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1. 发明授权

US08648116B2 Derivatives of N-(arylamino) sulfonamides including polymorphs as inhibitors of MEK as well as compositions, methods of use and methods for preparing the same 有权
标题翻译：包括作为MEK抑制剂的多晶型物的N-（芳基氨基）磺酰胺的衍生物以及组合物，使用方法及其制备方法
公开(公告)号：US08648116B2
公开(公告)日：2014-02-11
申请号：US12671287
申请日：2008-07-28
申请人： Jean-Michel Vernier , Colin Edward Rowlings , Jean-Luc Girardet , Stuart Dimock , Barry Quart , Jeffrey N. Miner
发明人： Jean-Michel Vernier , Colin Edward Rowlings , Jean-Luc Girardet , Stuart Dimock , Barry Quart , Jeffrey N. Miner
IPC分类号： A61K31/185 , C07C311/00
CPC分类号： A61K45/06 , A61K31/352 , A61K2300/00
摘要： This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.
摘要翻译：本发明涉及作为MEK的抑制剂的N-（2-芳基氨基）芳基磺酰胺化合物，其包括具有特定的粉末X射线衍射图和/或特异性差示扫描量热分析图的结晶多晶型。本发明还涉及包含本文所述化合物和本文所述化合物和组合物的使用方法的药物组合物，包括用于治疗和/或预防癌症，过度增殖性疾病和炎性病症。本发明还涉及制备本文所述的化合物和组合物的方法。

2. 发明申请

US20110060049A1 DERIVATIVES OF N-(ARYLAMINO) SULFONAMIDES INCLUDING POLYMORPHS AS INHIBITORS OF MEK AS WELL AS COMPOSITIONS, METHODS OF USE AND METHODS FOR PREPARING THE SAME 有权
标题翻译：包括作为组合物的MEK的抑制剂的聚（对甲苯胺）磺酰胺的衍生物，使用方法和制备它们的方法
公开(公告)号：US20110060049A1
公开(公告)日：2011-03-10
申请号：US12671287
申请日：2008-07-28
申请人： Jean-Michel Vernier , Colin Edward Rowlings , Jean-Luc Girardet , Stuart Dimock , Barry Quart , Jeffrey N. Miner
发明人： Jean-Michel Vernier , Colin Edward Rowlings , Jean-Luc Girardet , Stuart Dimock , Barry Quart , Jeffrey N. Miner
IPC分类号： A61K31/18 , A61P35/00 , A61P29/00 , C12N9/99 , C12N5/02
CPC分类号： A61K45/06 , A61K31/352 , A61K2300/00
摘要： This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.
摘要翻译：本发明涉及作为MEK的抑制剂的N-（2-芳基氨基）芳基磺酰胺化合物，其包括具有特定的粉末X射线衍射图和/或特异性差示扫描量热分析图的结晶多晶型。本发明还涉及包含本文所述化合物和本文所述化合物和组合物的使用方法的药物组合物，包括用于治疗和/或预防癌症，过度增殖性疾病和炎性病症。本发明还涉及制备本文所述的化合物和组合物的方法。

3. 发明授权

US09095581B2 Combinations of MEK inhibitors and Raf kinase inhibitors and uses thereof 有权
标题翻译： MEK抑制剂和Raf激酶抑制剂的组合及其用途
公开(公告)号：US09095581B2
公开(公告)日：2015-08-04
申请号：US12956177
申请日：2010-11-30
申请人： Jeffrey N. Miner , Mark S. Chapman , Barry Quart , Alex Adjei , Chunrong Yu
发明人： Jeffrey N. Miner , Mark S. Chapman , Barry Quart , Alex Adjei , Chunrong Yu
IPC分类号： A61K31/4439 , A61K31/18 , A61K31/4412 , A61K45/06
CPC分类号： A61K31/4412 , A61K31/18 , A61K31/44 , A61K31/4439 , A61K31/702 , A61K45/06 , A61N5/10 , A61K2300/00
摘要： This invention concerns combinations of inhibitors of MEK, Raf protein kinases, and other kinases including VEGFR1-3 and PDGFR-β. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer and other hyperproliferative disorders.
摘要翻译：本发明涉及MEK，Raf蛋白激酶和其它激酶（包括VEGFR1-3和PDGFR-＆bgr）的抑制剂的组合。本发明还涉及包含本文所述化合物和本文所述化合物和组合物的使用方法的药物组合物，包括用于治疗和/或预防癌症和其它过度增殖性疾病。

4. 发明申请

US20080031983A1 Method for Treatment of Constipation-Predominant Irritable Bowel Syndrome 有权
标题翻译：便秘治疗优势性肠易激综合征的方法
公开(公告)号：US20080031983A1
公开(公告)日：2008-02-07
申请号：US11741796
申请日：2007-04-30
申请人： Barry Quart , David Rosenbaum
发明人： Barry Quart , David Rosenbaum
IPC分类号： A61K36/47 , A61P1/00
CPC分类号： A61K36/47
摘要： The present invention provides methods for treating constipation-predominant irritable bowel syndrome comprising administering to a patient in need thereof, a polymeric proanthocyanidin composition from a Croton species or Calophyllum species in an amount sufficient to treat constipation-predominant irritable bowel syndrome (c-IBS). Treatment of c-IBS includes the treatment of the constipation component of c-IBS as well as the pain and abdominal discomfort associated with c-IBS. In one embodiment, the polymeric proanthocyanidin compound is crofelemer. The present invention in an alternative embodiment also provides methods for treating alternating constipation-predominant/diarrhea-predominant irritable bowel syndrome.
摘要翻译：本发明提供了治疗便秘型肠易激综合征综合征的方法，其包括向有需要的患者施用足以治疗便秘型肠易激综合征（c-IBS）的来自巴豆种或Calophyllum物种的聚合原花青素组合物，。 c-IBS的治疗包括治疗c-IBS的便秘成分以及与c-IBS相关的疼痛和腹部不适。在一个实施方案中，聚合物原花青素化合物是疏水剂。在替代实施方案中的本发明还提供了治疗交替便秘型/腹泻型肠易激综合征的方法。

