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1. 发明申请

WO2008121687A3 IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2008121687A3
公开(公告)日：2008-10-09
申请号：PCT/US2008/058385
申请日：2008-03-27
申请人： ARRAY BIOPHARMA INC. , MARMSÄTER, Fredrik, P. , MUNSON, Mark, C. , RIZZI, James, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , TOPALOV, George, T. , ZHAO, Qian , LYSSIKATOS, Joseph, P.
发明人： MARMSÄTER, Fredrik, P. , MUNSON, Mark, C. , RIZZI, James, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , TOPALOV, George, T. , ZHAO, Qian , LYSSIKATOS, Joseph, P.
IPC分类号： C07D471/04 , A61K31/4709 , A61P35/00
摘要： Compounds of Formula (I): are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class (3) and class (5) receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

2. 发明申请

WO2013055645A1 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES 审中-公开
标题翻译： 5,7-取代的咪唑并[1,2-C]嘧啶类
公开(公告)号：WO2013055645A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059282
申请日：2012-10-09
申请人： ARRAY BIOPHARMA INC. , BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
发明人： BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P37/00
CPC分类号： C07D487/04
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X 1 and X 2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要翻译： R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂合物是一种或多种JAK激酶的抑制剂，并且是有用的治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。

3. 发明申请

WO2009089462A1 5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： 5H-CYCLOPENTA [D]吡啶类作为AKT蛋白激酶抑制剂
公开(公告)号：WO2009089462A1
公开(公告)日：2009-07-16
申请号：PCT/US2009/030617
申请日：2009-01-09
申请人： ARRAY BIOPHARMA INC. , GENENTECH, INC. , BANKA, Anna , BENCSIK, Josef R. , BLAKE, James F. , HENTEMANN, Martin F. , KALLAN, Nicholas C. , LIANG, Jun , MITCHELL, Ian S. , SCHLACHTER, Stephen T. , WALLACE, Eli M. , XU, Rui , TANG, Tony, P.
发明人： BANKA, Anna , BENCSIK, Josef R. , BLAKE, James F. , HENTEMANN, Martin F. , KALLAN, Nicholas C. , LIANG, Jun , MITCHELL, Ian S. , SCHLACHTER, Stephen T. , WALLACE, Eli M. , XU, Rui , TANG, Tony, P.
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00 , C07D401/04 , C07D401/10 , C07D409/04 , C07D417/04 , C07D487/04
CPC分类号： C07D401/10 , C07D211/08 , C07D211/46 , C07D239/70 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D409/04 , C07D417/04 , C07D417/10 , C07D487/04
摘要： Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula (I).
摘要翻译：式I化合物可用于抑制AKT蛋白激酶。公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。式（I）。

4. 发明申请

WO2008124323A1 IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-A]吡啶化合物作为受体酪氨酸激酶抑制剂
公开(公告)号：WO2008124323A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/058395
申请日：2008-03-27
申请人： ARRAY BIOPHARMA INC. , ALLEN, Shelley , GRESCHUK, Julie, Marie , KALLAN, Nicholas, C. , MARMSÄTER, Fredrik, P. , MUNSON, Mark, C. , RIZZI, James, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , TOPALOV, George, T. , ZHAO, Qian , LYSSIKATOS, Joseph, P.
发明人： ALLEN, Shelley , GRESCHUK, Julie, Marie , KALLAN, Nicholas, C. , MARMSÄTER, Fredrik, P. , MUNSON, Mark, C. , RIZZI, James, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , TOPALOV, George, T. , ZHAO, Qian , LYSSIKATOS, Joseph, P.
IPC分类号： C07D471/04 , A61K31/33 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of Formula I: in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 R 6 , R 7 and R 8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
摘要翻译：式I化合物：其中A，B，R 1，R 1a，R 2，R 3， R 4，R 5，R 6，R 7和R 8都具有说明书中给出的含义是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。本发明的具体化合物也被发现是Pim-1的抑制剂。

5. 发明申请

WO2008121687A2 IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-A]吡啶化合物作为受体酪氨酸激酶抑制剂
公开(公告)号：WO2008121687A2
公开(公告)日：2008-10-09
申请号：PCT/US2008058385
申请日：2008-03-27
申请人： ARRAY BIOPHARMA INC , MARMSAETER FREDRIK P , MUNSON MARK C , RIZZI JAMES P , ROBINSON JOHN E , SCHLACHTER STEPHEN T , TOPALOV GEORGE T , ZHAO QIAN , LYSSIKATOS JOSEPH P
发明人： MARMSAETER FREDRIK P , MUNSON MARK C , RIZZI JAMES P , ROBINSON JOHN E , SCHLACHTER STEPHEN T , TOPALOV GEORGE T , ZHAO QIAN , LYSSIKATOS JOSEPH P
IPC分类号： C07D471/04 , A61K31/4709 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of Formula (I) in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
摘要翻译：其中A，B，R 1，R 1a，R 2，R 3，O 3的式（I）化合物 R 4，R 5，R 6，R 7和R 8，R 8， >具有说明书中给出的含义，是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。本发明的具体化合物也被发现是Pim-1的抑制剂。

