公开(公告)号：US08383832B2

公开(公告)日：2013-02-26

申请号：US13229459

申请日：2011-09-09

Applicant: John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

Inventor： John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

IPC: C07D235/04 ,  C07D403/02 ,  C07D235/18

CPC classification number: C07D235/06 ,  C07C201/08 ,  C07C205/58 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18 ,  C07C229/60

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ib-1的苯并咪唑羧酸核心结构：其中Z，X1，X2，X5，R2b和R10如本文所定义。 式Ib-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：US08362037B2

公开(公告)日：2013-01-29

申请号：US12532374

申请日：2008-03-19

Applicant: Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

IPC: A61K31/445 ,  C07D417/14

CPC classification number: C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04

Abstract: Provided are compounds 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: 提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。 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：US08324257B2

公开(公告)日：2012-12-04

申请号：US12444221

申请日：2007-10-03

Applicant: Kateri Ahrendt ,  Robert Kirk Delisle ,  Jeremy Hans ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Eli M. Wallace ,  Qian Zhao

Inventor： Kateri Ahrendt ,  Robert Kirk Delisle ,  Jeremy Hans ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Eli M. Wallace ,  Qian Zhao

IPC: A01N43/82 ,  A61K31/41 ,  C07D285/08

CPC classification number: C07D285/12 ,  C07D413/06 ,  C07D413/12

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 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各种疾病的方法。

公开(公告)号：US20120258952A1

公开(公告)日：2012-10-11

申请号：US13517938

申请日：2010-12-20

Applicant: Mark Laurence Boys ,  Michael F. Bradley ,  Robert Kirk DeLisle ,  D. David Hennings ,  April L. Kennedy ,  Fredrik P. Marmsater ,  Matthew David Medina ,  Mark C. Munson ,  Bryson Rast ,  James P. Rizzi ,  Martha E. Rodriguez ,  George T. Topalov ,  Qian Zhao

Inventor： Mark Laurence Boys ,  Michael F. Bradley ,  Robert Kirk DeLisle ,  D. David Hennings ,  April L. Kennedy ,  Fredrik P. Marmsater ,  Matthew David Medina ,  Mark C. Munson ,  Bryson Rast ,  James P. Rizzi ,  Martha E. Rodriguez ,  George T. Topalov ,  Qian Zhao

IPC: A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4985 ,  A61K31/541 ,  A61P25/00 ,  A61P19/08 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P9/00 ,  C07D471/04 ,  A61K31/551

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.

Abstract translation: 其中R1，R2，R3，R4和R5具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是cFMS的抑制剂，可用于治疗骨相关疾病，癌症，自身免疫 疾病，炎性疾病，心血管疾病和疼痛。

公开(公告)号：US08278314B2

公开(公告)日：2012-10-02

申请号：US12249421

申请日：2008-10-10

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

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

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

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

Abstract: This invention provides quinazoline analogs of Formula I: where A 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 two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式I的喹唑啉类似物：其中A与双环的5,6,7或8位上的至少一个碳键合，并且该环被至多两个独立的R 3基团取代。 本发明还包括使用式I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：US08268871B2

公开(公告)日：2012-09-18

申请号：US12822066

申请日：2010-06-23

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 ,  C07D417/04

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：US20120208995A1

公开(公告)日：2012-08-16

申请号：US13450885

申请日：2012-04-19

Applicant: Lawrence M. Blatt ,  Scott D. Seiwert ,  Steven W. Andrews ,  Pierre Martin ,  Andreas Schumacher ,  Bradley Barnett ,  C. Todd Eary ,  Robert Kaus ,  Timothy Kercher ,  Weidong Liu ,  Michael Lyon ,  Paul Nichols ,  Bin Wang ,  Tarek Sammakia ,  April Kennedy ,  Yutong Jiang

Inventor： Lawrence M. Blatt ,  Scott D. Seiwert ,  Steven W. Andrews ,  Pierre Martin ,  Andreas Schumacher ,  Bradley Barnett ,  C. Todd Eary ,  Robert Kaus ,  Timothy Kercher ,  Weidong Liu ,  Michael Lyon ,  Paul Nichols ,  Bin Wang ,  Tarek Sammakia ,  April Kennedy ,  Yutong Jiang

IPC: C07D498/18

CPC classification number: C07K5/0806 ,  A61K38/00 ,  A61K38/1793 ,  A61K38/212 ,  A61K38/217 ,  A61K38/2292 ,  A61K38/55 ,  C07D471/04 ,  C07D487/04 ,  C07K5/0804 ,  A61K2300/00

Abstract: The embodiments provide compounds of the general Formulae I through general Formula VIII, 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: 实施方案提供通式I至通式VIII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。

公开(公告)号：US20120208801A1

公开(公告)日：2012-08-16

申请号：US13445749

申请日：2012-04-12

Applicant: George A. Doherty ,  Zachary Jones

Inventor： George A. Doherty ,  Zachary Jones

IPC: A61K31/5513 ,  A61P11/06 ,  A61P37/08 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D243/20

Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US20120202854A1

公开(公告)日：2012-08-09

申请号：US13448689

申请日：2012-04-17

Applicant: George Doherty ,  Adam Cook

Inventor： George Doherty ,  Adam Cook

IPC: A61K31/4402 ,  A61K31/4172 ,  A61K31/381 ,  A61K31/27 ,  C07C317/48 ,  C07D213/78 ,  C07D233/84 ,  C07D333/22 ,  C07C255/59 ,  C07C271/28 ,  A61K31/44 ,  A61K31/195

CPC classification number: C07C311/19 ,  C07C233/75 ,  C07C233/87 ,  C07C235/46 ,  C07C255/57 ,  C07C271/22 ,  C07C307/06 ,  C07C311/06 ,  C07C317/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/10 ,  C07D213/71 ,  C07D213/81 ,  C07D213/82 ,  C07D233/42 ,  C07D333/16 ,  Y02P20/55

Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中R1，R2，R7，R8，R9，R10和A具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US08211920B2

公开(公告)日：2012-07-03

申请号：US12186273

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: C07D213/74 ,  C07D213/75 ,  C07D213/55 ,  C07D213/56 ,  A61K31/4412

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 V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and 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 diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式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以及W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中的过度增生性疾病，如癌症和炎症以及炎性病症。 还公开了使用这些化合物治疗哺乳动物的过度增殖性疾病和炎性病症的方法以及含有这些化合物的药物组合物。