公开(公告)号：US06326387B1

公开(公告)日：2001-12-04

申请号：US09616539

申请日：2000-07-14

申请人： David M. Armistead

发明人： David M. Armistead

IPC分类号： A61K3144

CPC分类号： A61K31/541 ,  A61K31/38 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K38/185 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.

摘要翻译： 本发明涉及用于刺激神经细胞中神经突生长的方法和药物组合物。 组合物包含神经营养量的结合FK-506结合蛋白（FKBP）的化合物和神经营养因子，例如神经生长因子NGF。 所述方法包括用上述包含FKBP结合化合物的组合物或组合物治疗神经细胞而没有神经营养因子。 本发明的方法可用于促进由疾病或身体创伤引起的神经损伤的修复。

公开(公告)号：US5932600A

公开(公告)日：1999-08-03

申请号：US816764

申请日：1997-03-14

申请人： Jeffrey O. Saunders ,  David M. Armistead ,  Michael C. Badia ,  Randy S. Bethiel ,  Catharine A. Frank ,  Doug Naegele ,  Perry M. Novak ,  David A. Pearlman ,  Steven M. Ronkin

发明人： Jeffrey O. Saunders ,  David M. Armistead ,  Michael C. Badia ,  Randy S. Bethiel ,  Catharine A. Frank ,  Doug Naegele ,  Perry M. Novak ,  David A. Pearlman ,  Steven M. Ronkin

IPC分类号： A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  C07D235/30 ,  C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  A61K31/425 ,  A61K31/42

CPC分类号： C07D263/58 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  C07D235/30 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

公开(公告)号：US20090221612A1

公开(公告)日：2009-09-03

申请号：US12370103

申请日：2009-02-12

申请人： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  David M. Armistead ,  Joseph Raker

发明人： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  David M. Armistead ,  Joseph Raker

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： C07D487/04

摘要： Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

摘要翻译： 在本文中提供了选自由式I表示的化合物的某些化学实体及其药学上可接受的盐及其混合物。 包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 公开了治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法，所述方法包括向所述患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症（例如B细胞淋巴瘤和白血病），自身免疫疾病，炎性疾病，急性炎症反应和过敏性疾病。 治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。

公开(公告)号：US07282504B2

公开(公告)日：2007-10-16

申请号：US11125614

申请日：2005-05-09

申请人： David M. Armistead ,  Jean E Bemis ,  Lucian V DiPietro ,  Stephanie D. Geuns-Meyer ,  Gregory J. Habgood ,  Joseph L. Kim ,  Joseph J. Nunes ,  Vinod F. Patel ,  Leticia M. Toledo-Sherman

发明人： David M. Armistead ,  Jean E Bemis ,  Lucian V DiPietro ,  Stephanie D. Geuns-Meyer ,  Gregory J. Habgood ,  Joseph L. Kim ,  Joseph J. Nunes ,  Vinod F. Patel ,  Leticia M. Toledo-Sherman

IPC分类号： C07D403/04 ,  A61K31/404

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.

摘要翻译： 本发明涉及激酶抑制剂，包含抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包含它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备激酶抑制剂化合物的方法，抑制激酶活性的方法，以及治疗疾病或疾病症状的方法。

公开(公告)号：US06967214B2

公开(公告)日：2005-11-22

申请号：US10351731

申请日：2003-01-23

申请人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

IPC分类号： A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  A61P31/22

CPC分类号： C07D413/12 ,  A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32 ,  Y02P20/55

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及一类新颖的IMPDH抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US06518291B1

公开(公告)日：2003-02-11

申请号：US09395798

申请日：1999-09-14

申请人： Jeffrey O. Saunders ,  David M. Armistead ,  Michael C. Badia ,  Randy S. Bethiel ,  Catherine A. Frank ,  Doug Naegele ,  Perry M. Novak ,  David A. Pearlman ,  Steven M. Ronkin

发明人： Jeffrey O. Saunders ,  David M. Armistead ,  Michael C. Badia ,  Randy S. Bethiel ,  Catherine A. Frank ,  Doug Naegele ,  Perry M. Novak ,  David A. Pearlman ,  Steven M. Ronkin

IPC分类号： A61K31136

CPC分类号： C07D263/58 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  C07D235/30 ,  C07D413/12 ,  C07D417/12 ,  Y02A50/385 ,  Y02A50/389

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

公开(公告)号：US06344465B1

公开(公告)日：2002-02-05

申请号：US08801780

申请日：1997-02-14

申请人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

IPC分类号： A61K31445

CPC分类号： C07D413/12 ,  A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及一类新颖的IMPDH抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US5717092A

公开(公告)日：1998-02-10

申请号：US626259

申请日：1996-03-29

申请人： David M. Armistead ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Jeffrey O. Saunders

IPC分类号： A61K31/00 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/70 ,  A61K31/7008 ,  A61K38/00 ,  A61K38/22 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/60 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D211/06 ,  C07D211/36

CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

摘要： The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.

公开(公告)号：US5665774A

公开(公告)日：1997-09-09

申请号：US027870

申请日：1993-03-08

申请人： David M. Armistead ,  Joshua S. Boger ,  Harold V. Meyers ,  Jeffrey O. Saunders ,  Roger D. Tung

发明人： David M. Armistead ,  Joshua S. Boger ,  Harold V. Meyers ,  Jeffrey O. Saunders ,  Roger D. Tung

IPC分类号： A61K31/34 ,  A61K31/16 ,  A61K31/165 ,  A61K31/341 ,  A61K31/343 ,  A61K31/357 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61P25/02 ,  A61P37/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/34 ,  C07D207/08 ,  C07D207/16 ,  C07D211/60 ,  C07D307/54 ,  C07D317/60 ,  C07D333/24 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07C229/36 ,  C07C229/24

CPC分类号： C07D401/06 ,  C07C233/56 ,  C07C235/34 ,  C07D211/60 ,  C07D317/60 ,  C07D403/06 ,  C07D405/06 ,  Y10S514/885

摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.