6. 发明申请

WO1995013267A1 PYRIMIDINE-THIOALKYL AND ALKYLETHER COMPOUNDS 审中-公开
标题翻译：哌嗪 - 噻二醇和烷基化合物
公开(公告)号：WO1995013267A1
公开(公告)日：1995-05-18
申请号：PCT/US1994012713
申请日：1994-11-09
申请人： THE UPJOHN COMPANY , NUGENT, Richard, A. , SCHLACHTER, Stephen, T. , MURPHY, Michael, J. , MORRIS, Joel , THOMAS, Richard, C. , WISHKA, Donn, G. , REUSSER, Fritz , CLEEK, Gary, J. , ALTHAUS, Irene, Wilson
发明人： THE UPJOHN COMPANY
IPC分类号： C07D239/46
CPC分类号： C07D239/47 , A61K31/505 , C07D239/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R4 is selected from the group consisting of -H or -NR15R16 where R15 is -H and R16 is -H, C1-C6 alkyl, -NH2 or R15 and R16 taken together with the -N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R6 is selected from the group consisting of -H, or halo (preferably -Cl); with the overall proviso that R4 and R6 are not both -H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
摘要翻译：本发明涉及式（I）的嘧啶 - 硫代烷基和烷基醚化合物和式（IA）的嘧啶 - 硫代烷基和烷基醚，即式（I）的化合物，其中R 4选自-H或-NR 15 R 16 其中R 15为-H且R 16为-H，C 1 -C 6烷基，-NH 2或R 15和R 16与-N形式的1-吡咯烷子基，1-吗啉代或1-哌啶子基一起使用; 并且R 6选自-H或卤素（优选-Cl）; 其总体条件是R4和R6不是-H。式（IA）的化合物可用于治疗HIV阳性的个体。

7. 发明申请

WO2010039825A2 IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-a]吡啶化合物作为受体酪氨酸激酶抑制剂
公开(公告)号：WO2010039825A2
公开(公告)日：2010-04-08
申请号：PCT/US2009/059017
申请日：2009-09-30
申请人： ARRAY BIOPHARMA INC. , ALLEN, Shelley , MARMSATER, Fredrik, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , LYSSIKATOS, Joseph, P.
发明人： ALLEN, Shelley , MARMSATER, Fredrik, P. , ROBINSON, John, E. , SCHLACHTER, Stephen, T. , LYSSIKATOS, Joseph, P.
IPC分类号： C07D487/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1.
摘要翻译：具有化学名称的顺式-6-氟-8-（3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶的式I和II化合物：吡啶-3-基）喹啉和6-氟-8-（反式-3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶-3-基）喹啉和对映异构体及其药学上可接受的盐是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。本发明的化合物也被发现是Pim-1的抑制剂。

8. 发明申请

WO2010022076A1 TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS 审中-公开
标题翻译：三唑啉化合物作为PIM激酶抑制剂
公开(公告)号：WO2010022076A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054193
申请日：2009-08-18
申请人： ARRAY BIOPHARMA INC. , ALLEN, Shelley , CELESTE, Laura L. , DAVIS, T. Gregg , DELISLE, Robert Kirk , GRESCHUK, Julie Marie , GROSS, Stefan, D. , HICKEN, Erik, James , JACKSON, Leila, J. , LYSSIKATOS, Joseph, P. , KALLAN, Nicholas C. , MARMSATER, Fredrik, P. , MUNSON, Mark, C. , PHENEGER, Jed , RAST, Bryson , ROBINSON, John, E. , SCHLACHTER, Stephen T. , TOPALOV, George T. , WRIGHT, A. Dale , ZHAO, Qian
发明人： ALLEN, Shelley , CELESTE, Laura L. , DAVIS, T. Gregg , DELISLE, Robert Kirk , GRESCHUK, Julie Marie , GROSS, Stefan, D. , HICKEN, Erik, James , JACKSON, Leila, J. , LYSSIKATOS, Joseph, P. , KALLAN, Nicholas C. , MARMSATER, Fredrik, P. , MUNSON, Mark, C. , PHENEGER, Jed , RAST, Bryson , ROBINSON, John, E. , SCHLACHTER, Stephen T. , TOPALOV, George T. , WRIGHT, A. Dale , ZHAO, Qian
IPC分类号： C07D471/04 , A61K31/47
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
摘要翻译：其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫细胞相关的受体酪氨酸抑制剂疾病和病症，如炎性和自身免疫性疾病。

