CAS: 50-65-7; 5-Chloro-N-(2-Chloro-4-Nitrophenyl)-2-Hydroxybenzamide

上下游产品

5-chloro-2-hydroxybenzoic acid 2-Chloro-4-nitroaniline 5-chloro-2-hydroxybenzoyl chloride 5-chloro-N-(2-chlorophenyl)-2-hydroxybenzamide6-chloro-3-(2-chloro-4-nitrophenyl)-2H-benzo[e][1,3]oxazine-2,4(3H)-dione 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-3-(piperidinomethyl)benzamide 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-3-(morpholinomethyl)benzamide e][1,3]oxazin-4-one6-chloro-3-(2-chloro-4-nitro-phenyl)-2-trifluoromethylimino-2,3-dihydro-benzo[e][1,3]oxazin-4-one

5-氯代水杨酸置于氯化亚砜体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,反应生成 氯硝柳胺
参考文献:针对 Sars-Cov-2 的氯硝柳胺类似物的设计,合成和生物学评价
标题:针对 Sars-Cov-2 的氯硝柳胺类似物的设计,合成和生物学评价
摘要:氯硝柳胺是一种广泛使用的驱虫药,通过tmem16F抑制和自噬诱导复制来抑制sars-Cov-2病毒进入,但相对较高的细胞毒性和较差的口服生物利用度限制了其应用.我们合成了 22 种氯硝柳胺类似物,其中发现化合物5具有最佳的抗 Sars-Cov-2 功效(ic 50 = 0.057 μm)和化合物6,10和11(ic 50 = 0.39,0.38 和 0.49 μm,分别)显示出与氯硝柳胺相当的功效.另一方面,化合物5,6,11在人血浆和肝脏s9酶测定中比氯硝柳胺具有更高的稳定性,口服给药时可以提高生物利用度和半衰期.荧光显微镜显示,与氯硝柳胺相比,化合物5在减少磷脂酰丝氨酸外化方面表现出更好的活性,这与 Tmem16F 抑制有关.应用人工智能预测的人tmem16F蛋白结构进行分子对接,揭示5的4'-No 2与arg809形成氢键,而氯硝柳胺则被2'-Cl阻断.
DOI:10.1016/j.Ejmech.2022.114295

专利信息

专利号:US-11708381-B2
优先权日:2016-11-25
标题:Inhibitors of androgen receptor signaling
发明人：WANG GUANGDI; LIU JIAWANG; ZHENG SHILONG; GUO SHANCHUN
权利人:XAVIER UNIV OF LOUISIANA
摘要:The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.

专利号:US-11434195-B2
优先权日:2017-07-20
标题:Compositions and methods for treatment of central nervous system tumors
发明人：SVETLOV STANISLAV IGOREVICH
权利人:UNIV FLORIDA
摘要:Compounds, pharmaceutical compositions, and methods for treating cancer, in particular brain cancer, are provided, including amphiphilic fatty acid/alcohol ethers (AIPs) comprising endocannabinoid and FABP motifs covalently linked to a beta-adrenoreceptor antagonist motif in one molecule. The invention includes methods for inhibiting growth of brain cancer cells by contacting the compound(s) with brain cancer cells. The invention provides a method for treating both brain cancer and brain cancer metastases, and for suppression of regrowth of brain cancer cells after radiation, surgical treatment, or chemotherapy of brain cancer. The invention also comprises an optimized chemical synthesis of the AIP compounds and methods of using the compounds, alone or in combination with another agent, for suppressing the growth of brain cancer cells, and enhancing survival of normal CNS cells, or improving recuperation from radiation, surgical or chemotherapy.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-9382288-B2
优先权日:2010-10-06
标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
发明人：BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

专利号:WO-2024028893-A1
优先权日:2022-08-01
标 题:Substituted benzimidazoles for treating viral diseases
发明人：CHAUDHARI VINOD DINKAR; THAKUR KRISHAN GOPAL; RINGE RAJESH PRAKASH; SINGH DESHKANWAR; KAUR SIMRAN; CHAWLA RAVNEET SINGH; JOSHI AKSHAY
权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S
摘要:The invention relates to benzimidazole compounds, pharmaceutically acceptable salts thereof and its pharmaceutical compositions for reducing/treating viral infections. The present invention also relates to synthesis of such benzimidazole compounds. The present invention further relates to compositions which comprise such benzimidazole compounds or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination. The compounds of the invention are useful in reducing/treating viral infections particularly coronavirus infections caused by SARS-CoV, MERS-CoV and SARS-CoV-2.

专利号:US-2024336679-A1
优先权日:2021-08-06
标题 :Methods for the treatment of cancer
发明人：LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.