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1. 发明申请

WO2007059359A3 SUBSTITUTED PYRAZALONES 审中-公开
公开(公告)号：WO2007059359A3
公开(公告)日：2007-05-24
申请号：PCT/US2006/045095
申请日：2006-11-21
申请人： BIOGEN IDEC MA INC. , LEE, Wen-Cherng , CARTER, Mary, Beth , CHUAQUI, Claudio , GUCKIAN, Kevin , LIN, Edward, Yin-shiang , CHOI, Michael, J. , DENG, Zhan , BORIACK-SJODIN, Paula, Ann , SUN, Lihong
发明人： LEE, Wen-Cherng , CARTER, Mary, Beth , CHUAQUI, Claudio , GUCKIAN, Kevin , LIN, Edward, Yin-shiang , CHOI, Michael, J. , DENG, Zhan , BORIACK-SJODIN, Paula, Ann , SUN, Lihong
IPC分类号： C07D401/14 , C07D403/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/14 , A61K31/4184 , A61P35/00
摘要： The invention is related to compounds of formula (I) as antagonists of the TGFβ family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable.

2. 发明申请

WO2011044157A1 HETEROCYCLIC COMPOUNDS USEFUL AS PDK1 INHIBITORS 审中-公开
标题翻译：杂环化合物可用作PDK1抑制剂
公开(公告)号：WO2011044157A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/051517
申请日：2010-10-05
申请人： BIOGEN IDEC MA INC. , SUNESIS PHARMACEUTICALS, INC. , ARNDT, Joseph , CHAN, Timothy , GUCKIAN, Kevin , KUMARAVEL, Gnanasambandam , LEE, Wen-Cherng , LIN, Edward, Yin-shiang , SCOTT, Daniel , SUN, Lihong , THOMAS, Jermaine , VAN VLOTEN, Kurt , WANG, Deping , ZHANG, Lei , ERLANSON, Daniel
发明人： ARNDT, Joseph , CHAN, Timothy , GUCKIAN, Kevin , KUMARAVEL, Gnanasambandam , LEE, Wen-Cherng , LIN, Edward, Yin-shiang , SCOTT, Daniel , SUN, Lihong , THOMAS, Jermaine , VAN VLOTEN, Kurt , WANG, Deping , ZHANG, Lei , ERLANSON, Daniel
IPC分类号： A61K31/50
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/452 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/5383 , C07D213/82 , C07D213/85 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , C07D473/34 , C07D487/04 , C07D491/052 , C07D498/04 , C07D519/00
摘要： The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.
摘要翻译：本发明提供可用作PDK1抑制剂的化合物。本发明还提供了其组合物，以及治疗PDK1介导的疾病的方法。

3. 发明申请

WO2008005457A2 PYRIDINONYL PDK1 INHIBITORS 审中-公开
标题翻译：吡啶酮PDK1抑制剂
公开(公告)号：WO2008005457A2
公开(公告)日：2008-01-10
申请号：PCT/US2007/015397
申请日：2007-07-02
申请人： SUNESIS PHARMACEUTICALS , BIOGEN IDEC, INC. , LIND, Kenneth, Egnard , CAO, Kathy , LIN, Edward, Yin-shiang , NGUYEN, Thinh, Ba , TANGONAN, Bradley, T. , ERLANSON, Daniel, A. , GUCKIAN, Kevin , SIMMONS, Robert, Lowell , LEE, Wen-cherng , SUN, Lihong , HANSEN, Stig , PATHAN, Nuzhat , ZHANG, Lei
发明人： LIND, Kenneth, Egnard , CAO, Kathy , LIN, Edward, Yin-shiang , NGUYEN, Thinh, Ba , TANGONAN, Bradley, T. , ERLANSON, Daniel, A. , GUCKIAN, Kevin , SIMMONS, Robert, Lowell , LEE, Wen-cherng , SUN, Lihong , HANSEN, Stig , PATHAN, Nuzhat , ZHANG, Lei
IPC分类号： A61K31/519
CPC分类号： C07D471/04 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D211/86 , C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
摘要翻译：本发明提供吡啶酮基PDK1抑制剂和使用其治疗癌症的方法。

