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1. 发明申请

WO2022246555A1 METHOD FOR PRODUCING AN IONIZABLE LIPID 审中-公开
公开(公告)号：WO2022246555A1
公开(公告)日：2022-12-01
申请号：PCT/CA2022/050835
申请日：2022-05-26
申请人： NANOVATION THERAPEUTICS INC.
发明人： CIUFOLINI, Marco A. , SAADATI, Fariba , TAM, Anthony , KUREK, Daniel , WITZIGMANN, Dominik , KULKARNI, Jayesh
IPC分类号： C07C323/23 , A61K9/51 , A61K47/14 , A61K47/18 , A61K47/20 , C07C45/65 , C07C49/203 , C07C69/42 , C07C229/12 , C07C323/12 , C07C323/22 , C07C323/52 , C07D323/52 , C07D317/24 , C07D317/28 , C07F7/18 , C11C3/00 , C12N15/87 , C12N15/88
摘要： Provided herein is a method for producing an ionizable lipid that comprises: (i) reacting fatty esters in a Claisen condensation reaction in the presence of a catalyst, the Claisen condensation employing a weak base and carried out at a temperature of between -10 and 60 degrees Celsius to produce a ketoester; (ii) reacting the ketoester produced in step (i) under conditions to produce a ketone from the ketoester in one or more steps via a hydrolysis and decarboxylation of the ketoester; and (iii) preparing the ionizable lipid from the ketone thereof using one or more synthesis steps resulting in an addition of an ionizable head group moiety to (a) the ketone; or (b) an alcohol produced from an optional reduction of the ketone to produce the alcohol, thereby producing the ionizable lipid. The ionizable lipid produced in step (iii) may be formulated in a drug delivery vehicle.

2. 发明申请

WO2020006229A1 COMPOUNDS FOR INHIBITION OF INFLAMMATION 审中-公开
公开(公告)号：WO2020006229A1
公开(公告)日：2020-01-02
申请号：PCT/US2019/039499
申请日：2019-06-27
申请人： CHILDREN'S MEDICAL CENTER CORPORATION
发明人： WU, Hao , LIEBERMAN, Judy , HU, Jun , LIU, Xing
IPC分类号： A61K31/10 , A61K31/27 , C07C323/00 , C07C323/23
摘要： The present application provides chemical compounds useful, for example, in inhibiting gasdermin pore formation in a cell, inhibiting inflammasome-mediated death of a cell (pyroptosis); inhibiting cytokine secretion from a cell, inhibiting an inflammatory caspase in a cell, and/or covalently reacting with a cysteine of a gasdermin protein in a cell. These compounds are also useful in treating or preventing diseases or conditions in which inflammasome activation is implicated in pathogenesis. One example of such disease or condition is sepsis.

3. 发明申请

WO9214696A3 SUBSTITUTED (ALPHA)-AMINOALDEHYDES AND DERIVATIVES 审中-公开
标题翻译：取代（ALPHA） - 胺衍生物和衍生物
公开(公告)号：WO9214696A3
公开(公告)日：1993-02-18
申请号：PCT/US9201077
申请日：1992-02-21
申请人： DU PONT MERCK PHARMA
发明人： HODGE CARL NICHOLAS
IPC分类号： A61K31/16 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/215 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/66 , A61K38/00 , C07C237/22 , C07C237/42 , C07C243/32 , C07C245/02 , C07C271/22 , C07C307/04 , C07C311/01 , C07C311/54 , C07C317/48 , C07C323/23 , C07C327/48 , C07C335/16 , C07D207/335 , C07D209/20 , C07D211/14 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/56 , C07D213/58 , C07D215/38 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/42 , C07D239/80 , C07D257/04 , C07D277/20 , C07D277/56 , C07D295/08 , C07D307/66 , C07D311/08 , C07D317/46 , C07D333/22 , C07D401/12 , C07F9/09 , C07K5/06 , C07K5/065 , C07K14/81 , A61K31/195 , A61K31/27 , C07C323/25
CPC分类号： C07D213/56 , A61K38/00 , C07C237/22 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07K5/06078
摘要： This invention relates to substituted α-aminoaldehydes, pharmaceutical compositions containing them and methods for using such compounds as antiviral agents.

4. 发明申请

WO2019178166A1 AMPHIPHILIC THIOL COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2019178166A1
公开(公告)日：2019-09-19
申请号：PCT/US2019/021944
申请日：2019-03-12
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： BREA FERNANDEZ, Roberto, Javier , RUDD, Andrew , DEVARAJ, Neal
IPC分类号： C07C323/16 , A61P25/00 , A61P35/00 , C07C323/12 , C07C323/22 , C07C323/23
摘要： Provided herein are, inter alia, amphiphilic thiol compounds and methods of using the same for the purpose of depalmitoylating proteins in cellular membranes (e.g., plasma membranes). The compounds provided herein include an amphiphilic tail, which enables them to associate with a cellular membrane and depalmitoylate (cleave native S-palmitoyl groups from) a protein in said membrane by native chemical ligation thereby triggering the protein's release from the plasma membrane. The compounds (amphiphilic thiol compounds of formula (I), (II), (III)) are, inter alia , useful for the treatment of diseases caused or associated with aberrant depalmitoylation of certain proteins (e.g., HRas, EGFR).