5. 发明授权

US08846113B2 Method for treatment of diarrhea-predominant irritable bowel syndrome 有权
标题翻译：治疗腹泻型肠易激综合征的方法
公开(公告)号：US08846113B2
公开(公告)日：2014-09-30
申请号：US13304604
申请日：2011-11-25
申请人： Barry Quart , David Rosenbaum , Thomas Neenan , Robert Blanks
发明人： Barry Quart , David Rosenbaum , Thomas Neenan , Robert Blanks
IPC分类号： A61K36/00 , A61K36/38 , A61K31/365 , A61K31/426 , A61K36/47
CPC分类号： A61K31/353 , A61K9/28 , A61K31/365 , A61K31/426 , A61K36/38 , A61K36/47
摘要： The present invention provides methods for treating diarrhea-predominant irritable bowel syndrome comprising administering to a patient in need thereof, an inhibitor of chloride-ion transport in an amount sufficient to treat diarrhea-predominant irritable bowel syndrome (d-IBS). Treatment of d-IBS includes the treatment of the diarrhea component of d-IBS as well as the pain, abdominal discomfort and other symptoms associated with d-IBS. In one embodiment, the inhibitor of chloride-ion transport is crofelemer.
摘要翻译：本发明提供了治疗腹泻型肠易激综合征综合征的方法，其包括向有需要的患者施用足以治疗腹泻型肠易激综合征（d-IBS）的氯离子转运抑制剂。 d-IBS的治疗包括治疗d-IBS的腹泻成分以及与d-IBS相关的疼痛，腹部不适和其他症状。在一个实施方案中，氯离子转运抑制剂是疏水剂。

6. 发明申请

US20080031984A1 Compositions and Methods for Treating or Preventing Inflammatory Bowel Disease, Familial Adenomatous Polyposis and Colon Cancer 有权
标题翻译：治疗或预防炎性肠病，家族性腺瘤性息肉病和结肠癌的组合物和方法
公开(公告)号：US20080031984A1
公开(公告)日：2008-02-07
申请号：US11741797
申请日：2007-04-30
申请人： Barry Quart
发明人： Barry Quart
IPC分类号： A61K36/47 , A61P1/00
CPC分类号： A61K31/353 , A61K36/185 , A61K36/38 , A61K36/47
摘要： The present invention provides methods for preventing colon cancer by administering, to a patient in need thereof, a polymeric proanthocyanidin composition from a Croton species or Calophyllum species in an amount sufficient to prevent colon cancer, which composition inhibits COX-2. The present invention also provides methods for treating inflammation locally in the intestines comprising administering to a patient in need thereof, a polymeric proanthocyanidin composition from a Croton species or Calophyllum species in an amount sufficient to treat inflammation. In one embodiment, the polymeric proanthocyanidin compound is crofelemer. The present invention in alternative embodiments provides methods for treating pain locally in the intestines and treating inflammatory bowel diseases, such as Crohn's disease and ulcerative colitis, as well as for treating familial adenomatous polyposis (FAP).
摘要翻译：本发明提供了用于预防结肠癌的方法，其中所述组合物抑制COX-2，所述方法通过向有需要的患者施用足以防止结肠癌的量的来自巴豆属物种或Calophyllum物质的聚合原花青素组合物。本发明还提供了在肠中局部治疗炎症的方法，其包括向有需要的患者施用足以治疗炎症的量的来自巴豆种或Calophyllum物质的聚合原花青素组合物。在一个实施方案中，聚合物原花青素化合物是疏水剂。替代实施方案中的本发明提供了用于在肠部局部治疗疼痛并治疗诸如克罗恩病和溃疡性结肠炎的炎症性肠病以及用于治疗家族性腺瘤性息肉病（FAP）的方法。

7. 发明申请

US20120136030A1 COMBINATIONS OF MEK INHIBITORS AND RAF KINASE INHIBITORS AND USES THEREOF 有权
标题翻译： MEK抑制剂和RAF激酶抑制剂的组合及其用途
公开(公告)号：US20120136030A1
公开(公告)日：2012-05-31
申请号：US12956177
申请日：2010-11-30
申请人： Jeffrey MINER , Mark Chapman , Barry Quart , Alex Adjei , Chunrong Yu
发明人： Jeffrey MINER , Mark Chapman , Barry Quart , Alex Adjei , Chunrong Yu
IPC分类号： A61K31/4439 , A61K31/4412 , A61P35/00 , A61K31/18
CPC分类号： A61K31/4412 , A61K31/18 , A61K31/44 , A61K31/4439 , A61K31/702 , A61K45/06 , A61N5/10 , A61K2300/00
摘要： This invention concerns combinations of inhibitors of MEK, Raf protein kinases, and other kinases including VEGFR1-3 and PDGFR-β. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer and other hyperproliferative disorders.
摘要翻译：本发明涉及MEK，Raf蛋白激酶和其它激酶（包括VEGFR1-3和PDGFR-＆bgr）的抑制剂的组合。本发明还涉及包含本文所述化合物和本文所述化合物和组合物的使用方法的药物组合物，包括用于治疗和/或预防癌症和其它过度增殖性疾病。

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