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1. 发明授权

US08951997B2 Substituted isoquinoline derivative 有权
标题翻译：取代的异喹啉衍生物
公开(公告)号：US08951997B2
公开(公告)日：2015-02-10
申请号：US13265246
申请日：2010-06-18
申请人： Hiroyoshi Hidaka , Kouichi Takahashi , Yoshihiro Inoue , Kengo Sumi , Ryohei Nakamura
发明人： Hiroyoshi Hidaka , Kouichi Takahashi , Yoshihiro Inoue , Kengo Sumi , Ryohei Nakamura
IPC分类号： C07D403/12 , A61K31/47 , A61K31/551 , A61K31/407 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D217/02 , C07D401/12 , C07D487/08
CPC分类号： A61K31/407 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D217/02 , C07D401/12 , C07D487/08
摘要： The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH═CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.
摘要翻译：本发明提供可用作新型药剂的异喹啉-6-磺酰胺衍生物。本发明提供由式（1）表示的异喹啉-6-磺酰胺衍生物，其盐或其衍生物或盐的溶剂合物：其中X和Y各自独立地表示直接键，NH，CH = CH，O ，或S; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，烷基等; R 3和R 4各自独立地表示氢原子，烷基等，或者R 3和R 4一起形成可以在两个碳原子之间桥接到任意位置的亚烷基或亚烯基; l，m和n表示1〜4的整数。

2. 发明授权

US08883792B2 Substituted isoquinoline derivative 有权
标题翻译：取代的异喹啉衍生物
公开(公告)号：US08883792B2
公开(公告)日：2014-11-11
申请号：US13995300
申请日：2011-12-21
申请人： Hiroyoshi Hidaka , Kengo Sumi , Kouichi Takahashi , Yoshihiro Inoue
发明人： Hiroyoshi Hidaka , Kengo Sumi , Kouichi Takahashi , Yoshihiro Inoue
IPC分类号： C07D401/12 , C07D217/04 , A61K31/4725 , C07D217/02 , C07D417/12 , C07D405/12 , C07D409/12 , C07D217/22
CPC分类号： C07D217/04 , C07D217/02 , C07D217/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.
摘要翻译：本发明提供了可用作药物的新型异喹啉-6-磺酰胺衍生物。本发明提供由式（1）表示的异喹啉-6-磺酰胺衍生物，其盐或衍生物或其盐的溶剂合物，其中R1和R2各自独立地表示氢原子等; R3和R4各自独立地表示氢原子，烷基等; R5表示氢原子，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的环烷基，任选取代的烷酰基等; A表示碳原子数2〜6的直链或支链亚烷基。

3. 发明申请

US20120035159A1 SUBSTITUTED ISOQUINOLINE DERIVATIVE 有权
标题翻译：取代的异喹啉衍生物
公开(公告)号：US20120035159A1
公开(公告)日：2012-02-09
申请号：US13265246
申请日：2010-06-18
申请人： Hiroyoshi Hidaka , Kouichi Takahashi , Yoshihiro Inoue , Kengo Sumi , Ryohei Nakamura
发明人： Hiroyoshi Hidaka , Kouichi Takahashi , Yoshihiro Inoue , Kengo Sumi , Ryohei Nakamura
IPC分类号： A61K31/551 , C07D217/04 , A61K31/4709 , C07D245/02 , C07D413/12 , A61P25/28 , C07D401/12 , A61K31/497 , C07D255/00 , A61P27/06 , A61P9/00 , C07D243/08 , A61K31/5377
CPC分类号： A61K31/407 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D217/02 , C07D401/12 , C07D487/08
摘要： The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH═CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.
摘要翻译：本发明提供可用作新型药剂的异喹啉-6-磺酰胺衍生物。本发明提供由式（1）表示的异喹啉-6-磺酰胺衍生物，其盐或其衍生物或盐的溶剂合物：其中X和Y各自独立地表示直接键，NH，CH = CH，O ，或S; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，烷基等; R 3和R 4各自独立地表示氢原子，烷基等，或者R 3和R 4一起形成可以在两个碳原子之间桥接到任意位置的亚烷基或亚烯基; l，m和n表示1〜4的整数。

