公开(公告)号：US06448250B1

公开(公告)日：2002-09-10

申请号：US09499276

申请日：2000-02-07

申请人： Gary A. DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

发明人： Gary A. DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

IPC分类号： A61K31496

CPC分类号： C07D211/46 ,  C07D211/66 ,  C07D211/96 ,  C07D295/26 ,  C07D309/08 ,  C07D309/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D491/10 ,  Y02P20/582

摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

公开(公告)号：US06372758B1

公开(公告)日：2002-04-16

申请号：US09884548

申请日：2001-06-19

申请人： Gary A DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

发明人： Gary A DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

IPC分类号： A61K314545

CPC分类号： C07D211/46 ,  C07D211/66 ,  C07D211/96 ,  C07D295/26 ,  C07D309/08 ,  C07D309/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D491/10 ,  Y02P20/582

摘要： A sulfamato hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease (mmp) activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

摘要翻译： 公开了特别是抑制基质金属蛋白酶（mmp）活性的氨基磺酸异羟肟酸化合物，其制备方法，可用于那些合成的中间体化合物，以及包括将预期的氨磺酸异羟肟酸化合物 MMP酶抑制有效量与具有与病理基质金属蛋白酶活性相关的病症的宿主。

公开(公告)号：US07067670B2

公开(公告)日：2006-06-27

申请号：US10887450

申请日：2004-07-08

申请人： Terri L. Boehm ,  Deborah A. Mischke ,  Gary A. DeCrescenzo ,  Joseph G. Rico ,  Shashidhar N. Rao ,  Darren J. Kassab ,  Jeffery N. Carroll

发明人： Terri L. Boehm ,  Deborah A. Mischke ,  Gary A. DeCrescenzo ,  Joseph G. Rico ,  Shashidhar N. Rao ,  Darren J. Kassab ,  Jeffery N. Carroll

IPC分类号： C07D401/12 ,  C07D405/14 ,  A61K31/4545

CPC分类号： C07D401/14 ,  C07D211/46 ,  C07D211/66 ,  C07D309/08 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D491/10

摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

公开(公告)号：US06800646B1

公开(公告)日：2004-10-05

申请号：US10262622

申请日：2002-09-30

申请人： Gary A. DeCrescenzo ,  Joseph G. Rico ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Darren J. Kassab ,  Deborah A. Mischke ,  Shashidhar Rao

发明人： Gary A. DeCrescenzo ,  Joseph G. Rico ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Darren J. Kassab ,  Deborah A. Mischke ,  Shashidhar Rao

IPC分类号： A61K314545

CPC分类号： C07D401/14 ,  C07D211/46 ,  C07D211/66 ,  C07D309/08 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D491/10

摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

摘要翻译： 公开了特别是抑制基质金属蛋白酶活性的氨基磺酸异羟肟酸化合物，其制备方法，可用于那些合成的中间体化合物，以及包括将预期的氨基磺酰氨基异羟肟酸化合物施用于MMP抑制有效的治疗方法 相当于具有与病理基质金属蛋白酶活性相关的病症的宿主。

公开(公告)号：US06683093B2

公开(公告)日：2004-01-27

申请号：US09989943

申请日：2001-11-21

申请人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Yvette M. Fobian ,  John N. Freskos ,  Daniel P. Getman ,  Joseph J. McDonald ,  Madeleine H. Li ,  Susan L. Hockerman ,  Carol Pearcy Howard ,  Steve A. Kolodziej ,  Deborah A. Mischke ,  Joseph G. Rico ,  Nathan W. Stehle ,  Michael B. Tollefson ,  William F. Vernier ,  Clara I. Villamil ,  Darren J. Kassab

发明人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Yvette M. Fobian ,  John N. Freskos ,  Daniel P. Getman ,  Joseph J. McDonald ,  Madeleine H. Li ,  Susan L. Hockerman ,  Carol Pearcy Howard ,  Steve A. Kolodziej ,  Deborah A. Mischke ,  Joseph G. Rico ,  Nathan W. Stehle ,  Michael B. Tollefson ,  William F. Vernier ,  Clara I. Villamil ,  Darren J. Kassab

