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1. 发明申请

WO2022143479A1 一种化合物的固体形式及其制备方法和用途审中-公开
公开(公告)号：WO2022143479A1
公开(公告)日：2022-07-07
申请号：PCT/CN2021/141429
申请日：2021-12-27
申请人：广东东阳光药业有限公司
发明人：徐巾超 , 张杰 , 杨柳鸿 , 张鹏伟 , 叶辉青 , 陈勇 , 黄芳芳
IPC分类号： C07D419/12 , A61K31/428 , A61P1/16
摘要：提供一种化合物的固体形式及其制备方法和用途，属于药物化学领域。所述固体形式包括化合物与肉桂酰胺的共晶或化合物的氨丁三醇盐。所述化合物的固体形式具有良好的稳定性和溶解度。

2. 发明申请

WO2021063967A1 NOVEL SUBSTITUTED 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF 审中-公开
公开(公告)号：WO2021063967A1
公开(公告)日：2021-04-08
申请号：PCT/EP2020/077266
申请日：2020-09-29
申请人： SANOFI
发明人： BOISNARD, Sabine , EL-AHMAD, Youssef , FETT, Eykmar , HALLEY, Frank , NICOLAI, Eric , TABART, Michel , TERRIER, Corinne , VIVET, Bertrand
IPC分类号： A61P5/32 , A61P35/00 , C07D207/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D419/12 , C07F5/02 , A61K31/40 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K33/22 , A61K31/4155 , A61K31/4178
摘要： The present invention relates to a compound of the formula (I) wherein Ar represents a phenyl or a 6-membered heteroaryl group, R1 and R2 represent independently a hydrogen atom or a deuterium atom, R3 represents (1) a -COR4 group, (2) a -BOR5OR6 group, (3) a -X-Z group, (4) a (C1-C6)alkyl group or a (C1-C6)alkenyl group, (5) a -X-S(O)n(R7)p(R8)q group, (6) a halogen atom, a -NH2 group or a -CN group, (7) a -O-R11 group, (8) a -NH-COR9 group, (9) a -C(=NH)NHOH group, (10) a -NH-C(NH)-R9' group, or (11) a -NHCOCOOR12 group or a -NHCOCONR12'R12'' group, X represents a bond, a -NH- group, a -CONH- group or a -CO- group, Z represents a 4 or 5-membered cycloalkyl, a 4 or 5-membered heterocylcloalkyl group, a 4 or 5-membered heteroaryl group or a phenyl group or a pharmaceutically acceptable salt thereof. The present invention further relates to a medicament comprising said compound of formula (I) and to said compound of formula (I) for use as an inhibitor and degrader of estrogen receptors.

3. 发明申请

WO2012173682A3 COMPOUNDS AND METHODS FOR THE TREATMENT OF ISOCITRATE DEHYDROGNASE RELATED DISEASES 审中-公开
标题翻译：用于治疗异烟肼脱氢酶相关疾病的化合物和方法
公开(公告)号：WO2012173682A3
公开(公告)日：2013-03-14
申请号：PCT/US2012031245
申请日：2012-03-29
申请人： BROAD INST INC , HARVARD COLLEGE , HUSSAIN MAHMUD , ITO DAISUKE , LAW JASON , LEIENDECKER MATTHIAS , LIU KE , MUNOZ BENITO , SCHREIBER STUART , SHAMJI ALYKHAN , STERN ANDREW
发明人： HUSSAIN MAHMUD , ITO DAISUKE , LAW JASON , LEIENDECKER MATTHIAS , LIU KE , MUNOZ BENITO , SCHREIBER STUART , SHAMJI ALYKHAN , STERN ANDREW
IPC分类号： C07D419/12 , A61K31/553 , A61K31/554 , A61P35/00 , C07D413/12
CPC分类号： C07D419/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The invention relates to compounds of Formula I pharmaceutically acceptable salt, ester or prodrug thereof:
摘要翻译：本发明涉及式I化合物的药学上可接受的盐，酯或前药：

