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    Quinazoline derivatives as kinase inhibitors
    1.
    发明授权
    Quinazoline derivatives as kinase inhibitors 失效
    喹唑啉衍生物作为激酶抑制剂

    公开(公告)号：US08324205B2

    公开(公告)日：2012-12-04

    申请号：US12471280

    申请日：2009-05-22

    申请人： Anjali Pandey ,  Robert M. Scarborough ,  Kenji Matsuno ,  Michio Ichimura ,  Yuji Nomoto ,  Shinichi Ide ,  Eiji Tsukuda ,  Junko Sasaki ,  Shoji Oda

    发明人： Anjali Pandey ,  Robert M. Scarborough ,  Kenji Matsuno ,  Michio Ichimura ,  Yuji Nomoto ,  Shinichi Ide ,  Eiji Tsukuda ,  Junko Sasaki ,  Shoji Oda

    IPC分类号： A61K31/535 ,  A61K31/497

    CPC分类号： C07D239/94 ,  A61K31/517 ,  C07D401/12 ,  C07D403/12

    摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译： 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化症。

    Easily Absorbable Oral Preparations of Xanthine Derivatives
    2.
    发明申请
    Easily Absorbable Oral Preparations of Xanthine Derivatives 审中-公开
    容易吸收的黄嘌呤衍生物口服制剂

    公开(公告)号：US20100168140A1

    公开(公告)日：2010-07-01

    申请号：US12086550

    申请日：2006-12-14

    申请人： Makoto Kigoshi ,  Hideki Kato ,  Noboru Aoki

    发明人： Makoto Kigoshi ,  Hideki Kato ,  Noboru Aoki

    IPC分类号： A61K31/522

    CPC分类号： A61K9/1617 ,  A61K9/0095 ,  A61K9/1611 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/52 ,  A61K31/522

    摘要： An object of the present invention is to provide an easily absorbable oral preparation containing a xanthine derivative or a pharmaceutically acceptable salt thereof and a fatty acid or a fatty acid derivative for the purpose of providing an easily absorbable oral preparation containing the xanthine derivative of which absorbability has been enhanced by dissolving the xanthine derivative that shows adenosine A1 receptor antagonistic activity and has diuretic activity, kidney-protecting activity, bronchodilating activity, cerebral function-improving activity, anti-dementia activity or the like in a solvent.

    摘要翻译： 本发明的目的是提供含有黄嘌呤衍生物或其药学上可接受的盐和脂肪酸或脂肪酸衍生物的容易吸收的口服制剂，其目的是提供含有可吸收性的黄嘌呤衍生物的容易吸收的口服制剂 通过在溶剂中溶解显示腺苷A1受体拮抗活性并具有利尿活性，肾保护活性，支气管扩张活性，脑功能改善活性，抗痴呆活性等的黄嘌呤衍生物而得到增强。

    COMPOSITION FOR RELIEVING SUBJECTIVE SYMPTOMS OF FATIGUE
    4.
    发明申请
    COMPOSITION FOR RELIEVING SUBJECTIVE SYMPTOMS OF FATIGUE 有权
    用于消除疲劳的主观症状的组合物

    公开(公告)号：US20090232917A1

    公开(公告)日：2009-09-17

    申请号：US12089078

    申请日：2006-10-04

    申请人： Miho Komatsu ,  Koji Morishita ,  Akemi Ogawa ,  Goro Hori ,  Miho Takada

    发明人： Miho Komatsu ,  Koji Morishita ,  Akemi Ogawa ,  Goro Hori ,  Miho Takada

    IPC分类号： A61K36/8962 ,  A61K31/198

    CPC分类号： A61K31/198 ,  A61K36/8962 ,  A61K2300/00

    摘要： There has been a demand in the marketplace for medicines, functional foods and so on which can relieve subjective symptoms of fatigue in persons having these subjective symptoms, and enabling the persons to have productive days. That is, an object of the present invention is to provide a composition for relieving subjective symptoms of fatigue. According to the present invention, a safe and effective composition for relieving subjective symptoms of fatigue which contains ornithine or a salt thereof as an active ingredient can be provided.

