公开(公告)号：WO2019053700A2

公开(公告)日：2019-03-21

申请号：PCT/IB2018/058935

申请日：2018-11-13

申请人： BATTELLE MEMORIAL INSTITUTE ,  WRIGHT, Aaron T. ,  RAMOS-HUNTER, Susan ,  SADLER, Natalie C. ,  FREDRICKSON, JIM K. ,  ROMINE, MARGARET F. ,  WHIDBEY, CHRISTOPHER-MYCHAEL ,  STODDARD, ETHAN G. ,  KILLINGER, BRYAN J. ,  NAIR, REJI N.

发明人： WRIGHT, Aaron T. ,  RAMOS-HUNTER, Susan ,  SADLER, Natalie C.

IPC分类号： G01N33/548 ,  C07H15/22 ,  C07H15/26 ,  C07H13/12 ,  C07H9/00 ,  C07C305/24 ,  C07D229/02 ,  C07F9/09 ,  G01N33/569

摘要： Probe embodiments for identifying analytes involved in biofuel or bioenergy production, bioremediation, or nutrient cycling as well as methods of making and use are described herein. In some embodiments, probes identifying cellulose degradation and/or sugar transport, lignin or chitin degradation, or peptide or toxin metabolism are included. In some embodiments, probes for identifying analytes in a soil sample are included in the compositions and methods disclosed herein.

公开(公告)号：WO2019008441A1

公开(公告)日：2019-01-10

申请号：PCT/IB2018/000847

申请日：2018-07-03

申请人： INTOCELL, INC. ,  PARK, Taekyo ,  WOO, Sung Ho ,  KIM, Sunyoung ,  PARK, Suho ,  CHO, Jongun ,  JUNG, Doohwan ,  SEO, Donghoon ,  LEE, Jaeho ,  LEE, Sangkwang ,  YUN, Sanghyeon ,  LEE, Hyang Sook ,  PARK, Okku ,  SEO, Beomseok

发明人： PARK, Taekyo ,  WOO, Sung Ho ,  KIM, Sunyoung ,  PARK, Suho ,  CHO, Jongun ,  JUNG, Doohwan ,  SEO, Donghoon ,  LEE, Jaeho ,  LEE, Sangkwang ,  YUN, Sanghyeon ,  LEE, Hyang Sook ,  PARK, Okku ,  SEO, Beomseok

IPC分类号： C07H15/203 ,  C07K16/40 ,  C07C305/24 ,  C01B33/00 ,  A61K47/22 ,  A61K47/68 ,  A61P35/00

摘要： Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO 2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

公开(公告)号：WO2010027594A2

公开(公告)日：2010-03-11

申请号：PCT/US2009052684

申请日：2009-08-04

申请人： UNIV VIRGINIA COMMONWEALTH ,  DESAL UMESH R ,  HENRY BRIAN L ,  LIANG AIYE ,  THAKKAR JAY ,  MANGRUM JOHN B ,  FILHO IVO TORRES ,  SPIESS BRUCE D ,  SAKAGAMI MASAHIRO ,  SALUJA BHAWANA

发明人： DESAL UMESH R ,  HENRY BRIAN L ,  LIANG AIYE ,  THAKKAR JAY ,  MANGRUM JOHN B ,  FILHO IVO TORRES ,  SPIESS BRUCE D ,  SAKAGAMI MASAHIRO ,  SALUJA BHAWANA

IPC分类号： C07C69/736 ,  A61K31/185 ,  A61K31/192 ,  A61K31/343 ,  A61P11/00 ,  A61P29/00 ,  C07C69/618 ,  C07C305/24 ,  C07D307/77 ,  C07D407/04

CPC分类号： C07D407/14 ,  A61K9/007 ,  A61K31/185 ,  A61K31/192 ,  A61K31/343 ,  C07C305/24 ,  C07D307/80 ,  C07D307/84

摘要： Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ß-O4 and ß-5 trimers and tetramers) are used as anticoagulants.

