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1. 发明授权

US5278156A 11-beta, 17-alpha, 21-trihydroxy-1, 4-pregnadiene-3, 20 21-[(E-E)-3,7, 11-trimethyl-2,6,10-dodecatrienoate] 失效
标题翻译： 11-β，17-α，21-三羟基-1,4-孕二烯-3,201 - [（E-E）-3,7,11-三甲基-2,6,10-十二碳三烯酸酯]
公开(公告)号：US5278156A
公开(公告)日：1994-01-11
申请号：US856858
申请日：1992-03-24
申请人： Yutaka Mizushima , Keiko Hoshi , Rie Igarashi , Hirofusa Ajioka , Noriyuki Yamamoto , Masahito Komuro , Koichi Kanehira , Masayuki Inoue , Takashi Nishida , Michio Terasawa , Kenzo Arizono
发明人： Yutaka Mizushima , Keiko Hoshi , Rie Igarashi , Hirofusa Ajioka , Noriyuki Yamamoto , Masahito Komuro , Koichi Kanehira , Masayuki Inoue , Takashi Nishida , Michio Terasawa , Kenzo Arizono
IPC分类号： C07J5/00 , A61K31/56
CPC分类号： C07J5/0053
摘要： 11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the formula ##STR1## an antiinflammatory composition thereof and a method for the production thereof.11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the present invention exhibits remarkably excellent antiinflammatory action and besides, displays reduced side effects and can be produced in high selectivity and good yield and conveniently.
摘要翻译： 11β，17α，21-三羟基-1,4-孕二烯-3,20-二酮21 - [（E，E）-3,7,11-三甲基-2,6,10-十二碳三烯酸酯] IMAGE>其抗炎组合物及其制备方法。 11β，17α，21-三羟基-1,4-孕二烯-3,20-二酮21 - [（E，E）-3,7,11-三甲基-2,6,10-十二碳三烯酸酯] 显示出显着优异的抗炎作用，此外，显示出副作用降低，并且可以以高选择性和良好的产率和方便地制备。

2. 发明授权

US5015746A 11.beta., 17.alpha.,21-trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] 失效
标题翻译： 11β，17α，21-三羟基-1,4-孕二烯-3,20-二酮21 - [（E，E）-3,7,11-三甲基-2,6,10-十二碳三烯酸酯]
公开(公告)号：US5015746A
公开(公告)日：1991-05-14
申请号：US299681
申请日：1989-01-23
申请人： Yutaka Mizushima , Keiko Hoshi , Rie Igarashi , Hirofusa Ajioka , Noriyuki Yamamoto , Masahito Komuro , Koichi Kanehira , Masayuki Inoue , Takashi Nishida , Manzo Shiono , Michio Terasawa , Kenzo Arizono
发明人： Yutaka Mizushima , Keiko Hoshi , Rie Igarashi , Hirofusa Ajioka , Noriyuki Yamamoto , Masahito Komuro , Koichi Kanehira , Masayuki Inoue , Takashi Nishida , Manzo Shiono , Michio Terasawa , Kenzo Arizono
IPC分类号： C07J5/00
CPC分类号： C07J5/0053
摘要： 11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the formula ##STR1## an antiinflammatory composition thereof and a method for the production thereof.11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the present invention exhibits remarkably excellent antiinflammatory action and besides, displays reduced side effects and can be produced in high selectivity and good yield and conveniently.

3. 发明授权

US4525348A Pranoprofen gelled ointment 失效
标题翻译：泼尼龙胶凝软膏
公开(公告)号：US4525348A
公开(公告)日：1985-06-25
申请号：US562570
申请日：1983-12-19
申请人： Kenzo Arizono , Michio Terasawa , Michiharu Nobutoki
发明人： Kenzo Arizono , Michio Terasawa , Michiharu Nobutoki
IPC分类号： A61K31/44 , A61K47/10 , A61K47/32 , A61K47/36 , A61K47/38 , A61K31/78
CPC分类号： A61K47/36 , A61K31/44 , A61K47/10 , A61K47/32 , A61K47/38 , A61K9/0014
摘要： An antiinflammatory and analgesic gelled ointment contains pranoprofen, at least one member selected from the group consisting of lower aliphatic alcohol, polyethylene glycol, methyl ethyl ketone and acetone, a gelling agent selected from the group consisting of carboxyvinyl polymer, hydroxyethyl cellulose, alginic acid and carboxymethyl cellulose, a water-soluble basic substance selected from the group consisting of ammonia, sodium hydroxide, potassium hydroxide, triethanolamine, diethanolamine, diisopropanolamine, triisopropanolamine and triethylamine, and water.
摘要翻译：抗炎止痛凝胶软膏含有双吡喃丙酸，选自低级脂肪醇，聚乙二醇，甲基乙基酮和丙酮中的至少一种，选自羧乙烯基聚合物，羟乙基纤维素，海藻酸和羧甲基纤维素，选自氨，氢氧化钠，氢氧化钾，三乙醇胺，二乙醇胺，二异丙醇胺，三异丙醇胺和三乙胺的水溶性碱性物质和水。

