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1. 发明授权

US5883121A Epoxysuccinamide derivative or salt thereof, and medicine comprising the same 失效
标题翻译：环氧琥珀酰胺衍生物或其盐，以及含有它们的药物
公开(公告)号：US5883121A
公开(公告)日：1999-03-16
申请号：US894050
申请日：1997-08-12
申请人： Tomohiro Yamashita , Yoshimitsu Suda , Yukio Tada , Nobuhiko Katunuma , Tetsuji Asao
发明人： Tomohiro Yamashita , Yoshimitsu Suda , Yukio Tada , Nobuhiko Katunuma , Tetsuji Asao
IPC分类号： C07D303/48 , A61K31/335 , C07D303/46
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and independently represent H or an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring together with the adjacent nitrogen atoms, R.sup.3 is H or an acyl group, R.sup.4 is H or an aralkyl group, and R.sup.5 is an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.5 may form an amino acid residue, which may be protected, together with the adjacent nitrogen atom, or a salt thereof, and a medicine comprising the derivative as an active ingredient; and this compound has an inhibiting activity against cathepsin, and particularly, specifically inhibits cathepsin L and is hence useful for prevention and treatment of osteopathy such as osteoporosis.
摘要翻译： PCT No.PCT / JP96 / 03603 Sec。 371日期：1997年8月12日 102（e）日期1997年8月12日PCT 1996年12月10日PCT PCT。出版物WO97 / 21694 日期：1996年6月19日本发明涉及由通式（1）表示的环氧琥珀酰胺衍生物彼此不同，独立地表示H或可被取代的芳香族烃基或芳烷基，或者R 1和R 2可以形成含氮杂环与相邻的氮原子一起，R3是H或酰基，R4是H或芳烷基，R5是可被取代的芳族烃基或芳烷基，或R5可以形成氨基酸残基，其中可以与相邻的氮原子或其盐一起保护，以及包含该衍生物作为活性成分的药物; 并且该化合物对组织蛋白酶具有抑制活性，特别是抑制组织蛋白酶L，因此可用于预防和治疗骨质疏松症等骨病。

2. 发明授权

US6110967A Epoxysuccinamide derivative or salt thereof 失效
标题翻译：环氧琥珀酰胺衍生物或其盐
公开(公告)号：US6110967A
公开(公告)日：2000-08-29
申请号：US202607
申请日：1998-12-17
申请人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
发明人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
IPC分类号： C07D303/40 , C07D303/48 , A61K31/495 , A61K31/41 , A61K31/435
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl or aminoalkyl group, R.sup.2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R.sup.3 and R.sup.4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.
摘要翻译： PCT No.PCT / JP98 / 01778 Sec。 371日期1998年12月17日第 102（e）1998年12月17日日期PCT提交1998年4月17日PCT公布。第WO98 / 47887号公报日期：1998年10月29日本发明涉及由式（I）表示的环氧琥珀酰胺衍生物：其中R1表示氢原子，烷基或氨基烷基，R2表示可以被取代的氨基烷基，可以被取代的芳基，可以被取代的杂环基，可以被取代的芳烷基或被可被取代的杂环取代的烷基，或者可以被R 1和R 2形成可以被取代的含氮杂环，和相邻的氮原子和R3和R4彼此相同或不同，并且独立地表示氢原子或烷基或芳烷基或其盐，其制备方法和包含这种衍生物或盐的药物作为活性成分。该化合物对组织蛋白酶L及其家族酶具有特异性抑制活性，可用作预防和治疗代谢性骨病如骨质疏松症和高钙血症的药剂。