摘要翻译： 提供肉桂酸类低聚物及其治疗用途。 低聚物用作抗炎剂，弹性蛋白酶和抗氧化剂的抑制剂，并且在一些情况下（例如治疗肺部疾病如肺癌），所有这三种活性同时是有益的。 寡聚体（例如ß-O4和ß-5三聚体和四聚体）的子集用作抗凝剂。

公开(公告)号：WO9911606A3

公开(公告)日：1999-07-08

申请号：PCT/US9817327

申请日：1998-08-24

申请人： UPJOHN CO ,  LARSEN SCOTT D ,  MAY PAUL D ,  BLEASDALE JOHN ,  LILJEBRIS CHARLOTTA ,  SCHOSTAREZ HEINRICH JOSEF ,  BARF TJEERD

发明人： LARSEN SCOTT D ,  MAY PAUL D ,  BLEASDALE JOHN ,  LILJEBRIS CHARLOTTA ,  SCHOSTAREZ HEINRICH JOSEF ,  BARF TJEERD

IPC分类号： C07D295/12 ,  A61K31/197 ,  A61K31/215 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  A61K38/00 ,  A61P3/10 ,  A61P43/00 ,  C07C233/18 ,  C07C235/34 ,  C07C235/74 ,  C07C235/80 ,  C07C237/22 ,  C07C237/52 ,  C07C271/02 ,  C07C271/22 ,  C07C275/24 ,  C07C275/42 ,  C07C305/24 ,  C07C311/06 ,  C07C311/13 ,  C07C311/37 ,  C07C311/46 ,  C07C311/47 ,  C07C317/50 ,  C07C323/59 ,  C07D295/13 ,  C07D295/20 ,  C07D295/215 ,  C07D521/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  A61K31/165 ,  A61K31/195 ,  A61K31/40 ,  A61K31/41 ,  C07C235/78 ,  C07C237/20 ,  C07D207/20 ,  C07D257/04

CPC分类号： C07D295/215 ,  A61K38/00 ,  C07C235/74 ,  C07C235/80 ,  C07C237/52 ,  C07C271/02 ,  C07C271/22 ,  C07C275/24 ,  C07C305/24 ,  C07C311/06 ,  C07C311/13 ,  C07C311/37 ,  C07C317/50 ,  C07C323/59 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/66 ,  C07C2603/70 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/13 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06156

摘要： The present invention comprises small molecular weight, non-peptidic inhibitors of formula (I) and (II) of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).

摘要翻译： 本发明包括可用于治疗和/或预防非胰岛素依赖性糖尿病（NIDDM）的蛋白酪氨酸磷酸酶1（PTP1）的式（I）和（II）的小分子量非肽抑制剂。

公开(公告)号：WO2019053700A3

公开(公告)日：2019-03-21

申请号：PCT/IB2018/058935

申请日：2018-11-13

申请人： BATTELLE MEMORIAL INSTITUTE ,  WRIGHT, Aaron T. ,  RAMOS-HUNTER, Susan ,  SADLER, Natalie C. ,  FREDRICKSON, JIM K. ,  ROMINE, MARGARET F. ,  WHIDBEY, CHRISTOPHER-MYCHAEL ,  STODDARD, ETHAN G. ,  KILLINGER, BRYAN J. ,  NAIR, REJI N.

发明人： WRIGHT, Aaron T. ,  RAMOS-HUNTER, Susan ,  SADLER, Natalie C.

IPC分类号： G01N33/548 ,  C07H15/22 ,  C07H15/26 ,  C07H13/12 ,  C07H9/00 ,  C07C305/24 ,  C07D229/02 ,  C07F9/09 ,  G01N33/569

摘要： Probe embodiments for identifying analytes involved in biofuel or bioenergy production, bioremediation, or nutrient cycling as well as methods of making and use are described herein. In some embodiments, probes identifying cellulose degradation and/or sugar transport, lignin or chitin degradation, or peptide or toxin metabolism are included. In some embodiments, probes for identifying analytes in a soil sample are included in the compositions and methods disclosed herein.

