-
公开(公告)号:WO2016197320A1
公开(公告)日:2016-12-15
申请号:PCT/CN2015/081054
申请日:2015-06-09
申请人: 浙江华海药业股份有限公司
IPC分类号: C07C255/59 , C07C253/30
CPC分类号: C07C253/30 , C07B49/00 , C07B2200/07 , C07C255/59 , C07F3/02
摘要: 本发明涉及一种式IV所示西酞普兰二醇的制备方法,包括以下步骤:在辅助试剂金属盐的存在下,使5-氰基苯酞先后与对氟苯基卤化镁和N,N-二甲基氨基丙基卤化镁在有机溶剂中进行格氏加成反应;反应结束后水解并分离得到式IV所示的西酞普兰二醇。本发明通过添加一种辅助试剂金属盐,显著地改善了格氏反应的活性和选择性,反应收率明显提高。
-
公开(公告)号:WO2014035860A8
公开(公告)日:2015-01-15
申请号:PCT/US2013056566
申请日:2013-08-26
发明人: BUKHTIYAROV YURI , CACATIAN SALVACION , DILLARD LAWRENCE WAYNE , DORNER-CIOSSEK CORNELIA , FUCHS KLAUS , GROSS ULRIKE , HEINE NIKLAS , JIA LANQI , LALA DEEPAK S , MORALES-RAMOS ANGEL , SINGH SURESH B , SAUER ACHIM , VENKATRAMAN SHANKAR , XU ZHENRONG , YUAN JING , ZHAO YI , ZHENG YAJUN
IPC分类号: C07D235/02 , A61K31/4184 , A61P25/28 , C07D401/06 , C07D403/04
CPC分类号: C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the &bgr;- secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of &bgr;-amyloid aggregates.
摘要翻译: 本发明涉及螺环酰基胍及其作为分泌酶(BACE1)活性的抑制剂,含有它们的药物组合物的用途,以及将其用作治疗神经变性疾病的治疗剂的方法,其特征在于认知功能障碍 衰退,认知障碍,痴呆和以淀粉样蛋白聚集体生产为特征的疾病。
-
公开(公告)号:WO2014018881A8
公开(公告)日:2014-12-04
申请号:PCT/US2013052316
申请日:2013-07-26
申请人: BIOGEN IDEC INC
发明人: GUCKIAN KEVIN , KUMARAVEL GNANASAMBANDAM , MA BIN , MI SHA , PENG HAIRUO , SHAO ZHAOHUI , SUN LIHONG , TAVERAS ARTHUR , WANG DEPING , XIN ZHILI , ZHANG LEI
IPC分类号: A61K31/015 , A61K31/4375 , A61K31/44
CPC分类号: C07D451/02 , A61K31/136 , A61K31/196 , A61K31/439 , A61K31/445 , A61K31/46 , A61K31/472 , A61K31/4725 , A61K31/5375 , A61K31/55 , A61K45/06 , C07B2200/07 , C07C217/22 , C07C229/46 , C07C229/48 , C07C255/59 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D209/52 , C07D211/34 , C07D211/62 , C07D217/22 , C07D221/22 , C07D223/06 , C07D295/096 , C07D401/06 , C07D471/08
摘要: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
摘要翻译: 公开了式(I)的双环芳基化合物,其可以调节autotaxin(ATX)酶的活性。 本发明进一步涉及作为ATX抑制剂的化合物,以及制备和使用这些化合物治疗因损伤或疾病引起的脱髓鞘以及治疗增殖性疾病如癌症的方法。
-
公开(公告)号:WO2014060852A3
公开(公告)日:2014-07-24
申请号:PCT/IB2013003031
申请日:2013-10-09
申请人: RESVERLOGIX CORP
IPC分类号: C07C233/25 , C07C255/59 , C07C255/60
CPC分类号: C07C255/59 , C07C233/25 , C07C235/38 , C07C255/60
摘要: The compounds of Formula (I) wherein R1 is selected from Br and CN; R2 is selected from H and Br; R3 is H or -(C=X)R; R is selected from H, CH3, CF3, CF2H, CFH2, CC13, CC12H, CC1H2, CBr3, CBr2H and CBrH2; X is O or S. The compounds are useful in the synthesis of 2-Amino-4,6-dimethoxybenzamide derivatives.
摘要翻译: 式(I)的化合物,其中R 1选自Br和CN; R2选自H和Br; R3是H或 - (C = X)R; R选自H,CH3,CF3,CF2H,CFH2,CC13,CC12H,CC1H2,CBr3,CBr2H和CBrH2; X是O或S.该化合物可用于2-氨基-4,6-二甲氧基苯甲酰胺衍生物的合成。
-
公开(公告)号:WO2014087298A1
公开(公告)日:2014-06-12
申请号:PCT/IB2013/060381
申请日:2013-11-25
申请人: PFIZER INC.
