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11. 发明申请

US20150183797A1 NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：新型化合物或其药学上可接受的盐，以及含有作为活性成分的药物组合物
公开(公告)号：US20150183797A1
公开(公告)日：2015-07-02
申请号：US14588804
申请日：2015-01-02
申请人： SNU R&DB FOUNDATION
发明人： Young-Ger SUH , Dong-Jo CHANG , Hongchan AN , Kyu-Won KIM , Young-Myeong KIM , Ho-Young LEE
IPC分类号： C07D493/14 , C07D311/58 , C07D493/04
CPC分类号： C07D493/14 , C07D311/58 , C07D311/74 , C07D493/04 , C07D493/12
摘要： The present invention relates to a compound inhibiting Hsp90 and a pharmaceutical composition comprising the same as an active ingredient. The compounds represented by formula 1 and formula 2 of the present invention suppress the expression of Hsp90 so that they can inhibit the accumulation of HIF-1α, the Hsp90 client protein, and also efficiently inhibit the activation of VEGF. In addition, these compounds display low cytotoxicity, so that they can be effectively used as an active ingredient of an anti-cancer agent, a diabetic retinopathy treating agent, and an anti-arthritic agent.
摘要翻译：本发明涉及一种抑制Hsp90的化合物和一种药物组合物，它包含其作为活性成分。由本发明的式1和式2表示的化合物抑制Hsp90的表达，从而可以抑制HIF-1α，Hsp90客户蛋白的积累，并且还有效抑制VEGF的活化。此外，这些化合物显示低的细胞毒性，因此它们可以有效地用作抗癌剂，糖尿病性视网膜病变治疗剂和抗关节炎剂的活性成分。

12. 发明申请

US20140287037A1 EXTENDED-RELEASE TOPIRAMATE CAPSULES 有权
公开(公告)号：US20140287037A1
公开(公告)日：2014-09-25
申请号：US14157646
申请日：2014-01-17
申请人： Upsher-Smith Laboratories, Inc.
发明人： Sarah Michelle Betterman , Jaidev Srinivas Tantry , Laura Marie Patrick
IPC分类号： A61K9/48 , A61K31/357
CPC分类号： A61K9/50 , A61K9/16 , A61K9/28 , A61K9/2866 , A61K9/4891 , A61K9/5047 , A61K31/357 , A61K31/7048 , C07D311/02 , C07D493/12 , C07D493/14 , Y10S514/963 , Y10S514/964
摘要： An extended-release topiramate capsule that includes a capsule shell containing a single population of coated particles; wherein each coated particle includes a core and a coating thereon; wherein each particle core includes a homogeneous mixture comprising topiramate throughout its core; and wherein the coating includes one or more release controlling agent(s).

13. 发明申请

US20140235876A1 Photochromic Double-Fused Naphthopyrans 有权
标题翻译：光致变色双熔石榴石
公开(公告)号：US20140235876A1
公开(公告)日：2014-08-21
申请号：US14347009
申请日：2012-09-26
申请人： RODENSTOCK GMBH
发明人： Udo Weigand , Herbert Zinner , Yven Rohlfing
IPC分类号： G02B1/04 , C07D493/04 , C07D493/14
CPC分类号： G02B1/041 , C07D493/04 , C07D493/14 , C08K5/156 , C09K9/02 , C09K2211/1088 , G02B5/23
摘要： The present invention relates to photochromic double-fused naphthopyrans of the general formula (I) or (II) and the use thereof in plastics of all kinds, particularly for ophthalmic purposes. The photochromic compounds according to the invention are characterized by two distinct absorption bands of the open form in the visible wavelength range, i.e. two conventional photochromic dyes, each having only one discrete absorption band, can be replaced with dye molecules of this type. The compounds according to the invention, moreover, have a very good lifetime with a very high performance.
摘要翻译：本发明涉及通式（I）或（II）的光致变色双稠合萘并吡喃及其在各种塑料中的用途，特别是用于眼用。根据本发明的光致变色化合物的特征在于在可见光波长范围内的开放形式的两个不同的吸收带，即每个仅具有一个离散吸收带的两个常规光致变色染料可以用这种类型的染料分子代替。此外，根据本发明的化合物具有非常好的寿命，具有非常高的性能。

