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1. 发明申请

US20040209919A1 Stabilized pharmaceutical composition 审中-公开
标题翻译：稳定的药物组合物
公开(公告)号：US20040209919A1
公开(公告)日：2004-10-21
申请号：US10835442
申请日：2004-04-28
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.
发明人： Tadashi Makino , Tetsuro Tabata , Shin-Ichiro Hirai
IPC分类号： A61K031/4439 , A61K033/00
CPC分类号： C07D401/12 , A61K9/1611 , A61K9/2009 , A61K9/5026 , A61K9/5078 , A61K31/44 , A61K31/4439 , A61K47/02 , Y10S514/951
摘要： The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1 wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.
摘要翻译：本发明的药物组合物，其包含下式的苯并咪唑化合物其中R 1是氢，烷基，卤素，氰基，羧基，烷酰氧基，烷氧羰基烷基，氨基甲酰基，氨基甲酰基烷基，羟基，烷氧基，羟基烷基，三氟甲基，酰基，氨基甲酰氧基，硝基，酰氧基，芳基，芳氧基，烷硫基或烷基亚磺酰基，R 2是氢，烷基，酰基，烷氧羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基羰基甲基，烷氧基羰基甲基或烷基磺酰基，R 3和R 5相同或不同的，各自为氢，烷基，烷氧基或烷氧基烷氧基，R 4为氢，烷基，可任选氟化的烷氧基或烷氧基烷氧基，m为0至4的整数，以及碱性无机盐稳定剂，身体稳定镁和钙碱性无机盐稳定剂是特别有用的。

2. 发明申请

US20040044223A1 Benzimidazole derivatives, their production and use 失效
标题翻译：苯并咪唑衍生物，其生产和使用
公开(公告)号：US20040044223A1
公开(公告)日：2004-03-04
申请号：US10612984
申请日：2003-07-07
申请人： Takeda Chemical Industries, Ltd.
发明人： Takehiko Naka , Kohei Nishikawa , Takeshi Kato
IPC分类号： C07D43/02
CPC分类号： C07D235/02 , C07D235/26 , C07D235/28 , C07D235/30 , C07D403/04 , C07D403/10 , C07D405/14
摘要： A method for producing a compound represented by the formula: 1 wherein the ring A is a benzene ring which may be substituted in addition to the Rnull group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is nullOnull, nullS(O)m- or nullN(R4)null wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; Rnull is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: 2 wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.
摘要翻译：一种制备由下式表示的化合物的方法：其中环A是除R'基之外可被取代的苯环; R 1是氢或任选取代的烃残基; X是在亚苯基和苯基之间具有原子长度或者两个或更少的直接键或间隔子; Y是-O - ， - S（O）m - 或-N（R 4） - ，其中m是0,1或2的整数，R 4是氢或任选取代的烷基; R'是羧基，其酯，其酰胺或能够形成阴离子的基团或可转化的基团; n为1或2的整数; 其包括使由下式表示的化合物脱保护：其中R是三苯甲基，2-四氢吡喃基，甲氧基甲基或乙氧基甲基，其它符号如上定义; 或其盐。

3. 发明申请

US20030133941A1 Method of separating protective components of bordetella pertussis 审中-公开
标题翻译：分离百日咳博德特氏菌保护成分的方法
公开(公告)号：US20030133941A1
公开(公告)日：2003-07-17
申请号：US10206989
申请日：2002-07-30
申请人： Takeda Chemical Industries, Ltd.
发明人： Akihiro Suehara , Eiji Yamamoto , Shigeo Fujii
IPC分类号： A61K039/02 , C07K014/235
CPC分类号： C07K14/235 , A61K39/00
摘要： To provide a method of efficiently separate protective components of Bordetella pertussis On the basis of differences in adsorbability to calcium phosphate gel formed by adding calcium ions to a Bordetella pertussis culture in the presence of excess phosphate ions, protective components of Bordetella pertussis are separated from the Bordetella pertussis culture. Traditionally, protective components of Bordetella pertussis have been separated using different purification methods for the respective components. According to the present invention, the use of the same means of purification for all subject components makes it possible to purify each component with high efficiency and high recovery rate, an aspect very advantageous for industrial production. It is also possible to efficiently produce an improved purified pertussis component vaccine comprising an effective combination of pertussis filamentous hemagglutinin (FHA), pertactin (PRN, 69K-OMP), pertussis fimbriae (FIM) and pertussis toxin (PT).
摘要翻译：提供一种有效分离百日咳博德特氏菌保护成分的方法根据在过量磷酸根离子存在下向百日咳杆菌培养物中加入钙离子而形成的磷酸钙凝胶的吸附性差异，将百日咳博德特氏菌的保护成分从博德特氏菌百日咳培养。传统上，百日咳博德特氏菌的保护性成分已经使用各种成分的不同纯化方法进行分离。根据本发明，对于所有被摄体成分使用相同的纯化方法使得可以以高效率和高回收率净化每种组分，这对于工业生产非常有利。还可以有效地制备改进的纯化的百日咳组分疫苗，其包括百日咳丝状血凝素（FHA），百日咳杆菌（PRN，69K-OMP），百日咳菌毛（FIM）和百日咳毒素（PT））的有效组合。

