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1. 发明申请

WO2007078813A8 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR ß-SECRETASE MODULATION 审中-公开
标题翻译： 2-氨基-5-PIPERIDINLIMIDAZOLONE化合物及其用于β-分泌酶调节
公开(公告)号：WO2007078813A8
公开(公告)日：2007-10-04
申请号：PCT/US2006047673
申请日：2006-12-14
申请人： WYETH CORP , ZHOU PING , BERNOTAS RONALD CHARLES , LI YANFANG , NOWAK PAWEL WOJCIECH , COLE DEREK CECIL , MANAS ERIC STEVEN , FAN YI , YAN YINFA
发明人： ZHOU PING , BERNOTAS RONALD CHARLES , LI YANFANG , NOWAK PAWEL WOJCIECH , COLE DEREK CECIL , MANAS ERIC STEVEN , FAN YI , YAN YINFA
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14
摘要： The present invention provides a 2-amino-5-piperidinylimidazolone compound of formula (I) The present invention also provides methods and compositions for the inhibition of ß-secretase (BACE) and the treatment of ß-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供式（I）的2-氨基-5-哌啶基咪唑酮化合物本发明还提供抑制β-分泌酶（BACE）和β-淀粉样蛋白沉积物和神经原纤维缠结的治疗方法和组合物。

2. 发明申请

WO2007078813A2 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR (INSERT BETA SYMBOL)-SECRETASE MODULATION 审中-公开
标题翻译： 2-氨基-5-哌啶基咪唑啉酮化合物及其用途（插入式符号）-SECRETASE调节
公开(公告)号：WO2007078813A2
公开(公告)日：2007-07-12
申请号：PCT/US2006047673
申请日：2006-12-14
申请人： WYETH CORP , ZHOU PING , BERNOTAS RONALD CHARLES , LI YANFANG , NOWAK PAWEL WOJCIECH , COLE DEREK CECIL , MANAS ERIC STEVEN , FAN YI , YAN YINFA
发明人： ZHOU PING , BERNOTAS RONALD CHARLES , LI YANFANG , NOWAK PAWEL WOJCIECH , COLE DEREK CECIL , MANAS ERIC STEVEN , FAN YI , YAN YINFA
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14
摘要： The present invention provides a 2-amino-5-piperidinylimidazolone compound of formula ( I ) The present invention also provides methods and compositions for the inhibition of ß-secretase (BACE) and the treatment of ß-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供式（I）的2-氨基-5-哌啶基咪唑酮化合物本发明还提供抑制β-分泌酶（BACE）和β-淀粉样沉积物和神经原纤维缠结的治疗的方法和组合物。

3. 发明申请

WO2008115974A3 PYRAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS 审中-公开
标题翻译：吡唑并嘧啶类似物及其作为MTOR激酶和PI3激酶抑制剂的用途
公开(公告)号：WO2008115974A3
公开(公告)日：2008-12-18
申请号：PCT/US2008057467
申请日：2008-03-19
申请人： WYETH CORP , ZASK ARIE , NOWAK PAWEL WOJCIECH , VERHEIJEN JEROEN , CURRAN KEVIN J , KAPLAN JOSHUA , MALWITZ DAVID , BURSAVICH MATTHEW GREGORY , COLE DEREK CECIL , AYRAL-KALOUSTIAN SEMIRAMIS , YU KER , RICHARD DAVID JAMES , LEFEVER MARK
发明人： ZASK ARIE , NOWAK PAWEL WOJCIECH , VERHEIJEN JEROEN , CURRAN KEVIN J , KAPLAN JOSHUA , MALWITZ DAVID , BURSAVICH MATTHEW GREGORY , COLE DEREK CECIL , AYRAL-KALOUSTIAN SEMIRAMIS , YU KER , RICHARD DAVID JAMES , LEFEVER MARK
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR -related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. The invention also relates to treating PI3K -related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog.
摘要翻译：本发明涉及吡唑并嘧啶类似物，制备吡唑并嘧啶类似物的方法，包含吡唑并嘧啶类似物的组合物和治疗mTOR相关病症的方法，包括向有需要的受试者施用有效量的吡唑并嘧啶类似物。本发明还涉及治疗PI3K相关疾病，包括向有需要的受试者施用有效量的吡唑并嘧啶类似物。

4. 发明申请

WO2007136668A9 N-BENZOYL-AND N-BENZYLPYRROLIDIN-3-YLAMINES AS HISTAMINE-3 ANTAGONISTS 审中-公开
标题翻译：作为组胺-3拮抗剂的N-苯甲酰和N-苄氧基吡咯烷-3-基
公开(公告)号：WO2007136668A9
公开(公告)日：2008-03-27
申请号：PCT/US2007011765
申请日：2007-05-16
申请人： WYETH CORP , COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , KIM JI-IN
发明人： COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , KIM JI-IN
IPC分类号： C07D207/12 , A61K31/4025 , A61K31/404 , A61K31/433 , A61K31/517 , A61K31/52 , A61P25/00 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D473/34 , C07D495/04
CPC分类号： C07D207/14 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound of Formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式（I）化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统疾病的用途。

