公开(公告)号：US08389742B2

公开(公告)日：2013-03-05

申请号：US13093202

申请日：2011-04-25

申请人： Daisuke Tanaka

发明人： Daisuke Tanaka

IPC分类号： C07D207/30

CPC分类号： C07D207/416

摘要： The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, wherein R3 is a tert-C4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.

摘要翻译： 本发明提供式（I）的3-肼基-2,5-二氧代吡咯烷-3-羧酸盐：其中R1是C1-6烷基等，R2是氢原子或COOR3基团，其中R3是 叔-C4-6烷基，2,2,2-三氯乙基或苄基，其中苯环部分可以任选地被一个或两个独立地选自以下的原子或基团取代：卤素原子， C 1-4烷基，C 1-4烷氧基，氰基和硝基及其盐，可用作制备四氢吡咯并[1,2-a]吡嗪-4-螺 - 3'-吡咯烷衍生物如兰尼斯特（Ranirestat）在短时间内以治疗糖尿病并发症为前景的治疗剂以及经济上有利和安全的方法及其制备方法。

公开(公告)号：US08287918B2

公开(公告)日：2012-10-16

申请号：US12637667

申请日：2009-12-14

申请人： Toshihiro Noguchi ,  Akemi Baba

发明人： Toshihiro Noguchi ,  Akemi Baba

IPC分类号： A01N43/04 ,  A01N59/16 ,  A61K31/70 ,  A61K33/24

CPC分类号： A61K45/06 ,  A61K31/65 ,  A61K33/24 ,  A61K31/35 ,  A61K2300/00

摘要： Lung cancer can be treated effectively by combination of amrubicin or a pharmaceutically acceptable salt thereof with cisplatin.

摘要翻译： 可以通过将氨柔比星或其药学上可接受的盐与顺铂组合来有效治疗肺癌。

公开(公告)号：US20120245327A1

公开(公告)日：2012-09-27

申请号：US13509968

申请日：2010-11-16

申请人： Shoichi Nishio

发明人： Shoichi Nishio

IPC分类号： C12N1/19 ,  C07K14/78 ,  C12P21/00

CPC分类号： C07K14/78 ,  C12N9/0071 ,  C12Y114/11002 ,  C12Y114/11004

摘要： Disclosed is a transformant in which all of the foreign genes (1)-(3) described below are transfected into a microbial cell in order to obtain collagen that can be a high-performance versatile material which is commercially more valuable as a pharmaceutical product, industrial product, cosmetic product, food and the like. (1) A foreign gene comprising a nucleotide sequence encoding the amino acid sequence of lysyl hydroxylase (2) A foreign gene comprising a nucleotide sequence encoding the amino acid sequence of prolyl hydroxylase (3) A foreign gene comprising a nucleotide sequence encoding the amino acid sequence of collagen.

摘要翻译： 公开了将下述全部外来基因（1） - （3）转染入微生物细胞的转化体，以获得作为医药产品商业上更有价值的高性能通用材料的胶原， 工业产品，化妆品，食品等。 （1）包含编码赖氨酰羟化酶的氨基酸序列的核苷酸序列的外源基因（2）包含编码脯氨酰羟化酶的氨基酸序列的核苷酸序列的外源基因（3）外源基因，其含有编码氨基酸的核苷酸序列 胶原序列

公开(公告)号：US20120237569A1

公开(公告)日：2012-09-20

申请号：US13432915

申请日：2012-03-28

申请人： Koichi SAITO ,  Yusuke OKAWA

发明人： Koichi SAITO ,  Yusuke OKAWA

IPC分类号： A61K39/00 ,  A61P37/04 ,  A61K47/44 ,  A61P35/00 ,  A61K47/14 ,  A61K9/107

CPC分类号： C07K7/08 ,  A61K9/0019 ,  A61K9/107 ,  A61K39/0011 ,  A61K47/14 ,  A61K2039/55566 ,  C07K7/06

摘要： Provided is an emulsified composition for diluting a cancer antigen peptide or a dimer thereof. Also provided is a novel cancer vaccine composition or specific CTL inducer that efficiently induces CTL irrespective of the type of cancer antigen peptide when mixing the emulsified composition for dilution and a water phase comprising a cancer antigen peptide or a dimer thereof.The present invention relates to an emulsified composition for diluting a cancer antigen peptide or a dimer thereof, comprising a particular ester, a particular surfactant, a particular emulsifier, and a water phase. The present invention also relates to a cancer vaccine composition or specific CTL inducer obtained by freshly diluting and mixing a water phase comprising a cancer antigen peptide or a dimer thereof with the emulsified composition for dilution.

