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1. 发明授权

US06303797B1 Sesterterpene derivatives exhibiting antifungal activities 失效
标题翻译：表现出抗真菌活性的西萜烯衍生物
公开(公告)号：US06303797B1
公开(公告)日：2001-10-16
申请号：US09744765
申请日：2001-01-30
申请人： Atsushi Hirano , Eiji Sugiyama , Hisao Kondo , Hiroyuki Suda , Hidenori Ogawa , Katsuhisa Kojiri
发明人： Atsushi Hirano , Eiji Sugiyama , Hisao Kondo , Hiroyuki Suda , Hidenori Ogawa , Katsuhisa Kojiri
IPC分类号： C07D30793
CPC分类号： C07D311/94
摘要： A compound represented by the formula [I] wherein Y1 represents an oxygen atom, or a group represented by NH, O—CO, O—SO2, O—CO—NH, O—CS—NH, NH—CO, NH—SO2, NH—CO—NH or NH—CS—NH, R1 represents an alkyl group, an alkenyl group, an alkynyl group, an aryl group, an aralkyl group, an arylalkenyl group, an arylalkynyl group, a cycloalkyl group, a cycloalkylalkyl group, an alkylcarbonyl group, an alkoxycarbonyl group, an arylcarbonyl group or a heterocyclic group, each optionally having a substituent, or a pharmacologically acceptable salt or ester thereof. The compound shows an excellent antifungal activity on fungi on which existing antifungal agents cannot sufficiently display their effects, and thus is useful as an antifungal agent.
摘要翻译：由式[I]表示的化合物，其中Y 1表示氧原子，或由NH，O-CO，O-SO 2，O-CO-NH，O-CS-NH，NH-CO，NH-SO 2表示的基团， NH-CO-NH或NH-CS-NH，R1表示烷基，烯基，炔基，芳基，芳烷基，芳基烯基，芳基炔基，环烷基，环烷基烷基，任选具有取代基的烷基羰基，烷氧基羰基，芳基羰基或杂环基，或其药理学上可接受的盐或酯。该化合物对现有的抗真菌剂不能充分显示其效果的真菌显示出优异的抗真菌活性，因此可用作抗真菌剂。

2. 发明授权

US6087390A Derivatives of antifungal substance BE-31405 and process for producing the same 失效
标题翻译：抗真菌物质BE-31405的衍生物及其制备方法
公开(公告)号：US6087390A
公开(公告)日：2000-07-11
申请号：US423643
申请日：1999-11-18
申请人： Atsushi Hirano , Koichiro Torigoe , Hidenori Ogawa , Seigo Kamiya , Hiromasa Okada , Masao Nagashima , Katsuhisa Kojiri , Hiroyuki Suda
发明人： Atsushi Hirano , Koichiro Torigoe , Hidenori Ogawa , Seigo Kamiya , Hiromasa Okada , Masao Nagashima , Katsuhisa Kojiri , Hiroyuki Suda
IPC分类号： C07H15/18 , A61K31/35 , C07D311/02
CPC分类号： C07H15/18
摘要： The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which is not substituted, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which has substituent(s), or a group represented by --Y--R.sup.3 (provided that when R.sup.2 is a hydrogen atom, R.sup.1 is not a methyl group or an acetyl group; when R.sup.2 is an acetyl group, R.sup.1 is not a methyl group), an antifungal agent containing it as an active ingredient and an antifungal composition containing it and an azole type antifungal agent.
摘要翻译： PCT No.PCT / JP98 / 02218 Sec。 371日期：1999年11月18日 102（e）1999年11月18日日期PCT提交1998年5月20日PCT公布。第WO98 / 52957号公报日本公开日1998年11月26日本发明涉及由通式（I）表示的化合物或其药学上可接受的盐或酯：其中R1和R2各自独立地为氢原子，C1-C16烷基，C2- C10链烯基，C3-C6炔基，C6-C12芳基，C7-C15芳烷基或未被取代的杂环基，C1-C16烷基，C2-C10链烯基，C3- C6炔基，C6-C12芳基，C7-C15芳烷基或具有取代基的杂环基，或由-Y-R3表示的基团（条件是当R2为氢原子时，R1不为甲基或乙酰基;当R 2是乙酰基时，R 1不是甲基），含有它作为活性成分的抗真菌剂和含有它的抗真菌组合物和唑类抗真菌剂。

