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    POLYMERS OF INTRINSIC MICROPOROSITY (PIMS) CONTAINING LOCKED SPIROBISINDANE STRUCTURES AND METHODS OF SYNTHESIS OF PIMS POLYMERS
    1.
    发明申请
    POLYMERS OF INTRINSIC MICROPOROSITY (PIMS) CONTAINING LOCKED SPIROBISINDANE STRUCTURES AND METHODS OF SYNTHESIS OF PIMS POLYMERS 审中-公开
    含有螺旋体结构的内在微结构聚合物（PIMS）和聚合物合成方法

    公开(公告)号：WO2017030450A1

    公开(公告)日：2017-02-23

    申请号：PCT/NZ2016/050133

    申请日：2016-08-22

    申请人： AUCKLAND UNISERVICES LIMITED

    发明人： JIN, Jianyong ,  ZHANG, Jian

    IPC分类号： C08G65/40 ,  C07D313/20

    CPC分类号： C07D313/06 ,  C08G65/40 ,  C08G65/4006 ,  C08G65/4031 ,  C08G65/4056

    摘要： A method of increasing the rigidity of PIM homo- or co-polymers including repeating units containing at least one biscatechol monomer having a fused spiro-bisindane (SBI) ring system of Formula (I), the SBI ring system including a bicyclic spiro-carbon: (I) wherein each R 1 can be the same or different, each R 2 can be the same or different and wherein R 1 and/or R 2 are selected from any one or more of H; straight or branched, saturated or unsaturated lower C 1 -C 6 alkyl groups, wherein the lower alkyl groups can include aromatic or non-aromatic ring structures; R 3 OR 4 , R 3 O(C=O)R 4 , R 3 C(=O)OR 4 , or R 3 OH, wherein each of R 3 and R 4 are the same or different and are selected from straight or branched, saturated or unsaturated lower C 1 - C 6 alkyl groups; and R 5 and R represent suitable linking monomers, wherein the linking monomers can be the same or different and are preferably selected from any one or more tetrahalo aromatic monomers; and wherein the method includes the step of introducing an intra- molecular lock between C1 and C2 of the biscatechol monomer of Formula (I).

    摘要翻译： 包括含有至少一种具有式（I）的稠合双 - 二茚满（SBI）环系的双酚A单体的重复单元的PIM均聚物或共聚物的刚性的增强方法，SBI环体系包括双环螺 - 碳 ：（I）其中每个R 1可以相同或不同，每个R 2可以相同或不同，并且其中R 1和/或R 2选自H中的任何一个或多个; 直链或支链，饱和或不饱和的低级C1-C6烷基，其中低级烷基可包括芳族或非芳族环结构; R 3 OR 4，R 3 O（C = O）R 4，R 3 C（= O）OR 4或R 3 OH，其中R 3和R 4各自相同或不同，并且选自直链或支链，饱和或不饱和的低级C 1 -C 6烷基; R5和R表示合适的连接单体，其中连接单体可以相同或不同，优选选自任何一种或多种四卤代芳族单体; 并且其中所述方法包括在式（I）的双儿茶酚单体的C1和C2之间引入分子内锁定的步骤。

    NATURAL BRASSINOSTEROIDS FOR USE FOR TREATING HYPERPROLIFERATION, TREATING PROLIFERATIVE DISEASES AND REDUCING ADVERSE EFFECTS OF STEROID DYSFUNCTION IN MAMMALS, PHARMACEUTICAL COMPOSITION AND ITS USE
    3.
    发明申请
    NATURAL BRASSINOSTEROIDS FOR USE FOR TREATING HYPERPROLIFERATION, TREATING PROLIFERATIVE DISEASES AND REDUCING ADVERSE EFFECTS OF STEROID DYSFUNCTION IN MAMMALS, PHARMACEUTICAL COMPOSITION AND ITS USE 审中-公开
    天然BRASSINOSTEROIDS用于治疗过度增殖，治疗增殖性疾病和减少哺乳动物，药物组合物及其应用中类固醇失调的不良反应

