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1. 发明申请

WO1997005860A1 PHOTOSTABLE AQUEOUS SOLUTION CONTAINING BENZYL ALCOHOL DERIVATIVES 审中-公开
标题翻译：含有BENZYL ALCOHOL衍生物的可溶性水溶液
公开(公告)号：WO1997005860A1
公开(公告)日：1997-02-20
申请号：PCT/JP1996001950
申请日：1996-07-12
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , KOSHINAKA, Eiichi , YAMAZAKI, Masahiro , MATSUO, Kazuya
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： A61K31/135
CPC分类号： C07C215/60 , A61K31/137 , A61K47/10 , A61K47/26 , C07B2200/07 , Y10S514/935
摘要： A photostable aqueous solution containing optically active (-)-(R)- alpha -[(tert-butylamino)methyl]-2-chloro-4-hydroxybenzyl alcohol represented by formula (I) or a pharmacologically acceptable salt thereof and at least one photostabilizer selected from the group consisting of saccharides, sugar alcohols and polyhydric alcohols.
摘要翻译：由式（I）表示的光学活性（ - ） - （R）-α-[（叔丁基氨基）甲基] -2-氯-4-羟基苄醇或其药学上可接受的盐和至少一种选自糖，糖醇和多元醇的光稳定剂。

2. 发明申请

WO1997014411A1 PERCUTANEOUS TULOBUTEROL PREPARATION AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：胰岛素的制备方法及其制备方法
公开(公告)号：WO1997014411A1
公开(公告)日：1997-04-24
申请号：PCT/JP1996002422
申请日：1996-08-28
申请人： NITTO DENKO CORPORATION , HOKURIKU SEIYAKU CO., LTD. , NAKAGAWA, Takeaki , NAKANO, Yoshihisa , OTSUKA, Saburo
发明人： NITTO DENKO CORPORATION , HOKURIKU SEIYAKU CO., LTD.
IPC分类号： A61K31/135
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/137
摘要： A percutaneous tulobuterol preparation obtained by laminating a pressure-sensitive adhesive layer comprising as the main component a synthetic rubber containing micro-crystalline tulobuterol of 2 to 20 mu m in average particle size onto a support; in particular, a percutaneous tulobuterol preparation wherein the micro-crystalline tulobuterol is one obtained by dissolving tulobuterol and a pressure-sensitive adhesive comprising as the main component a synthetic resin in a good solvent followed by recrystallization; and a process for producing the preparation which comprises homogeneously dissolving the adhesive and tulobuterol in a good solvent, applying the resulting adhesive solution onto one face of a peelable film and drying to thereby form an adhesive layer; then laminating the adhesive layer onto a support; and recrystallizing tulobuterol at 10 to 30 DEG C to thereby give an adhesive layer wherein microcrystals of 2 to 20 mu m in average particle size have been homogeneously dispersed. The preparation is excellent in the long-lasting drug effect. The above process makes it possible to efficiently produce the preparation.
摘要翻译：通过将包含作为主要成分的含有平均粒径为2〜20μm的微晶杜洛特罗的合成橡胶的压敏粘合剂层层压到载体上而获得的经皮珠杜特醇制剂; 特别是一种经皮十四指醇制剂，其中微结晶丁特罗是通过将妥洛特罗和包含合成树脂作为主要成分的压敏粘合剂溶解在良溶剂中，随后重结晶得到的那种; 以及制备该制剂的方法，该方法包括将粘合剂和十四指醇均匀地溶解在良溶剂中，将所得粘合剂溶液施加到可剥离膜的一个表面上并干燥从而形成粘合剂层; 然后将粘合剂层层压到载体上; 并在10〜30℃下重结晶十四指醇，得到平均粒径为2〜20μm的微晶均匀分散的粘合剂层。该制剂具有优异的长效药物作用。上述方法使得可以有效地制备该制剂。

