专利号:WO-2025101716-A1 优先权日:2023-11-07 标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds 发明人:LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes described.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-9833457-B2 优先权日:2008-01-25 标题:Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors 发明人:MJALLI ADNAN M M; GADDAM BAPU; POLISETTI DHARMA RAO; KOSTURA MATTHEW J; GUZEL MUSTAFA 权利人:VTV THERAPEUTICS LLC 摘要:The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to psoriatic arthritis.
专利号:WO-2025068371-A1 优先权日:2023-09-28 标 题:Inhibitors of the proprotein convertase furin, methods of production thereof and use 发明人:STEINMETZER TORSTEN; LANGE ROMAN WERNER; BOLLER CHARLOTTE; FRIEBERTSHÄUSER EVA; BLOCH KONSTANTIN 权利人:PHILIPPS UNIV MARBURG 摘要:The invention relates to novel inhibitors of the serine protease furin and to related furin-like proprotein convertases according to claim 1, and to methods of synthesis thereof and to use for production of medicaments for treatment of furin-dependent viral and bacterial infection diseases, and other disorders involving furin, such as cystic fibrosis, cancer, osteoarthritis, hypertension, and neurodegenerative disorders.
专利号:US-6320049-B1 优先权日:1997-08-05 标题 :Alpha 1a adrenergic receptor antagonists 发明人:SIDLER DANIEL R; LARSEN ROBERT D; LI WENJIE 权利人:MERCK & CO INC 摘要:This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
参考文献:10.1023/b:jcam.0000004601.34056.c1 摘要:López-Rodríguez ML, Benhamú B, Murcia M, Álvaro E, Campillo M, Pardo L. Benzimidazole derivatives. 4. The recognition of the voluminous substituent attached to the basic amino group of 5-HT4 receptor antagonists. Journal of Computer-Aided Molecular Design. 2003 Aug;17(8):515–24. doi: 10.1023/b:jcam.0000004601.34056.c1.