4. 发明申请

US20030113909A1 G protein coupled receptor protein, production and use thereof 审中-公开
标题翻译： G蛋白偶联受体蛋白，其生产和使用
公开(公告)号：US20030113909A1
公开(公告)日：2003-06-19
申请号：US09929752
申请日：2001-08-14
申请人： Takeda Chemical Industries, Ltd.
发明人： Shuji Hinuma , Ryo Fujii , Yuji Kawamata
IPC分类号： C12Q001/68 , G01N033/53 , G01N033/567 , C12P021/06 , C12N015/00 , C12N015/09 , C12N015/63 , C12N015/70 , C12N015/74 , C07K005/00 , C07K007/00 , C07K016/00 , C07K017/00 , A61K038/00 , C12N005/00 , C12N005/02 , C12P021/08
CPC分类号： C07K14/705
摘要： Rabbit gastropyrolic part smooth muscle-derived G protein coupled receptor proteins, partial peptides thereof; and DNAs containing said protein or partial peptide-encoding DNA are provided. The receptor protein and the DNA coding for said protein can be used for {circle over (1)} determination of ligands; {circle over (2)} acquisition of antibody and antiserum; {circle over (3)} construction of expression system for of a recombinant type receptor protein; {circle over (4)} development of the receptor binding assay system using said expression system and screening of the candidate compounds for pharmaceuticals; {circle over (5)}conducting a drug design based upon a comparison with structurally analogous ligands and receptors; {circle over (6)} preparation of probes and PCR primers for a gene diagnosis; {circle over (7)} preparation of transgenic animals; and {circle over (8)}preparation of model patient animals deficient in the receptor protein DNA. Elucidation of the structure and property of the G protein coupled receptor is particularly related to the development of unique pharmaceuticals which act on such a system.
摘要翻译：兔子胃部分平滑肌衍生的G蛋白偶联受体蛋白，其部分肽; 并提供含有所述蛋白质或部分肽编码DNA的DNA。受体蛋白和编码所述蛋白质的DNA可以用于（循环（1个配体的测定; {循环（2次获得抗体和抗血清; {circle over（3构建重组型受体蛋白质的表达系统 ;（循环（使用所述表达系统的受体结合测定系统的4个开发和用于药物的候选化合物的筛选）; {循环（基于与结构上类似的配体和受体的比较来设计药物设计; {循环（6 制备用于基因诊断的探针和PCR引物;（循环（7个转基因动物的制备;和循环（8个制备缺陷受体蛋白DNA的模型患者动物），阐明G蛋白偶联受体的结构和性质特别是与这种系统的独特药物的开发有关。

5. 发明申请

US20020103210A1 Nitrogen-containing heterocyclic compounds, their production and use 失效
标题翻译：含氮杂环化合物，其生产和使用
公开(公告)号：US20020103210A1
公开(公告)日：2002-08-01
申请号：US10042229
申请日：2002-01-11
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.
发明人： Shuichi Furuya , Toshihiro Imaeda , Satoshi Sasaki
IPC分类号： A61K031/519 , A61K031/4745 , A61K031/404
CPC分类号： C07D487/04 , A61K31/506
摘要： A compound of the formula: 1 wherein one of A and D is N and the other is C, or both are N; B is N or C; m is 0-3; R1, R2 and R3 each is (i) H or (ii) a group bound via C, N, O or S; R4 is a group bound via C; R5 is H or a group bound via C or O; R6 is H or a group bound via C; R7 is a homo- or hetero-cyclic group which may be substituted; or a salt thereof possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful as a prophylactic or therapeutic agent for sex hormone-dependent diseases, and so forth.
摘要翻译：下式的化合物：其中A和D中的一个为N，另一个为C，或两者均为N; B是N或C; m为0-3; R1，R2和R3各自为（i）H或（ii）通过C，N，O或S键合的基团; R4是通过C键合的基团; R5是H或通过C或O键合的基团; R6是H或通过C键合的基团; R7是可以被取代的同 - 或异环 - 基团; 或其盐具有优异的促性腺激素释放激素拮抗活性，并且可用作性激素依赖性疾病的预防或治疗剂等。

6. 发明授权

US5889009C1 Method of inhibiting cell adhesion 失效
标题翻译：抑制细胞粘附的方法
公开(公告)号：US5889009C1
公开(公告)日：2002-05-07
申请号：US93145397
申请日：1997-09-17
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： MIYAKE AKIO , NAKAMURA MASAHIRA , FUKUSHI HIDETO
IPC分类号： C07D215/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04 , C07D519/00 , A61K31/495 , A61K31/44 , A61K31/47 , A61K31/50
CPC分类号： C07D401/04 , C07D215/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04