3. 发明授权

US07067476B2 Peptide derivative, and pharmaceutically acceptable salt thereof, process for producing the same, and use thereof 失效
标题翻译：肽衍生物及其药学上可接受的盐，其制备方法及其用途
公开(公告)号：US07067476B2
公开(公告)日：2006-06-27
申请号：US10493060
申请日：2002-11-14
申请人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
发明人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
IPC分类号： A01N61/00 , A61K38/00
CPC分类号： C07C279/36 , Y02P20/55
摘要： The present invention provides a peptide derivative of formula (I) or a pharmaceutically acceptable salt thereof wherein X is —CH(OH)— or —CO—; R1 is hydrogen or an amino protecting group; R2 is hydroxyl or lower alkoxy; one of R3 and R4 is the side chain (R group) of lysine the amino group of which may be protected with a protecting group and the other of R3 and R4 is the side chain (R group) of arginine the guanidino group of which may be protected with a protecting group; and R5 and R6 may be the same or different and are hydrogen, lower alkyl or aralkyl. The present invention further provides a production process and use thereof.
摘要翻译：本发明提供式（I）的肽衍生物或其药学上可接受的盐，其中X为-CH（OH） - 或-CO-; R 1是氢或氨基保护基; R 2是羟基或低级烷氧基; R 3和R 4之一是赖氨酸的侧链（R基团），其氨基可被保护基保护，另一个R ^{3和R 4是其胍基可被保护基保护的精氨酸的侧链（R基团）; R 5和R 6可以相同或不同，为氢，低级烷基或芳烷基。本发明还提供了一种制备方法及其用途。}

4. 发明授权

US06951843B2 Peptide derivatives and their pharmaceutically acceptable salts, thereof, processes for preparation of both and use thereof 失效
标题翻译：肽衍生物及其药学上可接受的盐，其制备方法及其用途
公开(公告)号：US06951843B2
公开(公告)日：2005-10-04
申请号：US10168540
申请日：2001-11-02
申请人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
发明人： Kenji Yamamoto , Yoshimitsu Suda , Tetsuji Asao
IPC分类号： A61K38/00 , A61P1/02 , A61P43/00 , C07C271/22 , C07D295/185 , C07K5/072 , C07K5/093
CPC分类号： C07D295/185 , A61K38/00 , C07C271/22 , C07K5/06104 , C07K5/0819 , Y02P20/55
摘要： The present invention provides a peptide derivative of formula (I) wherein X is —CHOH— or —CO—; R1 and R2 are hydrogen or substituted oxycarbonyl; R3 is substituted oxycarbonyl; R4 is hydroxyl, lower alkoxy, optionally substituted piperazinyl or the like; R5 is a R-group side chain of an α-amino acid optionally protected by a protective group, R6 is hydroxyl, lower alkoxy or the like; m is 0 or 1; and n is an integer of 2 to 6; or a pharmaceutically acceptable salt thereof. The present invention further provides a production process and use thereof.
摘要翻译：本发明提供式（I）的肽衍生物，其中X是-CHOH-或-CO-; R 1和R 2是氢或取代的氧羰基; R 3是取代的氧羰基; R 4是羟基，低级烷氧基，任选取代的哌嗪基等; R 5是任选被保护基保护的α-氨基酸的R基侧链，R 6是羟基，低级烷氧基等; m为0或1; n为2〜6的整数。或其药学上可接受的盐。本发明还提供了一种制备方法及其用途。

5. 发明授权

US06294535B1 Uracil derivatives and antitumor effect potentiator and antitumor agent containing the same 有权
标题翻译：尿嘧啶衍生物和抗肿瘤作用增强剂和抗肿瘤药含有相同的作用
公开(公告)号：US06294535B1
公开(公告)日：2001-09-25
申请号：US09457668
申请日：1999-12-09
申请人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
发明人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
IPC分类号： A61K31535
CPC分类号： C07D239/54 , C07D231/12 , C07D233/56 , C07D239/553 , C07D249/08 , C07D403/06 , C07D403/12
摘要： The invention relates to novel uracil derivatives having excellent inhibiting effects on human derived thymidine phosphorylates and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators and antitumor agents containing such novel compounds, and a process for their preparation and use are described. The novel uracil derivative compounds are represented by the general formula (1′):
摘要翻译：本发明涉及对人衍生的胸苷磷酸酯具有优异抑制作用的新型尿嘧啶衍生物和抗肿瘤活性。描述了含有这些新化合物的药物组合物，抗肿瘤增强剂和抗肿瘤剂及其制备和使用方法。新型尿嘧啶衍生物化合物由通式（1'）表示：

