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1. 发明授权

US4479942A Tetrahydrofurnancarboxylic acid derivatives, processes for preparation thereof and pharmaceutical compositions thereof 失效
标题翻译：四氢呋喃羧酸衍生物，其制备方法及其药物组合物
公开(公告)号：US4479942A
公开(公告)日：1984-10-30
申请号：US403117
申请日：1982-07-29
申请人： Michio Yamashita , Tadaaki Komori , Junji Hosoda , Yoshio Kawai , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Kazuo Sakane , Hiroyuki Setoi , Tsutomu Teraji
发明人： Michio Yamashita , Tadaaki Komori , Junji Hosoda , Yoshio Kawai , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Kazuo Sakane , Hiroyuki Setoi , Tsutomu Teraji
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P31/04 , C07H19/16 , C12P19/40 , C07H17/00 , C07H19/06
CPC分类号： C12R1/645 , C07H19/16 , C12P19/40 , Y02P20/55
摘要： This invention relates to tetrahydrofuran-carboxylic acid derivatives, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is amino or acylamino andR.sup.3 is carboxy or a protected carboxy groupor a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及抗微生物活性的四氢呋喃 - 羧酸衍生物，其具有下式：其中R1是氨基或被保护的氨基，R2是氨基或酰基氨基，R3是羧基或被保护的羧基或药学上可接受的盐其中。

2. 发明授权

US4313935A Antibiotic FR-900129 substance, a process for the preparation thereof and pharmaceutical compositions containing the same 失效
标题翻译：抗生素FR-900129物质，其制备方法和含有它们的药物组合物
公开(公告)号：US4313935A
公开(公告)日：1982-02-02
申请号：US125486
申请日：1980-02-28
申请人： Tadaaki Komori , Michio Yamashita , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Tadaaki Komori , Michio Yamashita , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
IPC分类号： C07G11/00 , C12P1/06 , C12R1/465 , A61K35/00 , C12P13/00
CPC分类号： C12R1/465 , C12P1/06 , Y10S435/886
摘要： Prodn. of FR-900129 comprises culturing a Streptomyces n. 4012 category which is analogous to Streptomyces misakiensis and Steptomyces aburaviensis, i.e. Streptomyces avellaneus No. 4012, at 25.degree. C. to 30.degree. C. during 50 to 100 hours in a culture medium which consists of a carbon source (e.g. glucose, fructose, glycerin, starch, galactose, maltose, dextrin), an organic or inorganic nitrogen source (e.g. yeast extract, peptone, cottonseed cake, soyabean powder, cornsteep liquor, dry yeast, ammonium nitrate, ammonium sulphate, ammonium phosphate, urea and amino acid) and an inorganic salt (e.g. calcium carbonate, sodium phosphate, potassium phosphate, sodium chloride, potassium chloride, magnesium salt and copper salt). The produced FR-900129 is isolated by a collecting step, a purifying step, a vacuum condensation step, a freeze-drying step, a pH adjusting step, a cationic, anionic or nonionic resin treating step, an active carbon adsorption step and a crystallizing and recrystallizing step. The isolated material may then be converted to its adduct salt or its ester conventionally.
摘要翻译：产品的FR-900129包括培养Streptomyces n。 4012类似于Streptomyces misakiensis和Steptomyces aburaviensis（即Streptomyces avellaneus No.4012），在25℃至30℃下在50至100小时内在由碳源（例如葡萄糖，果糖，甘油，淀粉，半乳糖，麦芽糖，糊精），有机或无机氮源（例如酵母提取物，蛋白胨，棉籽饼，大豆粉，玉米浸液，干酵母，硝酸铵，硫酸铵，磷酸铵，尿素和氨基酸）和无机盐（例如碳酸钙，磷酸钠，磷酸钾，氯化钠，氯化钾，镁盐和铜盐）。生产的FR-900129通过收集步骤，纯化步骤，真空冷凝步骤，冷冻干燥步骤，pH调节步骤，阳离子，阴离子或非离子树脂处理步骤，活性炭吸附步骤和结晶和重结晶步骤。然后可以将分离的材料通常转化为其加合物盐或其酯。

