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31. 发明申请

WO1997005858A1 AEROSOL PREPARATION 审中-公开
标题翻译：气溶胶制备
公开(公告)号：WO1997005858A1
公开(公告)日：1997-02-20
申请号：PCT/JP1996002124
申请日：1996-07-29
申请人： TAISHO PHARMACEUTICAL CO., LTD. , URUSHIZAKI, Fumio , SHIMAMURA, Haruo , UCHIYAMA, Tsuyoshi , KIMURA, Fuminori , KATO, Keiko
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/045
CPC分类号： A61K9/12 , A61K31/125 , A61K31/045 , A61K2300/00
摘要： Object: to provide a preparation having excellent antipruritic effects on the immediate reaction due to insect bite and also on itching as the delayed reaction. Constitution: an aerosol preparation composed of a stock solution which comprises the following components (A) to (C) in a solvent mixture consisting of water and a lower alcohol and a propellant: (A) one or more surfactants selected from the group consisting of polyoxyethylene sorbitan fatty acid esters and sorbitan fatty acid esters; (B) 0.5 to 8 % by weight of menthol; and (C) 1 to 0.5 parts by weight, per part by weight of menthol, of camphor.
摘要翻译：目的：提供对由于昆虫咬伤引起的即时反应以及作为延迟反应的瘙痒具有优异的止痒作用的制剂。构成：由在水和低级醇和推进剂组成的溶剂混合物中由以下组分（A）至（C）组成的储备溶液组成的气溶胶制剂：（A）一种或多种选自下列组分的表面活性剂：聚氧乙烯山梨糖醇酐脂肪酸酯和脱水山梨醇脂肪酸酯; （B）0.5〜8重量％的薄荷醇; 和（C）1至0.5重量份，每重量份薄荷醇，樟脑。

32. 发明申请

WO1997003075A1 THIAZOLINE DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：WO1997003075A1
公开(公告)日：1997-01-30
申请号：PCT/JP1995001361
申请日：1995-07-07
申请人： TAISHO PHARMACEUTICAL CO., LTD.
发明人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Masakazu , MANAKA, Akira , TAKAHASHI, Keiko , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
IPC分类号： C07D491/113
CPC分类号： C07D491/10
摘要： Object: to provide a thiazoline derivative having an excellent effect of inhibiting platelet agglutination through not only parenteral but also oral administration. Constitution: a thiazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents C1-C4 alkyl; and R2 represents hydrogen or C1-C4 alkyl.
摘要翻译：目的：提供通过不仅肠胃外但也口服给药具有优异的抑制血小板凝集的效果的噻唑啉衍生物。结构：由通式（I）表示的噻唑啉衍生物或其药理学上可接受的盐，其中R 1表示C1-C4烷基; 并且R 2表示氢或C 1 -C 4烷基。

33. 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。

34. 发明申请

WO1997001493A1 CONTAINER FOR LIQUID PREPARATIONS 审中-公开
标题翻译：液体制剂容器
公开(公告)号：WO1997001493A1
公开(公告)日：1997-01-16
申请号：PCT/JP1996001702
申请日：1996-06-20
申请人： TAISHO PHARMACEUTICAL CO., LTD. , KUKITA, Takuya , TAKADA, Junko , OKAMOTO, Kouichi , OHTSUKI, Tomohiro , KOUCHIWA, Takanori , KATO, Muneyoshi
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： B65D41/32
CPC分类号： B65D1/0238
摘要： A container for liquid preparations comprising a bottle-shaped synthetic resin container body (1) and a mouth (10), wherein the mouth (10) is sealed with a synthetic resin cap (2) fused thereto so as to be opened by breaking and means (3) for resealing the mouth (10) is formed at either or both of the body of the cap (2) and the mouth (10) or on the upper part of a holding piece (14) or the cap (2). The whole or necessary parts of the container contain antibacterial zeolite dispersed therein. As the container body (1) can be recapped in a hermetically sealed state even when the cap (2) is opened by breaking, the container is convenient for repeated use as required when carried after filling liquid preparations therein in such a quantity as to permit the administration thereof several times. As the container is always in a sterilized state, the filled preparations are protected from primary and secondary contaminations even when they do not contain any antiseptic, and the safety of the container itself is high.
摘要翻译：一种用于液体制剂的容器，其包括瓶形合成树脂容器体（1）和口（10），其中所述口（10）用合成树脂帽（2）密封，以便通过破碎而打开，用于重新密封嘴（10）的装置（3）形成在帽（2）的主体和嘴（10）的一个或两个上，或在保持件（14）或帽（2）的上部上，。容器的整个或必需的部分含有分散在其中的抗菌沸石。由于容器主体（1）即使在盖（2）通过断开而打开时也能够重新密封，所以容器在容纳了液体制剂之后必要时可以根据需要重复使用，允许给予它几次。当容器总是处于灭菌状态时，即使不含有任何防腐剂，填充的制剂也不受一次和二次污染，并且容器本身的安全性高。

