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51. 发明授权

US08937095B2 Anticancer compounds 有权
标题翻译：抗癌化合物
公开(公告)号：US08937095B2
公开(公告)日：2015-01-20
申请号：US13937437
申请日：2013-07-09
申请人： Stephan Karl Zahn , Patrizia Sini , Bojan Bister
发明人： Stephan Karl Zahn , Patrizia Sini , Bojan Bister
IPC分类号： C07D209/14 , C07D209/34
CPC分类号： C07D209/34 , C07D209/14 , C12Q1/6886 , C12Q2600/106 , C12Q2600/156
摘要： The invention describes dual Aurora kinase/MEK inhibitors and their use in therapy.
摘要翻译：本发明描述了双极Aurora激酶/ MEK抑制剂及其在治疗中的用途。

52. 发明申请

US20140256782A1 Opsin-Binding Ligands, Compositions and Methods of Use 有权
标题翻译：组合物和使用方法
公开(公告)号：US20140256782A1
公开(公告)日：2014-09-11
申请号：US14352178
申请日：2012-10-19
申请人： David S. Garvey , Gregory J. Larosa , Jeremy R. Greenwood , Leah L. Frye , Tan Quach , Jamie B. Cote , Judd Berman
发明人： David S. Garvey , Gregory J. Larosa , Jeremy R. Greenwood , Leah L. Frye , Tan Quach , Jamie B. Cote , Judd Berman
IPC分类号： C07C49/443 , C07C233/58 , C07C69/75 , C07C35/32 , C07D307/83 , C07D209/34
CPC分类号： C07D307/83 , C07C35/32 , C07C49/443 , C07C49/553 , C07C69/75 , C07C233/58 , C07C251/44 , C07C2102/24 , C07D209/34 , C07D209/46
摘要： Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
摘要翻译：公开的化合物可用于治疗由生产有毒的视觉循环产物引起的或与生物相关的眼部疾病，其是积聚在眼睛中的视觉循环产物，例如干性成年黄斑变性，以及由突变视蛋白质蛋白质错误折叠引起或与之相关的病症和/或视蛋白蛋白质的错误定位。还描述了这些化合物单独或与其它治疗剂组合的组合物，以及使用这些化合物和/或组合物的治疗方法。还公开了合成这些试剂的方法。

53. 发明申请

US20140031363A1 NMDA Receptor Antagonists for Neuroprotection 审中-公开
标题翻译： NMDA受体拮抗剂用于神经保护
公开(公告)号：US20140031363A1
公开(公告)日：2014-01-30
申请号：US13862647
申请日：2013-04-15
申请人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Scott Myers , Yesim Altas Tahirovic
发明人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Scott Myers , Yesim Altas Tahirovic
IPC分类号： C07D295/088 , C07D213/74 , C07D209/34 , C07D211/52 , C07D215/227 , C07D233/32 , C07C311/08 , C07D263/58
CPC分类号： C07D209/34 , C07C217/20 , C07C235/20 , C07C311/08 , C07D211/52 , C07D213/74 , C07D215/227 , C07D233/32 , C07D233/34 , C07D235/26 , C07D263/58 , C07D295/088
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(═O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
摘要翻译：提供了治疗或预防与NMDA受体活性相关的病症的化合物，药物组合物和方法，包括神经性疼痛，中风，创伤性脑损伤，癫痫以及相关的神经系统事件或神经变性。化合物为通式I，或其药学上可接受的盐，酯，前药或衍生物：其中：（L）k-Ar1为取代或未取代的单或双环芳基或杂芳基; W是键，烷基或烯基; X是键，NR 1或O，并且每个R 1和R 2独立地是H，烷基，烯基或芳烷基，或者R 1和R 2一起形成5-8元环; R 3 -R 6选自某些具体取代基或羰基; Y是键，O，S，SO，SO 2，CH 2，NH，N（烷基）或NHC（= O）; 并且Z是OH，NR 6 R 7，NR 8 SO 2（烷基），NR 8 C（O）NR 6 R 7，NR 8 C（O）O（烷基），NR 8 - 二氢噻唑或NR 8 - 二氢咪唑，或其中Z可与Ar 2融合形成选定的杂环。

54. 发明授权

US08629148B2 Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses 有权
标题翻译：取代的羟吲哚衍生物及其用于治疗加压素依赖性疾病的用途
公开(公告)号：US08629148B2
公开(公告)日：2014-01-14
申请号：US12810561
申请日：2008-12-23
申请人： Wilfried Braje , Astrid Netz , Thorsten Oost , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Andrea Hager-Wernet
发明人： Wilfried Braje , Astrid Netz , Thorsten Oost , Wolfgang Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
IPC分类号： A61K31/496 , A61K31/444 , C07D401/04 , C07D401/14 , C07D209/34
CPC分类号： C07D401/14 , C07D209/34 , C07D401/04
摘要： The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.
摘要翻译：本发明涉及式（I）的新型取代的羟基吲哚衍生物，含有所述衍生物的药物及其用于治疗加压素依赖性疾病的用途。

55. 发明授权

US08623906B2 Carboxy isatin hydrazones and their esters as Shp2 inhibitors 有权
标题翻译：羧基靛红腙及其酯类作为Shp2抑制剂
公开(公告)号：US08623906B2
公开(公告)日：2014-01-07
申请号：US13274699
申请日：2011-10-17
申请人： Jie Wu , Nicholas James Lawrence , Said M. Sebti , Harshani Rithma Lawrence
发明人： Jie Wu , Nicholas James Lawrence , Said M. Sebti , Harshani Rithma Lawrence
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/34 , C07D209/12 , C07D209/40 , C07D215/36
摘要： Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
摘要翻译：蛋白酪氨酸磷酸酶（PTP）Shp2是参与细胞信号传导和调节细胞增殖，分化和迁移的非受体PTP。 Shp2介导参与人类癌症发病机制的激酶活化。高通量筛选鉴定抑制PTP Shp2的化合物。鉴定出几种化合物选择性地抑制Shp2超过Shp1，具有低至亚微摩尔的活性。还公开了抑制细胞中的蛋白质酪氨酸磷酸酶并通过选择性抑制Shp2治疗癌症的方法。

