2相同或不同，R1和R2各自为氢，烷基或苄基; R3是氢，羟基，二烷基氨基亚甲基氨基或-NH-X; X是氢，烷基，烯基，羟基，氨基，羟基烷基，苄基或酰基; R4是氢，烷基，卤素，硝基，氨基，羟基，苄氧基，氰基，羧基，烷氧基羰基，烷氧基磺酰基，氨基磺酰基，二烷基氨基磺酰基或磺基; R5是氢，烷基或氨基。由于支气管扩张作用优异，支气管哮喘的快速作用补救能够缓解哮喘发作时呼吸急促的症状。它不仅可用作过敏性哮喘，还可用于各种支气管哮喘，如内源性哮喘，外源性哮喘和灰尘哮喘。

3. 发明申请

US20080262230A1 Benzyloxypropylamine Derivative 有权
标题翻译：苄氧基丙胺衍生物
公开(公告)号：US20080262230A1
公开(公告)日：2008-10-23
申请号：US11887072
申请日：2006-03-29
申请人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa
发明人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa
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。

4. 发明申请

US20100004456A1 Oxepin derivative 有权
标题翻译：奥克辛衍生物
公开(公告)号：US20100004456A1
公开(公告)日：2010-01-07
申请号：US12311215
申请日：2007-09-27
申请人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa , Yuriko Yamazaki
发明人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa , Yuriko Yamazaki
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。

5. 发明授权

US08653285B2 Aminopropylidene derivative 有权
标题翻译：氨基亚丙基衍生物
公开(公告)号：US08653285B2
公开(公告)日：2014-02-18
申请号：US13055780
申请日：2009-07-31
申请人： Kunihiko Higashiura , Takashi Ogino , Taizo Ito , Koji Kunimasu , Kazuhito Furukawa
发明人： Kunihiko Higashiura , Takashi Ogino , Taizo Ito , Koji Kunimasu , Kazuhito Furukawa
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。

6. 发明授权

US08222419B2 Oxepin derivative 有权
标题翻译：奥克辛衍生物
公开(公告)号：US08222419B2
公开(公告)日：2012-07-17
申请号：US12311215
申请日：2007-09-27
申请人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa , Yuriko Yamazaki
发明人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa , Yuriko Yamazaki
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。

7. 发明申请

US20110124856A1 AMINOPROPYLIDENE DERIVATIVE 有权
标题翻译：氨基酚衍生物
公开(公告)号：US20110124856A1
公开(公告)日：2011-05-26
申请号：US13055780
申请日：2009-07-31
申请人： Kunihiko Higashiura , Takashi Ogino , Taizo Ito , Koji Kunimasu , Kazuhito Furukawa
发明人： Kunihiko Higashiura , Takashi Ogino , Taizo Ito , Koji Kunimasu , Kazuhito Furukawa
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。

8. 发明授权

US06242452B1 7-aminopyrido[2,3-D]pyrimidine derivatives 失效
标题翻译： 7-氨基吡啶并[2,3-D]嘧啶衍生物
公开(公告)号：US06242452B1
公开(公告)日：2001-06-05
申请号：US09418982
申请日：1999-10-14
申请人： Takashi Ogino , Kazuhito Furukawa
发明人： Takashi Ogino , Kazuhito Furukawa
IPC分类号： A61K31505
CPC分类号： C07D471/04
摘要： Compounds which exhibit excellent bronchodilating action with low side effects and are 7-amino-1-phenylpyrido[2,3-d]pyrimidine-2,4-dione derivatives represented by the formula (I) or a pharmaceutically acceptable salt or hydrate thereof: wherein R1 is hydrogen, lower alkenyl, phenyl or lower alkyl which is optionally substituted with a substituent selected from the following substituents(a) to (i); (a) oxo, (b) lower alkoxy, (c) phenyl which is optionally substituted with one or more lower alkyl, lower alkoxy, carboxyl, lower alkoxycarbonyl, mercapto, halogen, trifluoromethyl and/or nitro; (d) naphthyl, (e) furyl, (f) isoxazolyl which is optionally substituted with one or more lower alkyl, (g) pyridyl which is optionally substituted with one or more lower alkyl and/or halogen, (h) thienyl which is optionally substituted with halogen, and (i) 1,3-dioxolanyl; and R2, R3 and R4 each independently is hydrogen, halogen, lower alkoxy, benzyloxy, carboxyl or lower alkoxycarbonyl. The compounds of the present invention exhibit unexpectedly superior bronchodilating action, safety, and rapid transfer into the blood stream and prolonged half life in the blood stream. Accordingly, the compounds and pharmaceutical compositions containing them are useful as therapeutic agents for bronchial asthma.
摘要翻译：表现出优异的副作用的支气管扩张作用的化合物和由式（I）表示的7-氨基-1-苯基吡啶并[2,3-d]嘧啶-2,4-二酮衍生物或其药学上可接受的盐或水合物：其中R 1是氢，低级烯基，苯基或被选自以下取代基（a）至（i）中的取代基取代的低级烷基;（a）氧代，（b）低级烷氧基，（c）低级烷氧基，羧基，低级烷氧基羰基，巯基，卤素，三氟甲基和/或硝基取代;（d）萘基，（e）呋喃基，（f）异唑基，其任选被一个或多个低级烷基，（g）任选被一个或多个低级烷基和/或卤素取代的吡啶基，（h）任选被卤素取代的噻吩基，和（i）1,3-二氧戊环基; R 2，R 3和R 4各自独立地为氢，卤素，低级烷氧基，苄氧基，羧基或低级烷氧基羰基。本发明的化合物显示出意想不到的优异的支气管扩张作用，安全性和快速转移到血液中并延长血液中的半衰期。因此，含有它们的化合物和药物组合物可用作支气管哮喘的治疗剂。

9. 发明授权

US07939552B2 Benzyloxypropylamine derivative 有权
标题翻译：苄氧基丙胺衍生物
公开(公告)号：US07939552B2
公开(公告)日：2011-05-10
申请号：US11887072
申请日：2006-03-29
申请人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa
发明人： Kunihiko Higashiura , Takashi Ogino , Kazuhito Furukawa
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。

10. 发明授权

US06906074B2 2-phenylpiperazine derivatives 失效
标题翻译： 2-苯基哌嗪衍生物
公开(公告)号：US06906074B2
公开(公告)日：2005-06-14
申请号：US10370918
申请日：2003-02-20
申请人： Takashi Ogino , Yukari Konishi , Kunihiko Higashiura , Kazuhito Furukawa
发明人： Takashi Ogino , Yukari Konishi , Kunihiko Higashiura , Kazuhito Furukawa
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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