- Facile Synthesis of Annelated NADH Model Precursors
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A convenient route to γ-cyano fused pyridine derivatives, which are precursors of NADH models, is described.The method involves the reaction of 3,3-dimethoxy-2-formyl-propionitrile sodium salt (1) with amino derivatives of electron donating heterocyles le
- Benoit, R.,Dupas, G.,Bourguignon, J.,Queguiner, G.
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- PREPARATION AND APPLICATION OF AROMATIC COMPOUND HAVING IMMUNOREGULATORY FUNCTION
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Provided are an aromatic compound having immunoregulatory effect, a preparation method thereof, and a use of the same in regulating immune responses or inhibiting PD-1/PD-L1.
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Paragraph 0073-0075
(2021/06/10)
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- BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
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Paragraph 0802
(2015/02/19)
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- AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
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Page/Page column
(2014/05/07)
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- FUSED MULTI-CYCLIC SULFONE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
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Paragraph 0638
(2014/08/07)
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- SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ?-SECRETASE-INHIBITING ACTIVITY
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The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example,. a compound represented by the formula (I): wherein ruing A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
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Page/Page column 78
(2011/04/25)
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- Synthesis and in vitro opioid receptor functional antagonism of analogues of the selective kappa opioid receptor antagonist (3R)-7-hydroxy-N-((1S)-1- {[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl) -1,2,3,4-tetrahydro-3-is
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In previous structure-activity relationship (SAR) studies, we identified (3R)-7-hydroxy-N-((1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1- piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3- isoquinolinecarboxamide (JDTic, 1) as the first poten
- Cai, Tingwei Bill,Zou, Zhou,Thomas, James B.,Brieaddy, Larry,Navarro, Hernán A.,Carroll, F. Ivy
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p. 1849 - 1860
(2008/09/21)
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- PROCESS FOR PRODUCING 4-AMINO-2-ALKYLTHIO-5-PYRIMIDINECARBALDEHYDE
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An industrially advantageous process for 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde production by which a 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde can be easily produced in a high yield; an intermediate compound for use in the process; and an industrially advantageous production process by which the intermediate compound can be easily and safely produced in a high yield. A process for producing an alkali metal salt of a 3,3-dialkoxy-2-hydroxymethylenepropanenitrile is provided which is characterized by reacting at least one nitrile compound selected from the group consisting of 3,3-dialkoxypropanenitriles and 3-alkoxy-2-propenenitriles with a formic ester at -10 to 30°C in the presence of a base containing an alkali metal. Also provided are: an alkali metal salt of 4-amino-2-mercapto-5-pyrimidinecarbaldehyde; a process for producing the alkali metal salt of 4-amino-2-mercapto-5-pyrimidinecarbaldehyde which is characterized by reacting the 3,3-dialkoxy-2-hydroxymethylenepropanenitrile alkali metal salt with thiourea; a process for producing a 4-amino-2-alkylthio-5-pyrmidinecarbaldehyde which is characterized by reacting the 4-amino-2-mercapto-5-pyrmidinecarbaldehyde alkali metal salt with an alkylating agent; and a use of the 4-amino-2-mercapto-5-pyrimidinecarbaldehyde alkali metal salt in producing the 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde.
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Page/Page column 15
(2008/06/13)
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