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1. 发明申请

WO2007146376A3 SUBSTITUTED 3-CYANOPYRIDINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：替代3-氰基吡啶作为蛋白激酶抑制剂
公开(公告)号：WO2007146376A3
公开(公告)日：2008-03-13
申请号：PCT/US2007013954
申请日：2007-06-13
申请人： WYETH CORP , COLE DEREK CECIL , BOSCHELLI DIANE HARRIS , WANG YANONG DANIEL , ASSELIN MAGDA , JOSEPH-MCARTHY DIANE MARIE , PRASHAD AMARNAUTH SHASTRIE , WISSNER ALLAN , DUSHIN RUSSELL , WU BIQI , TUMEY LAWRENCE NATHAN , NIU CHUAN S , CHEN JOAN
发明人： COLE DEREK CECIL , BOSCHELLI DIANE HARRIS , WANG YANONG DANIEL , ASSELIN MAGDA , JOSEPH-MCARTHY DIANE MARIE , PRASHAD AMARNAUTH SHASTRIE , WISSNER ALLAN , DUSHIN RUSSELL , WU BIQI , TUMEY LAWRENCE NATHAN , NIU CHUAN S , CHEN JOAN
IPC分类号： C07D213/85 , A61K31/465 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present teachings provide compounds of formula I or a pharmaceutically acceptable salt, hydrate, or ester thereof, wherein: X is selected from a) -NR 3 -Y-, b) -O-Y-, c) -S(O) m -Y-, d) -S(O) m NR 3 - Y-, e) -NR 3 S(O) m -Y-, f) -C(O)NR 3 -Y-, g) -C(S)NR 3 -Y-, h) -NR 3 C(O)- Y-, i) -NR 3 C(S)-Y-, j) -C(O)O-Y-, k) -OC(O)-Y-, and I) a covalent bond; Y, at each occurrence, independently is selected from a) a divalent C 1-10 to alkyl group, b) a divalent C 2-10 alkenyl group, c) a divalent C 2-10 alkynyl group, d) a divalent C 1-10 haloalkyl group, and e) a covalent bond; R 1 is selected from a) a C 1-10 alkyl group, b) a C 3-14 cycloalkyl group, c) a 3-14 membered cycloheteroalkyl group, d) a C 8-14 polycyclic aryl group and e) a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 -Y-R 4 ; R 2 is a C 6-14 aryl group or a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 groups independently selected from -Y-R 4 Or -O-Y-R 4 . The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐，水合物或酯，其中：X选自a）-NR 3 -Y-，b）-OY-，c） -S（O）m -Y-，d）-S（O）m NR 3 - ， - Y - ， - S（O）m -Y-，f）-C（O）NR 3 -Y-，g）-C（S）（O）-Y-，i）-NR 3 -Y-，h）-NR 3 C（O）-Y-，i）-NR 3 -S（S） - Y-，j）-C（O）OY-，k）-OC（O）-Y-，和I）共价键; Y在每次出现时独立地选自a）二价C 1-10烷基，b）二价C 2〜2-烯基，c）a 二价C 2-10炔基，d）二价C 1-10 1-10卤代烷基，和e）共价键; R 1选自a）C 1-10烷基，b）C 3-14环烷基，c）3 -14元环杂烷基，d）C 8-14多环芳基和e）5-14元杂芳基，其中每个基团任选被1-4 -OR 4取代 ; R 2是C 6-14芳基或5-14元杂芳基，其中每个基团任选被1-4个独立地选自-YR SUP> 4或-OYR <4> 。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

