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1. 发明授权

EP3040329B1 AROMATIC COMPOUND AND USE THEREOF IN THE TREATMENT OF DISORDERS ASSOCIATED WITH BONE METABOLISM 失效
公开(公告)号：EP3040329B1
公开(公告)日：2018-10-10
申请号：EP14840281.1
申请日：2014-08-29
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： SHIRAHASE, Hiroaki , TAKAHASHI, Kenji , SHOJI, Yoshimichi , TAKEDA, Shigemitsu
IPC分类号： C07D205/04 , A61K31/165 , A61K31/275 , A61K31/341 , A61K31/351 , A61K31/382 , A61K31/443 , A61K31/444 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61P19/00 , A61P19/10 , C07C235/84 , C07D211/46 , C07D295/02 , C07D295/08 , C07D295/14
CPC分类号： C07D205/04 , C07C235/84 , C07C237/40 , C07D211/46 , C07D295/14 , C07D295/15 , C07D295/155 , C07D307/20 , C07D307/33 , C07D309/12 , C07D319/12 , C07D335/02 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14
摘要： Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.

2. 发明公开

EP1915996A1 Agents for treating intraocular inflammation caused by irradiation with lasers, containing 1,4-dihydropyridine derivatives 审中-公开
标题翻译： Mittel mit 1,4-Dihydropyridinderivaten zur Behandlung durch Laserstrahlung hervorgerufener introkularerEntzündungen
公开(公告)号：EP1915996A1
公开(公告)日：2008-04-30
申请号：EP08001756.9
申请日：2000-01-27
申请人： Senju Pharmaceutical Co., Ltd. , Kyoto Pharmaceutical Industries, Ltd.
发明人： Waki, Mitsunori
IPC分类号： A61K31/496 , A61P27/00 , A61P29/00 , C07D211/90
CPC分类号： A61K31/496
摘要： The present invention provides a 1,4-dihydropyridine derivative of the formula (I)

wherein X 1 and X 2 are the same or different and each is hydrogen atom, fluoromethyl, fluoromethoxy, halogen, cyano or nitro, R 1 is lower alkyl, R 2 is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, hetero ring-alkyl, haloalkyl, alkenyl or alkynyl, A is alkylene having a carbon atom bonded with two alkyls and 5 or more carbon atoms in total, and m is an integer of 1 to 3,
or an acid addition salt thereof, and a medicament containing said compound of formula (I) as an active ingredient for topically treating intraocular inflammation caused by laser irradiation.
摘要翻译：本发明提供式（I）的1,4-二氢吡啶衍生物，其中X 1和X 2相同或不同，各自为氢原子，氟甲基，氟甲氧基，卤素，氰基或硝基，R 1为低级烷基， R 2是酰基，烷氧基羰基，酰基烷基，N-烷基取代的氨基甲酰基烷基，烷氧基烷基，烷氧基羰基烷基，酰氧基烷基，硝基烷基，氰基烷基，杂环烷基，卤代烷基，烯基或炔基，A是具有与两个烷基和5个或更多的碳原子，m为1〜3的整数，或其酸加成盐，以及含有上述式（I）化合物作为局部治疗由激光照射引起的眼内炎的有效成分的药物。

3. 发明公开

EP1857444A1 TETRAHYDROISOQUINOLINE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
标题翻译： DEREN MEDIZINISCHE VERWENDUNG四氯乙烯
公开(公告)号：EP1857444A1
公开(公告)日：2007-11-21
申请号：EP06729291.2
申请日：2006-03-10
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： TAKAHASHI, K., c/o KYOTO PHARMACEUTICAL IND. LTD. , SHIRAHASE, H., c/o KYOTO PHARMACEUTICAL IND. LTD. , KUNISHIRO, K., c/o KYOTO PHARMACEUTICAL IND. LTD. , KASAI, M., c/o KYOTO PHARMACEUTICAL IND. LTD.
IPC分类号： C07D217/26 , A61K31/472 , A61K31/496 , A61K31/5377 , A61P3/06 , A61P9/10 , A61P29/00 , A61P43/00 , C07D401/12
CPC分类号： C07D401/12 , C07D217/26 , C07D401/06
摘要： The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有优异的ACAT抑制活性和/或抗氧化作用的四氢异喹啉化合物，特别是由式（I）表示的新化合物（其中各符号如说明书所述）及其药学上可接受的盐。

