中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

2080 records (took 0.06 seconds)

    BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS
    284.
    发明申请
    BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS 审中-公开

    公开(公告)号：US20110124626A1

    公开(公告)日：2011-05-26

    申请号：US13054688

    申请日：2009-07-17

    Applicant: Parminder Kaur Pooni ,  Kevin John Merchant ,  Catrina Morvern Kerr ,  Stuart Richard Crosby ,  Tomohiro Okawa ,  Mitsuru Sasaki ,  Mika Gotou ,  Graham Andrew Showell ,  Martin Richard Teall

    Inventor： Parminder Kaur Pooni ,  Kevin John Merchant ,  Catrina Morvern Kerr ,  Stuart Richard Crosby ,  Tomohiro Okawa ,  Mitsuru Sasaki ,  Mika Gotou ,  Graham Andrew Showell ,  Martin Richard Teall

    IPC: A61K31/397 ,  C07D403/12 ,  A61K31/55 ,  C07D401/12 ,  C07D223/16 ,  C07D413/10 ,  C07D403/14 ,  A61P25/28

    CPC classification number: C07D403/12 ,  C07D223/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

    Abstract: A compound having the formula (1) wherein: R1 is a group selected from C3-8 cycloalkyl, C1-6 alkyl, C1-6 alkylene-C3-8 cycloalkyl, each of which groups may optionally be substituted with C1-6 alkyl, halogen, haloC1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C1-6 alkyl, haloC1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group —(CH2)m— formed thereby being optionally substituted with a group selected from C1-4 alkyl, C3-8 cycloalkyl and arylsulfonyl; A is a group selected from —N(R2)CO—, —CON(R2)-, —OC(O)—, —C(O)O—, —CO—, —C(R2)(OR3)-, —C(═N—O—R3)-, —C(═CR2R3)-, —C3-8 cycloalkylene-, —C(R2)(haloC1-6alkyl)-, C1-4 alkylene and —C(OR3)(haloC1-6alkyl)-; R2 and R3 are each independently selected from H, C1-6 alkyl, and C3-8 cycloalkyl, or, when A is —N(R2)CO— and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C14 alkylene or C24 alkenylene, each of which may optionally be substituted with one or more C1-4 alkyl groups, OR16, halogen or haloC1-6 alkyl; Z is selected from aryl, heteroaryl, C3-8 cycloalkyl, and heterocyclyl, each of which may optionally be substituted by a group selected from —Y-aryl, heteroaryl, —Y—C3-8 cycloalkyl and —Y-heterocyclyl, or, when X is present, Z may be H, or, when X is absent and A is —C(R2)(OR3)- or —N(R2)CO—, Z may be H, or, when A is —N(R2)CO— and X is absent, Z may form, together with the adjacent nitrogen atom and R2, an N-containing heterocyclyl group which may optionally be substituted, wherein, when A is —CO—, Z is linked to X or A via a carbon atom and wherein, when A is —N(R2)CO— and Z is H, R1 is C3-8 cycloalkyl; and Y represents a bond, C1-6 alkylene, CO, NR14, COC2-6 alkenylene, O, SO2 or NHCOC1-6 alkylene; wherein said cycloalkyl, aryl, heteroaryl and heterocyclyl groups Z may be optionally substituted by one or more substituents which may be the same or different, and which are selected from halogen, haloC1-6 alkyl, hydroxy, cyano, nitro, ═O, —R4, —CO2R4, —COR4, —NR5R6, —C1-6 alkyl-NR5R6, —C3-8 cycloalkyl-NR5R6, —CONR12R13, —NR12COR13, —NR5SO2R6, —OCONR5R6, —NR5CO2R6, —NR4CONR5R6 or —SO2NR5R6-SHR8, -alkyl-OR8, —SOR8, —OR9, —SO2R9, —OSO2R9, -alkyl-SO2R9, -alkyl-CONHR9, -alkyl-SONHR9, -alkyl-COR10, —CO-alkyl-R10, —O-alkyl-R11 (wherein R4, R5 and R6 independently represent hydrogen, C1-6 alkyl, —C3-8 cycloalkyl, —C1-6 alkylene-C3-8 cycloalkyl, aryl, heterocyclyl or heteroaryl, wherein R8 represents C1-6 alkyl, wherein R9 represents C1-6 alkyl or aryl, wherein R10 represents aryl, wherein R11 represents C3-8 cycloalkyl or aryl, R12, R13, R14, R15 and R16 each independently represent H or C1-6 alkyl, and wherein —NR5R6 and —NR12R13 may represent a nitrogen containing heterocyclyl group); wherein said R4, R5, R6 R8, R9, R11 and R11 groups may be optionally substituted by one or more substituents which may be the same or different, and which are selected from the group consisting of halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, cyano, amino, ═O or trifluoromethyl; and wherein substituents of Z selected from —Y-aryl, —Y-heteroaryl, —Y—C3-8cycloalkyl and —Y-heterocyclyl may be optionally substituted by one or more substituents selected from ═O, hydroxy, cyano, nitro, halogen, haloC1-6 alkyl and C1-6alkyl; and wherein, when A is C1-4 alkylene, said cycloalkyl, aryl, heteroaryl or heterocyclyl group Z (such as a heterocyclyl group Z) is substituted at least with hydroxy, CF3, or ═O; and wherein, when A is CON(R2) n is 1; or a pharmaceutically acceptable salt or ester thereof, provided that: when A is —CO—, R1 is CH3, C3-8 cycloalkyl-substituted C1-6 alkylene or n-butyl, n is 0 and X is —CH2CH2—, Z is not N-benzyl substituted 4-piperidinyl, N-(3-fluorobenzyl)-substituted 4-piperidinyl or N-acetyl substituted 4-piperidinyl; when A is —OC(O)—, R1 is cyclobutyl, n is 0 and X is —CH2CH2—, Z is not H; when A is —OC(O)—, R1 is n-propyl, n is 0 and X is —CH2—, Z is not H; and when A is —CO—, R1 is CH3, n is 0 and X is CH2, Z is not H.