56. 发明申请

US20130281711A1 PROCESS FOR THE PREPARATION OF OXINDOLES AND ORTHO-SUBSTITUTED ANILINES AND THEIR USE AS INTERMEDIATES FOR SYNTHESES 有权
标题翻译：制备氧化物和取代的苯胺的方法及其作为合成中间体的使用
公开(公告)号：US20130281711A1
公开(公告)日：2013-10-24
申请号：US13915898
申请日：2013-06-12
申请人： Bayer CropScience AG
发明人： Mark James Ford , Gunter Karig
IPC分类号： C07D209/34
CPC分类号： C07D209/34 , C07C323/58
摘要： The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above −65° C.In a subsequent process, this compound is further reacted in the presence of an acid catalyst to give the indole of formula (7) or the oxindole of formula (8):
摘要翻译：本发明涉及制备羟吲哚和邻位取代苯胺的方法及其作为合成中间体的用途。本发明还涉及制备式（4）化合物的方法：其中苯胺（式Q化合物）的混合物与硫醚（式W化合物）反应：在氯化剂和在随后的方法中，该化合物在酸催化剂的存在下进一步反应，得到式（7）的吲哚或式（8）的羟吲哚，：

57. 发明授权

US08563749B2 Process for preparing substituted 1,3-dihydro-2H-indol-2-ones 有权
标题翻译：制备取代的1,3-二氢-2H-吲哚-2-酮的方法
公开(公告)号：US08563749B2
公开(公告)日：2013-10-22
申请号：US13103673
申请日：2011-05-09
申请人： Konrad Siegel , Gunter Karig
发明人： Konrad Siegel , Gunter Karig
IPC分类号： C07D209/34
CPC分类号： C07D209/34
摘要： Process for preparing 1,3-dihydro-2H-indol-2-ones, starting from thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds, involving a) dissolving or suspending the thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds in a polar solvent, b) adding a sulfur-containing salt to the solution or suspension, and c) heating the reaction mixture under reflux at a temperature which corresponds at most to the boiling temperature of the solvent. Use of the inventively prepared 1,3-dihydro-2H-indol-2-one as intermediates for the synthesis of fine chemicals and active ingredients from pharmacy and/or agriculture.
摘要翻译：从硫代烷基或硫代环烷基取代的吲哚-2-酮化合物制备1,3-二氢-2H-吲哚-2-酮的方法，包括：a）将硫代烷基 - 或硫代环烷基取代的吲哚-2-酮 - 在极性溶剂中的一种化合物，b）向溶液或悬浮液中加入含硫盐，和c）在相当于溶剂沸点温度的温度下将反应混合物加热回流。使用本发明制备的1,3-二氢-2H-吲哚-2-酮作为合成精细化学品和药物和/或农业的活性成分的中间体。

58. 发明申请

US20130217679A1 Compositions and Methods for Treatment of Neurodegenerative Disease 审中-公开
标题翻译：治疗神经退行性疾病的组合物和方法
公开(公告)号：US20130217679A1
公开(公告)日：2013-08-22
申请号：US13636415
申请日：2011-03-23
申请人： Donald J. Zack , Thomas Bannister , Tomas Vojkovsky , Zhiyong Yang , Cynthia Berlinicke
发明人： Donald J. Zack , Thomas Bannister , Tomas Vojkovsky , Zhiyong Yang , Cynthia Berlinicke
IPC分类号： C07D209/34 , A61K31/55 , A61K31/454 , C07D403/06 , A61K31/496 , C07D453/02 , A61K31/439 , A61K45/06 , A61K31/404 , A61K31/5377
CPC分类号： A61K31/404 , A61K31/439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/34 , C07D403/06 , C07D403/14 , C07D453/02 , C07D495/04 , A61K2300/00
摘要： Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
摘要翻译：公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。

59. 发明授权

US08466190B2 Polymorphic forms of Sunitinib base 失效
标题翻译：舒尼替尼碱的多形态
公开(公告)号：US08466190B2
公开(公告)日：2013-06-18
申请号：US12988173
申请日：2008-04-16
申请人： Srinivasa Krishna Murthy Konduri , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
发明人： Srinivasa Krishna Murthy Konduri , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/4015 , C07D209/34
CPC分类号： C07D403/06
摘要： The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.
摘要翻译：本发明涉及N- [2-（二乙基氨基）乙基] -5 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基）甲基-2' 4-二甲基-1H-吡咯-3-甲酰胺 - 舒尼替尼碱（I）。本发明还涉及制备这种多晶型晶体的方法。

60. 发明申请

US20130131114A1 NOVEL ALKENE OXINDOLE DERIVATIVES 失效
标题翻译：新型碱性氧化物衍生物
公开(公告)号：US20130131114A1
公开(公告)日：2013-05-23
申请号：US13744480
申请日：2013-01-18
申请人： Hoffmann-La Roche Inc.
发明人： Li Chen , Lichun Feng , Mengwei Huang , Jia Li , Fajun Nan , Tao Pang , Lifang Yu , Mei Zhang
IPC分类号： C07D209/34 , C07D401/06 , C07D417/06 , C07D409/06
CPC分类号： C07D417/06 , C07D209/34 , C07D401/06 , C07D409/06
摘要： The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中R 1至R 7具有本文给出的含义。该化合物可用于治疗与AMPK调节相关的疾病的预防。

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