公开(公告)号：WO2005113534A3

公开(公告)日：2006-10-26

申请号：PCT/US2005016507

申请日：2005-05-11

Applicant: SCHERING CORP ,  CHAO JIANHUA ,  TAVERAS ARTHUR G ,  AKI CYNTHIA J ,  LUNDELL DANIEL ,  FINE JAY ,  PRIESTLEY TONY ,  REGGIANI ANGELO

Inventor： CHAO JIANHUA ,  TAVERAS ARTHUR G ,  AKI CYNTHIA J ,  LUNDELL DANIEL ,  FINE JAY ,  PRIESTLEY TONY ,  REGGIANI ANGELO

IPC: C07D333/36 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/427 ,  A61K31/4436 ,  A61P17/06 ,  A61P29/00 ,  A61P35/00 ,  C07D207/34 ,  C07D231/38 ,  C07D275/02 ,  C07D275/03 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D333/36 ,  C07D207/34 ,  C07D207/36 ,  C07D231/38 ,  C07D231/46 ,  C07D275/03 ,  C07D277/54 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

Abstract: The present invention is directed to a compound having the general structure of formula (1) useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.

Abstract translation: 本发明涉及具有式（1）的通式结构的化合物，其可用于治疗，预防或改善CXCR1或CXCR2趋化因子介导的疾病。

公开(公告)号：WO2007139860A3

公开(公告)日：2008-04-03

申请号：PCT/US2007012343

申请日：2007-05-22

Applicant: ALANTOS PHARMACEUTICALS INC ,  BLUHM HARALD ,  SUCHOLEIKI IRVING ,  HOCHGUERTEL MATTHIAS ,  TAVERAS ARTHUR G ,  DENG HONGBO ,  WU XINYUAN ,  VAN VELDHUIZEN JOSHUA ,  GALLAGHER BRIAN M

Inventor： BLUHM HARALD ,  SUCHOLEIKI IRVING ,  HOCHGUERTEL MATTHIAS ,  TAVERAS ARTHUR G ,  DENG HONGBO ,  WU XINYUAN ,  VAN VELDHUIZEN JOSHUA ,  GALLAGHER BRIAN M

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic rnetalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic ADAMTS-4 inhibiting compounds.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环型rnetalloprotease抑制剂化合物。 更具体地，本发明提供了一类新型的异双环ADAMTS-4抑制化合物。

公开(公告)号：WO2007139856A2

公开(公告)日：2007-12-06

申请号：PCT/US2007/012337

申请日：2007-05-22

Applicant: ALANTOS PHARMACEUTICALS, INC. ,  GEGE, Christian ,  KROTH, Heiko ,  STEENECK, Christoph ,  RICHTER, Frank ,  HOCHGUERTEL, Matthias ,  NOLTE, Bert ,  VAN VELDHUIZEN, Joshua ,  ESSERS, Michael ,  GALLAGHER, Brian ,  FEUERSTEIN, Tim ,  ARNDT, Torsten ,  SCHNEIDER, Matthias ,  WU, Xinyuan ,  TAVERAS, Arthur, G. ,  BLUHM, Harald ,  SUCHOLEIKI, Irving ,  BIESINGER, Ralf ,  DENG, Hongbo

Inventor： GEGE, Christian ,  KROTH, Heiko ,  STEENECK, Christoph ,  RICHTER, Frank ,  HOCHGUERTEL, Matthias ,  NOLTE, Bert ,  VAN VELDHUIZEN, Joshua ,  ESSERS, Michael ,  GALLAGHER, Brian ,  FEUERSTEIN, Tim ,  ARNDT, Torsten ,  SCHNEIDER, Matthias ,  WU, Xinyuan ,  TAVERAS, Arthur, G. ,  BLUHM, Harald ,  SUCHOLEIKI, Irving ,  BIESINGER, Ralf ,  DENG, Hongbo

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/02

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地说，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比表现出增加的效力。

