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公开(公告)号:US20070189970A1
公开(公告)日:2007-08-16
申请号:US10590295
申请日:2005-01-13
IPC分类号: A61K49/04 , C07D211/12 , C07D211/22 , C07D401/06
CPC分类号: C07D295/185 , A61K51/0406 , A61K51/0455 , C07C257/18 , C07C317/50 , C07D211/34 , C07D211/60 , Y02P20/55
摘要: It is intended to provide a contrast medium for thrombus capable of binding specifically to a thrombus, lowering background noise and thus improving the resolution in a contrast examination for thrombus formation; and a method of detecting a thrombus by using the same. A contrast medium for thrombus comprising, as the active substance, a substance obtained by labeling a compound capable of binding to GPIIb/IIIa which is selected from among compounds represented by the general formulae (I) to (IV) and physiologically acceptable salts thereof, and a method of detecting a thrombus by using the same.
摘要翻译: 旨在提供能够特异性结合血栓的血栓造影剂,降低背景噪音,从而提高血栓形成对比检查中的分辨率; 以及使用该血栓检测血栓的方法。 一种用于血栓的造影剂,其特征在于,作为活性物质,通过将通式(I)〜(IV)表示的化合物及其生理学上可接受的盐中选择的能够结合GPIIb / IIIa的化合物进行标记而得到的物质, 以及使用该血栓检测血栓的方法。
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公开(公告)号:US20090181964A1
公开(公告)日:2009-07-16
申请号:US11887384
申请日:2006-03-30
申请人: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号: A61K31/5377 , C07D235/04 , A61K31/4184 , C07D401/02 , A61K31/4439 , C07D403/02 , A61K31/496 , C07D413/14 , A61K31/506 , A61K31/501 , A61P35/00
CPC分类号: C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译: 旨在提供可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙烷-1,3-二酮衍生物。 结果证实,在具有2-(1,3-二氢-2H-苯并咪唑)的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基)具有优异的GnRH受体拮抗作用,完成了本发明。 因为本发明的化合物具有强的GnRH受体拮抗作用,因此可用于治疗性激素依赖性疾病,特别是GnRH相关疾病。 此外,由于本发明的化合物在人体中具有优异的代谢稳定性,药物相互作用少,因此作为上述疾病的药物具有优选的特性。
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公开(公告)号:US20060229236A1
公开(公告)日:2006-10-12
申请号:US10500113
申请日:2002-12-27
申请人: Shigeki Satoh , Yasuharu Urano , Kazuhiko Osoda , Mitsuru Hosaka , Kozo Sawada , Takayuki Inoue , Hiroaki Mori , Shoji Takagaki , Takao Fujimura , Hideaki Matsuoka , Katsuhiko Yoshizawa
发明人: Shigeki Satoh , Yasuharu Urano , Kazuhiko Osoda , Mitsuru Hosaka , Kozo Sawada , Takayuki Inoue , Hiroaki Mori , Shoji Takagaki , Takao Fujimura , Hideaki Matsuoka , Katsuhiko Yoshizawa
摘要: A cyclic tetrapeptide compound of the formula (I): wherein R1 is hydrogen; R2 is lower alkyl, aryl, optionally substituted ar(lower)alkyl, heterocyclic(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, lower alkylcarbamoyl(lower)alkyl or arylcarbamoyl(lower)alkyl; R3 and R4 are each independently hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic(lower)alkyl or cyclo(lower)alkyl(lower)alkyl, or R3 and R4 are linked together to form lower alkylene or condensed ring, or one of R3 and R4 is linked to the adjacent nitrogen atom to form a ring; R5 is lower alkylene or lower alkenylene, Y is [wherein RY1 is hydrogen, halogen or optionally protected hydroxy, RY2 is hydrogen, halogen, lower alkyl or phenyl, and RY3 is hydrogen or lower alkyl]; R8 is hydrogen or lower alkyl; and n is an integer of 1 or 2, or a salt thereof.
摘要翻译: 式(I)的环状四肽化合物:其中R 1是氢; R 2是低级烷基,芳基,任选取代的芳(低级)烷基,杂环(低级)烷基,环(低级)烷基(低级)烷基,低级烷基氨基甲酰基(低级)烷基或芳基氨基甲酰基 烷基; R 3和R 4各自独立地为氢,低级烷基,任选取代的芳(低级)烷基,任选取代的杂环(低级)烷基或环(低级)烷基(低级) )烷基或R 3和R 4连接在一起形成低级亚烷基或稠环,或者R 3和R 3中的一个 > 4 SUB>与相邻的氮原子连接形成环; R 5是低级亚烷基或低级亚烯基,Y是[其中R Y1是氢,卤素或任选保护的羟基,R Y2是氢, 卤素,低级烷基或苯基,R 3 Y 3是氢或低级烷基]。 R 8是氢或低级烷基; n为1或2的整数,或其盐。
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公开(公告)号:US07960562B2
公开(公告)日:2011-06-14
申请号:US11887384
申请日:2006-03-30
申请人: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号: A61K31/4184 , C07D235/12
CPC分类号: C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译: 旨在提供可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙烷-1,3-二酮衍生物。 结果证实,在具有2-(1,3-二氢-2H-苯并咪唑)的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基)具有优异的GnRH受体拮抗作用,完成了本发明。 因为本发明的化合物具有强的GnRH受体拮抗作用,因此可用于治疗性激素依赖性疾病,特别是GnRH相关疾病。 此外,由于本发明的化合物在人体中具有优异的代谢稳定性,药物相互作用少,因此作为上述疾病的药物具有优选的特性。
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公开(公告)号:US06495542B1
公开(公告)日:2002-12-17
申请号:US09600857
申请日:2000-10-16
申请人: Hiroyuki Setoi , Takehiko Ohkawa , Yuki Sawada , Kazuhiko Osoda , Teruo Oku
发明人: Hiroyuki Setoi , Takehiko Ohkawa , Yuki Sawada , Kazuhiko Osoda , Teruo Oku
IPC分类号: A61K3155
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要: A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.
摘要翻译: 式(I)的化合物:其中A是任选取代的杂环基,R是低级烷氧基; Z是C = O或CH 2; 并且B是具有加压素拮抗活性并且可用作加压素拮抗剂的苯并氮杂基,其可以是任选被取代的,或其盐。
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