    公开(公告)号：WO2009024103A2

    公开(公告)日：2009-02-26

    申请号：PCT/CZ2008/000097

    申请日：2008-08-20

    申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY, V.V.I. ,  UNIVERZITA PALACKEHO V OLOMOUCI ,  OKLESTKOVA, Jana ,  HOFFMANNOVÁ, Lucie ,  STEIGEROVÁ,, Jana ,  KOHOUT, Ladislav ,  KOLAR, Zdenek ,  STRNAD, Miroslav

    发明人： OKLESTKOVA, Jana ,  HOFFMANNOVÁ, Lucie ,  STEIGEROVÁ,, Jana ,  KOHOUT, Ladislav ,  KOLAR, Zdenek ,  STRNAD, Miroslav

    CPC分类号： C07J17/005 ,  C07D313/06 ,  C07D313/10 ,  C07J9/00 ,  C07J73/00

    摘要： The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH 2 or O-CH 2 group, R 2 is hydrogen or hydroxyl, R 3 is hydroxyl, R 24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R 25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo , especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids. This invention also describes new use for treating consisting in a new therapeutic way for modifying cell viability of human breast and prostate cancer cells.

    摘要翻译： 本发明涉及通式（I）的天然油菜素内甾体，其中R为CH 2或O-CH 2基团， 其中R 2是氢或羟基，R 3是羟基，R 24是烷基或链烯基，其选自甲基，乙基， 丙基，异丙基，亚甲基，亚乙基和丙基，而R 25是选自甲基和乙基的烷基及其药学上可接受的盐，用于治疗过度增殖，治疗增殖性疾病和减少 类固醇功能障碍在哺乳动物中的不良作用。 本发明还提供了能够通过天然油菜素类固醇抑制细胞周期从而导致癌细胞凋亡改变的方法。 更具体地说，本发明涉及通过施用组合物治疗哺乳动物过度增殖对哺乳动物细胞体外和体内的不利影响，特别是治疗哺乳动物过度增殖性疾病的用途， 含有天然油菜素内酯。 本发明还描述了用于治疗的新用途，其构成用于修饰人乳房细胞和前列腺癌细胞的细胞活力的新的治疗方法。

    EXCITATORY AMINO ACID DERIVATIVES
    8.
    发明申请
    EXCITATORY AMINO ACID DERIVATIVES 审中-公开
    激素氨基酸衍生物

    公开(公告)号：WO0132644A2

    公开(公告)日：2001-05-10

    申请号：PCT/US0028865

    申请日：2000-10-30

    申请人： LILLY CO ELI ,  BAKER STEPHEN RICHARD ,  HANCOX TIMOTHY COLIN

    发明人： BAKER STEPHEN RICHARD ,  HANCOX TIMOTHY COLIN

    IPC分类号： C07D311/02 ,  C07D313/06 ,  C07D335/04 ,  C07D337/06 ,  C07D337/00

    CPC分类号： C07D313/06 ,  C07D311/02 ,  C07D335/04 ,  C07D337/06

    摘要： Compounds for formula (I) in which: Y represents O, NR , S, SO or SO2; X represents (CR R )m; X represents (CR R )n; one of m and n is 1 and the other is 0 or 1; and R , R , R and R are each as defined in the specification; and non-toxic metabolically labile esters or amides thereof; and pharmaceutically acceptable salts thereof; are useful as modulators of metabotropic glutamate receptor function.

    摘要翻译： 式（I）化合物，其中：Y表示O，NR a，S，SO或SO 2; X 1表示（CR 1 R 2）m; X 2表示（CR 3 R 4）n; m和n之一是1，另一个是0或1; R 1，R 2，R 3和R 4各自如说明书中所定义; 和无毒的代谢不稳定的酯或其酰胺; 及其药学上可接受的盐; 可用作代谢型谷氨酸受体功能的调节剂。

    PENTACYCLIC OXEPINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS
    9.
    发明申请
    PENTACYCLIC OXEPINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS 审中-公开
    PENTACYCLIC OXEPINES及其衍生物，其制备方法及含有它们的药物组合物