4. 发明授权

US5686479A Immunosuppressive drug 失效
标题翻译：免疫抑制药
公开(公告)号：US5686479A
公开(公告)日：1997-11-11
申请号：US244811
申请日：1994-06-10
申请人： Takeki Okumoto , Kenji Chiba , Yukio Hoshino , Hirotsugu Komatsu , Mariko Nagasawa , Hidekazu Aratani , Michio Terasawa , Minoru Moriwaki
发明人： Takeki Okumoto , Kenji Chiba , Yukio Hoshino , Hirotsugu Komatsu , Mariko Nagasawa , Hidekazu Aratani , Michio Terasawa , Minoru Moriwaki
IPC分类号： A61K31/55 , C07D495/14 , C07D495/22 , A61K31/41
CPC分类号： C07D495/14 , A61K31/55
摘要： An immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor, each containing a thienotriazolodiazepine compound wherein the 2-position of its diazepine ring is alkylated as an active ingredient, an immunosuppression method, an autoimmune disease treating method, an immunosuppression enhancing method and a cell adhesion inhibiting method, each of which comprising administering the compound, and uses of the compound for the production of an immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor.
摘要翻译： PCT No.PCT / JP92 / 01619 Sec。 371日期：1994年6月10日 102（e）日期1994年6月10日PCT提交1992年12月10日PCT公布。公开号WO93 / 12117 日期：1993年6月24日免疫抑制药物，自身免疫疾病治疗药物，免疫抑制增强药物和细胞粘附抑制剂，其各自含有噻吩并三氮杂环庚烯化合物，其中二氮杂环的2位被烷基化为活性成分，免疫抑制法，一种自身免疫疾病治疗方法，免疫抑制增强方法和细胞粘附抑制方法，其包括施用该化合物，以及该化合物用于制备免疫抑制药物，自身免疫疾病治疗药物，免疫抑制增强药物和细胞粘附抑制剂。

5. 发明授权

US4576940A Anti-allergic 3-indolecarboxamides 失效
标题翻译：抗过敏3-吲哚酰胺
公开(公告)号：US4576940A
公开(公告)日：1986-03-18
申请号：US639292
申请日：1984-08-10
申请人： Tetsuya Tahara , Tsuguo Ikebe , Michio Terasawa , Tomonori Imayoshi
发明人： Tetsuya Tahara , Tsuguo Ikebe , Michio Terasawa , Tomonori Imayoshi
IPC分类号： C12N9/99 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/55 , A61P3/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12
摘要： 3-Indolecarboxamide compounds of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-8 alkyl, allyl, propargyl, or phenyl or phenyl-C.sub.1-4 alkyl which may be optionally substituted, on the benzene ring, by at least one substituent selected from the group consisting of halogen, trifluoromethyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H, halogen, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.1-4 alkoxy, benzyloxy, hydroxy or C.sub.1-4 alkyl; R.sup.4 is H, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy; R.sup.5 is H or C.sub.1-4 alkoxy; A is ethylene or trimethylene, which may be optionally substituted by C.sub.1-4 alkyl; n is zero, 1 or 2; and m is zero or 1, are useful as drugs for the prevention and treatment of various allergic diseases.
摘要翻译：具有下式的3-吲哚甲酰胺化合物：包括其药学上可接受的酸加成盐和/或其水合物形式，其中R 1是C 1-8烷基，C 3-8环烷基，C 3-8环烷基-C 1-8烷基，烯丙基，炔丙基，或苯基或可任意取代的苯基-C 1-4烷基在苯环上，被至少一个选自卤素，三氟甲基，C 1-4烷基和C 1-4烷氧基的取代基取代; R2是H或C1-6烷基; R3是H，卤素，C2-6烷酰氧基，苯甲酰氧基，C1-4烷氧基，苄氧基，羟基或C1-4烷基; R4是H，卤素，C1-4烷基，C1-4烷氧基或羟基; R5是H或C1-4烷氧基; A是乙烯或三亚甲基，其可任选被C 1-4烷基取代; n为零，1或2; m为0或1，可用作预防和治疗各种过敏性疾病的药物。

