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1. 发明授权

US10927086B2 Substituted sulfoximine compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors 有权
公开(公告)号：US10927086B2
公开(公告)日：2021-02-23
申请号：US16483957
申请日：2018-02-19
申请人： Merck Sharp & Dohme Corp. , Kun Liu , Dane Clausen , Liangqin Guo , Yongxin Han , Shuwen He , Joseph Kozlowski , Derun Li , Qinglin Pu , Wensheng Yu , Hongjun Zhang
发明人： Kun Liu , Dane Clausen , Liangqin Guo , Yongxin Han , Shuwen He , Joseph Kozlowski , Derun Li , Qinglin Pu , Wensheng Yu , Hongjun Zhang
IPC分类号： C07D271/08 , C07D413/12
摘要： Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

2. 发明申请

US20170267695A1 ERK INHIBITORS 有权
公开(公告)号：US20170267695A1
公开(公告)日：2017-09-21
申请号：US15531771
申请日：2015-12-10
申请人： Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
发明人： Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
IPC分类号： C07D498/18 , C07D471/22 , C07D471/18
CPC分类号： C07D498/18 , A61K31/437 , A61K31/444 , C07D471/18 , C07D471/22
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).

3. 发明申请

US20150258074A1 NOVEL COMPOUNDS THAT ARE ERK INHIBITORS 有权
标题翻译：新的化合物是ERK抑制剂
公开(公告)号：US20150258074A1
公开(公告)日：2015-09-17
申请号：US14431485
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
发明人： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC分类号： A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译：公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。还公开了使用式（1.0）化合物治疗癌症的方法。

4. 发明申请

US20130332605A1 ADVERTISING AND FACILITATING MANAGEMENT ACCESS TO ADDED CAPABILITIES OF INTELLIGENT DEVICES IN A SYSTEM 有权
标题翻译：广告和促进管理访问系统中智能设备的添加能力
公开(公告)号：US20130332605A1
公开(公告)日：2013-12-12
申请号：US13494648
申请日：2012-06-12
申请人： Joseph Kozlowski , Abeye Teshome , Jon Hass
发明人： Joseph Kozlowski , Abeye Teshome , Jon Hass
IPC分类号： G06F15/173
CPC分类号： G06F9/5044
摘要： A network interface device (NID) or management access point of a system is configured to: receive requests to register one or more additional capabilities provided by a second intelligent device integrated into the system; in response to the request, register the additional capabilities within a capabilities listing; advertise the additional capabilities as being an available within the system; and respond to a request from an external requestor for access to one of the additional capabilities by forwarding the management protocol and payload to the second intelligent device to enable the second intelligent device to perform all substantive processing required for the request. The NID establishes and maintains a network session between the second intelligent device and any external requestor requesting access to the additional capabilities. In response to receiving a response from the second intelligent device, the NID packages the response and forwards the response to the external requestor.
摘要翻译：系统的网络接口设备（NID）或管理接入点被配置为：接收注册由集成到系统中的第二智能设备提供的一个或多个附加功能的请求; 响应于该请求，在能力列表中注册附加功能; 将附加功能宣传为系统内可用的功能; 以及通过将所述管理协议和有效负载转发到所述第二智能设备来响应来自外部请求者的用于访问附加能力之一的请求，以使得所述第二智能设备能够执行所述请求所需的所有实质性处理。 NID建立并维护第二智能设备和请求访问附加功能的任何外部请求者之间的网络会话。响应于接收到来自第二智能设备的响应，NID封装响应并将响应转发给外部请求者。

5. 发明授权

US08488025B2 Sub-frame tapered reset 有权
标题翻译：子框架锥形复位
公开(公告)号：US08488025B2
公开(公告)日：2013-07-16
申请号：US12582316
申请日：2009-10-20
申请人： Ying Huang , Giuseppe Rossi , Lester Joseph Kozlowski , Laurent Blanquart , Qianjiang Mao , Gregory Chow
发明人： Ying Huang , Giuseppe Rossi , Lester Joseph Kozlowski , Laurent Blanquart , Qianjiang Mao , Gregory Chow
IPC分类号： H04N5/217 , H04N5/335
CPC分类号： H04N5/363 , H04N5/343 , H04N5/3532 , H04N5/374 , H04N5/3765
摘要： Systems and methods are provided that facilitate employing a plurality of independent reset buses for a column of pixels in a pixel array of a CMOS sensor imager. Utilization of the plurality of independent reset buses for the column of pixels can enable independent reset to be effectuated when employing sub-frame integration. For example, rows to be read and reset during a given readout time interval can be selected based upon one or more criteria. Further, each of the rows selected during the given readout time interval can be associated with a respective distinct reset bus. By leveraging the plurality of independent reset buses, uniformity in pixel operation can be maintained whether operating in full frame integration mode or sub-frame integration mode. Thus, noise resultant from changing between integration modes can be mitigated by using the plurality of independent reset buses.
摘要翻译：提供了系统和方法，其便于对CMOS传感器成像器的像素阵列中的像素列采用多个独立的复位总线。对于像素列，多个独立复位总线的利用可以使得在采用子帧集成时能够实现独立的复位。例如，可以基于一个或多个标准来选择在给定的读出时间间隔期间要读取和复位的行。此外，在给定读出时间间隔期间选择的每行都可以与相应的不同的复位总线相关联。通过利用多个独立的复位总线，无论是在全帧集成模式还是子帧集成模式下操作，都可以保持像素操作的均匀性。因此，可以通过使用多个独立复位总线来减轻由积分模式之间变化引起的噪声。