4. 发明申请

WO2008030584A2 MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 审中-公开
标题翻译：白细胞介素-1受体相关激酶的调节剂
公开(公告)号：WO2008030584A2
公开(公告)日：2008-03-13
申请号：PCT/US2007/019588
申请日：2007-09-07
申请人： BIOGEN IDEC MA INC. , GUCKIAN, Kevin , JEWELL, Charles , CONLAN, Patrick , LIN, Edward, Yin-Shiang , CHAN, Timothy
发明人： GUCKIAN, Kevin , JEWELL, Charles , CONLAN, Patrick , LIN, Edward, Yin-Shiang , CHAN, Timothy
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention relates to modulators of IRAK kinases and provides compositions comprising such modulators, as well as methods therewith for treating IRAK- mediated or IRAK-associated conditions or diseases.
摘要翻译：本发明涉及IRAK激酶的调节剂并提供包含这种调节剂的组合物，以及其用于治疗IRAK介导的或与IRAK相关的病症或疾病的方法。

5. 发明申请

WO2012109108A1 S1P MODULATING AGENTS 审中-公开
标题翻译： S1P调节剂
公开(公告)号：WO2012109108A1
公开(公告)日：2012-08-16
申请号：PCT/US2012/023799
申请日：2012-02-03
申请人： BIOGEN IDEC MA INC. , THOMAS, Jermaine , MI, Sha , LIN, Edward, Yin-shiang , ZHENG, Guo, Zhu , MA, Bin , CALDWELL, Richard, D. , GUCKIAN, Kevin , KUMARAVEL, Gnanasambandam
发明人： THOMAS, Jermaine , MI, Sha , LIN, Edward, Yin-shiang , ZHENG, Guo, Zhu , MA, Bin , CALDWELL, Richard, D. , GUCKIAN, Kevin , KUMARAVEL, Gnanasambandam
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： A61K31/445 , A61K31/225 , A61K31/4545 , A61K31/4709 , A61K31/498 , A61K31/517 , A61K31/55 , A61K31/695 , A61K38/21 , A61K39/3955 , C07D211/34 , C07D211/60 , C07D211/62 , C07D215/20 , C07D401/06 , C07D405/12 , C07K16/2842
摘要： Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
摘要翻译：式（I）或（II）的化合物可以调节SIP受体的活性。

6. 发明申请

WO2009023854A1 BICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS 审中-公开
标题翻译：双相磷脂酸1-磷酸酯类似物
公开(公告)号：WO2009023854A1
公开(公告)日：2009-02-19
申请号：PCT/US2008/073378
申请日：2008-08-15
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , BIOGEN IDEC MA INC. , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , GUCKIAN, Kevin , LIN, Edward, Yin-shiang
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , GUCKIAN, Kevin , LIN, Edward, Yin-shiang
IPC分类号： C07F9/09 , C07C215/08 , C07C215/10 , C07D271/06 , C07D333/16 , C07D413/04 , A61K31/133 , A61K31/381 , A61K31/4245 , A61K31/661 , A61P19/00
CPC分类号： C07C323/32 , C07C215/38 , C07C217/74 , C07D271/06 , C07D333/16 , C07D413/04 , C07F9/091
摘要： Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors. Formula (I):
摘要翻译：提供了在一种或多种S1P受体上具有激动剂活性的化合物。化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。式（I）：

7. 发明申请

WO2008094556A2 IMIDAZOLONE COMPOUNDS AND METHODS OF MAKING AND USING THE SAME 审中-公开
标题翻译：咪唑啉酮化合物及其制备方法和使用方法
公开(公告)号：WO2008094556A2
公开(公告)日：2008-08-07
申请号：PCT/US2008/001172
申请日：2008-01-30
申请人： BIOGEN IDEC MA INC. , GUCKIAN, Kevin , LEE, Wen-cherng , LIN, Edward (Ted)
发明人： GUCKIAN, Kevin , LEE, Wen-cherng , LIN, Edward (Ted)
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： In one aspect, the invention features a compound of the general Formula (I). Compounds of Formula (I) possess high affinity for Alk 5 and/or AIk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.
摘要翻译：一方面，本发明的特征在于通式（I）的化合物。式（I）的化合物对Alk 5和/或AIk 4具有高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化病症在内的许多疾病。

