CAS: 115308-98-0; Tallimustine

该化合物是一种属于氮芥子类的合成烷基制剂,主要特征是能够与DNA形成共价联系,导致DNA的交叉连接并随后抑制DNA的复制和转录.这一行动机制使Tallimustine成为用于癌症化学治疗,特别是某些类型的恶性肿瘤的候选药物.该化合物通常在临床环境中施用,并因其可能对快速分裂细胞产生细胞毒性影响而闻名.在物理特性方面,Tallimustine在室温上是固态的,在有机溶剂中可溶解,有助于其配制治疗用途.安全和处理预防措施由于其毒性性质至关重要,被归类为危险物质.研究继续探索其功效和安全特征及其潜在副作用,其中可包括叶酸抑制和与电动剂有关的其他系统毒性.

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      专利信息


      专利号:US-8734846-B2
      优先权日:2008-06-16
      标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
      发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
      权利人:BIND BIOSCIENCES INC
      摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

      专利号:US-2013035307-A1
      优先权日:2010-01-26
      标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
      发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
      权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
      摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

      专利号:US-9220714-B2
      优先权日:2006-03-16
      标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
      发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
      权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
      摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

      专利号:US-2024382626-A1
      优先权日:2023-05-16
      标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof
      发明人:PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA
      权利人:UNIV TEXAS
      摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.

      专利号:WO-2023091726-A1
      优先权日:2021-11-18
      标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
      发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
      权利人:SYROS PHARMACEUTICALS INC
      摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).

      专利号:US-2008281105-A1
      优先权日:2005-01-18
      标题:Novel Quinolinium Salts and Derivatives
      发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE
      权利人:IMMUSOL INC
      摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.

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      主要参考文献

      1. Pezzoni G, Grandi M, Biasoli G, Capolongo L, Ballinari D, Giuliani FC, Barbieri B, Pastori A, Pesenti E, Mongelli N, et al. Biological profile of FCE 24517, a novel benzoyl mustard analogue of distamycin A. Br J Cancer. 1991 Dec;64(6):1047-50. doi: 10.1038/bjc.1991.463.

      合成参考文献


      参考文献:10.1186/1475-9268-3-2
      摘要:Nelson SM, Ferguson LR, Denny WA. DNA and the chromosome - varied targets for chemotherapy. Cell Chromosome. 2004 May 24;3(1):2.
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