- NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
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Described herein are new, selective modulators of the 5 -HT7 receptor. These selective compounds can be useful for the treatment of CNS and non-CNS indications. Compounds described herein can be selective in targeting 5-HT7 receptors
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Paragraph 000725-000726
(2021/05/21)
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- Synthesis of optically active (R)- And (S)-β-arginine from pyroglutamic acid
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– The first synthesis of optically active β-arginine was achieved starting from commercially available pyroglutamic acid. The new synthetic protocol is characterized by the use of nitrile as a carboxylic acid surrogate which could be transformed to the co
- Yasuno, Yoko,Sawai, Akira,Sekihara, Ai,Shinada, Tetsuro
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p. 165 - 176
(2020/02/04)
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- NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
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Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5- hydroxytryptamine receptor 7 activity. A is selected
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Paragraph 01132; 01133
(2019/11/28)
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- BETA-LACTAMASE INHIBITOR COMPOUNDS
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The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts are useful in combination with beta- lactam antibiotics, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3, R4, R5 and R6 are described herein.
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Page/Page column 167; 168
(2018/04/13)
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- Total synthesis of (-)-martinellic acid
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An enantioselective formal total synthesis of the pyrrolo[3,2-c]quinoline natural product martinellic acid has been achieved. The key steps involve a Pd-catalyzed aryl amidation reaction of a pyrroglutamate derivative, an intramolecular [3+2] azomethine ylide-alkene cycloaddition and a reductive ring opening reaction.
- Badarinarayana, Vivek,Lovely, Carl J.
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p. 2607 - 2610
(2007/10/03)
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- Total synthesis of (+)-batzelladine A and (-)-batzelladine D via [4 + 2]-annulation of vinyl carbodiimides with N-alkyl imines
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A diastereoselective [4 + 2]-annulation of vinyl carbodiimides with chiral N-alkyl imines has been developed to access the stereochemically rich polycyclic guanidine cores of the batzelladine alkaloids. Application of this strategy, together with additional key steps such as long-range directed hydrogenation and diastereoselective intramolecular iodo-amination, led to highly convergent total syntheses of (-)-batzelladine D and (+)-batzelladine A with excellent stereocontrol.
- Arnold, Michael A.,Day, Kenneth A.,Duron, Sergio G.,Gin, David Y.
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p. 13255 - 13260
(2008/03/11)
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- The synthesis of di(hydroxyalkyl) substituted bicyclic guanidines
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The synthesis of the enantiomerically pure bicyclic guanidines 3a and 3b is described.The convergent strategy is based on methodology developed by Schmidtchen.The therefore required amine components 6 and 9 obtained from methionine and L-glutamic acid, respectively.
- Madder, A.,Muenster, I.,Rolle, U.,Clercq, P. J. De
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p. 613 - 622
(2007/10/03)
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- Synthesis of a Chiral Di(hydroxyalkyl) Substituted Bicyclic Guanidine
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Schmidtchen's methodology is used successfully for the synthesis of the chiral disubstituted bicyclic guanidinium salt 2.The two therefore required primary amine compounds 6 and 9 are obtained from L-methionine and L-glutamic acid, respectively.
- Muenster, Ingo,Rolle, Ulrike,Madder, Annemieke,Clerq, Pierre J. De
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p. 2673 - 2674
(2007/10/03)
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- Process for preparing 5-vinyl-2-pyrrolidinone and intermediates therefor
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4-Amino-5-hexenoic acid is prepared by: (a) reacting 5-oxo-2-pyrrolidine-acetonitrile with hydrogen and dimethylamine in the presence of a palladium catalyst to form N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine; (b) oxidizing N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]-ethylamine to produce the corresponding N-oxide derivative; (c) pyrolysis of the N-oxide derivative to form 5-vinyl-2-pyrrolidinone; (d) optionally, separating N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine by-product from the 5-vinyl-2-pyrrolidinone product; and (e) hydrolyzing 5-vinyl-2-pyrrolidinone to form 4-amino-5-hexenoic acid.
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