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1. 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。

2. 发明授权

US07910611B2 Therapeutic agent for restenosis 失效
标题翻译：再狭窄治疗剂
公开(公告)号：US07910611B2
公开(公告)日：2011-03-22
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： A61K31/41
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。

3. 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。

4. 发明申请

US20080262049A1 Therapeutic Agent for Hematopoietic Tumor 审中-公开
标题翻译：造血肿瘤治疗剂
公开(公告)号：US20080262049A1
公开(公告)日：2008-10-23
申请号：US11909324
申请日：2006-03-22
申请人： Ryuichiro Nakai , Seiho Okamoto , Hideaki Kusaka , Yoshinori Yamashita , Hiroyuki Ishida
发明人： Ryuichiro Nakai , Seiho Okamoto , Hideaki Kusaka , Yoshinori Yamashita , Hiroyuki Ishida
IPC分类号： A61K31/433 , C07D285/08 , A61P35/00 , A61P35/04
CPC分类号： A61K31/433 , A61K31/454 , C07D285/135 , C07D417/04
摘要： A therapeutic and/or prophylactic agent for a hematopoietic tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof:[Formula 1] [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.
摘要翻译：包含通式（I）表示的噻二唑啉衍生物或其药学上可接受的盐的造血肿瘤的治疗和/或预防剂：[式1] [其中，n表示1〜3的整数，R 代表氢原子，R 2表示低级烷基，或R 1和R 2结合在一起至表示亚烷基，R 3表示低级烷基，R 4表示NHSO 2 R 6（其中R 0） 6表示羟基等）等，R 5表示芳基等]等。

5. 发明授权

US6107064A Process for producing xanthine derivatives with bacteria and fungi 失效
标题翻译：用细菌和真菌生产黄嘌呤衍生物的方法
公开(公告)号：US6107064A
公开(公告)日：2000-08-22
申请号：US581533
申请日：1996-01-17
申请人： Junichi Shimada , Tamotsu Eguchi , Kenichi Mochida , Akira Horiguchi , Tohru Yasuzawa , Hideaki Kusaka , Hiromi Nonaka , Fumio Suzuki
发明人： Junichi Shimada , Tamotsu Eguchi , Kenichi Mochida , Akira Horiguchi , Tohru Yasuzawa , Hideaki Kusaka , Hiromi Nonaka , Fumio Suzuki
IPC分类号： C07D473/04 , C07D473/06 , C12P17/18 , C12P17/16
CPC分类号： C07D473/04 , C07D473/06 , C12P17/18
摘要： The present invention relates to a process for producing a xanthine derivative represented by formula (II), comprising converting a xanthine derivative represented by formula (I) {hereinafter, referred to as Compound (I)}: ##STR1## (wherein R.sup.1 and R.sup.2 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl) into a xanthine derivative represented by formula (II) {hereinafter, referred to as Compound (II)}: ##STR2## (wherein R.sup.3 and R.sup.4 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl; R.sup.5 and R.sup.6 independently represent hydrogen, hydroxy, or oxo; with the proviso that R.sup.5 and R.sup.6 are both hydrogen, at least one of R.sup.3 and R.sup.4 is hydroxy-substituted or oxo-substituted lower alkyl; and X and Y both represent hydrogen or are combined with each other to form a single bond) in the presence of an enzyme source for catalyzing hydroxylation or carbonylation of Compound (I) into Compound (II), and collecting the produced Compound (II).
摘要翻译： PCT No.PCT / JP95 / 00929 Sec。 371日期1996年1月17日 102（e）日期1996年1月17日PCT提交1995年5月16日PCT公布。公开号WO95 / 31460 日本特开平9-1252号公报发明内容本发明涉及由式（II）表示的黄嘌呤衍生物的制造方法，其特征在于，将由式（I）表示的黄嘌呤衍生物{以下称为化合物（I）} 和R2独立地表示氢或羟基取代的，取代或未取代的低级烷基）转化为由式（II）表示的黄嘌呤衍生物（以下称为化合物（II）}：（其中R 3和R 4独立地表示氢或羟基取代的，取代或未取代的低级烷基; R 5和R 6独立地表示氢，羟基或氧代;条件是R 5和R 6都是氢，R 3和R 4中的至少一个是羟基取代的或氧代取代的低级烷基; X和Y均表示氢或彼此结合形成单键）在用于催化化合物（I）羟化或羰基化成化合物（II）的酶源的存在下，以及大学将所制备的化合物（II）。

