公开(公告)号：WO2006103120A3

公开(公告)日：2007-02-15

申请号：PCT/EP2006003787

申请日：2006-03-29

Applicant: INSA ROUEN ,  GOUS INC ,  MARSAIS FRANCIS ,  BOHN PIERRE ,  LEVACHER VINCENT ,  LE FUR NICOLAS

Inventor： MARSAIS FRANCIS ,  BOHN PIERRE ,  LEVACHER VINCENT ,  LE FUR NICOLAS

IPC: C07D211/84 ,  A61K31/44 ,  A61K31/47 ,  A61P25/28 ,  C07D211/82 ,  C07D211/86 ,  C07D215/20 ,  C07D215/24 ,  C07D215/36 ,  C07D217/22 ,  C07D217/24 ,  C07D413/04

CPC classification number: C07D211/96 ,  C07D211/86 ,  C07D211/90 ,  C07D215/34 ,  C07D215/36 ,  C07D215/54 ,  C07D217/22 ,  C07D217/24 ,  C07D413/04

Abstract: The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

Abstract translation: 本发明涉及包含至少一个基团C = Y，Y为O或S的氧化和不可质子化的氮原子N的化合物，其中基团C的至少一个碳原子之间的距离（d） 当氧化时，Y和氮原子在0.3和0.8纳米之间。 本发明涉及由式G定义的新的杂环化合物，其制备方法，包含它们的药物组合物和它们作为治疗剂的用途，特别是用于治疗神经变性或阿尔茨海默病。

公开(公告)号：WO2016193997A3

公开(公告)日：2017-01-19

申请号：PCT/IN2016000142

申请日：2016-06-03

Applicant: MSN LABORATORIES PRIVATE LTD ,  THIRUMALAI RAJAN SRINIVASAN ,  ESWARAIAH SAJJA ,  VENKAT REDDY GHOJALA ,  VENKAT REDDY MALLEPALLY

Inventor： THIRUMALAI RAJAN SRINIVASAN ,  ESWARAIAH SAJJA ,  VENKAT REDDY GHOJALA ,  VENKAT REDDY MALLEPALLY

IPC: C07D215/56

CPC classification number: C07D215/34

Abstract: The present invention relates to a process for the preparation of 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid represented by the following structural formula-1 and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及制备6-（3-氯-2-氟苄基）-1 - [（2S）-1-羟基-3-甲基丁-2-基] -7-甲氧基-4-氧代 -1,4-二氢喹啉-3-羧酸及其药学上可接受的盐。

公开(公告)号：WO2016193997A2

公开(公告)日：2016-12-08

申请号：PCT/IN2016/000142

申请日：2016-06-03

Applicant: MSN LABORATORIES PRIVATE LIMITED ,  THIRUMALAI RAJAN, Srinivasan ,  ESWARAIAH, Sajja ,  VENKAT REDDY, Ghojala ,  VENKAT REDDY, Mallepally

Inventor： THIRUMALAI RAJAN, Srinivasan ,  ESWARAIAH, Sajja ,  VENKAT REDDY, Ghojala ,  VENKAT REDDY, Mallepally

CPC classification number: C07D215/34

Abstract: The present invention relates to a process for the preparation of 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid represented by the following structural formula-1 and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及制备6-（3-氯-2-氟苄基）-1 - [（2S）-1-羟基-3-甲基丁-2-基] -7-甲氧基-4-氧代 -1,4-二氢喹啉-3-羧酸及其药学上可接受的盐。

公开(公告)号：WO2015172722A1

公开(公告)日：2015-11-19

申请号：PCT/CN2015/078918

申请日：2015-05-14

Applicant: 浙江省医学科学院

Inventor： 黄文海 ,  沈正荣 ,  杨叶伟 ,  马臻 ,  王尊元

IPC: C07D215/34 ,  C07D215/26 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/496 ,  A61P25/28

CPC classification number: A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D215/26 ,  C07D215/34

