- Benzo Annulenes as Antiviral Agents
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The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, dengue, influenza, and zika, usi
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- Rh2(II)-Catalyzed Ring Expansion of Cyclobutanol-Substituted Aryl Azides to Access Medium-Sized N-Heterocycles
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A new reactivity pattern of Rh2(II)-N-arylnitrenes was discovered that facilitates the synthesis of medium-sized N-heterocycles from ortho-cyclobutanol-substituted aryl azides. The key ring-expansion step of the catalytic cycle is both chemosel
- Mazumdar, Wrickban,Jana, Navendu,Thurman, Bryant T.,Wink, Donald J.,Driver, Tom G.
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p. 5031 - 5034
(2017/05/04)
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- CARBOXY X RHODAMINE ANALOGS
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The present invention provides novel fluorescent dyes and kits containing the same, which are useful for labeling a wide variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes f
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- The application of the schmidt reaction and beckmann rearrangement to the synthesis of bicyclic lactams: Some mechanistic considerations
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The syntheses of some methoxy-substituted bicyclic lactams, of the types 3 and 4, are reported employing two different conditions for the Schmidt reaction of appropriate ketones and employing two different conditions for the Beckmann rearrangement of the corresponding ketoximes. The alkyl to aryl migration ratios of the reactions were determined by high-performance liquid chromatography analysis of the reactions. The mechanisms of the reactions reported are discussed, some limitations of the reported mechanisms identified, and an alternative mechanism proposed in light of the outcomes of the various reactions. Application of the Schmidt reaction and Beckmann rearrangement was used for the synthesis of some chloro bicyclic lactams, of the types 3 and 4. CSIRO 2010.
- Crosby, Ian T.,Shin, James K.,Capuano, Ben
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p. 211 - 226
(2011/06/21)
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- FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND C-MET INHIBITORS
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The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
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Page/Page column 361
(2008/12/05)
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- TETRAHYDRO-PYRIDOAZEPIN-8-ONES AND RELATED COMPOUNDS FOR THE TREATMENT OF SCHIZOPHRENIA
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Compounds of formula 1 are disclosed, wherein G, D, A, Q, Y, Z, and R1 through R10 are defined in the specification. Also provided are descriptions of processes for preparing compounds of formula 1, intermediates used in making the same, and pharmaceutical compositions containing such compounds and their use in the treatment of central nervous system disorders and other disorders.
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- Substituted 1-benzazepines and derivatives thereof
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This invention relates to substituted 1-benzazepines and derivatives thereof useful as antibacterial agents, to compositions, including pharmaceutical compositions, comprising such compounds, to processes for making these compounds and to methods of using these compounds for killing bacteria or inhibiting bacterial growth.
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- Synthesis of paullones with aminoalkyl side chains
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Paullones 3 and 4 with aminoalkyl side chains in 2- or 3-position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1-inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be suitable tools for affinity studies directed to find additional intracellular paullone targets.
- Wieking, Karen,Knockaert, Marie,Leost, Maryse,Zaharevitz, Daniel W.,Meijer, Laurent,Kunick, Conrad
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p. 311 - 317
(2007/10/03)
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- Novel benzo-fused lactam scaffolds as factor Xa inhibitors
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Rigid benzolactam P3-P2 dipeptide mimics were designed and prepared as potential inhibitors of blood coagulation factor Xa. Methoxy substitution of the tetrahydrobenzazepinone scaffold led to potent and selective inhibitors. The synt
- Tamura, Susan Y.,Goldman, Erick A.,Bergum, Peter W.,Semple, J. Edward
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p. 2573 - 2578
(2007/10/03)
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- Azabenzocycloheptenones. Part 20. Synthesis and utilisation of 4-amino-1,2,3,4-tetrahydro-1(1H)-benzazepines
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1,2,3,4-Tetrahydro-6- and -7-methoxy-4-oxo-1-(p-tolylsulfonyl)quinolines 3 (R = tosyl, X = 6- and 7-OMe) and 1-ethoxycarbonylmethyl-1,2,3,4-tetrahydro-7-methoxy-4-oxoquinoline3 (R = CH2CO2Et, X = 7-OMe) have been ring-expanded in two
- Booker-Milburn, Kevin I.,Dunkin, Ian R.,Kelly, Frances C.,Khalaf, Abedawn I.,Learmonth, David A.,Proctor, George R.,Scopes, David I. C.
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p. 3261 - 3273
(2007/10/03)
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- Benzo-fused lactams that promote the release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
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- 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
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Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotensin converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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- 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
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Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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- ω-[2-(N-Lower alkyl-benzamido)-phenyl]-alkanoic acids, their use, and medicaments containing them
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The invention relates to ω-[2-(N-lower alkyl-benzamido)-phenyl]-alkanoic acids, their use and preparation, and medicaments containing them.
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