公开(公告)号：US07271147B2

公开(公告)日：2007-09-18

申请号：US10239324

申请日：2001-03-28

申请人： Tomio Takeuchi ,  Hideki Hashizume ,  Masayuki Igarashi ,  Hiroshi Naganawa ,  Masa Hamada

发明人： Tomio Takeuchi ,  Hideki Hashizume ,  Masayuki Igarashi ,  Hiroshi Naganawa ,  Masa Hamada

IPC分类号： A01K31/16 ,  C12P21/06 ,  C12N1/20

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K11/02

摘要： By culturing Lysobacter sp. BMK333-48F3 (deposit number of FERM BP-7477), an antibiotic, tripropeptin Z, tripropeptin A, tripropeptin B, tripropeptin C or tripropeptin D represented by the general formula (I): wherein R is 7-methyl-octyl group, 8-methyl-nonyl group, 9-methyl-dodecyl group, 10-methyl-undecyl group or 11-methyl-dodecyl group, is obtained as antibiotics having excellent antibacterial activities against bacteria and having a novel molecular structure. These tripropeptins each have an excellent antibacterial activity against various bacteria and drug-resistant strains thereof, such as methicillin-resistant strains and vancomycin-resistant strains.

摘要翻译： 通过培养溶菌杆菌 BMK333-48F3（FERM BP-7477的保藏号），抗生素，三聚胰蛋白酶Z，三聚肽A，三聚蛋白B，三抗抑素C或由通式（I）表示的三聚蛋白D：其中R为7-甲基 - 辛基，8 甲基 - 壬基，9-甲基 - 十二烷基，10-甲基 - 十一烷基或11-甲基 - 十二烷基作为对细菌具有优异抗菌活性并具有新的分子结构的抗生素。 这些三柔比星各自对各种细菌和耐药菌株具有优异的抗菌活性，如耐甲氧西林株和万古霉素抗性菌株。

公开(公告)号：US07157268B2

公开(公告)日：2007-01-02

申请号：US10852153

申请日：2004-05-25

申请人： Atsushi Takahashi ,  Kenji Kanbe ,  Tetsuya Mori ,  Yuichi Kita ,  Tsuyoshi Tamamura ,  Tomio Takeuchi

发明人： Atsushi Takahashi ,  Kenji Kanbe ,  Tetsuya Mori ,  Yuichi Kita ,  Tsuyoshi Tamamura ,  Tomio Takeuchi

IPC分类号： C12P19/02 ,  C12N1/20

CPC分类号： C12R1/18 ,  C12P19/02 ,  C12R1/38 ,  C12R1/64

摘要： Provided are novel processes for the efficient production of L-epi-2-inosose and epi-inositol which are useful either as various medicines or intermediates for the syntheses of various medicines. In the processes, inexpensive myo-inositol is used as a starting compound which is reacted with a gram-negative bacterium capable of converting myo-inositol into L-epi-2-inosose, and thereby producing L-epi-2-inosose by conversion of myo-inositol into L-epi-2-inosose. A biologically pure culture of Pseudomonas sp. AB 10215 strain is also provided which has a characteristic nature of being capable of converting myo-inositol into L-epi-2-inosose.

摘要翻译： 提供了用于有效生产L-外 - 二糖和外消旋肌醇的新方法，其可用作各种药物或用于合成各种药物的中间体。 在该方法中，使用廉价的肌醇作为起始化合物，其与能够将肌醇转化为L-外 - 二糖的革兰氏阴性细菌反应，从而通过转化产生L-表二-2-糖 的肌醇变为L-epi-2-inosose。 假单胞菌属的生物纯培养物 还提供了AB 10215菌株，其特征在于能够将肌醇转化为L-表 - 2-inosose。

公开(公告)号：US06780616B1

公开(公告)日：2004-08-24

申请号：US10049970

申请日：2002-05-09

申请人： Tomio Takeuchi ,  Masayuki Igarashi ,  Hiroshi Naganawa ,  Masa Hamada

发明人： Tomio Takeuchi ,  Masayuki Igarashi ,  Hiroshi Naganawa ,  Masa Hamada

IPC分类号： A61K3170

CPC分类号： C07H19/06 ,  C12P17/16 ,  Y10S435/886

摘要： There have been obtained, by cultivation of Streptomyces sp. MK730-62F2 (deposit number of FERM BP-7218), antibiotic caprazamycins A to F having by the following general formula (I) wherein R is tridecyl group, 11-methyl-dodecyl group, and others. These caprazamycins have excellent antibacterial activities against various acid-fast bacteria and various bacteria as well as their drug-resistant strains.

