公开(公告)号：US08685980B2

公开(公告)日：2014-04-01

申请号：US13060154

申请日：2009-08-20

Applicant: Gilbert Ebai Besong ,  Christopher Thomas Brain ,  Clinton Alan Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Neil Mortenson ,  Troy D. Smith ,  Moo Je Sung ,  Steven John Woodhead ,  Wojciech Wrona ,  Bharat Lagu

Inventor： Gilbert Ebai Besong ,  Christopher Thomas Brain ,  Clinton Alan Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Neil Mortenson ,  Troy D. Smith ,  Moo Je Sung ,  Steven John Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

Abstract translation: 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US20050234042A1

公开(公告)日：2005-10-20

申请号：US11099941

申请日：2005-04-06

Applicant: Mark Palermo ,  Sushil Sharma ,  Christopher Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanlin Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark Charest ,  Feng He

Inventor： Mark Palermo ,  Sushil Sharma ,  Christopher Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanlin Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark Charest ,  Feng He

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/55 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D207/16 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/02 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D207/16 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract translation: 抑制Smac蛋白与抑制凋亡蛋白抑制剂（IAP）的新型化合物

公开(公告)号：US20110152244A1

公开(公告)日：2011-06-23

申请号：US13060154

申请日：2009-08-20

Applicant: Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Morteson ,  Troy Smith ,  Moo Sung ,  Steven Woodhead ,  Wojciech Wrona

Inventor： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Morteson ,  Troy Smith ,  Moo Sung ,  Steven Woodhead ,  Wojciech Wrona

IPC: C07D487/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/551 ,  A61K31/5377 ,  A61K31/501 ,  C12N9/99 ,  A61P35/04 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

Abstract translation: 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US5969133A

公开(公告)日：1999-10-19

申请号：US83652

申请日：1998-05-22

Applicant: Mitsunori Ono ,  Keizo Koya ,  Lijun Sun ,  Yumiko Wada ,  Wojciech Wrona ,  Natalie Dales ,  Xueliang Tao ,  Sylvia Holden

Inventor： Mitsunori Ono ,  Keizo Koya ,  Lijun Sun ,  Yumiko Wada ,  Wojciech Wrona ,  Natalie Dales ,  Xueliang Tao ,  Sylvia Holden

IPC: C07C229/56 ,  C07C229/60 ,  C07C229/64 ,  C07D209/08 ,  C07D209/12 ,  C07D235/12 ,  C07D295/112 ,  C07D307/42 ,  C07D307/79 ,  C07D265/30 ,  C07D235/02 ,  C07Z229/60 ,  C07Z261/00

CPC classification number: C07D295/112 ,  C07C229/56 ,  C07C229/60 ,  C07C229/64 ,  C07D209/08 ,  C07D209/12 ,  C07D235/12 ,  C07D307/42 ,  C07D307/79 ,  C07C2101/02 ,  C07C2101/04 ,  C07C2101/16

Abstract: A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.

Abstract translation: 由包含吸电子基团的主动烷基化部分，含有至少两个双键的生物还原部分和连接主动烷基化部分和生物还原部分的连接体组成的化合物。

公开(公告)号：US6137003A

公开(公告)日：2000-10-24

申请号：US181436

申请日：1998-10-28

Applicant: Mitsunori Ono ,  Keizo Koya ,  Lijun Sun ,  Wojciech Wrona ,  Sylvia Holden ,  Noriaki Tatsuta

Inventor： Mitsunori Ono ,  Keizo Koya ,  Lijun Sun ,  Wojciech Wrona ,  Sylvia Holden ,  Noriaki Tatsuta

IPC: C07D307/58 ,  A61K31/196 ,  A61K31/245 ,  A61K31/341 ,  A61K31/343 ,  A61P35/00 ,  C07C229/60 ,  C07C229/64 ,  C07D307/42 ,  C07C229/00

CPC classification number: C07D307/42 ,  C07C229/60 ,  C07C229/64 ,  C07C2101/02 ,  C07C2101/04

