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1. 发明申请

WO2005101838A3 PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为化合物受体拮抗剂的哌嗪衍生物
公开(公告)号：WO2005101838A3
公开(公告)日：2006-03-02
申请号：PCT/US2005012265
申请日：2005-04-12
申请人： INCYTE CORP , XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALF BRIAN
发明人： XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALF BRIAN
IPC分类号： A61K31/496 , A61K45/06 , C07D401/06 , C07D401/14 , C07D417/14 , C07D471/04 , A61K31/495
CPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula (I): wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
摘要翻译：本发明涉及式（I）的化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。在一些实施方案中，本发明的化合物对CCR5是选择性的。该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。

2. 发明申请

WO2005101838A8 Piperazinylpiperidine derivatives as chemokine receptor antagonists 审中-公开
标题翻译：哌嗪基哌啶衍生物作为趋化因子受体拮抗剂
公开(公告)号：WO2005101838A8
公开(公告)日：2006-05-11
申请号：PCT/US2005012265
申请日：2005-04-12
申请人： XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALF BRIAN , INCYTE CORP
发明人： XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALE BRIAN
IPC分类号： A61K31/496 , A61K45/06 , C07D401/06 , C07D401/14 , C07D417/14 , C07D471/04
CPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula (I): wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
摘要翻译：本发明涉及式（I）的化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。在一些实施方案中，本发明的化合物对CCR5是选择性的。该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。

3. 发明申请

WO2004108086A3 HYDANTOIN DERIVATIVES AS INHIBITORS OF TUMOR NECROSIS FACTOR-alpha CONVERTING ENZYME (TACE) 审中-公开
标题翻译：作为肿瘤坏死因子-α转化酶（TACE）的抑制剂的羟丁胍衍生物
公开(公告)号：WO2004108086A3
公开(公告)日：2005-03-31
申请号：PCT/US2004017538
申请日：2004-06-03
申请人： SQUIBB BRISTOL MYERS CO , DUAN JINGWU , XUE CHU-BIAO , SHEPPECK JAMES , JIANG BIN , CHEN LIHUA
发明人： DUAN JINGWU , XUE CHU-BIAO , SHEPPECK JAMES , JIANG BIN , CHEN LIHUA
IPC分类号： A61K20060101 , A61K31/4164 , A61K31/47 , C07D413/04 , C07D413/14 , C07D453/00
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables L, Z , R , R , R , and R are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-alpha converting enzyme (TACE), aggrecanase, or a combination thereof
摘要翻译：本发明提供式（I）化合物或其立体异构体或药学上可接受的盐形式，其中变量L，Z 0，R 1，R 4，R 5和R 11 定义如本文所定义，其可用作基质金属蛋白酶（MMP），TNF-α转化酶（TACE），聚集蛋白聚糖蛋白聚糖酶或其组合的抑制剂

4. 发明申请

WO2007084314A3 MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME 审中-公开
标题翻译： 11-羟基甾体脱氢酶1型的调节剂，其药物组合物及其使用方法
公开(公告)号：WO2007084314A3
公开(公告)日：2008-03-27
申请号：PCT/US2007000695
申请日：2007-01-11
申请人： INCYTE CORP , YAO WENQING , BURNS DAVID M , CHEN LIHUA , ZHUO JINCONG , HE CHUNHONG
发明人： YAO WENQING , BURNS DAVID M , CHEN LIHUA , ZHUO JINCONG , HE CHUNHONG
IPC分类号： C07D207/16 , A61K31/40 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P27/00 , C07D403/04
CPC分类号： C07D403/04 , C07D207/16 , C07D209/96 , C07D471/10 , C07D487/10
摘要： The present invention relates to inhibitors of 11-ß hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-ß hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.
摘要翻译：本发明涉及1型11-羟基类固醇脱氢酶抑制剂及其药物组合物。本发明的化合物可用于治疗与11-β羟基类固醇脱氢酶1（例如肥胖症和糖尿病）的表达或活性相关的各种疾病。

5. 发明专利

ZA202003749B POSTOPERATIVE UPPER LIMB EXERCISE DEVICE 未知
公开(公告)号：ZA202003749B
公开(公告)日：2021-04-28
申请号：ZA202003749
申请日：2020-06-15
申请人： CHEN LIHUA
发明人： CHEN LIHUA , GAO HONG , SHEN DAN
摘要： Disclosed is a post-operation upper limb exercise device, comprising a housing assembly (10), a connecting assembly (20) and a rotating assembly (30). The housing assembly (10) comprises a support frame (11), a connecting frame (12), a slider (13), a sliding block (14), a telescopic rod (15) and a fixed rod (16), wherein the connecting frame (12) is arranged on an upper surface of a front end of the support frame (11) and is rotatably connected to the support frame (11); the fixed rod (16) is arranged on an upper surface of a rear end of the support frame (11) and is rotatably connected to the support frame (11); and the telescopic rod (15) is arranged inside the fixed rod (16) and is slidably connected to the fixed rod (16). A fixed block (31) is arranged on the sliding block (14), and a rotary shaft (33) is arranged inside the fixed block (31); and a patient can hold a rotary handle (34) and then rotate a connecting column (36) such that a connecting rod (35) moves circumferentially around the fixed block (31), thereby achieving the effect of exercising the shoulder of the patient, and the function is more comprehensive. A weight block (23) is provided with a thread, and the weight block (23) is fixed to the sliding block (14) by means of the thread, thereby preventing the weight block (23) from slipping down from the sliding block (14) and facilitating use. The interior of an insertion slot (141) is coated with a wear-resistant layer, thereby being able to effectively slow down wear to the insertion slot (141) and prolonging the service life thereof.

