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11. 发明申请

US20060035875A1 Remedy for hormone-dependent cancer 审中-公开
标题翻译：补充激素依赖性癌症
公开(公告)号：US20060035875A1
公开(公告)日：2006-02-16
申请号：US10531099
申请日：2003-10-09
申请人： Yukimasa Shiotsu , Hiroyuki Ishida , Chikara Murakata , Hideaki Kusaka , Shiro Akinaga
发明人： Yukimasa Shiotsu , Hiroyuki Ishida , Chikara Murakata , Hideaki Kusaka , Shiro Akinaga
IPC分类号： A61K31/56
CPC分类号： A61K31/567 , A61K45/06 , A61K2300/00
摘要： A therapeutic agent for a hormone-dependent cancer, which comprises (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy, which may be administered together or separately at an interval, is provided. A method for treating a hormone-dependent cancer, which comprises administering (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy together or separately at an interval, is also provided. A steroid-sulfatase inhibitor which is used in combination with an agent for hormone therapy and/or an agent for chemotherapy, and which is administered together therewith or separately therefrom at an interval, is also provided. A kit for treating a hormone-dependent cancer, which comprises a first component comprising (a) a steroid-sulfatase inhibitor and a second component comprising (b) an agent for hormone therapy and/or an agent for chemotherapy, is also provided. A pharmaceutical composition, which comprises (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy, is also provided. Further, use of (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy for the manufacture of a therapeutic agent for a hormone-dependent cancer is provided.
摘要翻译：提供激素依赖性癌症的治疗剂，其包含（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗药物和/或化疗药剂，其可以一个或一个间隔一起施用或分开施用。还提供了一种用于治疗激素依赖性癌症的方法，其包括一次或一次间隔地施用（a）类固醇 - 硫酸酯酶抑制剂和（b）用于激素治疗的药剂和/或化学药剂。还提供了与激素治疗药物和/或化学药剂组合使用的类固醇 - 硫酸酯酶抑制剂，并且其间隔一起或与其一起施用。还提供了一种用于治疗激素依赖性癌症的试剂盒，其包含第一组分，其包含（a）类固醇 - 硫酸酯酶抑制剂和第二组分，所述第二组分包含（b）激素治疗剂和/或化学药剂。还提供了一种药物组合物，其包含（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗剂和/或化疗剂。此外，提供了（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗剂和/或化疗剂用于制造激素依赖性癌症治疗剂的用途。

12. 发明授权

US5624926A Piperidinyl-dioxoquinazolines as adenosine reuptake inhibitors 失效
标题翻译：哌啶基 - 二氧喹唑啉作为腺苷再摄取抑制剂
公开(公告)号：US5624926A
公开(公告)日：1997-04-29
申请号：US318876
申请日：1994-10-17
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , A61K31/50 , A61K31/505
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译： PCT No.PCT / JP94 / 00229 Sec。 371日期：1994年10月17日 102（e）日期1994年10月17日PCT 1994年2月16日PCT PCT。 WO94 / 19342 PCT公开号日期：1994年9月1日本发明涉及一种腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物式（I）：其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，羟基，低级烷氧基，低级烷硫基，羧基，低级烷氧基羰基，低级烷酰基，芳烷氧基或低级烷酰氧基; R 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

13. 发明申请

US20100029625A1 Therapeutic Agent for Restenosis 失效
标题翻译：再狭窄治疗剂
公开(公告)号：US20100029625A1
公开(公告)日：2010-02-04
申请号：US11993757
申请日：2006-06-22
申请人： Ryuichiro Nakai , Emi Shimoike , Hideaki Kusaka , Chikara Murakata , Yoshinori Yamashita
发明人： Ryuichiro Nakai , Emi Shimoike , Hideaki Kusaka , Chikara Murakata , Yoshinori Yamashita
IPC分类号： A61K31/433 , C07D285/135 , C07D417/12 , C07D491/056 , A61K31/506 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/438 , A61P9/00
CPC分类号： A61K31/433 , C07D285/12 , C07D285/135 , C07D417/12 , C07D491/10
摘要： A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].
摘要翻译：用于再狭窄的治疗和/或预防剂，其包含由通式（0）表示的噻二唑啉衍生物或其药学上可接受的盐：[其中，n表示1至3的整数，R 0表示芳基，-NR 1 CONR 2（式中，R 1表示氢原子等，R 2表示低级烷基等），R 3表示低级烷基，R 4表示氢原子等，R 5表示芳基等。

14. 发明申请

US20060193772A1 Drugs for treating cancer 审中-公开
标题翻译：用于治疗癌症的药物
公开(公告)号：US20060193772A1
公开(公告)日：2006-08-31
申请号：US10573528
申请日：2004-09-24
申请人： Atsushi Ochiai , Hideaki Kusaka , Tadakazu Akiyama
发明人： Atsushi Ochiai , Hideaki Kusaka , Tadakazu Akiyama
IPC分类号： A61K51/00 , A61K39/395
CPC分类号： A61K31/351 , A61K45/06 , A61K2300/00
摘要： The invention aims to provide a medicament for treating cancer in which a cancer therapeutic effect is synergistically increased using a substance inhibiting activities of insulin-like growth factor-I (IGF-I) and insulin-like growth factor-II (IGF-II). According to the invention, there are provided a medicament for treating cancer which comprises a substance inhibiting activities of IGF-I and IGF-II and which is administered in combination with irradiation; and a medicament for treating cancer comprising a combination of a substance inhibiting activities of IGF-I and IGF-II and a substance having an antitumor activity.
摘要翻译：本发明旨在提供一种治疗癌症的药物，其中使用胰岛素样生长因子-I（IGF-I）和胰岛素样生长因子-II（IGF-II）的抑制活性的物质协同增加癌症治疗效果，。根据本发明，提供了一种治疗癌症的药物，其包含IGF-I和IGF-II的抑制活性的物质，并与照射组合施用; 以及用于治疗癌症的药物，其包含IGF-1和IGF-II的物质抑制活性和具有抗肿瘤活性的物质的组合。

15. 发明授权

US5658917A Isoquinolines having adenosine uptake inhibitor activity 失效
标题翻译：具有腺苷摄取抑制剂活性的异喹啉
公开(公告)号：US5658917A
公开(公告)日：1997-08-19
申请号：US430234
申请日：1995-04-28
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , A61K31/445 , A61K31/50 , A61K31/505
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含由式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物：（I）其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，羟基，低级烷氧基，低级烷硫基，羧基，低级烷氧基羰基，低级烷酰基，芳烷氧基或低级烷酰氧基; R 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

16. 发明授权

US5605900A Benzotriazines having adenosine uptake inhibitor activity 失效
标题翻译：具有腺苷摄取抑制剂活性的苯并三嗪
公开(公告)号：US5605900A
公开(公告)日：1997-02-25
申请号：US430227
申请日：1995-04-28
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , C07D401/04 , A61K31/445 , A61K31/50 , A61K31/53
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含由式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物：（I）其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，羟基，低级烷氧基，低级烷硫基，羧基，低级烷氧基羰基，低级烷酰基，芳烷氧基或低级烷酰氧基; R 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

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