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11. 发明授权

US4888417A Therapeutic and prophylactic agents for peptic ulcer 失效
标题翻译：消化性溃疡的治疗和预防剂
公开(公告)号：US4888417A
公开(公告)日：1989-12-19
申请号：US867169
申请日：1986-05-27
申请人： Yusei Shiraga , Chikara Fukaya , Toshiaki Akira , Masakazu Iwai , Kazumasa Yokoyama , Mamoru Tabata , Hiroshi Fukui , Shigeo Tanaka , Yoshiro Iga , Tadakazu Suyama , Kanemichi Okano
发明人： Yusei Shiraga , Chikara Fukaya , Toshiaki Akira , Masakazu Iwai , Kazumasa Yokoyama , Mamoru Tabata , Hiroshi Fukui , Shigeo Tanaka , Yoshiro Iga , Tadakazu Suyama , Kanemichi Okano
IPC分类号： A61K31/12 , A61K31/70 , A61K36/54 , C07C49/242 , C07C49/255 , C07C49/647 , C07C49/743 , C07H15/18 , C07H15/203 , C07H15/207
CPC分类号： C07C403/08 , C07C403/10 , C07C403/12 , C07H15/18 , C07H15/203 , C07C2101/16 , Y10S514/927
摘要： A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or =O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.6 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;X represents group (A):.dbd.C.dbd.CH--COR.sub.8 (A) or group (B): ##STR2## wherein R.sub.8 represents alkyl, and R.sub.9 and R.sub.10 each represents hydrogen or an organic residue; with the proviso that when X represents group (A), then R.sub.1 and R.sub.3 both represent hydrogen, R.sub.2 represents --OR.sub.5 ; R.sub.4 represents OR.sub.7 and the bond between the carbon atoms to which X is attached and the carbon atom to which R.sub.4 is attached is a single bond, and when X represents group (B), then R.sub.1 represents .dbd.O, R.sub.2 represents hydrogen, R.sub.3 represents --OR.sub.6 and the bond between the carbon atom to which X is attached and the carbon atom to which R.sub.4 is attached is a double bond, or a pharmaceutically acceptable salt thereof, or a compound of the general formula (II): ##STR3## wherein R.sub.11 represents hydrogen or an organic residue, and R.sub.12, R.sub.13 and R.sub.14 each represents an organic residue, or a pharmaceutically acceptable salt thereof. The compounds of the general formulae (I) and (II) can be derived from compounds contained in a hot water extract of cinnamon.
摘要翻译：含有作为活性成分的通式（I）的化合物的消化性溃疡的治疗和预防剂：其中R1表示氢或= O; R2代表氢或-OR5; R3表示氢或-OR6; 在不存在双键的情况下，R4代表-OR7; R5，R6和R7各自表示氢或有机残基; X表示基团（A）：= C = CH-COR 8（A）或基团（B）：其中R 8表示烷基，R 9和R 10各自表示氢或有机残基; 条件是当X表示基团（A）时，则R1和R3都表示氢，R2表示-OR5; R4表示OR7，X所连接的碳原子和与R4连接的碳原子之间的键为单键，当X表示基团（B）时，则R 1表示= O，R 2表示氢，R 3表示 -OR 6和X所连接的碳原子和与R 4连接的碳原子之间的键是双键，或其药学上可接受的盐或通式（II）的化合物：（ II）其中R 11表示氢或有机残基，R 12，R 13和R 14各自表示有机残基或其药学上可接受的盐。通式（I）和（II）的化合物可以衍生自肉桂热水提取物中所含的化合物。

