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21. 发明授权

US5683710A Percutaneous absorption preparation 失效
标题翻译：经皮吸收制剂
公开(公告)号：US5683710A
公开(公告)日：1997-11-04
申请号：US527535
申请日：1995-09-13
申请人： Hitoshi Akemi , Takateru Muraoka , Kazuhiro Higashio , Saburo Otsuka , Takashi Kinoshita
发明人： Hitoshi Akemi , Takateru Muraoka , Kazuhiro Higashio , Saburo Otsuka , Takashi Kinoshita
IPC分类号： A61K9/70 , A61K31/34 , A61K47/14 , A61P9/08 , A61P9/10 , A61F13/02
CPC分类号： A61K9/7061 , A61K31/34
摘要： A percutaneous absorption preparation for use in the administration of isosorbide dinitrate (ISDN) as a coronary vasodilator into the living body by percutaneous absorption, which has excellent adhesion to the skin and does not cause pain and damage to stratum corneum when peeled off, is disclosed. The pressure-sensitive adhesive layer comprises an acrylic copolymer prepared by copolymerization of a monomer mixture comprising a (meth)acrylic acid alkyl ester and a functional monomer as the essential components, a fatty acid ester having a specified number of carbon atoms, a monoglyceride having a specified number of carbon atoms, and ISDN, and the pressure-sensitive adhesive layer is crosslinked. Since its skin adhesive property is improved by the inclusion of the monoglyceride, release of ISDN is improved and the area of the preparation can be decreased.
摘要翻译：公开了一种用于通过经皮吸收将硝酸异山梨酯（ISDN）作为冠状血管扩张剂施用于生物体的经皮吸收制剂，其对皮肤具有优异的粘附性，并且在剥离时不引起疼痛和对角质层的损伤。压敏粘合剂层包含通过将包含（甲基）丙烯酸烷基酯和官能单体作为主要组分的单体混合物，具有特定碳原子数的脂肪酸酯，具有特定碳原子数的单酸酯酯，特定数量的碳原子和ISDN，并且压敏粘合剂层交联。由于通过包含单酸甘油酯改善其皮肤粘合性，因此改善了ISDN的释放，并且可以减少制剂的面积。

22. 发明授权

US5459254A Process for preparing synthetic intermediates of 2-alkynyladenosines and 2-alkynyladenosines 失效
标题翻译：制备2-炔基腺苷和2-炔基腺苷合成中间体的方法
公开(公告)号：US5459254A
公开(公告)日：1995-10-17
申请号：US149943
申请日：1993-11-10
申请人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/067
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2,[V] A=NHR.sup.4,wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译：本发明涉及可用作2-炔基腺苷合成中间体的下式[I]表示的新型化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷[Ⅳ]的方法。此外，本发明涉及具有优异的储存稳定性的由下式[V]表示的2-炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。 [I] A =离去基团，[II] A = NH 2，[V] A = NHR 4，其中R 1至R 4表示氢原子或保护基，n表示1至15的整数， R1至R4同时不表示氢原子。

23. 发明授权

US4420470A Percutaneous absorption type pharmaceutical preparation of isosorbide dinitrate or pentaerythritol tetranitrate in pressure-sensitive laminate 失效
标题翻译：硝酸异山梨酯或季戊四醇四硝酸酯在压敏层压板中的经皮吸收型药物制剂
公开(公告)号：US4420470A
公开(公告)日：1983-12-13
申请号：US338190
申请日：1982-01-08
申请人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuuseke Ito
发明人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuuseke Ito
IPC分类号： A61K9/70 , A61K31/21 , A61P9/08 , A61P9/10 , A61L15/03 , A61F13/00
CPC分类号： A61K9/7053 , A61K9/7061 , A61K9/7076
摘要： A pharmaceutical preparation comprising a flexible backing and a base material provided thereon is described wherein the base material consists essentially of a polymer having a glass transition temperature of from -70.degree. C. to -10.degree. C. and exhibiting pressure-sensitivity at room temperature, and isosorbide dinitrate or pentaerythritol tetranitrate. This pharmaceutical preparation is applied to the skin, and permits the active ingredient to be absorbed through the skin into the body at a constant rate, and gradually over a long period of time.
摘要翻译：描述了一种包含柔性背衬和其上提供的基材的药物制剂，其中所述基材主要由玻璃化转变温度为-70℃至-10℃的聚合物组成，并且在室温下表现出压敏性，硝酸异山梨酯或季戊四醇四硝酸酯。这种药物制剂适用于皮肤，并且允许活性成分以恒定的速率通过皮肤吸收到体内，并且逐渐地长时间地吸收。

