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1. 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。

2. 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.

3. 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。

4. 发明授权

US08138197B2 Spirochromanon derivatives 有权
标题翻译：螺二色素衍生物
公开(公告)号：US08138197B2
公开(公告)日：2012-03-20
申请号：US12518466
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
IPC分类号： A61K31/438 , C07D221/20
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[ 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-a]吡啶，其具有Ar 2，并且任选具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a）-Q 2 -R b的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或次甲基; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

5. 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。

6. 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。

7. 发明授权

US5691315A Endothelin antagonistic peptide derivatives 失效
标题翻译：内皮素拮抗肽衍生物
公开(公告)号：US5691315A
公开(公告)日：1997-11-25
申请号：US494818
申请日：1995-06-26
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/103 , C07K5/08 , C07K7/06
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/1008 , A61K38/00
摘要： The invention relates to compounds which are antagonists of endothelin, to processes for their preparation, and to their use as pharmaceuticals. The compounds of the invention are Useful in the treatment of hypertension, pulmonary hypertension, Reynaud's disease, myocardial infarction, angina pectoris, acute renal failure, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension.
摘要翻译：本发明涉及作为内皮素拮抗剂的化合物，其制备方法及其作为药物的用途。本发明化合物可用于治疗高血压，肺动脉高压，雷诺氏病，心肌梗塞，心绞痛，急性肾衰竭，脑梗塞，脑血管痉挛，动脉硬化，哮喘，内毒素休克，内毒素诱导的多器官功能衰竭或弥散性血管内凝血和/或环孢菌素诱导的肾衰竭或高血压。

8. 发明授权

US5496928A Endothelin antagonistic substance 失效
标题翻译：内皮素拮抗物质
公开(公告)号：US5496928A
公开(公告)日：1996-03-05
申请号：US230534
申请日：1994-04-20
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/087 , C07K5/103 , A61K38/06
CPC分类号： C07K5/1008 , C07K5/0202 , C07K5/0205 , C07K5/06034 , C07K5/06043 , C07K5/0808 , C07K5/0812 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：（I）抑制内皮素的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

9. 发明授权

US5470833A Endothelin antagonistic peptide derivatives 失效
标题翻译：内皮素拮抗肽衍生物
公开(公告)号：US5470833A
公开(公告)日：1995-11-28
申请号：US213829
申请日：1994-03-14
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/103 , C07K5/00 , C07K5/08 , C07K5/10
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/1008 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：抑制内皮素与其受体的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

10. 发明授权

US4839353A Anti-ulcer substituted pyridine derivatives 失效
标题翻译：抗溃疡取代的吡啶衍生物
公开(公告)号：US4839353A
公开(公告)日：1989-06-13
申请号：US110369
申请日：1987-10-20
申请人： Masaaki Hosoi , Ryo Nishioka , Yoshio Hioki , Yoshiaki Iida , Hiroshi Takeshita , Kenji Niiyama , Yusuke Hidaka
发明人： Masaaki Hosoi , Ryo Nishioka , Yoshio Hioki , Yoshiaki Iida , Hiroshi Takeshita , Kenji Niiyama , Yusuke Hidaka
IPC分类号： C07D213/16 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04
CPC分类号： C07D213/16 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04
摘要： A substituted pyridine derivative represented by the general formula ##STR1## wherein R.sup.1 represents a phenyl or naphthyl group which may optionally be substituted by a substituent selected from the class consisting of a hydroxyl group, lower alkyl groups, lower alkoxy groups, cycloalkyl groups, lower alkoxycarbonyl groups, a phenyl group and halogen atoms; X represents an oxygen atom, a sulfur atom, a carbonyl group, or a group of the formula --CH(OH)-- or --N(R.sup.a)-- in which R.sup.a is a hydrogen atom or a lower alkyl group; Y represents a linear or branched lower alkylene group or a vinylene group which may optionally be substituted by a lower alkyl group, with the proviso that when X is an oxygen or sulfur atom, Y represents the lower alkylene group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a cycloalkyloxy group, a lower alkylthio group, a cycloalkylthio group, an aryloxy group, an aralkyloxy groups or a group of the formula ##STR2## in which R.sup.b and R.sup.c are identical or different and each represents a hydrogen atom or a lower alkyl group. or R.sup.b and R.sup.c, taken together, may form together with the adjacent nitrogen atom a 5- to 7-membered saturated heterocyclic ring which may optionally contain at least one additional hetero atom selected from the group consisting of oxygen, sulfur and nitrogen atoms and may optionally be substituted by a lower alkyl group; m and n are each 0 or 1, with the proviso that m and n are not 0 at the same time, or an acid addition salt thereof. This compound is useful as an antiulcer agent.
摘要翻译：由通式[IMAGE] [I]表示的取代的吡啶衍生物，其中R 1表示可任选被选自羟基，低级烷基，低级烷氧基，环烷基的取代基取代的苯基或萘基基团，低级烷氧基羰基，苯基和卤素原子; X表示氧原子，硫原子，羰基或式-CH（OH） - 或-N（Ra） - 的基团，其中Ra为氢原子或低级烷基; Y表示可以任选被低级烷基取代的直链或支链低级亚烷基或亚乙烯基，条件是当X是氧或硫原子时，Y代表低级亚烷基; R2和R3相同或不同，各自表示氢原子或低级烷基; R 4表示氢原子，低级烷氧基，环烷氧基，低级烷硫基，环烷硫基，芳氧基，芳烷氧基或式中的R 1和R c相同或不同的式各自表示氢原子或低级烷基。或Rb和Rc一起可以与相邻的氮原子一起形成5-7元饱和杂环，其可以任选地含有至少一个选自氧，硫和氮原子的另外的杂原子，并且可以任选被低级烷基取代; m和n各自为0或1，条件是m和n不同时为0，或其酸加成盐。该化合物可用作抗溃疡剂。

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