12. 发明授权

US4687762A Water soluble drug complex and method for production of same 失效
标题翻译：水溶性药物复合物及其制备方法
公开(公告)号：US4687762A
公开(公告)日：1987-08-18
申请号：US716436
申请日：1985-03-27
申请人： Tsunekazu Fukushima , Hiroshi Emoto , Yoshio Kagitani , Kazumasa Yokoyama , Masayuki Nishida , Tadakazu Suyama
发明人： Tsunekazu Fukushima , Hiroshi Emoto , Yoshio Kagitani , Kazumasa Yokoyama , Masayuki Nishida , Tadakazu Suyama
IPC分类号： B01J13/02 , A61K9/00 , A61K9/127 , A61K9/50 , A61K31/70 , A61K31/545 , A61K31/685
CPC分类号： A61K47/48053 , A61K9/1277
摘要： The invention provides a method of producing a water-soluble complex comprising a water-insoluble drug and a phospholipid, comprising the steps of (1) dissolving a water-insoluble drug and a phospholipid in an organic solvent, (2) removing the solvent to leave behind a drug-containing phospholipid film, (3) suspending the resulting film in an aqueous solution, (4) ultrasonicating the film, (5) centrifuging the resulting suspension, and (6) recovering the lowermost layer of the resulting sediment to yield the water-soluble complex. The above complex can be administered parenterally as well as by the oral and other routes, and is so rich in the drug component that a remarkably increased drug activity can be realized.
摘要翻译：本发明提供一种生产包含水不溶性药物和磷脂的水溶性络合物的方法，包括以下步骤：（1）将水不溶性药物和磷脂溶于有机溶剂中，（2）除去溶剂至留下含药磷脂膜，（3）将所得膜悬浮在水溶液中，（4）使膜超声波化，（5）离心所得悬浮液，（6）回收所得沉淀物的最下层，得到水溶性复合物。上述复合物可以肠胃外给药，口服给药或其他途径给药，药物成分丰富，药物活性显着提高。

13. 发明授权

US4605650A Perfluoro-1-azatricyclic amine compounds useful as oxygen carriers in artificial blood and infusion fluids 失效
标题翻译：全氟-1-氮杂环胺化合物可用作人造血液和输注液中的氧载体
公开(公告)号：US4605650A
公开(公告)日：1986-08-12
申请号：US751850
申请日：1983-07-05
申请人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
IPC分类号： A61K9/00 , C07D453/02 , C07D471/08 , C07D487/08 , C25B3/08 , A61K31/40
CPC分类号： A61K9/0026 , C07D453/02 , C07D471/08 , C07D487/08 , C25B3/08 , Y10S514/832 , Y10S514/833
摘要： A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 to 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.

14. 发明授权

US4849451A Fat emulsion containing prostaglandin 失效
标题翻译：含有前列腺素的脂肪乳液
公开(公告)号：US4849451A
公开(公告)日：1989-07-18
申请号：US865647
申请日：1986-05-16
申请人： Yutaka Mizushima , Hironaka Aihara , Susumu Otomo , Kazumasa Yokoyama , Hiroyuki Okamoto , Tadakazu Suyama
发明人： Yutaka Mizushima , Hironaka Aihara , Susumu Otomo , Kazumasa Yokoyama , Hiroyuki Okamoto , Tadakazu Suyama
IPC分类号： B01J13/00 , A61K9/107 , A61K31/555 , A61K31/557 , A61K47/24 , A61K47/44 , A61P43/00
CPC分类号： A61K31/557 , A61K9/1075
摘要： A fat emulsion containing a prostaglandin E.sub.1 alkyl ester represented by the general formula ##STR1## wherein R denotes an alkyl group having 1 to 30 carbon atoms. The fat emulsion can be administered intravenously, has a long half-life of its effective ingredient, prostaglandin E.sub.1 alkyl ester, in the living body as well as a focus selectivity.
摘要翻译：含有由通式（IMAGE）表示的前列腺素E1烷基酯的脂肪乳剂，其中R表示碳原子数1〜30的烷基。脂肪乳剂可以静脉内施用，其有效成分的半衰期长，前列腺素E1烷基酯在生物体中以及焦点选择性。

15. 发明授权

US4733002A Lipoxygenase inhibitor 失效
标题翻译：脂氧合酶抑制剂
公开(公告)号：US4733002A
公开(公告)日：1988-03-22
申请号：US737005
申请日：1985-05-23
申请人： Kazumasa Yokoyama , Chikara Fukaya , Masanori Sugiura , Youichiro Naito , Youichiro Nishida , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Chikara Fukaya , Masanori Sugiura , Youichiro Naito , Youichiro Nishida , Tadakazu Suyama
IPC分类号： A61K31/05 , A61K31/085 , A61K31/09 , A61K31/12 , A61K31/165 , A61K31/216 , C07C39/19 , C07C43/23 , C07C45/67 , C07C45/72 , C07C49/248 , C07C49/255 , C07C69/732 , C07C235/34 , C07D309/12 , A61K31/215
CPC分类号： C07D309/12 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/12 , A61K31/165 , A61K31/216 , C07C235/34 , C07C39/19 , C07C43/23 , C07C45/673 , C07C45/72 , C07C49/248 , C07C49/255 , C07C69/732
摘要： A lipoxygenase inhibitor comprising as active ingredient a substituted styrene derivative having a radical of the general formula ##STR1## wherein X denotes a hydroxyl group or a lower alkoxy group and q is an integer of 2 or 3, and containing carbon atoms in total of at least 8.

