- TRICYCLIC PSYCHOPLASTOGENS AND USES THEREOF
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Disclosed herein are compounds, compositions, and methods for promoting neuronal growth and/or improving neuronal structure with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the loss of synaptic connectivity and/or plasticity, such as neurological diseases and disorders, with non-hallucinogenic psychoplastogens.
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Paragraph 00267; 00269
(2021/12/30)
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- 5-(4-PYRIDYLOXY)PYRAZOLE COMPOUNDS SERVING AS TGF-BETA R1 KINASE INHIBITOR
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Disclosed are a group of 5-(4-pyridyloxy)pyrazole compounds serving as a TGF-βR1 kinase inhibitor, and applications of same in preparing a TGF-βR1 kinase inhibitor medicament. Specifically disclosed are the compounds as represented by formula (I), a pharm
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Paragraph 0092-0093
(2021/12/23)
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- Pyrazolo-cyclic compound, pharmaceutical composition containing pyrazolo-cyclic compound, and preparation method and application of pyrazolo-cyclic compound
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The invention belongs to the field of medicinal chemistry, and relates to a pyrazolo-cyclic compound, a pharmaceutical composition containing the pyrazolo-cyclic compound, and a preparation method and application of the pyrazolo-cyclic compound. Specifica
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Paragraph 0408-0412
(2021/04/26)
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- Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
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1,2,4-Triazolo[3,4-a]pyridines and related heterocycles and substituted triazines were commonly discovered scaffolds in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as a catalyst, the mild reaction condition tolerates a broad substrate range and substitutes. The prepared 3-unsubstituted 1,2,4-triazolo[3,4-a]pyridine and derivatives allow further introduction of a variety of functional group1 at 3-position.
- Liu, Lingfeng,Qiao, Chunhua,Shen, Bei,Xu, Yiwen
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supporting information
(2020/04/01)
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- ASK1 inhibitor and application thereof
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The invention relates to compounds represented by a general formula (I) shown in the specification, a pharmaceutically acceptable salt and ester, or a stereoisomer of the compounds. The invention alsorelates to a preparation method of the compounds, a pharmaceutical preparation and a pharmaceutical composition containing the compounds. The compounds provided by the invention can effectively inhibit the amino acid phosphorylation of ASK1 and inhibit the activation of the ASK1; therefore, the compounds can treat and/or prevent ASK1-mediated diseases and related diseases.
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Paragraph 0169-0173
(2020/02/10)
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- PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT 1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
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Paragraph 0630-0632; 0640-0642
(2020/01/04)
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 0719
(2018/04/17)
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- Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia
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Small-molecule inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clinical development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increased erythropoiesis. Herein we describe the discovery, synthesis, structure–activity relationship (SAR), and proposed binding mode of novel 2,4-diheteroaryl-1,2-dihydro-3H-pyrazol-3-ones as orally bioavailable HIF-PH inhibitors for the treatment of anemia. High-throughput screening of our corporate compound library identified BAY-908 as a promising hit. The lead optimization program then resulted in the identification of molidustat (BAY 85-3934), a novel small-molecule oral HIF-PH inhibitor. Molidustat is currently being investigated in clinical phase III trials as molidustat sodium for the treatment of anemia in patients with CKD.
- Beck, Hartmut,Jeske, Mario,Thede, Kai,Stoll, Friederike,Flamme, Ingo,Akbaba, Metin,Ergüden, Jens-Kerim,Karig, Gunter,Keldenich, J?rg,Oehme, Felix,Militzer, Hans-Christian,Hartung, Ingo V.,Thuss, Uwe
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supporting information
p. 988 - 1003
(2018/04/19)
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- Exploring the unexplored practical and alternative synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate for Sitagliptin
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The practical synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate of Sitagliptin and 3-(trifluoromethyl)-triazolopyridine was carried out employing industrially feasible transformations. The other advantage of this method is the new environment friendly approach to synthesize triazolopiperazine and triazolopyridines by eliminating the commonly used trifluoroacetic anhydride and polyphosphoric acid.
- Nitlikar, Lakshmikant H.,Darandale, Sunil N.,Shinde, Devanand B.
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p. 348 - 352
(2013/07/26)
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- Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists
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Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(1) triazole, compound 51, was identified as a potent and selective Kv1.5 inhibitor with an acceptable PK and liability profile.
- Finlay, Heather J.,Jiang, Ji,Caringal, Yolanda,Kover, Alexander,Conder, Mary Lee,Xing, Dezhi,Levesque, Paul,Harper, Timothy,Hsueh, Mei Mann,Atwal, Karnail,Blanar, Michael,Wexler, Ruth,Lloyd, John
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supporting information
p. 1743 - 1747
(2013/04/10)
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- Therapeutic Pyrazolyl Thienopyridines
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The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGFβ-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
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Page/Page column 16
(2008/06/13)
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- Condensed pyrazole derivatives, process for producing the same and use thereof
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Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.
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- Heterocyclic substituted-amino-pyrazolines
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This invention relates to novel 3-amino-1-heteroaryl-2-pyrazolines and their C4 and C5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
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