PHARMACEUTICAL COMPOSITION FOR TREATMENT OF OSTEOARTHRITIS
    2.
    发明申请
    PHARMACEUTICAL COMPOSITION FOR TREATMENT OF OSTEOARTHRITIS 审中-公开
    用于治疗OSTEOARTHRITIS的药物组合物

    公开(公告)号:US20130072720A1

    公开(公告)日:2013-03-21

    申请号:US13337661

    申请日:2011-12-27

    CPC classification number: C07C235/56

    Abstract: A pharmaceutical composition including 2-hydroxy-N—[3-(trifluoromethyl)phenyl]benzamide and used for treatment of osteoarthritis is revealed. The pharmaceutical composition inhibits tumor necrosis factor (TNF) induced interferon regulatory factor (IRF). The activated IRF stimulates chondrocytes to secret matrix metalloproteinases, inducible nitric oxide synthase (iNOS), aggrecanases, etc. This leads to loss of collagen II and further causes degradation of proteoglycan. By suppression of signaling pathways of interferon regulatory factor, symptoms are relieved and osteoarthritis is treated.

    Abstract translation: 揭示了用于治疗骨关节炎的包含2-羟基-N- [3-(三氟甲基)苯基]苯甲酰胺的药物组合物。 该药物组合物抑制肿瘤坏死因子(TNF)诱导的干扰素调节因子(IRF)。 激活的IRF刺激软骨细胞分泌基质金属蛋白酶,诱导型一氧化氮合酶(iNOS),聚集蛋白聚糖蛋白聚糖酶等。这导致胶原蛋白II的丧失,并进一步导致蛋白聚糖的降解。 通过抑制干扰素调节因子的信号通路,缓解症状并治疗骨关节炎。

    PHARMACEUTICAL COMPOSITION FOR INHIBITING OSTEOCLAST GROWTH
    4.
    发明申请
    PHARMACEUTICAL COMPOSITION FOR INHIBITING OSTEOCLAST GROWTH 有权
    用于抑制OSTEOCLAST生长的药物组合物

    公开(公告)号:US20120232105A1

    公开(公告)日:2012-09-13

    申请号:US13180253

    申请日:2011-07-11

    CPC classification number: A61K31/167 A61K31/18 A61K31/426 A61K31/505

    Abstract: A pharmaceutical composition for inhibiting osteoclast growth is disclosed in the present invention. The pharmaceutical composition includes a compound represented by a formula (I), and a pharmaceutically acceptable salt and carrier: wherein R1, R2, R3, R4 can be one selected from a group consisting of hydrogen, halogen, C1≈C10 alkyl group, C2≈C10 alkynyl group, amino group, haloalkyl group and sulfonamide group.

    Abstract translation: 用于抑制破骨细胞生长的药物组合物在本发明中公开。 药物组合物包含式(I)表示的化合物及其药学上可接受的盐和载体:其中R 1,R 2,R 3,R 4可以选自氢,卤素,C 1〜C 10烷基,C 2 ≈C10炔基,氨基,卤代烷基和磺酰胺基。

    Anti-cancer compound and manufacturing method thereof
    5.
    发明授权
    Anti-cancer compound and manufacturing method thereof 有权
    抗癌化合物及其制造方法

    公开(公告)号:US08053583B2

    公开(公告)日:2011-11-08

    申请号:US12399935

    申请日:2009-03-07

    Applicant: Hsu-Shan Huang

    Inventor: Hsu-Shan Huang

    CPC classification number: C07D401/12

    Abstract: Anti-cancer compounds and manufacturing methods thereof are disclosed. The anti-cancer compounds are 1,8-diamidoanthraquinone derivatives with amino compounds. The manufacturing method includes the steps of: add 1,8-bis(chloroacetamido)anthraquinone or 1,8-bis(3-chloropropionamido)-anthraquinone with amino compounds, catalysts, and dehydrated dimethylformamide (DMF) to form a mixture and react with one another. Then by purification and recrystallization, the anti-cancer compounds are obtained. The anti-cancer compounds of the present invention are compounds with whole new structure that overcome serious cardiac toxicity of the conventional anti-cancer drug-doxorubincin.