14. 发明授权

US08664410B2 Fluorescent dye and use thereof 有权
标题翻译：荧光染料及其用途
公开(公告)号：US08664410B2
公开(公告)日：2014-03-04
申请号：US13168288
申请日：2011-06-24
申请人： Pablo Wessig , Kristian Möllnitz , Robert Wawrzinek
发明人： Pablo Wessig , Kristian Möllnitz , Robert Wawrzinek
IPC分类号： C07D317/64 , C07D317/68 , C07D493/04 , C07D493/10 , C07D493/14 , C07K1/13 , C09B57/00 , G01N33/52 , G01N33/533
CPC分类号： C09B57/00 , A61K49/0021 , C07D317/64 , C07D493/04 , C07D493/10 , C07D493/14 , G01N33/52
摘要： The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.
摘要翻译：本发明涉及通式I或II的荧光染料，其中R 1，R 2，R 3和R 4独立地为氢或支链或非支链，饱和或不饱和的脂族或芳族官能取代或未取代的烃基，其中至少一个的R 1或R 2基团中的一个并且R 3或R 4基团之一不是氢，并且式I中的R 1和R 3基团和/或R 2和R 4基团可以彼此桥连，并且X和Y独立地表示取代或未取代的其中任何一个碳单元可被N或S杂原子代替的C 1或C 2烃基。该染料由于其高荧光强度和大的斯托克斯位移结合长荧光寿命而显着。

15. 发明授权

US08507549B2 Methods for synthesizing glycinols, glyceollins I and II and isoflavenes and chromanes using a Wittig reaction, and compositions made therewith 失效
标题翻译：使用维蒂希反应合成大豆醇，甘氨酸I和II以及异亮氨酸和色度的方法，以及由此制成的组合物
公开(公告)号：US08507549B2
公开(公告)日：2013-08-13
申请号：US13346059
申请日：2012-01-09
申请人： Paul W. Erhardt , Rahul S. Khupse , Amarjit Luniwal
发明人： Paul W. Erhardt , Rahul S. Khupse , Amarjit Luniwal
IPC分类号： A61K31/353 , C07D493/04 , C07D493/14 , C07D311/58
CPC分类号： A61K31/353 , C07D311/58 , C07D493/04 , C07D493/14
摘要： Methods for synthesizing glycinols, glyceollins I and II, and isoflavene and chromane compounds using a Wittig reaction, compositions made therewith, and uses thereof are described.
摘要翻译：描述了使用Wittig反应合成大豆醇，glyceollins I和II以及异黄酮和苯并二氢吡喃化合物的方法及其制备方法及其用途。

16. 发明申请

US20130197241A1 CYCLIZATION METHODS 有权
标题翻译：循环方法
公开(公告)号：US20130197241A1
公开(公告)日：2013-08-01
申请号：US13756069
申请日：2013-01-31
申请人： REGENTS OF THE UNIVERSITY OF MINNESOTA
发明人： Thomas R. Hoye , Beeraiah Baire , Dawen Niu , Patrick H. Willoughby , Brian P. Woods
IPC分类号： C07F7/08 , C07D311/94 , C07F7/18
CPC分类号： C07F7/083 , C07D307/88 , C07D311/94 , C07D491/048 , C07D493/04 , C07D493/14 , C07F7/0827 , C07F7/1876 , C07F7/1892
摘要： The invention provides methods for cyclizing poly-yne compounds under mild conditions to provide cyclic compounds.
摘要翻译：本发明提供了在温和条件下环化多元醇化合物以提供环状化合物的方法。

17. 发明授权

US08436155B2 7,2″-dehydrate puerarin and its salts, preparation method and use thereof 有权
标题翻译： 7,2“ - 脱水葛根素及其盐，其制备方法和用途
公开(公告)号：US08436155B2
公开(公告)日：2013-05-07
申请号：US13177575
申请日：2011-07-07
申请人： Hongxiang Lou , Jian Gao , Xia Xue
发明人： Hongxiang Lou , Jian Gao , Xia Xue
IPC分类号： C07H15/00 , C07H17/00 , C07H17/02 , C07H15/04 , C07H1/00 , C07H3/00
CPC分类号： C07D493/14
摘要： A 7,2″-dehydrate puerarin represented by formula (I) and salt derivatives thereof. The compounds are prepared from puerarin by intramolecular mitsunobu reaction. They are capable of shortening arrhythmia duration and prolonging coagulation time. They can be prepared into oral formulations or injections for treatment of cardiovascular and cerebrovascular diseases including arrhythmia, coronary heart disease, angina pectoris, myocardial infarction, and cerebral infarction.
摘要翻译：由式（I）表示的7,2“ - 脱水葛根素及其盐衍生物。该化合物由葛根素通过分子内mitsunobu反应制备。它们能够缩短心律失常持续时间并延长凝血时间。它们可以制备成口服制剂或注射用于治疗心血管和脑血管疾病，包括心律失常，冠心病，心绞痛，心肌梗死和脑梗死。