公开(公告)号：WO2006128184A3

公开(公告)日：2007-03-08

申请号：PCT/US2006020970

申请日：2006-05-22

Applicant: ALANTOS PHARMACEUTICALS INC ,  STEENECK CHRISTOPH ,  GEGE CHRISTIAN ,  RICHTER FRANK ,  HOCHGUERTEL MATTHIAS ,  FEURSTEIN TIM ,  BLUHM HARALD ,  SUCHOLEIKI IRVING ,  BOER JURGEN ,  WU XINYUAN ,  SCHNEIDER MATTHIAS ,  NOLTE BERT ,  GALLAGHER BRIAN ,  VAN VELDHUIZEN JOSHUA ,  DENG HONGBO ,  ESSERS MICHAEL ,  KROTH HEIKO ,  KIELY ANDREW ,  POWERS TIMOTHY ,  TAVERAS ARTHUR G

Inventor： STEENECK CHRISTOPH ,  GEGE CHRISTIAN ,  RICHTER FRANK ,  HOCHGUERTEL MATTHIAS ,  FEURSTEIN TIM ,  BLUHM HARALD ,  SUCHOLEIKI IRVING ,  BOER JURGEN ,  WU XINYUAN ,  SCHNEIDER MATTHIAS ,  NOLTE BERT ,  GALLAGHER BRIAN ,  VAN VELDHUIZEN JOSHUA ,  DENG HONGBO ,  ESSERS MICHAEL ,  KROTH HEIKO ,  KIELY ANDREW ,  POWERS TIMOTHY ,  TAVERAS ARTHUR G

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/00

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制化合物，其表现出与目前已知的MMP-13抑制剂相关的效力增加。

公开(公告)号：WO2005113534A2

公开(公告)日：2005-12-01

申请号：PCT/US2005/016507

申请日：2005-05-11

Applicant: SCHERING CORPORATION ,  CHAO, Jianhua ,  TAVERAS, Arthur, G. ,  AKI, Cynthia, J. ,  LUNDELL, Daniel ,  FINE, Jay ,  PRIESTLEY, Tony ,  REGGIANI, Angelo

Inventor： CHAO, Jianhua ,  TAVERAS, Arthur, G. ,  AKI, Cynthia, J. ,  LUNDELL, Daniel ,  FINE, Jay ,  PRIESTLEY, Tony ,  REGGIANI, Angelo

IPC: C07D333/36

CPC classification number: C07D333/36 ,  C07D207/34 ,  C07D207/36 ,  C07D231/38 ,  C07D231/46 ,  C07D275/03 ,  C07D277/54 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

Abstract: The present invention is directed to a compound having the general structure of formula (1) useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.

Abstract translation: 本发明涉及具有式（1）的通式结构的化合物，其可用于治疗，预防或改善CXCR1或CXCR2趋化因子介导的疾病。

公开(公告)号：WO2005068460A1

公开(公告)日：2005-07-28

申请号：PCT/US2004/042720

申请日：2004-12-20

Applicant: SCHERING CORPORATION ,  PHARMACOPEIA DRUG DISCOVERY, INC. ,  TAVERAS, Arthur, G. ,  ZHENG, Junying ,  BIJU, Purakkattle, J. ,  YU, Younong ,  CHAO, Jianhua ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J. ,  LAI, Gaifa ,  WU, Minglang

Inventor： TAVERAS, Arthur, G. ,  ZHENG, Junying ,  BIJU, Purakkattle, J. ,  YU, Younong ,  CHAO, Jianhua ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J. ,  LAI, Gaifa ,  WU, Minglang

IPC: C07D417/12

CPC classification number: C07D275/03 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Abstract translation: 公开了式（IA）的新化合物及其药学上可接受的盐和溶剂化物。 D和E是不同的组，其中一个是N，另一个是CR 50。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和心脏再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：WO2010138901A1