Abstract: The present invention relates to bis(haloethyl)aminobenzene derivatives featured by having carboxyl-containing moiety and one other moiety at the ortho position with respect to the bis(haloethyl)amino substituent of the benzene ring. The moiety at the ortho position can be alkyl, cycloalkyl, heterocycloalkyl, aryl heteroaryl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), alkyl(heteroaryl), alkyl(aryl), --(--O-alkyl).sub.2-5 or --Y.sup.1 --Y.sup.2 in which Y.sup.1 is O, S, or N(R.sup.5) wherein R.sup.5 is hydrogen or alkyl, and Y.sup.2 is alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroacryl, alkyl(cycloalkyl), alkyl(hetero-cycloalkyl), alkyl(aryl), or alkyl(heteroaryl).

Abstract translation: 本发明涉及通过在相对于苯环的双（卤代乙基）氨基取代基的邻位具有含羧基的部分和一个其它部分而特征的双（卤代乙基）氨基苯衍生物。 邻位的部分可以是烷基，环烷基，杂环烷基，芳基杂芳基，烷基（环烷基），烷基（杂环烷基），烷基（杂芳基），烷基（芳基）， - （ - O-烷基）2-5或-Y1 -Y 2，其中Y 1是O，S或N（R 5），其中R 5是氢或烷基，并且Y 2是烷基，烯基，环烷基，杂环烷基，芳基，异丙基丙烯酰基，烷基（环烷基），烷基（杂环烷基） （芳基）或烷基（杂芳基）。

公开(公告)号：US20170183352A1

公开(公告)日：2017-06-29

申请号：US15231005

申请日：2016-08-08

Applicant: Gilbert BESONG ,  Christopher Thomas BRAIN ,  Clinton A. BROOKS ,  Miles Stuart CONGREVE ,  Claudio DAGOSTIN ,  Guo HE ,  Ying HOU ,  Steven HOWARD ,  Yue LI ,  Yipin LU ,  Paul MORTENSON ,  Troy SMITH ,  Moo Je SUNG ,  Steven WOODHEAD ,  Wojciech WRONA ,  Bharat LAGU

Inventor： Gilbert BESONG ,  Christopher Thomas BRAIN ,  Clinton A. BROOKS ,  Miles Stuart CONGREVE ,  Claudio DAGOSTIN ,  Guo HE ,  Ying HOU ,  Steven HOWARD ,  Yue LI ,  Yipin LU ,  Paul MORTENSON ,  Troy SMITH ,  Moo Je SUNG ,  Steven WOODHEAD ,  Wojciech WRONA ,  Bharat LAGU

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US20140135312A1

公开(公告)日：2014-05-15

申请号：US14158358

申请日：2014-01-17

Applicant: Gilbert BESONG ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Ll ,  Yipin Lu ,  Paul Mortenston ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

Inventor： Gilbert BESONG ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Ll ,  Yipin Lu ,  Paul Mortenston ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC: C07D487/08 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

Abstract translation: 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US08338440B2

公开(公告)日：2012-12-25

申请号：US13456274

申请日：2012-04-26

Applicant: Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanlin Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

Inventor： Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanlin Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

IPC: A61K31/427 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/435 ,  A61K31/40 ,  A61K31/506 ,  A61K31/41

CPC classification number: C07D207/16 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).

公开(公告)号：US08207183B2

公开(公告)日：2012-06-26

申请号：US13178946

申请日：2011-07-08

Applicant: Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanling Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

Inventor： Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanling Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

IPC: A61K31/427 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/435 ,  A61K31/40 ,  A61K31/506 ,  A61K31/41 ,  C07D277/20 ,  C07D271/06 ,  C07D263/30 ,  C07D401/02 ,  C07D239/02 ,  C07D403/02

CPC classification number: C07D207/16 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).

公开(公告)号：US20100105653A1

公开(公告)日：2010-04-29

申请号：US12545322

申请日：2009-08-21

Applicant: Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona

Inventor： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Huo ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona

IPC: A61K31/519 ,  C07D487/04 ,  A61K31/551 ,  C12N5/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

Abstract translation: 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。