3. 发明授权

US5589365A Process for producing glycosylated indolopyrrolocarbazole derivatives by culturing certain microorganisms 失效
标题翻译：通过培养某些微生物生产糖基化吲哚并吡咯咔唑衍生物的方法
公开(公告)号：US5589365A
公开(公告)日：1996-12-31
申请号：US381286
申请日：1995-01-31
申请人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
IPC分类号： C07H19/044 , C12P19/28
CPC分类号： C12R1/01 , C07H19/044 , C12P19/28
摘要： A compound of formula (VIII) ##STR1## is added to a culture media containing Microtetraspora sp. A34549 or Saccharothrix aerocolonigenes ATCC 39243. The compound is glycosylated to form an indolopyrrolocarbazole of formula (VII) ##STR2##
摘要翻译：将式（VIII）化合物（VIII）加入到含有微型菌丝孢菌（Microtetraspora sp。）的培养基中。 A34549或产糖酵母（Saccharothrix aerocolonigenes）ATCC 39243。该化合物被糖基化以形成式（VII）的吲哚并吡咯并咔唑（VII）

4. 发明授权

US5804564A Antitumor indolopyrrolocarbazole derivatives 失效
标题翻译：抗肿瘤吲哚并吡咯并咔唑衍生物
公开(公告)号：US5804564A
公开(公告)日：1998-09-08
申请号：US737382
申请日：1996-11-08
申请人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
IPC分类号： C07C243/16 , C07D403/04 , C07D403/14 , C07D487/14 , C07H19/04 , C07H19/044 , A61K31/70 , C07H17/02
CPC分类号： C07D403/04 , C07C243/16 , C07D403/14 , C07D487/14 , C07H19/04 , C07H19/044
摘要： This invention relates to compounds of the general formula ##STR1## or pharmaceutically salts thereof, wherein R.sup.1 and R.sup.2 each represent an OH group, R.sup.1 is located at the 1- or 2-position, R.sup.2 is located at the 10- or 11-position, R.sup.2 is located at the 11-position when R.sup.1 is located at the 1-position, and R.sup.2 is located at the 10-position when R.sup.1 is located at the 2-position. The compounds of the present invention have an excellent antitumor effect and are hence useful as antitumor agents in the field of medicine.
摘要翻译： PCT No.PCT / JP95 / 00868 Sec。 371日期：1996年11月8日 102（e）日期1996年11月8日PCT 1995年5月2日PCT PCT。公开号WO95 / 30682 日本公开公报1995年11月16日本发明涉及通式为“IMAGE”的化合物或其药学上可接受的盐，其中R 1和R 2各自表示OH基，R 1位于1或2位，R 2位于10 - 或11位置，当R1位于1位置时，R2位于11位，当R1位于2位时，R2位于10位。本发明的化合物具有优异的抗肿瘤效果，因此可用作医药领域的抗肿瘤剂。

5. 发明授权

US5643760A Microbial process for preparation of indolopyrrolocarbazole derivatives 失效
标题翻译：制备吲哚并吡咯并咔唑衍生物的微生物工艺
公开(公告)号：US5643760A
公开(公告)日：1997-07-01
申请号：US486640
申请日：1995-06-07
申请人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
IPC分类号： C07H19/044 , C12P19/28 , C12N1/20
CPC分类号： C07H19/044 , C12P19/28 , C12R1/01
摘要： Indolopyrrolocarbazole derivatives, such as, for example, 12,13-dihydro-1,11-dihydroxy-13-(.beta.-D-glucopyranosyl)-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-(6H)-dione or 6-amino derivative thereof, are produced by glycosylating a precursor compound by cultivating with Microtetraspora sp. A34549, Saccharothrix aerocolonigenes ATCC 39243 or mutants thereof, in a nutrient medium containing the precursor compound.
摘要翻译：吲哚并吡咯并咔唑衍生物，例如12,13-二氢-1,11-二羟基-13-（β-D-吡喃葡萄糖基）-5H-吲哚并[2,3-a]吡咯并[3,4-c]咔唑 -5,7-（6H） - 二酮或其6-氨基衍生物，是通过用Microtetraspora sp。 A34549，产糖酵母（Saccharothrix aerocolonigenes）ATCC 39243或其突变体，在含有前体化合物的营养培养基中。

