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    NOVEL BENZYLIDENE AZOLIDINE DERIVATIVE OR SALT THEREOF
    3.
    发明公开
    NOVEL BENZYLIDENE AZOLIDINE DERIVATIVE OR SALT THEREOF 有权
    苯甲酰胆碱衍生物

    公开(公告)号：EP2832727A1

    公开(公告)日：2015-02-04

    申请号：EP13767915.5

    申请日：2013-03-27

    申请人： Rohto Pharmaceutical Co., Ltd.

    发明人： SHIMIZU,Takashi

    IPC分类号： C07D233/96 ,  A61K8/49 ,  A61Q17/04 ,  A61Q19/00 ,  C09K3/00

    CPC分类号： C07D233/96 ,  A61K8/49 ,  A61K8/494 ,  A61K8/4946 ,  A61Q17/04 ,  A61Q19/00

    摘要： Provided is a novel compound which has excellent ultraviolet-absorbing function (especially UVA absorbing function) and excellent hydrophilicity. A benzylidene azolidine derivative of the present invention or a salt thereof is characterized by being a benzylidene azolidine derivative represented by specif ic structural formula (I) or a salt thereof. (In structural formula (I), n represents an integer of 1-5; A 1 represents O, S or N-A 4 ; and each of A 2 , A 3 and A 4 independently represents a hydrogen atom, an alkyl group which may be substituted by a hydroxyl group and has 1-8 carbon atoms, or the like (provided that at least one of A 2 , A 3 and A 4 contains one or more hydroxyl groups). In this connection, when n is an integer of 2-5, the plurality of A 3 O- moieties may be the same as or different from each other.)

    摘要翻译： 提供具有优异的紫外线吸收功能（特别是UVA吸收功能）和优异的亲水性的新型化合物。 本发明的亚苄基偶氮烷衍生物或其盐的特征在于由特定的结构式（I）表示的亚苄基偶氮唑衍生物或其盐。 （结构式（I）中，n表示1〜5的整数，A 1表示O，S或NA 4，A 2，A 3和A 4各自独立地表示氢原子， 被羟基取代并具有1-8个碳原子等（前提是A 2，A 3和A 4中的至少一个含有一个或多个羟基），在这一点上，当n为2的整数时 -5，多个A 3 O-部分可以彼此相同或不同。）

    COUPLED RECOGNITION/DETECTION SYSTEM FOR IN VIVO AND IN VITRO USE
    6.
    发明公开
    COUPLED RECOGNITION/DETECTION SYSTEM FOR IN VIVO AND IN VITRO USE 审中-公开
    加之检测/探测系统在体内和体外应用

    公开(公告)号：EP2398775A4

    公开(公告)日：2013-01-02

    申请号：EP10744308

    申请日：2010-02-18

    申请人： UNIV CORNELL

    发明人： JAFFREY SAMIE R ,  PAIGE JEREMY S

    IPC分类号： C07D233/96 ,  A61K49/00 ,  C07D403/06

    CPC分类号： C07D233/96 ,  A61K49/0032 ,  A61K49/0054 ,  C07D403/06

    摘要： The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.

    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS
    9.
    发明授权
    CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS 有权
    骑行肼TNF-α抑制剂

    公开(公告)号：EP1137640B1

    公开(公告)日：2005-09-21

    申请号：EP99965432.0

    申请日：1999-12-02

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： BROADHURST, Michael John ,  JOHNSON, William Henry ,  WALTER, Daryl Simon

    IPC分类号： C07D233/80 ,  A61K31/395 ,  C07D239/54 ,  C07D285/18 ,  C07D495/04 ,  C07D233/34 ,  C07D251/34 ,  C07D249/12 ,  C07D241/08 ,  C07D235/02 ,  C07D233/84 ,  C07D471/10 ,  C07D239/96 ,  C07D401/06 ,  C07D233/96 ,  C07D285/10 ,  C07D487/04

    CPC分类号： C07D235/02 ,  C07D233/34 ,  C07D233/80 ,  C07D233/84 ,  C07D233/96 ,  C07D239/54 ,  C07D239/96 ,  C07D241/08 ,  C07D249/12 ,  C07D251/34 ,  C07D285/10 ,  C07D285/18 ,  C07D401/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

    摘要： Hydrazine derivatives of formula (I) wherein W represents O, S, CO, NR?5, (CR3R4)¿m, or CR11; X represents CO, NR6, (CH2)n, CR?12 or CHR13¿; Y represents CO, NR7, (CH2)p, or CHR14; Z represents CO, CS, SO¿2?, or CH2; m stands for 0 or 1; n and p each individually stand for 0, 1, or 2; R?1¿ represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula V-aryl, V-heterocyclyl or -(CH¿2?)q-CH=CR?8R9; R3, R4, R5, R6 and R7¿ each independently represent hydrogen, optionally substituted lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; or R?3 and R4¿ together with the carbon atom to which they are attached form a 3- to 8-membered ring; or R?5 and R6 or R5 and R7¿ together with the nitrogen atoms to which they are attached form a 3- to 8-membered ring; or R?11 and R12¿ together with the sp2 carbon atoms to which they are attached form a fused lower cycloalkenyl, aryl or heteroaryl ring; or R5 with either R?13 or R14¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; or either R?6 or R7¿ with either R3 or R4 together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; or R?3 and R4¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; V represents a spacer group; R?8 and R9¿ together represent lower alkylene in which a CH¿2? group is optionally replaced by a heteroatom; and q stands for 1 or 2; with the provisos that (i) at least one of W, X and Y represents one of the heteroatoms previously indicated for these substituents or CO, (ii) Z represents CO or SO2 or CS when W represents O; (iii) W, X, Y and Z are not all CO and (iv) W, X and Y are not all NR?5, NR6 and NR7¿, respectively; and pharmaceutically acceptable salts thereof inhibit the release of tumour necrosis factor alpha (TNF-α) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.

    NITRIC OXIDE DONORS, COMPOSITIONS AND METHODS OF USE
    10.
    发明公开
    NITRIC OXIDE DONORS, COMPOSITIONS AND METHODS OF USE 审中-公开
    氮氧化物捐助者和组合物的方法

    公开(公告)号：EP1497268A2

    公开(公告)日：2005-01-19

    申请号：EP03719621.9

    申请日：2003-04-07

    申请人： Nitromed, Inc.

    发明人： FANG, Xinqin ,  GARVEY, David, S. ,  GASTON, Ricky, D. ,  LIN, Chia-En ,  RANATUNGA, Ramani, R. ,  RICHARDSON, Stewart, K. ,  WANG, Tiansheng ,  WANG, Weiheng ,  WEY, Shiow-Jyi

    IPC分类号： C07D235/00

    CPC分类号： C07D213/74 ,  C07C313/36 ,  C07C2602/08 ,  C07C2602/42 ,  C07C2603/74 ,  C07D211/54 ,  C07D217/02 ,  C07D233/96 ,  C07D239/47 ,  C07D241/08 ,  C07D241/24 ,  C07D295/155 ,  C07D317/22 ,  C07D453/02 ,  C07F9/383 ,  C07F9/4018

    摘要： The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.