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11. 发明申请

WO1994004534A1 TETRAHYDROPYRROLOINDOLE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND INTERMEDIATES THEREFOR 审中-公开
标题翻译：四氢衍生物衍生物，其生产方法及其中间体
公开(公告)号：WO1994004534A1
公开(公告)日：1994-03-03
申请号：PCT/JP1993001158
申请日：1993-08-19
申请人： KYORIN PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER , TERASHIMA, Shiro , FUKUDA, Yasumichi
发明人： KYORIN PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： The invention provides an intermediate for the production of a compound which is prospective as a carcinostatic agent, a process for producing the same, and a starting material therefor. Tetrahydropyrroloindole derivatives represented by general formula (1) and optically active isomers thereof. General formula (1) wherein R1 represents hydrogen or a hydroxyl-protecting group; R2 represents hydrogen or an amino-protecting group; and X represents halogen, hydroxyl, alkylcarbonyloxy, arylcarbonyloxy, alkylsulfonyloxy or arylsulfonyloxy.
摘要翻译：本发明提供了制备作为制癌剂的化合物的中间体，其制备方法及其原料。由通式（1）表示的四氢吡咯并吲哚衍生物及其旋光异构体。通式（1）其中R1表示氢或羟基保护基; R2表示氢或氨基保护基; X表示卤素，羟基，烷基羰基氧基，芳基羰基氧基，烷基磺酰氧基或芳基磺酰氧基。

12. 发明申请

WO1997010207A1 NOVEL BENZAMIDE DERIVATIVES 审中-公开
标题翻译：新的苯甲酸衍生物
公开(公告)号：WO1997010207A1
公开(公告)日：1997-03-20
申请号：PCT/JP1996002605
申请日：1996-09-12
申请人： KYORIN PHARMACEUTICAL CO., LTD. , TAKADOI, Masanori , KOBAYASHI, Fumiyoshi , SEKIGUCHI, Haruo
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/04
CPC分类号： C07D211/56
摘要： Novel benzamide derivatives represented by general formula (I) or pharmacologically acceptable acid addition salts thereof; a process for producing the same; and an enterokinesis regulator comprising the same as the active ingredient which has the action of stimulating 5-HT4 and also acts directly on the digestive tract smooth muscles.
摘要翻译：由通式（I）表示的新型苯甲酰胺衍生物或其药理学上可接受的酸加成盐; 其制造方法; 以及包含与作为刺激5-HT4的作用的活性成分相同的肠激酶调节剂，并且也直接作用于消化道平滑肌。

13. 发明申请

WO1996038428A1 N-BENZYLDIOXOTHIAZOLIDYLBENZAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译： N-苯并二氧杂环戊二烯基苯并咪唑衍生物及其制备方法
公开(公告)号：WO1996038428A1
公开(公告)日：1996-12-05
申请号：PCT/JP1996001459
申请日：1996-05-30
申请人： KYORIN PHARMACEUTICAL CO., LTD. , MAEDA, Toshio , NOMURA, Masahiro , AWANO, Katsuya , KINOSHITA, Susumu , SATOH, Hiroya , MURAKAMI, Koji , TSUNODA, Masaki
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/34
CPC分类号： C07D417/12 , C07D277/34
摘要： Novel N-benzyldioxothiazolidylbenzamide derivatives represented by general formula (1) which improve insulin resistance and have potent hypoglycemic and lipid-lowering effects, wherein R and R are the same or different and each represents hydrogen, lower (C1-4) alkyl, lower (C1-3) alkoxy, lower (C1-3) haloalkyl, lower (C1-3) haloalkoxy, halogeno, hydroxy, nitro, amino optionally substituted by lower (C1-3) alkyl or a heterocycle, or R and R may be bonded to each other to thereby form methylenedioxy; R represents lower (C1-3) alkoxy, hydroxy or halogeno; and --- represents a double or single bond.
摘要翻译：由通式（1）表示的新型N-苄基二硫代噻唑烷基苯甲酰胺衍生物，其改善胰岛素抵抗并具有有效的降血糖和降脂作用，其中R 1和R 2相同或不同，各自表示氢，低级（C1- 4）烷基，低级（C 1-3）烷氧基，低级（C 1-3）卤代烷基，低级（C 1-3）卤代烷氧基，卤代，羟基，硝基，任选被低级（C 1-3）烷基或杂环取代的氨基，或 R 1和R 2可以彼此键合，从而形成亚甲二氧基; R 3表示低级（C 1-3）烷氧基，羟基或卤素; 并且 --- 表示双键或单键。

