- Novel domino synthesis of 2-(2,3.4-substituted phenyl) quinazolin-4-amine
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Convenient domino protocol was developed for the synthesis of 2-arylquinazolin-4-amines by the reaction of N-(2-cyanophenyl) substituted benzimidoyl isothiocyanates with isopropyl amine. The major advantages of this protocol are short reaction times, mild conditions, simple work up, high yields, and pure products. The efficacy of this protocol owes to the competence of synthesis, pure isolation of imidoyl isothiocyanates, and the unique structure conformation of the corresponding intermediate thiourea derivatives.
- Ali, Ibrahim A. I.,El Rayes, Samir M.,Fathalla, Walid,Khalifa, Mohamed E.,Pazdera, Pavel
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- VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides
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Herein, we report the structure-activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9-5.8 and Kp,uu 0.4-1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 (11a) emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.
- Reed, Carson W.,McGowan, Kevin M.,Spearing, Paul K.,Stansley, Branden J.,Roenfanz, Hanna F.,Engers, Darren W.,Rodriguez, Alice L.,Engelberg, Eileen M.,Luscombe, Vincent B.,Loch, Matthew T.,Remke, Daniel H.,Rook, Jerri M.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
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supporting information
p. 1326 - 1330
(2017/12/26)
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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 0690; 0706
(2015/03/13)
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- SOLID FORMS OF (4-ISOPROPOXY-3-METHOXYPHENYL)(2'-METHYL-6'-(TRIFLUOROMETHYL)-3',4'-DIHYDRO-2'H-SPIRO[PIPERIDINE-4,1'-PYRROLO[1,2-A]PYRAZINE]-1-YL)METHANONE
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The invention relates to solid state forms, for example, crystalline forms, of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3,,4'- dihydro-2'H-spiro[piperidine-4, 1 '-pyrrolo[ 1,2-a]pyrazine]- 1 -yl)methanone (Compound 1) or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods therewith. The present invention also relates to a method of preparing Compound 1 in various solid forms. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders such as pain.
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Paragraph 00188-00190
(2014/02/16)
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- PYRAN-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition
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- PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Paragraph 0350; 0351; 0352
(2013/03/26)
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- Synthesis and topoisomerase i inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D
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A novel 5-oxa-6a,8-diazaindeno[2,1-b]phenanthren-7-one scaffold was designed and synthesized as an active analogue of the cytotoxic marine alkaloid Lamellarin D. The design was based on molecular modeling of the site of interaction of Lamellarin D with DNA-topoisomerase I cleavable complex, whereas the synthesis capitalized on a simple Friedel-Crafts cyclization of indole to a β-carbolinone nucleus. The product exhibited topoisomerase I poisoning activity and submicromolar cytotoxicity on human non-small cell lung cancer H460 cell line.
- Cananzi, Salvatore,Merlini, Lucio,Artali, Roberto,Beretta, Giovanni Luca,Zaffaroni, Nadia,Dallavalle, Sabrina
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p. 4971 - 4984
(2011/10/05)
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- (3,4-DISUBSTITUTED)PROPANOIC CARBOXYLATES AS S1P (EDG) RECEPTOR AGONISTS
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The present invention encompasses compounds of Formula A: A as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
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Page/Page column 47-48
(2008/06/13)
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