公开(公告)号：WO2018096504A1

公开(公告)日：2018-05-31

申请号：PCT/IB2017/057403

申请日：2017-11-27

申请人： KALYTERA THERAPEUTICS, INC

发明人： SALZMAN, Andrew ,  FLOWER, Kevin ,  GARNER, C. Edwin ,  JAGTAP, Parkash ,  MUSA, Saana

IPC分类号： C07F9/38 ,  C07C279/14 ,  C07C203/10 ,  C07C305/24 ,  C07C229/18 ,  C07F9/40 ,  A61K31/255 ,  A61P17/00

CPC分类号： C07F9/3834 ,  A61P17/10 ,  C07C201/02 ,  C07C203/10 ,  C07C227/20 ,  C07C269/06 ,  C07C277/08 ,  C07C279/14 ,  C07C303/24 ,  C07C305/24 ,  C07C2603/18 ,  C07F9/3882 ,  C07F9/4006 ,  C07C229/06 ,  C07C271/22

摘要： Compounds of Formula (I), including stereoisomers and salts thereof, and compositions, methods of treatment and prevention, and methods of preparing, the same: Formula (I) wherein X is O or a direct bond; wherein when X is O, R 1 and R 2 are each independently selected from -H, -SO 3 Na, -PO(ONa) 2 , -PO(OCH 2 CH 3 ), -CH 2 PO(ONa) 2 , -NO 2 , -(L)-valine ester, -(L)-N-methyl arginine ester, -α-guanidinoglutaric acid ester, -2-iminobiotin ester, -3- hydroxy anthranilic acid ester, -(L)-nitroarginine ester, -(L)- N5-(1-iminoethyl)-(L)- ornithine (NIO) ester, -(L)-N,N dimethylarginine ester, -(L)- N6-(1-iminoethyl)-(L)-lysine (NIL) ester, -(L)- N-monomethyl-(L)-arginine (NMMA) ester, -N-amino-(L)-arginine ester, -N-propyl-(L)-arginine ester, -S-methyl-(L)-thiocitrulline ester, -methyl-(L)-NIO ester, - vinyl -(L)-NIO ester, and -propenyl-(L)-NK) ester; and wherein when X is a direct bond, R 1 and R 2 are Formula (II).

公开(公告)号：WO2012159997A1

公开(公告)日：2012-11-29

申请号：PCT/EP2012/059293

申请日：2012-05-18

申请人： PAMGENE B.V. ,  UNIVERSITEIT UTRECHT HOLDING B.V. ,  RUIJTENBEEK, Robby ,  VAN AMEIJDE, Jeroen ,  LISKAMP, Robertus Matthias Joseph

发明人： RUIJTENBEEK, Robby ,  VAN AMEIJDE, Jeroen ,  LISKAMP, Robertus Matthias Joseph

IPC分类号： C07C305/24 ,  C07F9/12 ,  C07K7/04 ,  C07K7/06 ,  G01N33/68

CPC分类号： G01N33/573 ,  C07C305/24 ,  C07F9/08 ,  C07F9/12 ,  C12Q1/42

摘要： The present invention relates to a method and tools which allow the kinetic monitoring of hydrolase enzyme activity. The present invention also aims to provide synthetic peptides and peptide residues modified such that they can be used in assays for monitoring hydrolase enzyme activity, and preferably phosphatase activity. Also claimed are modified tyrosine amino acid derivatives of formula (IV), wherein Y is chosen from -PO y 2- with y equal to 2 or 3 and esters thereof, -SO Z - with z equal to 2 or 3 and esters thereof, a carbohydrate or carbohydrate derivatives; and; wherein X 1 and/or X 2 is selected from -N 3 , -NO 2 , -CI, or -CN, -SCN, a C 1 to C 8 alkyl, or H, wherein either X 1 or X 2 is not H.