6. 发明授权

US4808620A Pyrazolopyridine compounds, their preparation and use as platelet aggregation inhibitors 失效
标题翻译：吡唑并吡啶化合物，其制备和用作血小板聚集抑制剂
公开(公告)号：US4808620A
公开(公告)日：1989-02-28
申请号：US076504
申请日：1987-07-22
申请人： Takanori Oe , Kazuyuji Kawasaki , Michio Terasawa , Tomonori Imayoshi , Yukihiro Yasunaga
发明人： Takanori Oe , Kazuyuji Kawasaki , Michio Terasawa , Tomonori Imayoshi , Yukihiro Yasunaga
IPC分类号： A61K31/44 , A61P7/02 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/61 , C07D471/04 , A61K31/38 , A61K31/395 , A61K31/435
CPC分类号： C07D471/04 , C07D213/61
摘要： A pyrazolopyridine compound of the formula: ##STR1## or a salt thereof, wherein each symbol is as defined in the specification. Said compounds exhibit antiinflammatory, analgesic, antipyretic, antiallergic, antiarthritic, antirheumatic activities or inhibitory activities on platelet aggregation.

7. 发明授权

US4728644A Purine derivative and pharmaceutical composition 失效
标题翻译：嘌呤衍生物和药物组合物
公开(公告)号：US4728644A
公开(公告)日：1988-03-01
申请号：US768535
申请日：1985-07-22
申请人： Hiroshi Yuki , Hiroyuki Sueoka , Mitsuyoshi Yasumoto , Michio Terasawa , Tomonori Imayoshi
发明人： Hiroshi Yuki , Hiroyuki Sueoka , Mitsuyoshi Yasumoto , Michio Terasawa , Tomonori Imayoshi
IPC分类号： A61K31/52 , A61P25/04 , A61P29/00 , C07D473/34 , C07D473/04
CPC分类号： C07D473/34
摘要： Purine derivatives of the formula: ##STR1## wherein R is hydrogen, alkyl or phenyl which may be substituted by at least one halogen, lower alkyl or lower alkoxy; each of R.sup.1 and R.sup.2 is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, dialkylaminoalkyl, cyclic aminoalkyl, alkenyl or aralkyl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form a heterocycle; and each of R.sup.3 and R.sup.4 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof and/or hydrates, methods of preparing said compounds and pharmaceutical compositions containing said compounds. The purine compounds exhibit antiinflammatory, analgesic, antipyretic and antiallergic activity, and inhibitory activity on platelet aggregation, and are useful as drugs.
摘要翻译： PCT No.PCT / JP84 / 00633 Sec。 371日期：1985年7月22日 102（e）日期1985年7月22日PCT提交1984年12月28日PCT公布。第WO85 / 03077号公报 1985年7月18日。具有下式的嘌呤衍生物：其中R是氢，可被至少一个卤素，低级烷基或低级烷氧基取代的烷基或苯基; R 1和R 2各自为氢，烷基，环烷基，羟基烷基，二烷基氨基烷基，环状氨基烷基，烯基或芳烷基，或者R 1和R 2与相邻的氮原子一起形成杂环; 并且R 3和R 4各自为氢或低级烷基，及其药学上可接受的酸加成盐和/或水合物，制备所述化合物的方法和含有所述化合物的药物组合物。嘌呤化合物具有抗炎，止痛，解热和抗过敏活性，对血小板聚集具有抑制活性，可用作药物。

