在 10 Wt% Pd(Oh)2 On Carbon,氢气体系中,用 四氢呋喃,乙醇 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 16.0H,反应生成 N-乙酰基胍 参考文献:Discovery Of 5,6,7,8-Tetrahydropyrido[3,4-D]Pyrimidine Inhibitors Of Erk2 标题:Discovery Of 5,6,7,8-Tetrahydropyrido[3,4-D]Pyrimidine Inhibitors Of Erk2 摘要:The Discovery And Optimization Of A Series Of Tetrahydropyridopyrimidine Based Extracellular Signal-Regulated Kinase (Erks) Inhibitors Discovered Via Hts And Structure Based Drug Design Is Reported. The Compounds Demonstrate Potent And Selective Inhibition Of Erk2 And Knockdown Of Phospho-Rsk Levels In Hepg2 Cells And Tumor Xenografts. (C) 2014 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2014.04.068
专利号:WO-2023086801-A1 优先权日:2021-11-09 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-2025049736-A1 优先权日:2021-12-16 标 题 :Sulfonamide derivatives and their use as soluble epoxide hydrolase inhibitors 发明人:IYER MALLIGA R; KUNDU BISWAJIT 权利人:THE US SECRETARY DEPARTMENT OF HEALTH 摘要:The present invention relates to compounds of formulae I and II. The compounds are useful for treating hypertension, atherosclerosis, pulmonary diseases, diabetes, pain, fibrosis, addictive disorders, inflammation, and immunological disorders or a condition treatable or preventable by inhibition of soluble epoxide hydrolase. Preferred compounds are N-((adamantan-1-yl)carbamoyl)-benzenesulfonamide derivatives. Exemplary compounds are e.g. •N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-methylbenzenesulfonamide (example 14, compound 4a) •4-(tert-butyl)-N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)benzenesulfonamide (example 15, compound 4b) •N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-(trifluoromethyl)benzenesulfonamide (example 16, compound 4j). The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof.
专利号:US-8623880-B2 优先权日:2009-03-23 标 题 :Fused pyrimidine-dione derivatives as TRPA1 modulators 发明人:CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; DESHMUKH VISHAL GOVINDRAO; DHONE SACHIN VASANTRAO; CHIKHALE RAJENDRA PRAKASH; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 权利人:CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; DESHMUKH VISHAL GOVINDRAO; DHONE SACHIN VASANTRAO; CHIKHALE RAJENDRA PRAKASH; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL; GLENMARK PHARMACEUTICALS SA 摘要:The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
专利号:US-9000159-B2 优先权日:2009-03-23 标 题 :Fused pyrimidine-dione derivatives as TRPA1 modulators 发明人:CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; DESHMUKH VISHAL GOVINDRAO; DHONE SACHIN VASANTRAO; CHIKHALE RAJENDRA PRAKASH; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 权利人:GLENMARK PHARMACEUTICALS SA; GLENMARK PHARMACEUTICALS SA 摘要:The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
专利号:WO-2014016766-A1 优先权日:2012-07-25 标 题:Guanidine derivatives as trpc modulators 发明人:LINGAM V S PRASADA RAO; THOMAS ABRAHAM; DAHALE DNYANESHWAR HARISHCHANDRA; RATHI VIJAY EKNATH; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 权利人:GLENMARK PHARMACEUTICALS SA 摘要:The present invention is directed to guanidine derivatives as inhibitors of transient receptor potential canonical channels (TRPC channels), in particular TRPC3 and/or TRPC6 and/or TRPC7 activity, more particularly TRPC6 activity. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by TRPC channels (Formula (I)).
[参考文献]: Takayuki Inoue, Et Al. Novel 1H-Imidazol-2-Amine Derivatives As Potent And Orally Active Vascular Adhesion Protein-1 (Vap-1) Inhibitors For Diabetic Macular Edema Treatment. Bioorg Med Chem. 2013 Jul 1;21(13):3873-81.