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1. 发明授权

US07153862B2 αv integrin receptor antagonists 失效
标题翻译： alphav整合素受体拮抗剂
公开(公告)号：US07153862B2
公开(公告)日：2006-12-26
申请号：US10618414
申请日：2003-07-10
申请人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
发明人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
IPC分类号： A61K31/55 , A61K31/505 , C07D471/02 , C07D265/36 , C07D498/02
CPC分类号： C07D213/73 , A61K45/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及其新的链烷酸衍生物，它们的合成及其作为αphav整合素受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体alphavbeta3和/或alphavbeta5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，炎性关节炎，癌症和转移性肿瘤生长。

2. 发明授权

US06784190B2 Integrin receptor antagonists 失效
标题翻译：整合素受体拮抗剂
公开(公告)号：US06784190B2
公开(公告)日：2004-08-31
申请号：US09916977
申请日：2001-07-27
申请人： Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
发明人： Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04
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 &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&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。更具体地说，本发明的化合物是整联蛋白受体alphavbeta3，alphavbeta5和/或alphavbeta6的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松，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。

3. 发明授权

US06232308B1 Bezazepine derivatives as &agr;v integrin receptor antagonists 失效
标题翻译：贝沙西平衍生物作为alphav整合素受体拮抗剂
公开(公告)号：US06232308B1
公开(公告)日：2001-05-15
申请号：US09496525
申请日：2000-02-02
申请人： Ben C. Askew
发明人： Ben C. Askew
IPC分类号： A61K315513
CPC分类号： C07D491/04
摘要： The present invention relates to benzazepine derivatives and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&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：本发明涉及苯并氮杂衍生物及其作为alphav整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体alphavbeta3，alphavbeta5和/或alphavbeta6的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松，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。

4. 发明授权

US06211184B1 Integrin antagonists 失效
标题翻译：整合素拮抗剂
公开(公告)号：US06211184B1
公开(公告)日：2001-04-03
申请号：US09242885
申请日：1999-06-14
申请人： Mark E. Duggan , George D. Hartman , William F. Hoffman , Robert S. Meissner , James J. Perkins , Ben C. Askew , Paul J. Coleman , John J. Hutchinson , Adel M. Naylor-Olsen
发明人： Mark E. Duggan , George D. Hartman , William F. Hoffman , Robert S. Meissner , James J. Perkins , Ben C. Askew , Paul J. Coleman , John J. Hutchinson , Adel M. Naylor-Olsen
IPC分类号： C07D40102
CPC分类号： C07D471/04 , A61K31/4375
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are &agr;v&bgr;3 antagonists, &agr;v&bgr;5 antagonists or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为玻连蛋白受体拮抗剂的用途。本发明的玻连蛋白受体拮抗剂化合物是可用于抑制骨吸收，治疗和预防骨质疏松症，抑制再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症和肿瘤生长的阿尔法博3拮抗剂，阿尔法肽5拮抗剂或双重阿尔法。

5. 发明授权

US6048861A Integrin receptor antagonists 失效
标题翻译：整合素受体拮抗剂
公开(公告)号：US6048861A
公开(公告)日：2000-04-11
申请号：US212082
申请日：1998-12-15
申请人： Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
发明人： Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
IPC分类号： C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04 , C07D519/00 , A61K31/435 , A61K31/44
CPC分类号： C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04
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, 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。更具体地说，本发明的化合物是整联蛋白受体αvβ3，αvβ5和/或αvβ6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。

6. 发明授权

US07393852B2 Piperazine derivatives and methods of use 失效
标题翻译：哌嗪衍生物和使用方法
公开(公告)号：US07393852B2
公开(公告)日：2008-07-01
申请号：US10874086
申请日：2004-06-21
申请人： Jian J. Chen , Ben C. Askew , Kaustav Biswas , Jennifer N. Chau , Derin C. D'Amico , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jiawang Zhu , Christopher H. Fotsch , Aiwen Li , Qingyian Liu , Nobuku Nishimura , Tanya Peterkin , Babak Riahi , Chester Chenguang Yuan , Nianhe Han , Rana Nomak , Kevin Yang
发明人： Jian J. Chen , Ben C. Askew , Kaustav Biswas , Jennifer N. Chau , Derin C. D'Amico , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jiawang Zhu , Christopher H. Fotsch , Aiwen Li , Qingyian Liu , Nobuku Nishimura , Tanya Peterkin , Babak Riahi , Chester Chenguang Yuan , Nianhe Han , Rana Nomak , Kevin Yang
IPC分类号： A61K31/54 , A61K31/4965 , C07D241/04 , C07D265/30 , C07D279/12
CPC分类号： C07D241/08 , C07D243/08 , C07D245/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14
摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