4. 发明申请

WO2012173682A2 COMPOUNDS AND METHODS FOR THE TREATMENT OF ISOCITRATE DEHYDROGNASE RELATED DISEASES 审中-公开
标题翻译：用于治疗异烟肼脱氢酶相关疾病的化合物和方法
公开(公告)号：WO2012173682A2
公开(公告)日：2012-12-20
申请号：PCT/US2012/031245
申请日：2012-03-29
申请人： THE BROAD INSTITUTE, INC. , PRESIDENT & FELLOWS OF HARVARD COLLEGE , HUSSAIN, Mahmud , ITO, Daisuke , LAW, Jason , LEIENDECKER, Matthias , LIU, Ke , MUNOZ, Benito , SCHREIBER, Stuart , SHAMJI, Alykhan , STERN, Andrew
发明人： HUSSAIN, Mahmud , ITO, Daisuke , LAW, Jason , LEIENDECKER, Matthias , LIU, Ke , MUNOZ, Benito , SCHREIBER, Stuart , SHAMJI, Alykhan , STERN, Andrew
IPC分类号： C07D419/12 , C07D413/12 , A61K31/554 , A61K31/553 , A61P35/00
CPC分类号： C07D419/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The invention relates to compounds of Formula I pharmaceutically acceptable salt, ester or prodrug thereof:
摘要翻译：本发明涉及式I化合物的药学上可接受的盐，酯或前药：

5. 发明申请

WO2011041655A1 QUINAZOLIN-4-AMINE DERIVATIVES; AND METHODS OF USE 审中-公开
标题翻译：喹唑啉-4-胺衍生物; 和使用方法
公开(公告)号：WO2011041655A1
公开(公告)日：2011-04-07
申请号：PCT/US2010/051090
申请日：2010-10-01
申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , THOMAS, Craig, J. , MOTT, Bryan, T. , TANEGA, Cordelle , SHEN, Min , AULD, Douglas, S. , ROSENTHAL, Andrew, S. , MALONEY, David, J.
发明人： THOMAS, Craig, J. , MOTT, Bryan, T. , TANEGA, Cordelle , SHEN, Min , AULD, Douglas, S. , ROSENTHAL, Andrew, S. , MALONEY, David, J.
IPC分类号： C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , C07D419/14 , A61K31/517
CPC分类号： C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed herein are novel quinazolin-4-amine derivatives that are inhibitors of Clk1, Clk2, Clk3, Clk4, or Dyrk1A. Also disclosed are quinazolin-4-amine derivatives as potent and selective inhibitors of Clk1, Clk4, and Dyrk1A. These agents provide useful tools for the study of Clk1, Clk4 and Dyrk1A and their respective roles in pre-mRNA splicing. Methods of treating Clk1, Clk2, Clk4, or Dyrk1A kinase mediated disorders with certain quinazolin-4-amine derivatives are also disclosed.
摘要翻译：本文公开的是作为Clk1，Clk2，Clk3，Clk4或Dyrk1A的抑制剂的新的喹唑啉-4-胺衍生物。还公开了喹唑啉-4-胺衍生物作为Clk1，Clk4和Dyrk1A的有效和选择性抑制剂。这些试剂为研究Clk1，Clk4和Dyrk1A及其各自在mRNA前剪接中的作用提供了有用的工具。还公开了用某些喹唑啉-4-胺衍生物治疗Clk1，Clk2，Clk4或Dyrk1A激酶介导的病症的方法。

