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1. 发明申请

US20050009838A1 Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 失效
标题翻译：哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸及其作为蛋白酶抑制剂的用途
公开(公告)号：US20050009838A1
公开(公告)日：2005-01-13
申请号：US10618288
申请日：2003-04-25
申请人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , David Brown , Jeffery Carroll , Yiyuan Chen , Yvette Fobian , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Robert Heintz , Susan Hockerman , Darren Kassab , Ish Khanna , Stephen Kolodziej , Mark Massa , Joseph McDonald , Brent Mischke , Deborah Mischke , Patrick Mullins , Mark Nagy , Monica Norton , Joseph Rico , Michelle Schmidt , Nathan Stehle , John Talley , William Vernier , Clara Villamil , Lijuan Wang , Thomas Wynn
发明人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , David Brown , Jeffery Carroll , Yiyuan Chen , Yvette Fobian , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Robert Heintz , Susan Hockerman , Darren Kassab , Ish Khanna , Stephen Kolodziej , Mark Massa , Joseph McDonald , Brent Mischke , Deborah Mischke , Patrick Mullins , Mark Nagy , Monica Norton , Joseph Rico , Michelle Schmidt , Nathan Stehle , John Talley , William Vernier , Clara Villamil , Lijuan Wang , Thomas Wynn
IPC分类号： C07D295/22 , A61K31/451 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/08 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P37/02 , A61P39/00 , A61P41/00 , A61P43/00 , C07D211/66 , C07D211/96 , C07D213/74 , 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 , A61K31/445 , C07D211/26
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。这种异羟肟酸通常在结构上对应于下式：（其中A 1，A 2，Y，E 1，E 2，E 3和R x如本说明书），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。

2. 发明申请

US20050209278A1 Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 审中-公开
标题翻译：哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸及其作为蛋白酶抑制剂的用途
公开(公告)号：US20050209278A1
公开(公告)日：2005-09-22
申请号：US10700202
申请日：2003-11-03
申请人： Joseph McDonald , Darren Kassab , Mark Massa , Margaret Grapperhaus , Michelle Schmidt , Joseph Rico , Patrick Mullins , David Brown
发明人： Joseph McDonald , Darren Kassab , Mark Massa , Margaret Grapperhaus , Michelle Schmidt , Joseph Rico , Patrick Mullins , David Brown
IPC分类号： A61K31/452 , C07D211/16 , C07D211/22 , C07D211/66 , C07D211/96 , C07D309/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D45/02
CPC分类号： C07D401/14 , C07D211/66 , C07D211/96 , C07D309/08 , C07D401/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
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。

3. 发明申请

US20060084688A1 Aromatic sulfone hydroxamic acid metalloprotease inhibitor 审中-公开
标题翻译：芳香砜异羟肟酸金属蛋白酶抑制剂
公开(公告)号：US20060084688A1
公开(公告)日：2006-04-20
申请号：US11046645
申请日：2005-01-28
申请人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil
发明人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil
IPC分类号： A61K31/426 , A61K31/421 , A61K31/4166 , A61K31/19
CPC分类号： C07D231/12 , A61K31/19 , A61K31/4166 , A61K31/421 , A61K31/426 , C07C317/44 , C07D207/48 , C07D211/54 , C07D211/66 , C07D211/86 , C07D211/94 , C07D211/96 , C07D225/02 , C07D233/56 , C07D239/04 , C07D249/08 , C07D263/06 , C07D265/06 , C07D279/06 , C07D281/08 , C07D309/08 , C07D309/28 , C07D319/06 , C07D325/00 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
摘要翻译：公开了一种处理方法，其包括施用有效量的显示出一种或多种基质金属蛋白酶（MMP）酶如MMP-2，MMP-9和MMP-13的优异抑制活性的芳香族砜异羟肟酸，同时显示至少对具有与病理基质金属蛋白酶活性相关的病症的宿主的MMP-1的抑制显着降低。施用的酶抑制剂在结构上对应于下式（I）或其药学上可接受的盐，其中R 1和R 2都是氢或R 2， 1和R 2与它们所键合的原子一起形成在环中含有一个，两个或三个杂原子的5-至8-元环，其为氧，硫，或氮气。式（I）中的R 3是任选取代的芳基或任选取代的杂芳基。还公开了具有这些选择活性的金属蛋白酶抑制剂化合物，制备这种化合物的方法和使用抑制剂的药物组合物。