摘要翻译： 提供了用于稀释癌抗原肽或其二聚体的乳化组合物。 还提供了当混合用于稀释的乳化组合物和包含癌抗原肽或其二聚体的水相时，与癌抗原肽类型无关地有效诱导CTL的新型癌症疫苗组合物或特异性CTL诱导剂。 本发明涉及用于稀释癌抗原肽或其二聚体的乳化组合物，其包含特定的酯，特定的表面活性剂，特定的乳化剂和水相。 本发明还涉及通过将包含癌抗原肽或其二聚体的水相与用于稀释的乳化组合物新鲜稀释和混合而获得的癌症疫苗组合物或特异性CTL诱导剂。

公开(公告)号：US08232405B2

公开(公告)日：2012-07-31

申请号：US13010194

申请日：2011-01-20

申请人： Tomohiro Toyoda ,  Hidefumi Yoshinaga

发明人： Tomohiro Toyoda ,  Hidefumi Yoshinaga

IPC分类号： C07D401/00 ,  A61K31/445

CPC分类号： C07C309/73 ,  C07D211/22 ,  C07D211/32 ,  C07D311/22 ,  C07D313/08 ,  C07D405/06

摘要： Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.)

摘要翻译： 公开了由式（1）表示的苄基哌啶化合物或其药学上可接受的盐，其可用作药物如抗抑郁剂。 （式（1）中，R 1表示氢原子或甲基，R 2表示相对于亚甲基的p位或m位的基团，表示在p位结合的氯原子，溴 在p位上键合的原子，在p位上键合的甲基，与m位相连的m位或与溴原子结合的氯原子; X表示亚甲基或氧原子; n表示 表示1〜3的整数。）

公开(公告)号：US08216833B2

公开(公告)日：2012-07-10

申请号：US10553639

申请日：2003-11-19

申请人： Izumu Saito ,  Yumi Saito

发明人： Izumu Saito ,  Yumi Saito

IPC分类号： C12N15/861 ,  C12N15/70

CPC分类号： C12N15/86 ,  C12N15/70 ,  C12N2710/10343

摘要： A novel cosmid vector and the like effectively used in generating a recombinant adenoviral vector are provided. More specifically, there are provided a cosmid vector characterized by: (1) containing an adenoviral genome having adenoviral inverted terminal repeat sequences each having a complete nucleotide sequence, (2) having a deletion in an adenovirus E1 gene region, and (3) containing a restriction enzyme recognition sequence not present in the adenoviral genome, on both sides of the adenoviral genome; a method of generating a recombinant adenoviral vector using the cosmid vector; and a reagent for generating a recombinant adenoviral vector containing the cosmid vector as a component.

摘要翻译： 提供了有效用于产生重组腺病毒载体的新型粘粒载体等。 更具体地，提供了一种粘粒载体，其特征在于：（1）含有腺病毒基因组，其具有各自具有完整核苷酸序列的腺病毒反向末端重复序列，（2）在腺病毒E1基因区域中具有缺失，和（3）含有 腺病毒基因组两侧不存在的限制酶识别序列; 使用粘粒载体产生重组腺病毒载体的方法; 以及用于产生含有粘粒载体作为组分的重组腺病毒载体的试剂。

公开(公告)号：US08178102B2

公开(公告)日：2012-05-15

申请号：US11814270

申请日：2006-01-19

申请人： Koichi Saito ,  Yusuke Okawa

发明人： Koichi Saito ,  Yusuke Okawa

IPC分类号： A61K39/39 ,  B01F3/08

CPC分类号： C07K7/08 ,  A61K9/0019 ,  A61K9/107 ,  A61K39/0011 ,  A61K47/14 ,  A61K2039/55566 ,  C07K7/06

摘要： Provided is an emulsified composition for diluting a cancer antigen peptide or a dimer thereof. Also provided is a novel cancer vaccine composition or specific CTL inducer that efficiently induces CTL irrespective of the type of cancer antigen peptide when mixing the emulsified composition for dilution and a water phase comprising a cancer antigen peptide or a dimer thereof.The present invention relates to an emulsified composition for diluting a cancer antigen peptide or a dimer thereof, comprising a particular ester, a particular surfactant, a particular emulsifier, and a water phase. The present invention also relates to a cancer vaccine composition or specific CTL inducer obtained by freshly diluting and mixing a water phase comprising a cancer antigen peptide or a dimer thereof with the emulsified composition for dilution.

