专利号:US-2004138238-A1 优先权日:2002-08-08 标题 :Substituted aminopyrimidine compounds as neurokinin antagonists 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY 摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-7030240-B2 优先权日:2003-03-31 标 题:Piperidinylamino-thieno[2,3-d] pyrimidine compounds 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; REDDY SEKAR A; CHERUKU SRINIVASA RAO; MELE NDEZ ROSA E; SHARADENDU ANURAG; CHEN DONGLI; MARANTZ YAEL; SHACHEM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; KESAVAN VENKITASAMY; BAR-HAIM SHAY 权利人:PREDIX PHARMACEUTICALS HOLDING 摘要:The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno[2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as anxiety, depression, schizophrenia, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
参考文献:10.1007/s10600-024-04266-x 摘要:Berdiev AU, Ortikov IS, Turgunov KK, Elmuradov BZ, Abdullaev ND, Tashkhodzhaev B. New Hybrid Cytisine Derivatives Containing a Thienopyrimidine Fragment. Chem Nat Compd. 2024 Jan;60(1):127–32. doi: 10.1007/s10600-024-04266-x. 参考文献:10.1007/978-3-031-91656-4_2 摘要:Hatvate N, Akolkar HN, Haghi AK. Applications in Chemistry. 2025 Jun 20. In: Synthesis Lectures on Chemical Engineering and Biochemical Engineering.