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1. 发明专利

IL197141A Crystals of phenoxypyridine derivatives, process for producing the same and compositions comprising same 未知
公开(公告)号：IL197141A
公开(公告)日：2014-01-30
申请号：IL19714109
申请日：2009-02-19
申请人： TAKAHASHI KEIKO , EISAI R&D MAN CO LTD , WAKASUGI KAZUNORI , SAKAGUCHI TAKAHISA , SHIROTORI SHUJI , KAMADA ATSUSHI , MATSUSHIMA TOMOHIRO
发明人： TAKAHASHI KEIKO , WAKASUGI KAZUNORI , SAKAGUCHI TAKAHISA , SHIROTORI SHUJI , KAMADA ATSUSHI , MATSUSHIMA TOMOHIRO
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101
摘要： The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor.

2. 发明专利

IL188670A PYRIDINE AND PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF 未知
公开(公告)号：IL188670A
公开(公告)日：2011-12-29
申请号：IL18867008
申请日：2008-01-08
申请人： MATSUSHIMA TOMOHIRO , OBAISHI HIROSHI , TAKAHASHI KEIKO , FUNASAKA SETSUO , EISAI R&D MAN CO LTD , SHIROTORI SHUJI
发明人： MATSUSHIMA TOMOHIRO , OBAISHI HIROSHI , TAKAHASHI KEIKO , FUNASAKA SETSUO , SHIROTORI SHUJI
摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R 1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R 2 and R 3 represent hydrogen; R 4 , R 5 , R 6 , and R 7 may be the same or different and each represents hydrogen, halogen, C 1-6 alkyl or the like; R 8 represents hydrogen or the like; R 9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen or the like.]

3. 发明专利

IL200466D0 PYRIDINE OR PYRIMIDINE DERIVATIVE HAVING EXCELLENT CELL GROWTH INHIBITION EFFECT AND EXCELLENT ANTI-TUMOR EFFECT ON CELL STRAIN HAVING AMPLIFICATION OF HGFR GENE 未知
公开(公告)号：IL200466D0
公开(公告)日：2010-04-29
申请号：IL20046609
申请日：2009-08-18
申请人： EISAI R&D MAN CO LTD , SHIROTORI SHUJI , MATSUSHIMA TOMOHIRO , OBAISHI HIROSHI , NAKAGAWA TAKAYUKI , FUNASAKA SETSUO , TAKAHASHI KEIKO
IPC分类号： C07D20100101
摘要： A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R 1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R 2 and R 3 represent hydrogen; R 4 , R 5 , R 6 , and R 7 may be the same or different and each represents hydrogen, halogen, C 1-6 alkyl or the like; R 8 represents hydrogen or the like; R 9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen.

5. 发明申请

WO1997003059A1 4-(SUBSTITUTED AMINOMETHYL)THIAZOLINE DERIVATIVES 审中-公开
标题翻译： 4-（取代的氨基甲酰基）噻唑啉衍生物
公开(公告)号：WO1997003059A1
公开(公告)日：1997-01-30
申请号：PCT/JP1996001923
申请日：1996-07-11
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, MASAKAZU , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/56
CPC分类号： C07D277/56
摘要： Object: to provide compounds having an excellent antiplatelet aggregation effect and a good oral activity. Constitution: thiazoline derivatives represented by general formula (I) and salts thereof, wherein R represents (II) (wherein R and R represent each hydrogen, alkyl, alkoxy-carbonyl, cycloalkyl, optionally substituted phenyl or optionally substituted aralkyl), imidazolin-2-yl, etc; R represents (III) (wherein R and R represent each hydrogen, alkyl, cycloalkyl, optionally substituted phenyl or optionally substituted aralkyl), etc.; R represents hydrogen or alkyl); and R represents alkyl.
摘要翻译：目的：提供具有优异抗血小板聚集效应和良好口服活性的化合物。结构式：由通式（I）表示的噻唑啉衍生物及其盐，其中R 1表示（II）（其中R 11和R 12表示各自的氢，烷基，烷氧基 - 羰基，环烷基，任选取代的苯基或任选取代的芳烷基），咪唑啉-2-基等; R 2表示（III）（其中R 41和R 42表示各个氢，烷基，环烷基，任选取代的苯基或任选取代的芳烷基）等; R 3表示氢或烷基）; R 4表示烷基。

6. 发明申请

WO1985001729A1 5-FLUOROURACIL DERIVATIVES AND MEDICINAL PREPARATION CONTAINING SAME 审中-公开
标题翻译： 5-氟尿嘧啶衍生物和含有其的药物制剂
公开(公告)号：WO1985001729A1
公开(公告)日：1985-04-25
申请号：PCT/JP1984000499
申请日：1984-10-19
申请人： TERUMO KABUSHIKI KAISHA , WAKABAYASHI, Toshio , TAKAHASHI, Keiko , KATAYAMA, Hajime
发明人： TERUMO KABUSHIKI KAISHA
IPC分类号： C07D273/04
CPC分类号： C07D239/553
摘要： 5-Fluorouracil derivatives represented by general formula (I): (wherein R represents an acyl group derived from an unsaturated higher fatty acid selected from the group consisting of triene higher fatty acids, pentaene higher fatty acids, and hexaene higher fatty acids) can be used as an agent for controlling platelet agglutination and a carcinostatic agent. They may be mixed with a pharmaceutically acceptable carrier or a diluente to form a medicinal preparation.

