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1. 发明授权

US08791125B2 Dihydropyrazolopyrimidinone derivatives 有权
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：US08791125B2
公开(公告)日：2014-07-29
申请号：US13053798
申请日：2011-03-22
申请人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子，卤素原子，羟基，低级烷基或-N（R1k）R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

2. 发明申请

US20070254892A1 Dihydropyrazolopyrimidinone derivatives 有权
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：US20070254892A1
公开(公告)日：2007-11-01
申请号：US11789548
申请日：2007-04-25
申请人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环 - 低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳族基团; R 2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R 3是氢原子或低级烷基; R 4是氢原子，卤素原子，羟基，低级烷基或-N（R 1）1个基团）的基团， SUP>; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

3. 发明授权

US07834019B2 Substituted pyrazolo[3,4-d]pyrimidinone derivatives 有权
标题翻译：取代的吡唑并[3,4-d]嘧啶酮衍生物
公开(公告)号：US07834019B2
公开(公告)日：2010-11-16
申请号：US11789548
申请日：2007-04-25
申请人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A61K31/519 , A61K31/497 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子，卤素原子，羟基，低级烷基或-N（R1k）R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

4. 发明申请

US20110189130A1 DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVES 有权
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：US20110189130A1
公开(公告)日：2011-08-04
申请号：US13053798
申请日：2011-03-22
申请人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/664 , A61K31/675 , A61K31/7008 , A61K31/7076 , A61K31/52 , A61K31/708 , A61K31/704 , A61K33/24 , A61K39/395 , A61K38/21 , A61P35/00 , A61P35/02
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子，卤素原子，羟基，低级烷基或-N（R1k）R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

5. 发明授权

US07935708B2 Dihydropyrazolopyrimidinone derivatives 有权
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：US07935708B2
公开(公告)日：2011-05-03
申请号：US12226707
申请日：2007-04-25
申请人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A01N43/90 , A01N43/56 , A61K31/519 , A61K31/415 , C07D487/00 , C07D403/02
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子，卤素原子，羟基，低级烷基或-N（R1k）R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

6. 发明申请

US20100063024A1 Dihydropyrazolopyrimidinone Derivatives 有权
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：US20100063024A1
公开(公告)日：2010-03-11
申请号：US12226707
申请日：2007-04-25
申请人： Toshihiro Sakamoto , Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人： Toshihiro Sakamoto , Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号： A61K31/397 , C07D487/04 , C07D413/14 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基，低级烯基，低级炔基或环低级烷基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R2是氢原子，低级烷基，低级烯基或低级炔基，或者是任选具有取代基的芳基，芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子，卤素原子，羟基，低级烷基或-N（R1k）R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用，因此可用于药物领域，特别是治疗各种癌症。

7. 发明授权

US08436004B2 Bicycloaniline derivative 有权
标题翻译：双苯胺衍生物
公开(公告)号：US08436004B2
公开(公告)日：2013-05-07
申请号：US12663729
申请日：2008-06-12
申请人： Makoto Bamba , Hidetomo Furuyama , Kenji Niiyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
发明人： Makoto Bamba , Hidetomo Furuyama , Kenji Niiyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04 , A61K31/522 , A61K31/5415 , A61K31/55 , A61K45/06 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ═NH or ═O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
摘要翻译：本发明涉及通式（I）的化合物：其中A1和A2各自表示氮原子或任选取代的次甲基; 环B表示由脂族环和任何其它3元至7元脂肪环形成的5元至7元脂族环或螺环或双环; R 1表示氢原子或任选取代的C 1 -C 6烷基，或任选取代的芳基，芳烷基或杂芳基; R 2表示任选取代的芳基，芳烷基或杂芳基; X表示一组= NH或= O等。基于其优异的Wee1激酶抑制作用，本发明化合物具有细胞生长抑制作用，与任何其他抗癌剂具有添加/协同作用，并且因此在医学领域是有用的。

8. 发明授权

US08288396B2 Pyrimidopyrimidoindazole derivative 失效
标题翻译：嘧啶并嘧啶并吲唑衍生物
公开(公告)号：US08288396B2
公开(公告)日：2012-10-16
申请号：US13202773
申请日：2010-02-18
申请人： Yasuhiro Goto , Kenji Niiyama , Satoshi Sunami , Keiji Takahashi
发明人： Yasuhiro Goto , Kenji Niiyama , Satoshi Sunami , Keiji Takahashi
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/14 , C07D519/00
摘要： The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): R1 means a —(C═O)aOb(C1-C6)alkyl group, a —(C═O)aOb(C2-C6)alkenyl group, a —(C═O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C═O)aOb(C1-C6)alkyl group or a group of —(C═O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
摘要翻译：本发明提供一种用于癌症化疗或放射治疗的新型抗癌剂或敏化剂。通式（I）的化合物：其中A表示芳基或杂芳基，或式（a）的基团：R 1表示 - （C = O）a O b（C 1 -C 6）烷基， - （C = O）a O b（C 2 -C 6）烯基， - （C = O）a O b（C 3 -C 6）环烷基，芳基或杂芳基; R2和R3各自表示氢原子，卤素原子，羟基，羧基， - （C = O）aOb（C1-C6）烷基或 - （C = O）aN（R1e） R2e; R4表示氢原子或（C1-C6）烷基等具有优异的Wee1激酶抑制作用，因此可用于医学领域，特别是在各种癌症治疗领域。

9. 发明申请

US20140005185A1 NOVEL IMIDAZO-OXAZINE COMPOUND OR SALT THEREOF 有权
标题翻译：新型咪唑氧化合物或其盐
公开(公告)号：US20140005185A1
公开(公告)日：2014-01-02
申请号：US14004446
申请日：2012-04-05
申请人： Masayuki Nakamura , Kenji Niiyama , Kaori Kamijo , Mitsuru Ohkubo , Toshiyasu Shimomura
发明人： Masayuki Nakamura , Kenji Niiyama , Kaori Kamijo , Mitsuru Ohkubo , Toshiyasu Shimomura
IPC分类号： C07D498/04 , C07D498/14 , A61K31/5365
CPC分类号： C07D498/04 , A61K31/5365 , C07D498/14
摘要： The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.
摘要翻译：本发明提供由式（I）表示的咪唑并恶嗪化合物或其盐，其中A，B，C和D如说明书中所定义。

10. 发明授权

US5114918A Endothelin antagonistic cyclic pentapeptides 失效
标题翻译：内皮素拮抗剂环糊精
公开(公告)号：US5114918A
公开(公告)日：1992-05-19
申请号：US630505
申请日：1990-12-20
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaru Nishikibe , Masaki Ihara , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaru Nishikibe , Masaki Ihara , Mitsuo Yano
IPC分类号： A61K38/00 , C07K7/64 , C07K14/575
CPC分类号： C07K14/57536 , A61K38/00 , Y10S514/826 , Y10S514/921 , Y10S514/922 , Y10S514/929 , Y10S530/80 , Y10S930/27
摘要： Cyclic pentapeptides of the formula:cyclo (-X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -X.sup.5 -) (I)wherein X.sup.n (n=1-5) represents amino acid residues. These compounds are useful as hypotensive drugs.

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