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1. 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。

2. 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。

3. 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。

4. 发明申请

WO1997003058A1 4-ALKYLTHIAZOLINE DERIVATIVES 审中-公开
标题翻译： 4-氨基噻唑衍生物
公开(公告)号：WO1997003058A1
公开(公告)日：1997-01-30
申请号：PCT/JP1996001862
申请日：1996-07-05
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： To provide compounds having an excellent platelet agglutination inhibiting effect and a good peroral activity. Thiazoline derivatives represented by general formula (I) and salts thereof; wherein R represents formula (II), wherein R and R represent each hydrogen, alkyl, alkoxy-carbonyl, cycloalkyl, optionally substituted phenyl or optionally substituted aralkyl; or by formula (III), wherein R and R represent each hydrogen or alkyl; m and n represent each an integer of 1 to 3; and A represents methylene, carbonyl, ethylenedioxymethylene, oxygen, sulfur, sulfinyl, sulfonyl or by formula (IV) or imidazolin-2-yl; R represents alkyl, cycloalkyl or phenyl; R represents hydrogen or alkyl; and R represents alkyl.
摘要翻译：提供具有优异的血小板凝集抑制作用和良好的口服活性的化合物。由通式（I）表示的噻唑啉衍生物及其盐; 其中R 1表示式（II），其中R 11和R 12表示每个氢，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; 或通式（III）表示，其中R 21和R 22表示各自的氢或烷基; m和n表示1〜3的整数。 A代表亚甲基，羰基，亚乙二氧基亚甲基，氧，硫，亚磺酰基，磺酰基或式（Ⅳ）或咪唑啉-2-基; R 2表示烷基，环烷基或苯基; R 3表示氢或烷基; 且R 4表示烷基。

5. 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。

6. 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。

7. 发明申请

WO1993013086A1 ANILIDE DERIVATIVE 审中-公开
标题翻译：辅助剂衍生物
公开(公告)号：WO1993013086A1
公开(公告)日：1993-07-08
申请号：PCT/JP1992001661
申请日：1992-12-18
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , KAWASE, Masahiro , MANAKA, Akira , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D295/08
CPC分类号： C07D239/42 , C07D213/74 , C07D295/088 , C07D295/112 , C07D295/185
摘要： To provide a compound with a potent ACAT inhibiting activity. An anilide derivative represented by general formula (I) and a salt thereof, wherein R and R may be the same or different from each other and each represents C1-C4 alkyl; n represents 0, 1 or 2; A represents C1-C14 alkylene or -CH2CO-; and Ar represents phenyl or benzyl each of which may be substituted by halogen, nitro, C1-C4 alkyl, C1-C4 alkoxy, C2-C5 alkanoyl or trifluoromethyl, or pyridyl or pyrimidyl each of which may be substituted by halogen or trifluoromethyl.
摘要翻译：以提供具有有效的ACAT抑制活性的化合物。由通式（I）表示的苯胺衍生物及其盐，其中R 1和R 2可以相同或不同，各自表示C1-C4烷基; n表示0,1或2; A表示C1-C14亚烷基或-CH2CO-; 并且Ar表示可以被卤素，硝基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 2 -C 5烷酰基或三氟甲基取代的苯基或苄基，或各自可被卤素或三氟甲基取代的吡啶基或嘧啶基。

8. 发明申请

WO1992007825A1 PHENOL DERIVATIVE 审中-公开
标题翻译： PHENOL衍生物
公开(公告)号：WO1992007825A1
公开(公告)日：1992-05-14
申请号：PCT/JP1991001506
申请日：1991-11-02
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C323/60
CPC分类号： C07C323/60
摘要： A phenol derivative represented by general formula (I) and its salt, wherein X represents C1 to C4 alkyl or C1 to C4 alkoxy; Y represents hydrogen or C1 to C4 alkoxy; and A represents C1 to C4 alkylene, etc. These compounds have an action of inhibiting ACAT and the formation of lipid peroxide and are useful as a remedy for arteriosclerosis.
摘要翻译：由通式（I）表示的苯酚衍生物及其盐，其中X表示C1至C4烷基或C1至C4烷氧基; Y表示氢或C1〜C4烷氧基; A表示C1〜C4亚烷基等。这些化合物具有抑制ACAT和形成脂质过氧化物的作用，可用作动脉硬化的补救剂。

