CAS: 737789-87-6; 1-(4-(1-(2,6-Difluorobenzyl)-5-((Dimethylamino)Methyl)-3-(6-Methoxypyridazin-3-yl)-2,4-Dioxo-1,2,3,4-Tetrahydrothieno[2,3-D]Pyrimidin-6-yl)Phenyl)-3-Methoxyurea

上下游产品

1-(4-(1-(2,6-Difluorobenzyl)-5-(((2-Methoxyethyl) (Methyl)Amino)Methyl)-3-(6-Methoxypyridazin-3-yl)-2,4-Dioxo-1,2,3,4-Tetrahydrothieno[2,3-D]Pyrimidin-6-yl)Ph Enyl)-3-Methoxyurea
6-(4-Aminophenyl)-1-(2,6-Difluorobenzyl)-5-((Dimethylamino)Methyl)-3-(6-Methoxypyridazin-3-yl)Thieno[2,3-D]Pyrimidine-2,4(1H,3H)-Dione 1589503-93-4
1-(2,6-Difluorobenzyl)-5-((Dimethylamino)Methyl)-3-(6-Methoxypyridazin-3-yl)-6-(4-Nitrophenyl)Thieno[2,3-D]Pyrimidine-2,4(1H,3H)-Dione
Ethyl 2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-(((2-Methoxyethyl)(Methyl)Amino)Methyl)-5-(4-(3-Methoxyureido)Phenyl)Thiophene-3-Carboxylate 737789-92-3
Ethyl 2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-(((2-Methoxyethyl)(Methyl)Amino)Methyl)-5-(4-Nitrophenyl)Thiophene-3-Carboxylate 308832-01-1
2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-(((2-Methoxyethyl)(Methyl) Amino)Methyl)-5-(4-(3-Methoxyureido)Phenyl)Thiophene-3-Carboxylic Acid 737789-93-4
Ethyl 5-(4-Aminophenyl)-2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-(((2-Methoxyethyl)(Methyl)Amino)Methyl)Thiophene-3-Carboxylate 577780-07-5
Ethyl 2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-((Dimethylamino)Methyl)-5-(4-Nitrophenyl)Thiophene-3-Carboxylate 1589503-97-8
4-(溴甲基)-2-((2,6-二氟苄基)(乙氧基羰基)氨基)-5-(4-硝基苯基)噻吩-3-羧酸乙酯 Ethyl 4-(Bromomethyl)-2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-5-(4-Nitrophenyl)Thiophene-3-Carboxylate 308831-95-0
2-((2,6-Difluorobenzyl)(Ethoxycarbonyl)Amino)-4-((Dimethylamino)Methyl)-5-(4-Nitrophenyl)Thiophene-3-Carboxylic Acid 1589503-95-6

乙基2-((乙氧羰基)氨基)-4-甲基-5-(4-硝基苯基)噻吩-3-甲酸基酯置于盐酸,N-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,1-氯乙基氯甲酸酯,氰基磷酸二乙酯,Palladium 10% On Activated Carbon,氢气,Sodium Methylate,Potassium Carbonate,N,N-二异丙基乙胺,Potassium Iodide,Sodium Hydroxide体系中,用 甲醇,乙醚,乙醇,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,-78.0~60.0 °C,101.33 Kpa 条件下,反应 161.5H,反应生成 瑞卢戈利
参考文献:1-{4-[1-(2,6-二氟苄基)-5-[(二甲基氨基)甲基]-3-(6-甲氧基吡啶并-3-基)-2,4-二氧-1,2,3的发现,4-四氢噻吩并[2,3-D]嘧啶-6-基]苯基}-3-甲氧基脲(tak-385)作为人促性腺激素释放激素受体的有效,口服活性,非肽类拮抗剂
标题:1-{4-[1-(2,6-二氟苄基)-5-[(二甲基氨基)甲基]-3-(6-甲氧基吡啶并-3-基)-2,4-二氧-1,2,3的发现,4-四氢噻吩并[2,3-D]嘧啶-6-基]苯基}-3-甲氧基脲(tak-385)作为人促性腺激素释放激素受体的有效,口服活性,非肽类拮抗剂
摘要:我们以前发现了一种口服活性人促性腺激素释放激素(gnrh)受体拮抗剂,Thieno [2,3-D]嘧啶-2,4-Dione衍生物1(sufugolix).为降低细胞色素p450(cyp)抑制活性并提高体内gnrh拮抗活性,对该支架进行了进一步优化.基于计算模型,我们将合成工作集中在噻吩并[2,3-D]嘧啶-2,4-二酮环的5和3位的化学修饰上,从而发现了1-{4-[1-(2,6-二氟苄基)-5-[(二甲氨基)甲基]-3-(6-甲氧基吡啶并-3-基)-2,4-二氧-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基]苯基}-3-甲氧基脲(16B)作为高效和口服活性的gnrh拮抗剂.在没有cyp抑制的胎牛血清(fbs)存在下,化合物16B表现出强大的体外gnrh拮抗活性.口服16B维持3 H / Kg剂量的去势食蟹猕猴血浆黄体反应生成激素水平的抑制作用超过24小时.化合
DOI:10.1021/jm200216Q

专利信息

专利号:WO-2022214645-A1
优先权日:2021-04-09
标 题:Processes and intermediates for the preparation of relugolix
发明人：ETAYO PÉREZ PABLO; BALLANO BALLANO Mª GEMA; PUJOL OLLÉ XAVIER; GOMOLLÓN FRANCO PEDRO ANGEL
权利人:FARMHISPANIA GROUP S L
摘要:The invention relates to processes for the preparation of relugolix of formula (VIII), or a pharmaceutically acceptable salt thereof. It also relates to intermediates of formula (IX), (X), and (XI) as defined herein useful in the synthesis of this molecule.

专利号:US-2023391824-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
发明人：JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
权利人:NARENDRAN ARUMUGAVADIVEL
摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.

专利号:US-11491246-B2
优先权日:2020-07-13
标 题:Radiopharmaceutical and methods
发明人：MCCANN JOE
权利人:POINT BIOPHARMA INC
摘要:The radiopharmaceutical 177 Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177 Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177 Lu-PSMA I&T.

专利号:US-2025281509-A1
优先权日:2021-04-26
标 题 :Sequential hormone therapy to improve survival and enhance response to immune therapy in men with prostate cancer
发明人：DENMEADE SAMUEL R; ISAACS JOHN T; ANTONARAKIS EMMANUEL S; KACHHAP SUSHANT; MARKOWSKI MARK CHRISTOPHER
权利人:UNIV JOHNS HOPKINS
摘要:Disclosed are methods for treating men with castrate resistant prostate cancer with a sufficient dose of testosterone to achieve supraphysiologic serum levels of testosterone in sequence with androgen ablative treatment or androgen synthesis inhibitors for one or more cycles until evidence of radiographic progression, at which point the subject will receive immune checkpoint blockade therapy.

专利号:EP-4288444-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent

专利号:WO-2022165606-A1
优先权日:2021-02-08
标 题:Rationale, design, synthesis and validation of a small molecule anticancer agent