7. 发明授权

US4385051A BICYCLIC COMPOUNDS, THEIR PRODUCTION AND USE 失效
标题翻译：双相化合物，其生产和使用
公开(公告)号：US4385051A
公开(公告)日：1983-05-24
申请号：US31263981
申请日：1981-10-19
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： OKA YOSHIKAZU , NISHIKAWA KOHEI , MIYAKE AKIO
IPC分类号： C07C213/08 , A61K38/00 , C07K5/02 , A61K37/00 , A61K31/195 , A61K31/335 , C07C103/52
CPC分类号： C07K5/022 , A61K38/00
摘要： New bicyclic compounds, inclusive, of salts thereof, of the formula: wherein R and R are the same or different and represents hydrogen, hydroxy or lower alkoxy, R is hydrogen or lower alkyl, R is hydrogen, lower alkyl, amino-lower-alkyl or acylamino-lower-alkyl, R is hydrogen, lower alkyl or aralkyl which may be substituted, R is hydroxyl, lower alkoxy, amino or lower alkylamino, and m and n each means 1 or 2, having inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.
摘要翻译：其中R 1和R 2相同或不同并且表示氢，羟基或低级烷氧基的新的双环化合物，包括其盐，其具有下式：其中R 1和R 2相同或不同，表示氢，羟基或低级烷氧基，R 3是氢或低级烷基 R 4为氢，低级烷基，氨基 - 低级 - 烷基或酰氨基 - 低级 - 烷基，R 5为氢，可被取代的低级烷基或芳烷基，R 6为羟基，低级烷氧基，氨基或低级烷基氨基，m和n各自表示1或2，具有血管紧张素转换酶和缓激肽分解酶的抑制活性，可用作抗高血压药。

8. 发明授权

US3923798A Process for recovering cephalosporin C from aqueous solutions thereof 失效
标题翻译：从其水溶液中回收头孢菌素C的方法
公开(公告)号：US3923798A
公开(公告)日：1975-12-02
申请号：US42415373
申请日：1973-12-12
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： HORII SATOSHI , MIZOKAMI NARIAKIRA , FUJINO MASAHIKO , SHINAGAWA SUSUMU , OCHIAI MICHIHIKO , OKUTANI TETSUYA
IPC分类号： C07D501/12 , C07D501/26
CPC分类号： C07D501/12
摘要： This invention relates to N-isobornyloxycarbonylcephalosporin C which is useful as an intermediate for the production of cephalosporin C and other cephalosporanic acid derivatives and is also useful as an antimicrobial agent.
摘要翻译：本发明涉及可用作产生头孢菌素C和其它头孢菌酸衍生物的中间体的N-异冰片氧基羰基头孢菌素C，也可用作抗微生物剂。

9. 发明授权

US3917825A Preparation for rectal or vaginal administration containing LH-RH or its analogs 失效
标题翻译：用于含有LH-RH或其类似物的直肠或阴道给药的制剂
公开(公告)号：US3917825A
公开(公告)日：1975-11-04
申请号：US40617473
申请日：1973-10-12
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： MATSUZAWA TAI , HIRAI SHIN-ICHIRO , FUJINO MASAHIKO , KOBAYASHI SHIGERU , YAMAZAKI IWAO
IPC分类号： A61K9/00 , A61K9/02 , A61K38/00 , A61K38/04 , C07K7/23 , A61K37/00
CPC分类号： A61K9/02 , A61K9/0034 , A61K38/00 , C07K7/23 , Y10S514/80 , Y10S930/13
摘要： Novel preparations essentially comprising nona- or deca-peptide having luteinizing hormone-releasing activity dispersed homogeneously in an oleaginous base or in a mixture of the oleaginous base and a non-ionic surfactant effectively exhibit a luteinizing hormone-releasing activity when administered to warmblooded animals by rectal or vaginal route.
摘要翻译：基本上包含具有促黄体激素释放活性的非 - 或十肽的新制剂，其均匀地分散在油性碱或含油碱和非离子表面活性剂的混合物中，当施用于温血时有效地显示促黄体激素释放活性动物通过直肠或阴道途径。

10. 发明授权

US3904684A Method for producing sodium citrate dihydrate 失效
标题翻译：生产柠檬酸钠二水合物的方法
公开(公告)号：US3904684A
公开(公告)日：1975-09-09
申请号：US35264473
申请日：1973-04-19
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： TSUDA MASAHIKO , FUJIWARA YOSHIAKI , SHIRAISHI TETSUYA
IPC分类号： C07C51/00 , C07C51/41 , C07C59/265 , C07C67/00 , C12P7/48 , C07C59/16
CPC分类号： C12P7/48 , C07C51/412 , Y10S435/83 , Y10S435/843 , Y10S435/923 , Y10S435/93 , Y10S435/94 , C07C59/265
摘要： Sodium citrate dihydrate is recovered directly from a citric acid fermentation broth by removing impurities at pH 9 to 13 and concentrating the resulting fluid at pH 10 to 13. The sodium citrate dihydrate is used as food additives, detergent builders as well as desulfurizing agents.
摘要翻译：柠檬酸钠二水合物通过去除pH9至13的杂质直接从柠檬酸发酵液中回收，并将所得流体浓缩至pH10至13.柠檬酸钠二水合物用作食品添加剂，洗涤剂助洗剂以及脱硫剂。

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