9. 发明申请

WO1992009572A1 ANILIDE DERIVATIVE 审中-公开
标题翻译：辅助剂衍生物
公开(公告)号：WO1992009572A1
公开(公告)日：1992-06-11
申请号：PCT/JP1991001602
申请日：1991-11-21
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C317/44
CPC分类号： C07C317/44 , C07C323/60 , C07C327/32
摘要： An anilide derivative useful for treating arteriosclerosis, represented by general formula (I), wherein X represents C1 to C4 alkyl or C1 to C4 alkoxy; Y represents hydrogen or C1 to C4 alkoxy; Z represents C1 to C4 alkyl or C1 to C4 alkoxy; A represents C1 to C4 alkylene, R represents C6 to C20 alkyl, C2 to C20 alkanoyl, or benzyl which may be substituted with C1 to C4 alkyl; and n represents 0, 1 or 2.

10. 发明申请

WO1993007113A1 ALKOXYPHENYLALKYLAMINE DERIVATIVE 审中-公开
标题翻译：烷氧基苯胺衍生物
公开(公告)号：WO1993007113A1
公开(公告)日：1993-04-15
申请号：PCT/JP1992001259
申请日：1992-09-30
申请人： TAISHO PHARMACEUTICAL CO., LTD. , NAKAZATO, Atsuro , SEKIGUCHI, Yoshinori , OHTA, Koumei , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C217/56
CPC分类号： C07D213/74 , C07C217/56 , C07C217/60 , C07C217/62 , C07C229/14 , C07D239/42 , C07D295/096 , C07D333/16
摘要： An alkoxyphenylalkylamine derivative represented by general formula (I) and a salt thereof, wherein X and X may be the same or different from each other and each represents hydrogen, halogen, hydroxyl, or C1 to C5 alkoxy which may be substituted by phenyl; R and R may be the same or different from each other and each represents hydrogen or C1 to C7 alkyl which may be terminated with hydroxyl, carboxyl or alkoxycarbonyl, or alternatively R and R are combined with the adjacent nitrogen atoms to represent optionally substituted pyrrolidine, piperidino, piperazino, etc.; A represents phenyl which may be substituted by one to three arbitrary substituents selected among halogen, hydroxyl and C1 to C5 alkoxy, or similarly substituted thienyl; m represents an integer of 2 to 5; and n represents an integer of 1 to 7. The above compounds are useful in treating schizophrenia without causing extrapyramidal disorder and in treating problematic behaviours accompanying cerebrovascular disorder or senile dementia.
摘要翻译：由通式（I）表示的烷氧基苯基烷基胺衍生物及其盐，其中X 1和X 2可以彼此相同或不同，各自表示氢，卤素，羟基或C 1至C 5烷氧基，其可以被苯基取代; R 1和R 2可以彼此相同或不同，并且各自表示氢或可以被羟基，羧基或烷氧基羰基封端的C 1 -C 7烷基，或者R 1和R 2可以是与相邻的氮原子结合以代表任选取代的吡咯烷，哌啶子基，哌嗪基等; A表示可以被一至三个选自卤素，羟基和C 1至C 5烷氧基的任意取代基取代的苯基，或类似取代的噻吩基; m表示2〜5的整数，并且n表示1〜7的整数。上述化合物可用于治疗精神分裂症而不引起锥体外系紊乱，并且用于治疗伴有脑血管障碍或老年痴呆的问题行为。

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