6. 发明申请

US20080039474A1 NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 有权
标题翻译：具有CXCR3拮抗剂活性的新型杂环取代的吡啶化合物
公开(公告)号：US20080039474A1
公开(公告)日：2008-02-14
申请号：US11688014
申请日：2007-03-19
申请人： STUART ROSENBLUM , Joseph Kozlowski , Neng-Yang Shih , Brian McGuinness , Douglas Hobbs
发明人： STUART ROSENBLUM , Joseph Kozlowski , Neng-Yang Shih , Brian McGuinness , Douglas Hobbs
IPC分类号： A61K31/497 , A61P29/00 , C07D401/02
CPC分类号： C07D401/14 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1. or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构或其药学上可接受的盐，溶剂合物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化），移植物排斥（非限制性实例，包括同种异体移植物排斥，移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

7. 发明申请

US20070197564A1 Compounds for the treatment of inflammatory disorders 有权
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US20070197564A1
公开(公告)日：2007-08-23
申请号：US11653511
申请日：2007-01-16
申请人： Brian Lavey , Joseph Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael Wong , Bandarpalle Shankar , Neng-Yang Shih , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong-Heon Kim
发明人： Brian Lavey , Joseph Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael Wong , Bandarpalle Shankar , Neng-Yang Shih , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong-Heon Kim
IPC分类号： A61K31/52 , C07D471/02 , A61K31/4745 , A61K31/513 , A61K31/519 , C07D473/02 , C07D487/02
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症。

8. 发明申请

US20060276506A1 Compounds for the treatment of inflammatory disorders 有权
公开(公告)号：US20060276506A1
公开(公告)日：2006-12-07
申请号：US11333663
申请日：2006-01-17
申请人： Wensheng Yu , Ling Tong , Lei Chen , Joseph Kozlowski , Brian Lavey , Neng-Yang Shih , Vincent Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael Wong , De-Yi Yang , Seong Kim , Bandarpalle Shankar , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Umar Mansoor , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li
发明人： Wensheng Yu , Ling Tong , Lei Chen , Joseph Kozlowski , Brian Lavey , Neng-Yang Shih , Vincent Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael Wong , De-Yi Yang , Seong Kim , Bandarpalle Shankar , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Umar Mansoor , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li
IPC分类号： A61K31/4709 , A61K31/4245 , A61K31/4178 , C07D413/14 , C07D403/02
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D491/04 , C07D495/04
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

9. 发明申请

US20180141962A1 AZACARBAZOLE BTK INHIBITORS 审中-公开
公开(公告)号：US20180141962A1
公开(公告)日：2018-05-24
申请号：US15564349
申请日：2016-04-04
申请人： JIAN LIU , JOSEPH KOZLOWSKI , RONALD KIM , XIAOLEI GAO , SOBHANA BABU BOGA , YOUNONG YU , HAO WU , SHILAN LIU , CHUNDAO YANG , MERCK SHARP & DOHME CORP.
发明人： JIAN LIU , JOSEPH KOZLOWSKI , RONALD KIM , XIAOLEI GAO , SOBHANA BABU BOGA , YOUNONG YU , HAO WU , SHILAN LIU , CHUNDAO YANG
IPC分类号： C07D519/00 , A61P19/02
CPC分类号： C07D519/00 , A61P19/02
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein CH, R1, R1a, R1b, R2, R3, and the subscripts m1, m2, p, q, and t are as set forth herein. The present invention also provides pharmaceutical compositions comprising these compounds and their use in therapy. In Cparticular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated dis orders.

10. 发明授权

US09828365B2 Fused tetracyclic heterocyclic compounds and methods of use thereof for the treatment of viral diseases 有权
公开(公告)号：US09828365B2
公开(公告)日：2017-11-28
申请号：US15104584
申请日：2014-12-15
申请人： MERCK SHARP & DOHME CORP. , Joseph Kozlowski , Craig Coburn , Wensheng Yu , Ling Tong , Bin Hu , Bin Zhong , Jinglai Hao , Dahai Wang , Tao Ji
发明人： Joseph Kozlowski , Craig Coburn , Wensheng Yu , Ling Tong , Bin Hu , Bin Zhong , Jinglai Hao , Dahai Wang , Tao Ji
IPC分类号： C07D493/04 , C07D405/14 , A61K45/06 , A61K31/4985 , A61K31/7072 , A61K31/4178
CPC分类号： C07D405/14 , A61K31/4155 , A61K31/4178 , A61K31/4985 , A61K31/7072 , A61K45/06 , C07D493/04 , A61K2300/00
摘要： The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A′, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.

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