公开(公告)号：US07893065B2

公开(公告)日：2011-02-22

申请号：US12186202

申请日：2008-08-05

Applicant: Allison L. Marlow ,  Eli M. Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

Inventor： Allison L. Marlow ,  Eli M. Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

IPC: C07D237/20 ,  A61K31/50 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D213/80 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/46 ,  C07D213/82 ,  C07D215/48 ,  C07D231/56 ,  C07D237/24 ,  C07D237/28 ,  C07D237/32 ,  C07D239/74 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8，R9和W如说明书中所定义。 这些化合物是MEK抑制剂，并且可用于治疗过度增殖性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些化合物治疗哺乳动物中过度增生和炎性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US20100260714A1

公开(公告)日：2010-10-14

申请号：US12824547

申请日：2010-06-28

Applicant: Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

Inventor： Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

IPC: A61K38/21 ,  A61K38/43 ,  A61K33/24 ,  A61K31/704 ,  A61K31/5375 ,  A61K31/513 ,  A61K31/4745 ,  A61K31/454 ,  A61K31/42 ,  A61K31/4184 ,  A61P35/00

CPC classification number: C07D235/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: Disclosed are pharmaceutical compositions comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.

Abstract translation: 公开了包含6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐的药物组合物。 还公开了使用这种组合物抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法。

公开(公告)号：US20100234378A1

公开(公告)日：2010-09-16

申请号：US12438339

申请日：2007-08-21

Applicant: Andrew M. Fryer ,  James Rizzi

Inventor： Andrew M. Fryer ,  James Rizzi

IPC: A61K31/4192 ,  C07D249/04 ,  C07D403/12 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/4439

CPC classification number: C07D249/04 ,  C07D401/12 ,  C07D403/12

Abstract: Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R2, R3, R4, R5, and Y are as defined herein, which are useful in the treatment and/or prevention of MMP mediated diseases and disorders.

Abstract translation: 提供具有式（I）的MMP-2，MMP-3，MMP-9，MMP-12和/或MMP-13抑制剂：其中R2，R3，R4，R5和Y如本文所定义，其是有用的 在治疗和/或预防MMP介导的疾病和病症中。

公开(公告)号：US07795282B2

公开(公告)日：2010-09-14

申请号：US11415455

申请日：2006-05-01

Applicant: Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtli

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtli

IPC: A61K31/41 ,  C07D285/14

CPC classification number: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D497/04 ,  C07F9/65395

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。

公开(公告)号：US20100216989A1

公开(公告)日：2010-08-26

申请号：US12614048

申请日：2009-11-06

Applicant: J. Jeffry Howbert ,  Venkat R. Kusukuntla ,  Alexander Tretyakov ,  Nathan Nielsen ,  Pavel Krasik ,  Ji-Long Jiang ,  Hong Woon Yang

Inventor： J. Jeffry Howbert ,  Venkat R. Kusukuntla ,  Alexander Tretyakov ,  Nathan Nielsen ,  Pavel Krasik ,  Ji-Long Jiang ,  Hong Woon Yang

IPC: C07D403/10

CPC classification number: C07D403/10 ,  C07D223/16

Abstract: The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

Abstract translation: 本公开描述了取代的苯并氮杂衍生物的合成方法。 根据本公开的优选方法允许大规模制备具有低水平金属杂质的苯并氮杂化合物。 在一些实施方案中，根据本公开的优选方法还允许制备苯并氮杂衍生物，而不使用色谱纯化方法，并且比以前使用的制备此类化合物的方法更好的产率。 本文公开的方法可用于合成有机化学以及药物化学。

公开(公告)号：US07777032B2

公开(公告)日：2010-08-17

申请号：US12496973

申请日：2009-07-02

Applicant: Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D239/00 ,  C07D239/70 ,  C07D471/00 ,  C07D487/00

CPC classification number: C07D498/10 ,  C04B35/632 ,  C07D239/94 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

Abstract: This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明涉及式I的喹唑啉类似物：其中A基团与双环的5,6,7或8位上的至少一个碳键合，并且该环被多达三个独立的R 3基团取代。 本发明还包括使用这些化合物作为I型受体酪氨酸激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US20100144751A1

公开(公告)日：2010-06-10

申请号：US12593041

申请日：2008-03-27

Applicant: Fredrik P. Marmsater ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlacter ,  George T. Topalov ,  Joseph P. Lyssikatos

Inventor： Fredrik P. Marmsater ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlacter ,  George T. Topalov ,  Joseph P. Lyssikatos

IPC: A61K31/496 ,  C07D471/04 ,  A61K31/4709 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I): are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class (3) and class (5) receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

Abstract translation: 式（I）化合物：可用于治疗由类（3）和类（5）受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。 本发明的具体化合物也被发现是Pim-1的抑制剂。

公开(公告)号：US20100099713A1

公开(公告)日：2010-04-22

申请号：US12524327

申请日：2008-01-16

Applicant: Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

IPC: A61K31/4439 ,  C07D417/12 ,  A61P3/10 ,  C07D417/14

CPC classification number: C07D495/04 ,  C07D417/14

Abstract: Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供具有式I的化合物或其盐，其中R2，L，R3，R11，D2和R13如本文所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病，例如 糖尿病 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：US20100063053A1

公开(公告)日：2010-03-11

申请号：US12577312

申请日：2009-10-12

Applicant: Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

Inventor： Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

IPC: A61K31/50 ,  C07D213/72 ,  A61K31/44 ,  C07D237/02 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D213/78 ,  C07D209/46 ,  C07D213/80 ,  C07D213/82 ,  C07D215/48 ,  C07D231/56 ,  C07D237/24 ,  C07D237/28 ,  C07D237/32 ,  C07D239/74 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式I和V的化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9，W，X和Y如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US20090297476A1

公开(公告)日：2009-12-03

申请号：US12118624

申请日：2008-05-09

Applicant: SCOTT SEIWERT ,  STEVEN W. ANDREWS ,  LEONID BEIGELMAN ,  LAWRENCE M. BLATT ,  BRAD BUCKMAN ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timonthy S. Kercher ,  Michael A. Lyon ,  Bin Wang

Inventor： SCOTT SEIWERT ,  STEVEN W. ANDREWS ,  LEONID BEIGELMAN ,  LAWRENCE M. BLATT ,  BRAD BUCKMAN ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timonthy S. Kercher ,  Michael A. Lyon ,  Bin Wang

IPC: A61K38/21 ,  C12N9/99 ,  A61K31/7088 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/427 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D217/26 ,  C07D401/12 ,  C07D417/14

Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案提供了通式II的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。