    Abstract translation: 公开了抗癌化合物及其制备方法。 抗癌化合物是具有氨基化合物的1,8-二酰氨基蒽醌衍生物。 该制造方法包括以下步骤:将氨基化合物,催化剂和脱水二甲基甲酰胺(DMF)中的1,8-双(氯乙酰胺基)蒽醌或1,8-双(3-氯丙酰胺基) - 蒽醌加入以形成混合物,并与 另一个。 然后通过纯化和重结晶获得抗癌化合物。 本发明的抗癌化合物是具有全新结构的化合物,其克服了常规抗癌药物多柔比辛的严重心脏毒性。

    HETEROANNELATED ANTHRAQUINONE DERIVATIVES AND THE SYNTHESIS METHOD THEREOF
    7.
    发明申请
    HETEROANNELATED ANTHRAQUINONE DERIVATIVES AND THE SYNTHESIS METHOD THEREOF 审中-公开
    HETEROANNELATED ANTHRAQUINONE衍生物及其合成方法

    公开(公告)号:US20090253707A1

    公开(公告)日:2009-10-08

    申请号:US12193564

    申请日:2008-08-18

    Applicant: Hsu-Shan HUANG

    Inventor: Hsu-Shan HUANG

    Abstract: A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1=n=12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.

    Abstract translation: 提供了杂化蒽醌衍生物化合物。 异构化蒽醌衍生物化合物由式(I)表示:其中R 1是选自以下的一个取代基:i)第一个取代基是选自由羟基,氨基,硝基 (CH 2)n X,直链(CH 2)n烷基,(CH 2)n烷氧基,支链(CH 2)n)烷基, 烷基,C 3〜C 12环烷基和C 3〜C 12环烷氧基,其中1 = n = 12,X为卤素,iii)第三取代基为选自直C1-C8 具有双键的烷基,具有双键的C1〜C8烷氧基,具有双键的支链C1〜C8烷基和具有双键的C3〜C8环状基团,以及iv)第四 C5〜C12杂环基的取代基。

    Synthesis and pharmaceuticals of novel bis-substituted anthraquinone derivatives
    8.
    发明申请
    Synthesis and pharmaceuticals of novel bis-substituted anthraquinone derivatives 审中-公开
    新型双取代蒽醌衍生物的合成和药物

    公开(公告)号:US20050009924A1

    公开(公告)日:2005-01-13

    申请号:US10615695

    申请日:2003-07-08

    Applicant: Hsu-Shan Huang

    Inventor: Hsu-Shan Huang

    Abstract: This invention relates to novel anthraquinone compounds useful in the treatment of allergic, inflammatory conditions, antioxidant, tumor condition, stem cell application, tissue engineering, applied in treating age-associate tissue degeneration, reverse organ failure in chronic high-turnover disease and therapeutic compositions containing such compounds. The compounds of the present invention are 1,4-, 1,5- and 1,8-difunctionalized anthraquinones or analogs thereof. According to the practice of the invention, there are provided bis-symmetrical substituted anthraquinone compounds according to formula I: wherein R1, R2, R3 and R4 present a straight, aminoalkylamino side chains or branched chain alkyl group having 1 to 6 carbons which may be substituted with one or more groups of R5, or R1, R2, R3 and R4 present phenyl or benzyl which may be substituted with one or two groups of R6; wherein R5 is selected from the group consisting of halogen, —RNH2, —RNH2R, —ROH, —NO2, —OCH3, —OCH2CH3, and —OCH2CH2CH3; and wherein R6 is selected from the group consisting of a straight or branched chain alkyl group having 1 to 4 carbons, halogen, —RNH2, —RNH2R, —ROH, —NO2, —OCH3, —OCH2CH3, —OCH2CH2CH3, —CH2Br, —CH2Cl, —CH2OH, —C(CH3)3, —(CH2)20H, —(CH2)3OH, —(CH2)4OH, —CH2NH2, —(CH2)2NH2, —(CH2)3NH2, —(CH2)4NH2, —(CH2)5NH2, —CH2N(CH3)2, —(CH2)2N(CH3)2, —(CH2)2NH(CH2)2OH, —(CH2)3NH(CH2)2OH, —(CH2)2NHCH2OH, —(CH2)3NHCH2OH, —CH2CH(CH3)2, —CHCl2, —CH(CH3)Cl, —(CH2)2Cl, —(CH2)3Cl, —(CH2)3Br, —(CH2)4Br, and —(CH2)4Cl. Chart 1. Activation of hTERT promoter-driven SEAP expression by c-Myc. About 1×107 hTERT-BJ1 cells were transfected with 13.5 μg each of plasmid pSEAP or pPhTERT-SEAP and of plasmid pMT2T or pMT2T-cMyc by electroporation. After 24 h, viable cells were harvested, and reinoculated at a density of 3×105/mL, and the SEAP activity after 24 h at 37 □. The transfection efficiency of each experiment was determined by cotransfection with 1.5 μg of plasmid pCMVβ. The values were determined from three experiments. P

