COMBINATION OF BRAF AND VEGF INHIBITORS
    21.
    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.

    MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES
    23.
    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。

    FLUORINATED COATINGS
    25.
    发明申请

    公开(公告)号:WO2007081554A3

    公开(公告)日:2007-07-19

    申请号:PCT/US2006/049333

    申请日:2006-12-27

    Inventor: KUMAR, Rakesh

    Abstract: Conformal coatings are disclosed. A fluorinated thin film, for example, is formed by vapor phase polymerization on a variety of sensitive surfaces that may include electronic and automotive sensors, biochips, implantable sensors and biomedical devices.

    PROCESS FOR PREPARING POLYFURFURYL ALCOHOL PRODUCTS
    29.
    发明申请
    PROCESS FOR PREPARING POLYFURFURYL ALCOHOL PRODUCTS 审中-公开
    制备聚氨酯酒精产品的方法

    公开(公告)号:WO2012123902A1

    公开(公告)日:2012-09-20

    申请号:PCT/IB2012/051201

    申请日:2012-03-14

    CPC classification number: C08L71/14

    Abstract: A process for producing a polyfurfuryl alcohol product includes mixing furfuryl alcohol (FA) and a catalyst component capable of catalyzing a condensation reaction of FA to polyfurfuryl alcohol (PFA). The mixing is effected at a temperature T mix , where T mix 1 , where T 1 > T mix and 50°C 1 for a period of time t 1 , where t 1 is sufficiently long for polymerization to take place and for the polymerized product that is formed to set. The polymerized product is heated to T 2 , where 90°C 2 2 for a period of time t 2 , where 0.5h 2 3 , where 150°C 3 3 for a period of time t 3 , where 0.5h 3

    Abstract translation: 制备聚糠醇产物的方法包括混合糠醇(FA)和能够催化FA与聚糠醇(PFA)的缩合反应的催化剂组分。 混合在温度Tmix,Tmix1,其中T1> Tmix和50℃C1的时间t1进行,其中t1足够长以进行聚合,并且对于形成的聚合产物进行设定。 将聚合的产物加热至T2,其中在90℃下加热一段时间t2,其中0.5h23,其中150℃33一段时间t3,其中0.5h 3 <2h,用于进一步固化聚合产物。

    COMBINATION
    30.
    发明申请
    COMBINATION 审中-公开
    组合

    公开(公告)号:WO2011146710A1

    公开(公告)日:2011-11-24

    申请号:PCT/US2011/037141

    申请日:2011-05-19

    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 N-{3-Chloro-4-[(3- fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4- quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(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, 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,其包括给予N- {3-氯-4 - [(3-氟苄基)氧基]苯基} -6- [5 - ({[2-(甲磺酰基)乙基]氨基 }甲基)-2-呋喃基] -4-喹唑啉胺或其药学上可接受的水合物和/或盐和N - {(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。

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