5. 发明申请

WO2003087047A1 METAL CHELATE COMPOSITION, MACROMOLECULE COMPLEX THEREOF, PREPARING METHOD THEREOF AND USE 审中-公开
标题翻译：金属螯合物组合物，其分子复合物，其制备方法和用途
公开(公告)号：WO2003087047A1
公开(公告)日：2003-10-23
申请号：PCT/KR2002/000948
申请日：2002-05-20
申请人： PEPTRON CO., LTD. , KIM, Seong-Kyu , CHOI, Ho-Il , JUNG, Young-Hwan , LIM, Chae-Jin
发明人： KIM, Seong-Kyu , CHOI, Ho-Il , JUNG, Young-Hwan , LIM, Chae-Jin
IPC分类号： C07C323/23
CPC分类号： C07C323/58 , B01J45/00
摘要： The present invention provides a novel metal chelate composition and its macromolecule complex. The invention also provides a preparation method of the metal chelate composition and method of using the metal chelate composition in purifying substance like peptide. The metal chelate composition of the present invention is expressed by the formula HS-R.sub.1 -CH(COOH)-N-(CH.sub.2 COOH).sub.2 (wherein R.sub.1 represents alkyl group linker having 1∼5 carbon atoms), and exhibits sufficient affinity and stability on the substance to be purified by simple process.
摘要翻译：本发明提供了一种新型金属螯合物组合物及其大分子复合物。本发明还提供了金属螯合物组合物的制备方法以及使用金属螯合物组合物来纯化物质如肽的方法。本发明的金属螯合物组合物由式HS-R表示-CH（COOH）-N-（CH 2 COOH）2（其中R 1表示烷基具有1〜5个碳原子的连接体），并且通过简单的方法对待纯化的物质表现出足够的亲和力和稳定性。

6. 发明申请

WO02053624A1 CROSSLINKED DISULPHIDE CONTAINING POLYMERS FOR DRUG DELIVERY 审中-公开
标题翻译：用于药物递送的含交联聚合物的交联聚合物
公开(公告)号：WO02053624A1
公开(公告)日：2002-07-11
申请号：PCT/GB2001/005787
申请日：2001-12-28
IPC分类号： A61K9/48 , C07C323/41 , C07C323/60 , C08G83/00 , C08G69/42 , A61K9/00 , C07C319/02 , C07C319/14 , C07C323/23 , C07C323/50
CPC分类号： C08G83/003 , A61K9/4891 , C07C323/41 , C07C323/60
摘要： A polymer crosslinked by means of disulphide bonds and which degrades at low redox potential sites in the body (e.g. colon, the ischaemic heart, post-stroke brain, rheumatoid joints, tumours etc.) is used to form a delivery device for selective delivery of an active agent to the site. Monomers useful for producing disulphide crosslinked polymers are trithiiols of formula (I), where A = straight or branched alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; B = NH, NHCO or CONH; K = straight or branched alkyl; D = a bond, CONH-alkylidene or NHCO-alkylidene; R1 = H or NR 2; R2 = H or COR ; R = H, alkyl, or an amino acid or peptide residue; R = OH, or an amino or peptide residue and alkyl is C1-C6 alkyl.
摘要翻译：通过二硫键交联并在体内的低氧化还原电位（例如结肠，缺血性心脏，中风后脑，类风湿关节，肿瘤等）中降解的聚合物用于形成递送装置，用于选择性递送一个活跃的代理到该网站。可用于生产二硫化物交联聚合物的单体是式（I）的三元醇，其中A =直链或支链烷基，取代或未取代的芳基或取代或未取代的杂芳基; B = NH，NHCO或CONH; K =直链或支链烷基; D =键，CONH-亚烷基或NHCO-亚烷基; R1 = H或NR1; R2 = H或COR11; R 1 = H，烷基或氨基酸或肽残基; R 11 = OH，或氨基或肽残基，烷基是C 1 -C 6烷基。

