- INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
-
Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 00317-00319; 00432-00434
(2021/10/15)
-
- Practical Intermolecular Hydroarylation of Diverse Alkenes via Reductive Heck Coupling
-
The hydroarylation of alkenes is an attractive approach to construct carbon-carbon (C-C) bonds from abundant and structurally diverse starting materials. Herein we report a palladium-catalyzed reductive Heck hydroarylation of aliphatic and heteroatom-substituted terminal alkenes and select internal alkenes with an array of (hetero)aryl iodides. The reaction is anti-Markovnikov selective with terminal alkenes and tolerates a wide variety of functional groups on both the alkene and (hetero)aryl coupling partners. Additionally, applications of this method to complex molecule diversifications are demonstrated. Mechanistic experiments are consistent with a mechanism in which the key alkylpalladium(II) intermediate is intercepted with formate and undergoes a decarboxylation/C-H reductive elimination cascade to afford the saturated product and turn over the cycle.
- Gurak, John A.,Engle, Keary M.
-
p. 8987 - 8992
(2018/09/11)
-
- COMPOUNDS, COMPOSITIONS AND METHODS OF USE
-
Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
- -
-
Page/Page column 55; 56; 57
(2018/11/22)
-
- Intramolecular cyclization of 1-(ω-Phenylalkyl)-2-(nitromethylene) pyrrolidines in triflic acid
-
1-(ω-Phenylalkyl)-2-(nitromethylene)pyrrolidines in triflic acid undergo a C,O-diprotonation, followed by loss of water, to form conjugated iminium-hydroxynitrilium dications, which react with the tethered phenyl ring by electrophilic aromatic substitution to afford tricyclic iminium compounds as triflate salts. The scope and mechanism of this reaction are discussed. Copyright
- Fante, Bamba,Soro, Yaya,Siaka, Sorho,Marrot, Jerome,Coustard, Jean-Marie
-
supporting information
p. 2377 - 2385
(2014/07/22)
-
- BIVALENT AMPA RECEPTOR POSITIVE ALLOSTERIC MODULATORS
-
Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMP A receptors.
- -
-
Paragraph 076
(2013/09/12)
-
- Organocatalytic diimide reduction of enamides in water
-
Bridged flavinium organocatalysts have displayed efficacy in the diimide mediated reduction of enamides in aqueous conditions. This represents the first diimide reduction of an electron rich alkene and offers a clean alternative to the use of alkylating agents for N-alkylation.
- Marsh, Barrie J.,Heath, Emma L.,Carbery, David R.
-
supporting information; experimental part
p. 280 - 282
(2011/02/23)
-
- A template-based mnemonic for monoamine oxidase (MAO-N) catalyzed reactions and its application to the chemo-enzymatic deracemisation of the alkaloid (±)-crispine A
-
A template-based mnemonic has been developed for the enzyme monoamine oxidase from Aspergillus niger and has been used to successfully identify the alkaloid (±)-crispine A as a target for chemo-enzymatic deracemisation yielding the biologically active (R)
- Bailey, Kevin R.,Ellis, Andrew J.,Reiss, Renate,Snape, Timothy J.,Turner, Nicholas J.
-
p. 3640 - 3642
(2008/03/14)
-
- HYDROXAMIC ACID DERIVATIVES FOR USE WITH THE TREATMENT OF DISEASES RELATED TO CONNECTIVE TISSUE DEGRADATION
-
The present invention provides novel hydroxamic acid derivatives represented by the compound of formula I I or pharmaceutical acceptable salts thereof, wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, including collagenase, stromelysin, and gelatinase, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthrits, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.
- -
-
-
- HYDROXAMIC ACID DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES RELATED TO CONNECTIVE TISSUE DEGRADATION
-
The present invention provides novel hydroxamic acid derivatives represented by the compound of formula I STR1 or pharmaceutical acceptable salts thereof, wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, including collagenase, stromelysin, and gelatinase, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthrits, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.
