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11. 发明申请

WO2004092155A1 FLUORO-AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 审中-公开
标题翻译：含氟和含三氟甲磺酸的苯甲酰胺酰胺抑制剂的制备及其衍生物
公开(公告)号：WO2004092155A1
公开(公告)日：2004-10-28
申请号：PCT/US2004/009268
申请日：2004-03-26
申请人： WYETH , KREFT, Anthony, Frank , RESNICK, Lynn , MAYER, Scott, Christian , DIAMANTIDIS, George , COLE, Derek, Cecil , WANG, Tingzhong , GALANTE, Rocco, John , HOKE, Molly , HARRISON, Boyd, Lynn , ZHANG, Minsheng
发明人： KREFT, Anthony, Frank , RESNICK, Lynn , MAYER, Scott, Christian , DIAMANTIDIS, George , COLE, Derek, Cecil , WANG, Tingzhong , GALANTE, Rocco, John , HOKE, Molly , HARRISON, Boyd, Lynn , ZHANG, Minsheng
IPC分类号： C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 )nalkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; N = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

12. 发明申请

WO2007038519A1 THIENO[2,3-B]PYRIDINE-5-CARBONITRILES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的噻吩并[2,3-B]吡啶-5-羰基
公开(公告)号：WO2007038519A1
公开(公告)日：2007-04-05
申请号：PCT/US2006/037502
申请日：2006-09-27
申请人： WYETH , BOSCHELLI, Diane, Harris , COLE, Derek, Cecil , ASSELIN, Magda , BARRIOS SOSA, Ana, Carolina , WU, Biqi , TUMEY, Lawrence, Nathan
发明人： BOSCHELLI, Diane, Harris , COLE, Derek, Cecil , ASSELIN, Magda , BARRIOS SOSA, Ana, Carolina , WU, Biqi , TUMEY, Lawrence, Nathan
IPC分类号： C07D495/04 , A61K31/4365 , A61P37/06
CPC分类号： C07D495/04
摘要： Disclosed are compounds of Formula I: Formula (I); wherein R 1 , R 2 , R 3 , R 4 , and X, are defined hereinbefore in the specification, which can be useful in the treatment of autoimmune and inflammatory diseases, and processes for producing said compounds.
摘要翻译：公开了式I的化合物：式（I）; 其中R 1，R 2，R 3，R 4和X在上文在本说明书中定义，其可用于治疗自身免疫性和炎性疾病，以及用于生产所述化合物的方法。

13. 发明申请

WO2005061477A1 BIARYL SULFONAMIDES AS MMP INHIBITORS 审中-公开
标题翻译： BIARYL SULFONAMIDES作为MMP抑制剂
公开(公告)号：WO2005061477A1
公开(公告)日：2005-07-07
申请号：PCT/US2003/040835
申请日：2003-12-22
申请人： WYETH , LEVIN, Jeremy, Ian , RUSH, Thomas, Saltmarsh, III , LOVERING, Frank , HU, Yonghan , LI, Jianchang , LI, Wei , WU, Jun, Jun , HOTCHANDANI, Rajeev , XIANG, Jason, Shaoyun , DU, Xuemei , COLE, Derek, Cecil
发明人： LEVIN, Jeremy, Ian , RUSH, Thomas, Saltmarsh, III , LOVERING, Frank , HU, Yonghan , LI, Jianchang , LI, Wei , WU, Jun, Jun , HOTCHANDANI, Rajeev , XIANG, Jason, Shaoyun , DU, Xuemei , COLE, Derek, Cecil
IPC分类号： C07D307/85
CPC分类号： C07D235/24 , C07D209/42 , C07D231/14 , C07D235/12 , C07D261/18 , C07D263/58 , C07D277/56 , C07D277/64 , C07D277/68 , C07D285/01 , C07D307/68 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/85 , C07D307/92 , C07D333/34 , C07D333/70 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/06 , C07D495/04
摘要： The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors: Formule (I).
摘要翻译：本发明涉及联芳基磺酰胺及其作为例如金属蛋白酶抑制剂：Formule（I）的用途。

14. 发明申请

WO2005012311A1 N-SULFONYLHETEROCYCLOPYRROLYLALKYLAMINE 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N-磺酰基环己基甲酰胺化合物
公开(公告)号：WO2005012311A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/023993
申请日：2004-07-23
申请人： WYETH , COLE, Derek, Cecil
发明人： COLE, Derek, Cecil
IPC分类号： C07D495/04
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体相关或受其影响的CNS紊乱的治疗用途。

15. 发明申请

WO2003053433A1 INDOLYLALKYLAMINE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基木聚糖-6配体的间苯二酚衍生物
公开(公告)号：WO2003053433A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/040217
申请日：2002-12-17
申请人： WYETH
发明人： COLE, Derek, Cecil , STOCK, Joseph, Raymond , LENNOX, William, Joseph , ZHOU, Ping
IPC分类号： A61K31/4162
CPC分类号： C07D471/04 , C07D513/04
摘要： The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式（I）化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

