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    GONADAL FUNCTION IMPROVING AGENTS
    291.
    发明申请
    GONADAL FUNCTION IMPROVING AGENTS 审中-公开
    全功能改善剂

    公开(公告)号：US20110052563A1

    公开(公告)日：2011-03-03

    申请号：US12710864

    申请日：2010-02-23

    Applicant: Tetsuya Ohtaki ,  Hisanori Matsui ,  Hirokazu Matsumoto ,  Chieko Kitada

    Inventor： Tetsuya Ohtaki ,  Hisanori Matsui ,  Hirokazu Matsumoto ,  Chieko Kitada

    IPC: A61K39/395 ,  A61K38/16 ,  A61K31/7088 ,  A61K31/711 ,  A61P15/08 ,  A61P15/00 ,  A61P5/00

    CPC classification number: G01N33/689 ,  A61K31/00 ,  A61K31/7088 ,  A61K38/1709

    Abstract: Metastin, compounds that promote the activity of metastin or its receptors and the like are excellent gonadal function improving agents, ovulation inducers or promoters, gonadotropic hormone secretion promoters, gonadotropic hormone secretion inhibitors, sex hormone secretion promoters, sex hormone secretion inhibitors, etc., and can be used as agents for preventing/treating sterility, hormone-sensitive cancers, endometriosis, etc. Metastin and its receptors are useful for screening for these pharmaceuticals.

    Abstract translation: 促甲状腺激素分泌抑制剂，雌激素分泌促进剂，性激素分泌抑制剂等的促性腺激素分泌抑制剂，促性腺激素分泌促进剂，性激素分泌抑制剂等的优良性腺功能改善剂，排卵诱导剂或促进剂，促性腺激素分泌促进剂， 并且可以用作预防/治疗无菌，激素敏感性癌症，子宫内膜异位症等的药剂.MCastin及其受体可用于筛选这些药物。

    SUSTAINED RELEASE PREPARATION
    292.
    发明申请
    SUSTAINED RELEASE PREPARATION 审中-公开
    持续发布准备

    公开(公告)号：US20110045028A1

    公开(公告)日：2011-02-24

    申请号：US12516536

    申请日：2007-11-29

    Applicant: Satoshi Iinuma ,  Yoshie Iinuma ,  Tomohiro Yoshinari ,  Tsuneaki Tottori

    Inventor： Satoshi Iinuma ,  Yoshie Iinuma ,  Tomohiro Yoshinari ,  Tsuneaki Tottori

    IPC: A61K31/513 ,  A61K9/00 ,  A61P7/02 ,  A61P9/10

    CPC classification number: A61K31/506 ,  A61K9/2018 ,  A61K9/2054

    Abstract: Disclosed is a sustained-release preparation which is prepared by shaping a granule comprising a blood coagulation factor Xa inhibitor and a mixture of at least two hydrophilic polymers. Also disclosed is a pharmaceutical composition comprising a combination of the sustained-release preparation and an immediate release preparation comprising a blood coagulation factor Xa inhibitor. It becomes possible to provide a controlled release preparation comprising a blood coagulation factor Xa inhibitor for the prevention or treatment of thrombosis, which can control the activity of blood coagulation factor Xa for a long term and is excellent in convenience and compliance. It is also becomes possible to provide a method for producing the controlled release preparation.

    Abstract translation: 公开了一种缓释制剂，其通过使包含凝血因子Xa抑制剂和至少两种亲水性聚合物的混合物的颗粒成形而制备。 还公开了包含缓释制剂和包含凝血因子Xa抑制剂的速释制剂的组合的药物组合物。 可以提供一种控制释放制剂，其包含凝血因子Xa抑制剂，用于预防或治疗血栓形成，其可以长期控制凝血因子Xa的活性，并且方便性和顺应性优异。 也可以提供一种制备控释制剂的方法。

    COMPOUND HAVING 6-MEMBERED AROMATIC RING
    293.
    发明申请
    COMPOUND HAVING 6-MEMBERED AROMATIC RING 审中-公开
    具有六层芳香环的化合物

    公开(公告)号：US20110009421A1

    公开(公告)日：2011-01-13

    申请号：US12919400

    申请日：2009-02-27

    Applicant: Masaki Setoh ,  Toshitake Kobayashi ,  Toshio Tanaka ,  Atsuo Baba

    Inventor： Masaki Setoh ,  Toshitake Kobayashi ,  Toshio Tanaka ,  Atsuo Baba

    IPC: A61K31/497 ,  C07D239/24 ,  C07D401/12 ,  C07D211/72 ,  C07D213/62 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4439 ,  A61P25/18

