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1. 发明申请

WO2019217926A8 APPLICATOR AND SYSTEM FOR PHARMACEUTICAL PREPARATION AND METHOD OF USE 审中-公开
公开(公告)号：WO2019217926A8
公开(公告)日：2019-11-14
申请号：PCT/US2019/031876
申请日：2019-05-10
申请人： BRICKELL BIOTECH, INC. , KAKEN PHARMACEUTICAL CO., LTD.
发明人： BRINKMAN, Herbert , KOLENG, John , ALZENSTAT, Aron , SKLAWER, Andrew , NAGAO, Tatsuro , TAKAOKA, Masayoshi
IPC分类号： A45D34/04 , A45D40/26 , A61M35/00 , A61Q15/00
摘要： An applicator and applicator system are provided for a topically or transdermally applying a pharmaceutical preparation or formulation. The applicator and applicator system can reduce drip during use, provide efficient transfer of a dose of the pharmaceutical preparation or formulation from the applicator to the skm of a patient, and can be used hands-free, which can reduce, prevent or eliminate cross-contamination to other areas, including undesired application to other parts of the skin or to other individuals. The applicator and applicator system include a therapeutic surface which can receive a single dose of the pharmaceutical preparation and can be manipulated by the user to transfer and apply the pharmaceutical preparation on a body surface.

2. 发明申请

WO2009088105A1 HUMANIZED ANTI-α9 INTEGRIN ANTIBODIES AND THE USES THEREOF 审中-公开
标题翻译：人类抗原抗体抗体及其用途
公开(公告)号：WO2009088105A1
公开(公告)日：2009-07-16
申请号：PCT/JP2009/050606
申请日：2009-01-13
申请人： GENE TECHNO SCIENCE CO., LTD. , KAKEN PHARMACEUTICAL CO., LTD. , KUMAR, Shankar , TSO, J., Yun , TSURUSHITA, Naoya , KON, Shigeyuki
发明人： KUMAR, Shankar , TSO, J., Yun , TSURUSHITA, Naoya , KON, Shigeyuki
IPC分类号： C12N15/09 , A61K39/395 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12P21/08 , G01N33/563 , G01N33/577
CPC分类号： C07K16/2839 , A61K2039/505 , C07K2317/24 , C07K2317/34 , C07K2317/56 , C07K2317/565
摘要： The present invention provides humanized antibodies that immunospecifically recognize human α9 integrin. Some of these antibodies inhibit the biological functions of the α9 integrin, thereby exhibiting therapeutic effects on various disorders or diseases that are associated with α9 integrin, including cancer, e.g., the growth and metastasis of a cancer cell, and inflammatory diseases, e.g., rheumatoid arthritis, osteoarthritis, hepatitis, bronchial asthma, fibrosis, diabetes, arteriosclerosis, multiple sclerosis, granuloma, an inflammatory bowel disease (ulcerative colitis and Crohn's disease), an autoimmune disease, and so forth.
摘要翻译：本发明提供免疫特异性识别人a9整联蛋白的人源化抗体。这些抗体中的一些抑制a9整联蛋白的生物学功能，从而对与α9整联蛋白（包括癌症）相关的各种疾病或疾病表现出治疗效果，例如癌细胞的生长和转移，以及炎性疾病，例如类风湿关节炎，骨关节炎，肝炎，支气管哮喘，纤维化，糖尿病，动脉硬化，多发性硬化，肉芽肿，炎性肠病（溃疡性结肠炎和克罗恩病），自身免疫性疾病等。

3. 发明申请

WO1994012473A1 ACETAMIDE DERIVATIVE 审中-公开
标题翻译：乙酰胺衍生物
公开(公告)号：WO1994012473A1
公开(公告)日：1994-06-09
申请号：PCT/JP1993001696
申请日：1993-11-18
申请人： KAKEN PHARMACEUTICAL CO., LTD. , ISHIYAMA, Nobuo , KOYAMA, Toshihiro , HAYASHIDA, Mitsuo , OTSUKA, Katsuyuki , FUJII, Masahiro , KIMURA, Kunio , HATA, Yoshiyuki , MIYAO, Nobuko
发明人： KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07C317/28
CPC分类号： C07D213/64 , C07C317/44 , C07C323/43 , C07D207/34 , C07D213/78 , C07D213/81 , C07D213/82 , C07D295/096 , C07D307/68 , C07D307/71 , C07D333/24 , C07D333/38 , C07D333/58 , C07D403/12 , Y10S514/927
摘要： An acetamide derivative represented by general formula (I) or a pharmacologically acceptable salt thereof; an intermediate for theproduction thereof; a remedy for peptic ulcer and gastritis containing the compound (I) as the active ingredient; and a method of treating peptic ulcer and gastritis with the compound (I).
摘要翻译：由通式（I）表示的乙酰胺衍生物或其药理学上可接受的盐; 生产中间体; 含有化合物（I）作为活性成分的消化性溃疡和胃炎的补救措施; 和化合物（I）治疗消化性溃疡和胃炎的方法。

