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    NOVEL ISOQUINOLINE DERIVATIVES
    1.
    发明申请
    NOVEL ISOQUINOLINE DERIVATIVES 审中-公开
    新型异喹啉衍生物

    公开(公告)号：WO2010117084A1

    公开(公告)日：2010-10-14

    申请号：PCT/JP2010/056635

    申请日：2010-04-07

    Applicant: BANYU PHARMACEUTICAL CO.,LTD. ,  SUGIMOTO, Yuichi ,  SATOH, Atsushi ,  NISHIMURA, Teruyuki

    Inventor： SUGIMOTO, Yuichi ,  SATOH, Atsushi ,  NISHIMURA, Teruyuki

    IPC: C07D217/24 ,  A61K31/472 ,  A61K31/4725 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P43/00 ,  C07D401/12

    CPC classification number: C07D217/24 ,  C07D401/12

    Abstract: The present invention relates to a compound represented by a formula (I): wherein: R is independently from each other a lower alkyl group and the like, X is an oxygen atom or a sulfur atom, Y is a lower alkylene group having 1 to 6 carbon atoms, R 1 is a phenyl group and the like which may be substituted by a halogen atom and the like, and any CH 2 in the following: (I-1) may be substituted by a lower alkyl group, and R 2 is a phenyl group or a pyridinyl group which may be substituted by a lower alkyl group and the like, m is 0, 1, 2 or 3, and n is 0 or 1, or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及由式（I）表示的化合物：其中：R彼此独立地为低级烷基等，X为氧原子或硫原子，Y为低级亚烷基，具有1〜 6个碳原子，R 1是可以被卤素原子等取代的苯基等，以下的任何CH 2：（I-1）可以被低级烷基取代，R 2是苯基 基团或可以被低级烷基等取代的吡啶基，m为0,1,2或3，n为0或1，或其药学上可接受的盐。

    RHESUS MONKEY BOMBESIN RECEPTOR SUBTYPE-3 (BRS-3), NUCLEOTIDES ENCODING SAME, AND USES THEREOF
    6.
    发明申请
    RHESUS MONKEY BOMBESIN RECEPTOR SUBTYPE-3 (BRS-3), NUCLEOTIDES ENCODING SAME, AND USES THEREOF 审中-公开
    RHESUS MONKEY BOMBESIN受体亚型3（BRS-3），编码它们的核苷酸及其用途

    公开(公告)号：WO2004093785A2

    公开(公告)日：2004-11-04

    申请号：PCT/US2004/011473

    申请日：2004-04-14

    Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  TAN, Carina, P. ,  HOWARD, Andrew, D. ,  SANO, Hideki

    Inventor： TAN, Carina, P. ,  HOWARD, Andrew, D. ,  SANO, Hideki

    IPC: A61K

    CPC classification number: C07K14/70571 ,  C07K14/723 ,  G01N2333/70571

    Abstract: A rhesus monkey bombesin receptor subtype-3 has been isolated, cloned and sequenced. This receptor is characteristic of the G-protein family of receptors. Isolated rhesus monkey bombesin receptor subtype-3 may be used to screen and identify novel bombesin receptor modulators that may contribute to the regulation of endocrine processes, metabolism, or the cell cycle. Such compounds may be used in the treatment of conditions that result from deregulated expression of bombesin receptor subtype-3.

    Abstract translation: 已经分离，克隆和测序了恒河猴铃蟾肽受体亚型3。 该受体是G-蛋白家族受体的特征。 分离的恒河猴铃蟾肽受体亚型-3可用于筛选和鉴定可能有助于调节内分泌过程，代谢或细胞周期的新型bombesin受体调节剂。 这些化合物可用于治疗由bombesin受体亚型-3的失调表达引起的病症。

    NOVEL BENZIMIDAZOLE DERIVATIVES
    8.
    发明申请
    NOVEL BENZIMIDAZOLE DERIVATIVES 审中-公开
    新型苯并咪唑衍生物

    公开(公告)号：WO2004002986A2

    公开(公告)日：2004-01-08

    申请号：PCT/JP2003/008161

    申请日：2003-06-26

    Applicant: BANYU PHARMACEUTICAL CO., LTD. ,  OTAKE, Norikazu ,  MORIYA, Minoru ,  OGINO, Yoshio ,  MATSUDA, Kenji ,  NAGAE, Yoshikazu ,  KANATANI, Akio ,  FUKAMI, Takehiro

    Inventor： OTAKE, Norikazu ,  MORIYA, Minoru ,  OGINO, Yoshio ,  MATSUDA, Kenji ,  NAGAE, Yoshikazu ,  KANATANI, Akio ,  FUKAMI, Takehiro

    IPC: C07D471/04

    CPC classification number: C07D473/30 ,  C07D405/04 ,  C07D471/04 ,  C07D471/10 ,  C07D473/00 ,  C07D491/04

    Abstract: A compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is - N(S0 2 R 4 )-, - N (COR 5 ) - or - CO-; Y is -C (R 6 ) (R 7 )_, -0- or -N (R 8 )_, provided that the compound (I) when E is nitrogen, n is 0, X is -CO-, and Y is - 0- is excluded) is useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome, hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation (Pickwickian syndrome), sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, and increased anesthetic risk.