35. 发明申请

WO1996039157A1 TESTOSTERONE 5'alpha'-REDUCTASE INHIBITOR 审中-公开
标题翻译： TESTOSTERONE5α-去氧化酶抑制剂
公开(公告)号：WO1996039157A1
公开(公告)日：1996-12-12
申请号：PCT/JP1995001117
申请日：1995-06-06
申请人： TAISHO PHARMACEUTICAL CO., LTD. , IMAMURA, Kouji , OKAJIMA, Takako , SUZUKI, Kenichi , URUSHIZAKI, Fumio
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K35/78
CPC分类号： A61K36/264
摘要： Object: to provide a testosterone 5 alpha -reductase inhibitor having an excellent inhibitory effect and being free from side effects such as hormonal effects. Constitution: a testosterone 5 alpha -reductase inhibitor containing an extract from the root of Aristolochia contorta BUNGE as the active ingredient.
摘要翻译：目的：提供具有优异抑制作用且不含副作用如激素效应的睾酮5α-还原酶抑制剂。体质：睾丸激素5α-还原酶抑制剂含有从马兜铃根的提取物作为活性成分。

36. 发明申请

WO1996028201A1 PREFILLED SYRINGE AND METHOD OF STERILIZING PREFILLED INJECTION 审中-公开
标题翻译：预先注射和预先注射灭菌的方法
公开(公告)号：WO1996028201A1
公开(公告)日：1996-09-19
申请号：PCT/JP1996000609
申请日：1996-03-12
申请人： TAISHO PHARMACEUTICAL CO., LTD. , OKAMOTO, Kouichi , KOSANO, Yoshinori , KURINO, Masuo , SUGANUMA, Hiromi , SOTTA, Niroh , ARAI, Isamu
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61M05/28
CPC分类号： A61M5/28 , A61L2/04 , A61L2/07 , A61M5/347 , A61M2005/3103 , A61M2005/3104 , A61M2005/3106 , A61M2005/312 , A61M2005/3132
摘要： A prefilled syringe provided with a cylinder (1), one or more rubber stoppers (5) and plungers (6) inserted into the cylinder (1) at given distances from each other, and a needle holder (2) that communicates with the tip of the cylinder (1) in a hermetically sealed state and has a needle-mounting section (2a) integrally attached to the tip of an injection cylinder section (20) having in the inner surface thereof passages (25) formed along the direction of flow of an injection in a state wherein the rubber stopper (5) has been inserted into the cylinder section, which syringe contains an injection prefilled in the space between the rubber stopper (5) and the plunger (6) in the cylinder (1) and which is provided with means for hermetically sealing the holder (2) on the side of the mounting section (2a); and a method of heat sterilizing a prefilled injection in such a hermetically sealed state. The prefilled injection can be sterilized with steam or hot water without allowing the steam to penetrate into the injection cylinder section.
摘要翻译：一种预充式注射器，其具有气瓶（1），一个或多个橡胶塞（5）和插入到气缸（1）中的柱塞（6），彼此以给定的距离;以及针头保持器（2），其与尖端（1）的气缸（1）的内表面上具有一体地安装在喷射筒部（20）的前端的针安装部（2a），所述针安装部在其内表面具有沿着流动方向形成的通路（25）在其中橡胶塞（5）已经插入到气缸部分中的注射器中的注射器中，该注射器包含预先填充在气缸（1）中的橡胶塞（5）和柱塞（6）之间的空间中的注射器，以及其设置有用于在所述安装部分（2a）侧密封所述保持器（2）的装置; 以及在这种气密密封状态下对预填充注射进行热灭菌的方法。预充式注射器可以用蒸汽或热水灭菌，而不允许蒸汽渗入注射筒部分。

