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    Benzene fused heterocyclic derivative and pharmaceutical composition comprising the same
    1.
    发明授权
    Benzene fused heterocyclic derivative and pharmaceutical composition comprising the same 有权

    公开(公告)号：US11091421B2

    公开(公告)日：2021-08-17

    申请号：US16620608

    申请日：2018-09-07

    申请人： TAIWANJ PHARMACEUTICALS CO., LTD.

    发明人： Syaulan S. Yang ,  Kuang Yuan Lee ,  Meng Hsien Liu ,  Yan-Feng Jiang ,  Yu-Shiou Fan ,  Chi-Han Chen ,  Sheng Hung Liu

    IPC分类号： C07C65/00 ,  C07C233/00 ,  C07C49/00 ,  C07D209/00 ,  C07D217/00 ,  C07C65/21 ,  C07C49/755 ,  C07C65/38 ,  C07C69/78 ,  C07C233/66 ,  C07C233/69 ,  C07C271/30 ,  C07C275/38 ,  C07D209/48 ,  C07D211/32 ,  C07D217/24 ,  C07D295/182 ,  C07D307/83

    摘要： The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is —CH2—, —CH(OH)—, or —C(O)—; G is C or N; X is —CH2—, O, or —C(O)—; Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, —NRy1Ry2, —ORy1, —Ry1C(O)Ry3, —C(O)Ry1, —C(O)ORy2, —C(O)ORy2Ry3, —NRy1C(O)Ry2, —NRy1C(O)NRy2Ry3, —NRy1C(O)ORy2Ry3, —NRy1C(O)Ry2ORy3, C(O)NRy1(Ry2Ry3), —C(O)NRy1(Ry2ORy1), —ORy2Ry3, and —ORy2ORy3, wherein each of Ry1 and Ry2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and Ry3 is aryl optionally substituted with at least one halogen; Z is —NRz1Rz2, —NRz1Rz3, —ORz1, —ORz1Rz3, —C(O)Rz1Rz3, —C(O)ORz1Rz3, —NRz1C(O)Rz2Rz3, —NRz1C(O)ORz2Rz3, —C(O)NRz1Rz3, or ORz2ORz3, wherein each of Rz1 and Rz2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and Rz3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, —RzaCOORzb, —ORzaCOORzb, —RzaSO2Rzb, —RzaSO2NRzbRzcRzd, —RzaC(O)RzbRzc, —RzaC(O)NRzbRzcRzd, —RZaC(O)NRzbSO2Rzc, wherein Rza is nil or alkyl, Rzb is H or alkyl, each of Rzb and Rzc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NRzbRzc is a nitrogen-containing heterocyclic alkyl ring, Rzd is nil or a sulfonyl alkyl group.

    Indolin-2-one derivatives as protein kinase inhibitors
    4.
    发明授权
    Indolin-2-one derivatives as protein kinase inhibitors 有权

    公开(公告)号：US08946282B2

    公开(公告)日：2015-02-03

    申请号：US13855916

    申请日：2013-04-03

    申请人： Annji Pharmaceutical Co., Ltd.

    发明人： Ji-Wang Chern ,  Ajit Dhananjay Jagtap ,  Hsiao-Chun Wang ,  Grace Shiahuy Chen

    IPC分类号： C07D209/34 ,  C07D403/06 ,  C07D401/06 ,  A61K38/45 ,  C07D401/14 ,  C07D409/06 ,  C07D405/06 ,  C07D403/14 ,  A61K31/522 ,  C07D473/32 ,  C07D209/00

    CPC分类号： C07D209/34 ,  A61K31/522 ,  A61K38/45 ,  C07D209/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D473/32