    CPC classification number: C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/42 ,  C07D295/12 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.[Means] A compound represented by the following formula (I) or salt thereof: wherein A represents —(CH2)n—CO—NRa— (n is an integer of 0 to 3) or —NRa—CO—, B represents a hydrogen atom, halogen atom, cyano group, hydroxy group, or the like, X1, X2, X3, and X4 represent the same or different —CRx═, or —N═, Y represents —O—, —S—, —S(O)—, —S(O)2—, or —NRy—, Z represents a bond, methylene, or ethylene, Ar1 represents a five- to ten-membered aromatic ring (except for thiazole) which may be substituted with one or more substituents selected from halogen atoms, optionally halogenated C1-6 alkyl groups, and the like, Ar2 represents a five- to six-membered aromatic ring which may be substituted with one or more substituents selected from halogen atoms, optionally halogenated C1-6 alkyl groups, and the like, and which may be condensed with an optionally substituted five- to six-membered ring, and Ra, Rb, Rx, and Ry represent the same or different hydrogen atom, halogen atoms, or the like].

    Abstract translation: 本发明的目的是提供一种用于预防或治疗精神分裂症等的药剂，其中本发明的化合物具有GPRS2激动剂活性。 [表示]下式（I）表示的化合物或其盐：其中A表示 - （CH 2）n -CO-NR a - （n为0〜3的整数）或-NR a -CO-，B表示 氢原子，卤素原子，氰基，羟基等，X 1，X 2，X 3和X 4表示相同或不同的-CR x =或-N =，Y表示-O - ， - S-，-S （O） - ， - S（O）2 - 或-NR y - ，Z表示键，亚甲基或亚乙基，Ar 1表示5至10元芳环（噻唑除外），可以被一个 或更多选自卤素原子，任选卤代C 1-6烷基等取代基，Ar 2表示可被一个或多个选自卤素原子，任意卤代C 1-6的取代基取代的五至六元芳环 烷基等，并且其可以与任选取代的五元至六元环稠合，并且R a，R b，R x和R y表示相同或不同的氢 原子，卤素原子等]。

    SUSTAINED-RELEASE MICROSPHERE CONTAINING SHORT CHAIN DEOXYRIBONUCLEIC ACID OR SHORT CHAIN RIBONUCLEIC ACID AND METHOD OF PRODUCING THE SAME
    296.
    发明申请
    SUSTAINED-RELEASE MICROSPHERE CONTAINING SHORT CHAIN DEOXYRIBONUCLEIC ACID OR SHORT CHAIN RIBONUCLEIC ACID AND METHOD OF PRODUCING THE SAME 审中-公开
    含有短链脱氨基酸或短链核糖核酸的保持性释放微球及其生产方法

    公开(公告)号：US20100310670A1

    公开(公告)日：2010-12-09

    申请号：US12065255

    申请日：2006-03-03

    Applicant: Hiroaki Okada ,  Yuki Takashima ,  Naoyuki Murata

    Inventor： Hiroaki Okada ,  Yuki Takashima ,  Naoyuki Murata

    IPC: A61K31/7105 ,  C07H21/04 ,  C07H21/02 ,  A61K31/711 ,  A61P29/00 ,  A61P31/12 ,  A61K9/14

    CPC classification number: A61K9/0048 ,  A61K9/0019 ,  A61K9/1647 ,  A61K31/7105 ,  A61K31/711 ,  A61K31/713 ,  A61K47/6455 ,  A61K48/00

    Abstract: A sustained-release microsphere formulation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid as an active ingredient, which has improved sustained-release properties and long-lasting efficacy, is provided. A fine particle formulation, encapsulating stably a short chain deoxyribonucleic acid or a short chain ribonucleic acid, being capable of inhibiting, for a long period, expression of a specific protein related to a disease, and which can be administered by injection or transmucosally, and a production method of the same are provided. A sustained-release microsphere formulation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid, particularly siRNA, as an active ingredient, especially a sustained-release microsphere prepared through a w1/o/w2 type emulsion, is characterized in that a positively charged basic substance, such as arginine, polyethylenimine, a cell permeable peptide, poly-L-lysine or poly-L-ornithine, is included in an in vivo degradable polymer.