3. 发明授权

US4767768A Nitro aliphatic compounds, process for preparation thereof and use thereof 失效
标题翻译：硝基脂族化合物，其制备方法和用途
公开(公告)号：US4767768A
公开(公告)日：1988-08-30
申请号：US559260
申请日：1983-12-08
申请人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： C07D207/416 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/26 , A61K31/445 , A61K31/495 , A61P7/02 , A61P9/08 , A61P9/12 , C07C43/23 , C07C45/41 , C07C57/03 , C07C205/51 , C07C233/02 , C07C233/09 , C07C233/20 , C07C233/49 , C07C235/28 , C07C249/04 , C07C251/32 , C07C251/38 , C07C251/40 , C07C251/60 , C07C255/10 , C07C255/19 , C07C255/23 , C07C255/64 , C07C291/12 , C07D207/40 , C07D207/404 , C07D295/18 , C07D295/185 , C07C103/22 , C07C103/34
CPC分类号： C07D207/404 , C07C205/44 , C07C205/51 , C07C255/00 , C07C43/23 , C07C45/41 , C07C57/03 , C07D295/185
摘要： New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.
摘要翻译：公开了新的硝基脂族化合物及其药学上可接受的盐。

4. 发明授权

US4643990A N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof 失效
标题翻译： N-酰基肽，其制备方法及其药物组合物
公开(公告)号：US4643990A
公开(公告)日：1987-02-17
申请号：US452827
申请日：1982-12-23
申请人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , A61K37/43 , C07C67/02 , C07C69/52 , C07C101/26 , C07C101/30 , C07C143/12 , C07K5/08
CPC分类号： C07K5/06104 , C07K5/06052 , C07K5/06078 , C07K5/06086 , A61K38/00
摘要： N-acylpeptides are disclosed of the formula: ##STR1## wherein R.sup.1 is alkanoyloxy or alkenoyloxy; R.sup.2 is alkyl or alkenyl; R.sup.3 and R.sup.4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R.sup.5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R.sup.6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A.sup.1, A.sup.2 and A.sup.3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.
摘要翻译： N-酰基肽公开于下式：其中R 1是烷酰氧基或烯酰基氧基; R2是烷基或烯基; R 3和R 4各自为低级烷基，羟基（低级）烷基，芳（低级）烷基，酯化羧基（低级）烷基，羧基（低级）烷基，被保护的氨基（低级）烷基或氨基（低级） R5是氢，羟基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基或酯化羧基（低级）烷基; R6是羧基，酯化的羧基或磺基（低级）烷基; A1，A2和A3各自为键或低级亚烷基; m和n分别为0或1的整数; 或其药学上可接受的盐。这些化合物具有抗互补活性和纤维蛋白溶解活性，并且可用作免疫复合物疾病或自身免疫性疾病如肾炎，风湿性疾病，系统性红斑狼疮等的治疗剂，以及血栓形成如脑中风，冠状动脉功能不全，肺栓塞等等

5. 发明授权

US4782088A Nitro aliphatic compounds and use thereof 失效
标题翻译：硝基脂肪族化合物及其用途
公开(公告)号：US4782088A
公开(公告)日：1988-11-01
申请号：US946868
申请日：1986-12-29
申请人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： C07D207/416 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/26 , A61K31/445 , A61K31/495 , A61P7/02 , A61P9/08 , A61P9/12 , C07C43/23 , C07C45/41 , C07C57/03 , C07C205/51 , C07C233/02 , C07C233/09 , C07C233/20 , C07C233/49 , C07C235/28 , C07C249/04 , C07C251/32 , C07C251/38 , C07C251/40 , C07C251/60 , C07C255/10 , C07C255/19 , C07C255/23 , C07C255/64 , C07C291/12 , C07D207/40 , C07D207/404 , C07D295/18 , C07D295/185 , C07C131/00
CPC分类号： C07D207/404 , C07C205/44 , C07C205/51 , C07C255/00 , C07C43/23 , C07C45/41 , C07C57/03 , C07D295/185
摘要： The invention relates to compounds of antihypertensive and antithrombotic activity of the formula or its pharmaceutically acceptable salt: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, or lower alkoxyphenyl,R.sup.2 is hydrogen or lower alkyl,R.sup.4 is lower alkyl,R.sup.6 is hydrogen or lower alkyl,R.sup.7 is lower alkyl which is optionally substituted by hydroxy or lower alkanoyloxy, andR.sup.10 is hydrogen or lower alkyl which is optionally substituted by carboxy or esterified carboxy.