24. 发明申请

US20190231724A1 THERAPEUTIC AGENT FOR GLAUCOMA 审中-公开
公开(公告)号：US20190231724A1
公开(公告)日：2019-08-01
申请号：US16317921
申请日：2017-07-21
申请人： TOA EIYO LTD.
发明人： Toshihiro SAWABE , Fumito MARUYAMA , Akiyuki TAKAYA , Takeshi HASEGAWA
IPC分类号： A61K31/197 , A61K31/381 , A61K31/353 , A61K31/343 , A61P27/06
摘要： Provided is a novel therapeutic agent for glaucoma, which has sGC-activating action. A therapeutic agent for glaucoma or an ocular hypotensive agent, which contains, as an effective component, a compound represented by Formula (I-a) or Formula (I-b) and having a LogD value of more than 1.5 and less than 2.5, or a pharmaceutically acceptable salt thereof. [In formulae (I-a) and (I-b), each symbol is as defined in the description.]

25. 发明授权

US09856250B2 Substituted tropane derivatives 有权
公开(公告)号：US09856250B2
公开(公告)日：2018-01-02
申请号：US15314020
申请日：2015-05-28
申请人： TOA EIYO LTD.
发明人： Hidekazu Masaki , Yoichi Iwasaki , Masayuki Kageyama , Yujiro Uchino
IPC分类号： C07D451/02 , C07D519/00 , A61K31/439
CPC分类号： C07D451/02 , A61K31/439 , C07D519/00
摘要： Provided is a compound which is useful as a prophylactic or therapeutic agent for various diseases in which T-type calcium channels are involved, such as hypertension, arrhythmia, pain and cancers, the compound having antagonistic activity against T-type calcium channels, being highly stable in the body and having low risk of, for example, genotoxicity. Disclosed is a compound represented by the following general formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein R1 represents —NH(C═O)—V—R3 or —(C═O)NH—V—R3; V represents a single bond, methylene, or —C(CH3)2O—; R2 represents a optionally substituted C1-6 alkyl group; X represents a hydrogen atom, an oxygen atom, a hydroxyl group, a methyl group, or a methylene group; A represents —NR6—, —O—CH2—, or —S—CH2—; n represents the number of methylene chains and represents an integer of 0, 1 or 2; and a doublet containing a dotted line represents a single bond or a double bond.

26. 发明授权

US09714213B2 4-aminomethylbenzoic acid derivative 有权
公开(公告)号：US09714213B2
公开(公告)日：2017-07-25
申请号：US15029452
申请日：2014-10-14
申请人： TOA EIYO LTD.
发明人： Kazuhiro Uemoto , Yoshimichi Sato , Naoki Okada , Emiko Iimori , Masayuki Kageyama
IPC分类号： A61K31/197 , A61K31/275 , A61K31/381 , A61K31/426 , C07C229/46 , C07C229/38 , C07C255/59 , C07C255/54 , C07D277/24 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/56 , C07D333/32
CPC分类号： C07C229/38 , A61K31/197 , A61K31/275 , A61K31/381 , A61K31/426 , A61P9/10 , A61P9/12 , A61P11/00 , A61P43/00 , C07C229/46 , C07C255/54 , C07C255/59 , C07C2601/02 , C07D277/24 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/56
摘要： A compound represented by general formula (1) a pharmaceutically acceptable salt thereof or a solvate thereof; wherein Ar represents an aryl group, or a 5- or 6-membered heteroaryl group containing a nitrogen atom, an oxygen atom or a sulfur atom; Y represents, for example, a hydrogen atom or a C1-C6 alkyl group; A represents a C1-C3 alkylene chain which may be substituted with two C1-C2 alkyl groups; X represents a hydrogen atom or a halogen atom; V represents an oxygen atom or a methylene chain; and R represents a group selected from the formulae below:

27. 发明授权

US09096531B2 Fused imidazole derivative 有权
标题翻译：熔融咪唑衍生物
公开(公告)号：US09096531B2
公开(公告)日：2015-08-04
申请号：US13699692
申请日：2011-05-24
申请人： Hidekazu Masaki , Hiroshi Takasugi , Tomoyuki Nagayama , Ryutaro Shimono , Yujiro Uchino , Koichi Takayanagi
发明人： Hidekazu Masaki , Hiroshi Takasugi , Tomoyuki Nagayama , Ryutaro Shimono , Yujiro Uchino , Koichi Takayanagi
IPC分类号： A61K31/44 , A61K31/415 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , C07D235/00 , C07D235/24 , C07D235/12 , C07D235/14 , C07D235/16 , C07D401/06 , C07D401/12 , C07D405/06 , C07D471/04 , C07D473/00
CPC分类号： C07D235/12 , C07D235/14 , C07D235/16 , C07D401/06 , C07D401/12 , C07D405/06 , C07D471/04 , C07D473/00
摘要： Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product.A compound represented by general formula (I), and a pharmaceutical agent containing the same, are disclosed: wherein n represents the number of nitrogen atoms contained in the 6-membered fused aromatic ring, and is 0, 1 or 2; p represents the number of nitrogen atoms contained in the 6-membered aromatic ring, and is 0 or 1; X represents an oxygen atom, —SO2— or —N(R9)—; and R1 to R5 each represents a hydrogen atom or other substituents.
摘要翻译：本发明提供了对T型钙通道具有拮抗作用的新化合物，作为药物有用。公开了由通式（I）表示的化合物和含有该化合物的药剂，其中n表示6元稠合芳环中所含的氮原子数，为0,1或2; p表示6元芳香环中含有的氮原子数，为0或1; X表示氧原子，-SO 2 - 或-N（R 9） - ; 并且R 1至R 5各自表示氢原子或其它取代基。

28. 发明申请

US20090170895A1 S1P3 RECEPTOR ANTAGONIST 失效
标题翻译： S1P3受体拮抗剂
公开(公告)号：US20090170895A1
公开(公告)日：2009-07-02
申请号：US12088861
申请日：2006-10-11
申请人： Shin-ya Ohnuma , Takeshi Hasegawa , Tomoyuki Sada
发明人： Shin-ya Ohnuma , Takeshi Hasegawa , Tomoyuki Sada
IPC分类号： A61K31/47 , C07D213/26 , A61K31/44 , C07D211/06 , A61K31/4453 , C07D307/48 , A61K31/341 , C07D471/00 , A61P3/10 , A61P9/04 , A61P9/10
CPC分类号： C07C317/34 , C07C257/22 , C07D213/74 , C07D215/04 , C07D217/02 , C07D295/185 , C07D307/46 , C07D333/22
摘要： The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P3 receptors and a medicine containing thereof as an active ingredient. The present invention provides an arylamidrazone derivative represented by the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a C2-C8 alkyl group which may be substituted, a phenyl group which may be substituted, an aromatic heterocyclic group which may be substituted, a C2-C8 alkoxy group which may be substituted, or —NR4R5 (wherein R4 and R5, which are identical or different, each represent a hydrogen atom or a lower alkyl group which may be substituted, or R4 and R5 may be joined with the adjacent nitrogen atom to form a nitrogen-containing heterocyclic ring which may be substituted); R2 and R3, which are identical or different, each represent a hydrogen atom, a halogen atom, a halo-lower alkyl group, a lower alkyl group, a lower alkynyl group, a lower alkoxy group, a cyano group, a lower alkanoyl group or a lower alkylsulfonyl group; A represents a benzene ring or a heterocyclic ring; D represents a single bond or methylene; m represents an integer from 1 to 3, and n represents an integer from 1 to 5 (with the proviso that the case where R1 is an ethoxy group, R2 is a 2,4-dichloro group, R3 is a hydrogen atom, A is a benzene ring, and D is methylene; and the case where R1 is an ethoxy group, R2 is a 2,4-dichloro group, R3 is a hydrogen atom, a 2-methyl group, a 4-methyl group, a 4-methoxy group or a 4-ethoxy group, A is a benzene ring, and D is a single bond, are excluded).
摘要翻译：本发明涉及一种药物，更具体地涉及对S1P3受体具有拮抗作用的新型芳基氨基腙衍生物和含有它们作为有效成分的药物。本发明提供由下式（1）表示的芳基腙基衍生物或其药学上可接受的盐：其中R 1表示可被取代的C 2 -C 8烷基，可被取代的苯基，可以被取代的苯基可被取代的C 2 -C 8烷氧基或-NR 4 R 5（其中R 4和R 5相同或不同，各自表示氢原子或可被取代的低级烷基，或者R 4和R 5可以是与相邻的氮原子一起形成可以被取代的含氮杂环）; R 2和R 3相同或不同，各自表示氢原子，卤素原子，卤代低级烷基，低级烷基，低级炔基，低级烷氧基，氰基，低级烷酰基或低级烷基磺酰基; A表示苯环或杂环; D表示单键或亚甲基; m表示1〜3的整数，n表示1〜5的整数（条件是R1为乙氧基的情况，R2为2,4-二氯基，R3为氢原子，A为苯环，D为亚甲基; R1为乙氧基，R2为2,4-二氯基，R3为氢原子，2-甲基，4-甲基，4-甲基，甲氧基或4-乙氧基，A为苯环，D为单键）。