IPC分类号： A61K31445

CPC分类号： C07D401/14 ,  C07D211/66 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/08 ,  C07D335/02 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

摘要翻译： 本发明涉及芳族砜异羟肟酸盐（也称为芳香砜异羟肟酸）及其盐，其特别是倾向于抑制基质金属蛋白酶（也称为基质金属蛋白酶或MMP）活性和/或软骨聚集蛋白聚糖酶活性。 本发明还涉及一种治疗方法，其包括将有效量的MMP抑制和/或聚集蛋白聚糖酶抑制剂的化合物或盐施用于具有（或设置为具有）与MMP相关的病理状况的动物，特别是哺乳动物 活性和/或蛋白聚糖蛋白聚糖酶活性。

公开(公告)号：US06492367B1

公开(公告)日：2002-12-10

申请号：US10084713

申请日：2002-02-26

申请人： Gary A DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

发明人： Gary A DeCrescenzo ,  Joseph G Rico ,  Terri Boehm ,  Jeffery N Carroll ,  Darren J Kassab ,  Deborah A Mischke ,  Shashidhar Rao

IPC分类号： A61K31496

CPC分类号： C07D211/46 ,  C07D211/66 ,  C07D211/96 ,  C07D295/26 ,  C07D309/08 ,  C07D309/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D491/10 ,  Y02P20/582

摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

摘要翻译： 公开了特别是抑制基质金属蛋白酶活性的氨基磺酸异羟肟酸化合物，其制备方法，可用于那些合成的中间体化合物，以及包括将预期的氨基磺酰氨基异羟肟酸化合物施用于MMP抑制有效的治疗方法 相当于具有与病理基质金属蛋白酶活性相关的病症的宿主。

公开(公告)号：US07119203B2

公开(公告)日：2006-10-10

申请号：US10618288

申请日：2003-04-25

申请人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  David L. Brown ,  Jeffery N. Carroll ,  Yiyuan Chen ,  Yvette M. Fobian ,  John N. Freskos ,  Alan F. Gasiecki ,  Margaret L. Grapperhaus ,  Robert M. Heintz ,  Susan L. Hockerman ,  Darren J. Kassab ,  Ish K. Khanna ,  Stephen A. Kolodziej ,  Mark A. Massa ,  Joseph J. McDonald ,  Brent V. Mischke ,  Deborah A. Mischke ,  Patrick B. Mullins ,  Mark A. Nagy ,  Monica B. Norton ,  Joseph G. Rico ,  Michelle A. Schmidt ,  Nathan W. Stehle ,  John J. Talley ,  William F. Vernier ,  Clara I. Villamil ,  Lijuan J. Wang ,  Thomas A. Wynn

发明人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  David L. Brown ,  Jeffery N. Carroll ,  Yiyuan Chen ,  Yvette M. Fobian ,  John N. Freskos ,  Alan F. Gasiecki ,  Margaret L. Grapperhaus ,  Robert M. Heintz ,  Susan L. Hockerman ,  Darren J. Kassab ,  Ish K. Khanna ,  Stephen A. Kolodziej ,  Mark A. Massa ,  Joseph J. McDonald ,  Brent V. Mischke ,  Deborah A. Mischke ,  Patrick B. Mullins ,  Mark A. Nagy ,  Monica B. Norton ,  Joseph G. Rico ,  Michelle A. Schmidt ,  Nathan W. Stehle ,  John J. Talley ,  William F. Vernier ,  Clara I. Villamil ,  Lijuan J. Wang ,  Thomas A. Wynn

IPC分类号： C07D405/14 ,  C07D405/12 ,  A61K31/496

CPC分类号： C07D213/74 ,  C07D211/66 ,  C07D211/96 ,  C07D309/08 ,  C07D335/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D411/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.

