专利号:WO-2008084057-A1 优先权日:2007-01-10 标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G 权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G 摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.
专利号:EP-4630405-A1 优先权日:2022-12-06 标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
专利号:US-8138174-B2 优先权日:2007-01-10 标 题:Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G 权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SOLVAY PHARM BV 摘要:Compounds with a combination of cannabinoid CB 1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. n In at least one embodiment, the invention relates to compounds of the general formula (1): n nwherein the substitutents have the definitions given in the specification.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:WO-2024123815-A1 优先权日:2022-12-06 标 题:Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
专利号:US-8796286-B2 优先权日:2005-06-10 标 题:Agent for treatment of liver diseases containing pyrazolopyrimidinone derivative 发明人:CHOI SEUL MIN; AHN BYONG OK; YOO MOOHI 权利人:CHOI SEUL MIN; AHN BYONG OK; YOO MOOHI; MEZZION PHARMA CO LTD 摘要:The present invention relates to the pharmaceutical composition for prevention and treatment of liver diseases containing pyrazolopyrimidine derivative as an active ingredient. According to the present invention, pyrazolopyrimidine derivative has an excellent effect on inhibiting collagen synthesis in hepatic stellate cells and acts directly on the portal vein. Particularly, it may increase the diameter and the amount of blood flow of the portal vein, and finally decrease the pressure thereof. Therefore, pyrazolopyrimidine derivative can be used advantageously for prevention and treatment of hepatic fibrosis, liver cirrhosis caused by hepatic fibrosis, portal hypertension and various complications caused by portal hypertension. In addition, pyrazolopyrimidine derivative according to the present invention can reduce dosing frequency because of its long half-life, and therefore, has an advantage to improve the drug compliance of patients suffering from chronical liver diseases.
1: Amdani S, Shezad MF, Kroslowitz B, Townsend M, Joong A, Najm H, Marino BS, Rosenthal DN, Lorts A, O'Connor MJ. Outcomes for Children With Congenital Heart Disease Undergoing Ventricular Assist Device Implantation: An ACTION Registry Analysis. J Am Coll Cardiol. 2024 Dec 19:S0735-1097(24)10047-2. doi: 10.1016/j.jacc.2024.10.083. Epub ahead of print. 16(8):e68117. doi: 10.7759/cureus.68117. 3: Ismail EA, El-Sakka AI. An overview of conventional and investigational phosphodiesterase 5 inhibitors for treating erectile dysfunction and other conditions. Expert Opin Investig Drugs. 2024 Sep;33(9):925-938. doi: 10.1080/13543784.2024.2388569. Epub 2024 Aug 11. 43(7):1686-1698. doi: 10.1002/nau.25337. Epub 2023 Nov 30. Pediatric Heart Network Investigators. The Effect of Udenafil on Heart Rate and Blood Pressure in Adolescents With the Fontan Circulation. Am J Cardiol. 2024 Jan 1;210:183-187. doi: 10.1016/j.amjcard.2023.09.115. Epub 2023 Oct 31.
合成参考文献
参考文献:10.1038/ijir.2015.23 摘要:Choi BR, Kumar SK, Zhao C, Zhang LT, Kim CY, Lee SW, Jeon J, So I, Kim SH, Park NC, Kim HK, Park JK. Additive effects of Artemisia capillaris extract and scopoletin on the relaxation of penile corpus cavernosum smooth muscle. International Journal of Impotence Research. 2015 Oct 08;27(6):225–32. doi: 10.1038/ijir.2015.23. 参考文献:10.1177/147323000303100608 摘要:Kang KK, Ahn GJ, Sohn YS, Ahn BO, Kim WB. DA-8159, a new PDE5 inhibitor, attenuates the development of compensatory right ventricular hypertrophy in a rat model of pulmonary hypertension. J Int Med Res. 2003 Nov;31(6):517–28. doi: 10.1177/147323000303100608. 参考文献:10.3346/jkms.2004.19.4.586 摘要:Cho HK, Kang KK, Ahn GJ, Shim HJ, Kim WB. Effect of DA-8159, a selective phosphodiesterase type 5 inhibitor, on electroretinogram and retinal histology in rabbits. J Korean Med Sci. 2004 Aug;19(4):586–90.