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公开(公告)号：US07026352B1
公开(公告)日：2006-04-11
申请号：US10470806
申请日：2002-02-01
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： A61K31/365 , C07D313/00
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it
摘要翻译： 本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。 即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。 梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法
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公开(公告)号：US20060079572A1
公开(公告)日：2006-04-13
申请号：US11213962
申请日：2005-08-30
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： A61K31/365 , C07D313/00
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.
摘要翻译： 本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。 即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。 梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法。
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公开(公告)号：US07667052B2
公开(公告)日：2010-02-23
申请号：US11213962
申请日：2005-08-30
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： C07D313/00 , C07D407/06 , A61K31/365
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.
摘要翻译： 本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。 即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。 梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法。
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公开(公告)号：US07256178B2
公开(公告)日：2007-08-14
申请号：US10522731
申请日：2003-07-31
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
CPC分类号： C07D407/06 , C07D313/00 , C12P17/08 , C12P17/16 , C12P17/162
摘要： Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
摘要翻译： 由以下通式（I）表示的化合物，其药学上可接受的盐或其水合物：其中W表示和R 3，R 7，R 7， SUP> 16，R 17，R 20，R 21和R 21'是 相同或不同，各自表示氢等。由于抑制血管生成并抑制VEGF的产生，特别是在缺氧中，化合物（I）可用作固体癌症的补救措施。
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公开(公告)号：US20050245514A1
公开(公告)日：2005-11-03
申请号：US10522731
申请日：2003-07-31
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
IPC分类号： C07D313/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D407/06 , C12P17/08 , C12P17/16 , A61K31/5377 , A61K31/365 , A61K31/4025 , A61K31/452 , A61K31/496 , C07D413/02 , C07D45/02
CPC分类号： C07D407/06 , C07D313/00 , C12P17/08 , C12P17/16 , C12P17/162
摘要： Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
摘要翻译： 由以下通式（I）表示的化合物，其药学上可接受的盐或其水合物：其中W表示和R 3，R 7，R 7， SUP> 16，R 17，R 20，R 21和R 21'是 相同或不同，各自表示氢等。由于抑制血管生成并抑制VEGF的产生，特别是在缺氧中，所以化合物（I）可用作固体癌的治疗方法。
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公开(公告)号：US07745198B2
公开(公告)日：2010-06-29
申请号：US10532412
申请日：2003-11-27
申请人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
发明人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
CPC分类号： C07D407/06 , A61K31/336 , C12P17/162
摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured myceha and oxygen, and then 11107D substance which is a target material is collected from the treating solution.
摘要翻译： 本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。 作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的肌肉和氧的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。
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公开(公告)号：US20060141589A1
公开(公告)日：2006-06-29
申请号：US10532412
申请日：2003-11-27
申请人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
发明人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
CPC分类号： C07D407/06 , A61K31/336 , C12P17/162
摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured mycelia and oxygen, and then 11107D substance which is a target material is collected from the treating solution.
摘要翻译： 本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。 作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的菌丝体和氧气的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。
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公开(公告)号：US20050131061A1
公开(公告)日：2005-06-16
申请号：US10506976
申请日：2003-03-06
申请人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Tetsuya Someno , Masaaki Ishiduka , Tomio Takeuchi
发明人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Tetsuya Someno , Masaaki Ishiduka , Tomio Takeuchi
IPC分类号： A61P17/06 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D303/32 , C07D493/04 , C12P17/02 , C12P17/18 , C12R1/66 , C12N1/16 , A61K31/336 , C07D303/12
CPC分类号： C07D493/04 , C07D303/32 , C12P17/02 , C12P17/181 , C12R1/66
摘要： Compounds represented by formula (I) below; a process for producing the compounds by culturing a microorganism belonging to the genus Aspergillus and isolating the above-mentioned compounds from the culture; an angiogenesis inhibitory agent containing as an active ingredient the compounds; and an Aspergillus sp. F-1491 (FERM BP-8288) strain capable of producing the compounds. In formula (I), R represents a methyl group or an ethyl group, R1 represents a hydrogen atom, a chlorine atom, a hydroxyl group or a methoxy group, R2 represents a hydroxyl group, or R1 and R2 taken together form an epoxy ring structure.
摘要翻译： 由下式（I）表示的化合物; 通过培养属于曲霉属的微生物并从培养物中分离上述化合物来生产化合物的方法; 含有化合物作为活性成分的血管发生抑制剂; 和曲霉属（Aspergillus sp。） 能够生产化合物的F-1491（FERM BP-8288）菌株。 式（I）中，R表示甲基或乙基，R 1表示氢原子，氯原子，羟基或甲氧基，R 2 O >表示羟基，或R 1和R 2一起形成环氧环结构。
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公开(公告)号：US07060821B2
公开(公告)日：2006-06-13
申请号：US10506975
申请日：2003-03-06
申请人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Kunio Isshiki , Hiroyuki Inoue , Tetsuya Someno , Masaaki Ishizuka , Tomio Takeuchi
发明人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Kunio Isshiki , Hiroyuki Inoue , Tetsuya Someno , Masaaki Ishizuka , Tomio Takeuchi
IPC分类号： C07D498/02 , C07D295/02
CPC分类号： C07D265/38 , C12P17/14 , C12P17/188 , C12R1/645
摘要： A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents —O— and R represents a hydroxyl group, by using a microorganism belonging to the genus Cunninghamella; and a Cunninghamella sp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents —O— or —CH2—, and R represents a hydroxyl group when X represents —O—, or a hydrogen atom when X represents —CH2—.
摘要翻译： 由式（I）表示的化合物; 通过使用属于葫芦科属的微生物，制备式（I）化合物（F-1490物质）的方法，其中X表示-O-，R表示羟基; 和unning ella ella 能够生产物质F-1490的F-1490菌株（FERM BP-8287）; 和破骨细胞分化抑制剂，其含有作为活性成分的式（I）表示的化合物：其中X表示-O-或-CH 2 - ，当X表示-O时，R表示羟基 - 或当X代表-CH 2 - 2时为氢原子。
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公开(公告)号：US20050124050A1
公开(公告)日：2005-06-09
申请号：US10506975
申请日：2003-03-06
申请人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Kunio Isshiki , Hiroyuki Inoue , Tetsuya Someno , Masaaki Sihizuka , Tomio Takeuchi
发明人： Hiroyuki Kumagai , Tomohiro Sameshima , Motoko Matsufuji , Naoto Kawamura , Kunio Isshiki , Hiroyuki Inoue , Tetsuya Someno , Masaaki Sihizuka , Tomio Takeuchi
IPC分类号： A61P19/02 , A61P19/10 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D265/38 , C07D498/04 , C12P17/14 , C12P17/18 , C12P17/16 , C07D498/02 , C12N1/21
CPC分类号： C07D265/38 , C12P17/14 , C12P17/188 , C12R1/645
摘要： A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents —O— and R represents a hydroxyl group, by using a microorganism belonging to the genus Cunninghamella; and a Cunninghamella sp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents —O— or —CH2—, and R represents a hydroxyl group when X represents —O—, or a hydrogen atom when X represents —CH2—.
摘要翻译： 由式（I）表示的化合物; 通过使用属于葫芦科属的微生物，制备式（I）化合物（F-1490物质）的方法，其中X表示-O-，R表示羟基; 和unning ella ella 能够生产物质F-1490的F-1490菌株（FERM BP-8287）; 和破骨细胞分化抑制剂，其含有作为活性成分的式（I）表示的化合物：其中X表示-O-或-CH 2 - ，当X表示-O时，R表示羟基 - 或当X代表-CH 2 - 2时为氢原子。
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