3. 发明申请

WO1997009330A1 CRYSTAL OF HYDRATE AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：水合物晶体及其制备方法
公开(公告)号：WO1997009330A1
公开(公告)日：1997-03-13
申请号：PCT/JP1996002352
申请日：1996-08-23
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , YASUDA, Shingo , KADO, Noriyuki , IWASAKI, Nobuhiko , NISHINO, Hiroyuki , TAKESHITA, Makoto
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07D491/044
CPC分类号： C07D491/04
摘要： A novel crystal of dihydrate of 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid giving high-intensity diffraction peaks at angles of diffraction (2 theta ) of about 4.2 DEG , 17.0 DEG and 21.3 DEG in the powder X-ray diffractometry; a drug containing this novel crystal; and a process for the preparation of the novel crystal which comprises treating a crystalline substance containing a crystal of anhydride of the above acid with hydrous acetone and subjecting the obtained product to drying and moistening.
摘要翻译： 3- [4-（8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基）哌啶子基]丙酸的二水合物的新晶体在角度处产生高强度衍射峰在粉末X射线衍射中约为4.2°，17.0°和21.3°的衍射（2θ）; 含有这种新型晶体的药物; 以及制备新型晶体的方法，其包括用含水丙酮处理含有上述酸的无水物结晶的结晶物质，并使所得产物干燥和润湿。

4. 发明申请

WO1992014705A1 BENZAMIDE DERIVATIVE 审中-公开
标题翻译：苯甲酸衍生物
公开(公告)号：WO1992014705A1
公开(公告)日：1992-09-03
申请号：PCT/JP1992000134
申请日：1992-02-12
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , YASUDA, Shingo , IWASAKI, Nobuhiko , NISHINO, Hiroyuki , TAKESHITA, Makoto
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07D207/14
CPC分类号： C07D451/04 , C07D211/58 , C07D451/14
摘要： A benzamide derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R represents hydrogen or lower alkanoyl; R represents hydrogen or halogen; R represents lower alkoxy; R represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl or lower alkoxy; A represents C1 to C7 alkylene which may be substituted by lower alkyl; X represents methylene, oxygen or sulfur; m represents an integer of 0 to 3; n represents an integer of 0 to 3; and p represents an integer of 0 to 2. These compounds are useful because of their activity of enhancing the function of a digestive tract, and a pharmaceutical composition containing the same as the active ingredient is useful for treating digestive system diseases.
摘要翻译：由通式（I）表示的苯甲酰胺衍生物及其药学上可接受的盐，其中R 1表示氢或低级烷酰基; R 2表示氢或卤素; R 3代表低级烷氧基; R 4代表氢或低级烷基; R 5表示氢，低级烷基或低级烷氧基; A表示可以被低级烷基取代的C1〜C7亚烷基; X表示亚甲基，氧或硫; m表示0〜3的整数， n表示0〜3的整数， p表示0〜2的整数。这些化合物由于其增强消化道功能的活性而有用，含有与活性成分相同的药物组合物可用于治疗消化系统疾病。

5. 发明申请

WO1998021177A1 BENZENESULFONAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME 审中-公开
标题翻译：苯并呋喃衍生物和含有它们的药物
公开(公告)号：WO1998021177A1
公开(公告)日：1998-05-22
申请号：PCT/JP1997004125
申请日：1997-11-12
申请人： HOKURIKU SEIYAKU CO., LTD. , YASUDA, Shingo , OGAWA, Nobuo , SAKURAI, Shunichiro
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07C311/19
CPC分类号： C07C311/19 , C07C311/29 , C07D333/24
摘要： Novel benzenesulfonamide derivatives of general formula (I); (wherein R is hydrogen, halogeno, lower alkyl, lower alkoxy or nitro; R is C4-C8 alkyl substituted with one or more fluorine atoms; R is hydrogen or lower alkyl; X is sulfur or CH=CH; and n is an integer of 2 to 4). Drugs containing the derivatives as the active ingredient are usable for the invention and/or treatment of thrombosis, asthma or allergic diseases.
摘要翻译：通式（I）的新型苯磺酰胺衍生物; （其中R 1是氢，卤代，低级烷基，低级烷氧基或硝基）; R 2是被一个或多个氟原子取代的C 4 -C 8烷基; R 3是氢或低级烷基; X是硫或 CH = CH; n为2〜4的整数）。含有衍生物作为活性成分的药物可用于本发明和/或治疗血栓形成，哮喘或过敏性疾病。