16. 发明申请

WO2003053970A1 AZAINDOLYLALKYLAMINE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基木聚糖-6配位体的二乙烯基胺衍生物
公开(公告)号：WO2003053970A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/040220
申请日：2002-12-17
申请人： WYETH
发明人： BERNOTAS, Ronald, Charles , COLE, Derek, Cecil , LENNOX, William, Joseph
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/4745
摘要： The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式（I）化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

17. 发明申请

WO2003050063A3 PROCESS FOR THE SYNTHESIS OF CHIRALLY PURE β-AMINO-ALCOHOLS 审中-公开
公开(公告)号：WO2003050063A3
公开(公告)日：2003-06-19
申请号：PCT/US2002/038119
申请日：2002-11-26
申请人： WYETH
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： C07C51/15
摘要： A process is provided for preparing chirally pure S-enantiomers of α-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the Formula (R) 2 CH(CH 2 ) n CH 2 X; 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 α-azido acid; h) reducing the α-azido acid to the α-amino acid; and i) recrystallizing the α-amino acid to the chirally pure α-amino acid. A process is also provided for preparing chirally pure S-enantiomers of β-amino alcohols further comprising the steps of reducing the crude α-amino acid to the β-amino alcohol and recrystallizing the β-amino alcohol to the chirally pure β-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl β-amino alcohols further comprising the steps of sulfonylating the β-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl β-amino alcohols.

18. 发明公开

EP2029543A2 SUBSTITUTED 3-CYANOPYRIDINES AS PROTEIN KINASE INHIBITORS 失效转让
标题翻译：替代3-氰基吡啶ALS蛋白激酶抑制剂
公开(公告)号：EP2029543A2
公开(公告)日：2009-03-04
申请号：EP07796104.3
申请日：2007-06-13
申请人： Wyeth
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) -NR3-Y-, b) -O-Y-, c) -S(O)m-Y-, d) -S(O)mNR3- Y-, e) -NR3S(O)m-Y-, f) -C(O)NR3-Y-, g) -C(S)NR3-Y-, h) -NR3C(O)- Y-, i) -NR3C(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 C1-10 to alkyl group, b) a divalent C2-10 alkenyl group, c) a divalent C2-10 alkynyl group, d) a divalent C1-10 haloalkyl group, and e) a covalent bond; R1 is selected from a) a C 1-10 alkyl group, b) a C3-14cycloalkyl group, c) a 3-14 membered cycloheteroalkyl group, d) a C8-14 polycyclic aryl group and e) a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 -Y-R4; R2 is a C6-14 aryl group or a 5-14 membered heteroaryl group, wherein each group optionally is substituted with 1-4 groups independently selected from -Y-R4 Or -O-Y-R4. 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.

19. 发明授权

EP1692124B1 BIARYL SULFONAMIDES AS MMP INHIBITORS 有权
标题翻译：作为MMP抑制剂的双芳基磺酰胺
公开(公告)号：EP1692124B1
公开(公告)日：2008-10-15
申请号：EP03800062.6
申请日：2003-12-22
申请人： Wyeth
发明人： LEVIN, Jeremy, Ian , RUSH, Thomas, Saltmarsh, III , LOVERING, Frank , HU, Yonghan , LI, Jianchang , LI, Wei , WU, Jun, Jun , HOTCHANDANI, Rajeev , XIANG, Jason, Shaoyun , DU, Xuemei , COLE, Derek, Cecil , TAM, Steve, Yikkai
IPC分类号： C07D307/85 , C07D209/42 , C07D333/70 , C07D413/04 , C07D405/12 , C07D235/24 , C07D277/56 , C07D409/12 , C07D417/04 , C07D495/04 , C07D491/06 , C07D407/04 , C07D405/04 , C07D263/58 , C07D277/68
CPC分类号： C07D235/24 , C07D209/42 , C07D231/14 , C07D235/12 , C07D261/18 , C07D263/58 , C07D277/56 , C07D277/64 , C07D277/68 , C07D285/01 , C07D307/68 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/85 , C07D307/92 , C07D333/34 , C07D333/70 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/06 , C07D495/04
摘要： The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors: Formule (I).
摘要翻译：本发明涉及联芳基磺酰胺及其作为例如金属蛋白酶抑制剂的用途：配方（I）。

20. 发明公开

EP1648891A1 SULFONYLDIHYDROIMID- AZOPYRIDINONE COMPOUNDS AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：磺酰基二氢咪唑 - 氮杂环丁酮化合物作为5-羟基烟酰胺-6配体
公开(公告)号：EP1648891A1
公开(公告)日：2006-04-26
申请号：EP04778629.8
申请日：2004-07-19
申请人： Wyeth
发明人： COLE, Derek, Cecil , BERNOTAS, Ronald, Charles
IPC分类号： C07D471/04 , A61K31/4188
CPC分类号： C07D471/04
摘要： The present invention provides a compound of formula (I) and the use thereof in the ttherapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供了式（I）化合物及其在治疗性治疗与5-HT 6受体相关或受其影响的中枢神经系统疾病中的用途。

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