    摘要： A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. In one aspect, the invention relates to a compound a compound of Formula A: or a pharmaceutically acceptable salt thereof, wherein: Ra is hydrogen, (C6-C18)aryl, halo(C6-C18)aryl, or (C1-C6)alkoxy(C6-C18)aryl; Rb is hydrogen, (C3-C18)heteroaryl, (C1-C6)alkoxy(C3-C18)heteroaryl; (C1-C6)alkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)carboxyalkyl(C3-C18)heteroaryl; (C1-C6)alkyl(C1-C6)alkylamino(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxycarbonyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C1-C6)oxyalkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclylcarbonyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclyl(C1-C6)oxyalkyl(C3-C18)heteroaryl, or (C1-C6)alkyl((C3-C6)heterocyclyl(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl; Rc is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Rd is hydrogen, halogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Re is-hydrogen, benzoylureido, halobenzoylureido, halo(C1-C6)alkoxybenzoylureido, (C1-C6)alkoxybenzoylureido, (C1-C6)alkylaminobenzoylureido, (C1-C6)alkylbenzoylureido, nitrobenzoylureido, (C1-C6)haloalkylbenzoylureido, (C1-C6)haloalkylhalobenzoylureido, halo(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbamoyl(C3-C6)cycloalkylamido, halo(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C3-C6)cycloalkyl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkylamino(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C1-C6)alkoxy(C6-C18)aryl(C3-C18) heteroarylcarbonylamino, (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkyl(C3-C18)heteroarylcarbonylamino, aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)haloalkylhalo(C6-C18)aryl(C3-C6)heterocyclylcarbonylamino, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)oxyalkyl(C3-C6)heterocyclylamido, (C1-C6)alkoxy(C1-C6)alkyl(C3-C18)heteroarylamido, (C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroarylamido, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C3-C18)heteroarylamido, or (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylamido; and Rf is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido.

    Colorants in foam form
    6.
    发明授权
    Colorants in foam form 有权
    泡沫形式的着色剂

    公开(公告)号：US08734530B2

    公开(公告)日：2014-05-27

    申请号：US13740344

    申请日：2013-01-14

    申请人： Henkel AG & Co. KGaA

    发明人： Frank Janssen ,  Jurgen Schopgens ,  Sabine Babiel ,  Armin Wadle ,  Udo Erkens

    IPC分类号： A61Q5/10 ,  C07D209/04 ,  A61Q5/06 ,  A61K8/04 ,  A61K8/64 ,  A61K8/49 ,  C07D209/00 ,  C07D209/08 ,  C09B29/40

    CPC分类号： C07D209/00 ,  A61K8/046 ,  A61K8/22 ,  A61K8/492 ,  A61K8/64 ,  A61K2800/30 ,  A61Q5/065 ,  A61Q5/10 ,  C07D209/04 ,  C07D209/08 ,  C09B29/3613

    摘要： An agent in foam form for coloring keratin-containing fibers, in particular human hair, under induction by atmospheric oxygen and methods for coloring keratin-containing fibers using such agent is provided. In an embodiment, the agent comprises, in a cosmetically acceptable carrier, at an alkaline pH of 8 to 10.5, (a) as a color-forming component in the form of a dye precursor of a nature-analogous dye an indole and/or indoline derivative, (b) an alkalizing agent, and (c) a propellant, the agent containing no additional oxidizing agent for the color-forming components.

    摘要翻译： 提供了一种泡沫形式的用于使含有角蛋白的纤维，特别是人类头发，通过大气氧诱导的成型剂，以及使用这种试剂使含有角蛋白的纤维着色的方法。 在一个实施方案中，所述试剂在化妆品可接受的载体中包含在8至10.5的碱性pH下，（a）作为自然 - 类似染料的染料前体形式的成色组分，吲哚和/或 二氢吲哚衍生物，（b）碱化剂，和（c）推进剂，所述试剂不含用于成色组分的另外的氧化剂。

    Heteropyrrole analogs acting on cannabinoid receptors
    8.
    发明授权
    Heteropyrrole analogs acting on cannabinoid receptors 有权
    作用于大麻素受体的异丙吡咯类似物

    公开(公告)号：US08410097B2

    公开(公告)日：2013-04-02

    申请号：US13334163

    申请日：2011-12-22

    申请人： Alexandros Makriyannis ,  Rajesh Thotapally ,  Venkata Kiran Rao Vemuri ,  Teresa Olszewska

    发明人： Alexandros Makriyannis ,  Rajesh Thotapally ,  Venkata Kiran Rao Vemuri ,  Teresa Olszewska

    IPC分类号： A61K31/41 ,  A61K31/405 ,  C07D207/00 ,  C07D209/00

    CPC分类号： C07D233/90 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10

    摘要： Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.

    摘要翻译： 公开了能够与CB1和/或CB2大麻素受体相互作用的生物活性杂吡咯类似物，例如咪唑，噻唑，恶唑和吡唑。 一方面公开了作为CB1和/或CB2受体拮抗剂的杂吡咯类似物。 另一方面公开了对CB1或CB2大麻素受体具有选择性的异构吡咯类似物。 还公开了采用公开的类似物的药物制剂和施用治疗有效量的所公开的类似物以提供生理作用的方法。