7. 发明申请

WO9301165A3 AROMATIC COMPOUNDS, COMPOSITIONS CONTAINING THEM AND THEIR USE IN THERAPY 审中-公开
标题翻译：芳香化合物，包含它们的组合物及其在治疗中的使用
公开(公告)号：WO9301165A3
公开(公告)日：1993-04-29
申请号：PCT/GB9201241
申请日：1992-07-08
申请人： MERCK SHARP & DOHME
发明人： OWENS ANDREW PATE , WILLIAMS BRIAN JOHN
IPC分类号： A61K31/165 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/695 , A61K38/00 , A61P3/08 , A61P11/00 , A61P17/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/08 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/10 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C237/22 , C07C255/13 , C07C255/24 , C07C255/54 , C07C261/04 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/28 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C317/18 , C07C323/23 , C07D207/28 , C07D209/04 , C07D233/64 , C07D235/04 , C07D241/08 , C07D257/04 , C07D295/084 , C07D295/185 , C07K5/06 , A61K31/135 , C07C251/40 , C07C255/22
CPC分类号： C07D295/185 , A61K38/00 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/10 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/13 , C07C255/24 , C07C255/54 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C2601/02 , C07D207/28 , C07D241/08 , C07D295/092 , C07K5/06026
摘要： Compounds of formula (I) and salts and prodrugs thereof wherein, Q is optionally substituted phenyl, heteroaryl or naphthyl; X and Y are each H, C1-6 alkyl, C2-6 alkenyl or X and Y are together =O; Z is O or S; R1 is H, optionally substituted C¿1-6? alkyl, optionally substituted phenyl(C1-4 alkyl), C2-6 alkylene, COC1-6 alkylhalo, COR?a, COORa, CONHRa¿, COC¿1-6?alkylNR?aRb¿ or CONRaC1-6alkylCONRaRb; R2 is substituted C¿1-6? alkyl, optionally substituted phenyl(C1-4 alkyl), C2-6 alkylene, C1-6alkylhalo, COR?a, COORa, CONHRa¿, COC¿1-6?alkylNR?aRb¿ or CONRaC1-6alkylCONR?aRb; or R1 and R2¿ together form a chain (CH¿2?)p optionally substituted by oxo; R?3¿ is H or C¿1-6? alkyl; R?4¿ is H, C¿1-6? alkyl or phenyl; and R?5¿ is optionally substituted (CH¿2?)qphenyl; are tachykinin antagonists useful for treating pain.

8. 发明申请

WO2020148617A1 3-SUBSTITUTED PHENYLAMIDINE COMPOUNDS, PREPARATION AND USE THEREOF 审中-公开
公开(公告)号：WO2020148617A1
公开(公告)日：2020-07-23
申请号：PCT/IB2020/050213
申请日：2020-01-13
申请人： PI INDUSTRIES LTD.
发明人： NAIK, Maruti , MAHAJAN, Vishal A. , SIVAKUMAR, S. , RATHOD, Kishor Singh , GUMME, Sachin Nagnath , AUTKAR, Santosh Shridhar , GARG, Ruchi , VENKATESHA, Hagalavadi M , KLAUSENER, Alexander G.M.
IPC分类号： C07C323/23 , C07C255/61 , C07C211/52 , C07C251/24 , C07D213/58 , C07C255/58 , A01N37/52 , A01N43/40 , A01N43/54 , A01N43/60 , A01N43/78 , C07D213/74 , C07D239/42 , C07D241/12 , C07D241/20 , C07D277/64
摘要： The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 4a , R 4b , A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent.

9. 发明申请

WO2019096325A1 一种双酰胺复合物及其制备方法和用途审中-公开
公开(公告)号：WO2019096325A1
公开(公告)日：2019-05-23
申请号：PCT/CN2018/116375
申请日：2018-11-20
申请人：江苏达骏生物科技有限公司
发明人：李谷丰 , 王贻杰 , 夏丽 , 邓双胜 , 刘勇
IPC分类号： C07C233/64 , C07C323/29 , C07C323/24 , C07C323/23 , C07C319/22 , C07C231/02 , G01N33/558 , G01N33/58
CPC分类号： C07C231/02 , C07C233/64 , C07C319/22 , C07C323/23 , C07C323/24 , C07C323/29 , G01N33/558 , G01N33/58
摘要：本发明涉及一种双酰胺复合物及其快速检测有机磷和氨基甲酸酯类农药的方法。本发明制备出的复合物能有效检测微量的有机磷和氨基甲酸酯类农药，而且使用方便、检测时间短、灵敏性高、稳定性好。故本发明可广泛应用于蔬菜、水果等农产品及环境中的微痕量有机磷和氨基甲酸酯类农药的残留检测，也可用于对食品和环境安全评价、监控其有机磷和氨基甲酸酯类农药的污染情况等。

10. 发明申请

WO2017053360A1 BICYCLIC AND TRICYCLIC CAP BEARING MERCAPTOACETAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：作为脱乙酰壳多糖酶抑制剂的双卡宾托胺衍生物
公开(公告)号：WO2017053360A1
公开(公告)日：2017-03-30
申请号：PCT/US2016/052780
申请日：2016-09-21
申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
发明人： KOZIKOWSKI, Alan , VALLERINI, Gian Paolo , SEGRETTI, Mariana , LV, Wei
IPC分类号： A61K31/16 , C07C233/05 , C07C323/23
CPC分类号： C07D215/40 , C07D215/08 , C07D215/18
摘要： Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
摘要翻译：公开了组蛋白脱乙酰酶抑制剂（HDACI）和包含其的组合物。治疗疾病和病症的方法，其中HDAC的抑制提供益处，如癌症，神经变性疾病，周围神经病，神经病，外伤性脑损伤，中风，高血压，疟疾，自身免疫疾病，自闭症，自闭症谱系障碍，和炎症，也被公开。

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