专利号:US-12054512-B2 优先权日:2017-11-10 标 题 :Sting modulator compounds, and methods of making and using 发明人:VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
专利号:US-2007287677-A1 优先权日:2004-03-30 标题 :Rad51 Expression Inhibitors, Pharmaceutical Agents Containing The Inhibitors As Active Ingredients, And Uses Thereof 发明人:KANEDA YASUFUMI 权利人:GENOMLDEA INC 摘要:A double stranded RNA having a specific nucleotide sequence is useful for treating cellular proliferative disorders. The double stranded RNA acts as siRNA against the Rad51 gene. The double stranded RNA of the present invention inhibits cellular proliferation itself. In addition, co-administration of the double stranded RNA with a chemotherapeutic agent further enhances its pharmacological effect. The combined use of the double stranded RNA with an agent having a nucleic acid synthesis-inhibitory activity or a nucleic acid-impairing activity is particularly effective.
专利号:US-8791263-B2 优先权日:2010-09-17 标 题 :Cortistatin A analog and use thereof 发明人:KOBAYASHI MOTOMASA; KOTOKU NAOYUKI; ARAI MASAYOSHI; TAMURA SATORU 权利人:KOBAYASHI MOTOMASA; KOTOKU NAOYUKI; ARAI MASAYOSHI; TAMURA SATORU; UNIV OSAKA 摘要:A compound represented by the general formula (M): n n n n n n n n n n n n (wherein R 1 represents a substituted or unsubstituted aromatic heterocyclic group, n R 2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR 3 , N(R 3 ) 2 , C(â•?O)OR 3 or C(â•?O)N(R 3 ) 2 , n R 3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, n R 4 represents a hydrogen atom, an oxygen atom or OR 5 , and n R 5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or n a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
1: Dou L, Xu Q, Wang M, Xiao Y, Cheng L, Li H, Huang W, Mei J, Jing Y, Bo J, Liu D, Yu L. Clinical efficacy of decitabine in combination with standard-dose cytarabine, aclarubicin hydrochloride, and granulocyte colony-stimulating factor in the treatment of young patients with newly diagnosed acute myeloid leukemia. Onco Targets Ther. 2019 Jun 28;12:5013-5023. doi: 10.2147/OTT.S200005. 2: Kawashima O, Kurihara T, Kamiyoshihara M, Sakata S, Ishikawa S, Morishita Y. Management of malignant pericardial effusion resulting from recurrent cancer with local instillation of aclarubicin hydrochloride. Am J Clin Oncol. 1999 Aug;22(4):396-8. doi: 10.1097/00000421-199908000-00015. 49(15):4357-62. 29(1):41-7. doi: 10.1177/147323000102900107. 33(5):618-22. 146(5):1457-1467. doi: 10.1002/ijc.32593. Epub 2019 Aug 14. 79(10):919-24. doi: 10.1002/jps.2600791016. 16(1):23-8. Japanese. 38(4):483-6. 97(16):e0434. doi: 10.1097/MD.0000000000010434. 11: Mori S, Shindo N, Miura H, Oki T, Inui T. [Studies on the stability of aclacinomycin hydrochloride. I. Stability of solution of aclacinomycin hydrochloride (author's transl)]. Jpn J Antibiot. 1980 Apr;33(4):466-71. Japanese. 66(11):2369-74. doi: 10.1002/1097-0142(19901201)66:11<2369::aid- cncr2820661120>3.0.co;2-z. 36(2):147-53. doi: 10.1111/j.1600-0609.1986.tb00819.x. 12(6):1318-22. Japanese.
合成参考文献
摘要:Drugs in Japan, -(5), 1995 摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 23(1999), 1981 摘要:Medicamentos de Actualidad., 18(513), 1982