- ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF
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The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
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Page/Page column 81
(2020/03/05)
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- ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I" PATHWAY AND METHODS OF USE THEREOF
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The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
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Paragraph 0523
(2020/03/01)
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- 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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Paragraph 0713; 0714; 0715; 0716
(2019/06/26)
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- Substituted benzene and heterocyclic compound and its preparation method and application
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The invention provides substituted benzoheterocyclic compounds and a preparation method thereof. The compounds have structures shown by formulas I and II. The invention also provides the effects of the compounds shown by formulas I and II in resisting virus, tumor and the like. The invention further provides a medicine composition taking the compounds shown by the formulas I and II as active ingredients, and the anti-virus or anti-tumor effect of the medicine composition. The invention lays a foundation for the future in-depth study and development of the anti-virus or anti-tumor medicine of the compounds.
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Paragraph 0393; 0394; 0395; 0465; 0466; 0467
(2016/10/20)
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- QUINAZOLINE-BASED KINASE INHIBITORS
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The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Page/Page column 125; 126
(2016/04/26)
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- ANTIVIRAL COMPOUNDS
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Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
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Paragraph 0542
(2015/03/13)
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- ARYL AMIDE KINASE INHIBITORS
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The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Page/Page column 176
(2015/02/02)
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- Synthesis and biological evaluation of berberine derivatives as IBS modulator
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Irritable bowel syndrome is the most common functional gastrointestinal disorder characterized by chronic abdominal pain or discomfort in association with a change in bowel habit. 5-HT receptor modulators have been developed as IBS therapeutic agents and proved to be effective in the treatment of the disease. In this letter, 12 berberine derivatives were designed and synthesized as 5-HT receptor modulators. Preliminary biological tests suggested that the new compounds exhibited promising activity for IBS therapy.
- Deng, Xin,Zhao, Xinxin,Han, Jing,Wang, Jingjie,Huang, Wenlong,Qian, Hai,Ge, Liang
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p. 489 - 493
(2012/08/29)
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- RADIOPROTECTOR COMPOUNDS AND METHODS
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The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection). Preferred compounds of the invention are those of Formula (II), as follows: wherein W represents -N(R1R2) where R1 and R2 are not both hydrogen and where they may together form a 5, 6 or 7 membered ring structure, -NHN(R1R2), NHR3N(R1R2), -NHR3OR2, -N(R3)R3OR2, -N(R1)R3OR3OR3, OR3NR1R2, -OR3 or W represents piperidyl, piperazinyl, morpholinyl, thiomorpholinyl or diazepanyl each of which may be optionally substituted by C1 to C4 alkyl, C2 to C4 alkenyl, -N(CO)N(R1R2), -N(CO)OR1, -N(CO)OR3OH, -(CO)NR1R2, -R3(CO)NR1R2, -R3OR1, -OR1, -N(R1R2) OR -NH-; R1 and R2 are the or different and are selected from hydrogen, C1 to C4 alkyl or C2 to C4 alkenyl; group or chain; Z is the same or different and represents N or CH; Z' is the same or different and represents N or C; X represents CH, N or NH, where .. is a double bond when X is CH or N and a single bond when X is NH; X' represents N or NH, wherein when X is CH or N X' is NH and wherein X and X' are different and further where ~~~is a double bond when X' is N and a single bond when X' is NH; Q represents H, alkoxyl, -NR1R2, F or Cl; Q1 is absent when Z' is N and when Z' is C it represents H, alkoxyl, -NR1R2, F or Cl; A represents a five to ten membered single or multiple ring structure with heterocyclic N or O located at the ortho position, said ring including optional double bonds, substitutions and/or other heteroatoms and pharmaceutically acceptable derivatives thereof.
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Page/Page column 118-119
(2011/10/31)
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- Syntheses of some thiazolidin-4-ones as potential antimicrobial agents
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4-Acetamido-2-methoxybenzoyl hydrazine (1) on condensation with different aromatic aldehydes yielded the substituted benzal-(4'- acetamido-2'- methoxybenzoyl)hydrazines (2a-f) which on cyclization with thioglycolic acid in presence of anhydrous aluminium chloride as catalyst afforded 2-(substituted phenyl)-3-(4'-acetamido-2'-methoxy benzamido)-5-H-thiazolidin-4-ones (3a-f). The structures of the newly synthesized compounds have been established by analytical and spectral methods. These compounds have also been screened for their biological activity.
- Havaldar, Freddy H.,Sharma, Azad Kumar S.
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scheme or table
p. 1314 - 1316
(2011/12/16)
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- Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors
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The synthesis and structure-activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded compounds with improved enzymatic and cellular potency.
