CAS: 133550-30-8; (E)-N-Benzyl-2-Cyano-3-(3,4-Dihydroxyphenyl)Acrylamide

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CAS号10412-93-8 N-苄基-2-氰基乙酰胺 | CAS号139-85-5 原儿茶醛; 原二茶醛; 茶酚甲... | CAS号100-46-9 苄胺

📜苄胺 反应 16.0H,反应生成酪氨酸磷酸化抑制剂ag 490
参考文献:Tyrphostins. Ii. Heterocyclic And .Alpha.-Substituted Benzylidenemalononitrile Tyrphostins As Potent Inhibitors Of Egf Receptor And Erbb2/neu Tyrosine Kinases
标题:Tyrphostins. Ii. Heterocyclic And .Alpha.-Substituted Benzylidenemalononitrile Tyrphostins As Potent Inhibitors Of Egf Receptor And Erbb2/neu Tyrosine Kinases
摘要:We Have Previously Described A Novel Series Of Low Molecular Weight Protein Tyrosine Kinase Inhibitors Which We Named Tyrphostins. The Characteristic Active Pharmacophore Of These Compounds Was The Hydroxy-Cis-Benzylidenemalononitrile Moiety. In This Article We Describe Three Novel Groups Of Tyrphostins: (I) One Group Has The Phenolic Moiety Of The Cis-Benzylidenemalononitrile Replaced Either With Other Substituted Benzenes Or With Heteroaromatic Rings,(II) Another Is A Series Of Conformationally Constrained Derivatives Of Hydroxy-Cis-Benzylidenemalononitriles In Which The Malononitrile Moiety Is Fixed Relative To The Aromatic Ring,And (III) Two Groups Of Compounds In Which The Position Trans To The Benzenemalononitrile Has Been Substituted By Ketones And Amides. Among The Novel Tyrphostins Examined We Found Inhibitors Which Discriminate Between The Highly Homologous Egf Receptor Kinase (Her1) And Erbb2/neu Kinase (Her2). These Findings May Lead To Selective Tyrosine Kinase Blockers For The Treatment Of Diseases In Which Erbb2/neu Is Involved.
Doi:10.1021/jm00110A022

专利信息

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:US-2008096868-A1
优先权日:2004-11-12
标题:1,4 Substituted Pyrazolopyrimidines as Kinase Inhibitors
发明人：SCHMIEDEBERG NIKO; FURET PASCAL; IMBACH PATRICIA; HOLZER PHILIPP
权利人:SCHMIEDEBERG NIKO; FURET PASCAL; IMBACH PATRICIA; HOLZER PHILIPP
摘要:The invention relates to 1,4-substituted pyrazolopyrimidine compounds of the formula I, n npharmaceuticals comprising a 1,4-substituted pyrazolopyrimidine compound, the use of a 1,4-substituted pyrazolopyrimidine compound in the treatment or the use thereof in the manufacture of a pharmaceutical formulation for the treatment of a disease that depends on inadequate activity of a protein kinase, methods of treatment comprising administering a 1,4-substituted pyrazolopyrimidine compound, methods for the manufacture of a novel compound of that class, and novel intermediates and partial steps for their synthesis.

专利号:US-2022396794-A1
优先权日:2019-06-04
标题:APTAMERS AGAINST TRANSFERRIN RECEPTOR (TfR)
发明人：HABIB NAGY; ROSSI JOHN; YOON SORAH; SWIDERSK PIOTR MAREK
权利人:APTERNA LTD; HOPE CITY
摘要:Methods of treating or preventing a disease or disorder are disclosed comprising administering to a subject in need thereof an effective amount of a nucleic acid compound comprising, or consisting of, a nucleic acid sequence capable of binding to a transferrin receptor (TfR) and an effective amount of an inhibitor of DNA synthesis. Also disclosed is a nucleic acid compound comprising, or consisting of, a nucleic acid sequence having at least 85% sequence identity to SEQ ID NO: 1, wherein said nucleic acid sequence is at least 30 nucleotides in length and at most 50 nucleotides in length, and wherein the nucleic acid sequence is capable of binding to a transferrin receptor (TfR).

专利号:US-2008096883-A1
优先权日:2004-08-11
标题 :Trifluoromethyl substituted benzamides as kinase inhibitors
发明人：CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO
权利人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO
摘要:The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.

专利号:CN-108358893-A
优先权日:2018-02-10
标题:A kind of one-pot synthesis method of tetrahydrobenzo-[1,4]-diazepane derivatives