4. 发明申请

US20130274269A1 NOVEL SUBSTITUTED ISOQUINOLINE DERIVATIVE 有权
标题翻译：新型取代的异喹啉衍生物
公开(公告)号：US20130274269A1
公开(公告)日：2013-10-17
申请号：US13995300
申请日：2011-12-21
申请人： Hiroyoshi Hidaka , Kengo Sumi , Kouichi Takahashi , Yoshihiro Inoue
发明人： Hiroyoshi Hidaka , Kengo Sumi , Kouichi Takahashi , Yoshihiro Inoue
IPC分类号： C07D217/04 , C07D405/12 , C07D417/12 , C07D401/12
CPC分类号： C07D217/04 , C07D217/02 , C07D217/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.
摘要翻译：本发明提供了可用作药物的新型异喹啉-6-磺酰胺衍生物。本发明提供由式（1）表示的异喹啉-6-磺酰胺衍生物，其盐或衍生物或其盐的溶剂合物，其中R1和R2各自独立地表示氢原子等; R3和R4各自独立地表示氢原子，烷基等; R5表示氢原子，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的环烷基，任选取代的烷酰基等; A表示碳原子数2〜6的直链或支链亚烷基。

5. 发明申请

US20080064681A1 Therapeutic agent for treating glaucoma 审中-公开
标题翻译：用于治疗青光眼的治疗剂
公开(公告)号：US20080064681A1
公开(公告)日：2008-03-13
申请号：US11518131
申请日：2006-09-11
申请人： Hiroyoshi Hidaka , Masahiro Nishio , Kengo Sumi
发明人： Hiroyoshi Hidaka , Masahiro Nishio , Kengo Sumi
IPC分类号： A61K31/551 , A61K31/496 , A61K31/4709
CPC分类号： A61K31/4709 , A61K31/496 , A61K31/551
摘要： The present invention provides compounds useful as therapeutic agent for treating glaucoma and methods for treating glaucoma. That is, a therapeutic agent for treating glaucoma containing, as an active ingredient, a compound represented by formula (1) below is synthesized, and the therapeutic agent is administered in the form of eye drops to a glaucoma patient. Thus, the intraocular pressure is reduced. In the above formula, ring A represents a 5- to 11-membered cyclic amino group, which may have a substituted group, and X represents a halogen.
摘要翻译：本发明提供可用作治疗青光眼的治疗剂的化合物和治疗青光眼的方法。也就是说，合成用于治疗青光眼的治疗剂，其含有作为活性成分的下述式（1）表示的化合物，并且所述治疗剂以眼药水的形式给予青光眼患者。因此，眼压降低。在上式中，环A表示可以具有取代基的5至11元环氨基，X表示卤素。