- Hasvold, Lisa A.,Wang, Le,Przytulinska, Magdalena,Xiao, Zhan,Chen, Zehan,Gu, Wen-Zhen,Merta, Philip J.,Xue, John,Kovar, Peter,Zhang, Haiying,Park, Chang,Sowin, Thomas J.,Rosenberg, Saul H.,Lin, Nan-Horng
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p. 2311 - 2315
(2008/09/21)
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- Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma
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The imaging potential of a series of [123I]benzamides was studied in mice bearing B16F0 melanoma tumors. Compound [123I]25 exhibited tumor uptake >8 %ID/g at 1 h, while that of [123I]14d and [123I]25 reached a maximum of 9-12 %ID/g at 6 h. Standardized uptake values of [123I]14d were higher than 100 between 24 and 72 h after injection. In haloperidol treated animals, the tumor uptake of [ 123I]14d was not significantly different to controls, while significant reduction of [123I]25 uptake was observed, supporting that [123I]14d uptake relates to melanin interaction, whereas part of the mechanism of [123I]25 uptake is related to its σ1-receptor affinity. Benzamides 14d and 25, which display rapid and high tumor uptake, appear to be promising imaging agents for melanoma detection, while 14d, which displays a long lasting and high melanoma/nontarget ratio, is more suitable for evaluation as a potential radiotherapeutic.
- Pham, Tien Q.,Greguric, Ivan,Liu, Xiang,Berghofer, Paula,Ballantyne, Patrice,Chapman, Janette,Mattner, Filomena,Dikic, Branko,Jackson, Timothy,Loc'h, Christian,Katsifis, Andrew
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p. 3561 - 3572
(2008/02/09)
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- 2-?(1H-benzimidazol-2-ylsulfinyl)methyl!benzenamines
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This invention relates to 2-?(1H-benzimidazol-2-ylsulfinyl)methyl!benzenamines that are useful in the treatment and prevention of ulcers.
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- Inotropic activity of heterocyclic analogues of isomazole
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Aryl-substituted benzimidazole, imidazopyridine, imidazopyrazine, imidazopyridazine, oxazolopyridine, purine, pyrollopyridine and thiazolopyridine derivatives have been prepared and evaluated as inotropic agents.Purine 8 and the 1H-imidazo- and pyridazines 9 and 10 proved to be of most interest, having similar in vivo inotropic potencies to sulmazole.The pKa's, protonation sites and lipophilicities for most heterocycles were determined experimentally and some of their electronic properties calculated.For a subset of active heterocycles a correlation was observed between in vitro inotropism and the charge density of the imidazo nitrogen adjacent to the electrostatic potential minimum.Structure-activity relationships are discussed in some detail.
- Barraclough, P.,Beams, R. M.,Black, J. W.,Cambridge, D.,Collard, D.,et al.
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p. 467 - 477
(2007/10/02)
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- SYNTHESIS OF THE BACTERIAL COENZYME METHOXATIN
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A short total synthesis of the bacterial coenzyme methoxatin (1) (4,5-dihydro-4,5-dioxo-1H-pyrroloquinoline-2,7,9-tricarboxylic acid) is described.The route involves the two step conversion of 4-acetamido-2-benzyloxybenzaldehyde (5b) into methyl 6-acetamido-4-benzyloxyindole-2-carboxylate (7b) (74percent), followed by regioselective annulation of the third ring (55percent), and debenzylation and oxidation with benzoyl t-butyl nitroxide to give the tricyclic quinone triester (13) (methoxatin triester) (83percent).
- MacKenzie, A. Roderick,Moody, Christopher J.,Rees, Charles W.
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p. 3259 - 3268
(2007/10/02)
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- Aromatic amides of heterocyclic compounds and therapeutic compositions containing same
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The invention relates to aromatic amides N-substituted by heterocyclic groups. More particularly, the invention relates to substituted benzoic acid amides of 1-arylalkylamino or aminoalkyl-N-heterocyclic rings and to pharmaceutical compositions thereof, which have the ability to antagonize the effects of dopamine or dopaminergic agents of endogenous or exogenous origin and which may be used for the treatment of nausea and vomiting resulting from gastrointestinal disorders, congestive heart failure, post operative conditions, etc., other gastrointestinal disorders such as dyspepsia, flatulence, bile regurgitations, hiatus hernia, peptic ulcer, reflux aerophagitis, gastritis, duodenitis, and cholethiasis, and a variety of conditions affecting the central nervous system such as acute and chronic psychoses, maniacal psychosis, schizophrenias, serious disturbances of behavior and non-melancholic depressive state and migraine.
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