16. 发明授权

US4613605A Perfluoro-1-azatricyclic amines as blood substitutes 失效
标题翻译：全氟-1-氮杂环胺作为血液代用品
公开(公告)号：US4613605A
公开(公告)日：1986-09-23
申请号：US751948
申请日：1985-07-05
申请人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
IPC分类号： A61K9/00 , C07D453/02 , C07D471/08 , C07D487/08 , C25B3/08 , A61K31/445 , C07D453/00
CPC分类号： A61K9/0026 , C07D453/02 , C07D471/08 , C07D487/08 , C25B3/08 , Y10S514/832 , Y10S514/833
摘要： A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 or 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.

17. 发明授权

US4613505A Ester of flurbiprofen and emulsion containing the same 失效
标题翻译：氟比洛芬酯和含有相同的乳液
公开(公告)号：US4613505A
公开(公告)日：1986-09-23
申请号：US622244
申请日：1984-06-19
申请人： Yutaka Mizushima , Katsuhiro Uchida , Shozoh Masumoto , Masao Tohno , Yoshinobu Hashimoto , Kazumasa Yokoyama , Hiroyuki Okamoto , Kiichiro Nabeta , Tadakazu Suyama
发明人： Yutaka Mizushima , Katsuhiro Uchida , Shozoh Masumoto , Masao Tohno , Yoshinobu Hashimoto , Kazumasa Yokoyama , Hiroyuki Okamoto , Kiichiro Nabeta , Tadakazu Suyama
IPC分类号： A61K9/107 , A61K31/215 , A61K31/365 , A61P25/04 , A61P29/00 , C07D307/33 , A61K31/235 , A61K31/685
CPC分类号： A61K31/365 , A61K31/215 , A61K9/1075
摘要： There is provided a fat emulsion of an ester of flurbiprofen having the formula ##STR1## wherein R is a group of the formula ##STR2## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, R.sub.2 is a C.sub.1 -C.sub.15 alkyl group or a C.sub.2 -C.sub.8 alkenyl group, and m is zero or an integer of 1; or a lactone group of the formula ##STR3## wherein R.sub.3 and R.sub.4 are same as or different from each other and are a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and n is an integer of 1 or 2.The emulsion containing particles of a vegetable oil dissolving the ester can be orally or parenterally administered to human or animal for analgesia, antiphlogosis and antipyresis in various diseases and exhibits a high activity with small amounts in terms of flurbiprofen as compared with flurbiprofen itself.
摘要翻译：提供了一种氟比洛芬的酯的脂肪乳剂，其具有式“IMAGE”，其中R是下式的基团：其中R 1是氢原子或C 1 -C 3烷基，R 2是C 1 -C 15烷基或C 2 -C 8烯基，m为0或1的整数; 或式“IMAGE”的内酯基团，其中R 3和R 4彼此相同或不同，为氢原子或C 1 -C 3烷基，n为1或2的整数。溶解酯的植物油可以口服或肠胃外给予人或动物用于各种疾病的镇痛，消炎和除血，并且与氟比洛芬本身相比，在氟比洛芬方面表现出较低的活性。

