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31. 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。

32. 发明授权

US5977115A Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US5977115A
公开(公告)日：1999-11-02
申请号：US973624
申请日：1997-12-04
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , A61K31/495 , C07D295/12
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译： PCT No.PCT / US96 / 09425 Sec。 371 1997年12月4日第 102（e）1997年12月4日PCT PCT 1996年6月6日PCT公布。出版物WO96 / 40136 日期：1996年12月19日本发明涉及某些新型化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

33. 发明授权

US5661163A Alpha-1a adrenergic receptor antagonists 失效
标题翻译： α-1a肾上腺素受体拮抗剂
公开(公告)号：US5661163A
公开(公告)日：1997-08-26
申请号：US488272
申请日：1995-06-07
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , C07D211/36
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

34. 发明申请

US20120283231A1 Delivery Of Corticosteroids Through Iontophoresis 审中-公开
标题翻译：通过离子电渗法递送皮质类固醇
公开(公告)号：US20120283231A1
公开(公告)日：2012-11-08
申请号：US13469481
申请日：2012-05-11
申请人： Mike Jaffe , Gary Cook , Perry Calias , Michael A. Patane
发明人： Mike Jaffe , Gary Cook , Perry Calias , Michael A. Patane
IPC分类号： A61K31/573 , A61P27/02 , A61P29/00
CPC分类号： A61K9/0048 , A61F9/0008 , A61K9/0009 , A61K31/573 , A61K41/00 , A61N1/044 , A61N1/0448 , A61N1/303
摘要： Disclosed herein are formulations of dexamethasone or a prodrug thereof suitable for delivery by ocular iontophoresis and methods of use thereof.
摘要翻译：本文公开了适合通过眼部离子电渗疗法递送的地塞米松或其前药的制剂及其使用方法。

35. 发明申请

US20100204159A1 ORGANIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：US20100204159A1
公开(公告)日：2010-08-12
申请号：US12440139
申请日：2007-09-11
申请人： Trixl Brandl , Sylvain Cottens , Claus Ehrhardt , Jiping Fu , Subramanian Karur , David Thomas Parker , Michael A. Patane , Prakash Raman , Stefan Andreas Randl , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic
发明人： Trixl Brandl , Sylvain Cottens , Claus Ehrhardt , Jiping Fu , Subramanian Karur , David Thomas Parker , Michael A. Patane , Prakash Raman , Stefan Andreas Randl , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic
IPC分类号： A61K38/06 , C07D417/14 , A61P31/14 , A61K38/05 , C07K5/083
CPC分类号： C07D417/14 , C07D401/12 , C07D419/14 , C07K5/06078 , C07K5/0808 , C07K5/0823 , C12N2770/24211
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

36. 发明授权

US06943156B2 Dibenzoxazepine αv integrin receptor antagonist 失效
标题翻译：二苯并氮杂吖嗪整合素受体拮抗剂
公开(公告)号：US06943156B2
公开(公告)日：2005-09-13
申请号：US10415032
申请日：2001-10-19
申请人： Michael A. Patane
发明人： Michael A. Patane
IPC分类号： A61K31/00 , A61K31/553 , A61K31/66 , A61K31/661 , A61K45/00 , A61K45/06 , A61P3/10 , A61P19/02 , A61P19/10 , A61P35/00 , A61P35/04 , A61P43/00 , C07D471/04 , C07D267/16
CPC分类号： C07D471/04 , A61K31/00 , A61K31/553 , A61K31/66 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an αv integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors αvβ3 and αvβ5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artheroscietosis, inflammatory arthritis, cancer and metastatic tumor growth.
摘要翻译：本发明涉及一种新的二苯并氮杂衍生物，其合成及其作为αphA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αphavbeta3和alphavbeta5的拮抗剂，可用于抑制骨吸收，治疗和/或预防骨质疏松症，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，炎症关节炎，癌症和转移性肿瘤生长。

37. 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。

38. 发明授权

US06472403B2 &agr;V integrin receptor antagonists 失效
标题翻译： αV整联蛋白受体拮抗剂
公开(公告)号：US06472403B2
公开(公告)日：2002-10-29
申请号：US09766148
申请日：2001-01-19
申请人： Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Aiwen Li , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Jiabing Wang , Michael A. Patane
发明人： Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Aiwen Li , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Jiabing Wang , Michael A. Patane
IPC分类号： A61K3144
CPC分类号： C07D213/73 , A61K45/06 , C07D401/14 , C07D405/14 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel imidazolidinone 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, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及其新颖的咪唑啉酮衍生物，其合成及其作为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α2和/或阿尔巴博5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，炎症性关节炎，病毒性疾病，癌症和转移性肿瘤生长。

39. 发明授权

US06376503B1 Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US06376503B1
公开(公告)日：2002-04-23
申请号：US09097947
申请日：1998-06-17
申请人： Michael A. Patane , Mark G. Bock , Randall C. Newton , Bharat Lagu
发明人： Michael A. Patane , Mark G. Bock , Randall C. Newton , Bharat Lagu
IPC分类号： A61K31513
CPC分类号： C07D401/12 , C07D211/58 , C07D265/32 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/04 , C07D491/10
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
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α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

40. 发明授权

US06172066B2 Dihydropyrimidines and uses thereof 失效
标题翻译：二氢嘧啶及其用途
公开(公告)号：US06172066B2
公开(公告)日：2001-01-09
申请号：US08858061
申请日：1997-05-16
申请人： Dhanapalan Nagarathnam , Wai C. Wong , Shou Wu Miao , Michael A. Patane , Charles Gluchowski
发明人： Dhanapalan Nagarathnam , Wai C. Wong , Shou Wu Miao , Michael A. Patane , Charles Gluchowski
IPC分类号： A61K31497
CPC分类号： C07D239/22
摘要： This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为人α1A受体的选择性拮抗剂的二氢嘧啶化合物。本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及治疗任何α1A受体拮抗作用的疾病的用途可能是有用的本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

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