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1. 发明授权

US06656905B1 Cyclic tetrapeptide compound and use thereof 失效
标题翻译：环状四肽化合物及其用途
公开(公告)号：US06656905B1
公开(公告)日：2003-12-02
申请号：US09806500
申请日：2001-05-04
申请人： Hiroaki Mori , Kazutoshi Sakamoto , Yasuhisa Tsurumi , Shigehiro Takase , Motohiro Hino
发明人： Hiroaki Mori , Kazutoshi Sakamoto , Yasuhisa Tsurumi , Shigehiro Takase , Motohiro Hino
IPC分类号： A61K3807
CPC分类号： A61K38/12 , C07K5/126
摘要： A cyclic tetrapeptide compound and use thereof. Especially, a compound WF27082, a process for production of the compound by culturing, in a nutrient medium, a WF27082-producing strain belonging to Acremonium and recovering the compound from a culture broth, a pharmaceutical composition containing the compound as an active ingredient, in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound for use as a medicament, a use of the compound for manufacture of a medicament for inhibiting histone deacetylase, a use of the compound for manufacture of a medicament for treating or preventing inflammatory disorders, diabetes, diabetic complications, homozygous thalassemia, fibrosis, cirrhosis, acute promyelocytic leukaemia (APL), protozoal infections, organ transplant rejections, autoimmune diseases, or tumors, a use of histone deacetylase inhibitors as an immunosuppressant or an antitumor agent, and a use of histone deacetylase inhibitors for manufacture of a medicament for treating or preventing organ transplant rejections, autoimmune diseases or tumors are described.
摘要翻译：一种环状四肽化合物及其用途。特别地，化合物WF27082是通过在营养培养基中培养属于顶孢菌属的WF27082产生菌株并从培养液中回收化合物，将含有该化合物作为活性成分的药物组合物生产化合物的方法，与药学上可接受的，基本上无毒的载体或赋形剂的相关联，用作药物的化合物，该化合物用于制备用于抑制组蛋白脱乙酰酶的药物的用途，该化合物用于制备用于治疗或预防炎性疾病，糖尿病，糖尿病并发症，纯合地中海贫血，纤维化，肝硬化，急性早幼粒细胞白血病（APL），原生动物感染，器官移植排斥，自身免疫疾病或肿瘤，组蛋白脱乙酰酶抑制剂作为免疫抑制剂或抗肿瘤剂的用途，以及使用组蛋白脱乙酰酶抑制剂来制造用于治疗或预防的药物描述器官移植排斥，自身免疫性疾病或肿瘤。

2. 发明授权

US07314719B2 Method for increasing productivity of secondary metabolite by conferring drug-resistant mutations 有权
标题翻译：通过赋予耐药性突变来提高次生代谢产物的生产力的方法
公开(公告)号：US07314719B2
公开(公告)日：2008-01-01
申请号：US10473364
申请日：2002-03-29
申请人： Kozo Ochi , Haifeng Hu , Motohiro Hino , Akihiko Fujie , Hideyuki Muramatsu
发明人： Kozo Ochi , Haifeng Hu , Motohiro Hino , Akihiko Fujie , Hideyuki Muramatsu
IPC分类号： G01N33/35 , C12P21/06
CPC分类号： C12N15/01
摘要： This invention relates to a method for increasing the productivity of the secondary metabolite in a micro-organism, for example, the improvement of antibiotic producers by conferring drug-resistant mutations to micro-organisms.
摘要翻译：本发明涉及一种用于提高微生物中次级代谢产物的生产率的方法，例如通过赋予微生物耐药突变来改善抗生素生产者。

3. 发明授权

US06521600B1 Compound, WF002, production thereof and use thereof 失效
标题翻译：化合物，WF002，其制备及其用途
公开(公告)号：US06521600B1
公开(公告)日：2003-02-18
申请号：US09720331
申请日：2001-01-18
申请人： Yasuhiro Hori , Masami Ezaki , Yasuhisa Tsurumi , Shigehiro Takase , Motohiro Hino
发明人： Yasuhiro Hori , Masami Ezaki , Yasuhisa Tsurumi , Shigehiro Takase , Motohiro Hino
IPC分类号： A61K317028
CPC分类号： C12R1/645 , C07J63/008 , C12P19/60 , Y10S435/911
摘要： The present invention provides a new bioactive compound of formula (I), which has an antimicrobial activity against pathogenic microorganisms, and a process for production thereof. Also provided are a pharmaceutical composition comprising the compound and pharmaceutically acceptable carrier, a use of the WF002 as a medicament and use of the compound for manufacture of the medicament for treatment of infectious disease.
摘要翻译：本发明提供了具有抗病原微生物的抗微生物活性的新的式（I）生物活性化合物及其生产方法。还提供了包含该化合物和药学上可接受的载体的药物组合物，该WF002作为药物的用途以及该化合物用于制备用于治疗感染性疾病的药物的用途。