摘要翻译： 提供了用于稀释癌抗原肽或其二聚体的乳化组合物。 还提供了当混合用于稀释的乳化组合物和包含癌抗原肽或其二聚体的水相时，与癌抗原肽类型无关地有效诱导CTL的新型癌症疫苗组合物或特异性CTL诱导剂。 本发明涉及用于稀释癌抗原肽或其二聚体的乳化组合物，其包含特定的酯，特定的表面活性剂，特定的乳化剂和水相。 本发明还涉及通过将包含癌抗原肽或其二聚体的水相与用于稀释的乳化组合物新鲜稀释和混合而获得的癌症疫苗组合物或特异性CTL诱导剂。

公开(公告)号：US08153161B2

公开(公告)日：2012-04-10

申请号：US10582174

申请日：2004-12-07

申请人： Keiichi Fujiwara ,  Kiyomi Sogo ,  Shizuo Okamoto ,  Koichiro Shibamori ,  Norihito Shimono

发明人： Keiichi Fujiwara ,  Kiyomi Sogo ,  Shizuo Okamoto ,  Koichiro Shibamori ,  Norihito Shimono

IPC分类号： A61K9/50 ,  A61K9/20

CPC分类号： A61K9/1652 ,  A61K9/0056 ,  A61K9/1623 ,  A61K9/2077 ,  A61K31/5375 ,  A61K47/26 ,  A61K47/38

摘要： The invention provides a medicament-containing particle wherein an unpleasant taste of the medicament is alleviated, which is obtainable by mixing and granulating the following ingredients: (1) the medicament with an unpleasant taste, (2) methylcellulose and (3) mannitol; and a solid preparation including the particle. The invention can make an unpleasant taste of the medicament alleviated and furthermore when the formulation including the particle is administered, the unpleasant taste can be masked and the formulation has a good dissolvability in gastrointestinal tract.

摘要翻译： 本发明提供了一种药物含有颗粒，其中药物的令人不快的味道得到缓解，其可通过混合和造粒以下成分获得：（1）具有不愉快味道的药物，（2）甲基纤维素和（3）甘露醇; 和包含该颗粒的固体制剂。 本发明可以使缓解的药物变得令人不愉快的味道，此外，当施用包含颗粒的制剂时，可以掩蔽不愉快的味道，并且制剂在胃肠道中具有良好的溶解性。

公开(公告)号：US08138172B2

公开(公告)日：2012-03-20

申请号：US12305801

申请日：2007-07-03

申请人： Anthony Cook ,  Tom McInally ,  Stephen Thom ,  Hiroki Wada

发明人： Anthony Cook ,  Tom McInally ,  Stephen Thom ,  Hiroki Wada

IPC分类号： C07D473/18 ,  A61K31/522 ,  C07D473/40 ,  A61P11/06 ,  A61P37/08 ,  A61P31/04 ,  A61P31/08 ,  A61P31/20

CPC分类号： C07D473/18

摘要： The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.

摘要翻译： 本发明提供8-氧代腺嘌呤衍生物，其制备方法，含有它们的药物组合物及其在治疗中的用途。 8-氧代腺嘌呤衍生物作为Toll样受体（TLR）7的调节剂，因此可用于治疗哮喘，肝炎，过敏性疾病，病毒和细菌感染以及癌症。

公开(公告)号：US08106230B2

公开(公告)日：2012-01-31

申请号：US12310524

申请日：2007-08-30

申请人： Takashi Inagaki ,  Yoshikazu Yamakawa

发明人： Takashi Inagaki ,  Yoshikazu Yamakawa

IPC分类号： C07C255/03 ,  C07C299/04

CPC分类号： C07D207/416 ,  C07B53/00 ,  C07C269/06 ,  C07C271/22 ,  C07C2601/14

摘要： The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic acid diester of the formula (2): wherein R1 is an amino group protected with a group removed by hydrogenolysis or a tert-butoxycarbonylamino group and R2 is an ethyl group optionally substituted with one or two methyl group(s) at α-position, provided that R2 is not a tert-butyl group when R1 is a tert-butoxycarbonylamino group; with alkali metal alkoxide and the compound (3) can be an important intermediate for production of ranirestat.

摘要翻译： 本发明提供了制备光学活性琥珀酰亚胺衍生物的方法，该衍生物是生产ranirestat的关键中间体。 通过处理式（2）的琥珀酸二酯的衍生物容易地制备化合物（3）：其中R1是被氢解除去的基团保护的氨基或叔丁氧基羰基氨基，R2是任选取代的乙基 在α位具有一个或两个甲基，条件是当R 1是叔丁氧基羰基氨基时，R 2不是叔丁基; 与碱金属醇盐和化合物（3）可以作为生产ranirestat的重要中间体。