    公开(公告)号：WO2004009578A2

    公开(公告)日：2004-01-29

    申请号：PCT/US2003/019561

    申请日：2003-07-18

    申请人： ELI LILLY AND COMPANY ,  HINKLIN, Ronald, Jay ,  WALLACE, Owen, Brendan

    发明人： HINKLIN, Ronald, Jay ,  WALLACE, Owen, Brendan

    IPC分类号： C07D313/00

    CPC分类号： C07D409/10 ,  C07D313/06 ,  C07D313/10 ,  C07D333/56 ,  C07D495/04

    摘要： The present invention provides a compound of the formula (I) wherein R 1 is -H, -OH, -O(C 1 -C 4 alkyl), -OCOC 6 H 5 , -OCO(C 1 -C 6 alkyl), or -OSO 2 (C 2 -C 6 alkyl); R 0 , R 2 and R 3 are each independently -H, -OH, -O(C 1 -C 4 alkyl), -OCOC 6 H 5 , -OCO(C 1 -C 6 alkyl), -OSO 2 (C 2 -C 6 alkyl) or halo; R 4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is -S- or -HC=CH-; G is -O-, -S-, -SO-, SO 2 , or -N(R 5 )-, wherein R 5 is -H or C 1 -C 4 alkyl; and Y is -O-, -S-, -NH-, -NMe-, or -CH 2 -; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

    摘要翻译： 本发明提供式（I）化合物，其中R 1是-H，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基）或-OSO 2（C 2 -C 1-6烷基）; R 0，R 2和R 3各自独立地为-H，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基），-OSO 2（C 2 -C 6 烷基）或卤素; R 4是1-哌啶基，1-吡咯烷基，甲基-1-吡咯烷基，二甲基-1-吡咯烷基，4-吗啉代，二甲基氨基，二乙基氨基，二异丙基氨基或1-六亚甲基亚氨基; n为2或3，X为-S-或-HC = CH-; G是-O - ， - S - ， - SO-，SO 2或-N（R 5） - ，其中R 5是-H或C 1 -C 4烷基; 且Y为-O - ， - S - ， - NH - ， - MeMe - 或-CH 2 - ; 或其药学上可接受的盐; 其药物组合物，任选与雌激素和孕激素组合; 抑制与雌激素剥夺有关的疾病的方法; 以及用于抑制与内源性雌激素异常生理反应相关的疾病的方法。

    PROCESS FOR THE PREPARATION OF ESTERS OR LACTONES
    10.
    发明申请
    PROCESS FOR THE PREPARATION OF ESTERS OR LACTONES 审中-公开
    制备胚芽或乳酪的方法

    公开(公告)号：WO00053593A1

    公开(公告)日：2000-09-14

    申请号：PCT/JP2000/000988

    申请日：2000-02-22

    IPC分类号： B01J27/10 ,  B01J27/125 ,  B01J27/135 ,  B01J31/02 ,  C07C67/42 ,  C07D307/33 ,  C07D313/04 ,  C07D313/06 ,  C07D315/00

    CPC分类号： C07D307/33 ,  C07D313/06 ,  C07D315/00

    摘要： A process for the preparation of esters or lactones, which comprises reacting a ketone represented by general formula (1) (wherein Ra and Rb are each independently an organic group having a carbon atom at the position where the carbonyl carbon atom adjacent thereto is bonded, or alternatively Ra and Rb together with the carbonyl carbon atom may form a ring) with hydrogen peroxide in the presence of a compound containing a metallic element selected from among Group 3, 13, 14 and 15 metallic elements of the periodic table to thereby obtain a compound represented by general formula (2) (wherein Ra and Rb are each independently an organic group having a carbon atom at the position where the carbonyl carbon atom or oxygen atom adjacent thereto is bonded, or alternatively Ra and Rb together with the carbonyl carbon atom and the oxygen atom may form a ring). This process makes it possible to convert ketones to the corresponding esters or lactones in high yield by using hydrogen peroxide.

    摘要翻译： 一种制备酯或内酯的方法，其包括使由通式（1）表示的酮（其中Ra和Rb各自独立地为与其相邻的羰基碳原子键合的位置具有碳原子的有机基团反应， 或者Ra和Rb与羰基碳原子一起形成环）与过氧化氢在含有选自元素周期表第3,13,14和15族金属元素的金属元素的化合物存在下反应，从而得到 由通式（2）表示的化合物（其中R a和R b各自独立地为与羰基碳原子或与其相邻的氧原子键合的位置具有碳原子的有机基团，或者Ra和Rb与羰基碳原子一起 并且氧原子可以形成环）。 该方法可以通过使用过氧化氢以高收率将酮转化为相应的酯或内酯。