8. 发明申请

WO2005105770A2 ARYLPHENYLAMINO-, ARYLPHENYLAMIDE-, AND ARYLPHENYLETHER-SULFIDE DERIVATIVES 审中-公开
标题翻译：芳基苯胺，芳基酰胺和芳基苯磺酰胺衍生物
公开(公告)号：WO2005105770A2
公开(公告)日：2005-11-10
申请号：PCT/US2005/014778
申请日：2005-04-28
申请人： ICOS CORPORATION , BIOGEN IDEC MA INC. , CHIN, Donovan , DURAND-REVILLE, Thomas , FAROUZ, Francine, S. , FOWLER, Kerry, W. , GUCKIAN, Kevin , JACOBSON, Irina , KASAR, Ramesh , PETTER, Russell, C. , SCOTT, Daniel , SOWELL, Gregory, C. , THORSETT, Eugene , YIN-SHIANG LIN, Edward
发明人： CHIN, Donovan , DURAND-REVILLE, Thomas , FAROUZ, Francine, S. , FOWLER, Kerry, W. , GUCKIAN, Kevin , JACOBSON, Irina , KASAR, Ramesh , PETTER, Russell, C. , SCOTT, Daniel , SOWELL, Gregory, C. , THORSETT, Eugene , YIN-SHIANG LIN, Edward
IPC分类号： C07D307/54
CPC分类号： C07D233/64 , C07C323/62 , C07C2601/14 , C07C2602/44 , C07D207/14 , C07D207/26 , C07D211/56 , C07D211/58 , C07D213/34 , C07D213/56 , C07D231/40 , C07D257/04 , C07D261/08 , C07D261/10 , C07D295/185 , C07D307/54 , C07D309/14 , C07D333/34 , C07D335/02 , C07D401/12 , C07D405/12 , C07D409/12 , C07D451/02 , C07D451/04
摘要： The present invention relates in part to compounds of formulas I and III: and pharmaceutically-acceptable salts and prodrugs thereof. These compounds can be useful for treating diseases such as inflammatory and immune diseases. The present invention also relates to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a subject.
摘要翻译：本发明部分地涉及式I和III的化合物及其药学上可接受的盐和前药。这些化合物可用于治疗疾病如炎症和免疫疾病。本发明还涉及包含这些化合物的药物组合物，以及抑制受试者的炎症或抑制免疫应答的方法。

9. 发明申请

WO2005105766A3 ARYLPHENYLAMINO-AND ARYLPHENYLETHER-SULFIDE DERIVATIVES, USEFUL FOR THE TREATMENT OF INFLAMMATORY AND IMMUNE DISEASES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
公开(公告)号：WO2005105766A3
公开(公告)日：2005-11-10
申请号：PCT/US2005/014802
申请日：2005-04-28
申请人： ICOS CORPORATION , BIOGEN IDEC MA INC. , GUCKIAN, Kevin , JACOBSON, Irina , SCOTT, Daniel , SOWELL, C., Gregory
发明人： GUCKIAN, Kevin , JACOBSON, Irina , SCOTT, Daniel , SOWELL, C., Gregory
IPC分类号： C07D295/18
摘要： The present invention relates in part to compounds of formulas (I) and (III): and pharmaceutically-acceptable salts and prodrugs thereof. These compounds can be useful for treating diseases such as inflammatory and immune diseases. The present invention also relates to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a subject.

