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1. 发明授权

US07176235B2 Epothilone derivatives and methods for making and using the same 有权
标题翻译：埃坡霉素衍生物及其制备和使用方法
公开(公告)号：US07176235B2
公开(公告)日：2007-02-13
申请号：US10845467
申请日：2004-05-12
申请人： Gary Ashley , John R. Carney , Brian Metcalf
发明人： Gary Ashley , John R. Carney , Brian Metcalf
IPC分类号： A61K31/335 , C07D225/04 , C07D491/00 , C07D225/02
CPC分类号： C07D405/06 , C07D313/00 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/181 , C12R1/01
摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.
摘要翻译：本发明涉及式（I）化合物及其药用盐和溶剂合物，其中R 1，R 2，R 3， R 4，R 5，W，X，Y和Ar如本文所定义。式（I）化合物可用于治疗以细胞过度增殖为特征的疾病或病症。本发明还涉及制备式（I）化合物的方法; 含有式（I）化合物的制剂; 以及在治疗以细胞过度增殖为特征的疾病或病症（包括癌症）中使用所述化合物和制剂的方法。

2. 发明授权

US06893859B2 Epothilone derivatives and methods for making and using the same 有权
标题翻译：埃坡霉素衍生物及其制备和使用方法
公开(公告)号：US06893859B2
公开(公告)日：2005-05-17
申请号：US10115198
申请日：2002-04-02
申请人： Gary Ashley , Robert L. Arslanian , John Carney , Brian Metcalf , Li Tang
发明人： Gary Ashley , Robert L. Arslanian , John Carney , Brian Metcalf , Li Tang
IPC分类号： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C12N1/21
CPC分类号： C07D405/06 , C07D313/00 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/181 , C12R1/01
摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.
摘要翻译：本发明涉及式（I）化合物及其药用盐和溶剂合物，其中R 1，R 2，R 3， R 4，R 5，W，X，Y和Ar如本文所定义。式（I）化合物可用于治疗以细胞过度增殖为特征的疾病或病症。本发明还涉及制备式（I）化合物的方法; 含有式（I）化合物的制剂; 以及在治疗以细胞过度增殖为特征的疾病或病症（包括癌症）中使用所述化合物和制剂的方法。

3. 发明授权

US06815463B2 Laulimalide derivatives 有权
标题翻译：酸性衍生物
公开(公告)号：US06815463B2
公开(公告)日：2004-11-09
申请号：US10364111
申请日：2003-02-10
申请人： Gary Ashley , Brian Metcalf
发明人： Gary Ashley , Brian Metcalf
IPC分类号： C07D41706
CPC分类号： C07D493/08
摘要： Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

4. 发明授权

US07070964B2 Epothilone compounds and methods for making the same 有权
标题翻译：埃坡霉素化合物及其制备方法
公开(公告)号：US07070964B2
公开(公告)日：2006-07-04
申请号：US10295342
申请日：2002-11-14
申请人： Li Tang , Brian Metcalf , Leonard Katz , Gary Ashley
发明人： Li Tang , Brian Metcalf , Leonard Katz , Gary Ashley
IPC分类号： C12P17/00
CPC分类号： C07D417/06 , C07D493/04 , C07D493/08 , C12P17/167 , C12P17/181
摘要： The present invention provides bioconversion methods for making epothilone analogs. These analogs differ from the starting material by the addition of one or more hydroxyl groups or by the addition of an epoxide. These compounds, in turn, can be further modified by chemical synthesis.
摘要翻译：本发明提供用于制备埃坡霉素类似物的生物转化方法。这些类似物通过加入一个或多个羟基或通过加入环氧化物与原料不同。这些化合物又可以通过化学合成进一步改性。

5. 发明申请

US20050038086A1 Epothilone derivatives and methods for making and using the same 有权
标题翻译：埃坡霉素衍生物及其制备和使用方法
公开(公告)号：US20050038086A1
公开(公告)日：2005-02-17
申请号：US10845467
申请日：2004-05-12
申请人： Gary Ashley , Robert Arslanian , John Carney , Brian Metcalf , Li Tang
发明人： Gary Ashley , Robert Arslanian , John Carney , Brian Metcalf , Li Tang
IPC分类号： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C07D417/02 , A61K31/427
CPC分类号： C07D405/06 , C07D313/00 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/181 , C12R1/01
摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和溶剂化物，其中R 1，R 2，R 3，R 4，R 5，W，X，Y ，Ar如本文所定义。式（I）化合物可用于治疗以细胞过度增殖为特征的疾病或病症。本发明还涉及制备式（I）化合物的方法; 含有式（I）化合物的制剂; 以及在治疗以细胞过度增殖为特征的疾病或病症（包括癌症）中使用所述化合物和制剂的方法。