18. 发明授权

US4605786A Perfluoro ether compound containing perfluorocycloalkyl moiety 失效
标题翻译：含全氟环烷基部分的全氟醚化合物
公开(公告)号：US4605786A
公开(公告)日：1986-08-12
申请号：US563436
申请日：1983-12-20
申请人： Kazumasa Yokoyama , Yoshihisa Inoue , Taizo Ono , Chikara Fukaya , Yoshio Arakawa , Youichiro Naito , Koichi Yamauchi , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Yoshihisa Inoue , Taizo Ono , Chikara Fukaya , Yoshio Arakawa , Youichiro Naito , Koichi Yamauchi , Tadakazu Suyama
IPC分类号： C07C41/00 , C07C43/12 , C07C43/192 , C07C43/313 , C07C67/00 , C25B3/02 , C25B3/08
CPC分类号： C07C43/123 , C07C43/192 , C07C43/313 , Y10S514/832
摘要： A perfluoroether compound having the following formula is useful as a thermostable, inert solvent and inter alia as an oxygen carrier in an artificial blood or infusion fluid. ##STR1## wherein Rf.sub.1 and Rf.sub.2 are different from each other and are selected from the group of a C.sub.1 or C.sub.3 perfluoroalkyl group which may be interrupted by an oxygen atom, and a C.sub.5 -C.sub.7 perfluorocycloalkyl group, and n and n' are zero or an integer of 1; one of Rf.sub.1 and Rf.sub.2 being the C.sub.5 -C.sub.7 perfluorocycloalkyl group and the total number of carbon atoms being 9-11 inclusive.
摘要翻译：具有下式的全氟醚化合物可用作热稳定的惰性溶剂，尤其用作人造血液或输注液中的氧载体。其中Rf1和Rf2彼此不同，并且选自可被氧原子中断的C1或C3全氟烷基和C5-C7全氟环烷基，n和n'为零或整数1; Rf1和Rf2之一是C5-C7全氟环烷基，碳原子总数为9-11（含）。

19. 发明授权

US4591593A Perfluoro compound and emulsion thereof 失效
标题翻译：全氟化合物及其乳液
公开(公告)号：US4591593A
公开(公告)日：1986-05-27
申请号：US442416
申请日：1982-11-17
申请人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Isuda , Taizo Ono , Yoshio Arakawa , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Isuda , Taizo Ono , Yoshio Arakawa , Tadakazu Suyama
IPC分类号： A01N1/02 , A61K9/00 , C07D209/30 , C07D209/44 , C07D209/52 , C07D215/18 , C07D217/22 , C07D221/04 , C25B3/08 , A61K31/47 , A61K31/40 , C07D209/10
CPC分类号： A61K9/0026 , A01N1/02 , A01N1/0226 , C07D209/30 , C07D209/44 , C07D209/52 , C07D215/18 , C07D217/22 , C07D221/04 , C25B3/08
摘要： A novel compound of the formula, ##STR1## wherein R denotes a lower perfluoroalkyl group l is an integer of 3 or 4, n+m is an integer of 2 or 3, provided that n may be zero, and at least one of ring A and ring B may be substituted by a lower perfluoroalkyl group, prepared by reacting the corresponding perhydro compound with fluorine is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.
摘要翻译：式（1）的新化合物，其中R表示低级全氟烷基1为3或4的整数，n + m为2或3的整数，条件是n可以为0，并且环中的至少一个为环 A和环B可以被通过使相应的全氢化合物与氟反应制备的低级全氟烷基取代，可用作能够在水性乳液中携带氧气的材料，用于挽救患有大量出血的患者和用于在移植中保存内脏。

20. 发明授权

US4530926A Perfluorotricyclic amines as oxygen carriers 失效
标题翻译：全氟三环胺作为氧载体
公开(公告)号：US4530926A
公开(公告)日：1985-07-23
申请号：US505324
申请日：1983-06-17
申请人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
发明人： Kazumasa Yokoyama , Chikara Fukaya , Yoshio Tsuda , Taizo Ono , Yoshio Arakawa , Yoshihisa Inoue , Youichiro Naito , Tadakazu Suyama
IPC分类号： A01N1/02 , C07D455/03 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , A61K31/55 , A61K31/40 , A61K31/445 , C07D455/06
CPC分类号： C07D455/00 , A01N1/021 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要： A novel compound of the formula, ##STR1## wherein k, j, l and m are zero or an integer of from 1 to 3, and n is an integer of from 1 to 3, the rings A, B and C being optionally substituted with at least one trifluoromethyl group, prepared by reacting the corresponding perhydro compound with fluorine is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.
摘要翻译：式（I）的新颖化合物，其中k，j，l和m为0或1〜3的整数，n为1〜3的整数，环A，B，C 任选地被至少一个三氟甲基取代，其通过使相应的全氢化合物与氟反应制备，可用作能够在水乳液中携带氧气的材料，用于挽救患有大量出血的患者和用于在移植中保存内脏。

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