6. 发明申请

WO1998013035A1 PERCUTANEOUS PREPARATIONS 审中-公开
标题翻译： PERCUTANEOUS准备
公开(公告)号：WO1998013035A1
公开(公告)日：1998-04-02
申请号：PCT/JP1997003412
申请日：1997-09-25
申请人： NITTO DENKO CORPORATION , HOKURIKU SEIYAKU CO., LTD. , NAKANO, Yoshihisa , YAMAMOTO, Keiji , NAKAGAWA, Takeaki , HORI, Mitsuhiko , OTSUKA, Saburo
发明人： NITTO DENKO CORPORATION , HOKURIKU SEIYAKU CO., LTD.
IPC分类号： A61K31/135
CPC分类号： A61K9/7061 , A61K31/137
摘要： Percutaneous preparations composed of a support and a plaster layer located on one face thereof and containing 2-tert-butylamino-1-(2-chloro-4-hydroxy-phenyl)ethan-1-o1 or its pharmacologically acceptable salt and a pressure-sensitive adhesive, wherein the adhesive is an acrylic polymer substantially free from carboxy or comprises a material containing at least one high-molecular-weight rubber component with an average molecular weight of from 300,000 to 2,500,000 and at least one additive selected from among C12-18 fatty acid esters, C8-10 fatty acid monoglycerides and C6-10 dibasic acid esters. These percutaneous preparations are excellent in percutaneous drug-absorption properties, can give long-lasting drug effects with little side effect and, therefore, are useful in the prevention and treatment of threatened abortion, premature birth, urination disorders such as urinary incontinence, etc.
摘要翻译：含有2-叔丁基氨基-1-（2-氯-4-羟基 - 苯基）乙-1-醇或其药理学上可接受的盐和压敏粘合剂的经皮制剂由载体和石膏层组成，其中所述粘合剂是基本上不含羧基的丙烯酸聚合物，或包含含有至少一种平均分子量为300,000至2,500,000的高分子量橡胶组分的材料和至少一种选自C12-18的添加剂脂肪酸酯，C8-10脂肪酸单甘油酯和C6-10二元酸酯。这些经皮制剂经皮药物吸收性优异，可以产生持久的药物作用，副作用小，因此可用于预防和治疗威胁性流产，早产，排尿障碍如尿失禁等。

7. 发明申请

WO1996038436A1 (2-THIENYL)ALKANOIC ACID DERIVATIVES 审中-公开
标题翻译：（2-噻吩基）烷基酸衍生物
公开(公告)号：WO1996038436A1
公开(公告)日：1996-12-05
申请号：PCT/JP1996001430
申请日：1996-05-28
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , YASUDA, Shingo , OGAWA, Nobuo , SAKURAI, Shunichiro
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07D333/24
CPC分类号： C07D333/24
摘要： Compounds represented by general formula (I) or a salt of the same, wherein R represents hydrogen, halogeno, lower alkyl, lower alkoxy or nitro; R represents C1-10 alkyl, C3-8 cycloalkyl optionally having lower alkyl on its ring or C1-6 alkyl substituted by C3-8 cycloalkyl; R represents hydrogen or lower alkyl; and n is an integer of from 2 to 4. The compounds have thromboxane A2 and leukotriene D4 antagonisms and are useful in the prevention and/or treatment of diseases selected from the group consisting of ischemic heart diseases, cerebrovascular disorders, thrombosis, asthma and allergic inflammation.
摘要翻译：由通式（I）表示的化合物或其盐，其中R 1表示氢，卤代，低级烷基，低级烷氧基或硝基; R 2表示C 1-10烷基，任选在其环上具有低级烷基的C 3-8环烷基或被C 3-8环烷基取代的C 1-6烷基; R 3表示氢或低级烷基; 并且n为2至4的整数。该化合物具有血栓素A2和白三烯D4拮抗剂，并且可用于预防和/或治疗选自缺血性心脏病，脑血管障碍，血栓形成，哮喘和过敏的疾病炎。