6. 发明授权

US06670389B2 Laulimalide derivatives 有权
公开(公告)号：US06670389B2
公开(公告)日：2003-12-30
申请号：US10071839
申请日：2002-02-08
申请人： Gary Ashley , Brian Metcalf
发明人： Gary Ashley , Brian Metcalf
IPC分类号： C07D41706
CPC分类号： C07D493/08
摘要： Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

7. 发明授权

US06489314B1 Epothilone derivatives and methods for making and using the same 有权
标题翻译：埃坡霉素衍生物及其制备和使用方法
公开(公告)号：US06489314B1
公开(公告)日：2002-12-03
申请号：US09825856
申请日：2001-04-03
申请人： Gary Ashley , Brian Metcalf
发明人： Gary Ashley , Brian Metcalf
IPC分类号： A61K3133
CPC分类号： C07D405/06 , C07D313/00 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/181 , C12R1/01
摘要： The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.
摘要翻译：本发明涉及16元大环化合物。在本发明的一个方面，提供下列化合物，其中：R1，R2，R3和R5各自独立地为氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; R4为氢卤素，C 1 -C 10烷基，C 1 -C 10羟基烷基，C 1 -C 10卤代烷基，芳基，-C（= O）R 6，-C（= O）OR 6，-NR 6 R 7，其中R 6和R 7各自独立地为氢，脂族，芳基或烷基芳基; W是O，NR8，其中R8是氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; X是O，CH2或碳 - 碳双键; Y是不存在或C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基; 且Ar为芳基; 条件是排除了10,11-脱氢抗坏血酸酮C.

8. 发明授权

US08637497B2 AZA spiro alkane derivatives as inhibitors of metalloproteases 有权
标题翻译： AZA螺烷烷衍生物作为金属蛋白酶的抑制剂
公开(公告)号：US08637497B2
公开(公告)日：2014-01-28
申请号：US13184860
申请日：2011-07-18
申请人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Fenglei Zhang , Brian Metcalf
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Fenglei Zhang , Brian Metcalf
IPC分类号： A61K31/03 , A61K31/44 , A61K31/50 , A61K31/4965 , A61K31/40 , C07D241/04 , C07D221/20 , C07D471/20 , C07D209/54
CPC分类号： A61K31/496 , A61K31/40 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4985 , A61K31/55 , A61K31/551 , C07D221/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
摘要翻译：本发明提供了式I或式II的化合物：对映异构体，非对映异构体，前药，溶剂合物，代谢物或药学上可接受的盐，其中在本文中提供了组成变量。式I和II的化合物是金属蛋白酶的调节剂，并且可用于治疗与金属蛋白酶活性相关的疾病，例如关节炎，癌症，心血管疾病，皮肤病，炎症和变态反应。

9. 发明申请

US20120122858A1 LACTAM COMPOUNDS AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： LACTAM化合物及其作为药物的用途
公开(公告)号：US20120122858A1
公开(公告)日：2012-05-17
申请号：US13355219
申请日：2012-01-20
申请人： Wenqing Yao , Chunhong He , David M. Burns , Jincong Zhuo , Meizhong Xu , Colin Zhang , Ding-Quan Qian , Brian Metcalf
发明人： Wenqing Yao , Chunhong He , David M. Burns , Jincong Zhuo , Meizhong Xu , Colin Zhang , Ding-Quan Qian , Brian Metcalf
IPC分类号： A61K31/5355 , A61K31/438 , A61K31/496 , A61K31/506 , A61K31/4725 , A61K31/4709 , A61K31/497 , A61K31/52 , A61K31/517 , C07D487/04 , A61K31/519 , A61P3/04 , A61P3/10 , A61P3/08 , A61P9/12 , A61P3/06 , A61P25/00 , A61P25/24 , A61P25/28 , A61P27/06 , A61P9/00 , A61P19/10 , A61P29/00 , A61P13/12 , A61P9/04 , A61P9/10 , A61P7/02 , A61P3/00 , C07D471/10
CPC分类号： C07D471/10
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11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，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11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

10. 发明申请

US20120035172A1 Purinone Derivatives as HM74A Agonists 有权
标题翻译：嘌呤酮衍生物作为HM74A激动剂
公开(公告)号：US20120035172A1
公开(公告)日：2012-02-09
申请号：US13275214
申请日：2011-10-17
申请人： Changsheng Zheng , Chu-Biao Xue , Ganfeng Cao , Michael Xia , Anlai Wang , Hai Fen Ye , Brian Metcalf
发明人： Changsheng Zheng , Chu-Biao Xue , Ganfeng Cao , Michael Xia , Anlai Wang , Hai Fen Ye , Brian Metcalf
IPC分类号： A61K31/5377 , C07D413/14 , A61P9/12 , A61P3/10 , A61P9/10 , A61P3/06 , C07D471/14 , A61K31/519
CPC分类号： C07D487/14
摘要： The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
摘要翻译：本发明涉及作为HM74a受体的激动剂的嘌呤酮衍生物。还提供了使用本文化合物及其药学上可接受的盐来治疗疾病的组合物和方法。

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