37. 发明申请

WO1996022102A1 REMEDY FOR DERMATITIS 审中-公开
标题翻译：补救措施
公开(公告)号：WO1996022102A1
公开(公告)日：1996-07-25
申请号：PCT/JP1996000064
申请日：1996-01-18
申请人： TAISHO PHARMACEUTICAL CO., LTD. , YONEDA, Akiko , KITAJIMA, Hideaki , TSUNODA, Kenji , HASEGAWA, Kazuo , ISHI, Takako
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K33/30
CPC分类号： A61K33/30 , A61K31/215 , A61K31/19 , A61K31/20 , A61K2300/00
摘要： A remedy for dermatitis comprising one or more compounds selected from the group consisting of (A) zinc compounds and (B) polyvalent unsaturated fatty acids and esters thereof and being highly efficacious against intestinal acrodermatitis and dermatitis seborrhoica showing similar skin symptoms, psoriasis vulgaris, bullous diseases, pruritus cutaneous or symptoms accompanying zinc deficiency caused by trauma, burn or frostbite.
摘要翻译：包含一种或多种选自（A）锌化合物和（B）多价不饱和脂肪酸及其酯的化合物的化合物的皮炎补救剂，并且对于显示类似皮肤症状的牛皮癣和皮脂疮皮病，牛皮癣，大疱疾病，皮肤瘙痒或伴有由创伤，烧伤或冻伤引起的锌缺乏症状。

38. 发明申请

WO1996004920A1 INTERLEUKIN-5 PRODUCTION INHIBITOR 审中-公开
标题翻译： INTERLEUKIN-5生产抑制剂
公开(公告)号：WO1996004920A1
公开(公告)日：1996-02-22
申请号：PCT/JP1995001592
申请日：1995-08-10
申请人： TAISHO PHARMACEUTICAL CO., LTD. , HOSHINO, Akihiko , KASHIMURA, Masato , ASAKA, Toshifumi , INOUE, Tomoyuki , OKUDAIRA, Hirokazu
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/70
CPC分类号： A61K31/7048 , C07H17/08
摘要： Object: to provide an erythromycin derivative having a potent interleukin-5 production inhibitory effect. Constitution: an interleukin-5 production inhibitor containing as the active ingredient an erythromycin derivative, such as 6-O-methylerythromycin A 9-[O-(2-chlorophenylmethyl)oxime], 6-O-methylerythromycin A 9-[O-(3-methoxy-4-t-butylbenzyl)oxime] 11,12-cyclic carbonate or 11-amino-9-N, 11-N-cyclic ethylene-9-deoxo-11-deoxy-6-O-methylerythromycin A 9-benzylamine 11-N, 12-O-cyclic carbamate, or a medicinally acceptable acid-addition salt thereof.
摘要翻译：目的：提供具有强白介素-5产生抑制作用的红霉素衍生物。结构：含有红霉素衍生物如6-O-甲基红霉素A 9- [O-（2-氯苯甲基）肟]，6-O-甲基红霉素A 9- [O-（ 3-甲氧基-4-叔丁基苄基）肟] 11,12-环状碳酸酯或11-氨基-9-N，11-N-环状乙烯-9-脱氧-11-脱氧-6-O-甲基红霉素A 9- 苄胺11-N，12-O-环状氨基甲酸酯或其药学上可接受的酸加成盐。