2. 发明申请

WO2007146323A2 SUBSTITUTED CYANOPYRIDINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：替代的CYANOPYRIDINES作为蛋白激酶抑制剂
公开(公告)号：WO2007146323A2
公开(公告)日：2007-12-21
申请号：PCT/US2007013851
申请日：2007-06-13
申请人： WYETH CORP , WANG YANONG DANIEL , PRASHAD AMARNAUTH SHASTRIE , ASSELIN MAGDA , BOSCHELLI DIANE HARRIS , DUSHIN RUSSELL , COLE DEREK CECIL , WISSNER ALLAN
发明人： WANG YANONG DANIEL , PRASHAD AMARNAUTH SHASTRIE , ASSELIN MAGDA , BOSCHELLI DIANE HARRIS , DUSHIN RUSSELL , COLE DEREK CECIL , WISSNER ALLAN
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present teachings provide compounds of formula I XR R2 XN and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I的化合物XR R2 XN及其药学上可接受的盐，水合物和酯，其中R1，R2和X如本文所定义。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

3. 发明申请

WO2009076602A1 5-ALKYL/ALKENYL-3-CYANOPYRIDINES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的5-烷基/亚苄基-3-氰基吡啶
公开(公告)号：WO2009076602A1
公开(公告)日：2009-06-18
申请号：PCT/US2008086594
申请日：2008-12-12
申请人： WYETH CORP , TUMEY LAWRENCE NATHAN , BOSCHELLI DIANE HARRIS , BHAGIRATH NIALA , CHEN JOAN JOWEN , FLOYD MIDDLETON BRAWNER , LI ZHONG , NIU CHUANSHENG , SHIM JAECHUL , WANG YAN , WANG YANONG DANIEL , WU BIQI , EID CLARK N
发明人： TUMEY LAWRENCE NATHAN , BOSCHELLI DIANE HARRIS , BHAGIRATH NIALA , CHEN JOAN JOWEN , FLOYD MIDDLETON BRAWNER , LI ZHONG , NIU CHUANSHENG , SHIM JAECHUL , WANG YAN , WANG YANONG DANIEL , WU BIQI , EID CLARK N
IPC分类号： C07D401/12 , A61K31/465 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/00 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14
摘要： Described herein are compounds of formula I: wherein G is and pharmaceutically acceptable salts thereof, wherein J, X, R1, R2, R1 1, R12' and p are as defined herein. Also provided herein are methods of making the compounds of formula I, and methods of using these compounds for inhibiting or treating a pathological condition or disorder linked to or mediated by a protein kinase in a mammal.
摘要翻译：本文描述的是式I的化合物：其中G是其药学上可接受的盐，其中J，X，R 1，R 2，R 1，R 12'和p如本文所定义。本文还提供了制备式I化合物的方法，以及使用这些化合物抑制或治疗哺乳动物中与蛋白激酶相关或介导的病理状况或病症的方法。

4. 发明申请

WO2006023395A3 4-(2,4-DICHLORO-5-METHOXYPHENYL)AMINO-6-METHOXY-7-{[5-(SUBSTITUTED-AMINO)METHYL]-3-FURYL}-3-QUINOLINECARBONITRILES AS KINASE INHIBITORS 审中-公开
标题翻译： 4-（2,4-二氯-5-甲氧基苯基）氨基-6-甲氧基-7 - {[5-（取代的氨基）甲基] -3-呋喃基} -3-喹唑啉酮作为激酶抑制剂
公开(公告)号：WO2006023395A3
公开(公告)日：2006-06-08
申请号：PCT/US2005028758
申请日：2005-08-12
申请人： WYETH CORP , BOSCHELLI DIANE HARRIS , ALIMARDANOV ASAF , WU BIQI , AFRAGOLA JAY THOMAS
发明人： BOSCHELLI DIANE HARRIS , ALIMARDANOV ASAF , WU BIQI , AFRAGOLA JAY THOMAS
IPC分类号： C07D405/04 , A61K31/4709 , A61P35/00 , C07D405/14
CPC分类号： C07D405/04 , C07D405/14
摘要： This invention relates to compounds having the structure of Formula (I) wherein R 1 , R 2 , R 3 , and R 4 are described herein.
摘要翻译：本发明涉及具有式（I）结构的化合物，其中R 1，R 2，R 3，R 4和R 4 在此描述。