6. 发明授权

US6159969A Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same 失效
标题翻译：尿嘧啶衍生物，抗肿瘤效果增强剂和抗肿瘤药含有相同的作用
公开(公告)号：US6159969A
公开(公告)日：2000-12-12
申请号：US6009
申请日：1998-01-12
申请人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
发明人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
IPC分类号： C07D239/54 , C07D239/553 , C07D403/06 , C07D403/12 , C07D521/00 , A61K31/535 , C07D239/02 , C07D401/00 , C07D413/00
CPC分类号： C07D239/54 , C07D231/12 , C07D233/56 , C07D239/553 , C07D249/08 , C07D403/06 , C07D403/12
摘要： The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described. The novel compounds satisfy the general formula (1): ##STR1##
摘要翻译：本发明涉及具有优异的人衍生胸苷磷酸化酶抑制作用的新型尿嘧啶衍生物和抗肿瘤活性。描述了药物组合物，抗肿瘤增强剂，含有这些新化合物的抗肿瘤剂及其制备和使用方法。新化合物满足通式（1）：

7. 发明授权

US5744475A Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same 失效
标题翻译：尿嘧啶衍生物，抗肿瘤效果增强剂和抗肿瘤药含有相同的作用
公开(公告)号：US5744475A
公开(公告)日：1998-04-28
申请号：US737677
申请日：1996-11-21
申请人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
发明人： Shingo Yano , Yukio Tada , Hideki Kazuno , Tsutomu Sato , Junichi Yamashita , Norihiko Suzuki , Tomohiro Emura , Masakazu Fukushima , Tetsuji Asao
IPC分类号： C07D239/54 , C07D239/553 , C07D403/06 , C07D403/12 , C07D521/00 , A01N43/54 , A01N43/64 , C07D239/00 , C07D239/02
CPC分类号： C07D239/54 , C07D231/12 , C07D233/56 , C07D239/553 , C07D249/08 , C07D403/06 , C07D403/12
摘要： The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described. The novel compounds satisfy the general formula (1): ##STR1##
摘要翻译： PCT No.PCT / JP96 / 00828 Sec。 371日期：1996年11月21日 102（e）1996年11月21日PCT PCT 1996年3月28日PCT公布。公开号WO96 / 30346 日期：1996年10月3日本发明涉及具有优异的人衍生胸苷磷酸化酶抑制作用的新型尿嘧啶衍生物和抗肿瘤活性。描述了药物组合物，抗肿瘤增强剂，含有这些新化合物的抗肿瘤剂及其制备和使用方法。新化合物满足通式（1）：（1）

8. 发明授权

US5733918A Condensed-Indan derivatives and pharmaceutically acceptable salts thereof 失效
标题翻译：缩合 - 茚满衍生物及其药学上可接受的盐
公开(公告)号：US5733918A
公开(公告)日：1998-03-31
申请号：US578542
申请日：1996-01-19
申请人： Shinji Okazaki , Tetsuji Asao , Motoji Wakida , Keisuke Ishida , Masato Washinosu , Teruhiro Utsugi , Yuji Yamada
发明人： Shinji Okazaki , Tetsuji Asao , Motoji Wakida , Keisuke Ishida , Masato Washinosu , Teruhiro Utsugi , Yuji Yamada
IPC分类号： A61K31/44 , A61K31/473 , A61P35/00 , C07D221/18 , C07D401/12 , C07D491/04 , C07D491/056 , C07D521/00 , A61K31/47 , C07D491/56
CPC分类号： C07D231/12 , C07D221/18 , C07D233/56 , C07D249/08 , C07D401/12 , C07D491/04
摘要： A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## wherein ring A represents an optionally substituted benzene ring or naphthalene ring, or a benzene ring having a lower alkylenedioxy group, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR=N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.3 represents a lower alkyl group optionally substituted by a substituted amino group, except when R represents an optionally substituted nitrogen-containing heterocyclic group; ring A and ring B are a benzene ring having no substituent group.
摘要翻译： PCT No.PCT / JP95 / 00944 Sec。 371日期1996年1月19日 102（e）日期1996年1月19日PCT提交1995年5月18日PCT公布。出版物WO95 / 32187 日期：1995年11月30日由式（1）表示的缩合 - 缩水甘油衍生物及其药学上可接受的盐：其中环A表示任选取代的苯环或萘环，或具有低级亚烷基二氧基基团，环B表示任选取代的苯环或具有较低亚烷基二氧基的苯环。 Y表示-N = CR-或-CR = N-，R表示-NR1R2基，任选取代的含氮杂环基或-OR 3基，其中R1和R2相同或不同，各自为氢原子 ; 苯基; 任选取代的含氮杂环基; 或可以被选自任选取代的氨基，低级烷氧基，苯基，含氮杂环基，被低级烷基取代的氧化胺基中的至少一种取代的低级烷基基团或羟基; R3表示任选被取代的氨基取代的低级烷基，除了当R表示任意取代的含氮杂环基时; 环A和环B是没有取代基的苯环。