6. 发明授权

US4778804A Nitro aliphatic compounds, process for preparation thereof and use thereof 失效
标题翻译：硝基脂族化合物，其制备方法和用途
公开(公告)号：US4778804A
公开(公告)日：1988-10-18
申请号：US786754
申请日：1985-10-11
申请人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Masanori Okamoto , Morita Iwami , Shigehiro Takase , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： C07D207/416 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/26 , A61K31/445 , A61K31/495 , A61P7/02 , A61P9/08 , A61P9/12 , C07C43/23 , C07C45/41 , C07C57/03 , C07C205/51 , C07C233/02 , C07C233/09 , C07C233/20 , C07C233/49 , C07C235/28 , C07C249/04 , C07C251/32 , C07C251/38 , C07C251/40 , C07C251/60 , C07C255/10 , C07C255/19 , C07C255/23 , C07C255/64 , C07C291/12 , C07D207/40 , C07D207/404 , C07D295/18 , C07D295/185 , C07C103/22 , C07C103/34
CPC分类号： C07D207/404 , C07C205/44 , C07C205/51 , C07C255/00 , C07C43/23 , C07C45/41 , C07C57/03 , C07D295/185
摘要： New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.

7. 发明授权

US4585789A New furanone derivatives, process for preparation thereof and use thereof 失效
标题翻译：新的呋喃酮衍生物，其制备方法和用途
公开(公告)号：US4585789A
公开(公告)日：1986-04-29
申请号：US508892
申请日：1983-06-29
申请人： Masanori Okamoto , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Masanori Okamoto , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： A61K31/34 , A61K31/341 , A61P27/02 , A61P27/12 , C07C43/166 , C07D303/22 , C07D307/33 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04 , C07D307/32
CPC分类号： C07D303/22 , C07C43/166 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04 , C12R1/645 , Y02P20/55
摘要： Described are compounds of the formula: ##STR1## Wherein A is a lower alkylene group;R.sup.1 is a carboxy, hydroxy, lower alkoxycarbonyl, lower alkoxycarbonylamino, phenyl(lower)alkyloxy, benzoyloxy or lower alkanoyloxy group;R.sup.2 is a hydrogen or halogen atom or a halo(lower)alkyl group;R.sup.3 is a hydrogen or halogen atom;R.sup.4 is hydroxy, lower alkoxy, lower alkanoyloxy or lower alkoxycarbonyloxy group; andR.sup.5 is a hydrogen or halogen atom;Q is the number of double bonds which is equal to 0 or 1;n is an integer of 0 or 1, provided that when Q is 0, n is 1 and when Q is 1, n is 0.
摘要翻译：描述的是下式的化合物：其中A是低级亚烷基; R1是羧基，羟基，低级烷氧基羰基，低级烷氧基羰基氨基，苯基（低级）烷氧基，苯甲酰氧基或低级烷酰氧基; R2是氢或卤素原子或卤代（低级）烷基; R3是氢或卤素原子; R4是羟基，低级烷氧基，低级烷酰氧基或低级烷氧基羰基氧基; R5为氢或卤素原子; Q是等于0或1的双键数; n是0或1的整数，条件是当Q为0时，n为1，当Q为1时，n为0。