6. 发明授权

US6143763A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US6143763A
公开(公告)日：2000-11-07
申请号：US849664
申请日：1997-05-29
申请人： Yasuo Koga , Yoshito Kihara , Minoru Okada , Takao Nishi , Yoshihiro Inoue , Yukio Kimura , Hiroyoshi Hidaka , Norio Fukuda
发明人： Yasuo Koga , Yoshito Kihara , Minoru Okada , Takao Nishi , Yoshihiro Inoue , Yukio Kimura , Hiroyoshi Hidaka , Norio Fukuda
IPC分类号： C07D215/22 , C07D215/227 , A61K31/4704
CPC分类号： C07D215/227
摘要： A carbostyril derivative of the formula (1): ##STR1## wherein A is lower alkylene, R is H, halogen or lower alkoxy, R.sup.1 and R.sup.2 are each lower alkyl being optionally substituted by OH, lower alkoxy, phenyl-lower alkoxy or lower alkanoyloxy; cycloalkyl being optionally substituted by OH, hydroxy-lower alkoxy or lower alkanoyloxy; or amino being optionally substituted by lower alkyl or cycloalkyl, R.sup.3 is H, lower alkyl, lower alkenyl or hydroxy-lower alkyl, and the bond between 3- and 4-positions of the carbostyril nucleus is single or double, provided that when R and R.sup.3 are H, R.sup.1 and R.sup.2 should not be either unsubstituted lower alkyl or unsubstituted cycloalkyl, or a salt thereof, which shows antithrombotic activities, intima thickening inhibitory activity, the platelet mass dissociating activity and increasing activity of the blood flow in the brain and the peripheral vessel, and hence, is useful as medicines in the prophylaxis or treatment of various ischemic diseases.
摘要翻译： PCT No.PCT / JP96 / 02892 Sec。 371日期：1998年5月29日 102（e）日期1998年5月29日PCT提交1996年10月4日PCT公布。公开号WO97 / 12869 日期：1997年04月10日式（1）的喹诺酮衍生物：其中A为低级亚烷基，R为H，卤素或低级烷氧基，R1和R2各自为低级烷基，任选被OH，低级烷氧基，苯基 - 低级烷氧基或低级烷酰氧基; 任选被OH，羟基 - 低级烷氧基或低级烷酰氧基取代的环烷基; 或氨基任选被低级烷基或环烷基取代，R 3是H，低级烷基，低级烯基或羟基 - 低级烷基，并且喹诺酮环的3-和4-位之间的键是单或双，条件是当R和 R3是H，R1和R2不应该是未取代的低级烷基或未取代的环烷基或其盐，其显示抗血栓形成活性，内膜增厚抑制活性，血小板质量分解活性和增加脑中血流的活性，外周血管，因此可用作预防或治疗各种缺血性疾病的药物。

7. 发明授权

US5972976A Aminostilbazole derivative and medicine 失效
标题翻译：氨基芪衍生物和药物
公开(公告)号：US5972976A
公开(公告)日：1999-10-26
申请号：US765131
申请日：1996-10-02
申请人： Hiroyoshi Hidaka , Akira Matsuura , Masato Matsuda
发明人： Hiroyoshi Hidaka , Akira Matsuura , Masato Matsuda
IPC分类号： C07D213/74 , A61K9/20 , A61K31/44 , A61K31/4427 , A61K31/53 , A61P35/00 , C07D213/42 , C07D213/76 , C07D213/89 , C07D239/26 , C07D239/28 , C07D241/12 , C07D241/14 , C07D401/06 , C07D405/06 , C07D413/00 , C07D211/72 , C07D213/36 , C07D241/02
CPC分类号： C07D213/42 , A61K31/44 , C07D213/76 , C07D213/89 , C07D239/26 , C07D241/12 , C07D405/06
摘要： The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. ##STR1## wherein R.sup.1 and R.sup.2 each represents hydrogen etc.; R.sup.3, R.sup.4, R.sup.13, and R.sup.14 each represents hydrogen, C.sub.1-3 acyl, halogen, hydroxy etc.; R.sup.5 represents hydrogen or hydroxy-substituted C.sub.1-3 alkyl etc.; R.sup.6 represents benzenesulfonyl substituted by C.sub.1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.
摘要翻译： PCT No.PCT / JP95 / 00658 Sec。 371日期1996年10月2日第 102（e）日期1996年10月2日PCT提交1995年4月5日PCT公布。公开号WO95 / 27699 日期：1995年10月19日本发明涉及下式的氨基芪衍生物或其水合物及其盐。其中R1和R2各自表示氢等; R3，R4，R13和R14各自表示氢，C1-3酰基，卤素，羟基等; R5表示氢或羟基取代的C1-3烷基等; R6表示被C 1-3烷氧基取代的苯磺酰基等。环Y表示苯基等。环Z表示4-吡啶基，其氧化物等。该化合物可用于或治疗各种恶性肿瘤。