6. 再颁专利

USRE37206E1 Gene encoding glycosyltransferase and its uses 失效
标题翻译：基因编码糖基转移酶及其用途
公开(公告)号：USRE37206E1
公开(公告)日：2001-06-05
申请号：US09337913
申请日：1999-06-22
申请人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
IPC分类号： C12N910
CPC分类号： C12P19/28 , C12N9/1048 , C12P17/182
摘要： This invention relates to glycosyltransferase, genes encoding glycosyltransferase, recombinant vectors having such a gene, host cells transformed with such a recombinant vector, and uses thereof. This invention makes it possible to glycosylate indolopyrrolocarbazole derivatives conveniently and economically.
摘要翻译：本发明涉及糖基转移酶，编码糖基转移酶的基因，具有这种基因的重组载体，用这种重组载体转化的宿主细胞及其应用。本发明使得可以方便和经济地对吲哚吡咯并咔唑衍生物进行糖基化。

7. 发明授权

US5861293A Gene encoding glycosyltransferase and its uses 失效
标题翻译：基因编码糖基转移酶及其用途
公开(公告)号：US5861293A
公开(公告)日：1999-01-19
申请号：US750524
申请日：1996-12-12
申请人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hajime Suzuki , Hisao Kondo , Hiroyuki Suda
IPC分类号： C12N9/10 , C12N15/54 , C12N15/56 , C12P17/18 , C12P19/28 , C12N15/63 , C12P21/02
CPC分类号： C12P19/28 , C12N9/1048 , C12P17/182
摘要： This invention relates to glycosyltransferase, genes encoding glycosyltransferase, recombinant vectors having such a gene, host cells transformed with such a recombinant vector, and uses thereof. This invention makes it possible to glycosylate indolopyrrolocarbazole derivatives conveniently and economically.
摘要翻译： PCT No.PCT / JP95 / 01065 Sec。 371日期：1996年12月12日 102（e）日期1996年12月12日PCT提交1995年5月31日PCT公布。公开号WO95 / 34663 日期1995年12月21日本发明涉及糖基转移酶，编码糖基转移酶的基因，具有这种基因的重组载体，用这种重组载体转化的宿主细胞及其用途。本发明使得可以方便和经济地对吲哚吡咯并咔唑衍生物进行糖基化。

8. 发明授权

US06703373B1 Indolopyrrolocarbazole derivatives and antitumor agents 失效
标题翻译：吲哚吡咯咔唑衍生物和抗肿瘤剂
公开(公告)号：US06703373B1
公开(公告)日：2004-03-09
申请号：US10070825
申请日：2002-03-11
申请人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
IPC分类号： A01N4304
CPC分类号： C07H19/00 , C07H15/00 , C07H19/22
摘要： A compound represented by the formula or a pharmaceutically acceptable salt thereof wherein R represents an unsubstituted pyridyl, furyl or thienyl group, or a pyridyl, furyl or thienyl group each of which has one or more substituents selected from the group consisting of a hydroxyl group, a lower alkoxy group, a hydroxy lower alkyl group and a hydroxy lower alkenyl group except that when the pyridyl, furyl or thienyl group has a lower alkoxy group as a substituent, each of which simultaneously has another substituent selected from the group consisting of a hydroxyl group, a lower alkoxy group, a hydroxy lower alkyl group and a hydroxy lower alkenyl group, m represents an integer of 1 to 3, and G represents a &bgr;-D-glucopyranosyl group, and the positions of substitution of the hydroxyl groups on the indolopyrrolocarbazole ring are the 1- and 11-positions, or the 2- and 10-positions, and an antitumore agent containing it as an effective ingredient. The compounds have a better antitumor action than known compounds having a similar structure.
摘要翻译：由下式表示的化合物或其药学上可接受的盐，其中R表示未取代的吡啶基，呋喃基或噻吩基，或吡啶基，呋喃基或噻吩基，其各自具有一个或多个选自羟基，低级烷氧基，羟基低级烷基和羟基低级烯基，不同之处在于当吡啶基，呋喃基或噻吩基具有低级烷氧基作为取代基时，其各自同时具有选自羟基的另一取代基，低级烷氧基，羟基低级烷基和羟基低级烯基，m表示1〜3的整数，G表示β-D-吡喃葡萄糖基，吲哚并吡咯并唑的羟基取代位置环是1-和11位，或2-和10-位，以及含有它作为有效成分的抗肿瘤剂。化合物具有更好的抗肿瘤比已知具有相似结构的化合物。