14. 发明申请

WO1996019472A1 8-ALKOXYQUINOLONECARBOXYLIC ACID HYDRATE WITH EXCELLENT STABILITY AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：具有优异稳定性的8-羟基喹啉酮羧酸水合物及其制造方法
公开(公告)号：WO1996019472A1
公开(公告)日：1996-06-27
申请号：PCT/JP1995002477
申请日：1995-12-05
申请人： KYORIN PHARMACEUTICAL CO., LTD. , MATSUMOTO, Toyomi , HARA, Masamoto , MIYASHITA, Kunio , KATO, Yukihiro
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D215/56 , C07D401/04
摘要： 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl )-4-oxo-3-quinolinecarboxylic acid sesquihydrate represented by formula (1) and excellent in stability.
摘要翻译：由式（1）表示的1-环丙基-6-氟-1,4-二氢-8-甲氧基-7-（3-甲基-1-哌嗪基）-4-氧代-3-喹啉羧酸倍半水合物，其稳定性优异。

15. 发明申请

WO1995007905A1 OPTICALLY ACTIVE IMIDAZOLIDINONE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：光活性的咪唑啉酮衍生物及其生产方法
公开(公告)号：WO1995007905A1
公开(公告)日：1995-03-23
申请号：PCT/JP1994001505
申请日：1994-09-12
申请人： KYORIN PHARMACEUTICAL CO., LTD. , TAKANO, Yasuo , OKAZAKI, Kei , HIRAYAMA, Takashi , ANRAKU, Tsuyoshi
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： An optically active imidazolidinone derivative represented by general formula (1), having a cholinergic activity (a muscarine M1 activity) and being useful for treating senile dementia, a pharmacologically acceptable acid-addition salt thereof, and a process for producing the same, wherein R and R may be the same or different and each represents hydrogen, halogen, optionally halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkoxycarbonyl, nitro, amino or cyano; and n represents 1 to 4.
摘要翻译：由通式（1）表示的具有胆碱能活性（毒蕈碱M1活性）并用于治疗老年性痴呆的光学活性咪唑烷酮衍生物及其药理学可接受的酸加成盐及其制备方法，其中R R 1可以相同或不同，各自表示氢，卤素，任选卤代的低级烷基，低级烷氧基，低级烷硫基，低级烷氧基羰基，硝基，氨基或氰基; n表示1〜4。

16. 发明申请

WO1992014730A1 THIAZOLIDINE-2,4-DIONE DERIVATIVE, SALT THEREOF, AND PRODUCTION THEREOF 审中-公开
标题翻译：噻唑烷-2,4-二酮衍生物，其盐及其生产
公开(公告)号：WO1992014730A1
公开(公告)日：1992-09-03
申请号：PCT/JP1992000190
申请日：1992-02-24
申请人： KYORIN PHARMACEUTICAL CO., LTD. , OHNOTA, Michiro , OKAMURA, Kyuya , HIRATA, Yoshihiro , MURAKAMI, Koji , OHASHI, Mitsuo
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D417/10
CPC分类号： C07D417/10
摘要： A novel thiazolidine-2,4-dione derivative with hypoglycemic and aldose reductase inhibitory activities, represented by general formula (1), a salt thereof, a process for producing the same, and a pharmaceutical containing the same, wherein R?1 and R2¿ may be the same or different from each other and each represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, nitro or amino which may be substituted by lower alkyl or lower alkanoyl; R3 represents hydrogen or lower alkyl; A represents lower alkylene or carbonyl; and B and W are different from each other and each represents lower alkylene, carbonyl or a free bond.

17. 发明申请

WO1989012055A1 ANTITUMOR AGENT 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1989012055A1
公开(公告)日：1989-12-14
申请号：PCT/JP1989000581
申请日：1989-06-07
申请人： KYORIN PHARMACEUTICAL CO., LTD. , KYOWA HAKKO KOGYO CO., LTD. , HOSOMI, Jiro , ASAHINA, Yoshikazu , SUZUE, Seigo
发明人： KYORIN PHARMACEUTICAL CO., LTD. , KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Thiazoloquinolonecarboxylic acid derivatives represented by general formula (I) [wherein R represents hydrogen or C1 - C6 lower alkyl, R and R each independently represents hydrogen, C1 - C6 lower alkyl or phenyl optionally substituted by 1 to 3 fluorine atoms, X and X each independently represents hydrogen or fluorine, and X represents halogen or ( alpha ) {( alpha ) represents ( beta ) (wherein R represents hydrogen or C1 - C3 lower alkyl optionally substituted by hydroxy, R represents hydrogen or alkoxycarbonyl, R independently represents hydrogen, methyl or ethyl, and n represents 0 or 1), piperazino, 3-methylpiperazino, 3-phenylpiperazino or 4-methylpiperazino}, and ---- represents a single bond or a double bond], and salts and hydrates thereof are useful as antitumor agents.
摘要翻译：由通式（I）表示的噻唑并喹啉羧酸衍生物[其中R表示氢或C1-C6低级烷基，R 1和R 2各自独立地表示氢，C1-C6低级烷基或任选被1至3个氟取代的苯基原子，X 1和X 3各自独立地表示氢或氟，X 2表示卤素或（α）{（α）表示（β）（其中R 5表示氢或C 1 -C 3低级任选被羟基取代的烷基，R 6表示氢或烷氧基羰基，R 7独立地表示氢，甲基或乙基，n表示0或1），哌嗪基，3-甲基哌嗪基，3-苯基哌嗪基或4-甲基哌嗪基} 和----表示单键或双键]，其盐和水合物可用作抗肿瘤剂。