    Polypeptide and the use thereof
    285.
    发明授权
    Polypeptide and the use thereof 有权
    多肽及其用途

    公开(公告)号：US07943580B2

    公开(公告)日：2011-05-17

    申请号：US11793760

    申请日：2005-12-22

    Applicant: Kenji Kangawa ,  Kenji Mori ,  Mikiya Miyazato ,  Masayasu Kojima

    Inventor： Kenji Kangawa ,  Kenji Mori ,  Mikiya Miyazato ,  Masayasu Kojima

    IPC: A61K38/16 ,  A61K51/08

    CPC classification number: G01N33/9406 ,  A01K2217/05 ,  A01K2227/10 ,  A61K38/17 ,  C07K14/47 ,  G01N33/6893 ,  G01N2500/00 ,  G01N2800/046 ,  G01N2800/306 ,  G01N2800/362 ,  G01N2800/367

    Abstract: The present invention provides a variety of useful polypeptides. In particular, a polypeptide comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 2 or SEQ ID NO: 3, its amide, or a salt thereof can be used as an agent for preventing/treating hypotension; an agent for preventing/treating obesity, hyperphagia, etc.; an agent for preventing/treating lethargy, time-zone change syndrome (jet lag), etc.; an agent for preventing/treating sterility, etc. A compound or its salt that promotes the activity of a polypeptide comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by any of SEQ ID NOS: 7 to 12 and 37 to 42, its partial peptide, or a salt thereof is useful as an agent for preventing/treating, e.g., menopausal symptoms or hyperthyroidism. A compound or its salt that inhibits the activity of said polypeptide is useful as an agent for preventing/treating, e.g., sterility or hypothyroidism.

    Abstract translation: 本发明提供了多种有用的多肽。 特别地，可以使用包含与SEQ ID NO：1，SEQ ID NO：2或SEQ ID NO：3所示的氨基酸序列相同或基本上相同的氨基酸序列的多肽，其酰胺或其盐 作为预防/治疗低血压的药剂; 用于预防/治疗肥胖症，食欲过多等的药剂; 预防/治疗嗜睡，时区变化综合征（时差）等的药剂; 用于预防/治疗不育症的药剂等。一种促进包含与SEQ ID NO：7至12和37中任一项所示的氨基酸序列相同或基本上相同的氨基酸序列的多肽的活性的化合物或其盐 至42，其部分肽或其盐可用作预防/治疗例如绝经症状或甲状腺功能亢进的药剂。 抑制所述多肽的活性的化合物或其盐可用作预防/治疗例如不育或甲状腺功能减退的药剂。

    Musclin receptor and use thereof
    286.
    发明申请
    Musclin receptor and use thereof 审中-公开
    Musclin受体及其用途

    公开(公告)号：US20110104705A1

    公开(公告)日：2011-05-05

    申请号：US12311447

    申请日：2006-09-30

    Applicant: Shunbun Kita ,  Iichirou Shimomura ,  Yukio Yamada

    Inventor： Shunbun Kita ,  Iichirou Shimomura ,  Yukio Yamada

    IPC: G01N33/53 ,  C07K14/435 ,  C07H21/04 ,  C07K16/00 ,  C12Q1/02

    CPC classification number: A61K31/7088 ,  A61K38/00 ,  A61K47/665 ,  B82Y5/00 ,  C07K14/47

    Abstract: The present invention provides a receptor of musclin and a screening system for an agonist and/or antagonist of the receptor by means of the interaction of musclin and the receptor. Hence, provided is a screening method for a substance that alters the bindability (i) a protein containing the same or substantially the same amino acid sequence as the amino acid sequence shown by SEQ ID NO:2 or a partial peptide thereof or a salt thereof and (ii) musclin or a partial peptide thereof or a salt thereof, containing using both.

