17903-89-8Relevant academic research and scientific papers
BCL-2 INHIBITORS AND THEIR USE AS PHARMACEUTICALS
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Paragraph 0486-0487; 0488-0489, (2021/11/13)
The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.
N-(3-nitro-4-alkoxybenzoyl)amino acid compounds as well as preparation method and application thereof
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Paragraph 0091-0095; 0108; 0109, (2019/10/01)
The invention discloses N-(3-nitro-4-alkoxybenzoyl)amino acid compounds as well as a preparation method and an application thereof and belongs to the field of medicines. 4-hydroxy-3-nitrobenzoic acidis subjected to methanol esterification, bromo-alkane substitution, hydrolysis and chlorination and then acylated with L-phenylglycine, R2 which is L-phenylglycine sodium salt is obtained, and the N-(3-nitro-4-alkoxybenzoyl)amino acid compounds are obtained after hydrolysis. The N-(3-nitro-4-alkoxybenzoyl)amino acid compounds have novel chemical structures, have good effects in an in-vitro xanthine oxidase inhibition activity test and can be used for treating and preventing gout diseases.
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases
Armani, Elisabetta,Amari, Gabriele,Rizzi, Andrea,Fanti, Renato De,Ghidini, Eleonora,Capaldi, Carmelida,Carzaniga, Laura,Caruso, Paola,Guala, Matilde,Peretto, Ilaria,La Porta, Elena,Bolzoni, Pier T.,Facchinetti, Fabrizio,Carnini, Chiara,Moretto, Nadia,Patacchini, Riccardo,Bassani, Franco,Cenacchi, Valentina,Volta, Roberta,Amadei, Francesco,Capacchi, Silvia,Delcanale, Maurizio,Puccini, Paola,Catinella, Silvia,Civelli, Maurizio,Villetti, Gino
supporting information, p. 793 - 816 (2014/03/21)
The first steps in the selection process of a new anti-inflammatory drug for the inhaled treatment of asthma and chronic obstructive pulmonary disease are herein described. A series of novel ester derivatives of 1-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3,5-dichloropyridin-4- yl) ethanol have been synthesized and evaluated for inhibitory activity toward cAMP-specific phosphodiesterase-4 (PDE4). In particular, esters of variously substituted benzoic acids were extensively explored, and structural modification of the alcoholic and benzoic moieties were performed to maximize the inhibitory potency. Several compounds with high activity in cell-free and cell-based assays were obtained. Through the evaluation of opportune in vitro ADME properties, a potential candidate suitable for inhaled administration in respiratory diseases was identified and tested in an in vivo model of pulmonary inflammation, proving its efficacy.
ARYLOXYPHENOXYACETYL-BASED COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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, (2012/05/05)
Disclosed are a compound inhibitory of HIF-1 activity, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound has anticancer activity which is attributable to its inhibitory activity against HIF-1, but not to non-selective cellular toxicity. Thus, having inhibitory activity against HIF-1, the compound or a pharmaceutically acceptable salt thereof can be used as an ingredient in an anticancer agent for various cancers including large intestine cancer, hepatic cancer, stomach cancer and breast cancer. Further, the compound or a pharmaceutically acceptable salt thereof is applicable to the treatment of diabetic retinopathy or arthritis which is aggravated upon the activation of VEGFA by HIF-1.
Novel bicyclic sulfonamide derivatives which are L-CPT1 inhibitors
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Page/Page column 29, (2010/11/28)
The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors
Lee, Kyeong,Lee, Jeong Hyung,Boovanahalli, Shanthaveerappa K.,Jin, Yinglan,Lee, Mijeoung,Jin, Xuejun,Kim, Jin Hwan,Hong, Young-Soo,Lee, Jung Joon
, p. 1675 - 1684 (2008/02/01)
Structural modification of a compound discovered during screening using an HRE-dependent reporter assay has revealed a novel class of HIF-1 inhibitors, which potently inhibit the HIF-1α protein accumulation and its target gene expression under hypoxic conditions in human hepatocellular carcinoma Hep3B cells.
SUBSTITUTED 4-BENZYLOXY-BENZOIC ACID AMIDE DERIVATIVES
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Page/Page column 29, (2010/11/25)
The present invention relates to novel substituted 4-benzyloxy-benzoic acid amide derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
