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11. 发明申请

WO1996020195A1 HYDANTOIN DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND HERBICIDES COMPRISING THE SAME AS ACTIVE INGREDIENTS 审中-公开
标题翻译： HYDANTOIN衍生物，其制造方法和包含其的除草剂作为活性成分
公开(公告)号：WO1996020195A1
公开(公告)日：1996-07-04
申请号：PCT/JP1995002683
申请日：1995-12-26
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , YANO, Tomoyuki , OKANO, Natuko , UGAI, Sadayuki , YAMADA, Osamu
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A01N43/90
摘要： Novel hydantoin derivatives having excellent herbicidal activities, a process for producing the same and herbicides comprising the same as active ingredients. The hydantoin derivatives represented by general formula (1) are produced by reacting an aryl isocyanate derivative represented by general formula (2), with a dehydropipecolinic acid derivative represented by general formula (3).
摘要翻译：具有优异除草活性的新型乙内酰脲衍生物，其制备方法以及含有活性成分的除草剂。由通式（1）表示的乙内酰脲衍生物通过使通式（2）表示的芳基异氰酸酯衍生物与通式（3）表示的脱氢哌啶酸衍生物反应来制备。

12. 发明申请

WO1995005840A1 PERIODONTAL DISEASE REMEDY 审中-公开
标题翻译：周围疾病补救
公开(公告)号：WO1995005840A1
公开(公告)日：1995-03-02
申请号：PCT/JP1993001211
申请日：1993-08-25
申请人： KAKEN PHARMACEUTICAL CO., LTD. , ASANO, Taiji , SUGIMOTO, Hajime , TERASHIMA, Akio , NAKANO, Yoshiko , AMAKAWA, Masahiro , SAGA, Katumasa
发明人： KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K37/24
CPC分类号： A61K38/1825
摘要： A periodontal disease remedy containing a basic fibroblast growth factor as the active ingredient, a method of treating periodontal diseases by using the same, and an implant fixation promoter and a dentin regenerating agent each containing the same. The remedy is excellent in the safety and effectiveness in healing the missed and/or damaged periodontium ultimately by regeneration or attachment of new material.
摘要翻译：包含碱性成纤维细胞生长因子作为活性成分的牙周病的治疗方法，使用该牙周病的牙周病的治疗方法，以及植入物固定促进剂和牙本质再生剂。补救措施在最终通过再生或附加新材料治愈错过和/或损坏牙周组织的安全性和有效性方面非常出色。

13. 发明申请

WO1993019039A1 TETRAHYDROPHTHALAMIDE DERIVATIVE, INTERMEDIATE FOR PRODUCING THE SAME, PRODUCTION OF BOTH, AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：四氢衍生物衍生物，用于生产它们的中间体，含有它们的二氧化碳和除草剂作为活性成分
公开(公告)号：WO1993019039A1
公开(公告)日：1993-09-30
申请号：PCT/JP1993000360
申请日：1993-03-25
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , MATSUKAWA, Tomoko , YANO, Tomoyuki , EJIRI, Emiko , AIZAWA, Kiyomi , SHIKAKURA, Koichi , YOSHII, Tomoko , UGAI, Sadayuki , YAMADA, Osamu , KISHI, Shigeki
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07C233/60
CPC分类号： C07D213/40 , A01N37/30 , A01N37/32 , A01N37/46 , A01N43/08 , A01N43/12 , A01N43/40 , A01N43/78 , A01N47/16 , C07C217/88 , C07C233/60 , C07C233/62 , C07C233/63 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/62 , C07C2603/66 , C07D211/58 , C07D277/04 , C07D295/185 , C07D307/52 , C07D307/90
摘要： A 3,4,5,6-tetrahydrophthalamide derivative and a 3,4,5,6-tetrahydroisophthalimide derivative, both having an excellent efficay as the active ingredient of a herbicide, and an industrial process for efficiently producing these higher-performance, herbicidally active compounds. A tetrahydrophthalamide derivative represented by general formula (I) is produced by the reaction of a tetrahydrophthalimide derivative, prepared by the reaction of a halogenated 5-cycloalkyloxyaniline derivative with 3,4,5,6-tetrahydrophthalic anhydride, or of the tetrahydroisophthalimide derivative of the invention with various amines. These tetrahydrophthalamide and tetrahydroisophthalimide derivatives have an excellent herbicidal effect in the treatment of lowland and upland soils and foliage treatment. The tetrahydroisophthalimide derivative is useful also as an intermediate for producing the tetrahydrophthalamide derivative and the like.
摘要翻译：作为除草剂的活性成分具有优异效果的3,4,5,6-四氢邻苯二甲酰亚胺衍生物和3,4,5,6-四氢邻苯二甲酰亚胺衍生物，以及用于有效地生产这些更高性能，除草的工业方法活性化合物。或通过卤代5-环烷氧基苯胺衍生物与3,4,5,6-四氢邻苯二甲酸酐的反应制备的四氢邻苯二甲酰亚胺衍生物或四氢邻苯二甲酰亚胺衍生物的反应制备由通式（I）表示的四氢邻苯二甲酰胺衍生物发明与各种胺类。这些四氢邻苯二甲酰胺和四氢邻苯二甲酰亚胺衍生物在处理低地和高地土壤和叶面处理方面具有优异的除草效果。四氢间苯二甲酰亚胺衍生物也可用作制备四氢邻苯二甲酰胺衍生物等的中间体。