    Abstract translation: 本发明通过莫斯林和受体的相互作用提供了受体的musclin受体和受体的激动剂和/或拮抗剂的筛选系统。 因此，提供了改变可结合性的物质的筛选方法（i）含有与SEQ ID NO：2所示的氨基酸序列或其部分肽或其盐相同或基本相同的氨基酸序列的蛋白质 和（ii）含有两者的musclin或其部分肽或其盐。

    Methods of screening for compounds which bind G protein-coupled receptors
    287.
    发明授权
    Methods of screening for compounds which bind G protein-coupled receptors 失效
    筛选结合G蛋白偶联受体的化合物的方法

    公开(公告)号：US07927821B2

    公开(公告)日：2011-04-19

    申请号：US11578325

    申请日：2005-04-11

    Applicant: Ryo Fujii ,  Shoichi Okubo ,  Kazunori Nishi ,  Shuji Hinuma ,  Masaaki Mori

    Inventor： Ryo Fujii ,  Shoichi Okubo ,  Kazunori Nishi ,  Shuji Hinuma ,  Masaaki Mori

    IPC: G01N33/53 ,  G01N33/567 ,  G01N33/566 ,  C07K1/00 ,  C07K14/00 ,  C07K17/00

    CPC classification number: G01N33/76 ,  A61K31/403 ,  A61K31/4155 ,  A61K31/4523 ,  A61K38/1796 ,  C07K14/705 ,  G01N2333/726

    Abstract: The present invention provides a method of screening an agonist or antagonist to 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 a salt thereof and the ligand or a salt thereof; etc. The present invention is useful for screening agents for the prevention/treatment of, e.g., leukopenia, leukemia, lymphoma, malignant tumor, ulcerative colitis, rheumatoid arthritis, inflammatory bowel disorders, tonsil disorders, collagen disease, inflammatory disease, leukocytosis, heart failure, inherited muscle disorders, muscular dystrophy, neuromuscular degenerative disease, myocardial infarction, obesity, mellitus diabetes, hyperlipemia, arteriosclerosis, metabolic syndrome, thrombocytopenia, thrombocytosis, cancer, pulmonary edema, multiple organ failure, etc.

    Abstract translation: 本发明提供筛选G蛋白偶联受体蛋白的激动剂或拮抗剂的方法，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; 本发明可用于预防/治疗例如白细胞减少症，白血病，淋巴瘤，恶性肿瘤，溃疡性结肠炎，类风湿性关节炎，炎性肠病，扁桃体病，胶原病，炎性疾病，白细胞增多症，心脏病 失败，遗传性肌肉疾病，肌营养不良症，神经肌肉退行性疾病，心肌梗死，肥胖症，糖尿病，高脂血症，动脉硬化，代谢综合征，血小板减少症，血小板增多症，癌症，肺水肿，多器官衰竭等。

    ORALLY DISINTEGRABLE TABLETS
    288.
    发明申请
    ORALLY DISINTEGRABLE TABLETS 审中-公开
    ORALLY DISINTABLE TABLETS

    公开(公告)号：US20110081412A1

    公开(公告)日：2011-04-07

    申请号：US12967858

    申请日：2010-12-14

    Applicant: Toshihiro SHIMIZU ,  Shuji MORIMOTO ,  Tetsuro TABATA

    Inventor： Toshihiro SHIMIZU ,  Shuji MORIMOTO ,  Tetsuro TABATA

    IPC: A61K9/50 ,  A61K9/28 ,  A61K31/4439 ,  A61K9/32 ,  A61K9/22 ,  A61K9/14 ,  A61P1/04

    CPC classification number: A61K9/28 ,  A61K9/0056 ,  A61K9/1611 ,  A61K9/1652 ,  A61K9/2081 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5073 ,  A61K31/4439

    Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 μm or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

    Abstract translation: 本发明的口腔崩解片，其特征在于，其包含（i）平均粒径为400μm以下的细颗粒，所述微粒包含通过肠溶衣层包被的组合物，所述组合物的10重量％以上 酸不稳定的生理活性物质和（ii）添加剂，在口腔中具有优异的崩解性或溶解性，因此其可用于治疗或预防各种疾病，作为能够施用于老年人的口腔崩解片剂 儿童，容易无水。 此外，由于本发明的片剂含有平均粒径不会使口腔粗糙的细颗粒，因此在施用时可以容易地施用，而不会不适。

    HEXAHYDROOXAZINOPTERINE COMPOUNDS
    290.
    发明申请
    HEXAHYDROOXAZINOPTERINE COMPOUNDS 有权
    十六氢X嗪化合物

    公开(公告)号：US20110053921A1

    公开(公告)日：2011-03-03

    申请号：US12869452

    申请日：2010-08-26

    Applicant: Bohan Jin ,  Nicholas Scorah ,  Qing Dong

    Inventor： Bohan Jin ,  Nicholas Scorah ,  Qing Dong

    IPC: A61K31/5383 ,  C07D498/14 ,  A61P35/00

    CPC classification number: C07D498/14

    Abstract: The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.

    Abstract translation: 本发明提供下式的mTOR抑制剂，其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 制备化合物及其中间体的方法; 和使用该化合物的方法。

Patent Agency Ranking