- Cyanato - benzimidazole salt and its preparation method
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The present invention discloses a new metal cyano-substituted benzimidazolide salt having formula (I) and its preparation. This new cyano-substituted benzimidazole derivatives exhibited excellent thermal stability. The organic salt of the present inventio
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Paragraph 0067
(2017/08/25)
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- NOVEL SUBSTITUTED BICYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS
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The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
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Paragraph 0275; 0276
(2016/06/13)
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- Novel substituted bicyclic compounds as bromodomain inhibitors
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The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
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Paragraph 0304; 0305
(2016/10/07)
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- A novel benzimidazole derivative binds to the DNA minor groove and induces apoptosis in leukemic cells
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DNA minor groove binders are an important class of chemotherapeutic agents. These small molecule inhibitors interfere with various cellular processes like DNA replication and transcription. Several benzimidazole derivatives showed affinity towards the DNA
- Hegde, Mahesh,Sharath Kumar, Kothanahally S.,Thomas, Elizabeth,Ananda, Hanumappa,Raghavan, Sathees C.,Rangappa, Kanchugarakoppal S.
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p. 93194 - 93208
(2015/11/17)
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- Synthesis of riboflavines, quinoxalinones and benzodiazepines through chemoselective flow based hydrogenations
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Robust chemical routes towards valuable bioactive entities such as riboflavines, quinoxalinones and benzodiazepines are described. These make use of modern flow hydrogenation protocols enabling the chemoselective reduction of nitro group containing building blocks in order to rapidly generate the desired amine intermediates in situ. In order to exploit the benefits of continuous processing the individual steps were transformed into a telescoped flow process delivering selected benzodiazepine products on scales of 50 mmol and 120 mmol respectively.
- Baumann, Marcus,Baxendale, Ian R.,Hornung, Christian H.,Ley, Steven V.,Rojo, Maria Victoria,Roper, Kimberley A.
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p. 9736 - 9759
(2014/08/05)
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- Synthesis and Catalytic Activity of Square-Planar Ni(II) Complexes of Bis-N,N′-disubstituted Oxamides and Related Ligands for Epoxidation of Olefins
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Four new monomeric square-planar nickel(II) complexes of two bis-N,N′-disubstitute oxamides and related ligands have been prepared and characterized, namely [NMe4]2[Ni(L)]·xH 2O, where L = dbopba = 3,5-dibromo-o-phenylenebis-(oxamate) and dbmeopba = 3,5-dibromo-o-phenylenebis-(N′-methyloxamidate), L = meopba = 4-methyl-o-phenylenebis-(oxamate) and memeopba = 4-methyl-o-phenylenebis- (N′-methyloxamidate). NMe4 is thetetramethylammonium cation. Based on elemental analyses, IR and UV spectroscopies and molar conductance data, the complexes are proposed to have a square-planar structure. Their catalytic activities for aerobic epoxidation of olefins with co-oxidation of iso-butylaldehyde have been discussed.
- Zheng,Wang,Yan
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- Glycine receptor antagonists and the use thereof
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Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal. Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
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- Synthesis and structure-activity relationships of substituted 1,4- dihydroquinoxaline-2,3-diones: Antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors
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A series of mono-, di-, tri-, and tetrasubstituted 1,4- dihydroquinoxaline-2,3-diones (QXs) were synthesized and evaluated as antagonists at N-methyl-D-aspartate (NMDA)/glycine sites and α-amino-3- hydroxy-5-methylisoxazole-4-propionic acid-preferring non-NMDA receptors. Antagonist potencies were measured by electrical assays in Xenopus oocytes expressing rat whole brain poly(A)+ RNA. Trisubstituted QXs 17a (ACEA 1021), 17b (ACEA 1031), 24a, and 27, containing a nitro group in the 5 position and halogen in the 6 and 7 positions, displayed high potency (K(b) ~ 6-8 nM) at the glycine site, moderate potency at non-NMDA receptors (K(b) = 0.9-1.5 μM), and the highest (120-250-fold) selectivity in favor of glycine site antagonism over non-NMDA receptors. Tetrasubstituted QXs 17d,e were more than 100-fold weaker glycine site antagonists than the corresponding trisubstituted QXs with F being better tolerated than Cl as a substituent at the 8 position. Di- and monosubstituted QXs showed progressively weaker antagonism compared to trisubstituted analogues. For example, removal of the 5-nitro group of 17a results in a ~100-fold decrease in potency (10a,b,z), while removal of both halogens from 17a results in a ~3000-fold decrease in potency (10v). In terms of steady-state inhibition, most QX substitution patterns favor antagonism at NMDA/glycine sites over antagonism at non-NMDA receptors. Among the QXs tested, only 17i was slightly selective for non- NMDA receptors.
- Keana,Kher,Sui Xiong Cai,Dinsmore,Glenn,Guastella,Huang,Ilyin,Lu,Mouser,Woodward,Weber
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p. 4367 - 4379
(2007/10/02)
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- Heterocyclic Systems Containing Bridgehead Nitrogen Atom: Part LXII - Synthesis of Thiazolobenzimidazol-3(2H)-ones
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2,4-Dibromo-6-nitroaniline (Ia), on reduction with Raney nickel and hydrazine hydrate followed by treatment of the resulting diamine with carbon disulfide in situ gives 4,6-dibromo-2-mercaptobenzimidazole (IIa).Compound (IIa) on reaction with chloroacetic
- Sharma, B. R.,Pujari, H. K.
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p. 121 - 127
(2007/10/02)
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