专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2012282255-A1 优先权日:2011-04-07 标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence 发明人:PLUCINSKI GREG 权利人:PLUCINSKI GREG 摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.
专利号:WO-2024146880-A1 优先权日:2023-01-03 标题:Fluoro-oxysterols positron emission tomography (pet) radiotracers 发明人:POIROT MARC; COURBON FRÉDÉRIC; SAMADI MOHAMMAD; DE MEDINA PHILIPPE; SILVENTE POIROT SANDRINE; BRILLOUET SÉVERINE 权利人:INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT; UNIV TOULOUSE III – PAUL SABATIER; INST CLAUDIUS REGAUD; CT HOSPITALIER UNIVERSITAIRE TOULOUSE; UNIV DE LORRAINE 摘要:Radiopharmaceuticals-based biomedical imaging plays a growing role in cancer management, including diagnosis, tumor staging and aggressiveness and treatment monitoring. Even though 18Fluoro-2-deoxy glucose and 18Fluoroestradiol are currently used for some types of breast cancer, a need remains to develop other candidate compounds which are useful as radiotracers in a different/ broader range of cancer types. Thus, it is described a family of 18F radiolabeled compounds of formula (I) (wherein one of R2, R4, R5, R6, R7 and R12 is 18F) for use as Positron Emission Tomography imaging agents for the detection of cancers and metastatic sites thereof, as well as for monitoring and predicting the efficacy of a cancer treatment, wherein the cancer is associated to cholesterol-5,6- epoxide hydrolase and/or lip-hydroxy steroid dehydrogenase type (2) overexpression. To overcome the issues linked to the lifetime of the radioisotope 18F and, to ensure an effective synthesis of the 18F radiolabeled compounds of formula (I), a group of novel intermediate compounds in the synthesis thereof is also described.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
专利号:US-9884844-B2 优先权日:2012-12-31 标 题:Heterocyclic compounds and methods of use thereof 发明人:FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
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
1: Yamaguchi J, Hirayama T, Sadahiro R, Nakahara R, Matsuoka H. Delirium due to Trousseau syndrome treated with memantine and perospirone: A case report. PCN Rep. 2023 Nov 16;2(4):e159. doi: 10.1002/pcn5.159. 2: Kikuchi K, Hasegawa C, Sasaki T, Sato Y, Owada T, Shindo Y, Kawamata Y, Sugawara N, Yasui-Furukori N. Continuous alcohol withdrawal delirium and physical illness-associated delirium in a man brought to the emergency department after a disaster: A case report. Neuropsychopharmacol Rep. 2024 Apr 25. doi: 10.1002/npr2.12446. Epub ahead of print. 44(2):464-467. doi: 10.1002/npr2.12425. Epub 2024 Mar 18. 4: Ding J, Yang L, Meng Z, Tian M, Chen Y, Gong Y, Hu J, Wei B, Cui X. Therapeutic drug monitoring of perospirone: The lowest effective plasma concentration in patients with schizophrenia. Asian J Psychiatr. 2023 Dec;90:103832. doi: 10.1016/j.ajp.2023.103832. Epub 2023 Nov 17.
合成参考文献
摘要:Kaneda Y, Kawamura I, Fujii A, Ohmori T. Impact of a switch from typical to atypical antipsychotic drugs on quality of life and gonadal hormones in male patients with schizophrenia. Neuro Endocrinol Lett. 2004 Feb;25(1-2):135–40. 参考文献:10.1007/s00213-004-1905-8 摘要:Iwakawa M, Terao T, Soya A, Kojima H, Inoue Y, Ueda N, Yoshimura R, Nakamura J. A novel antipsychotic, perospirone, has antiserotonergic and antidopaminergic effects in human brain: findings from neuroendocrine challenge tests. Psychopharmacology (Berl). 2004 Nov;176(3-4):407–11. doi: 10.1007/s00213-004-1905-8. 参考文献:10.1017/s1461145705006292 摘要:Nakagawa M, Matsumura T, Kato D, Kishida I, Kawanishi C, Tamura K, Hirayasu Y. Neuroleptic malignant syndrome induced by perospirone. Int J Neuropsychopharmacol. 2006 Oct;9(5):635–6. doi: 10.1017/s1461145705006292.