8. 发明授权

US5286858A Optically active thienotriazolodiazepine compounds 失效
标题翻译：光学活性噻吩并三唑并噻嗪化合物
公开(公告)号：US5286858A
公开(公告)日：1994-02-15
申请号：US774945
申请日：1991-10-11
申请人： Minoru Moriwaki , Syuji Yuasa , Hiroyuki Kitani , Michio Terasawa
发明人： Minoru Moriwaki , Syuji Yuasa , Hiroyuki Kitani , Michio Terasawa
IPC分类号： A61K31/55 , A61K31/00 , A61K31/554 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D495/14 , C07D495/12
CPC分类号： C07D495/14
摘要： Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R.sup.1 is hydrogen, R.sup.2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R.sup.1 and R.sup.2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R.sup.3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R.sup.4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R.sup.5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.
摘要翻译：光学活性噻吩并三唑并噻嗪类化合物或其水合物（*化学结构*）（I）的酸加成盐的稳定晶体，其中R 1为氢，R 2为被具有1至5个碳原子的烷基取代的2-苯乙基，吗啉代羰基乙基或具有6至12个碳原子的烷基，或者R 1和R 2可以组合形成具有一个选自吗啉代甲基，吗啉代羰基和N，N-二丙基氨基甲酰基的一个取代基的饱和五元环，R 3是卤素， 5个碳原子或具有1至5个碳原子的烷氧基，R4是三氟甲基或具有1-5个碳原子的烷基，R5是氢或甲基，m是1-2，n是0-2。本发明提供具有优异结晶性的显色稳定结晶的具有强PAF拮抗作用的光学活性噻吩并三唑并氮杂化合物，可以通过重结晶进行纯化，化学纯度高，光学纯度高，从而可实现工业化的大规模合成。此外，其结晶有助于药物标准化和药物制剂。

9. 发明授权

US5198452A Styryl phridyl compounds and their pharmaceutical compositions 失效
标题翻译：苯乙烯基短链烯基化合物及其药物组合物
公开(公告)号：US5198452A
公开(公告)日：1993-03-30
申请号：US728128
申请日：1991-07-10
申请人： Mitsuhiro Konishi , Minoru Kawakami , Michio Terasawa , Toshio Hamasaki
发明人： Mitsuhiro Konishi , Minoru Kawakami , Michio Terasawa , Toshio Hamasaki
IPC分类号： C07D213/30 , C07D213/32 , C07D213/40 , C07D215/12 , C07D215/22 , C07D215/233 , C07D401/12 , C07D405/12
CPC分类号： C07D213/30 , C07D213/32 , C07D213/40 , C07D215/12 , C07D215/233 , C07D401/12 , C07D405/12
摘要： A styryl compound of the formula(I): ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt or an ester thereof is disclosed.Since the compounds of the present invention possess potent and long-lasting leukotriene-antagonistic actions and inhibitory actions against leukotriene, and exhibit better absorption by the oral administration.Further, the compounds of the present invention possess 5-lipoxygenase-inhibitory actions and/or cyclooxygenase-inhibitory actions, inhibitory actions to biosynthesis of LTB4, chemotactic actions against human leucoccyte, chymase-inhibitory actions, inhibitory actions to release of histamine or antihistamine actions.Therefore, they are useful as the prophylactic and therapeutic medicines for brochial asthma, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic arthritis, allergic conjunctivitis, hay fever, urticaria, alimentary allergy, pain, pyretolysis, rheumatoid, thrombosis, coronary vascular diseases, ischemic heart disease, peptic or duodenal ulcer and the like.
摘要翻译：公开了式（I）的苯乙烯基化合物：其中每个符号如说明书中所定义，其药学上可接受的盐或酯。由于本发明的化合物具有强效的和持久的白三烯拮抗作用和对白细胞三烯的抑制作用，并且通过口服给药表现出更好的吸收。此外，本发明的化合物具有5-脂氧合酶抑制作用和/或环加氧酶抑制作用，对LTB4的生物合成的抑制作用，对人类白细胞的趋化作用，糜酶抑制作用，释放组胺或抗组织胺作用的抑制作用。因此，它们可用作小儿哮喘，慢性支气管炎，特应性皮炎，过敏性鼻炎，过敏性关节炎，过敏性结膜炎，花粉症，荨麻疹，消化道变态反应，疼痛，并发症，类风湿，血栓形成，冠状动脉血管疾病等预防和治疗药物。缺血性心脏病，消化性溃疡或十二指肠溃疡等。

10. 发明授权

US5028603A Ester-substituted thienotriazolodiazepine compounds and pharmaceutical uses thereof 失效
标题翻译：酯取代的噻吩并三唑并噻嗪类化合物及其药物用途
公开(公告)号：US5028603A
公开(公告)日：1991-07-02
申请号：US350589
申请日：1989-02-03
申请人： Tetsuya Tahara , Minoru Moriwaki , Masao Abe , Michio Terasawa
发明人： Tetsuya Tahara , Minoru Moriwaki , Masao Abe , Michio Terasawa
IPC分类号： A61K31/55 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/08 , C07D495/14
CPC分类号： C07D495/14
摘要： There are provided novel ester-substituted thienotriazolodiazepines useful for the treatment of various PAF-induced diseases.

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