39. 发明申请

WO1996004919A1 INTERLEUKIN-5 PRODUCTION INHIBITOR 审中-公开
标题翻译： INTERLEUKIN-5生产抑制剂
公开(公告)号：WO1996004919A1
公开(公告)日：1996-02-22
申请号：PCT/JP1995001591
申请日：1995-08-10
申请人： TAISHO PHARMACEUTICAL CO., LTD. , HOSHINO, Akihiko , KASHIMURA, Masato , ASAKA, Toshifumi , INOUE, Tomoyuki , OKUDAIRA, Hirokazu
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/70
CPC分类号： C07H17/08 , A61K31/7048
摘要： Object: to provide an erythromycin derivative having a potent interleukin-5 production inhibitory effect. Constitution: an interleukin-5 production inhibitor containing as the active ingredient an erythromycin derivative, such as 3-0-(4-biphenyl)acetyl-5-0-desosaminyl-6-0-methylerythronolide A 11,12-cyclic carbonate or 3-0-(2-nitro-3,4,5,6-tetrafluoro)phenyl-5-0-desosaminyl-6-0-methylerythronolide A, or a medicinally acceptable acid-addition salt thereof.
摘要翻译：目的：提供具有强白介素-5产生抑制作用的红霉素衍生物。构成：含有红霉素衍生物如3-0-（4-联苯基）乙酰基-5-0-去氨基甲酰基-6-0-甲基红霉内酯A 11,12-环状碳酸酯或3 -O-（2-硝基-3,4,5,6-四氟）苯基-5-0-去氨基甲酰基-6-0-甲基红霉内酯A或其药学上可接受的酸加成盐。

40. 发明申请

WO1995033845A1 PROCESS FOR PRODUCING OPTICALLY ACTIVE PROPARGYL ALCOHOL COMPOUND 审中-公开
标题翻译：用于生产光学活性丙醇醇化合物的方法
公开(公告)号：WO1995033845A1
公开(公告)日：1995-12-14
申请号：PCT/JP1995001064
申请日：1995-05-31
申请人： TAISHO PHARMACEUTICAL CO., LTD. , KAMEO, Kazuya , TANAMI, Tohru , TANAKA, Hideo , SHIMAZAKI, Yohichi , MUTOH, Masaru , TSUBOI, Mie , ONO, Naoya , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C12P41/00
CPC分类号： C12P41/004 , C12P7/62
摘要： A process for stereoselectively obtaining an optically active O-acylpropargyl alcohol compound represented by general formula (2) (wherein R and R represent each hydrogen or C1-C3 alkyl; R represents phenyl which may be substituted by C1-C5 alkyl, halogeno or trifluoromethyl at an arbitrary position of the ring, C1-C8 alkyl or C5-C8 cycloalkyl; R represents C1-C10 alkyl or phenyl which may be substituted by phenyl or halogeno at an arbitrary position of the ring; and the asterisk represents optical activity) by the reaction of an (RS)-propargyl alcohol compound represented by general formula (1) (wherein R , R and R are each as defined above) with an acylating agent R COOR (wherein R is as defined above; and R represents arbitrary alkyl or alkenyl) in the presence of an enzyme; and a process for obtaining an optically active propargyl alcohol compound either by hydrolyzing the above O-acyl compound or from the solution of the above acylation reaction.
摘要翻译：立体选择性地获得由通式（2）表示的光学活性O-酰基炔丙醇化合物的方法（其中R 1和R 2各自表示氢或C 1 -C 3烷基; R 3表示可被取代的苯基） C 1 -C 5烷基，C 1 -C 8烷基或C 5 -C 8环烷基上的C 1 -C 5烷基，卤代或三氟甲基; R 4表示任选位置可被苯基或卤素取代的C 1 -C 10烷基或苯基通过由通式（1）表示的（RS） - 炔丙醇化合物（其中R 1，R 2和R 3各自如上所定义）反应而得到的环，星号表示光学活性）上述）与酰化剂R 4 COOR（其中R 4如上所定义; R表示任意的烷基或链烯基）; 以及通过水解上述O-酰基化合物或从上述酰化反应的溶液获得光学活性炔丙醇化合物的方法。

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