9. 发明授权

US5922860A Antitumor indolopyrrolocarbazole derivatives 失效
标题翻译：抗肿瘤吲哚并吡咯并咔唑衍生物
公开(公告)号：US5922860A
公开(公告)日：1999-07-13
申请号：US3602
申请日：1998-01-07
申请人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
IPC分类号： C07C243/16 , C07D403/04 , C07D403/14 , C07D487/14 , C07H19/04 , C07H19/044 , C07H17/02 , C07H19/00 , C07H19/22
CPC分类号： C07D403/04 , C07C243/16 , C07D403/14 , C07D487/14 , C07H19/04 , C07H19/044
摘要： This invention relates to compounds of the general formula ##STR1## or pharmaceutically salts thereof, wherein R.sup.1 and R.sup.2 each represent an OH group, R.sup.1 is located at the 1- or 2-position, R.sup.2 is located at the 10- or 11-position, R.sup.2 is located at the 11-position when R.sup.1 is located at the 1-position, and R.sup.2 is located at the 10-position when R.sup.1 is located at the 2-position. The compounds of the present invention have an excellent antitumor effect and are hence useful as antitumor agents in the field of medicine.
摘要翻译：本发明涉及通式的化合物或其药学上可接受的盐，其中R 1和R 2各自表示OH基，R 1位于1或2位，R 2位于10或11位，R 2为当R1位于1位时位于11位，当R1位于2位时R2位于10位。本发明的化合物具有优异的抗肿瘤效果，因此可用作医药领域的抗肿瘤剂。

10. 发明授权

US5668271A Indolopyrrolocarbazole derivatives 失效
标题翻译：吲哚并吡咯并咔唑衍生物
公开(公告)号：US5668271A
公开(公告)日：1997-09-16
申请号：US474659
申请日：1995-06-07
申请人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
发明人： Katsuhisa Kojiri , Hisao Kondo , Hiroharu Arakawa , Mitsuru Ohkubo , Hiroyuki Suda
IPC分类号： C07H19/044 , C07H19/23 , C07D273/00
CPC分类号： C07H19/044
摘要： Indolopyrrocarbazole derivatives represented by formula (I) and the pharmaceutically acceptable salts thereof have excellent antitumor activity as evidenced by their in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell, ##STR1## wherein R.sup.1 and R.sup.2 independently represent, for example, a hydrogen atom or various hydrocarbon groups which may be substituted or heterocyclic groups which may also be substituted; or a group --Y--R.sup.3 where Y represents a carbonyl group, thiocarbonyl group or sulfonyl group and R.sup.3 represents a hydrogen atom or one of various aliphatic, cycloaliphatic, aryl, nitrogen-containing (e.g. amino, hydrazino, etc) or heterocyclic groups, which groups may be substituted by various substituents; or R.sup.1 and R.sup.2 may combine to represent a lower alkylidene group which may be substituted; or R.sup.1 and R.sup.2, together with the N-atom to which they are bonded form a heterocyclic group which may be substituted;G represents a pentose or hexose group; and X.sup.1 and X.sup.2, independently, represent, for example, hydrogen, halogen, amino, hydroxyl, alkoxy, aryloxy, carboxyl, alkoxycarbonyl or alkyl. These compounds have improved water solubility as compared to rebeccamycin.
摘要翻译：由式（I）表示的吲哚并吡咔唑衍生物及其药学上可接受的盐具有优异的抗肿瘤活性，如通过其对小鼠白血病细胞，人胃癌细胞，人肺癌细胞和人结肠癌细胞的体外增殖抑制活性所证明的。其中R1和R2独立地表示例如氢原子或可以是取代的各种烃基或也可以被取代的杂环基; 或其中Y表示羰基，硫代羰基或磺酰基且R 3表示氢原子或各种脂族，脂环族，芳基，含氮（例如氨基，肼基等）或杂环基之一的基团-Y-R3，哪些基团可以被各种取代基取代; 或者R 1和R 2可以组合以表示可被取代的低级亚烷基; 或R 1和R 2与它们所键合的N-原子一起形成可被取代的杂环基; G表示戊糖或己糖基团; X 1和X 2独立地表示例如氢，卤素，氨基，羟基，烷氧基，芳氧基，羧基，烷氧基羰基或烷基。与雷贝卡霉素相比，这些化合物具有改善的水溶性。

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