8. 发明申请

WO1996022988A1 QUINOLINECARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：喹喔啉羧酸衍生物
公开(公告)号：WO1996022988A1
公开(公告)日：1996-08-01
申请号：PCT/JP1995002614
申请日：1995-12-20
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , YASUDA, Shingo , KADO, Noriyuki , YOSHIDA, Toshihiko , YAMAMOTO, Yoichi
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07D401/04
CPC分类号： A61K31/47 , C07D401/04
摘要： 5-Amino-7-((3S,4S)-3-amino-4-methyl(or ethyl)-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acids represented by general formula (I), pharmaceutically acceptable salts thereof, and an antibacterial agent containing the same as the active ingredient, wherein each asterisked asymmetric carbon atome has the S-configuration; an R represents methyl or ethyl.
摘要翻译： 5-氨基-7 - （（3S，4S）-3-氨基-4-甲基（或乙基）-1-吡咯烷基）-1-环丙基-6-氟-1,4-二氢-8-甲基-4- 由通式（I）表示的氧代喹啉-3-羧酸，其药学上可接受的盐和含有与活性成分相同的抗菌剂，其中每个星号的不对称碳原子具有S-构型; R 1表示甲基或乙基。

9. 发明申请

WO1994007848A1 BENZENESULFONAMIDE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：苯并呋喃衍生物及其用途
公开(公告)号：WO1994007848A1
公开(公告)日：1994-04-14
申请号：PCT/JP1993001382
申请日：1993-09-29
申请人： HOKURIKU SEIYAKU CO., LTD. , ITO, Yasuo , KATO, Hideo , YASUDA, Shingo , OGAWA, Nobuo , SAKURAI, Shunichiro , SUZUKI, Tomio
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07C311/19
CPC分类号： C07C311/29 , C07C311/19
摘要： A benzenesulfonamide derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R1 represents hydrogen, lower alkyl, lower alkoxy or halogen; R2 represents C1-C10 linear or branched alkyl, C3-C8 cycloalkyl optionally substituted by C1-C6 alkyl, C1-C6 alkyl substituted by C3-C8 cycloalkyl, 1-adamantylmethyl, 2-norbornylmethyl or phenyl-substituted C1-C6 alkyl which may be substituted on the benzene ring; R3 represents hydrogen or lower alkyl; and n represents an integer of 2 to 4. The compound has a thromboxane A2 antagonism, a leucotriene antagonism, and so on, thus being useful as platelet aggregation inhibitor, antithrombotic, antiasthmatic, and antiallergic.
摘要翻译：由通式（I）表示的苯磺酰胺衍生物及其药理学上可接受的盐，其中R1表示氢，低级烷基，低级烷氧基或卤素; R 2表示C 1 -C 10直链或支链烷基，任选被C 1 -C 6烷基取代的C 3 -C 8环烷基，被C 3 -C 8环烷基取代的C 1 -C 6烷基，1-金刚烷甲基，2-降冰片基甲基或苯基取代的C 1 -C 6烷基，在苯环上取代; R3代表氢或低级烷基; n表示2〜4的整数。该化合物具有血栓素A2拮抗作用，白三烯拮抗作用等，因此可用作血小板聚集抑制剂，抗血栓形成，抗哮喘药和抗过敏药。

10. 发明申请

WO1992017440A1 TRICYCLIC COMPOUND 审中-公开
标题翻译：三聚体化合物
公开(公告)号：WO1992017440A1
公开(公告)日：1992-10-15
申请号：PCT/JP1992000365
申请日：1992-03-26
申请人： HOKURIKU SEIYAKU CO., LTD. , SAWANISHI, Hiroyuki , ITO, Yasuo , KATO, Hideo , KOSHINAKA, Eiichi , OGAWA, Nobuo , MORIKAWA, Kouji
发明人： HOKURIKU SEIYAKU CO., LTD.
IPC分类号： C07C229/14
CPC分类号： C07D313/14 , C07C229/14 , C07C2603/32 , C07D311/82 , C07D313/12
摘要： Tricyclic compounds represented by general formula (I), pharmacologically acceptable salts thereof, and a process for producing the same. In formula (I) X represents -CH=CH-, -CH2O- or -O-; R1 represents lower alkyl; R2 represents hydrogen or lower alkyl; and n represents an integer of 1 to 5. They have antiallergic and antihistaminic activities with alleviated side effects and hence are useful as an antiallergic and antihistaminic.

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