摘要翻译： 本发明涉及允许动态监测水解酶活性的方法和工具。 本发明还旨在提供经修饰的合成肽和肽残基，使得它们可用于监测水解酶活性的测定，优选用于磷酸酶活性。 还要求保护的是式（IV）的修饰的酪氨酸氨基酸衍生物，其中Y选自-Yyy2-，其中y等于2或3，其酯，-SOZ-，其中z等于2或3及其酯，碳水化合物 或碳水化合物衍生物; 和; 其中X 1和/或X 2选自-N 3，-NO 2，-C 1或-CN，-SCN，C 1至C 8烷基或H，其中X 1或X 2不为H.

公开(公告)号：WO02034715A1

公开(公告)日：2002-05-02

申请号：PCT/EP2001/012127

申请日：2001-10-19

IPC分类号： A61P1/00 ,  A61K31/255 ,  A61P1/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/28 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B61/00 ,  C07C303/24 ,  C07C305/24 ,  A61K31/095

CPC分类号： C07C305/24

摘要： The invention relates to novel sulfoxybenzamides of formula (I), wherein: Z represents a group selected among formulas -X -(CH2)r-X - and -CR R -; A and A , independent of one another, represent a 1,4-phenylene group or 1,3-phenylene group optionally substituted by one or more halogen atoms, C1-C8 alkyl groups, C2-C8 alkenyl groups, C1-C8 alkyl halide groups or by C1-C8 alkoxy groups; Z and Z , independent of one another, represent a group of formula -X -(CH2)8-X - or a single bond; m and n, independent of one another, represent 0 or 1, and; radicals R , R , R , R , R , X , X , X , X , r and s have the meanings cited in the description. The invention also relates to a method for producing these novel compounds and to their use as medicaments, especially as leukotriene B4(LTB4) antagonists.

摘要翻译： 本发明涉及式（I）的新颖Sulfooxybenzamide，其中Z <0>表示从下式中选择的基团-X <1> - （CH2）RX <2> - 和-CR <4> - [R <5> - ， - 一个<1>和<2>各自独立地表示任选被一个或多个卤素原子，C1-C8烷基，C2-C8链烯基，C1-C8卤代烷基或C1-C8烷氧基取代的取代的1,4-亚苯基 - 或1,3-亚苯基，Z <1>和Z <2>各自独立地表示下式基团-X <3> - （CH2）8-X <4> - 或单键，m和n 各自独立地为0或1，并且其中基团R <1>，R <2>，R <3>，R <4>，R <5>中，X <1>中，X <2>中，X < 3>，X <4>，r和s具有在说明书中提到的含义，它们的制备方法和它们作为药物的用途，特别是作为白三烯B4（LTB4）拮抗剂。

公开(公告)号：WO01072680A1

公开(公告)日：2001-10-04

申请号：PCT/GB2001/001341

申请日：2001-03-26

IPC分类号： A61K49/00 ,  A61K31/12 ,  A61K31/121 ,  A61K31/15 ,  A61K31/222 ,  A61K31/235 ,  A61P1/04 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  C07C49/84 ,  C07C69/017 ,  C07C69/157 ,  C07C251/40 ,  C07C251/48 ,  C07C305/24 ,  C07F9/12 ,  G01N33/574

CPC分类号： G01N33/574 ,  A61K31/12 ,  A61K31/15 ,  A61K31/222 ,  C07C69/017 ,  C07C251/40 ,  C07C305/24 ,  C07F9/12 ,  G01N2333/90209

摘要： This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is -H, -OH, -OC(=O)R , -OS(=O)2OH, or -OP(=O)2(OH)2; Y is -H or a C1-4alkyl group; Z is -H or -OCH3; R is -H, a C1-4alkyl group, or C1-4fluoroalkyl group; R is -H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is -H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