公开(公告)日：2010-12-02

申请号：PCT/US2010/036709

申请日：2010-05-28

Applicant: BIOGEN IDEC MA INC ,  PENG, Hairuo ,  CUERVO, Julio, H. ,  ISHCHENKO, Alexey ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LUGOVSKOY, Alexey ,  TALREJA, Tina ,  TAVERAS, Arthur, G. ,  XIN, Zhili

Inventor： PENG, Hairuo ,  CUERVO, Julio, H. ,  ISHCHENKO, Alexey ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LUGOVSKOY, Alexey ,  TALREJA, Tina ,  TAVERAS, Arthur, G. ,  XIN, Zhili

IPC: A01N43/40

CPC classification number: A61K31/435 ,  C07C59/56 ,  C07C59/68 ,  C07C229/34 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/14 ,  C07D211/34 ,  C07D263/26 ,  C07D277/30 ,  C07D295/155

Abstract: Compounds that modulate gamma secretase (e.g., alter the cleavage pattern of gamma secretase) are described herein. Also disclosed are pharmaceutical compositions, methods of modulating the activity of gamma secretase, and methods of treating Alzheimer's Disease using the compounds described herein.

Abstract translation: 本文描述了调节γ-分泌酶（例如，改变γ-分泌酶的切割模式）的化合物。 还公开了药物组合物，调节γ-分泌酶的活性的方法，以及使用本文所述的化合物治疗阿尔茨海默病的方法。

公开(公告)号：WO2010051030A1

公开(公告)日：2010-05-06

申请号：PCT/US2009/005897

申请日：2009-10-30

Applicant: BIOGEN IDEC MA INC. ,  GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

Inventor： GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

IPC: A01N47/10 ,  A61K31/27 ,  A61K31/135

CPC classification number: A61K31/135 ,  A61K31/27 ,  C07C205/26 ,  C07C205/50 ,  C07C217/52 ,  C07C217/60 ,  C07C229/32 ,  C07C271/16 ,  C07D263/38 ,  C07F9/091 ,  C07F9/093 ,  C07F9/653 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S lP receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 这些化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：WO2005075447A1

公开(公告)日：2005-08-18

申请号：PCT/US2005/003414

申请日：2005-01-28

Applicant: SCHERING CORPORATION ,  HU, Mengwei ,  YU, Younong ,  DWYER, Michael ,  TAVERAS, Arthur, G. ,  KIM-MEADE, Agnes ,  YIN, Jianguo ,  FU, Xiaoyong ,  MCALLISTER, Timothy ,  ZHANG, Shuyi ,  KLOPFER, Kevin

Inventor： HU, Mengwei ,  YU, Younong ,  DWYER, Michael ,  TAVERAS, Arthur, G. ,  KIM-MEADE, Agnes ,  YIN, Jianguo ,  FU, Xiaoyong ,  MCALLISTER, Timothy ,  ZHANG, Shuyi ,  KLOPFER, Kevin

IPC: C07D307/52

CPC classification number: C07D307/52

Abstract: The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure (A). These four polymorphic forms, herein referred to as Forms I , II , III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.

Abstract translation: 本发明涉及具有以下化学结构（A）的化合物A的一水合物的四种不同的结晶多晶型物。 这些四种多晶型物，在本文中称为形式I，II，III和IV，作为CXC-趋化因子受体配体是有活性的。 本发明还涉及制剂，治疗方法和这些多晶型物合成方法。

公开(公告)号：WO2005066147A1

公开(公告)日：2005-07-21

申请号：PCT/US2004/042060

申请日：2004-12-16

Applicant: SCHERING CORPORATION ,  PHARMACOPEIA DRUG DISCOVERY, INC. ,  BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

Inventor： BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

IPC: C07D285/10

CPC classification number: C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain ( e.g. , acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).

Abstract translation: 公开了式（IA）的新化合物及其药学上可接受的盐和溶剂化物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式（IA）化合物。