Abstract: 一种具有如式I所示结构的6,8-双取代喹啉化合物、其药学上可接受的盐、制备方法及其在治疗老年痴呆疾病方面的应用，该化合物具有乙酰胆碱酯酶抑制活性和Aβ聚集抑制能力，其水解产物具有金属离子螯合作用。

公开(公告)号：WO2010086860A3

公开(公告)日：2011-02-24

申请号：PCT/IL2010000080

申请日：2010-01-31

Applicant: YEDA RES & DEV ,  TECHNION RES & DEV FOUNDATION ,  YOUDIM MOUSSA B H ,  FRIDKIN MATI ,  ZHENG HAILIN

Inventor： YOUDIM MOUSSA B H ,  FRIDKIN MATI ,  ZHENG HAILIN

IPC: C07C211/38 ,  A61K31/131 ,  A61K31/135 ,  A61K31/47 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  C07C259/10 ,  C07C271/40 ,  C07D215/34 ,  C07D401/12

CPC classification number: C07C259/10 ,  C07C211/38 ,  C07C271/40 ,  C07C2602/08 ,  C07C2603/74 ,  C07D215/34 ,  C07D401/06 ,  C07D401/12

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to Vl.

Abstract translation: 提供多官能化合物，其包含两个或多个选自以下的官能部分：（i）赋予铁螯合剂功能的部分; （ii）赋予神经保护功能的部分; （iii）赋予组合的抗细胞凋亡，神经保护和/或神经恢复功能的部分; （iv）赋予脑MAO抑制的部分，优选在肝脏和小肠中几乎没有MAO抑制作用; （v）赋予胆碱酯酶抑制功能的部分; 和（vi）赋予N-甲基-D-天冬氨酸受体（NMDAR）抑制的部分及其药学上可接受的盐和旋光异构体。 多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复，和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。 本发明包括式I至VI的化合物。

公开(公告)号：WO2014117670A1

公开(公告)日：2014-08-07

申请号：PCT/CN2014/071090

申请日：2014-01-22

Applicant: 中山大学

Inventor： 黎兴术 ,  毛斐 ,  黄玲

IPC: C07D215/26 ,  A61P25/28 ,  A61K31/47

CPC classification number: A61K31/47 ,  C07D215/26 ,  C07D215/34

Abstract: 本申请提供了一种式I的苯乙基喹啉化合物，以及其在治疗、改善和/或预防阿尔茨海默病的药物组合物中的应用。式I的R 1 -R 7 如说明书所定义。

公开(公告)号：WO2012006276A1

公开(公告)日：2012-01-12

申请号：PCT/US2011/042941

申请日：2011-07-05

Applicant: NORTH CAROLINA STATE UNIVERSITY ,  MELANDER, Christian ,  ROGERS, Steven A.

Inventor： MELANDER, Christian ,  ROGERS, Steven A.

IPC: C07D215/34

CPC classification number: C07D249/04 ,  A01N43/40 ,  A01N43/42 ,  A01N43/647 ,  C07D213/55 ,  C07D213/58 ,  C07D215/08 ,  C07D215/34 ,  C07J41/0055 ,  C07J43/003

Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.

Abstract translation: 提供了用于防止，除去和/或抑制生物膜形成的氨基甲酸酯化合物的公开内容，包括这些化合物的组合物，包括这些化合物的装置及其使用方法。

公开(公告)号：WO2010086860A2

公开(公告)日：2010-08-05

申请号：PCT/IL2010/000080

申请日：2010-01-31

Applicant: Yeda Research and Development Co. Ltd. ,  Technion Research and Development Foundation Ltd. ,  YOUDIM, Moussa B.H. ,  FRIDKIN, Mati ,  ZHENG, Hailin

Inventor： YOUDIM, Moussa B.H. ,  FRIDKIN, Mati ,  ZHENG, Hailin

IPC: C07C211/38

CPC classification number: C07C259/10 ,  C07C211/38 ,  C07C271/40 ,  C07C2602/08 ,  C07C2603/74 ,  C07D215/34 ,  C07D401/06 ,  C07D401/12

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.