8. 发明授权

US4510307A 6-Quinazolinesulfonyl derivatives and process for preparation thereof 失效
标题翻译： 6-喹唑啉磺酰基衍生物及其制备方法
公开(公告)号：US4510307A
公开(公告)日：1985-04-09
申请号：US293192
申请日：1981-08-17
申请人： Hiroyoshi Hidaka , Takanori Sone , Yasuharu Sasaki , Taisuke Sugihara , Seiji Takagi , Kiyohide Sako
发明人： Hiroyoshi Hidaka , Takanori Sone , Yasuharu Sasaki , Taisuke Sugihara , Seiji Takagi , Kiyohide Sako
IPC分类号： C07D239/86 , C07D239/88 , C07D239/94 , C07D265/00 , C07D247/00 , C07D403/00
CPC分类号： C07D239/94 , C07D239/86 , C07D239/88 , Y10S514/929
摘要： A 6-quinazolinesulfonyl derivative of Formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1-12 alkyl group:R.sub.2 is a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.4-10 cycloalkyl group, an aryl group or an aralkyl group; andR.sub.1 and R.sub.2 may be linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring together with the adjacent nitrogen atom; andR.sub.3 is a ##STR2## group wherein R.sub.4 is a C.sub.1-8 alkyl group; a --HN(CH.sub.2).sub.n NH.sub.2 group wherein n is an integer of 2 to 10; or a ##STR3## group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
摘要翻译：式（I）的6-喹唑啉磺酰基衍生物：其中R1是氢原子或C1-12烷基：R2是氢原子，C1-12烷基，C4-10环烷基，芳基或芳烷基; R1和R2可以直接或通过氧原子连接，与相邻的氮原子一起形成5-至7-元杂环; 并且R 3是一个基团，其中R 4是C 1-8烷基; 其中n为2〜10的整数的-HN（CH 2）n NH 2基; 或组及其药学上可接受的盐; 及其制备方法。本发明的化合物对于血管平滑肌具有松弛作用，并且可用作血管扩张剂和低血压。

9. 发明授权

US4125730A Preparation of -aminoalkanoic acid arylamides 失效
标题翻译：氨基链烷酸芳基酰胺的制备
公开(公告)号：US4125730A
公开(公告)日：1978-11-14
申请号：US621408
申请日：1975-10-10
申请人： Hiroyoshi Hidaka , Ikuo Matsumoto , Yoshiaki Ito , Nobuo Aoki
发明人： Hiroyoshi Hidaka , Ikuo Matsumoto , Yoshiaki Ito , Nobuo Aoki
IPC分类号： A61K31/16 , A61K31/165 , A61K31/245 , A61P7/02 , C07C20060101 , C07C67/00 , C07C69/78 , C07C231/00 , C07C231/02 , C07C237/04 , C07C237/22 , C07C103/50
CPC分类号： C07D221/24 , Y10S514/822
摘要： .omega.-Aminoalkanoic acid arylamides having the formula:R'(CH.sub.2).sub.n CONHRwherein R represents phenyl or naphthyl which can be substituted by halogen, nitro, alkyl, alkoxy, hydroxyl, acetoamino or alkoxycarbonyl; R' represents amino or acylated amino; and n is an integer of 4-8, exhibit blood platelet aggregation inhibiting effects.
摘要翻译： ω-氨基链烷酸芳基酰胺，其具有下式：

10. 发明授权

US07858615B2 (S)-(-)-1-(4-fluoroisoquinolin-5-Yl)Sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate 有权
标题翻译：（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物
公开(公告)号：US07858615B2
公开(公告)日：2010-12-28
申请号：US11720288
申请日：2005-11-29
申请人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
发明人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
IPC分类号： A61P9/10 , A61K31/551 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
摘要翻译：本发明涉及（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物，生产二水合物的方法和药物含有二水合物的组合物。与（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐无水晶体相比，本发明的化合物具有较少的吸湿性，化学稳定性。

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