CAS: 14080-50-3; Thieno[2,3-D]Pyrimidin-4(3H)-One

相似化合物

56844-40-7 1378867-62-9 18740-38-0

上下游产品

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Methyl 2-Formylaminothiophene-3-Carboxylate置于甲酸铵,Formamide体系中,化学反应 4.0H,以86%的收率获得噻吩并[2,3-D]嘧啶-4(3H)-酮
参考文献:表皮生长因子受体的不可逆抑制剂:具有 α,β-不饱和酰胺侧链的噻吩并嘧啶核
标题:表皮生长因子受体的不可逆抑制剂:具有 α,β-不饱和酰胺侧链的噻吩并嘧啶核
摘要:表皮生长因子受体 (Egfr) 酪氨酸激酶的过度表达已在多种癌症中发现,例如乳腺癌,卵巢癌,结肠癌和非小细胞肺癌,这与患者的不良预后有关.为了寻找有效的 Egfr 酪氨酸激酶家族(主要是 Her2)的不可逆抑制剂,以噻吩并 [3,2-D] 吡啶和噻吩并 [2,3-D] 吡啶为中心部分的两个系列 Her2 酪氨酸激酶抑制剂和开发了具有碱性α,β-不饱和酰胺侧链的化合物.位于 6 位的 α,β-不饱和酰胺侧链(迈克尔受体)与位于 Egfr 酶的 Atp 结合口袋中的 Cys773 形成共价键,是产生不可逆抑制的主要因素.在我们的研究中,使用噻吩并嘧啶代替喹唑啉作为中心结构,并在4位引入不同的取代基以研究构效关系.噻吩并[2,3-D]嘧啶衍生物16A-D对sk-Br-3细胞显示出有效的her2酶抑制和抗增殖活性.特别是,(E)-N-(4-((3-Chloro-4-(Pyridin-2-Ylmet
Doi:10.1002/ardp.201400098

专利信息

专利号:WO-2023052971-A1
优先权日:2021-09-30
标题 :Automated synthesis of polymeric dual drugs

专利号:CN-105753877-A
优先权日:2012-04-12
标题:Asymmetric Synthesis of Spiro-Oxindole Compounds as Therapeutic Agents

专利号:CN-104350057-A
优先权日:2012-04-12
标题 :Asymmetric synthesis of spiro-oxindole compounds for use as therapeutic agents

专利号:US-2004138238-A1
优先权日:2002-08-08
标题 :Substituted aminopyrimidine compounds as neurokinin antagonists
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY
摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-7030240-B2
优先权日:2003-03-31
标 题:Piperidinylamino-thieno[2,3-d] pyrimidine compounds
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; REDDY SEKAR A; CHERUKU SRINIVASA RAO; MELE NDEZ ROSA E; SHARADENDU ANURAG; CHEN DONGLI; MARANTZ YAEL; SHACHEM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; KESAVAN VENKITASAMY; BAR-HAIM SHAY
权利人:PREDIX PHARMACEUTICALS HOLDING
摘要:The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno[2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as anxiety, depression, schizophrenia, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.