14. 发明申请

WO1997011939A1 PROCESS FOR THE PREPARATION OF 4-METHYLENEPIPERIDINES 审中-公开
标题翻译：制备4-甲基哌啶的方法
公开(公告)号：WO1997011939A1
公开(公告)日：1997-04-03
申请号：PCT/JP1996002810
申请日：1996-09-26
申请人： KAKEN PHARMACEUTICAL CO., LTD. , NAITO, Takanobu
发明人： KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D211/16
CPC分类号： C07D211/62 , C07D211/22 , C07D211/70
摘要： A process for the preparation of 4-methylenepiperidines of general formula (VII) which comprises reacting an isonipecotate of general formula (I) (wherein R is methyl or ethyl) with an acylating agent of general formula (II): R X or the general formula (II'): (R )2O (wherein R is benzoyl or acetyl; and X is chlorine or bromine) in the presence or absence of a base to form an ester of general formula (III) (wherein R and R are each as defined above), reducing the ester with sodium borohydride or lithium borohydride in an organic solvent containing methanol, reacting the alcohol thus obtained with a halogenating agent without any solvent or in an organic solvent in the presence or absence of a base to obtain a halide, reacting this halide with a dehydrohalogenating agent in an organic solvent to obtain a methylene compound of general formula (VI) (wherein R is as defined above), and hydrolyzing the methylene compound with a strong alkali in water or an organic solvent containing water.
摘要翻译：制备通式（Ⅶ）的4-亚甲基哌啶的方法，该方法包括使通式（I）的异哌啶酸酯（其中R 1为甲基或乙基）与通式（II）的酰化剂反应：（R 2）2 O（其中R 2是苯甲酰基或乙酰基，X是氯或溴）在存在或不存在碱的情况下形成将通式（III）（其中R 1和R 2各自如上所定义），在含有甲醇的有机溶剂中用硼氢化钠或硼氢化锂还原酯，将所得醇与卤化剂反应，在有机溶剂存在或不存在下，在有机溶剂中，在有机溶剂存在或不存在下，得到卤化物，使该卤化物与脱卤化氢剂在有机溶剂中反应，得到通式（VI）的亚甲基化合物（其中R 2如上所定义）并用强碱在水或有机溶剂中水解亚甲基化合物含水。

15. 发明申请

WO1996033992A1 OPTICALLY ACTIVE QUINOLINECARBOXYLIC ACID DERIVATIVES AND SALTS THEREOF 审中-公开
标题翻译：光学活性喹啉羧酸衍生物及其盐
公开(公告)号：WO1996033992A1
公开(公告)日：1996-10-31
申请号：PCT/JP1996001120
申请日：1996-04-24
申请人： KAKEN PHARMACEUTICAL CO., LTD. , SHIBATA, Tetsuo , FUKUI, Hideto , NAITO, Takanobu , NAKANO, Jun , MAEJIMA, Tetsuro , TATSUMI, Yoshiyuki , ARIKA, Tadashi
发明人： KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D471/04
摘要： Optically active trans-quinolinecarboxylic acid derivatives represented by general formula (I), having potent antibacterial activities against gram-positive bacteria and MRSA, and salts thereof, antibacterial agents containing the same as the active ingredient; and optically active pyrrolidine derivatives represented by general formula (II) and salts thereof, serving as intermediates for the synthesis of the above quinolinecarboxylic acid derivatives.
摘要翻译：由通式（I）表示的对革兰氏阳性菌和MRSA具有强力抗菌活性的光学活性反式喹啉羧酸衍生物及其盐，含有与活性成分相同的抗菌剂; 和由通式（II）表示的光学活性吡咯烷衍生物及其盐，用作合成上述喹啉羧酸衍生物的中间体。