Abstract translation: 提供多官能化合物，其包含两个或多个选自以下的官能部分：（i）赋予铁螯合剂功能的部分; （ii）赋予神经保护功能的部分; （iii）赋予组合的抗细胞凋亡，神经保护和/或神经恢复功能的部分; （iv）赋予脑MAO抑制的部分，优选在肝脏和小肠中几乎没有MAO抑制作用; （v）赋予胆碱酯酶抑制功能的部分; 和（vi）赋予N-甲基-D-天冬氨酸受体（NMDAR）抑制的部分及其药学上可接受的盐和旋光异构体。 多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复，和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。

公开(公告)号：WO2006103120A2

公开(公告)日：2006-10-05

申请号：PCT/EP2006/003787

申请日：2006-03-29

Applicant: INSA ROUEN ,  GOUS INC. ,  MARSAIS, Francis ,  BOHN, Pierre ,  LEVACHER, Vincent ,  LE FUR, Nicolas

Inventor： MARSAIS, Francis ,  BOHN, Pierre ,  LEVACHER, Vincent ,  LE FUR, Nicolas

IPC: C07D211/84 ,  C07D413/04 ,  C07D211/82 ,  C07D211/86

CPC classification number: C07D211/96 ,  C07D211/86 ,  C07D211/90 ,  C07D215/34 ,  C07D215/36 ,  C07D215/54 ,  C07D217/22 ,  C07D217/24 ,  C07D413/04

Abstract: The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

Abstract translation: 本发明涉及包含至少一个基团C = Y，Y为O或S的氧化和不可质子化的氮原子N的化合物，其中基团C的至少一个碳原子之间的距离（d） 当氧化时，Y和氮原子在0.3和0.8纳米之间。 本发明涉及由式G定义的新的杂环化合物，其制备方法，包含它们的药物组合物及其作为治疗剂的用途，特别是用于治疗神经变性或阿尔茨海默病。

公开(公告)号：WO2002070494A1

公开(公告)日：2002-09-12

申请号：PCT/US2002/006452

申请日：2002-03-01

Applicant: ICOS CORPORATION

Inventor： KEEGAN, Kathleen, S. ,  KESICKI, Edward, A. ,  GAUDINO, John, Joseph ,  COOK, Adam, Wade ,  COWEN, Scott, Douglas ,  BURGESS, Laurence, Edward

IPC: C07D241/20

CPC classification number: A61K45/06 ,  A61K31/4965 ,  A61K31/498 ,  C07D213/30 ,  C07D213/40 ,  C07D213/75 ,  C07D213/77 ,  C07D215/34 ,  C07D231/12 ,  C07D231/40 ,  C07D233/56 ,  C07D239/42 ,  C07D239/47 ,  C07D241/12 ,  C07D241/20 ,  C07D241/44 ,  C07D249/08 ,  C07D251/22 ,  C07D253/07 ,  C07D257/06 ,  C07D277/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D453/02 ,  A61K2300/00

Abstract: Aryl- and heteroaryl substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed. Wherein W' is a six-membered aromatic ring containing at least 2 introgen atoms and optionally substitutedas defined in the claims, Z' is a five- or six membered aromatic or heteraromatic ring as defined in the claims, Y' is O or S.

Abstract translation: 公开了可用于治疗与DNA复制中的DNA损伤或病变相关的疾病和病症的芳基和杂芳基取代的脲化合物。 还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗癌症和其它以DNA复制，染色体分离或细胞分裂缺陷为特征的疾病。 其中W'是包含至少2个内源原子和任选取代的6元芳环，如权利要求中所定义，Z'是如权利要求中所定义的五元或六元芳族或杂芳环，Y'是O或S.