- -
-
-
- α-Nitrogenated organolithium compounds from α-amidomethyl and α-aminomethyl sulfones
-
Successive reaction of α-amidomethyl sulfones 7a,b, derived from primary amides, with n-butyllithium and primary alkyl bromides (CH2 = CHCH2Br, CH2 = CMeCH2Br, CH2 = CBrCH2Br, CH ≡ CCH
- Alonso, Diego A.,Alonso, Emma,Najera, Carmen,Ramon, Diego J.,Yus, Miguel
-
p. 4835 - 4856
(2007/10/03)
-
- Synthesis of Pyrrolidines and Pyrrolidinones by the Rhodium Complex Catalyzed Cyclization of Unsaturated Amines
-
N-Allylic arylamines react with carbon monoxide, sodium borohydride, 2-propanol, and catalytic amounts of the zwitterionic complex η6-C6H6BPh3-Rh(COD)+ (1), to form pyrrolidines as the main products in most cases.Pyrrolidinones result from N-allylic alkylamines.An alternate route to the lactams from N-allylic alkylamines involves synthesis gas instead of CO/NaBH4, together with the dual catalytic system 1/2.Complementary to the N-allylic arylamine route to pyrrolidines with NaBH4 and 1 is the use of synthesis gas, 1, and 1,4-bis(diphenylphosphino)butane.
- Zhou, Jian-Qiang,Alper, Howard
-
p. 3328 - 3331
(2007/10/02)
-
- The Reduction of Tertiary N-Styrylenamides
-
Magnesium and methanol reduction of N,9-dibenzyl-8-azabicyclonon-1(6)-en-7-one (6) gave all four racemates of N,9-dibenzyl-8-azabicyclononan-7-one (1)-(4), with a 13:6 ratio of cis-fused to trans-fused products.Selective reduction of N,9-dibenzyl-8-azabicyclonon-1(6),3-dien-7-one (5) gave almost exclusively the two cis-fused racemates of N,9-dibenzyl-8-azabicyclonon-3-en-7-one (9) and (10).Magnesium and methanol did not reduce (E)-N-benzyl-9-benzylidene-cis-bicyclononan-7-one (7) and (E)-N-benzyl-N-(1-methyl-2-phenylvinyl)-acetamide (16a), but did reduce (E)-N-benzyl-N-styrylacetamide (16b) and (E)- and (Z)-N-styrylpyrrolidin-2-one (13) and (14); incomplete reduction of (Z)-N-benzyl-N-(1-methyl-2-phenylvinyl)-acetamide (15a) and (Z)-N-benzyl-N-styrylacetamide (15b) was observed.Reduction does not occur when the styryl phenyl group is twisted out of conjugation.Sodium and liquid ammonia reduction of (E)-N-benzyl-9-benzylidene-cis-8-azabicyclononan-7-one (7) gave (1RS,6SR,9RS)-9-benzyl-8-azabicyclononan-7-one and N-benzyl-2-(2-phenylethyl)cyclohexane-1-carboxamide (20).A similar cleavage of the β-styryl-nitrogen bond was observed in the reduction of (Z)-N-benzyl-N-(1-methyl-2-phenylvinyl)acetamide (15a), but not with (E)-N-styrylpyrrolidin-2-one (13).Several tertiary N-styrylenamides were not reduced by sodium cyanoborohydride in acetic acid but N-benzyl-9-benzylidene-cis-8-azabicyclonon-3-en-7-one (8) and N-benzyl-9-benzylidene-cis-8-azabicyclononan-7-one (7) gave (1RS,6SR,9RS)-N,9-dibenzyl-8-azabicyclonon-3-en-7-one (9) and (1RS,6SR,9RS)-N,9-dibenzyl-8-azabicyclononan-7-one (2) respectively.
- Ainscow, R. Barry,Brettle, Roger,Shibib, Sa'ad M.
-
p. 1781 - 1786
(2007/10/02)
-