29. 发明申请

US20090169604A1 Adhesive Pharmaceutical Preparation Containing Bisoprolol 有权
标题翻译：含有比索洛尔的胶粘剂药物制剂
公开(公告)号：US20090169604A1
公开(公告)日：2009-07-02
申请号：US12097260
申请日：2006-12-13
申请人： Yoshihiro Iwao , Katsuyuki Ookubo , Katsuhiro Okada , Kunihiro Minami , Shuichiro Yuasa
发明人： Yoshihiro Iwao , Katsuyuki Ookubo , Katsuhiro Okada , Kunihiro Minami , Shuichiro Yuasa
IPC分类号： A61K9/70 , A61K31/135 , A61P9/00
CPC分类号： A61K9/7053 , A61K31/138 , A61K47/10 , A61K47/32
摘要： In the adhesive pharmaceutical preparation of the invention containing bisoprolol, a pressure-sensitive adhesive layer is laminated on one side of the backing. The pressure-sensitive adhesive layer contains a branched monoalcohol having from 12 to 28 carbon atoms, a free base of bisoprolol and a polyisobutylene pressure-sensitive adhesive. Accordingly, compatibility of the polyisobutylene pressure-sensitive adhesive with the free base of bisoprolol can be specifically increased. As a result, not only it becomes possible to increase blending amount of the free base of bisoprolol but also bleed of the free base of bisoprolol from the pressure-sensitive adhesive layer can be suppressed and, what is more, the pressure-sensitive adhesion characteristics sufficient from the practical point of view can be obtained.
摘要翻译：在含有比索洛尔的本发明的粘合剂药物制剂中，在背衬的一侧层压压敏粘合剂层。压敏粘合剂层含有具有12至28个碳原子的支链一元醇，比索洛尔的游离碱和聚异丁烯压敏粘合剂。因此，可以特异性地增加聚异丁烯压敏粘合剂与比索洛尔的游离碱的相容性。结果，可以抑制比索洛尔的游离碱的混合量的增加，而且可以抑制比索洛尔的游离碱从压敏粘合剂层的渗出，而且还可以抑制压敏粘合特性从实用的角度来看可以获得足够的。

30. 发明授权

US5283327A Tri-O-acetyl-2-alkynyladenosines 失效
标题翻译：三-O-乙酰基-2- alkynyladenosines
公开(公告)号：US5283327A
公开(公告)日：1994-02-01
申请号：US655354
申请日：1991-04-17
申请人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/167
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译： PCT No.PCT / JP90 / 00807 Sec。 371日期：1991年4月17日 102（e）中的日期1991年4月17日提交的PCT 1990年6月20日的PCT公布。出版物WO90 / 15812 PCT 日本1990年12月27日。本发明涉及可用作2-炔基腺苷合成中间体的下式（I）表示的新化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷（Ⅳ）的方法。此外，本发明涉及具有优异储存稳定性的下式（V）表示的2-链炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。（*化学结构*）（*化学结构*）其中R1至R4表示氢原子或保护基，n表示1至15的整数，条件是R1至R4同时不表示氢原子。

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