4. 发明授权

US5614788A Automated ambient condition responsive daytime running light system 失效
标题翻译：自动环境条件反应白天行车灯系统
公开(公告)号：US5614788A
公开(公告)日：1997-03-25
申请号：US510092
申请日：1995-08-01
申请人： Patrick Mullins , Charles Benedict , Jay S. Tiedeberg
发明人： Patrick Mullins , Charles Benedict , Jay S. Tiedeberg
IPC分类号： B60Q1/14 , B60Q1/02 , B60Q1/04
CPC分类号： B60Q1/143 , B60Q2300/052 , B60Q2300/312 , B60Q2300/314 , B60Q2400/30
摘要： An automated daytime running light system for surface transport vehicles having headlights and taillights which includes a daytime running light control circuit which activates the highbeam filament of the headlights at a reduced power level whenever the vehicle ignition is ON and the starter motor OFF during daylight conditions. In one embodiment, the daytime running light control circuit activates the high beam filaments of the headlight at a reduced power level and also activates the parking lights to provide taillights whenever the vehicle ignition is ON and the starter motor OFF during daylight conditions. The system further includes a navigational lighting control circuit which is responsive to ambient condition sensor inputs such as low light level sensors, fog or moisture sensors, windshield wiper actuation sensors and the like, to de-activate the daytime running light control circuit and activate the vehicles headlights and taillights and other running lights at normal power levels as long as such sensors are activated or whenever the vehicle headlights are manually activated. The system may further include an emergency brake indicator circuit which turns off the daytime running light and navigational lighting control circuits, and the vehicle headlights and/or taillights controlled thereby, whenever the emergency brake is engaged and may further include an external shut-off circuit for turning off the daytime running light and navigational lighting control circuits, or portions thereof, when activated.
摘要翻译：一种用于地面运输车辆的自动日间行车灯系统，其具有头灯和尾灯，其包括白天行驶的光控制电路，其每当车辆点火开启并且起动电机在日光条件期间断开时，以降低的功率水平激活前灯的高束灯。在一个实施例中，日间行驶光控制电路以降低的功率水平激活前灯的远光灯丝，并且在日光条件期间当车辆点火开启并且起动器电动机关闭时也激活驻车灯以提供尾灯。该系统还包括导航照明控制电路，其响应诸如低光级传感器，雾或湿度传感器，挡风玻璃刮水器致动传感器等的环境条件传感器输入，以去激活白天行驶的光控制电路并激活只要这些传感器被激活，或者当车辆前灯被手动启动时，车辆头灯和尾灯以及其他正常功率水平的行驶灯。该系统可以进一步包括紧急制动指示器电路，其在紧急制动器接合时关闭日间行车灯和导航照明控制电路以及由此控制的车辆前灯和/或尾灯，并且还可以包括外部切断电路用于在激活时关闭日间行车灯和导航照明控制电路或其部分。

5. 发明授权

US07569802B1 Photosensor control unit for a lighting module 失效
标题翻译：用于照明模块的光电传感器控制单元
公开(公告)号：US07569802B1
公开(公告)日：2009-08-04
申请号：US11435020
申请日：2006-05-15
申请人： Patrick Mullins
发明人： Patrick Mullins
IPC分类号： G01J1/32 , H05B37/02
CPC分类号： F21V23/0442 , F21S8/08 , F21W2131/10 , F21W2131/103 , F21Y2115/10 , H01L23/3677 , H01L2924/0002 , H05B37/0218 , Y02B20/46 , H01L2924/00
摘要： A photosensor control unit for use in a lighting module has a light sensor and a switch adapted to operably control a light source such as a plurality of LEDs responsive to the light sensor. The light source is adapted to be mounted in the lighting module, and is configured to produce light having wavelengths within a first range of wavelengths. The light sensor is adapted to be mounted on or about the lighting module, and is responsive to light having wavelengths within a second range of wavelengths. The second range of wavelengths is exclusive of the first range of wavelengths. The switch is adapted to operably control the light source responsive to the light sensor such that the light source emits light having wavelengths within the first range of wavelengths responsive to the presence or absence of light within the second range of wavelengths.
摘要翻译：用于照明模块的光传感器控制单元具有光传感器和适于可操作地控制光源的开关，诸如响应于光传感器的多个LED。光源适于安装在照明模块中，并且被配置为产生波长在第一波长范围内的光。光传感器适于安装在照明模块上或周围，并响应于波长在第二波长范围内的光。第二波长范围不包括第一波长范围。开关适于响应于光传感器可操作地控制光源，使得光源发射响应于在第二波长范围内存在或不存在光的第一波长范围内的波长的光。

6. 发明授权

US5886471A Automatic vehicle light relay switching system for providing daytime running lights 失效
标题翻译：自动车灯继电器切换系统，提供日间行车灯
公开(公告)号：US5886471A
公开(公告)日：1999-03-23
申请号：US819040
申请日：1997-03-17
申请人： Charles E. Benedict , Patrick Mullins
发明人： Charles E. Benedict , Patrick Mullins
IPC分类号： B60Q1/14 , H05B37/00
CPC分类号： B60Q1/143 , B60Q2300/052 , B60Q2300/21 , B60Q2300/314
摘要： Relay switching circuits for supplying power to a vehicle exterior lighting system to provide for daytime running lights and which are controlled by solid state logic circuits, depending upon the condition of either or both of the vehicle starter and ignition switches.
摘要翻译：继电器开关电路，用于向车辆外部照明系统供电，以提供白天行车灯，并且由固态逻辑电路控制，这取决于车辆起动器和点火开关中的任一个或两者的状况。

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