16. 发明申请

WO1996026930A1 PROCESS FOR THE PREPARATION OF 3-(SUBSTITUTED PHENYL)-5-ALKYLIDENE-1,3-OXAZOLIDINE-2,4-DIONE DERIVATIVES 审中-公开
标题翻译：制备3-（取代的苯基）-5-甲氧基-1,3-氧杂环丁烷-2,4-二酮衍生物的方法
公开(公告)号：WO1996026930A1
公开(公告)日：1996-09-06
申请号：PCT/JP1996000430
申请日：1996-02-26
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , MASUDA, Katsuyuki , YANO, Tomoyuki , OHNO, Ryuta , MATUKAWA, Tomoko , IMAI, Kiyomi , OKANO, Natsuko , YOSHII, Tomoko , MOURI, Takehito
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D263/44
CPC分类号： C07D263/44 , C07C67/31 , C07C69/708
摘要： An industrial process for efficiently preparing a 3-(substituted phenyl)-5-isopropylidene-1,3-oxazolidine-2,4-dione derivative having a potent herbicidal activity without using phosgene or the like. More precisely, a process for preparing a 3-(substituted phenyl)-5-alkylidene-1,3-oxazolidine-2,3-dione derivative of general formula (III) by reacting an N-(substituted phenyl)carbamate of general formula (I) with a 2-hydroxy-3-alkenoate of general formula (II) or a 3-alkoxy-2-hydroxyalkanoate of general formula (IV), wherein Ar is substituted phenyl; R is C1-C6 alkyl; R and R are each independently hydrogen or C1-C12 alkyl; and R and R are each independently C1-C6 alkyl.
摘要翻译：用于有效地制备具有强效除草活性而不使用光气等的3-（取代苯基）-5-异亚丙基-1,3-恶唑烷-2,4-二酮衍生物的工业方法。更精确地说，通过使通式（III）的N-（取代苯基）氨基甲酸酯与通式（III）的N-（取代苯基）-5-亚烷基-1,3-恶唑烷-2,3-二酮衍生物（I）与通式（II）的2-羟基-3-烯酸酯或通式（IV）的3-烷氧基-2-羟基链烷酸酯，其中Ar是取代的苯基; R 1是C 1 -C 6烷基; R 2和R 3各自独立地为氢或C 1 -C 12烷基; R 4和R 5各自独立地为C 1 -C 6烷基。

17. 发明申请

WO1995010509A1 4-IMINOOXAZOLIDIN-2-ONE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译： 4-IMINOOXAZOLIDIN-2-ONE衍生物，其制备方法和含有它们的除草剂作为活性成分
公开(公告)号：WO1995010509A1
公开(公告)日：1995-04-20
申请号：PCT/JP1994001683
申请日：1994-10-07
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , MATSUKAWA, Tomoko , YANO, Tomoyuki , MASUDA, Katsuyuki , YOSHII, Tomoko , MOURI, Takehito , UGAI, Sadayuki , YAMADA, Osamu
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D263/48
CPC分类号： C07D263/48 , A01N43/76
摘要： A 4-iminooxazolidin-2-one derivative represented by general formula (1) (wherein X represents hydrogen or halogen; X represents hydrogen, halogen or alkyloxy; and X represents hydrogen, halogen, alkyloxy, cycloalkyloxy or alkynyloxy); a process for producing the above compound by the reaction of an aryl isocyanate represented by general formula (2) with methacrolein cyanohydrin in the presence of a base; a herbicide containing the above compound as the active ingredient; and a process for producing an oxazolidinedione derivative useful as a herbicide by hydrolyzing the above compound.
摘要翻译：由通式（1）表示的4-亚氨基恶唑烷-2-酮衍生物（其中X 1表示氢或卤素; X 2表示氢，卤素或烷氧基; X 3表示氢，卤素，烷氧基，环烷氧基或炔氧基）; 通过在碱存在下通过通式（2）表示的异氰酸酯与异丁烯醛氰醇反应制备上述化合物的方法; 含有上述化合物作为活性成分的除草剂; 以及通过水解上述化合物制备可用作除草剂的恶唑烷二酮衍生物的方法。