6. 发明申请

WO03053941A2 BARBITURIC ACID DERIVATIVES AS INHIBITORS OF TNF-ALPHA CONVERTING ENZYME (TACE) AND/OR MATRIX METALLOPROTEINASES 审中-公开
标题翻译：用作TNF-α转化酶（TACE）和/或基质金属蛋白酶抑制剂的巴比妥酸衍生物
公开(公告)号：WO03053941A2
公开(公告)日：2003-07-03
申请号：PCT/US0240458
申请日：2002-12-17
申请人： SQUIBB BRISTOL MYERS CO , DUAN JINGWU , JIANG BIN , CHEN LIHUA , LU ZHONGHUI , BARBOSA JOSEPH , PITTS WILLIAM
发明人： DUAN JINGWU , JIANG BIN , CHEN LIHUA , LU ZHONGHUI , BARBOSA JOSEPH , PITTS WILLIAM
IPC分类号： A61P9/04 , A61P19/02 , A61P25/28 , C07D239/54 , C07D239/62 , C07D239/70 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10 , C07D487/10 , C07D491/10 , A61K31/513 , A61K31/515 , C07D239/56 , C07D239/58 , C07D239/68
CPC分类号： C07D239/54 , C07D239/62 , C07D239/70 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10 , C07D487/10 , C07D491/10
摘要： The present application describes novel barbituric acid derivatives of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-a converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
摘要翻译：本申请描述了式（I）的新型巴比妥酸衍生物或其药学上可接受的盐或前药形式，其中A，B，L，R1，R2，R3，R4，R5，n，W，U，X，Y，Z ，Ua，Xa，Ya和Za在本说明书中定义，其可用作TNF-α转化酶（TACE）和基质金属蛋白酶（MMP）抑制剂。

7. 发明专利

JP2012036210A Piperazinylpiperidine derivatives as chemokine receptor antagonists 审中-公开
标题翻译：作为化合物受体拮抗剂的哌嗪衍生物
公开(公告)号：JP2012036210A
公开(公告)日：2012-02-23
申请号：JP2011220378
申请日：2011-10-04
申请人： Incyte Corp , インサイト・コーポレイションIncyte Corporation
发明人： XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALF BRIAN
IPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/00 , A61K45/06 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/04 , A61P43/00 , C07D401/06 , C07D417/14 , C07D471/04
CPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide novel compounds that modulate the activity of or bind to chemokine receptors such as CCR5.SOLUTION: The present invention relates to compounds of Formula I: wherein the compounds modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
摘要翻译：要解决的问题：提供调节趋化因子受体如CCR5的活性或结合趋化因子受体的新型化合物。解决方案：本发明涉及式I化合物：其中所述化合物调节趋化因子受体如CCR5的活性或与其结合。在一些实施方案中，化合物对CCR5是选择性的。该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。版权所有（C）2012，JPO＆INPIT

8. 发明公开

EP1734966A4 PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS 有权转让
标题翻译： PIPERAZINYLPIPERIDINDERIVATE ALS趋化因子受体拮抗剂
公开(公告)号：EP1734966A4
公开(公告)日：2009-04-22
申请号：EP05755295
申请日：2005-04-12
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , CAO GANFENG , HUANG TAISHENG , CHEN LIHUA , ZHANG KE , WANG ANLAI , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH , METCALF BRIAN
IPC分类号： A61K31/495 , A61K31/496 , A61K45/06 , A61P31/00 , C07D401/06 , C07D401/14 , C07D417/14 , C07D471/04
CPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

9. 发明专利

GEP20094680B PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS 未知
公开(公告)号：GEP20094680B
公开(公告)日：2009-05-10
申请号：GEAP2005009702
申请日：2005-04-12
申请人： INCYTE CORP
发明人： METCALF BRIAN , GLENN JOSEPH , ANAND RAJAN , MELONI DAVID , WANG ANLAI , ZHANG KE , CHEN LIHUA , HUANG TAISHENG , CAO GANFENG , XUE CHU-BIAO
IPC分类号： A61K31/495 , A61K31/496 , A61K45/06 , C07D401/06 , C07D401/14 , C07D417/14 , C07D471/04
摘要： A compound of the formula wherein R1 - R5 and r are provided in the claims; said compounds can modulate the activity of bind to chemokine receptors such as CCR5 and accor¬dingly the pharmaceutical compositions comprising that are useful for treatment of diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

10. 发明专利

NO20065151L 未知
公开(公告)号：NO20065151L
公开(公告)日：2007-01-04
申请号：NO20065151
申请日：2006-11-09
申请人： INCYTE CORP
发明人： METCALF BRIAN , WANG ANLAI , XUE CHU-BIAO , CAO GANFENG , CHEN LIHUA , ZHANG KE , HUANG TAISHENG , MELONI DAVID , ANAND RAJAN , GLENN JOSEPH
IPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , A61P31/12 , C07D401/14 , C07D413/06 , C07D417/14 , C07D471/04
摘要： The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

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