8. 发明授权

US4436726A N-Acylpeptide compound, processes for the preparation thereof and the pharmaceutical compositions 失效
标题翻译： N-酰基肽化合物，其制备方法和药物组合物
公开(公告)号：US4436726A
公开(公告)日：1984-03-13
申请号：US329075
申请日：1981-12-09
申请人： Kazuyoshi Umehara , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Keizo Yoshida
发明人： Kazuyoshi Umehara , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Keizo Yoshida
IPC分类号： C12P21/00 , A61K38/00 , A61P7/02 , A61P7/04 , A61P37/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/47 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/28 , C07C237/12 , C07C237/22 , C07K1/113 , C07K1/20 , C07K5/06 , C07K5/062 , C07K14/195 , C07K14/41 , C12R1/20 , C07C103/52 , A61K37/02 , C07C67/02
CPC分类号： C07K5/06026 , A61K38/00
摘要： This invention relates to new N-acylpeptide compounds of immunological activity, said compounds being of the formula: ##EQU1## wherein R.sup.1 and R.sup.2 are each alkyl or alkenyl;R.sup.3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, heterocyclic(lower)alkyl or ar(lower)alkyl, wherein the aryl moiety may have hydroxy or protected hydroxy;R.sup.4 is carboxy, esterified carboxy, carboxy(lower)alkyl or esterified carboxy(lower)alkyl;X is bond or lower alkylene;Y is lower alkylene or lower alkylidene; andn is an integer of 0 to 1;or its pharmaceutically acceptable salt.
摘要翻译：本发明涉及免疫活性的新的N-酰基肽化合物，所述化合物具有下式：其中R 1和R 2各自为烷基或链烯基; R3是氢，低级烷基，羟基（低级）烷基，杂环（低级）烷基或芳（低级）烷基，其中芳基部分可以具有羟基或被保护的羟基; R4是羧基，酯化的羧基，羧基（低级）烷基或酯化的羧基（低级）烷基; X是键或低级亚烷基; Y为低级亚烷基或低级亚烷基; n为0〜1的整数。或其药学上可接受的盐。

9. 发明授权

US4797417A Furanone derivatives, process for preparation thereof and use thereof 失效
标题翻译：呋喃酮衍生物，其制备方法和用途
公开(公告)号：US4797417A
公开(公告)日：1989-01-10
申请号：US31199
申请日：1987-03-27
申请人： Masanori Okamoto , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Masanori Okamoto , Itsuo Uchida , Kazuyoshi Umehara , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： A61K31/34 , A61K31/341 , A61P27/02 , A61P27/12 , C07C43/166 , C07D303/22 , C07D307/33 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04 , C07D307/32 , A61K31/365 , C07D307/34
CPC分类号： C07D303/22 , C07C43/166 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04 , C12R1/645 , Y02P20/55
摘要： The invention relates to novel furanone derivatives, having an aldose reductase-inhibitory activity, of the formula ##STR1## wherein A is a lower alkylene group,R.sup.1 is a carboxy, hydroxy, protected hydroxy or lower alkoxycarbonyl group,R.sup.2 is a hydrogen or halogen atom or a halo (lower) alkyl group, andR.sup.3 is a hydrogen atom or a hydroxy, carboxy, lower alkoxy or lower alkoxycarbonyl group.

10. 发明授权

US4666890A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4666890A
公开(公告)日：1987-05-19
申请号：US380061
申请日：1982-05-20
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/072 , C07K9/00 , C07K5/08 , C07K5/10
CPC分类号： C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06052 , C07K5/06069 , C07K5/06078 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要： The invention relates to novel peptides of enhanced pharmacological activity of the formula: ##STR1## wherein R.sup.1 is alkanoyl;R.sup.2 and R.sup.q are each hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.P is hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above; R.sup.r is hydrogen or amino protective group;m is an integer 1 to 3;or its pharmaceutically acceptable salt.
摘要翻译：本发明涉及增强的药理活性的新肽，其具有下式：其中R1是烷酰基; R 2和R q各自为氢，羧基，被保护的羧基或下式的基团：其中R 2a是单或二羧基（或保护的羧基）低级烷基或芳（羧基或保护的羧基）低级烷基，其芳基部分可以被羟基取代，Rb2是氢或低级烷基; RP是氢，羧基，保护的羧基，条件是当R 2和R q中的一个是氢时，另一个是羧基或被保护的羧基或下式的基团：其中Ra2和Rb2各自如上所定义; Rr为氢或氨基保护基; m为整数1〜3; 或其药学上可接受的盐。

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