IMMUNOMODULATORY COMPOSITIONS AND METHODS OF USE THEREOF
    1.
    发明申请
    IMMUNOMODULATORY COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
    免疫组化及其使用方法

    公开(公告)号:WO2017033123A1

    公开(公告)日:2017-03-02

    申请号:PCT/IB2016/055016

    申请日:2016-08-22

    CPC classification number: A61K35/74

    Abstract: The present disclosure provides immunomodulatory compositions comprising live Caulobacter crescentus (CC). Immunomodulatory compositions of the present disclosure are useful for modulating an immune response in an individual. The present disclosure thus provides methods of modulating an immune response in an individual, involving administering an immunomodulatory composition comprising live CC to the individual.

    Abstract translation: 本公开提供包含活细弧新月牙(CC)的免疫调节组合物。 本公开的免疫调节组合物可用于调节个体的免疫应答。 本公开因此提供了调节个体的免疫应答的方法,包括向个体施用包含活CC的免疫调节组合物。

    COMBINATION
    3.
    发明申请
    COMBINATION 审中-公开
    组合

    公开(公告)号:WO2012106302A1

    公开(公告)日:2012-08-09

    申请号:PCT/US2012/023261

    申请日:2012-01-31

    Abstract: The present invention relates to a method of treating breast cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a breast cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and (S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7] indolizino [1,2-b]quinoline-3,14-(4H,12H)-dione, or a pharmaceutically acceptable salt thereof, to a human in need thereof.

    Abstract translation: 本发明涉及治疗人类乳腺癌的方法和用于治疗的药物组合物。 特别地,该方法涉及一种乳腺癌治疗方法,其包括施用5 - [[4 - [(2,3-二甲基-2H-吲唑-6-基)甲基氨基] -2-嘧啶基]氨基] -2-甲基苯磺酰胺 ,或其药学上可接受的盐,和(S)-10 - [(二甲基氨基)甲基] -4-乙基-4,9-二羟基-1H-吡喃并[3',4':6,7]吲哚并[ 2-b]喹啉-3,14-(4H,12H) - 二酮或其药学上可接受的盐。

    COMBINATION
    4.
    发明申请
    COMBINATION 审中-公开
    组合

    公开(公告)号:WO2012097021A1

    公开(公告)日:2012-07-19

    申请号:PCT/US2012/020863

    申请日:2012-01-11

    Inventor: KUMAR, Rakesh

    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and /\/-{(1 S )-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1 - methyl-1 H -pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof.

    Abstract translation: 本发明涉及一种治疗人类癌症的方法和用于治疗的药物组合物。 特别地,该方法涉及一种癌症治疗方法,其包括施用蛋白酶体抑制化合物和/或 - ((1S)-2-氨基-1 - [(3-氟苯基)甲基]乙基} -5-氯 - 4-(4-氯-1-甲基-1H-吡唑-5-基)-2-噻吩甲酰胺或其药学上可接受的盐和任选的另外的抗肿瘤药物。

    COMBINATION OF BRAF AND VEGF INHIBITORS
    6.
    发明申请

    公开(公告)号:WO2012036919A3

    公开(公告)日:2012-03-22

    申请号:PCT/US2011/050302

    申请日:2011-09-02

    Inventor: KUMAR, Rakesh

    Abstract: A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H- indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-{3-[5- (2-Amino-4-pyrimidinyl)-2-(1,1 -dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6- difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial.

    COMBINATION OF BRAF AND VEGF INHIBITORS
    7.
    发明申请
    COMBINATION OF BRAF AND VEGF INHIBITORS 审中-公开
    BRAF和VEGF抑制剂的组合

    公开(公告)号:WO2012036919A2

    公开(公告)日:2012-03-22

    申请号:PCT/US2011050302

    申请日:2011-09-02

    Inventor: KUMAR RAKESH

    Abstract: A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H- indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-{3-[5- (2-Amino-4-pyrimidinyl)-2-(1,1 -dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6- difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial.

    Abstract translation: 包含VEGFR抑制剂5 - [[4 - [(2,3-二甲基-2H-吲唑-6-基)甲基氨基] -2-嘧啶基]氨基] -2-甲基苯磺酰胺或其药学上可接受的盐的新型组合, 与B-Raf抑制剂,特别是N- {3- [5-(2-氨基-4-嘧啶基)-2-(1,1-二甲基乙基)-1,3-噻唑-4-基] -2-氟苯基 } -2,6-二氟苯磺酰胺或其药学上可接受的盐,包含其的药物组合物以及在治疗其中抑制VEGFR和/或B-Raf有益的条件下使用这些组合和组合物的方法。

    MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES
    9.
    发明申请
    MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES 审中-公开
    微波诱导的单步绿色合成一些新型二芳基醛及其类似物

    公开(公告)号:WO2010097811A1

    公开(公告)日:2010-09-02

    申请号:PCT/IN2010/000110

    申请日:2010-02-25

    Abstract: The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N- iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1min- 30min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55 %, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2- diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.

    Abstract translation: 本发明提供了制备一些新的2-芳基和2,2-二芳基醛和类似物的方法,它们是商业上重要的非甾体抗炎药物的特权中间体,包括萘普生,氟比洛芬和有效的抗癌药物候选物,包括通过 利用芳基烯烃形式的容易获得的底物以及以水和DMSO或二恶烷的混合物和二恶烷的溶剂形式的环境友好的水性反应条件的独特的单步合成方法和试剂N-溴代琥珀酰亚胺,N-碘代琥珀酰亚胺,N-氯代琥珀酰亚胺 和相转移催化剂如十六烷基三甲基溴化铵,N-己基氯化铵,反应时间根据微波或常规加热反应时间为1min-30min,而不使用昂贵的过渡金属催化剂或路易斯酸/碱,产率从35-55 取决于所用的溶剂和底物。 开发的方法提供了一种干净和方便的替代方案,用于获得各种各样的药物重要的2-芳基和2,2-二芳基醛基支架,代替采用昂贵且危险的过渡金属催化剂和路易斯酸/碱的常规多步骤方案。

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