5. 发明申请

WO2004048386A3 THIENO[3,2-b]PYRIDINE-6-CARBONITRILES AND THIENO[2,3-b]PYRIDINE-5-CARBONITRILES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：噻吩并[3,2-b]吡啶-6-羰基和噻吩并[2,3-b]吡啶-5-羰基酮作为蛋白激酶抑制剂
公开(公告)号：WO2004048386A3
公开(公告)日：2004-10-07
申请号：PCT/US0336206
申请日：2003-11-14
申请人： WYETH CORP , BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
发明人： BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
IPC分类号： A61P9/10 , A61P13/12 , A61P19/10 , A61P35/00 , C07D495/04 , A61K31/4365
CPC分类号： C07D495/04
摘要： This invention provides compounds of Formula (1 a) - (1f) wherein:X, R , and R are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection and process for producing said compounds.
摘要翻译：本发明提供式（1a） - （1f）的化合物，其中：X，R 1和R 2在本说明书中定义，其可用于治疗癌症，中风，骨质疏松症，多囊肾疾病，自身免疫性疾病，类风湿性关节炎和移植排斥反应以及用于制备所述化合物的方法。

6. 发明申请

WO2005113560A2 THIENO[3,2-b]PYRIDINE-6-CARBONITRILES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：噻吩并[3,2-b]吡啶-6-羰基酮作为蛋白激酶抑制剂
公开(公告)号：WO2005113560A2
公开(公告)日：2005-12-01
申请号：PCT/US2005016150
申请日：2005-05-10
申请人： WYETH CORP , BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
发明人： BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , A61K31/44 , A61K31/497 , A61K31/535
摘要： This invention provides compounds of Formula II: (I) wherein: R , R and X are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, myocardial infarction, neuropathic pain, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection. The invention also provides processes for producing said compounds.
摘要翻译：本发明提供式II化合物：（I）其中：R 1，R 2和X在本说明书中定义，其可用于治疗癌症，中风，心肌梗塞，神经性疼痛，骨质疏松症，多囊肾病，自身免疫性疾病，类风湿性关节炎和移植排斥反应。本发明还提供了生产所述化合物的方法。

7. 发明申请

WO2004048386A9 THIENO[3,2-b]PYRIDINE-6-CARBONITRILES AND THIENO[2,3-b]PYRIDINE-5-CARBONITRILES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：噻吩并[3,2-b]吡啶-6-羰基和噻吩并[2,3-b]吡啶-5-羰基酮作为蛋白激酶抑制剂
公开(公告)号：WO2004048386A9
公开(公告)日：2005-07-14
申请号：PCT/US0336206
申请日：2003-11-14
申请人： WYETH CORP , BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
发明人： BOSCHELLI DIANE HARRIS , ZHANG NAN , BARRIOS SOSA ANA CAROLINA , DURUTLIC HARIS , WU BIQI
IPC分类号： A61P9/10 , A61P13/12 , A61P19/10 , A61P35/00 , C07D495/04 , A61K31/4365
CPC分类号： C07D495/04
摘要： This invention provides compounds of Formula (1 a) - (1f) wherein:X, R , and R are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection and process for producing said compounds.
摘要翻译：本发明提供式（1a） - （1f）的化合物，其中：X，R 1和R 2在本说明书中定义，其可用于治疗癌症，中风，骨质疏松症，多囊肾疾病，自身免疫性疾病，类风湿性关节炎和移植排斥反应以及用于制备所述化合物的方法。