发明人: ANDERSON, James, Thomas , CHEKLER, Eugene, Lvovich, Piatnitski , ELLSWORTH, Edmund, L. , ERICKSON, Bruce, Kipp , GILBERT, Adam, Matthew , RICKETTS, Anthony, P. , THOMPSON, David, P. , UNWALLA, Rayomand, Jal , VERHOEST, Patrick, Robert
IPC分类号: C07D217/26 , C07C255/58 , C07D401/04 , C07D417/04 , C07D205/04 , C07D207/08 , C07D285/10 , C07D211/22 , A61K31/4725 , A61P5/26 , A61P5/28 , A61P21/00 , A61P19/00 , A61P25/00 , A61P3/00
CPC分类号: C07D417/04 , C07C255/58 , C07C255/59 , C07D205/04 , C07D207/08 , C07D211/22 , C07D217/26 , C07D285/10 , C07D401/04
摘要: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or –CR 0 --, where R 0 is hydrogen, C 1 -C 6 linear or branched chain alkyl, etc., Z is –CR e --, or, –N--, where R e is hydrogen, C 1 -C 6 linear or branched chain alkyl,etc.; R 1 is hydrogen, C 1 -C 6 linear or branched chain alkyl, etc.; R 2 are independently hydrogen or C 1 -C 6 linear or branched chain alkyl; R 3 and R 4 are independently hydrogen, C 1 -C 6 linear or branched chain alkyl, etc.;. R 5 and R 6 are independently hydrogen or C 1 -C 6 linear or branched chain alkyl, etc.; R 8 is hydrogen, C 1 -C 6 linear or branched chain alkyl, etc.; R 9 and R 10 are independently hydrogen or C 1 -C 6 linear or branched chain alkyl, etc.; Q is --CO--, --(CH 2 ) q --, --(CHR S ) q --, or –(CR S R t ) q --, where R S and R t are independently C 1 -C 6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.
摘要翻译: 本发明涉及式1,2或3的化合物:其中A为N或-CR 0 - ,其中R 0为氢,C 1 -C 6直链或支链烷基等,Z为-CRe - 或 ,-N--,其中Re为氢,C1-C6直链或支链烷基等; R1是氢,C1-C6直链或支链烷基等; R2独立地是氢或C1-C6直链或支链烷基; R3和R4独立地是氢,C1-C6直链或支链烷基等。 R5和R6独立地是氢或C1-C6直链或支链烷基等; R8是氢,C1-C6直链或支链烷基等; R9和R10独立地为氢或C1-C6直链或支链烷基等; Q是--CO - , - (CH 2)q - , - (CHRS)q - 或 - (CRS R t)q - ,其中RS和R 5独立地是C 1 -C 6直链或支链烷基 ,芳基,烷基芳基,杂芳基或烷基杂芳基; 其中q是0,1,2或3; 并且其中n为0,2,3,4或5; 或其药学上可接受的盐包含含有这些化合物的组合物; 以及这些化合物在治疗各种疾病,特别是受雄激素受体影响或介导的疾病的用途。
-
6.
公开(公告)号:WO2013175053A1
公开(公告)日:2013-11-28
申请号:PCT/FI2013/000026
申请日:2013-05-23
申请人: ORION CORPORATION
发明人: AHLMARK, Marko , DIN BELLE, David , KAUPPALA, Mika , LUIRO, Anne , PAJUNEN, Taina , PYSTYNEN, Jarmo , TIAINEN, Eija , VAISMAA, Matti , MESSINGER, Josef
IPC分类号: C07C255/53 , A61K31/277 , A61P25/00 , C07C255/54 , C07C255/57 , C07D333/24 , C07D333/60 , C07C311/29 , C07C317/22 , C07C321/28 , C07C321/30 , C07D265/30 , C07D207/08 , C07D207/337 , C07D277/30
CPC分类号: A61K31/277 , A61K31/198 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/382 , A61K31/40 , A61K31/5377 , C07C255/53 , C07C255/54 , C07C255/57 , C07C255/59 , C07C309/66 , C07C311/29 , C07C317/46 , C07C323/29 , C07C323/62 , C07D207/337 , C07D211/14 , C07D213/57 , C07D213/62 , C07D231/12 , C07D231/14 , C07D277/30 , C07D277/34 , C07D277/74 , C07D295/155 , C07D295/192 , C07D307/54 , C07D307/80 , C07D307/81 , C07D309/06 , C07D309/12 , C07D309/22 , C07D333/24 , C07D333/28 , C07D333/60 , C07D333/70
摘要: Compounds of formula (I), wherein R 1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
摘要翻译: 式(I)化合物,其中R 1如权利要求中所定义,表现出COMT酶抑制活性,因此可用作COMT抑制剂。
-
公开(公告)号:WO2012013727A1
公开(公告)日:2012-02-02
申请号:PCT/EP2011/062947
申请日:2011-07-27
申请人: ORYZON GENOMICS S.A. , FYFE, Matthew Colin Thor , ORTEGA MUÑOZ, Alberto , CASTRO-PALOMINO LARIA, Julio , MARTINELL PEDEMONTE, Marc , ESTIARTE-MARTÍNEZ, Maria de los Ángeles , VALLS VIDAL, Nuria