18. 发明申请

WO1998024431A1 NOVEL N-SUBSTITUTED PYRROLIDINE DERIVATIVES AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：新型N-取代的吡咯烷衍生物及其制备方法
公开(公告)号：WO1998024431A1
公开(公告)日：1998-06-11
申请号：PCT/JP1997004306
申请日：1997-11-26
申请人： KYORIN PHARMACEUTICAL CO., LTD. , MIYACHI, Hiroyuki , HOSHINO, Masato , ANDO, Naoki , KOBAYASHI, Fumiyoshi
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/40
CPC分类号： C07D207/12
摘要： Novel N-substituted pyrrolidine derivatives having a highly selective and potent antagonism against smooth muscle muscarine receptors and being useful for the treatment of irritable bowel syndrome and the like, characterized by being represented by general formula (1) (wherein R represents a hydrogen atom, a halogen atom, or a lower alkoxy group and a process for preparing the same.
摘要翻译：新型N-取代的吡咯烷衍生物，其具有对平滑肌毒蕈碱受体的高度选择性和有效的拮抗作用，并且可用于治疗肠易激综合征等，其特征在于通式（1）（其中R表示氢原子，卤素原子或低级烷氧基及其制备方法。

19. 发明申请

WO1998022111A1 ANTI-HELICOBACTER PYLORI DRUGS 审中-公开
标题翻译：抗真菌药吡啶药物
公开(公告)号：WO1998022111A1
公开(公告)日：1998-05-28
申请号：PCT/JP1997004199
申请日：1997-11-19
申请人： KYORIN PHARMACEUTICAL CO., LTD. , MOMO, Kenjiro , ISHIBASHI, Yuji
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/445
CPC分类号： A61K31/4462
摘要： Anti-Helicobacter pylori drugs containing troxipide as the active ingredient and usable in preventing or treating various diseases in the onset or recurrence of which Helicobacter pylori participates, for example, gastrointestinal mucosal disorder, hyperammonemia, hepatitis, hepatic cirrhosis, gastric cancer and liver cancer.
摘要翻译：抗幽门螺旋杆菌药物含有作为活性成分的曲奇哌啶，可用于预防或治疗幽门螺杆菌发病或复发中的各种疾病，例如胃肠粘膜紊乱，高氨血症，肝炎，肝硬化，胃癌和肝癌。

20. 发明申请

WO1997022600A1 N-SUBSTITUTED DIOXOTHIAZOLIDYLBENZAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译： N-取代二氧杂环丁烷基苯甲酸衍生物及其制备方法
公开(公告)号：WO1997022600A1
公开(公告)日：1997-06-26
申请号：PCT/JP1996003664
申请日：1996-12-16
申请人： KYORIN PHARMACEUTICAL CO., LTD. , MAEDA, Toshio , NOMURA, Masahiro , AWANO, Katsuya , KINOSHITA, Susumu , SATOH, Hiroya , MURAKAMI, Koji , TSUNODA, Masaki
发明人： KYORIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/34
CPC分类号： C07D417/12 , C07D277/34
摘要： Novel N-substituted dioxothiazolidylbenzamide derivatives having an improved insulin resistance and potent hypoglycemic and hypolipidemic effects and represented by general formula (1), wherein R and R may be the same or different and each represents hydrogen, C1-4 alkyl, C1-3 alkoxy, C1-3 haloalkyl, C1-3 haloalkoxy, halogeno, or hydroxy, or R and R are bonded to each other to thereby form methylenedioxy; R represents hydrogen, C1-3 alkoxy, hydroxy, or halogeno; R represents hydrogen or C1-3 alkyl; n represents an integer of 0 to 2; and X represents N or CH.
摘要翻译：具有改善的胰岛素抵抗和有效的降血糖和降血脂作用并由通式（1）表示的新型N-取代的二氧代噻唑烷基苯甲酰胺衍生物，其中R 1和R 2可以相同或不同，各自代表氢，C1-4 烷基，C 1-3烷氧基，C 1-3卤代烷基，C 1-3卤代烷氧基，卤代或羟基，或R 1和R 2彼此键合，形成亚甲二氧基; R 3表示氢，C 1-3烷氧基，羟基或卤素; R 4表示氢或C 1-3烷基; n表示0〜2的整数， X表示N或CH。

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