8. 发明申请

WO2005019201A3 PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES 审中-公开
标题翻译：制备4-氨基-3-喹啉酮的方法
公开(公告)号：WO2005019201A3
公开(公告)日：2005-08-04
申请号：PCT/US2004026329
申请日：2004-08-13
申请人： WYETH CORP , WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
发明人： WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
IPC分类号： C07D215/54 , C07D405/04 , C07D495/04
CPC分类号： C07D405/04 , C07D215/54 , C07D495/04
摘要： This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
摘要翻译：本发明公开了一种制备4-氨基-3-喹啉腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与醇溶剂和原甲酸三烷基酯中的任选的上述四取代的苯胺缩合，得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与磷酰氯在乙腈，丁腈，甲苯或二甲苯中，任选在催化剂存在下合并，得到4-氨基-3-喹啉腈，并公开了制备7-氨基 - 噻吩并[ 3,2-b]吡啶-6-甲腈，其包括将3-氨基噻吩与氰基乙酰胺组合并在醇溶剂中试验草酸甲酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和还公开了一种制备4氨基-3-喹啉腈的方法，包括：将胺化合物与氰基乙酸和肽偶联剂混合以获得悬浮液; 过滤悬浮液; 得到氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合，得到4-氨基-3-喹啉腈，本发明公开了一种获得氰基乙酰胺的方法。

9. 发明申请

WO9833798A3 PYRIDO (2,3-D) PYRIMIDINES AND 4-AMINOPYRIMIDINES AS INHIBITORS OF CELLULAR PROLIFERATION 审中-公开
标题翻译：吡咯烷（2,3-D）嘧啶和4-氨基嘧啶作为细胞增殖的抑制剂
公开(公告)号：WO9833798A3
公开(公告)日：1998-11-05
申请号：PCT/US9801343
申请日：1998-01-26
申请人： WARNER LAMBERT CO , BOSCHELLI DIANE HARRIS , DOBRUSIN ELLEN MYRA , DOHERTY ANNETTE MARIAN , FATTACY ALI , FRY DAVID W , BARVIAN MARK R , KALLMEYER SUSANNE TRUMPP , WU ZHIPEI
发明人： BOSCHELLI DIANE HARRIS , DOBRUSIN ELLEN MYRA , DOHERTY ANNETTE MARIAN , FATTACY ALI , FRY DAVID W , BARVIAN MARK R , KALLMEYER SUSANNE TRUMPP , WU ZHIPEI
IPC分类号： A61K31/505 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P17/06 , A61P35/00 , A61P43/00 , C07D239/46 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D471/00
CPC分类号： C07D239/47 , C07D239/48 , C07D471/04
摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 4-aminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II), where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R?8 and R9¿ include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.

10. 发明专利

BRPI0712737A2 未知
公开(公告)号：BRPI0712737A2
公开(公告)日：2012-05-08
申请号：BRPI0712737
申请日：2007-06-13
申请人： WYETH CORP
发明人： COLE DEREK CECIL , BOSCHELLI DIANE HARRIS , WANG YANONG DANIEL , ASSELIN MAGDA , JOSEPH-MCARTHY DIANE MARIE , PRASHAD AMARNAUTH SHASTRIE , WISSNER ALLAN , DUSHIN RUSSELL , WU BIQI , TUMEY LAWRENCE NATHAN , NIU CHUAN S , CHEN JOAN
IPC分类号： C07D213/85 , A61K31/465 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present teachings provide compounds of formula I or a pharmaceutically acceptable salt, hydrate, or ester thereof, wherein: X is selected from a) -NR 3 -Y-, b) -O-Y-, c) -S(O) m -Y-, d) -S(O) m NR 3 - Y-, e) -NR 3 S(O) m -Y-, f) -C(O)NR 3 -Y-, g) -C(S)NR 3 -Y-, h) -NR 3 C(O)- Y-, i) -NR 3 C(S)-Y-, j) -C(O)O-Y-, k) -OC(O)-Y-, and I) a covalent bond; Y, at each occurrence, independently is selected from a) a divalent C 1-10 to alkyl group, b) a divalent C 2-10 alkenyl group, c) a divalent C 2-10 alkynyl group, d) a divalent C 1-10 haloalkyl group, and e) a covalent bond; R 1 is selected from a) a C 1-10 alkyl group, b) a C 3-14 cycloalkyl group, c) a 3-14 membered cycloheteroalkyl group, d) a C 8-14 polycyclic aryl group and e) a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 -Y-R 4 ; R 2 is a C 6-14 aryl group or a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 groups independently selected from -Y-R 4 Or -O-Y-R 4 . The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

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