CAS: 1222998-36-8; 1-(4-(4-Propionylpiperazin-1-yl)-3-(Trifluoromethyl)Phenyl)-9-(Quinolin-3-yl)Benzo[h][1,6]Naphthyridin-2(1H)-One

上下游产品

quinolin-3-ylboronic acid tert-butyl 4-(4-amino-2-(trifluoromethyl)phenyl)piperazine-1-carboxylate 6-bromo-4-chloroquinoline-3-carboxylic acid ethyl ester 9-(6-aminopyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one

6-溴-4-氯-3-喹啉羧酸乙酯置于sodium Tetrahydroborate,四(三苯基膦)钯,乙醇,Sodium Carbonate,Potassium Carbonate,戴斯-马丁氧化剂,三乙胺,三氟乙酸体系中,用 四氢呋喃,甲醇,乙醇,二氯甲烷,水,1,2-二氯乙烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 12.67H,反应生成N-3-吡啶-4-[[3-[[5-(三氟甲基)-2-吡啶]氧基]苯基]甲基]-1-哌啶羧酰胺
参考文献: Method Of Blocking Transmission Of Malarial Parasite[fr] Procédé De Blocage De La Transmission D'Un Parasite Paludéen
标题: Method Of Blocking Transmission Of Malarial Parasite[fr] Procédé De Blocage De La Transmission D'Un Parasite Paludéen

专利信息

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2022185854-A1
优先权日:2019-04-16
标题 :Tfeb mutants and their use in the treatment and/or prevention of disorders that require the induction of the cellular autophagy-lysosomal system
发明人：ROJAS-FERNANDEZ ALEJANDRO; BURGOS PATRICIA; GONZÃ?LEZ ALEXIS
权利人:UNIV AUSTRAL DE CHILE
摘要:The invention relates to constitutively active mutants of the transcription factor TFEB, which can mutate the lysine of one or both sites of positions 219 and 347; and/or also mutate the glutamic acid of one or both sites of positions 221 and 349, in order to eliminate the SUMOylation of the protein. By replacing these residues either from positions 219 and/or 221 and/or 347 and/or 349 by any other amino acid (such as arginine or alanine), it gives rise to a mutated TFEB, which more actively induces the expression of genes and protein synthesis of the lysosomal and autophagic pathway. Such as lysosomal storage disorders, neurodegenerative diseases, liver diseases, muscle diseases and metabolic diseases, and/or disorders or processes in the aging of the skin.

专利号:US-2017153225-A1
优先权日:2014-07-09
标题 :A method of screening for a compound capable of stimulating glucose transport into brown and/or brite adipocytes of a mammal, a kit for use in such a method
发明人：BENGTSSON TORE
权利人:ATROGI AB
摘要:A method of screening for a candidate compound for use in the treatment of a condition involving dysregulation of metabolism in a mammal by identifying a compound capable of stimulating de novo synthesis of GLUT1 (Glucose transporter 1) in brown and/or brite adipocytes of the mammal and/or capable of stimulating translocation of GLUT1 in brown and/or brite adipocytes of the mammal. A kit for use in the method.

专利号:US-2025268920-A1
优先权日:2022-04-20
标 题:Use of androgen receptor-mediated mechanisms in the treatment of acute myeloid leukemia
发明人：QIAN FENGHUA; PRABHU KUMBLE SANDEEP; PAULSON ROBERT F
权利人:PENN STATE RES FOUND
摘要:Provided is a method for treating a blood cancer in an individual in need thereof by administrating to the individual an agent that inhibits activity or expression of one or more enzymes that participate in synthesis of either or both dihydrotestosterone (DHT) or androgen receptor (AR), or an antagonist AR, or a combination of an agent and the antagonist. The methods are shown in connection with acute myeloid leukemia (AML).

专利号:US-12150934-B2
优先权日:2016-11-30
标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
发明人：SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD
权利人:BANTAM PHARMACEUTICAL LLC
摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

专利号:EP-4058432-A1
优先权日:2019-11-14
标 题:Improved synthesis of kras g12c inhibitor compound