📜苯甲基苯酚置于偶氮二甲酸二异丙酯,Potassium Carbonate,三苯基膦体系中,用 四氢呋喃,甲苯 作为反应溶剂,化学反应 18.0H,反应生成 苯托沙敏 参考文献:Dopamine/serotonin Receptor Ligands. 9. Oxygen-Containing Midsized Heterocyclic Ring Systems And Nonrigidized Analogues. A Step Toward Dopamine D5 Receptor Selectivity 标题:Dopamine/serotonin Receptor Ligands. 9. Oxygen-Containing Midsized Heterocyclic Ring Systems And Nonrigidized Analogues. A Step Toward Dopamine D5 Receptor Selectivity 摘要:Eleven-Membered Heterocycles (Dibenz[g,J]-1-Oxa-4-Azacycloundecenes) And Open-Chain Analogues Were Synthesized And Investigated For Affinities To Human Dopamine Receptor Subtypes. The Moderately Rigidized Rings Displayed Nanomolar And Sulmanomolar K-I Values At D-1-Like Receptors With A Significant D-1 To D-2 And A Slight D-5 To D-6 Selectivity. The Open-Chain Analogues Showed Lower Affinities But Significant D-1 To D-2 Selectivities. Compound 3 (K-I(D-5) = 0.57 Nmol) Showed Antagonistic Or Inverse Agonistic Binding Characteristics In A Functional Ca Assay. DOI:10.1021/jm049720X
专利号:WO-2023075715-A1 优先权日:2021-10-26 标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids) 发明人:OYTUN FARUK; CAN EFE 权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI 摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.
专利号:US-5922335-A 优先权日:1995-05-15 标 题:Uses for ascorbyl-phosphoryl-cholesterol in topical compositions 发明人:PTCHELINTSEV DMITRI 权利人:AVON PROD INC 摘要:Novel uses of 3'-(L-ascorbyl-2-o-phosphoryl)-cholesterol, 3'-(L-ascorbyl-3-o-phosphoryl)-cholesterol, structural or functional isomers thereof and salts thereof (referred to collectively as 'APC compounds') are disclosed. Such novel uses include a method of reducing epidermal synthesis of abnormal elastin, especially epidermal synthesis of abnormal elastin that results from exposure to UV radiation. Also disclosed is a novel method of stimulating keratinocyte formation of triglycerides. In addition, a novel method of achieving antioxidant activity, both in the skin and also in topical compositions, is disclosed.
专利号:US-2013030282-A1 优先权日:2011-07-18 标题:Synthesis and characterization of near ir fluorescent magnetic and non-magnetic albumin nanoparticles for biomedical applications 发明人:MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL 权利人:UNIV BAR ILAN; MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL 摘要:The present invention discloses Near Infrared (NIR) fluorescent albumin nanoparticles having a structure selected from a core structure or a core-shell structure. Also disclosed are a process of preparing these NIR fluorescent albumin nanoparticles, and a method of in vivo detection of pathologies, in particular cancer pathology, by using administering these NIR fluorescent albumin nanoparticles to a patient.
专利号:CA-2190468-A1 优先权日:1994-05-19 标题 :Synthesis of optically pure 4-alkenyl- or 4-alkanyl-2-hydroxytetronic acids
专利号:US-2005053642-A1 优先权日:2000-08-23 标题:Biocompatible materials 发明人:ULBRICHT MATHIAS; THOM VOLKMAR; JANKOVA KATJA; ALTANKOV GEORGE; JONSSON GUNNAR 摘要:The present invention teaches a novel approach of creating biocmpatible surfaces, said surfaces being capable of functionally interact with biological material. SAid biocompatible surfaces comrise at least two comonents, such as a hydrophobic substratum and a macromolecule of hydrophilic nature, which, in a cooperativity, form together the novel biocoompatible surfaces. The novel approach is ased on contacting said hydrophobic substratum with a laterally patterned monomolecular layer of said hydrophilic and flexible macromolecules, exhibiting a pronounced excluded volume. The htus formed two component surface is, in respect to polarity and morphology, a molecularly heterogeneous surface. Structural features of said macromolecular monolayer (as e.g. the layer thickness or its lateral density) are determined by: i) the structural features of the layer forming macromolecules (as e.g. their MW or their molecular architecture) and ii) the method of creating said monomolecular layer (as e.g. by physi- or chemisorbing, or by chemically binding said macromolecules). The structural features of the layer forming macromolecules(s) is in turn determined by synthesis. AMount and conformation and thus also biological activity of biological material (as e.g. polypeptides) which contact the novel biocompatible surface, is determined and maintained by the cooperative action of the underlying hydrophobic substratum and the macromolecular layer. In this way it becomes possible to maintain and control biological interactions between said contacted polypeptides and other biological compounds as e.g. cells, antibodies and the like. Consequently, the present invention aims to reduce and/or eliminate the deactivation and/or denaturation associated with the contacting of polypeptides and/or other biological material to a hydrophobic substratum surface.
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Phenyltoloxamine. 2017 Jan 16. 163(5):357. 36(6):678-9. doi: 10.1016/0039-9140(89)80263-2. 4(4):221-6. doi: 10.1002/j.1875-9114.1984.tb03362.x. 55(10):1465-7. 36(5):403-16. doi: 10.1016/0024-3205(85)90252-8. 59(1):486-497. doi: 10.1021/acs.jcim.8b00521. Epub 2018 Dec 14. 24(3):147-57. Italian. 41(3):140-4. 91:1015-8.