4. 发明申请

WO1993015739A1 REMEDY FOR WOUND OR HEMORRHOID 审中-公开
标题翻译：为伤或救济补救
公开(公告)号：WO1993015739A1
公开(公告)日：1993-08-19
申请号：PCT/JP1993000151
申请日：1993-02-05
申请人： KAKEN PHARMACEUTICAL CO., LTD. , TORAY INDUSTRIES, INC. , OKUMURA, Makoto , OKUDA, Toshiaki , NAKAMURA, Tsutomu , YAMIJA, Motoyuki
发明人： KAKEN PHARMACEUTICAL CO., LTD. , TORAY INDUSTRIES, INC.
IPC分类号： A61K31/557
CPC分类号： A61K31/5575 , A61K31/557 , A61K31/5585 , Y10S514/882 , Y10S514/925 , Y10S514/928
摘要： A remedy for wounds or hemorrhoids, in particular, an external preparation containing at least one member selected among prostaglandin I2, prostaglandin E1 and derivatives thereof, in particular, beroprost, one of the prostaglandin I2 derivatives, or a salt thereof as the active ingredient; and a therapy for wounds or hemorrhoids characterized by administering the above active ingredient.

5. 发明申请

WO1999018113A1 TAXOID DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：紫杉醇衍生物及其生产方法
公开(公告)号：WO1999018113A1
公开(公告)日：1999-04-15
申请号：PCT/JP1997003615
申请日：1997-10-08
申请人： BIO RESEARCH CORPORATION OF YOKOHAMA , ENSUIKO SUGAR REFINING CO., LTD. , KAKEN PHARMACEUTICAL CO., LTD. , MANDAI, Tadakatsu , OKUMOTO, Hiroshi , HARA, Koji , MIKUNI, Katsuhiko , HARA, Kozo , TSUCHIYA, Yoshinori , NAKAMURA, Kosho , UMETSU, Teruhiko
发明人： BIO RESEARCH CORPORATION OF YOKOHAMA , ENSUIKO SUGAR REFINING CO., LTD. , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07H15/04
CPC分类号： C07H15/04 , C07H15/26
摘要： To develop galactose or mannose derivatives such as docetaxel improved both in solubility and physiological activity to thereby give efficacious remedies for cancer while inposing lessened burden to patients. Taxoid derivatives consisting of paclitaxel, docetaxel or 10-deacetylbaccatin III bonded via a spacer to galactose or mannose; and a process for producing taxoid derivatives characterized by reacting paclitaxel, docetaxel or 10-deacetylbaccatin III with hydroxygalactoside tetrabenzylacetate or hydroxymannoside tetrabenzylacetate and debenzylating the reaction product optionally followed by detriethylsilylation.
摘要翻译：为了发展半乳糖或甘露糖衍生物如多西紫杉醇，改善了溶解性和生理活性，从而为癌症提供了有效的补救措施，同时对患者减轻了负担。由紫杉醇，多西紫杉醇或通过间隔物与半乳糖或甘露糖键合的10-脱乙酰基浆果赤霉素III组成的紫杉烷衍生物; 以及生产紫杉醇衍生物的方法，其特征在于使紫杉醇，多西紫杉醇或10-脱乙酰基浆果赤霉素III与羟基半乳糖苷四苄基乙酸酯或羟基甘露糖苷四苄基乙酸酯反应，然后任选地进行脱乙基硅烷化脱苄基化。

6. 发明申请

WO1997041864A1 OPHTHALMIC PREPARATIONS 审中-公开
标题翻译：眼科准备
公开(公告)号：WO1997041864A1
公开(公告)日：1997-11-13
申请号：PCT/JP1997001504
申请日：1997-05-01
申请人： KAKEN PHARMACEUTICAL CO., LTD. , TORAY INDUSTRIES, INC. , IKARI, Takashi , MATSUMURA, Yuzuru , NAKAMURA, Tsutomu , YAJIMA, Motoyuki , KURUMATANI, Hajimu , KAWASHIMA, Ayako , ISOGAYA, Masafumi , WAKITA, Hisanori
发明人： KAKEN PHARMACEUTICAL CO., LTD. , TORAY INDUSTRIES, INC.
IPC分类号： A61K31/557
CPC分类号： A61K31/5585 , C07D307/93 , Y10S514/913
摘要： Ophthalmic preparations exhibiting excellent pharmacological effects against various ophthalmic diseases, which comprise 4,8-inter-m-phenyleneprostaglandin I2 derivatives of general formula (I) or pharmacologically acceptable salts thereof as active ingredients.
摘要翻译：对各种眼科疾病具有优异的药理作用的眼科制剂，其包含通式（I）的4-8-间间苯二甲基前列腺素I2衍生物或其药理学上可接受的盐作为活性成分。

7. 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。

8. 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。

9. 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。

10. 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。

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