发明人: FYFE, Matthew Colin Thor , ORTEGA MUÑOZ, Alberto , CASTRO-PALOMINO LARIA, Julio , MARTINELL PEDEMONTE, Marc , ESTIARTE-MARTÍNEZ, Maria de los Ángeles , VALLS VIDAL, Nuria
IPC分类号: C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D239/26 , C07D277/28 , C07D333/20 , C07D401/04 , C07D405/04 , C07D409/04 , C07C211/35 , C07C311/21 , A61K31/44 , A61P35/00
CPC分类号: C07C211/40 , C07B2200/07 , C07C215/64 , C07C217/74 , C07C255/53 , C07C255/54 , C07C255/59 , C07C311/08 , C07C311/09 , C07C311/21 , C07C2601/02 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D213/64 , C07D239/26 , C07D277/28 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10
摘要: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
摘要翻译: 本发明涉及环丙胺化合物,特别是式(I)的化合物及其在治疗中的应用,包括例如。 治疗或预防癌症,神经系统疾病或病症或病毒感染。
-
公开(公告)号:WO2012007644A1
公开(公告)日:2012-01-19
申请号:PCT/FI2011/050655
申请日:2011-07-14
发明人: RATILAINEN, Jari , KOISTINAHO, Milla , MUONA, Anu
IPC分类号: C07C237/20 , C07C255/60 , C07C317/46 , C07D295/145
CPC分类号: C07C255/59 , A61K31/277 , A61K31/341 , A61K45/00 , C07C237/20 , C07C255/60 , C07C317/46 , C07D295/15 , C07D307/54
摘要: The invention relates to novel arylamide derivatives having formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, where R1 - R11, R', R", z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.
摘要翻译: 本发明涉及具有式(I)的新型芳基酰胺衍生物及其立体异构体和药学上可接受的盐,其中R 1 -R 11,R',R“,Z和X如权利要求中所定义。式(I)的芳基酰胺衍生物具有式 本发明还涉及用作药物的式(I)化合物和包含它们的药物组合物及其制备方法。
-
公开(公告)号:WO2011068987A3
公开(公告)日:2011-11-10
申请号:PCT/US2010058757
申请日:2010-12-02
IPC分类号: C07C217/58 , A61K31/138 , A61K31/275 , A61P33/02 , C07C255/53
CPC分类号: C07C217/58 , A61K31/055 , A61K31/122 , A61K31/137 , A61K31/437 , A61K31/4453 , A61K31/497 , A61K31/52 , A61K31/65 , C07C215/50 , C07C219/28 , C07C255/59 , C07C2601/14
摘要: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.
摘要翻译: 本文描述了治疗接触贾第鞭毛虫(Giardia lamblia)和/或贾第虫病(Giardia)和/或贾第鞭毛虫病(Giardiaisis)的方法和拮抗贾第鞭毛虫属(Giardia lamblia)附着于受试者肠壁的方法。
-
公开(公告)号:WO2011032277A1
公开(公告)日:2011-03-24
申请号:PCT/CA2010/001443
申请日:2010-09-16
申请人: BOEHRINGER INGELHEIM INTERNATIONAL GmbH , STAMMERS, Timothy , BARBEAU, Xavier , BEAULIEU, Pierre , BERTRAND-LAPERLE, Megan , BROCHU, Christian , EDWARDS, Paul, J. , FORGIONE, Pasquale , GODBOUT, Cédrickx , HUCKE, Oliver , JOLY, Marc-André , LANDRY, Serge , LEPAGE, Olivier , NAUD, Julie , PESANT, Marc , POIRIER, Martin , POIRIER, Maude , THAVONEKHAM, Bounkham
发明人: STAMMERS, Timothy , BARBEAU, Xavier , BEAULIEU, Pierre , BERTRAND-LAPERLE, Megan , BROCHU, Christian , EDWARDS, Paul, J. , FORGIONE, Pasquale , GODBOUT, Cédrickx , HUCKE, Oliver , JOLY, Marc-André , LANDRY, Serge , LEPAGE, Olivier , NAUD, Julie , PESANT, Marc , POIRIER, Martin , POIRIER, Maude , THAVONEKHAM, Bounkham
IPC分类号: C07D401/12 , A61K31/517 , A61K31/14 , C07C211/29 , C07C233/13 , C07C237/44 , C07C251/48 , C07C255/58 , C07D213/74 , C07D239/42 , C07D239/88 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07F5/02
CPC分类号: C07D401/12 , A61K31/14 , A61K31/517 , C07C211/29 , C07C233/11 , C07C237/44 , C07C251/48 , C07C255/58 , C07C255/59 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07F5/025
摘要: Compounds of formula I: (I) wherein X, R 2 , R 3 , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译: 式I化合物(其中X,R 2,R 3,R 5和R 6在本文中定义)可用作丙型肝炎病毒NS5B聚合酶的抑制剂。
-
-
-
-
-
-
-
-
-