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1. 发明授权

US09000161B2 Processes for preparing JAK inhibitors and related intermediate compounds 有权
标题翻译：制备JAK抑制剂和相关中间体化合物的方法
公开(公告)号：US09000161B2
公开(公告)日：2015-04-07
申请号：US13761742
申请日：2013-02-07
申请人： Jiacheng Zhou , Pingli Liu , Qiyan Lin , David Meloni , Yongchun Pan , Michael Xia , Mei Li , Tai-Yuen Yue , Brian W. Metcalf
发明人： Jiacheng Zhou , Pingli Liu , Qiyan Lin , David Meloni , Yongchun Pan , Michael Xia , Mei Li , Tai-Yuen Yue , Brian W. Metcalf
IPC分类号： C07D487/00 , C07D487/04 , C07F7/18 , C07F7/10
CPC分类号： C07D487/04 , C07F5/025 , C07F7/083 , C07F7/10 , C07F7/1892 , Y02P20/55
摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
摘要翻译：本发明涉及制备式III的手性取代吡唑并吡咯并[2,3-d]嘧啶的方法和相关的合成中间体化合物。手性取代的吡唑基吡咯并[2,3-d]嘧啶可用作Janus Kinase家族蛋白酪氨酸激酶（JAKs）的抑制剂，用于治疗炎性疾病，骨髓增生性疾病和其他疾病。

2. 发明申请

US20140155404A1 PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS 有权
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：US20140155404A1
公开(公告)日：2014-06-05
申请号：US14176781
申请日：2014-02-10
申请人： Chu-Biao Xue , Genfeng Cao , Taisheng Huang , Lihua Chen , Ke Zhang , Anlai Wang , David J. Meloni , Rajan Anand , Joseph Glenn , Brian W. Metcalf
发明人： Chu-Biao Xue , Genfeng Cao , Taisheng Huang , Lihua Chen , Ke Zhang , Anlai Wang , David J. Meloni , Rajan Anand , Joseph Glenn , Brian W. Metcalf
IPC分类号： C07D401/14 , C07D417/14 , A61K31/496 , C07D471/04 , A61K31/506 , A61K31/502
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

US20110251168A1 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS 有权
标题翻译：作为化合物受体的调节剂的3-氨基吡啶衍生物
公开(公告)号：US20110251168A1
公开(公告)日：2011-10-13
申请号：US13162286
申请日：2011-06-16
申请人： Chu-Biao Xue , Brian W. Metcalf , Hao Feng , Ganfeng Cao , Taisheng Huang , Changsheng Zheng , Darius J. Robinson , Amy Qi Han
发明人： Chu-Biao Xue , Brian W. Metcalf , Hao Feng , Ganfeng Cao , Taisheng Huang , Changsheng Zheng , Darius J. Robinson , Amy Qi Han
IPC分类号： A61K31/397 , A61K31/501 , A61K31/506 , C07D403/10 , C07D417/08 , A61K31/427 , C07D401/08 , A61K31/4439 , C07D207/14 , A61K31/40 , A61K31/4178 , C07D401/14 , A61K31/497 , C07D413/10 , A61K31/5377 , A61K31/422 , C07D413/14 , A61P35/00 , A61P29/00 , A61P17/02 , A61P9/00 , A61P17/06 , A61P31/12 , C07D403/08
CPC分类号： C07D491/107 , C07D207/14 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D405/04 , C07D405/08 , C07D405/10 , C07D405/14 , C07D409/08 , C07D413/08 , C07D413/10 , C07D413/14 , C07D417/08 , C07D417/10 , C07D417/14 , C07D491/10 , C07D495/10
摘要： The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
摘要翻译：本发明涉及可用作趋化因子受体调节剂的式I的3-氨基吡咯烷衍生物（其中R1，R2，R3，R4，R5，R6，R7，R8，X，Y和X如本文所定义）活动。特别地，这些化合物可用作趋化因子受体的调节剂，更具体地可用作CCR2和/或CCR5受体的调节剂。本发明的化合物和组合物可以结合趋化因子受体，例如CCR2和/或CCR5趋化因子受体，并且可用于治疗与趋化因子（例如CCR2和/或CCR5）相关的疾病，例如动脉粥样硬化，再狭窄，狼疮，器官移植排斥和类风湿关节炎。

4. 发明授权

US07618970B2 3-aminocyclopentanecarboxamides as modulators of chemokine receptors 有权
标题翻译： 3-氨基环戊烷甲酰胺作为趋化因子受体的调节剂
公开(公告)号：US07618970B2
公开(公告)日：2009-11-17
申请号：US11167329
申请日：2005-06-27
申请人： Chu-Biao Xue , Changsheng Zheng , Hao Feng , Michael Xia , Joseph Glenn , Ganfeng Cao , Brian W. Metcalf
发明人： Chu-Biao Xue , Changsheng Zheng , Hao Feng , Michael Xia , Joseph Glenn , Ganfeng Cao , Brian W. Metcalf
IPC分类号： A61K31/497 , A61K31/445 , C07D403/08 , C07D295/23 , C07D401/08
CPC分类号： C07D309/14 , C07D405/12 , C07D405/14
摘要： The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
摘要翻译：本发明涉及式I化合物：其是趋化因子受体的调节剂。本发明的化合物及其组合物可用于治疗与趋化因子受体表达和/或活性相关的疾病。