    摘要翻译： 药品，功能性食品等市场需求可以减轻患有这些主观症状的人的疲劳主观症状，使人们有生产日。 也就是说，本发明的目的是提供一种减轻疲劳主观症状的组合物。 根据本发明，可以提供一种用于缓解含有鸟氨酸或其盐作为活性成分的疲劳主观症状的安全有效的组合物。

    PROCESS FOR PRODUCING DIPEPTIDES
    5.
    发明申请
    PROCESS FOR PRODUCING DIPEPTIDES 有权
    生产皂苷的方法

    公开(公告)号：US20090191589A1

    公开(公告)日：2009-07-30

    申请号：US12406330

    申请日：2009-03-18

    申请人： Shin-ichi Hashimoto ,  Kazuhiko Tabata ,  Aya Kubota ,  Hajime Ikeda

    发明人： Shin-ichi Hashimoto ,  Kazuhiko Tabata ,  Aya Kubota ,  Hajime Ikeda

    IPC分类号： C12P21/02

    CPC分类号： C12P21/02 ,  C12N9/00 ,  C12N9/54

    摘要： The present invention provides a protein which catalyzes the synthesis of a dipeptide different from L-Ala-L-Ala, a process for producing the protein which catalyzes the synthesis of a dipeptide, a process for producing a dipeptide using the protein which catalyzes the synthesis of a dipeptide, and a process for producing the dipeptide using a culture of a microorganism producing the protein which catalyzes the synthesis of a dipeptide or the like as an enzyme source.

    摘要翻译： 本发明提供了催化不同于L-Ala-L-Ala的二肽的合成的蛋白质，用于生产催化二肽合成的蛋白质的方法，使用催化合成的蛋白质生产二肽的方法 的二肽的方法，以及使用产生作为酶源的二肽等的合成的蛋白质的微生物的培养物来生成二肽的方法。

    CRYSTALS OF L-ORNITHINE AND PROCESS FOR PRODUCING THE SAME
    6.
    发明申请
    CRYSTALS OF L-ORNITHINE AND PROCESS FOR PRODUCING THE SAME 失效
    L-ORNITHINE的晶体及其生产方法

    公开(公告)号：US20090082594A1

    公开(公告)日：2009-03-26

    申请号：US11719122

    申请日：2005-11-14

    申请人： Hideki Murata ,  Ikuhiro Nakatani ,  Mariko Shitashige ,  Kenji Tajima

    发明人： Hideki Murata ,  Ikuhiro Nakatani ,  Mariko Shitashige ,  Kenji Tajima

    IPC分类号： C07C229/26

    CPC分类号： C07C227/42 ,  C07C229/26

    摘要： The present invention provides crystals of L-ornithine and a process for producing the crystals of L-ornithine including the steps of (i) exposing L-ornithine or a salt thereof, a composition comprising L-ornithine or a salt thereof, or a solution containing L-ornithine, a salt thereof, or the composition to a cation exchange resin to adsorb L-ornithine onto the cation exchange resin; (ii) eluting L-ornithine from the cation exchange resin on which L-ornithine is adsorbed with an aqueous alkaline solution, and removing an alkaline component from the resulting eluate to prepare an aqueous L-ornithine solution; and (iii) mixing the aqueous L-ornithine solution with a hydrophilic organic solvent, and crystallizing L-ornithine from the resulting mixed solution.

    摘要翻译： 本发明提供L-鸟氨酸的晶体和L-鸟氨酸晶体的制造方法，其特征在于，包括以下步骤：（i）使L-鸟氨酸或其盐，包含L-鸟氨酸或其盐的组合物或溶液 将含有L-鸟氨酸的盐或其组合物或阳离子交换树脂，将L-鸟氨酸吸附到阳离子交换树脂上; （ii）从碱性水溶液中吸附L-鸟氨酸的阳离子交换树脂中洗脱L-鸟氨酸，从得到的洗脱液中除去碱性成分，制备L-鸟氨酸水溶液; 和（iii）将L-鸟氨酸水溶液与亲水性有机溶剂混合，并从所得混合溶液中结晶L-鸟氨酸。

    METHOD FOR PRODUCING INDAZOL-3-YLMETHYL PHOSPHONIUM SALT
    7.
    发明申请
    METHOD FOR PRODUCING INDAZOL-3-YLMETHYL PHOSPHONIUM SALT 失效
    生产辛烷-3-基甲基硫酸盐的方法

    公开(公告)号：US20090069568A1

    公开(公告)日：2009-03-12

    申请号：US11912355

    申请日：2006-04-28

    申请人： Koji Hagihara ,  Tsutomu Matsumura ,  Masahiro Hoshikawa ,  Iwao Chujo

    发明人： Koji Hagihara ,  Tsutomu Matsumura ,  Masahiro Hoshikawa ,  Iwao Chujo

    IPC分类号： C07F9/645

    CPC分类号： C07D231/56 ,  C07F9/65031

    摘要： The present invention provides a method for producing an indazol-3-ylmethyl phosphonium salt represented by Formula (IV): [wherein X represents halogen, OSO2Ra (wherein Ra represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or OC(═O)Rb (wherein Rb has the same meaning as the above Ra), or the like, and R1, R2 and R3 may be the same or different and each represents substituted or unsubstituted aryl or the like] or a salt thereof, which comprises reacting a compound represented by Formula (I): a compound represented by Formula (II): H—X  (II) (wherein X has the same meaning as defined above), and a compound represented by Formula (III): (wherein R1, R2 and R3 have the same meanings as defined above, respectively), and the like.