6. 发明申请

US20070021355A1 Antidepressants or foods and beverage for antidepression 审中-公开
标题翻译：抗抑郁药或抗抑郁食品和饮料
公开(公告)号：US20070021355A1
公开(公告)日：2007-01-25
申请号：US10558706
申请日：2004-05-28
申请人： Hiroaki Kohno , Hideaki Kusaka
发明人： Hiroaki Kohno , Hideaki Kusaka
IPC分类号： A61K31/7056
CPC分类号： C07D405/04 , A23L2/52 , A23L33/10 , A61K31/404 , A61K31/7056 , C07H7/06
摘要： An object of the present invention is to provide antidepressants or foods and drinks for antidepression. To solve the present problem, the present invention provides antidepressants or foods and drinks for antidepression comprising, as an active ingredient, a compound represented by formula (I): (wherein R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, or the like; R7 represents a hydrogen atom or substituted or unsubstituted lower alkyl; and R8, R9, R10 and R11, which may be the same or different, each represent a hydrogen atom or substituted or unsubstituted lower alkyl) or a salt thereof.
摘要翻译：本发明的目的是提供抗抑郁药或食品和饮料用于抗抑郁。为了解决本发明的问题，本发明提供了抗抑郁药或抗抑郁药的食品和饮料，其含有作为活性成分的式（I）表示的化合物：（其中R 1，R 2，R 2， R 3，R 3和R 4可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等; R 5是氢原子，羟基等; R 6表示氢原子等; R 7表示氢原子，或取代或未取代的低级烷基;和R 8，R 9，R 10和R 11，其可以相同或不同，各自表示氢原子或取代或未取代的低级烷基）或其盐。

7. 发明授权

US5648353A Quinazolines and phthalazines having adenosine uptake inhibitor activity 失效
标题翻译：喹唑啉和具有腺苷摄取抑制剂活性的酞嗪酮
公开(公告)号：US5648353A
公开(公告)日：1997-07-15
申请号：US446235
申请日：1995-05-22
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 , A61K31/505
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。

8. 发明授权

US5395836A 8-tricycloalkyl xanthine derivatives 失效
标题翻译： 8-三环烷基黄嘌呤衍生物
公开(公告)号：US5395836A
公开(公告)日：1995-03-07
申请号：US222938
申请日：1994-04-05
申请人： Junichi Shimada , Takashi Kuwabara , Tohru Yasuzawa , Hiroshi Magara , Hiromi Nonaka , Hideaki Kusaka , Fumio Suzuki
发明人： Junichi Shimada , Takashi Kuwabara , Tohru Yasuzawa , Hiroshi Magara , Hiromi Nonaka , Hideaki Kusaka , Fumio Suzuki
IPC分类号： C07D473/04 , A61K31/52 , C07D473/06
CPC分类号： C07D473/04 , Y10S514/869
摘要： There is provided a novel xanthine Compound(I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represent hydroxy-substituted, oxo-substituted or unsubstituted lower alkyl, Y is a single bond or alkylene, and Q is ##STR2## wherein R.sup.3 and R.sup.4 are the same or different and each represent hydrogen or hydroxy, n is 0 or 1; provided that when both of R.sup.3 and R.sup.4 are hydrogen, at least one of R.sup.1 and R.sup.2 is hydroxy-substituted or oxo-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.The xanthine compound has adenosine A.sub.1 receptor antagonizing activity, and thus shows diuretic effect, renal-protecting effect, bronchodilatory effect, cerebral function improving effect and anti-dementia effect.
摘要翻译：提供了一种新颖的黄嘌呤化合物（I）其中R 1和R 2相同或不同，各自表示羟基取代的，取代或未取代的低级烷基，Y是单键或亚烷基，Q 其中R 3和R 4相同或不同，各自表示氢或羟基，n为0或1; 条件是当R 3和R 4都是氢时，R 1和R 2中的至少一个是羟基取代的或氧代取代的低级烷基; 或其药学上可接受的盐。黄嘌呤化合物具有腺苷A1受体拮抗活性，因此具有利尿作用，肾保护作用，支气管扩张作用，脑功能改善作用和抗痴呆作用。

9. 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。

10. 发明申请

US20060252780A1 Fused pyrimidine derivatives 审中-公开
标题翻译：融合嘧啶衍生物
公开(公告)号：US20060252780A1
公开(公告)日：2006-11-09
申请号：US10554254
申请日：2004-04-23
申请人： Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
发明人： Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/14
摘要： A fused pyrimidine derivative is presented. The derivatie has an insulin secretion stimulating activity represented by Formula (I): {wherein R1 represents a hydrogen atom, lower alkyl, or the like; n represents an integer of 0 to 3; and X1 and X2 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like; and formula (II): represents formula (III): [wherein X—Y—Z represents R2C═CR3—NR4 (wherein R2, R3 and R4 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like)]}, or a pharmaceutically acceptable salt thereof.
摘要翻译：提出了一种稠合的嘧啶衍生物。衍生物具有由式（I）表示的胰岛素分泌刺激活性：其中R 1表示氢原子，低级烷基等; n表示0〜3的整数， X 1和X 2可以相同或不同，各自表示氢原子，低级烷基等; 和式（II）：表示式（III）：[其中XYZ表示R 2 C-CR 3 -NR 4（其中R' O 2，R 3和R 4可以相同或不同，各自表示氢原子，低级烷基等）]}，或其药学上可接受的盐。

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