18. 发明授权

US08367622B2 Sulfated C-glycoside, method for isolating same and method for synthesizing same 失效
标题翻译：硫酸化C-糖苷，其分离方法及其合成方法
公开(公告)号：US08367622B2
公开(公告)日：2013-02-05
申请号：US13143111
申请日：2009-12-25
申请人： Hitoshi Ishida
发明人： Hitoshi Ishida
IPC分类号： A01N43/04 , A61K31/70 , C07H5/02 , C07H1/00 , C07H1/06 , C07H1/08
CPC分类号： C07D407/04 , A61K36/82 , C07D493/14
摘要： Provided are a sulfated C-glycoside which is a novel compound serving as a precursor of chafuroside and chafuroside analogs; a method for efficiently producing the sulfated C-glycoside; and a method for efficiently producing chafuroside and chafuroside analogs using said sulfated C-glycoside. A sulfated C-glycoside represented by general formula (A1) or (B1) [wherein R1, R2 and R3 independently represent each a hydrogen atom or an OH group] is obtained by extracting tea leaves or tea tannins with water, a lower alcohol solvent having 1 to 3 carbon atoms or a liquid mixture comprising the same. Alternatively, the sulfated C-glycoside is produced by reacting a flavone C-glycoside such as isovitexin or vitexin with a sulfate group-introducing agent to thereby sulfate the flavone C-glycoside. By heating the sulfated C-glycoside thus obtained, chafuroside and chafuroside analogs are efficiently produced.
摘要翻译：提供一种硫酸化的C-糖苷，它是一种新的化合物，用作沙夫沙罗和沙夫罗内酯类似物的前体; 一种有效生产硫酸化C-糖苷的方法; 以及使用所述硫酸化C-糖苷有效生产沙非罗非和类胡萝卜素类似物的方法。通过用水，低级醇溶剂萃取茶叶或茶单宁来获得由通式（A1）或（B1）表示的硫酸化C-糖苷[其中R 1，R 2和R 3各自独立地表示氢原子或OH基团] 具有1至3个碳原子或包含该碳原子的液体混合物。或者，硫酸化C-糖苷通过使异黄酮苷或牡荆素等黄酮C糖苷与硫酸酯基导入剂反应从而硫酸化黄酮C-糖苷而制备。通过加热由此获得的硫酸化的C-糖苷，可有效地制备沙夫罗辛和类胡萝卜素类似物。

19. 发明申请

US20130022542A1 RADIOLABELLED ROTENONE DERIVATIVES AND THEIR USE IN SPECT IMAGING 有权
标题翻译：放射性罗丹明衍生物及其在SPECT成像中的应用
公开(公告)号：US20130022542A1
公开(公告)日：2013-01-24
申请号：US13549093
申请日：2012-07-13
申请人： Lihui WEI , Xuxu Yan , Corinne Bensimon , Terrence David Ruddy
发明人： Lihui WEI , Xuxu Yan , Corinne Bensimon , Terrence David Ruddy
IPC分类号： A61K51/04 , C07D493/14
CPC分类号： C07D493/14
摘要： The present application discloses a compound of formula (I) or (II): wherein X is gamma-emitting radionuclide. Also disclosed is a pharmaceutical composition comprising the compound of formula (I), the compound of formula (II), or a mixture thereof, and a physiologically acceptable vehicle and a method of imaging a region in a patient, which includes administering to the patient a diagnostically effective amount of the pharmaceutical composition comprising the compound of formula (I), the compound of formula (II), or a mixture thereof.
摘要翻译：本申请公开了式（I）或（II）的化合物：其中X是发射γ射线的放射性核素。还公开了包含式（I）化合物，式（II）化合物或其混合物的药物组合物和生理学上可接受的载体和对患者的区域成像的方法，其包括向患者施用诊断有效量的包含式（I）化合物，式（II）化合物或其混合物的药物组合物。

20. 发明申请

US20110319639A1 Fluorescent Dye and Use Thereof 有权
标题翻译：荧光染料及其用途
公开(公告)号：US20110319639A1
公开(公告)日：2011-12-29
申请号：US13168288
申请日：2011-06-24
申请人： Pablo Wessig , Kristian MÖLLNITZ , Robert Wawrzinek
发明人： Pablo Wessig , Kristian MÖLLNITZ , Robert Wawrzinek
IPC分类号： C07D493/10 , C07D317/68 , C07D493/04
CPC分类号： C09B57/00 , A61K49/0021 , C07D317/64 , C07D493/04 , C07D493/10 , C07D493/14 , G01N33/52
摘要： The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.
摘要翻译：本发明涉及通式I或II的荧光染料，其中R 1，R 2，R 3和R 4独立地为氢或支链或非支链，饱和或不饱和的脂族或芳族官能取代或未取代的烃基，其中至少一个的R 1或R 2基团中的一个并且R 3或R 4基团之一不是氢，并且式I中的R 1和R 3基团和/或R 2和R 4基团可以彼此桥连，并且X和Y独立地表示取代或未取代的其中任何一个碳单元可被N或S杂原子代替的C 1或C 2烃基。该染料由于其高荧光强度和大的斯托克斯位移结合长荧光寿命而显着。

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