- As neuroprotective agents of pharmaceutical compounds
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The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
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- Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents
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A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 μg mL?1 and 6g was the most active compound (MIC = 0.625 μg mL?1). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 μg mL?1) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 μg mL?1). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.
- Zhang, Niu-niu,Liu, Zhi-yong,Liang, Jie,Tang, Yun-xiang,Qian, Lu,Gao, Ya-min,Zhang, Tian-Yu,Zhang, Tian-yu,Yan, Ming
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supporting information
p. 1293 - 1304
(2018/08/28)
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- Preparation technology of 3-cyano-5-anisole-1-sulfonyl chloride
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The invention discloses a preparation technology of 3-cyano-5-anisole-1-sulfonyl chloride. The technology comprises the following steps: performing substitution reaction on a raw material which is 3,5-dinitrobenzene to obtain 3-anisyl-5-nitrobenzoic acid;
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Paragraph 0014-0016; 0031-0033; 0048-0050; 0065-0067
(2018/03/26)
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- Synthesis of an Advanced Fragment of (+)-Trienomycinol
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The synthesis of the fully functionalized eastern fragment of trienomycins A-F, ansamycin antibiotics is described. A key step involves a peptidic coupling between a sulfonyl aniline and an enantiopure carboxylic acid obtained by a completely diastereosel
- Choppin, Sabine,Barbarotto, Marie,Obringer, Michel,Colobert, Fran?oise
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p. 3263 - 3271
(2016/09/09)
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- HETEROCYCLIC DERIVATIVES AND USE THEREOF
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A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
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Page/Page column 73; 74
(2015/01/06)
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- PHENYL-UREA AND PHENYL-CARBAMATE DERIVATIVES AS INHIBITORS OF PROTEIN AGGREGATION
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The present invention relates to certain phenyl-urea and phenyl-carbamate derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, and multiple system atrophy.
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Paragraph 0093
(2013/10/21)
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- NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
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Page/Page column 65
(2011/10/04)
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- NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
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Page/Page column 55
(2011/10/02)
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- BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 73
(2010/09/17)
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- Synthesis of potential early-stage intermediates in the biosynthesis of FR900482 and mitomycin c
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Beyond the identification of 3-amino-5-hydroxybenzoic acid (AHBA) and D-glucosamine as biosynthetic precursors to mitomycin C (5) and FR900482 (6), little is known about the pathway Nature uses to prepare these antitumor antibiotics. To gain some insight
- Chamberland, Stephen,Grueschow, Sabine,Sherman, David H.,Williams, Robert M.
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supporting information; experimental part
p. 791 - 794
(2009/08/15)
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- Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus
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Inhibition of the protein chaperone Hsp90 is a promising new approach to cancer therapy. We describe the preparation of potent non-benzoquinone ansamycins. One of these analogues, generated by feeding 3-amino-5-chlorobenzoic acid to a genetically engineer
- Menzella, Hugo G.,Tran, Thomas-Toan,Carney, John R.,Lau-Wee, Janice,Galazzo, Jorge,Reeves, Christopher D.,Carreras, Christopher,Mukadam, Sophie,Eng, Sara,Zhong, Ziyang,Timmermans, Pieter B. M. W. M.,Murli, Sumati,Ashley, Gary W.
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supporting information; experimental part
p. 1518 - 1521
(2010/02/28)
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- LEUKOTRIENE B4 INHIBITORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
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Page/Page column 35
(2009/07/18)
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- Macrolactams by engineered biosynthesis
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Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the biosynt
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Page/Page column 16
(2008/12/07)
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- NOVEL CONDENSED IMIDAZOLE DERIVATIVE
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Disclosed is a compound represented by the formula (1) below which has a high DPP-IV inhibitory activity and is improved in safety, toxicity and the like. Also disclosed is a prodrug of such a compound and pharmaceutically acceptable salts of them. (In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like; R2 and R3 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; R4 and R5 independently represent a hydrogen atom, an optionally substituted alkyl group or the like: R6 represents a hydrogen atom, an optionally substituted aryl group or the like; and -Y-NH2, represents a group represented by the following formula (A): (wherein m is 0, 1 or 2; and R7 may not exist or one or two R7 may exist and independently represent an optionally substituted alkyl group or the like) or the like.]
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Page/Page column 177-178
(2010/11/23)
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- Stereochemical assignment of intermediates in the rifamycin biosynthetic pathway by precursor-directed biosynthesis
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Natural and semisynthetic rifamycins are clinically important inhibitors of bacterial DNA-dependent RNA polymerase. Although the polyketide-nonribosomal peptide origin of the naphthalene core of rifamycin B is well established, the absolute and relative c
- Hartung, Ingo V.,Rude, Mathew A.,Schnarr, Nathan A.,Hunziker, Daniel,Khosla, Chaitan
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p. 11202 - 11203
(2007/10/03)
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- Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents
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A new series of 3-aminobenzophenone compounds as potent inhibitors of tubulin polymerization was discovered based on the mimic of the aminocombretastatin molecular skeleton. Lead compounds 5 and 11, with alkoxy groups at the C-4 position of B-ring, were p
- Liou, Jing-Ping,Chang, Jang-Yang,Chang, Chun-Wei,Chang, Chi-Yen,Mahindroo, Neeraj,Kuo, Fu-Ming,Hsieh, Hsing-Pang
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p. 2897 - 2905
(2007/10/03)
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- Antibiotic compounds
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The present invention relates to carbapenems and provides a compound of the formula (I): STR1 or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4 alkyl, nitro, hydroxy, carboxy, C1-4 alkoxy, C1-4 alkoxycarbonyl, aminosulphonyl, C1-4 alkylaminosulphonyl, di-C1-4 alkylaminosulphonyl, carbamoyl, C1-4 alkylcarbamoyl, di-C1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4 alkylamino, di-C1-4 alkylamino, C1-4 alkanoylamino, C1-4 alkanoyl(N-C1-4 alkyl)amino, C1-4 alkanesulphonamido and C1-4 alkylS(O)n -- wherein n is zero, one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the --NR2 --. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
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- Synthesis and biological activity of C-4 and C-15 Aryl azide derivatives of anguidine
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Potential trichothecene photoaffinity reagents were prepared by coupling either the C-4 or C-15 alcohols derived from anguidine with (3-azido-5-methoxyphenoxy) acetic acid, 4-(3-azido-5-methoxyphenoxy)butyric acid, or N-(3-azido-5-methoxyphenyl) N'-(carbo
- Richardson, Stewart K.,Jeganathan, Alwarsamy,Mani, Rajarathnam S.,Haley, Boyd E.,Watt, David S.,Trusal, Lynn R.
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p. 2925 - 2934
(2007/10/02)
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- Synthesis of Unlabelled and Carboxyl-Labelled 3-Amino-5-hydroxybenzoic Acid
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Efficient syntheses are reported of the natural amino acid 3-amino-5-hydroxybenzoic acid in unlabelled and carboxyl-labelled forms from 3,5-dinitrobenzoic acid and 3,5-dinitroanisole, respectively.
- Herlt, Anthony J.,Kibby, Jeffrey J.,Rickards, Rodney W.
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p. 1319 - 1324
(2007/10/02)
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- PRODUCTS FROM NITRATION OF 3,5-SUBSTITUTED BENZOIC ACIDS
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During the nitration of 3,5-substituted benzoic acids by a nitrating mixture one isomer is formed if one of the substituents is an acetylamino group.
- Nekhoroshev, A. A.,Sevbo, D. P.,Ginzburg, O. A.
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p. 313 - 317
(2007/10/02)
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