9. 发明申请

WO1995011235A1 PYRIMIDINONES AS ANTIARTHRITIC AND ANTI-INFLAMMATORIES 审中-公开
标题翻译：吡咯烷酮作为抗炎和抗炎药
公开(公告)号：WO1995011235A1
公开(公告)日：1995-04-27
申请号：PCT/US1994010571
申请日：1994-09-21
申请人： THE UPJOHN COMPANY , NUGENT, Richard, Allen , SCHLACHTER, Stephen, T.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D239/36
CPC分类号： C07D239/36 , C07D239/47 , C07D239/52 , C07D239/56 , C07F9/6512
摘要： Compounds useful in the treatment of inflammation structurally represented as formula (I) or pharmaceutically acceptable salts thereof, wherein R is a) (CH2)n-Y i) where n is 1 then Y is C1-C6 alkoxy, morpholinyl, piperdinyl, pyrrolidinyl, phenoxy, phenylthio, phenylsulfonyl, phenylsulfinyl, -NHC(O)-C1-C6 carboxylic acid, N3, NH2, diethylamino, hydrogen (provided R is benzyloxy), halogen (provided R is a C1-C6 alkyl) or CH("EWG")2 where "EWG" is an electron withdrawing group each individually selected from the group consisting of CO2R or PO(OR )2, or ii) n is 2 then Y is CH("EWG")2, or b) a terminal olefin substituted with i) an aryl or heteroaryl, ii) hydroxyl and a C1-C6 alkyl, phenyl or (CH2)m-CO2R where m is 1 to 3, or c) C3-C6 cycloalkyl (optionally substituted with a halogen, (PO(OC2H5)2)2 or CN); R is hydrogen or C1-C6 alkyl; R is hydrogen, hydroxyl, C1-C6 alkyl, alkoxy, benzyloxy or phenoxy; R is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, phenoxy, C1-C6 alkylthio, thiophenyl, NH2, aryl (except that R is other than phenyl when R and Y are both hydrogen) or heteroaryl; R is H, C1-C6 alkyl, benzyl, phenyl, phenyl substituted with one to five F, C1, Br, I, NO2, OCH3 or C1-C4 alkyl; and R is H, C1-C6 alkyl, benzyl, phenyl, phenyl substituted with one to five F, C1, Br, I, NO2, OCH3 or C1-C4 alkyl, or where both R 's are taken together to form a CH2-CH2, CH2-CH2-CH2 or CH2-C(CH3)2-CH2 whereby a heterocyclic ring containing the bonded P atom and the two O atoms is formed. The compounds are useful as anti-inflammatory and antiarthritic agents.
摘要翻译：用于治疗结构上用式（I）表示的炎症的化合物或其药学上可接受的盐，其中R 2是a）（CH 2）n Y i）其中n是1，则Y是C 1 -C 6烷氧基，吗啉基，哌啶基，吡咯烷基，苯氧基，苯硫基，苯基磺酰基，苯基亚磺酰基，-NHC（O）-C1-C6羧酸，N3，NH2，二乙基氨基，氢（条件是R 4是苄氧基），卤素（R 3是C1- C6烷基）或CH（“EWG”）2，其中“EWG”是各自分别选自CO 2 R 6或PO（OR 7））2的吸电子基团，或ii）n是2，然后是Y 是CH（“EWG”）2，或b）用i）芳基或杂芳基取代的末端烯烃，ii）羟基和C 1 -C 6烷基，苯基或（CH 2）m -CO 2 R 6，其中m为1至 3，或c）C 3 -C 6环烷基（任选被卤素取代，（PO（OC 2 H 5）2）2或CN）; R 3是氢或C 1 -C 6烷基; R 4是氢，羟基，C 1 -C 6烷基，烷氧基，苄氧基或苯氧基; R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，苯氧基，C 1 -C 6烷硫基，噻吩基，NH 2，芳基（R 4和R 4不同之处在于R 5不是苯基氢）或杂芳基; R 6是H，C 1 -C 6烷基，苄基，苯基，被1至5个F，C 1，Br，I，NO 2，OCH 3或C 1 -C 4烷基取代的苯基; R 7为H，C 1 -C 6烷基，苄基，苯基，被1至5个F，Cl，Br，I，NO 2，OCH 3或C 1 -C 4烷基取代的苯基，或其中两个R 7为一起形成CH2-CH2，CH2-CH2-CH2或CH2-C（CH3）2-CH2，由此形成含有键合的P原子和两个O原子的杂环。该化合物可用作抗炎和抗关节炎药物。

10. 发明申请

WO2010039825A3 IMIDAZO [1, 2-A] PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-A]吡啶化合物作为受体酪氨酸激酶抑制剂
公开(公告)号：WO2010039825A3
公开(公告)日：2010-10-07
申请号：PCT/US2009059017
申请日：2009-09-30
申请人： ARRAY BIOPHARMA INC , ALLEN SHELLEY , MARMSATER FREDRIK P , ROBINSON JOHN E , SCHLACHTER STEPHEN T , LYSSIKATOS JOSEPH P
发明人： ALLEN SHELLEY , MARMSATER FREDRIK P , ROBINSON JOHN E , SCHLACHTER STEPHEN T , LYSSIKATOS JOSEPH P
IPC分类号： C07D487/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1.
摘要翻译：具有化学名称的顺式-6-氟-8-（3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶的式I和II化合物：吡啶-3-基）喹啉和6-氟-8-（反式-3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶-3-基）喹啉和对映异构体及其药学上可接受的盐是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。本发明的化合物也被发现是Pim-1的抑制剂。

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