5. 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。

6. 发明申请

WO2007136668A2 N-BENZOYL-AND N-BENZYLPYRROLIDIN-3-YLAMINES AS HISTAMINE-3 ANTAGONISTS 审中-公开
标题翻译：作为组胺-3拮抗剂的N-苯甲酰和N-苄氧基吡咯烷-3-基
公开(公告)号：WO2007136668A2
公开(公告)日：2007-11-29
申请号：PCT/US2007011765
申请日：2007-05-16
申请人： WYETH CORP , COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , KIM JI-IN
发明人： COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , KIM JI-IN
IPC分类号： C07D207/12 , A61K31/4025 , A61K31/404 , A61K31/433 , A61K31/517 , C07D401/12 , C07D473/34 , C07D495/04
CPC分类号： C07D207/14 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound of Formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式（I）化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统疾病的用途。

7. 发明申请

WO2007108936A3 N-SUBSTITUTED-AZACYCLYLAMINES AS HISTAMINE-3 ANTAGONISTS 审中-公开
标题翻译：作为组胺-3拮抗剂的N-取代 - 亚胺基亚胺
公开(公告)号：WO2007108936A3
公开(公告)日：2007-11-01
申请号：PCT/US2007005776
申请日：2007-03-08
申请人： WYETH CORP , COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , ROBICHAUD ALBERT JEAN , KIM JI-IN , SOLVIBILE WILLIAM RONALD , GROSS JONATHAN LAIRD
发明人： COLE DEREK CECIL , ASSELIN MAGDA , STOCK JOSEPH RAYMOND , ROBICHAUD ALBERT JEAN , KIM JI-IN , SOLVIBILE WILLIAM RONALD , GROSS JONATHAN LAIRD
IPC分类号： C07D401/10 , A61K31/404 , A61P25/00 , C07D403/10 , C07D471/04 , C07D471/14
CPC分类号： C07D403/10 , C07D401/10 , C07D471/04 , C07D471/14
摘要： The present invention provides a compound of formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式（I）化合物及其用于治疗与组胺-3受体相关或受其组合的受体的中枢神经系统病症的用途。

8. 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。

9. 发明申请

WO02051837A3 HETEROCYCLINDAZOLE AND AZAINDAZOLE COMPOUNDS AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基木聚糖-6配位体的杂环化合物和唑烷化合物
公开(公告)号：WO02051837A3
公开(公告)日：2003-01-16
申请号：PCT/US0147935
申请日：2001-12-11
申请人： WYETH CORP
发明人： ZHOU PING , COLE DEREK CECIL , KELLY MICHAEL GERARD , LENNOX WILLIAM JOSEPH
IPC分类号： C07D487/04 , A61K31/381 , A61K31/404 , A61K31/4188 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4985 , A61P1/04 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/04 , C07D403/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D513/04 , A61K31/40 , A61K31/435 , A61K31/44
CPC分类号： C07D401/04 , A61K31/404 , A61K31/427 , A61K31/454 , A61K31/4545 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I) and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式（I）化合物及其在治疗与5-HT 6受体有关或受其影响的病症中的用途。

10. 发明申请

WO03050063A2 PROCESS FOR THE SYNTHESIS OF CHIRALLY PURE beta -AMINO-ALCOHOLS 审中-公开
标题翻译：合成纯度β-氨基醇的方法
公开(公告)号：WO03050063A2
公开(公告)日：2003-06-19
申请号：PCT/US0238119
申请日：2002-11-26
申请人： WYETH CORP
发明人： KREFT ANTHONY FRANK , ANTANE MADELENE MIYOKO , COLE DEREK CECIL , KUBRAK DENNIS MARTIN , RESNICK LYNN , STOCK JOSEPH RAYMOND , WANG ZHENG
IPC分类号： A61K31/381 , C07B53/00 , C07B61/00 , C07C209/00 , C07C213/00 , C07C215/08 , C07C227/04 , C07C229/08 , C07C247/12 , C07D227/12 , C07D263/26 , C07D333/32 , C07D333/34 , C07C
CPC分类号： C07C215/20 , C07B2200/07 , C07C215/08 , C07C215/24 , C07C215/28 , C07C215/56 , C07C229/08 , C07C229/28 , C07C229/30 , C07C229/36 , C07C247/12 , C07C323/63 , C07D263/26 , C07D333/34
摘要： A process is provided for preparing chirally pure S-enantiomers of alpha -amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the Formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an alpha -azido acid; h) reducing the alpha -azido acid to the alpha -amino acid; and i) recrystallizing the alpha -amino acid to the chirally pure alpha -amino acid. A process is also provided for preparing chirally pure S-enantiomers of beta -amino alcohols further comprising the steps of reducing the crude alpha -amino acid to the beta -amino alcohol and recrystallizing the beta -amino alcohol to the chirally pure beta -amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl beta -amino alcohols further comprising the steps of sulfonylating the beta -amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl beta -amino alcohols.
摘要翻译：提供了制备α-氨基酸的手性纯的S-对映异构体的方法，包括以下步骤：a）由式（R）2CH（CH 2）n CH 2 X的烷基卤制备有机金属试剂; b）将有机金属试剂加入到二氧化碳中，得到羧酸; c）在叔胺碱存在下用酰氯，三氯化磷，酸酐或亚硫酰氯活化羧酸; d）使步骤c）的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e）用强非亲核碱处理步骤d）的产物以形成烯醇化物阴离子; f）用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子，得到恶唑烷酮叠氮化物; g）用碱水溶液水解恶唑烷酮叠氮化物，得到α-叠氮酸; h）将α-叠氮酸还原成α-氨基酸; 和i）将α-氨基酸重结晶到手性纯的α-氨基酸。还提供了制备β-氨基醇的手性纯的S-对映异构体的方法，该方法还包括将α-氨基酸粗制还原成β-氨基醇并将β-氨基醇重结晶至手性纯的β-氨基醇。还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法，其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。

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