4. 发明授权

US5502033A Antimicrobial polypeptide compound a pharmaceutical composition comprising the same, and a method for treating infectious diseases 失效
标题翻译：抗微生物多肽化合物，包含其的药物组合物和治疗感染性疾病的方法
公开(公告)号：US5502033A
公开(公告)日：1996-03-26
申请号：US218883
申请日：1994-03-28
申请人： Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara
发明人： Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara
IPC分类号： C12N1/14 , A61K38/00 , A61P31/04 , A61P31/10 , C07K1/20 , C07K5/12 , C07K7/56 , C07K14/195 , C07K14/41 , C12P21/04 , C12R1/645 , C07K7/00 , C07K7/06
CPC分类号： C07K7/56 , A61K38/00
摘要： A compound having antimicrobial activity of the following general formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy, R.sup.2 is hydrogen or hydroxy, R.sup.3 is hydroxy or hydroxysulfonyloxy, with proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen, or a phamaceutically acceptable salt thereof. The compound can be used in a method for treating infectious diseases caused by pathogenic microorganism.
摘要翻译：具有以下通式的抗微生物活性的化合物：其中R 1是氢或羟基，R 2是氢或羟基，R 3是羟基或羟基磺酰氧基，条件是当R 1是氢时，R 2是氢或药学上可接受的盐其中。该化合物可用于治疗由病原微生物引起的感染性疾病的方法。

5. 发明授权

US5376634A Polypeptide compound and a process for preparation thereof 失效
标题翻译：多肽化合物及其制备方法
公开(公告)号：US5376634A
公开(公告)日：1994-12-27
申请号：US715961
申请日：1991-06-17
申请人： Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara , Kazuo Sakane , Kohji Kawabata , Hidenori Ohki
发明人： Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara , Kazuo Sakane , Kohji Kawabata , Hidenori Ohki
IPC分类号： A61K38/00 , A61K38/12 , A61P31/04 , A61P31/10 , C07C309/43 , C07K1/06 , C07K7/56 , C07K7/64 , C12P21/04 , C12R1/645 , C07K5/12 , A61K37/02 , C07K7/06
CPC分类号： C07K7/56 , A61K38/00
摘要： A polypeptide compound having antimicrobial activity of the following general formula: ##STR1## wherein R.sup.1 is hydrogen or acyl group, R.sup.2 is hydroxy or acyloxy,R.sup.3 is hydroxysulfonyloxy, andR.sup.4 is hydrogen or carbamoyl,with proviso thatR.sup.1 is not palmitoyl, when R.sup.2 is hydroxy,R.sup.3 is hydroxysulfonyloxy andR.sup.4 is carbamoyl,and a pharmaceutically acceptable salt thereof.
摘要翻译：具有以下通式的抗微生物活性的多肽化合物：其中R1是氢或酰基，R2是羟基或酰氧基，R3是羟基磺酰氧基，R4是氢或氨基甲酰基，条件是R1不是棕榈酰基，当R2 是羟基，R3是羟基磺酰氧基，R4是氨基甲酰基，及其药学上可接受的盐。

6. 发明授权

US5241064A Enzymatic process for preparing optically active 3-substituted azetidinones 失效
标题翻译：用于制备光学活性3-取代的AZETIDINONES的酶法
公开(公告)号：US5241064A
公开(公告)日：1993-08-31
申请号：US587037
申请日：1990-09-24
申请人： Masayoshi Murata , Toshiyuki Chiba , Fumiyuki Shirai , Kenichi Washizuka , Motohiro Hino
发明人： Masayoshi Murata , Toshiyuki Chiba , Fumiyuki Shirai , Kenichi Washizuka , Motohiro Hino
IPC分类号： C07B53/00 , C07D205/08 , C12P7/42 , C12P41/00
CPC分类号： C12R1/07 , C07D205/08 , C12P41/004 , C12P7/42 , Y02P20/55
摘要： Preparation of optically active 3-substituted azetidinones of the formula (I) ##STR1## in which R.sup.1 is a hydroxy-protective group wherein an allylic alcohol of the formula (II) ##STR2## is acylated, then subjected to asymmetric enzymatic hydrolysis yielding the R-allylic alcohol. The hydroxyl group is protected and then stereoselectively reacted with an amine which is subsequently cyclized to yield the desired 3-substituted azetidinone. Two new species of microorganisms have been isolated, Pimelobacter sp. No. 1254 and Bacillus megaterium No. 1253 which exhibit stereoselective esterase activity.