摘要翻译： 本发明一般涉及蛋白酶（也称为“蛋白酶”）抑制剂，尤其涉及哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸，其特别是抑制基质金属蛋白酶（也称为“基质金属蛋白酶”或“MMP “）活性和/或蛋白聚糖蛋白聚糖酶活性。 这样的异羟肟酸通常在结构上对应于下式：（其中A 1，A 2，Y，E 1， 2，E 3和R x如本说明书中所定义），并且还包括这些化合物的盐。 本发明还涉及这种异羟肟酸的组合物，用于合成这种异羟肟酸的中间体，制备这种异羟肟酸的方法，以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性相关的病症（特别是病理状态）的方法。

公开(公告)号：US06890928B2

公开(公告)日：2005-05-10

申请号：US10657034

申请日：2003-09-05

申请人： John N. Freskos ,  Yvette M. Fobian ,  Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffrey N. Carroll ,  Gary A. DeCrescenzo ,  Susan L. Hockerman ,  Darren J. Kassab ,  Steve A. Kolodziej ,  Joseph McDonald ,  Deborah A. Mischke ,  Monica B. Norton ,  Joseph G. Rico ,  John J. Talley ,  Clara I. Villamil ,  Lijuan Jane Wang

发明人： John N. Freskos ,  Yvette M. Fobian ,  Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffrey N. Carroll ,  Gary A. DeCrescenzo ,  Susan L. Hockerman ,  Darren J. Kassab ,  Steve A. Kolodziej ,  Joseph McDonald ,  Deborah A. Mischke ,  Monica B. Norton ,  Joseph G. Rico ,  John J. Talley ,  Clara I. Villamil ,  Lijuan Jane Wang

IPC分类号： C07D491/048 ,  A61K31/35 ,  A61K31/351 ,  A61K31/357 ,  A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4355 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P37/06 ,  A61P39/00 ,  A61P43/00 ,  C07D211/66 ,  C07D309/08 ,  C07D309/12 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  C07D401/02

CPC分类号： C07D401/12 ,  A61K31/351 ,  A61K31/41 ,  A61K31/453 ,  A61K31/454 ,  C04B35/632 ,  C07D211/66 ,  C07D309/08 ,  C07D309/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  Y02A50/411

摘要： This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

摘要翻译： 本发明涉及特别是抑制基质金属蛋白酶（也称为“基质金属蛋白酶”或“MMP”）活性和/或软骨聚集蛋白聚糖酶活性的芳香族砜异羟肟酸（包括异羟肟酸盐）及其盐。 本发明还涉及一种预防或治疗方法，其包括将有效量的MMP抑制和/或聚集蛋白聚糖蛋白酶抑制剂的这种化合物或盐施用于动物，特别是哺乳动物，所述动物特别是哺乳动物具有（或处置）具有相关的病理状态 具有MMP和/或蛋白聚糖蛋白聚糖酶活性。

公开(公告)号：US06689794B2

公开(公告)日：2004-02-10

申请号：US10142737

申请日：2002-05-10

申请人： John N. Freskos ,  Yvette M. Fobian ,  Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Susan L. Hockerman ,  Darren J. Kassab ,  Steve A. Kolodziej ,  Joseph McDonald ,  Deborah A. Mischke ,  Monica B. Norton ,  Joseph G. Rico ,  John J. Talley ,  Clara I. Villamil ,  Lijuan Jane Wang

发明人： John N. Freskos ,  Yvette M. Fobian ,  Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Susan L. Hockerman ,  Darren J. Kassab ,  Steve A. Kolodziej ,  Joseph McDonald ,  Deborah A. Mischke ,  Monica B. Norton ,  Joseph G. Rico ,  John J. Talley ,  Clara I. Villamil ,  Lijuan Jane Wang

IPC分类号： A61K31445

CPC分类号： C07D401/12 ,  A61K31/351 ,  A61K31/41 ,  A61K31/453 ,  A61K31/454 ,  C04B35/632 ,  C07D211/66 ,  C07D309/08 ,  C07D309/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  Y02A50/411

摘要： This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.