摘要翻译： 本发明涉及具有治疗应用的取代的查尔酮，特异性取代的1-（4-甲氧基苯基）-3-（3,5-二甲氧基苯基）丙-1-烯-3-酮，例如作为有效的抗增殖剂和抗炎药 并且具有式（I）的化合物，其中：X是-H，-OH，-OC（= O）R 3，-OS（= O）2 OH或-OP（= O）2 2; Y是-H或C 1-4烷基; Z是-H或-OCH 3; R 1是-H，C 1-4烷基或C 1-4氟烷基; R 2是-H，C 1-4烷基或C 1-4氟烷基; 且R 3为-H，C 1-6烷基，C 3-20杂环基或C 5-20芳基; 和其药学上可接受的盐，酯和保护形式。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内用于诊断和治疗例如增生性疾病如癌症和炎性病症的用途。

公开(公告)号：WO00040529A1

公开(公告)日：2000-07-13

申请号：PCT/GB1999/004436

申请日：1999-12-24

IPC分类号： C07D295/08 ,  A61K31/165 ,  A61K31/167 ,  A61K31/192 ,  A61K31/197 ,  A61K31/198 ,  A61K31/225 ,  A61K31/255 ,  A61K31/265 ,  A61K31/27 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/661 ,  A61K31/704 ,  A61P9/00 ,  A61P35/00 ,  C07B53/00 ,  C07C68/02 ,  C07C69/96 ,  C07C213/00 ,  C07C217/74 ,  C07C231/02 ,  C07C231/12 ,  C07C233/23 ,  C07C233/43 ,  C07C237/04 ,  C07C237/48 ,  C07C249/12 ,  C07C251/44 ,  C07C253/20 ,  C07C255/60 ,  C07C257/14 ,  C07C269/04 ,  C07C269/06 ,  C07C271/22 ,  C07C271/24 ,  C07C271/52 ,  C07C273/18 ,  C07C275/42 ,  C07C301/02 ,  C07C303/28 ,  C07C303/40 ,  C07C305/24 ,  C07C307/08 ,  C07C309/15 ,  C07F9/09 ,  C07F9/40 ,  C07H15/248 ,  C07C13/547 ,  A61K31/19 ,  A61K31/22

CPC分类号： A61K31/165

摘要： The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R )- wherein R is hydrogen, hydroxy, C1-7alkoxy, -OR or -NR R (wherein R is a group -Y R (wherein Y is a direct bond, -C(O)-, -C(S)-, -S-, -C(O)O, -C(O)NR -, -SO2- or -SO2NR - (wherein R and R , which may be the same or different, each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl) and R is as defined herein, and R includes hydrogen; R , R and R are as defined herein and are preferably methyl; R , R and R are as defined herein with the proviso that R is not hydroxy, alkoxy, substituted alkoxy, -OPO3H2, -O-C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.

摘要翻译： 本发明涉及式（I）化合物的用途：其中X是-C（O） - ， - C（S） - ， - C = NOH或-CH（R 7） - ，其中R 7 >是氢，羟基，C 1-7烷氧基，-OR 8或-NR 8 R 9（其中R 8是基团-Y 1 R 10（其中Y 1是 -C（O） - ， - C（O）O，-C（O）NR 11 - ， - SO 2 - 或-SO 2 NR 12 - （其中R 11和R 12可以相同或不同，各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基），R 10如本文所定义，R 9， 包括氢; R 1，R 2和R 3如本文所定义，并且优选为甲基; R 4，R 5和R 6如本文所定义，条件是R“ 5>不是羟基，烷氧基，取代的烷氧基，-OPO 3 H 2，-O-C 1-7烷酰基或苄氧基;及其盐在制备用于在温血动物如人中产生血管损伤作用的药物 本发明还涉及式（I）的化合物，含有它们的药物组合物， 以及使用该化合物在温血动物如人中产生血管损伤作用的治疗方法。 式（I）化合物及其药学上可接受的盐可用于治疗许多疾病状态，包括癌症和类风湿性关节炎。