    摘要翻译： 本发明提供由式（IV）表示的吲唑-3-基甲基鏻盐的制备方法：[式中，X表示卤素，OSO 2 R a（其中R a表示取代或未取代的低级烷基，取代或未取代的芳基等），或 OC（-O）R b（其中R b具有与上述Ra相同的含义）等，R 1，R 2和R 3可以相同或不同，各自表示取代或未取代的芳基等]或其盐 其中包括使由式（I）表示的化合物：由式（II）表示的化合物：<？in-line-formula description =“In-Line Formulas”end =“lead”→HX（II） （其中X具有与上述相同的含义）和由式（III）表示的化合物：其中R1，R2和R3具有式 分别与上述相同的含义）等。

    Therapeutic agent for diabetes mellitus
    8.
    发明授权
    Therapeutic agent for diabetes mellitus 失效
    糖尿病治疗剂

    公开(公告)号：US07485662B2

    公开(公告)日：2009-02-03

    申请号：US10549155

    申请日：2004-03-19

    申请人： Toshikazu Kamiya ,  Akio Shirai ,  Miho Takada ,  Fumiko Ogino

    发明人： Toshikazu Kamiya ,  Akio Shirai ,  Miho Takada ,  Fumiko Ogino

    IPC分类号： A61K31/40 ,  A61K31/21

    CPC分类号： A61K31/401 ,  A23K20/142 ,  A23L2/52 ,  A23L33/175 ,  A23V2002/00 ,  A23V2250/064

    摘要： An object of the present invention is to provide a therapeutic agent for diabetes mellitus or insulin resistance improving agent, or to provide foods and drinks, food and drink additives, and feeds or feed additives for treating diabetes mellitus or improving insulin diabetes.In order to achieve such an object, the present invention provides a therapeutic agent for diabetes mellitus and insulin resistance improving agent comprising hydroxyproline, a hydroxyproline derivative or a pharmaceutically acceptable salt thereof or foods and drinks, food and drink additives, feeds or feed additives for treatment of diabetes mellitus or improvement of insulin resistance comprising the same.

    摘要翻译： 本发明的目的是提供糖尿病或胰岛素抵抗性改善剂的治疗剂，或提供食品和饮料，食品和饮料添加剂以及用于治疗糖尿病或改善胰岛素糖尿病的饲料或饲料添加剂。 为了达到上述目的，本发明提供了含有羟脯氨酸，羟脯氨酸衍生物或其药学上可接受的盐或食品和饮料的糖尿病和胰岛素抵抗改善剂的治疗剂，食品和饮料添加剂，饲料添加剂或饲料添加剂 糖尿病的治疗或胰岛素抵抗的改善包括它们。

    Composition for Suppressing Expression of Target Gene
    9.
    发明申请
    Composition for Suppressing Expression of Target Gene 审中-公开
    抑制靶基因表达的组成

    公开(公告)号：US20090011003A1

    公开(公告)日：2009-01-08

    申请号：US11883168

    申请日：2005-10-24

    申请人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

    发明人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

    IPC分类号： A61K9/127 ,  A61K31/7105 ,  A61K48/00

    CPC分类号： C12N15/1135 ,  A61K9/127 ,  A61K31/7105 ,  C12N2310/14

    摘要： The present invention has its object to provide a composition for suppressing the expression of a target gene and the like, and provides a composition, comprising an RNA-encapsulated liposome which comprises complex particles comprising as constituent components a lead particle and an RNA comprising a sequence consisting of 15 to 30 contiguous nucleotides of a target gene mRNA and a sequence complementary to the sequence, and a lipid membrane for coating the complex particles, wherein constituent components of the lipid membrane can be solved in a polar organic solvent, and wherein the polar organic solvent can be contained in a liquid at such a concentration that the constituent components of the lipid membrane are dispersible and the complex particles are dispersible, and the like.

    摘要翻译： 本发明的目的是提供抑制靶基因表达等的组合物，提供包含RNA包封的脂质体的组合物，其包含作为铅粒子的构成成分的复合粒子和包含序列的RNA 由靶基因mRNA的15〜30个连续核苷酸和与该序列互补的序列构成，以及用于涂布复合粒子的脂质膜，其中脂质膜的构成成分可以在极性有机溶剂中溶解，其中极性 有机溶剂可以以使得脂质膜的组成成分可分散并且复合颗粒可分散的浓度包含在液体中。