6. 发明申请

WO2011023795A1 (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：（THIO）吗啉衍生物作为S1P调节剂
公开(公告)号：WO2011023795A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062552
申请日：2010-08-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
发明人： IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
IPC分类号： C07D265/30 , C07D265/32 , C07D413/12 , C07D419/12 , C07D471/04 , A61K31/5377 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , C07D279/12 , C07D417/12 , C07D487/04
CPC分类号： C07D295/15 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04 , C07F9/6533
摘要： The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO 2 -(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH 3 -O- and the linking group –Y-(CH 2 ) n -X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -CH 2 -O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH 2 ) 2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH 2 -R5, wherein R5 is -OH, -PO 3 H 2 , -OPO 3 H 2 , -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO 2 -; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的（硫代）吗啉衍生物，其中R 1选自氰基，（2-4C）炔基，（1-4C）烷基，（3-6C）环烷基，（4-6C）环烷基，（6-8C）双环烷基，（8-10C）双环基团，各自任选被（1-4C）烷基，苯基，联苯基，萘基取代，各自任选被一个或多个独立地选自卤素，（1- 氨基，二（1-4C）烷基氨基，-SO 2 - （1-4C）烷氧基，被一个或多个氟原子烷基取代的（2-4C）炔基，任选被一个或多个氟原子取代的（1-4C）） - （1-4C）烷基，-CO-O-（1-4C）烷基，-NH-CO-（1-4C）烷基和（3-6C）环烷基，被苯氧基取代的苯基（1-4C）烷基或任选被（1-4C）烷基任意取代的苯基的单环杂环，和任选被取代的（1-4C）烷基的双环杂环，与（1-4C）烷基; A选自-CO-O-，-O-CO-，-NH-CO-，-CO-NH，-C = C-，-CCH 3 -O-和连接基-Y-（CH 2）n X- 其中Y连接到R 1并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - CH 2 -O-，-CO-，-O-CO-，-CO-O-， -CO-NH-，-NH-CO-，-C≡C-和-C = C-; n为1〜10的整数，并且X连接到亚苯基/吡啶基上，并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH，-CO - ， - C = C - 和-C = C- ; 环结构B任选地含有一个氮原子; R2是H，任选被一个或多个氟原子取代的（1-4C）烷基，（1-4C）任选被一个或多个氟原子取代的烷氧基或卤素; 并且R 3是（1-4C）亚烷基-R 5，其中亚烷基可以被（CH 2）2取代以形成环丙基部分或一个或两个卤素原子，或者R 3是（3-6C）亚环烷基-R 5或-CO -CH 2 -R 5，其中R 5是-OH，-PO 3 H 2，-OPO 3 H 2，-COOH，-COO（1-4C）烷基或四唑-5-基; R4是H或（1-4C）烷基; R6是一个或多个独立地选自H，（1-4C）烷基或氧代的取代基; W是-O - ， - S - ， - SO-或-SO 2 - ; 或其药学上可接受的盐，溶剂合物或水合物; 条件是式（I）的衍生物不是2-（4-乙基苯基）-4-吗啉代乙醇或4- [4-（2-羟乙基）-2-吗啉基]苯乙腈或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物对S1P受体具有亲和力，可用于治疗，缓解或预防S1P受体介导的疾病和病症。

7. 发明申请

WO2009027393A3 PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS 审中-公开
标题翻译：用于控制无节幼虫的吡唑类化合物
公开(公告)号：WO2009027393A3
公开(公告)日：2009-09-24
申请号：PCT/EP2008061136
申请日：2008-08-26
申请人： BASF SE , GROSS STEFFEN , BREUNINGER DELPHINE , BASTIAANS HENRICUS MARIA MARTI , DEYN WOLFGANG VON , PUHL MICHAEL , KOERBER KARSTEN , ANSPAUGH DOUGLAS D , CULBERTSON DEBORAH L , OLOUMI-SADEGHI HASSAN
发明人： GROSS STEFFEN , BREUNINGER DELPHINE , BASTIAANS HENRICUS MARIA MARTINUS , VON DEYN WOLFGANG , PUHL MICHAEL , KOERBER KARSTEN , ANSPAUGH DOUGLAS D , CULBERTSON DEBORAH L , OLOUMI-SADEGHI HASSAN
IPC分类号： A01N43/56 , A01N43/707 , A01N43/74 , A01N47/18 , A01P7/00 , C07D419/12 , C07D419/14
CPC分类号： A01N43/64 , A01N43/56 , A01N43/707 , A01N43/74 , A01N47/18 , C07D401/12 , C07D401/14 , C07D417/14
摘要： The present invention relates to novel pyrazole compounds of the formulae (I) and (II), to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae (A1), (A2) or (A3) # denotes the binding site to the remainder of formulae (I) or (II); X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.
摘要翻译：本发明涉及式（I）和（II）的新型吡唑化合物，涉及它们的盐和它们的N-氧化物，它们可用于防治或控制无脊椎动物害虫，特别是节肢动物害虫。本发明还涉及使用这些化合物防治无脊椎害虫的方法。本发明还涉及种子以及包含所述化合物的农业和兽医学组合物。其中A是式（A1），（A2）或（A3）的吡唑基团，表示与式（I）或（II）的其余部分的结合位点; X1是S，O或NR1a; X2是OR2a，NR2bR2c，S（O）mR2d; X3是孤对或氧; R 1，R 2和R 3尤其是氢，并且其中R 41，R 42，R 43，R 51，R 52，R 53，R 61，R 62，R 63如权利要求1中所定义。