摘要翻译： 已经通过培养链霉菌获得了。 MK730-62F2（FERM BP-7218的保藏号），具有以下通式（I）的抗生素caprazamycins A至F，其中R为十三烷基，11-甲基 - 十二烷基等。 这些caprazamycins对各种耐酸菌和各种细菌以及耐药菌株具有优异的抗菌活性。

公开(公告)号：US06426420B1

公开(公告)日：2002-07-30

申请号：US09610362

申请日：2000-07-05

申请人： Toshio Tsuchida ,  Hazuki Nagai ,  Takashi Nakashima ,  Masashi Yoshida ,  Kaname Konuki ,  Asako Kuroda ,  Kunio Isshiki ,  Tomio Takeuchi

发明人： Toshio Tsuchida ,  Hazuki Nagai ,  Takashi Nakashima ,  Masashi Yoshida ,  Kaname Konuki ,  Asako Kuroda ,  Kunio Isshiki ,  Tomio Takeuchi

IPC分类号： C07D31176

CPC分类号： C07D311/76 ,  C07C67/31 ,  C07C67/343 ,  C07C67/46 ,  C07C69/92 ,  Y02P20/55 ,  C07C69/88

摘要： Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

摘要翻译： 提供了一种制备异香豆素-3-基 - 乙酸衍生物的方法，其特征在于使由式（其中Rc，R2和R主要是保护基团）表示的均苯二甲酸衍生物与由式 （其中，R为低级烷基的有机基团，R3为羧基的保护基，X为卤原子或-OM基）（其中，M为碱金属或碱土金属）。 根据上述方法，可以有效地提供各种异香豆素-3-基 - 乙酸衍生物。

公开(公告)号：US5886167A

公开(公告)日：1999-03-23

申请号：US990461

申请日：1997-12-15

申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

IPC分类号： C07H19/04 ,  C07H19/052 ,  C07H19/16

CPC分类号： C07H19/04 ,  C07H19/052

摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。 此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。 这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。 特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。 此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

公开(公告)号：US5773607A

公开(公告)日：1998-06-30

申请号：US620396

申请日：1996-03-22

申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

IPC分类号： C07H19/04 ,  C07H19/052 ,  C07H1/00 ,  C07H19/00

CPC分类号： C07H19/04 ,  C07H19/052

摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。 此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。 这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。 特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。 此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

公开(公告)号：US5618795A

公开(公告)日：1997-04-08

申请号：US524644

申请日：1995-09-08

申请人： Shinichi Kondo ,  Seiji Shibahara ,  Takayuki Usui ,  Toshiaki Kudo ,  Shuichi Gomi ,  Atsushi Tamura ,  Yoko Ikeda ,  Daishiro Ikeda ,  Tomio Takeuchi

发明人： Shinichi Kondo ,  Seiji Shibahara ,  Takayuki Usui ,  Toshiaki Kudo ,  Shuichi Gomi ,  Atsushi Tamura ,  Yoko Ikeda ,  Daishiro Ikeda ,  Tomio Takeuchi

IPC分类号： C07H15/236 ,  A61K31/70

CPC分类号： C07H15/234

摘要： As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

摘要翻译： 现在提供新的二卡辛衍生物和新的阿贝卡星衍生物2' - 氨基-2' - 脱氧胆碱，2“ - 氨基-5,2” - 脱氧胆酸，2“ - 氨基-2'-脱氧阿糖胞苷，2 “ - 氨基-5,2” - 双脱氧肉豆蔻素，2“ - 氨基-5,2” - 双脱氧-5-表 - 氟代贝卡星和2“ - 氨基-5,2” - 双脱氧-5-表 所有这些都表现出对各种革兰氏阳性和革兰氏阴性细菌的高抗菌活性，包括耐甲氧西林金黄色葡萄球菌等抗性细菌，对哺乳动物毒性低，可用作细菌治疗的抗菌剂 感染。

