公开(公告)号：US08232402B2

公开(公告)日：2012-07-31

申请号：US12402910

申请日：2009-03-12

申请人： Peter T. Lansbury, Jr. ,  Craig J. Justman ,  Ross A. Fredenburg ,  Robin Kate Meray ,  Mark E. Duggan ,  Peter Lin

发明人： Peter T. Lansbury, Jr. ,  Craig J. Justman ,  Ross A. Fredenburg ,  Robin Kate Meray ,  Mark E. Duggan ,  Peter Lin

IPC分类号： C07D215/38 ,  A61K31/04

CPC分类号： C07F9/65583 ,  C07D215/36 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14

摘要： Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. The treatment including administering to a subject a therapeutically effective amount of an inventive farnesyl transferase inhibitor compound.

摘要翻译： 提供了新的喹啉酮法呢基转移酶抑制剂。 这些新化合物可用于治疗或预防突触核蛋白病，如帕金森病，弥漫性路易体病，多系统萎缩，脑铁浓度紊乱，包括泛酸激酶相关神经变性（如PANK1）或其他神经变性/神经系统疾病 疾病 提供的化合物也可用于治疗增殖性疾病如癌症，以及治疗诸如认知障碍，抑郁和焦虑的神经疾病。 治疗包括向受试者施用治疗有效量的本发明的法呢基转移酶抑制剂化合物。

公开(公告)号：US07507836B2

公开(公告)日：2009-03-24

申请号：US10550968

申请日：2004-03-22

申请人： Mark E. Duggan ,  Craig W. Lindsley ,  David D. Wisnoski

发明人： Mark E. Duggan ,  Craig W. Lindsley ,  David D. Wisnoski

IPC分类号： C07D209/48 ,  C07C233/05 ,  A61K31/40 ,  A61K31/165

CPC分类号： C07D417/12 ,  C07D209/48 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D513/04

摘要： The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及代谢型谷氨酸受体的变构调节剂（包括mGluR5受体）的化合物，它们可用于治疗或预防与谷氨酸能力障碍相关的神经和精神疾病以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US07399764B2

公开(公告)日：2008-07-15

申请号：US10530252

申请日：2003-10-24

申请人： Mark E. Duggan ,  Craig W. Lindsley ,  Zhijian Zhao

发明人： Mark E. Duggan ,  Craig W. Lindsley ,  Zhijian Zhao

IPC分类号： A61K31/50 ,  A61K31/497 ,  C07D241/00 ,  C07D487/00

CPC分类号： A61K31/495 ,  A61K45/06 ,  C07D487/04 ,  C07D495/04

摘要： The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有与被抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代吡嗪部分稠合的五元杂环的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US07223738B2

公开(公告)日：2007-05-29

申请号：US10510069

申请日：2003-04-04

申请人： Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Peter J. Manley ,  Zhicai Wu ,  Zhijian Zhao

发明人： Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Peter J. Manley ,  Zhicai Wu ,  Zhijian Zhao

IPC分类号： A01N43/04 ,  A01N43/58 ,  A01N43/60 ,  A01N43/42 ,  A61K31/70 ,  A61K31/50 ,  A61K31/495 ,  A61K31/52 ,  A61K31/47 ,  C07D487/00 ,  C07D491/00 ,  C07H15/00 ,  C07H17/00 ,  C07H17/02 ,  C09B25/00

CPC分类号： C07D401/10 ,  A61K31/498 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

公开(公告)号：US06211191B1

公开(公告)日：2001-04-03

申请号：US09212510

申请日：1998-12-15

申请人： Mark E. Duggan ,  James J. Perkins ,  Robert S. Meissner

发明人： Mark E. Duggan ,  James J. Perkins ,  Robert S. Meissner

IPC分类号： C07D40306

CPC分类号： C07D471/04 ,  A61K41/00 ,  A61K45/06

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;&ngr;&bgr;3, &agr;&ngr;&bgr;5, and/or &agr;&ngr;&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为整联蛋白受体拮抗剂的用途。 更具体地，本发明的化合物是整联蛋白受体α3，α3，α5和/或α6β6的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，并抑制血管再狭窄，糖尿病性视网膜病变， 黄斑变性，血管生成，动脉粥样硬化，炎症，伤口愈合，病毒性疾病，肿瘤生长和转移。

公开(公告)号：US06066648A

公开(公告)日：2000-05-23

申请号：US212123

申请日：1998-12-15

申请人： Mark E. Duggan ,  Robert S. Meissner ,  James J. Perkins

发明人： Mark E. Duggan ,  Robert S. Meissner ,  James J. Perkins

IPC分类号： A61K31/66 ,  A61K45/06 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A01N43/40

CPC分类号： C07D401/14 ,  A61K31/66 ,  A61K45/06 ,  C07D471/04

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the vitronectin receptors .alpha..nu..beta.3 and/or .alpha..nu..beta.5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.

摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为玻连蛋白受体拮抗剂的用途。 更具体地说，本发明的化合物是玻连蛋白受体αnββ3和/或αnuβ5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性， 血管生成，动脉粥样硬化，炎症，病毒性疾病和肿瘤生长。

公开(公告)号：US6017926A

公开(公告)日：2000-01-25

申请号：US212079

申请日：1998-12-15

申请人： Ben C. Askew ,  Paul J. Coleman ,  Mark E. Duggan ,  Wasyl Halczenko ,  John H. Hutchinson ,  Robert S. Meissner ,  Michael A. Patane ,  Jiabing Wang

发明人： Ben C. Askew ,  Paul J. Coleman ,  Mark E. Duggan ,  Wasyl Halczenko ,  John H. Hutchinson ,  Robert S. Meissner ,  Michael A. Patane ,  Jiabing Wang

IPC分类号： A61K31/66 ,  A61K45/06 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A61K31/435

CPC分类号： C07D401/14 ,  A61K31/66 ,  A61K45/06 ,  C07D471/04

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5 and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.

摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为整联蛋白受体拮抗剂的用途。 更具体地，本发明的化合物是整联蛋白受体αvβ3，αvβ5和/或αvβ6的拮抗剂，并且可用于抑制骨吸收，治疗和预防骨质疏松症和抑制血管再狭窄，糖尿病 视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症，伤口愈合，病毒性疾病和肿瘤生长和转移。