18. 发明申请

WO1994018167A1 SUBSTITUTED DIBENZYLAMINE DERIVATIVE 审中-公开
标题翻译：取代二苯胺衍生物
公开(公告)号：WO1994018167A1
公开(公告)日：1994-08-18
申请号：PCT/JP1994000132
申请日：1994-01-31
申请人： KAKEN PHARMACEUTICAL CO., LTD. , MAEDA, Tetsuya , INOGUCHI, Kiyoshi , NAKANO, Jun , ASANO, Taiji , ARIKA, Tadashi
发明人： KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/325
CPC分类号： C07D207/333 , C07D263/32 , C07D333/16 , C07D333/18
摘要： A substituted dibenzylamine derivative represented by general formula (I) or a salt thereof; and a drug and a method for preventing and treating hyperlipemia, hypercholesterolemia or arteriosclerosis by using the same; wherein R represents lower alkyl or lower alkenyl; R represents hydrogen, lower alkyl or lower alkoxy; and R represents phenyl or thienyl each substituted by a heterocyclic group having one to four heteroatoms.
摘要翻译：由通式（I）表示的取代二苄胺衍生物或其盐; 以及通过使用它们预防和治疗高脂血症，高胆固醇血症或动脉硬化的药物和方法; 其中R 1表示低级烷基或低级烯基; R 2表示氢，低级烷基或低级烷氧基; 并且R 3表示苯基或噻吩基，各自被具有一至四个杂原子的杂环基取代。

19. 发明申请

WO1992001671A1 HETEROCYCLE-SUBSTITUTED BENZENE DERIVATIVE, PRODUCTION THEREOF, AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：取代苯并噻唑衍生物，其生产物和含有它们的除草剂作为活性成分
公开(公告)号：WO1992001671A1
公开(公告)日：1992-02-06
申请号：PCT/JP1991000950
申请日：1991-07-16
申请人： CHISSO CORPORATION , SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , YAMASHITA, Mitsuo , TATENO, Tomoko , EJIRI, Emiko , HARASAWA, Kikuko , ONJI, Yuichi , UGAI, Sadayuki , NAGATO, Shoin
发明人： CHISSO CORPORATION , SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , A01N37/32 , A01N43/56 , C07C69/96 , C07C205/43 , C07C217/88 , C07C219/34 , C07C271/28 , C07C2601/08 , C07C2601/14 , C07D231/56
摘要： A heterocycle-substituted benzene derivative represented by general formula (I) wherein R represents C3 to C8 cycloalkyl, X represents halogen, and Z represents (Ia) or (Ib) provided that the cycloalkyl may be substituted with C1 to C6 alkyl. This compound is excellent in that it has a remarkably high herbicidal effect against weeds growing in both upland and lowland fields in a low dose, while it has a remarkably low phytotoxicity against main crops.

20. 发明申请

WO1996022285A1 1,2,4-TRIAZINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND HERBICIDE COMPRISING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译： 1,2,4-三唑衍生物，其生产方法和包含其的除草剂作为活性成分
公开(公告)号：WO1996022285A1
公开(公告)日：1996-07-25
申请号：PCT/JP1996000077
申请日：1996-01-19
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , SHIKAKURA, Koiti , YANO, Tomoyuki , ISHIKAWA, Chikako , UGAI, Sadayuki , YAMADA, Osamu
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D253/075
CPC分类号： C07D253/075 , A01N43/707
摘要： 1,2,4-Triazine derivatives represented by general formula (1) and having excellent effects as an efficacious active ingredient of a herbicide and a process for producing the same, wherein X represents halogeno; X represents halogeno; X represents C1-12 alkoxy, C3-6 alkenyloxy, C3-6 alkynyloxy, C3-10 cycloalkyloxy or C7-8 aralkyloxy; R represents hydrogen, C1-12 alkyl, C3-8 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl or phenyl; R represents hydrogen, C1-12 alkyl, C3-8 alkenyl, C3-6 alkynyl, C3-8 cycloalkyl or C7-8 aralkyl; and Y represents oxygen or sulfur. The compounds can be produced by reacting a 4-(2,4-dihalogeno-5-alkoxyphenyl)thiosemicarbazide with an alpha -ketoester and exert an excellent herbicidal effect in upland and paddy soil treatments and foliage treatments.
摘要翻译：通式（1）表示的1,2,4-三嗪衍生物作为除草剂的有效活性成分具有优异的效果及其制造方法，其中X 1表示卤代; X 2表示卤代; X 3表示C 1-12烷氧基，C 3-6烯氧基，C 3-6炔氧基，C 3-10环烷氧基或C 7-8芳烷氧基; R 1表示氢，C 1-12烷基，C 3-8烯基，C 3-8环烷基，C 3-8环烯基或苯基; R 3表示氢，C 1-12烷基，C 3-8烯基，C 3-6炔基，C 3-8环烷基或C 7-8芳烷基; Y表示氧或硫。该化合物可以通过使4-（2,4-二卤代-5-烷氧基苯基）氨基硫脲与α-酮酯反应并在高地和稻田土壤处理和叶面处理中发挥出色的除草效果来制备。

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