4. 发明公开

EP1398314A1 CARBAPENEM COMPOUND 审中-公开
标题翻译： CARBAPENEM VERBINDUNG
公开(公告)号：EP1398314A1
公开(公告)日：2004-03-17
申请号：EP02771714.9
申请日：2002-05-17
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： MATSUI, Hiroshi
IPC分类号： C07D477/20 , A61K31/407 , A61P31/04
CPC分类号： C07D477/20
摘要： A carbapenem compound represented by the formula (I'):
wherein each symbol is as defined in the specification, and an antibacterial agent containing this compound as an active ingredient are provided.
The carbapenem compound of the present invention is superior in absorbability from the gastrointestinal tract by oral administration and extremely useful for the prophylaxis or treatment of infectious diseases (particularly, bacterial infectious diseases).
摘要翻译：新的碳青霉烯化合物（I）。式（I）的碳青霉烯化合物是新的。 [图] R 1CH 2OCOC（Me）3，CH 2OCOOCH（Et）2，CH（Me）OCOOCH（Et）2或CH 2OCOOC 3; 环：环己基或环戊基; R 2CH 2CH 2CH 3，CH 2CH 3或CH（Me）3; 条件是：（1）当R 1 = CH 2 OCOC（Me）3时，R 2 = CH 2 CH 2 CH 3; 和（2）当R 1 = CH 2 COO 2Cyc时，R 2不是Et。活性：抗菌。在给予新戊酰氧基甲基（1R，5S，6S）-2 - [（3S，5S） - （5-N，N-二甲基氨基羰基-1-丁酰氧基甲氧基羰基）吡咯烷-3-基硫基] -6 - [（1R ）-1-羟基乙基] -1-甲基碳代青霉-2-烯-3-羧酸酯（Ia）以20mg / kg口服得到5.06μg/ hr的AUC（0-3小时）。行动机制：无给予。

5. 发明公开

EP0937457A1 REMEDIES FOR ALLERGIC DERMATITIS 失效
标题翻译： ARZNEIMITTEL GEGEN ALLERGISCHE DERMATITIS
公开(公告)号：EP0937457A1
公开(公告)日：1999-08-25
申请号：EP97935880.1
申请日：1997-08-25
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： SHIRAHASE, Hiroaki , YOSHIMI, Akihisa , NAKAMURA, Shohei , KANDA, Mamoru , FUKATA, Fumio
IPC分类号： A61K31/35
CPC分类号： C07D311/24 , A61K31/352 , Y10S514/886
摘要： A therapeutic agent for allergic dermatitis caused by type IV allergic reaction, which contains diethyl L-lysylcromoglycate of the formula
or a nontoxic salt thereof as an active ingredient. This therapeutic agent for allergic dermatitis is effective for the treatment of allergic dermatitis caused by type IV allergic reaction, such as contact dermatitis mainly induced by type IV allergic reaction and atopic dermatitis induced by type I and type IV allergic reactions.
摘要翻译：由IV型过敏反应引起的过敏性皮炎的治疗剂，其包含式CHEM的L-赖氨酰色甘酸二乙酯或其无毒盐作为活性成分。这种过敏性皮炎治疗剂对于治疗由IV型过敏反应引起的过敏性皮炎，如主要由IV型过敏反应引起的接触性皮炎和I型和IV型过敏反应引起的特应性皮炎是有效的。

6. 发明公开

EP0597112A1 NOVEL IMIDAZOLE DERIVATIVE, PHARMACEUTICAL USE THEREOF, AND INTERMEDIATE THEREFOR 失效
标题翻译： IMIDAZOLDERIVATE，IHRE PHARMAZEUCHSCHE VERWENDUNG UND IHRE INTERMEDIATE。
公开(公告)号：EP0597112A1
公开(公告)日：1994-05-18
申请号：EP93906837.5
申请日：1993-03-26
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： MATSUI, Hiroshi , KAMIYA, Shoji, 202, Dai-5-Kopo-Nakagawa , SHIRAHASE, Hiroaki , NAKAMURA, Shohei, 6004, Rezidensu-Bere-Shanburu
IPC分类号： C07D401/14 , C07D403/04 , C07D403/06 , A61K31/415 , A61K31/445 , A61K31/495
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： An imidazole derivative represented by general formula (I), wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. A process for producing the derivative or salt, and a pharmaceutical use thereof, in particular, a prophylactic and/or therapeutic agent for diseases induced by thromboxane A₂ or histamine. A compound represented by genenral formula (II) or (IV), wherein each symbol is as defined in the specification. The imidazole derivative and the salt are useful as a prophylactic and/or therapeutic agent for diseases induced by thromboxane A₂ or histamine, and the compounds (II) and (IV) are novel.
摘要翻译：由通式（I）表示的咪唑衍生物，其中每个符号如说明书中所定义，或其药学上可接受的盐。用于制备衍生物或盐的方法及其药物用途，特别是由血栓素A2或组胺诱导的疾病的预防和/或治疗剂。由通式（II）或（IV）表示的化合物，其中每个符号如说明书中所定义。咪唑衍生物和盐可用作由血栓素A2或组胺诱导的疾病的预防和/或治疗剂，化合物（II）和（IV）是新颖的。