    Abstract translation: 式（I）的化合物：其中A，B，C和D独立地为氮或任选取代的次甲基; E为氮，次甲基或羟基取代的次甲基; n为0或1; T，U，V和W为 独立的氮或任选取代的次甲基; X是-N（SO 2 R 4） - ， - N（COR 5） - 或 - CO-; Y是-C（R 6） 其中当E为氮时，化合物（I）为n，n为0，X为-CO-，Y为0〜 - 被排除）可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗塞，高血压，肾病，电解质异常，血管痉挛，动脉硬化等， 中枢神经系统疾病如贪食症，抑郁症，焦虑症，癫痫发作，癫痫症，痴呆症，酗酒，戒酒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖 ，糖尿病，激素异常，高胆固醇血症，高脂血症，痛风，脂肪肝等，生殖器官或生殖障碍如不育症，早产，性功能障碍等，胃肠疾病，呼吸系统疾病，炎性疾病或青光眼，以及 例如动脉粥样硬化，性腺机能减退，雄激素过多症，多囊卵巢综合征，多毛症，胃肠动力障碍，肥胖相关的胃食管反流，肥胖低通气（皮克维克综合征），睡眠呼吸暂停，炎症，脉管系统的全身炎症， 骨关节炎，胰岛素抵抗，支气管收缩，酒精偏爱，代谢综合征，阿尔茨海默病，心脏肥大，左心室肥大，高甘油三酯血症，低HDL胆固醇，心血管疾病如冠心病（CHD），脑血管疾病，中风，外周血管疾病，突发 死亡，胆囊疾病，癌症（乳腺癌，子宫内膜癌，结肠癌） ），呼吸困难，高尿酸血症，生育能力受损，腰痛，麻醉风险增加。

    RHESUS MONKEY, DOG AND FERRET MELANIN-CONCENTRATING HORMONE TYPE 2 RECEPTOR
    9.
    发明申请
    RHESUS MONKEY, DOG AND FERRET MELANIN-CONCENTRATING HORMONE TYPE 2 RECEPTOR 审中-公开
    鹿茸，OG OG AND ET TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR

    公开(公告)号：WO2002097394A2

    公开(公告)日：2002-12-05

    申请号：PCT/US2002/016702

    申请日：2002-05-28

    Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  TAN, Carina ,  SANO, Hideki

    Inventor： TAN, Carina ,  SANO, Hideki

    IPC: G01N

    CPC classification number: C07K14/72 ,  G01N33/74 ,  G01N33/9406

    Abstract: The present invention identifies the presence of MCH-2R in the dog, ferret and rhesus monkey. MCH-2R is a G-protein coupled receptor that responds to MCH and is distinct from MCH-1R. MCH-2R polypeptide and nucleic acid sequences related to the dog, ferret, and rhesus monkey MCH-2R are described herein along with uses of such polypeptides and nucleic acids.

    Abstract translation: 本发明鉴定了狗，白鼬和恒河猴中MCH-2R的存在。 MCH-2R是对MCH反应的G蛋白偶联受体，不同于MCH-1R。 本文中描述了与狗，白鼬和恒河猴MCH-2R相关的MCH-2R多肽和核酸序列以及这些多肽和核酸的用途。

    PROCESS FOR PRODUCING HALOGENATED HETEROARYL COMPOUNDS
    10.
    发明申请
    PROCESS FOR PRODUCING HALOGENATED HETEROARYL COMPOUNDS 审中-公开
    生产羟基化合物的方法

    公开(公告)号：WO1998025906A1

    公开(公告)日：1998-06-18

    申请号：PCT/JP1997004508

    申请日：1997-12-09

    Applicant: BANYU PHARMACEUTICAL CO., LTD. ,  OKADA, Shigemitsu ,  USHIJIMA, Ryosuke ,  ISHIKAWA, Kiyofumi

    Inventor： BANYU PHARMACEUTICAL CO., LTD.

    IPC: C07D213/61

    CPC classification number: C07D213/79 ,  C07D213/61 ,  C07D213/85 ,  C07D215/48 ,  C07D241/44

    Abstract: A process for producing compounds represented by general formula (II), wherein X represents halogeno; A , A , and A are the same or different and each represents carbon or nitrogen, provided that at least one of A , A , and A is nitrogen; and R , R , R and R are the same or different and each represents hydrogen, lower alkyl, cyano, carboxy, lower alkyloxycarbonyl, carbamoyl, halogeno, nitro, hydroxy, or lower aminoalkyl, provided that when R and R are adjacent substituents, the two can be bonded to each other to form a five- or six-membered ring optionally having on the ring one substituent selected from the group consisting of lower alkyl, nitryl, carboxy, lower alkyloxycarbonyl, carbamoyl, halogeno, nitro, hydroxy, and lower aminoalkyl, characterized by reacting a compound represented by general formula (I), wherein A , A , A , R , R , R , and R have the same meaning as the above, with a halogenated quaternary ammonium salt in the presence of phosphorus pentaoxide.

    Abstract translation: 一种制备由通式（II）表示的化合物的方法，其中X表示卤代; A 1，A 2和A 3相同或不同，各自表示碳或氮，条件是A 1，A 2和A 3中的至少一个为氮 ; R 1，R 2，R 3和R 4相同或不同，各自代表氢，低级烷基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，卤代，硝基，羟基或低级 氨基烷基，条件是当R 1和R 2是相邻的取代基时，两个可以彼此键合以形成任选地在环上具有一个选自下面的取代基的五元或六元环：低级 烷基，硝基，羧基，低级烷氧基羰基，氨基甲酰基，卤代，硝基，羟基和低级氨基烷基，其特征在于使通式（I）表示的化合物，其中A 1，A 2， 卤化季铵盐在五氧化二磷存在下，R 1，R 2，R 3和R 4具有与上述相同的含义。

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