7. 发明申请

WO1994002472A1 THIAZOLINE DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：WO1994002472A1
公开(公告)日：1994-02-03
申请号：PCT/JP1993000937
申请日：1993-07-08
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/48
CPC分类号： C07D417/12 , C07D277/56
摘要： To provide a compound excellent in fibrinogen receptor antagonism and cell adhesion factor antagonism. A thiazoline derivative represented by general formula (I) and a salt thereof, wherein R1 represents cyano, carbamoyl, thiocarbamoyl, morpholinothiocarbonyl, alkylthioimidoyl, -C(=NH)-NR11R12 (wherein R11 and R12 represent each hydrogen, alkyl, alkoxycarbonyl, cycloalkyl, phenyl, substituted phenyl, aralkyl or substituted aralkyl, or alternatively R11 and R12 may be combined with each other to represent a monovalent heterocyclic group together with the adjacent nitrogen atom) or imidazolin-2-yl; R2 represents alkyl or aralkyl; R3 represents carboxy, hydroxy, alkoxycarbonyl, benzyloxycarbonyl or pyridyl-methyloxycarbonyl; and n represents an integer of 1 to 3.
摘要翻译：提供纤维蛋白原受体拮抗作用和细胞粘附因子拮抗作用优异的化合物。由通式（I）表示的噻唑啉衍生物及其盐，其中R1表示氰基，氨基甲酰基，硫代氨基甲酰基，吗啉代硫代羰基，烷硫基亚氨基，-C（= NH）-NR11R12（其中R11和R12各自表示氢，烷基，烷氧基羰基，，苯基，取代的苯基，芳烷基或取代的芳烷基，或者R 11和R 12可以彼此结合以与相邻的氮原子一起代表一价杂环基）或咪唑啉-2-基; R2代表烷基或芳烷基; R3表示羧基，羟基，烷氧基羰基，苄氧基羰基或吡啶基甲氧基羰基; n表示1〜3的整数。

8. 发明申请

WO1995034543A1 THIAZOLINE DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：WO1995034543A1
公开(公告)日：1995-12-21
申请号：PCT/JP1995001169
申请日：1995-06-12
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/44
CPC分类号： C07D277/56
摘要： Object: To provide a compound useful as an antiplatelet aggregation for intravenous administration. Constitution: A thiazoline derivative represented by general formula (I) and a salt thereof, wherein R represents hydroxy, alkoxy, cycloalkoxy or R NH-(R being cycloalkyl); R represents alkyl or cycloalkyl; R represents hydrogen or alkyl; and n represents an integer of 2 to 9.
摘要翻译：目的：提供用作静脉内给药的抗血小板聚集体的化合物。结构：由通式（I）表示的噻唑啉衍生物及其盐，其中R 1表示羟基，烷氧基，环烷氧基或R 4 NH-（R 4为环烷基）; R 2表示烷基或环烷基; R 3表示氢或烷基; n表示2〜9的整数。

9. 发明申请

WO1998005668A1 p-TOLUENESULFONATE HYDRATE OF THIAZOLINE COMPOUND 审中-公开
标题翻译：噻唑啉化合物的对羟基苯甲酸酯水合物
公开(公告)号：WO1998005668A1
公开(公告)日：1998-02-12
申请号：PCT/JP1997002715
申请日：1997-08-05
申请人： TAISHO PHARMACEUTICAL CO., LTD. , HATAYAMA, Sachiko +hf , SATO, Masakazu , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka
发明人： TAISHO PHARMACEUTICAL CO., LTD. , HATAYAMA, Sachiko +hf , HATAYAMA, Katsuo +di
IPC分类号： C07D491/113
CPC分类号： C07D491/10
摘要： p-Toluenesulfonate dihydrate of the thiazoline compound of formula (1); and fibrinogen receptor antagonists comprising the same as the active ingredient. The above dihydrate exhibits an excellent antagonism against fibrinogen receptors and is easy of storage and formulation into oral drugs because of its non-hygroscopic property.
摘要翻译：式（1）的噻唑啉化合物的对甲苯磺酸盐二水合物; 和包含与活性成分相同的纤维蛋白原受体拮抗剂。上述二水合物对纤维蛋白原受体表现出优异的拮抗作用，并且由于其不吸湿性而易于储存和制备成口服药物。

10. 发明申请

WO1995002586A1 5-ACETYLTHIAZOLINE OXIME DERIVATIVE 审中-公开
标题翻译： 5-乙酰胆碱衍生物衍生物
公开(公告)号：WO1995002586A1
公开(公告)日：1995-01-26
申请号：PCT/JP1994001107
申请日：1994-07-07
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/44
CPC分类号： C07D277/46
摘要： To provide a compound excellent in fibrinogen receptor and cell adhesion factor antagonism. A 5-acetylthiazoline oxime derivative represented by general formula (I) and a salt thereof, wherein R represents cyano, thiocarbamoyl, alkylthioimidoyl or a group represented by formula (II) wherein R and R represent each independently hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, benzyl or substituted benzyl provided R and R may be combined with each other to represent a heterocyclic group together with the nitrogen atom to which they are bonded; R represents alkyl, alkenyl or aralkyl; and R represents hydrogen, alkyl or 4-methoxybenzyl.
摘要翻译：提供纤维蛋白原受体和细胞粘附因子拮抗作用优异的化合物。由通式（I）表示的5-乙酰基噻唑啉肟衍生物及其盐，其中R 1表示氰基，硫代氨基甲酰基，烷硫基亚氨基或由式（II）表示的基团，其中R 11和R 12各自表示独立地，氢，烷基，环烷基，苯基，取代的苯基，苄基或取代的苄基，其中R 11和R 12可以彼此结合以与它们所键合的氮原子一起表示杂环基; R 2表示烷基，烯基或芳烷基; R 3表示氢，烷基或4-甲氧基苄基。

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