7. 发明授权

US06730776B1 WF14573 or its salt, production thereof and use thereof 失效
标题翻译： WF14573或其盐，其制备及其用途
公开(公告)号：US06730776B1
公开(公告)日：2004-05-04
申请号：US09646342
申请日：2000-09-18
申请人： Yasuhiro Hori , Shigehiro Takase , Yasuhisa Tsurumi , Michizane Hashimoto , Motohiro Hino
发明人： Yasuhiro Hori , Shigehiro Takase , Yasuhisa Tsurumi , Michizane Hashimoto , Motohiro Hino
IPC分类号： C07K750
CPC分类号： C07K7/56 , A61K38/00
摘要： The present invention provides a new antimicrobial compound WF14573, and a process for producing WF14573 by (a) culturing a WF14573A and/or B-producing microorganism in a nutrient medium and recovering WF14573A and/or B from the resultant cultured broth or (b) deacylating WF14573A and/or B in the presence of a microbial substance which is capable of deacylating WF14573A and/or B. Also provided are an antimicrobial agent comprising WF14573 and carrier(s), a pharmaceutical composition comprising an effective amount of WF14573 and pharmaceutically acceptable carrier(s), a method for killing microorganisms by applying WF14573 to the microorganisms, and use of WF14573 for the treatment of infectious diseases caused by pathogenic microorganisms.
摘要翻译：本发明提供了一种新的抗微生物化合物WF14573，以及（a）在营养培养基中培养WF14573A和/或产生B生物的微生物并从所得培养液中回收WF14573A和/或B或（b）生产WF14573的方法，在能够脱酰基WF14573A和/或B的微生物物质存在下脱酰基WF14573A和/或B。还提供了包含WF14573和载体的抗微生物剂，包含有效量的WF14573和药学上可接受的药物组合物载体，通过向微生物施用WF14573杀死微生物的方法，以及使用WF14573来治疗由病原微生物引起的感染性疾病。

8. 依法登记的发明

USH1638H Use of the polypeptide compound 失效
标题翻译：多肽化合物的用途
公开(公告)号：USH1638H
公开(公告)日：1997-03-04
申请号：US311434
申请日：1994-09-26
申请人： Takahisa Furuta , Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara
发明人： Takahisa Furuta , Toshiro Iwamoto , Akihiko Fujie , Kumiko Nitta , Yasuhisa Tsurumi , Nobuharu Shigematsu , Chiyoshi Kasahara , Motohiro Hino , Masakuni Okuhara
IPC分类号： A61K38/12 , C07K7/56 , A61K38/00
CPC分类号： A61K38/12 , C07K7/56
摘要： A pharmaceutical composition comprising an amount of a polypeptide of the formula: ##STR1## wherein R.sup.1 is hydrogen or an acyl group, R.sup.2 is hydroxy or an acyloxy group, R.sup.3 is hydrogen, hydroxy or hydroxysulfonyloxy, R.sup.4 is hydrogen or carbamoyl, and R.sup.5 and R.sup.6 are each hydrogen or hydroxy, with the proviso that (i) R.sup.2 is acyloxy when R.sup.3 is hydrogen, and (ii) R.sup.5 is hydrogen when R.sup.6 is hydrogen, or a pharmaceutically acceptable salt thereof, is useful in the prevention or treatment of Pneumocystis carinii infection.
摘要翻译：一种药物组合物，其包含一定量下式的多肽：其中R 1是氢或酰基，R 2是羟基或酰氧基，R 3是氢，羟基或羟基磺酰氧基，R 4是氢或氨基甲酰基，和R 5和 R6各自为氢或羟基，条件是当R 3为氢时，（ⅰ）R 2为酰氧基，和（ⅱ）R 6为氢时R 5为氢或其药学上可接受的盐可用于预防或治疗肺孢子虫卡利尼病感染。

9. 发明授权

US4605559A Compound, FR-900447, production and use thereof 失效
标题翻译：化合物，FR-900447，其生产和使用
公开(公告)号：US4605559A
公开(公告)日：1986-08-12
申请号：US646090
申请日：1984-08-31
申请人： Yasuhiro Hori , Motohiro Hino , Hiroshi Terano , Masashi Hashimoto , Masanobu Kohsaka
发明人： Yasuhiro Hori , Motohiro Hino , Hiroshi Terano , Masashi Hashimoto , Masanobu Kohsaka
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , A61P35/00 , C07G99/00 , C12N1/20 , C12P1/06 , C12R1/465
CPC分类号： C12P1/06 , H05K1/0298
摘要： The invention relates to a new compound, FR-900447, and pharmaceutically acceptable salts thereof having antimicrobial and antitumor activity, to a pharmaceutically composition thereof, and to a process for production thereof by culturing Streptomyces rubropurpureus FERM BP-584 in nutrient medium under aerobic condition.
摘要翻译：本发明涉及一种具有抗微生物和抗肿瘤活性的新化合物FR-900447及其药学上可接受的盐及其药物组合物，以及通过在需氧条件下在营养培养基中培养罗氏假单胞菌FERM BP-584的方法。

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