7. 发明申请

US20160137646A1 Novel Compounds and Uses Thereof 有权
标题翻译：新型化合物及其用途
公开(公告)号：US20160137646A1
公开(公告)日：2016-05-19
申请号：US14894214
申请日：2014-05-30
申请人： Ben C. ASKEW , Andrew GOOD , Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , Ben C. Askew , Andrew Good
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
摘要翻译：本发明提供式（I） - （IV）中任一项的新化合物及其药物组合物。还提供了包含粘液穿透的式（I） - （IV）中任一项的化合物及其药物组合物的颗粒（例如纳米颗粒）。本发明还提供了用于使用本发明化合物及其药物组合物用于治疗和/或预防与生长因子信号传导途径的异常或病理性血管生成和/或异常信号传导相关的疾病的方法和试剂盒（例如，血管内皮生长因子 VEGF）），例如增殖性疾病（例如癌症，良性肿瘤，炎症性疾病，自身免疫性疾病）和眼部疾病（例如，黄斑变性，青光眼，糖尿病性视网膜病变，视网膜母细胞瘤，水肿，葡萄膜炎，干眼症，睑炎炎，手术炎症）。

8. 发明申请

US20090054460A1 Piperazine derivatives and methods of use 审中-公开
标题翻译：哌嗪衍生物和使用方法
公开(公告)号：US20090054460A1
公开(公告)日：2009-02-26
申请号：US12008696
申请日：2008-01-11
申请人： Jian J. Chen , Ben C. Askew , Kaustav Biswas , Jennifer N. Chau , Derin C. D'Amico , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jiawang Zhu , Christopher H. Fotsch , Aiwen Li , Qingyian Liu , Nobuku Nishimura , Tanya Peterkin , Babak Riahi , Chester Chenguang Yuan , Nianhe Han , Rana Nomak , Kevin Yang
发明人： Jian J. Chen , Ben C. Askew , Kaustav Biswas , Jennifer N. Chau , Derin C. D'Amico , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jiawang Zhu , Christopher H. Fotsch , Aiwen Li , Qingyian Liu , Nobuku Nishimura , Tanya Peterkin , Babak Riahi , Chester Chenguang Yuan , Nianhe Han , Rana Nomak , Kevin Yang
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D241/08 , C07D243/08 , C07D245/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14
摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

9. 发明授权

US06693101B2 &agr;v integrin receptor antagonists 失效
标题翻译： alphav整合素受体拮抗剂
公开(公告)号：US06693101B2
公开(公告)日：2004-02-17
申请号：US09767471
申请日：2001-01-23
申请人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
发明人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
IPC分类号： A61K3144
CPC分类号： C07D213/73 , A61K45/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及其新的链烷酸衍生物，它们的合成及其作为αphav整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体alphavbeta3和/或alphavbeta5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，炎性关节炎，癌症和转移性肿瘤生长。

10. 发明授权

US06413955B1 Integrin receptor antagonists 失效
标题翻译：整合素受体拮抗剂
公开(公告)号：US06413955B1
公开(公告)日：2002-07-02
申请号：US09677677
申请日：2000-10-02
申请人： Ben C. Askew , Garry R. Smith
发明人： Ben C. Askew , Garry R. Smith
IPC分类号： A61K3155
CPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K45/06 , A61K2300/00
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 integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic 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，本发明的化合物是整联蛋白受体alphavbeta3和/或alphavbeta5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，炎症性关节炎，癌症和转移性肿瘤生长。

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