7. 发明公开

EP0293771A3 Cephalosporin compound and pharmaceutical composition thereof 失效
标题翻译： CEPHOROSPORIN化合物及其药物组合物
公开(公告)号：EP0293771A3
公开(公告)日：1990-10-17
申请号：EP88108456.0
申请日：1988-05-27
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： Nishizawa, Susumu , Muro, Hiroyuki , Kasai, Masayasu , Hatano, Satoru , Kamiya, Syouzi 202, Nakagawa Co.op 5 , Kakeya, Nobuharu , Kitao, Kazuhiko
IPC分类号： C07D501/20 , C07D277/20 , C07D285/08 , A61K31/545
CPC分类号： C07D277/587 , C07D285/08 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula (I): wherein R 1 and R 5 independently represented a hydrogen atom or a protective group for an amino group; R 2 represents an alkyl group or a cycloalkyl group; R 3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R 4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds. Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.

8. 发明公开

EP0186706A1 PROCESS FOR PREPARING CEPHALOSPORIN DERIVATIVES 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON CEPHALOSPORIN-ABKÖMMLINGEN。
公开(公告)号：EP0186706A1
公开(公告)日：1986-07-09
申请号：EP84902068.0
申请日：1984-05-24
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： NISHIZAWA, Susumu 1, Yamaden, Shimomisu , TAMAKI, Satoshi , KAKEYA, Nobuharu , KITAO, Kazuhiko 12, Sandan Osa-cho Matsugasaki
IPC分类号： C07D501/04 , C07D501/06
CPC分类号： C07D501/04
摘要： A process for preparing cephalosporin derivatives represented by general formula (I), which comprises reacting a compound of general formula (II) or its reactive derivative with a compound of general formula (III) or eliminating an R' group from a compound of general formula (IV). In the above-mentioned formulae, R' represents formyl, t-butoxycarbonyl, 1-methyl-2-methoxycarbonylvinyl, 1-methyl-2- ethoxycarbonylvinyl, benzyloxycarbonyl, p-methoxybenzyloxycarbonyl, chloroacetyl, trityl, silyl or 2,2,2-trichloroethoxycarbonyl, and R 2 represents a hydrogen atom or a hydroxy group.
摘要翻译：一种制备由通式（I）表示的头孢菌素衍生物的方法，其包括使通式（II）的化合物或其反应性衍生物与通式（III）的化合物反应或从通式（I）的化合物中除去R min基团（IV）。在上述式中，R 1表示甲酰基，叔丁氧基羰基，1-甲基-2-甲氧基羰基乙烯基，1-甲基-2-乙氧基羰基乙烯基，苄氧基羰基，对甲氧基苄氧羰基，氯乙酰基，三苯甲基，甲硅烷基或2,2， 2-三氯乙氧基羰基，R 2表示氢原子或羟基。

9. 发明公开

EP0153418A1 MANDELIC ACID DERIVATIVES 失效
标题翻译：曼德尔酸衍生物
公开(公告)号：EP0153418A1
公开(公告)日：1985-09-04
申请号：EP84903200.8
申请日：1984-08-27
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： NISHIZAWA, Susumu , TAMAKI, Satoshi , KAWAMURA, Toshiyuki , KAKEYA, Nobuharu , KITAO, Kazuhiko
IPC分类号： C07C101/18 , C07C103/38 , C07C125/065 , C07D309/12 , C07D501/32 , C07F7/04
CPC分类号： C07D207/16
摘要： Mandelic acid derivatives represented by general formula (I), wherein R 1 represents a hydrogen atom or a hydroxy group, X represents a halogen atom or OR 2 (wherein R 2 represents a hydrogen atom, benzyl, benzhydryl, t-butyl, tetrahydropyranyl or silyl), and A represents an optionally protected amino acid residue, or salts thereof. These compounds are useful as intermediates for synthesizing cephalosporin derivatives, etc.
摘要翻译：由通式（I）表示的扁桃酸衍生物，其中R1代表氢原子或羟基，X代表卤原子或OR2（其中R2代表氢原子，苄基，二苯甲基，叔丁基，四氢吡喃基或甲硅烷基）， A代表任选保护的氨基酸残基或其盐。这些化合物可用作合成头孢菌素衍生物等的中间体。

10. 发明公开

EP3607944A1 NOVEL CYCLIN-DEPENDENT KINASE 8 AND/OR 19 INHIBITOR 无效
公开(公告)号：EP3607944A1
公开(公告)日：2020-02-12
申请号：EP18780484.4
申请日：2018-04-02
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： KITAO, Tatsuya , TAKEDA, Shigemitsu , SHOJI, Yoshimichi , SHIRAHASE, Hiroaki
IPC分类号： A61K31/166 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/382 , A61K31/397 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P5/00 , A61P11/00 , A61P13/08
摘要： The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I):

[wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.

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