    Abstract translation: 本发明涉及可用于治疗变应性,炎性病症,抗氧化剂,肿瘤状况,干细胞应用,组织工程,用于治疗年龄 - 关联组织变性,慢性高转化病症中的逆转器官衰竭和治疗组合物的新型蒽醌化合物 含有这些化合物。 本发明的化合物是1,4-,1,5-和1,8-二官能化蒽醌或其类似物。 根据本发明的实践,提供了根据式I的双对称取代蒽醌化合物:其中R 1,R 2,R 3和R 4具有直链,氨基烷基氨基侧链或具有1至6个碳的支链烷基,其可以是 被一个或多个R 5基团取代,或R 1,R 2,R 3和R 4表示可被一个或两个R 6基团取代的苯基或苄基; 其中R5选自卤素,-RNH2,-RNH2R,-ROH,-NO2,-OCH3,-OCH2CH3和-OCH2CH2CH3; 并且其中R 6选自具有1至4个碳的直链或支链烷基,卤素,-RNH 2,-RNH 2 R,-ROH,-NO 2,-OCH 3,-OCH 2 CH 3,-OCH 2 CH 2 CH 3,-CH 2 Br, - CH 2 Cl,-CH 2 OH,-C(CH 3)3, - (CH 2)20 H, - (CH 2)3 OH, - (CH 2)4 OH,-CH 2 NH 2, - (CH 2)2 NH 2, - (CH 2)3 NH 2, - (CH 2) , - (CH 2)5 NH 2,-CH 2 N(CH 3)2, - (CH 2)2 N(CH 3)2, - (CH 2)2 NH(CH 2)2 OH, - (CH 2)

    Synthesis of 1,8-dichloro-anthracene analogues and pharmaceutical compositions based thereon
    9.
    发明授权
    Synthesis of 1,8-dichloro-anthracene analogues and pharmaceutical compositions based thereon 失效
    1,8-二氯 - 蒽类似物的合成和基于其的药物组合物

    公开(公告)号:US06372785B1

    公开(公告)日:2002-04-16

    申请号:US09563915

    申请日:2000-05-04

    Applicant: Hsu-Shan Huang

    Inventor: Hsu-Shan Huang

    Abstract: The invention provides novel anthracene compounds useful in the treatment of allergic, inflammatory, and tumor conditions and therapeutic compositions containing such compounds or their pharmaceutically acceptable salts. The compounds of the invention are novel 1,8-dichloro-anthracene derivatives or analogs thereof. According to the practice of the invention, there are provided 9-substituted 1,8-dichloro-anthracene compounds of the Formula III: wherein R represents a straight or branched chain alkyl group having 1-6 carbons and may be substituted with one or more of the groups R1, wherein R1 represents the groups selected from COOH or an ester alky thereof having 1 to 4 carbons, —OH, halogen, NO2, CH3O, CH3CH2O, phenyl and CH3CH2CH2O. Alternatively, R may be phenyl, benzyl, or phenyl or benzyl substituted with one or more groups R2, wherein R2 represents the a group select from a straight or branched chain alkyl group having 1 to 4 carbon atoms, halogen, NO2, CH3O, CH3CH2O, CH3CH2CH2O and an ester alkyl having an alkyl group of 1 to 4 carbon atoms.

    Abstract translation: 本发明提供了可用于治疗过敏性,炎性和肿瘤病症的新型蒽化合物和含有这些化合物或其药学上可接受的盐的治疗组合物。 本发明的化合物是新颖的1,8-二氯 - 蒽衍生物或其类似物。 根据本发明的实践,提供了式III的9-取代的1,8-二氯 - 蒽化合物:其中R表示具有1-6个碳原子的直链或支链烷基,并可被一个或多个 的基团R 1,其中R 1表示选自COOH或其具有1至4个碳的酯基的基团,-OH,卤素,NO 2,CH 3 O,CH 3 CH 2 O,苯基和CH 3 CH 2 CH 2 O. 或者,R可以是苯基,苄基或被一个或多个基团R 2取代的苯基或苄基,其中R 2表示选自具有1至4个碳原子的直链或支链烷基的基团,卤素,NO 2,CH 3 O,CH 3 CH 2 O CH 3 CH 2 CH 2 O和具有1至4个碳原子的烷基的酯烷基。

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