公开(公告)号：US5527820A

公开(公告)日：1996-06-18

申请号：US356267

申请日：1995-01-20

申请人： Masaaki Ishizuka ,  Mitsuhiro Ueno ,  Hironobu Iinuma ,  Hiroshi Naganawa ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

发明人： Masaaki Ishizuka ,  Mitsuhiro Ueno ,  Hironobu Iinuma ,  Hiroshi Naganawa ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

IPC分类号： C07D207/36 ,  C07D207/38 ,  C07D209/96 ,  C12P17/10 ,  A61K31/40

CPC分类号： C07D207/38 ,  C07D207/36 ,  C07D209/96 ,  C12P17/10

摘要： As new antibiotics are obtained delaminomycins A, B and C having a formula (I) or (I') shown below, or salts thereof. Delaminomycins preferentially inhibit T cells and are useful as immunosuppressants, antineoplastic agents and antibacterial agents. ##STR1## wherein X is a hydroxyl group for delaminomycin A, a methoxy group for delaminomycin B and a hydrogen atom for delaminomycin C.

摘要翻译： PCT No.PCT / JP93 / 00845 Sec。 371 1995年1月20日第 102（e）日期1995年1月20日PCT提交1993年6月22日PCT公布。 公开号WO94 / 00430 日期为1994年6月1日。作为新抗生素，得到具有下式（I）或（I'）的脱氨霉素A，B和C或其盐。 脱氨霉素优先抑制T细胞，可用作免疫抑制剂，抗肿瘤剂和抗菌剂。 （I）其中X是脱氨基霉素A的羟基，德拉霉素B的甲氧基和脱氨基霉素C的氢原子。

公开(公告)号：US5359138A

公开(公告)日：1994-10-25

申请号：US905792

申请日：1992-06-29

申请人： Tomio Takeuchi ,  Takaaki Aoyagi ,  Masa Hamada ,  Hiroshi Naganawa ,  Keiji Ogawa ,  Machiko Nagai ,  Yasuhiko Muraoka ,  Makoto Tsuda

发明人： Tomio Takeuchi ,  Takaaki Aoyagi ,  Masa Hamada ,  Hiroshi Naganawa ,  Keiji Ogawa ,  Machiko Nagai ,  Yasuhiko Muraoka ,  Makoto Tsuda

IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  C07C229/00 ,  A61K37/00 ,  A61K37/02 ,  C07K5/00

CPC分类号： C07K5/0202 ,  C07K7/02 ,  A61K38/00

摘要： A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.

摘要翻译： 已经从属于链霉菌的微生物的培养基中分离出一种新的生物活性物质，后抑制素。 该新物质是具有新结构的肽化合物，其中肽链具有酮基。 因此，物质具有高内肽酶抑制活性。 可以在肽链中化学合成具有酮基的后抑制素相关化合物。 这些化合物还具有内肽酶抑制活性。

公开(公告)号：US5098935A

公开(公告)日：1992-03-24

申请号：US524576

申请日：1990-05-17

申请人： Masaaki Ishizuka ,  Takashi Yamashita ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Kunio Isshiki ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

发明人： Masaaki Ishizuka ,  Takashi Yamashita ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Kunio Isshiki ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

IPC分类号： A61K31/195 ,  A61P35/00 ,  C07C235/12 ,  C12N1/20 ,  C12P13/02 ,  C12R1/465

CPC分类号： C12R1/465 ,  C07C235/12 ,  C12P13/02

摘要： A new antibiotic, named Conagenin, is provided which can exhibit useful carcinostatic or antitumor activities on carcinomas and tumors, particularly malignant tumors, of mammalian animals including man. Conagenin can be produced by fermentation of microorganisms of genus Streptomyces, typically Streptomyces roseosporus MI696-AF3 strain identified under the deposit number FERM BP-2738. Conagenin has formula (I) and is useful for medicinal purposes, particularly as carcinostatic agent or antitumor agent for inhibiting carcinomas and malignant tumors of mammalian animals, including man.