9. 发明授权

US4897503A 1,1,2-triaryl-1-alkene derivatives 失效
标题翻译： 1,1,2-三芳基-1-烯烃衍生物
公开(公告)号：US4897503A
公开(公告)日：1990-01-30
申请号：US159590
申请日：1988-01-27
申请人： Tetsuji Asao , Setsuo Takeda , Yoshikazu Sugimoto , Toshiyuki Toko , Yuji Yamada , Kazuo Ogawa , Norio Unemi
发明人： Tetsuji Asao , Setsuo Takeda , Yoshikazu Sugimoto , Toshiyuki Toko , Yuji Yamada , Kazuo Ogawa , Norio Unemi
IPC分类号： C07F9/12
CPC分类号： C07F9/12
摘要： This invention provides a 1,1,2-triaryl-1-butene derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, one of R.sub.3 and R.sub.4 is a lower alkyl group and the other is a group of the formula ##STR2## (in which R.sub.5 is a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom or --OPO(OH).sub.2 group); or a pharmacologically acceptable salt thereof, its preparation and agents containing the derivative for treating mammary cancer and anovulatory infertility.

10. 发明授权

US5763453A Condensed indan derivatives and salts thereof 失效
标题翻译：稠合茚满衍生物及其盐
公开(公告)号：US5763453A
公开(公告)日：1998-06-09
申请号：US809602
申请日：1997-04-03
申请人： Shinji Okazaki , Tetsuji Asao , Teruhiro Utsugi , Yuji Yamada
发明人： Shinji Okazaki , Tetsuji Asao , Teruhiro Utsugi , Yuji Yamada
IPC分类号： A61K31/47 , A61K31/473 , A61P35/00 , C07D221/18 , C07D401/04 , C07D491/056
CPC分类号： C07D401/04 , C07D221/18
摘要： A condensed indan derivative represented by the formula (1) ##STR1## wherein the ring A is an optionally substituted benzene ring or a benzene ring which has lower alkylenedioxy group(s), the ring B is an optionally substituted benzene ring or a benzene ring which has lower alkylene dioxy group(s), and R is a group --NR.sub.1 R.sub.2, an optionally substituted nitrogen-containing heterocyclic group, a group --OR.sub.3 or a group --SR.sub.4 (wherein R.sub.1 and R.sub.2 are the same or different and each represent a hydrogen atom, a phenyl group, an optionally substituted nitrogen-containing heterocyclic group, or a lower alkyl group which may be substituted by optionally substituted amino group(s), lower alkoxy group(s), phenyl group(s), nitrogen-containing heterocyclic group(s) or hydroxyl group(s), and R.sub.3 and R.sub.4 each represent a lower alkyl group which may be substituted by substituted amino group(s)), provided that at least one of the rings A and B is a substituted benzene ring and R is not --NHCH.sub.3, and salts thereof, and medical use of said derivative and salts.
摘要翻译： PCT No.PCT / JP96 / 02195 Sec。 371日期1997年4月3日 102（e）日期1997年4月3日PCT提交1996年8月2日PCT公布。公开号WO97 / 06145 日本公报1997年2月20日由式（1）表示的缩合茚满衍生物（1）其中环A为任选取代的苯环或具有低亚烷基二氧基的苯环，环B为任选取代的苯环或具有低级亚烷基二氧基的苯环，R为基团-NR1R2，任选取代的含氮杂环基，-OR3基或-SR4基（其中R1和R2为相同或不同，各自表示氢原子，苯基，任选取代的含氮杂环基或可被任选取代的氨基取代的低级烷基，低级烷氧基，苯基基团，含氮杂环基或羟基，R 3和R 4各自表示可以被取代的氨基取代的低级烷基），条件是至少一个环A和B是取代的苯环，R不是-NHCH 3及其盐，以及所述衍生物和盐的医疗用途。

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