8. 发明申请

WO0170692A3 HETEROCYCLIC ACYLSULFIMIDES, A METHOD FOR THEIR PRODUCTION, AGENTS CONTAINING THE SAME AND THEIR USE AS PESTICIDES 审中-公开
标题翻译：杂环ACYLSULFIMIDE，制作方法，代理商含相同的，它们作为杀虫剂
公开(公告)号：WO0170692A3
公开(公告)日：2002-03-14
申请号：PCT/EP0103083
申请日：2001-03-17
申请人： AVENTIS CROPSCIENCE GMBH , KORNUTA NATALIYA OLEXANDRIVNA , SHERMOLOVICH YURIY GRIGORIEVIC , DOELLER UWE , ORT OSWALD , SCHAPER WOLFGANG , JANS DANIELA , SANFT ULRICH , THOENESSEN MARIA THERESIA , BECKMANN MARION , WAIBEL JUTTA MARIA , PAZENOK SERGIY
发明人： KORNUTA PAVEL PETROVICH DI , SHERMOLOVICH YURIY GRIGORIEVIC , DOELLER UWE , ORT OSWALD , SCHAPER WOLFGANG , JANS DANIELA , SANFT ULRICH , THOENESSEN MARIA-THERESIA , BECKMANN MARION , WAIBEL JUTTA MARIA , PAZENOK SERGIY
IPC分类号： A01N43/40 , A01N43/54 , A01N43/80 , A01N43/84 , A01N43/88 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/549 , A61K31/55 , A61K31/554 , A61P31/10 , A61P33/14 , C07D213/78 , C07D213/82 , C07D239/28 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D417/12 , C07D419/12
CPC分类号： C07D213/78 , A01N43/40 , A01N43/54 , C07D239/28 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D419/12
摘要： The invention relates to acylsulfimides of formula (I), in which the symbols and indices are defined as per the description. Said acylsulfimides are suitable for controlling animal pests.
摘要翻译：式（I）的Acylsulfimide其中符号和标记具有在说明书中所示的含义，适于防治动物害虫。

9. 发明申请

WO98051665A2 NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：新型MACROCYCLIC化合物作为金属蛋白酶抑制剂
公开(公告)号：WO98051665A2
公开(公告)日：1998-11-19
申请号：PCT/US1998/009789
申请日：1998-05-14
IPC分类号： A61K31/395 , A61K31/422 , A61K31/427 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K38/00 , A61P1/02 , A61P1/14 , A61P7/02 , A61P7/04 , A61P19/02 , A61P21/00 , A61P25/32 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/18 , A61P37/06 , A61P43/00 , C07D245/02 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , C07D498/08 , C07D521/00 , C07K5/06 , C07K5/065 , C07K5/078 , C12Q1/37 , C07D
CPC分类号： C07D231/12 , A61K38/00 , C07D233/56 , C07D245/02 , C07D249/08 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/12 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C12Q1/37
摘要： This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.
摘要翻译：本发明涉及抑制金属蛋白酶（包括软骨聚集蛋白聚糖酶）和肿瘤坏死因子（TNF）产生的大环分子。特别地，化合物是参与组织降解的金属蛋白酶抑制剂和肿瘤坏死因子释放抑制剂。本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗炎性疾病的方法。

10. 发明申请

WO2020021215A1 DERIVES DEUTERES DU LANIFIBRANOR 审中-公开
公开(公告)号：WO2020021215A1
公开(公告)日：2020-01-30
申请号：PCT/FR2019/051860
申请日：2019-07-26
申请人： INVENTIVA
发明人： MONTALBETTI, Christian , BOUBIA, Benaissa
IPC分类号： C07D419/12 , A61K31/428 , A61P1/00 , A61P11/00 , A61P37/00 , A61P13/12
摘要： La présente invention concerne des dérivés deutérés du lanifibranor, notamment pour leur usage en thérapie, en particulier dans le traitement des maladies fibrotiques.

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