10. 发明申请

WO2014081752A1 S1P AND/OR ATX MODULATING AGENTS 审中-公开
标题翻译： S1P和/或ATX调节剂
公开(公告)号：WO2014081752A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/070878
申请日：2013-11-20
申请人： BIOGEN IDEC MA INC.
发明人： PENG, Hairuo , LIN, Edward, Yin-shiang , CHAO, Jianhua , XIN, Zhili , MA, Bin , GUCKIAN, Kevin , CHAN, Timothy , KUMARAVEL, Gnanasambandam , TAVERAS, Arthur, G.
IPC分类号： C07D207/08 , C07D211/22 , C07D211/56 , C07D211/62 , C07D211/70 , C07D213/74 , C07D237/22 , C07D239/47 , C07D295/15 , C07D295/155 , C07D401/12 , A61K31/40 , A61K31/451 , A61K31/4545 , A61K31/495
CPC分类号： C07D211/22 , A61K31/451 , A61K31/4545 , A61K31/495 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/08 , C07D211/56 , C07D211/62 , C07D211/70 , C07D213/74 , C07D237/22 , C07D239/47 , C07D295/15 , C07D295/155 , C07D401/04 , C07D401/12 , C07D403/04
摘要： Compounds of formula (I) wherein: X is -0-, -S(0) r -, -CH 2 -, or -NR-, wherein r is 0, 1, or 2; X 1 , X 2 , and X 5 are each independently CR 7 or N; one of X 3 or X 4 is C and is attached by a single bond to -L-, and the other is CR 7 or N, provided that no more than three of X 1 , X 2 , X 3 , X or X 5 are N; Ring A is monocyclic C 5-6 scycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or 0; wherein Ring A is further optionally substituted with from 1 to 3 R 4 ; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, -0-, -NR-, -S(0) n -, -CH 2 -,or -C(O)-, wherein n is 0, 1, or 2; 1 2 L 1 is an C 1-8 alkylene, C 3-s cycloalkylene, -CH 2 -L 2 -, or a 3- to 8- membered heterocyclylene comprising 1 to 5; R 1 is C 6-20 alkyl or a monocyclic C 3-8 cycloalkyl; wherein said C 3-8 cycloalkyl is substituted with at least one R 6 and may be optionally substituted with from 1 to 5 additional R 6 substituents, wherein R 6 for each occurrence is independently selected; and R 2 is -C(0)OR 3 , -C(0)N(R 3 )-S(0) 2 R 3 , -S(0) 2 OR 3 , -C(0)NHC(0) R 3 , -Si(0)OH, - B(OH) 2 , -N(R 3 )S(0) 2 R 3 , -S(0) 2 N(R 3 ) 2 , -O-P(O) (OR 3 ) 2 , or -P(0)(OR 3 ) 2 , -CN, - S(0) 2 NHC(0)R 3 , -C(0)NHS(0) 2 R3, - C(0)NHOH, -C(0)NHCN, -CH(CF 3 )OH, -C(CF 3 ) 2 OH, or a selected heteroaryl or heterocyclyl; and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
摘要翻译：式（I）化合物其中：X为-O - ， - S（O）r - ， - CH 2 - 或 - NR-，其中r为0,1或2; X 1，X 2和X 5各自独立地为CR 7或N; X 3或X 4中的一个为C并且通过单键连接至-L-，另一个为CR 7或N，条件是X 1，X 2，X 3，X或X 5中不超过3个为N; 环A是单环C 5-6环烷基或包含1至5个独立地选自N，S或0的杂原子的5至6元单环杂环基; 其中环A进一步任选被1至3个R 4取代; 环A不是吗啉基，硫代吗啉基或四氢-2H-吡喃基; L是键，-O - ， - NR - ， - S（O）n - ， - CH 2 - 或-C（O） - ，其中n是0,1或2; 1 2 L 1是C 1-8亚烷基，C 3 - 亚环亚烷基，-CH 2 -L 2 - 或包含1至5的3-至8-元亚杂环基; R1是C6-20烷基或单环C3-8环烷基; 其中所述C 3-8环烷基被至少一个R 6取代，并且可以任选被1至5个另外的R 6取代基取代，其中每次出现的R 6是独立选择的; 并且R 2是-C（O）OR 3，-C（O）N（R 3）-S（O）2 R 3，-S（O）2 OR 3，-C（O）NHC（O）R 3，-Si ， - B（OH）2，-N（R3）S（O）2R3，-S（O）2N（R3）2，-OP（O）（OR3）2或-P（0）（OR3）2 ，-CN，-S（O）2 NHC（O）R 3，-C（O）NHS（O）2 R 3，-C（O）NHOH，-C（O）NHCN，-CH（CF 3）OH，-C CF 3）2 OH，或选择的杂芳基或杂环基; 和其药学上可接受的盐可调节一种或多种SIP受体的活性和/或自分泌素（ATX）的活性。

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