    Abstract translation: 提供了含有短链脱氧核糖核酸或短链核糖核酸作为活性成分的持续释放微球制剂，其具有改善的持续释放性能和持久功效。 能够稳定地包封短链脱氧核糖核酸或短链核糖核酸的微粒制剂能够长时间地抑制与疾病相关的特异性蛋白质的表达，并且可以通过注射或经粘膜施用，以及 提供了其制造方法。 含有短链脱氧核糖核酸或短链核糖核酸，特别是siRNA作为活性成分，特别是通过w1 / o / w2型乳剂制备的持续释放微球的缓释微球制剂的特征在于： 带电的碱性物质，例如精氨酸，聚乙烯亚胺，细胞可渗透肽，聚-L-赖氨酸或聚-L-鸟氨酸，被包括在体内可降解的聚合物中。

    Ligands for G protein-coupled receptor protein and use thereof
    297.
    发明授权
    Ligands for G protein-coupled receptor protein and use thereof 失效
    G蛋白偶联受体蛋白质的配体及其用途

    公开(公告)号：US07833722B2

    公开(公告)日：2010-11-16

    申请号：US11587631

    申请日：2005-04-26

    Applicant: Ryo Fujii ,  Masataka Harada ,  Shuji Hinuma

    Inventor： Ryo Fujii ,  Masataka Harada ,  Shuji Hinuma

    IPC: G01N33/53

    CPC classification number: C07K14/705 ,  A61K31/7088 ,  A61K38/00 ,  G01N33/6896 ,  G01N33/74 ,  G01N2333/726 ,  G01N2500/04

    Abstract: The present invention provides a method of screening an agonist/antagonist of a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or its salt and a ligand or its salt; and so on. The screening method of the present invention is useful for screening an agent for the prevention/treatment of nervous system diseases or neuropathic pains.

    Abstract translation: 本发明提供筛选G蛋白偶联受体蛋白激动剂/拮抗剂的方法，其包含与SEQ ID NO：1所示的氨基酸序列相同或基本上相同的氨基酸序列，或其盐，其包含 使用受体蛋白或其盐和配体或其盐; 等等。 本发明的筛选方法可用于筛选用于预防/治疗神经系统疾病或神经性疼痛的药剂。

    GNRH agonist combination drugs
    298.
    发明申请
    GNRH agonist combination drugs 审中-公开
    GNRH激动剂联合药物

    公开(公告)号：US20100286063A1

    公开(公告)日：2010-11-11

    申请号：US12662866

    申请日：2010-05-07

    Applicant: Shuichi Furuya ,  Masami Kusaka

    Inventor： Shuichi Furuya ,  Masami Kusaka

    IPC: A61K38/08 ,  A61P35/00

    CPC classification number: A61K45/06 ,  A61K31/4535 ,  A61K31/58 ,  A61K2300/00

    Abstract: In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.

    Abstract translation: 在药物领域中，旨在提供药物，由此可以增强GnRH激动剂对各种疾病的预防和治疗作用，并且可以改善生活质量。 更具体地，药物组合的特征在于GnRH激动剂与选自SERM，SARM，性激素合成抑制剂，受体型酪氨酸激酶抑制剂，骨代谢调节剂，免疫治疗药物，细胞因子/趋化因子抑制剂和内皮素的化学物质组合 受体拮抗剂。 由于这些组合，可以提供增强GnRH激动剂对各种疾病和缓解副作用的预防和治疗效果的优异效果。 此外，可以改善生活质量。

    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF
    299.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF 有权
    熔融杂环衍生物及其用途

    公开(公告)号：US20100273788A1

    公开(公告)日：2010-10-28

    申请号：US12263949

    申请日：2008-11-03

    Applicant: Nozomu SAKAI ,  Shinichi IMAMURA ,  Naoki MIYAMOTO ,  Takaharu HIRAYAMA

    Inventor： Nozomu SAKAI ,  Shinichi IMAMURA ,  Naoki MIYAMOTO ,  Takaharu HIRAYAMA

    IPC: A61K31/5025 ,  C07D487/04 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00

    CPC classification number: C07D487/04

    Abstract: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

    Abstract translation: 本发明提供具有强激酶抑制活性的稠合杂环衍生物及其应用。 由式（I）表示的化合物：其中每个符号如说明书中所定义，除了特定化合物或其盐，以及含有作为激酶的化合物或其前药的药物（VEGFR，VEGFR2 ，PDGFR，Raf）抑制剂，血管发生抑制剂，用于预防或治疗癌症的药物，癌症生长抑制剂或癌症转移抑制剂。

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