5. 发明授权

US07449467B2 3-aminocyclopentanecarboxamides as modulators of chemokine receptors 有权
标题翻译： 3-氨基环戊烷甲酰胺作为趋化因子受体的调节剂
公开(公告)号：US07449467B2
公开(公告)日：2008-11-11
申请号：US11167816
申请日：2005-06-27
申请人： Chu-Biao Xue , Changsheng Zheng , Hao Feng , Michael Xia , Joseph Glenn , Ganfeng Cao , Brian W. Metcalf
发明人： Chu-Biao Xue , Changsheng Zheng , Hao Feng , Michael Xia , Joseph Glenn , Ganfeng Cao , Brian W. Metcalf
IPC分类号： A61K31/497 , A61K31/445 , C07D403/12 , C07D241/04 , C07D211/02
CPC分类号： C07D405/14 , C07D309/14 , C07D405/12
摘要： The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
摘要翻译：本发明涉及式I化合物：其是趋化因子受体的调节剂。本发明的化合物及其组合物可用于治疗与趋化因子受体表达和/或活性相关的疾病。

6. 发明授权

US07307086B2 3-(4-heteroarylcyclohexylamino)cyclopentanecarboxamides as modulators of chemokine receptors 有权
标题翻译： 3-（4-杂芳基环己基氨基）环戊烷甲酰胺作为趋化因子受体的调节剂
公开(公告)号：US07307086B2
公开(公告)日：2007-12-11
申请号：US11125647
申请日：2005-05-10
申请人： Chu-Biao Xue , Changsheng Zheng , Ganfeng Cao , Hao Feng , Michael Xia , Rajan Anand , Joseph Glenn , Brian W. Metcalf
发明人： Chu-Biao Xue , Changsheng Zheng , Ganfeng Cao , Hao Feng , Michael Xia , Rajan Anand , Joseph Glenn , Brian W. Metcalf
IPC分类号： C07D471/02 , A61K31/47
CPC分类号： C07D471/04 , C07D217/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
摘要翻译：本发明涉及式I化合物：其是趋化因子受体的调节剂。本发明的化合物及其组合物可用于治疗与趋化因子受体表达和/或活性相关的疾病。

7. 发明授权

US07304081B2 Amido compounds and their use as pharmaceuticals 有权
标题翻译：酰胺化合物及其作为药物的用途
公开(公告)号：US07304081B2
公开(公告)日：2007-12-04
申请号：US11122309
申请日：2005-05-04
申请人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
IPC分类号： A61K31/427 , A61K31/422 , A61K31/4155 , A61K31/4015 , C07D249/08 , C07D413/14 , C07D403/04 , C07D277/20 , C07D211/04 , C07D237/02 , C07D273/01
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), 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-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及1型11-β羟基类固醇脱氢酶抑制剂，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与1-β羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病的表达或活性相关的各种疾病。

8. 发明授权

US5041433A 11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-.alpha.-reductase 失效
标题翻译： 11-酮或羟基-3,5-二烯类固醇作为抑制剂的steriod 5-α-还原酶
公开(公告)号：US5041433A
公开(公告)日：1991-08-20
申请号：US430152
申请日：1989-11-01
申请人： Dennis A. Holt , Brian W. Metcalf , Mark A. Levy
发明人： Dennis A. Holt , Brian W. Metcalf , Mark A. Levy
IPC分类号： A61K31/56 , A61P13/02 , A61P15/00 , C07J1/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J61/00 , C07J63/00 , C07J71/00
CPC分类号： C07J1/0011 , C07J1/0022 , C07J1/007 , C07J21/00 , C07J3/00 , C07J3/005 , C07J31/006 , C07J41/0066 , C07J41/0094 , C07J51/00 , C07J61/00 , C07J63/002 , C07J7/0095 , C07J71/001 , C07J9/00 , C07J9/005
摘要： Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.
摘要翻译：发明的是羧基和羧基烷基酯取代的合成甾族化合物的11-酮基和羟基类似物，含有这些化合物的药物组合物，以及使用这些化合物抑制类固醇5-α-还原酶的方法。

9. 再颁专利

USRE31980E Olefinic derivatives of amino acids 失效
标题翻译：氨基酸的烯烃衍生物
公开(公告)号：USRE31980E
公开(公告)日：1985-09-03
申请号：US458116
申请日：1983-01-14
申请人： Brian W. Metcalf , Michel Jung
发明人： Brian W. Metcalf , Michel Jung
IPC分类号： C07C237/00
CPC分类号： C07C237/00
摘要： Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is .[.selected from.]. hydrogen.[., alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl.].; R.sub.2 is .[.selected from.]. hydroxy.[., a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl.].; R.sub.3 is .[.selected from.]. hydrogen.[., chlorine, bromine, and iodine.].; [A] is .[.selected from.]. ##STR4## .[.and --CH.dbd.CH--.]. wherein R.sub.1 is .[.selected from.]. hydrogen.[., lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##STR5## R and R.sub.1 represent hydrogen.]. and n is the integer 2 .[.or 3.]. and pharmaceutically acceptable salts and individual optical isomers thereof.

10. 发明授权

US4322416A 10-Alkynyl steroids 失效
标题翻译： 10-炔基类固醇
公开(公告)号：US4322416A
公开(公告)日：1982-03-30
申请号：US258214
申请日：1981-04-27
申请人： Brian W. Metcalf , J. O'Neal Johnston
发明人： Brian W. Metcalf , J. O'Neal Johnston
IPC分类号： A61K31/565 , A61P5/00 , C07J1/00 , C07J21/00 , C07J71/00 , A61K31/56
CPC分类号： C07J71/001 , C07J1/0011 , C07J1/0022 , C07J21/008
摘要： Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, when the 5,6-bond is saturated, R.sup.5 is divalent .dbd.O; R.sup.6 and R.sup.7 are each H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.2-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, and methods of using the aromatase inhibitors of the invention are also provided.
摘要翻译：提供了具有式“IMAGE”+ TR

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