CAS: 285983-48-4; 1-(3-(Tert-Butyl)-1-(P-Tolyl)-1H-Pyrazol-5-yl)-3-(4-(2-Morpholinoethoxy)Naphthalen-1-yl)Urea

上下游产品

3-(tert-butyl)-5-is°Cyanato-1-(p-tolyl)-1H-pyrazole 4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-ylamine phosgene 3-amino-5-tert-butyl-2-(p-tolyl)-2H-pyrazole hydr°Chloride1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-{4-[2-(4-oxy-morpholin-4-yl)-ethoxy]-naphthalen-1-yl}-urea 2-methyl-2-(5-{3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-ureido}-1-p-tolyl-1H-pyrazol-3-yl)-propionic acid 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea.hydr°Chloride

(4-(2-吗啉乙氧基)萘-1-基)氨基甲酸叔丁酯置于盐酸,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环 用作溶剂,化学反应 20.0H,反应生成1-[2-(4-甲基苯基)-5-叔丁基吡唑-3-基]-3-[4-(2-吗啉-4-基乙氧基)萘-1-基]脲
参考文献:Pyrazole Urea-Based Inhibitors Of P38 Map Kinase: From Lead Compound To Clinical Candidate
标题:Pyrazole Urea-Based Inhibitors Of P38 Map Kinase: From Lead Compound To Clinical Candidate
摘要:We Report On A Series Of N-Pyrazole,N'-Aryl Ureas And Their Mode Of Binding To P38 Mitogen Activated Protein Kinase. Importantly,A Key Binding Domain That Is Distinct From The Adenosine 5'-Triphoshate (Atp) Binding Site Is Exposed When The Conserved Activation Loop,Consisting In Part Of Asp168-Phe169-Gly170,Adopts A Conformation Permitting Lipophilic And Hydrogen Bonding Interactions Between This Class Of Inhibitors And The Protein. We Describe The Correlation Of The Structure-Activity Relationships And Crystallographic Structures Of These Inhibitors With P38. In Addition,We Incorporated Another Binding Pharmacophore That Forms A Hydrogen Bond At The Atp Binding Site. This Modification Affords Significant Improvements In Binding,Cellular,And In Vivo Potencies Resulting In The Selection Of 45 (Birb 796) As A Clinical Candidate For The Treatment Of Inflammatory Diseases.
Doi:10.1021/jm020057R

专利信息

专利号:US-12006337-B2
优先权日:2018-05-30
标题:Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof
发明人：HOLTZMAN MICHAEL J; ROMERO ARTHUR G; GEROVAC BENJAMIN J; HAN ZHENFU; KEELER SHAMUS P; WU KANGYUN; ZHANG YONG
权利人:WASHINGTON UNIVERSITY ST LOUIS
摘要:Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutically for a variety of diseases, including cancer and respiratory diseases. Methods of synthesis of the compounds are also disclosed.

专利号:US-6894173-B2
优先权日:1999-07-09
标 题 :Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same
发明人：ZHANG LIN-HUA; ZHU LEI
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-6916924-B2
优先权日:2001-02-15
标 题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
发明人：TAN ZHULIN; SONG JINHUA J
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): which are useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. X, Ar, L, Q and are described herein.

专利号:US-2003166931-A1
优先权日:1999-07-09
标 题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents

专利号:WO-2023241717-A1
优先权日:2022-06-16
标题:Substance for promoting regeneration and repair of organs of mammals and use thereof
发明人：LI WEI; ZHOU QI; He zheng-quan; LU ZONGBAO; WANG SHUAI; WANG XIN; YUAN XUEWEI; WANG LIU
权利人:INST ZOOLOGY CAS; BEIJING INST FOR STEM CELL AND REGENERATIVE MEDICINE
摘要:Provided is use of a substance capable of up-regulating ISG gene expression in preparing a drug or reagent for promoting the regeneration and repair capacity of tissues or complex structures or organs of mammals. The substance for up-regulating ISG gene expression is selected from one or two or more of an MAPK inhibitor, a retinoic acid receptor-related orphan receptor inhibitor, a protein synthesis inhibitor, and an interferon (IFNγ, β, λ) or alarmin (S100A8/A9) protein. The regeneration and repair refer to promoting the regeneration of tissues or complex structures or organs after tissue or organ resection or damage.