- As neuroprotective agents of pharmaceutical compounds
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The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
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Paragraph 0502; 0503; 0504; 0505
(2019/06/26)
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- Synthesis of Indole-Dihydroisoquinoline Sulfonyl Ureas via Three-Component Reactions
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Isoquinolines activated with sulfamoyl chlorides were reacted with indoles in a 3-component reaction to generate a library of dihydroisoquinoline derivatives. Using a differential protecting group strategy, products could be further derivatised. Synthesis of isoquinoline starting materials using several different methods is also described.
- Pearson, Stuart E.,Fillery, Shaun M.,Goldberg, Kristin,Demeritt, Julie E.,Eden, Jonathan,Finlayson, Jonathan,Patel, Anil
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p. 4963 - 4981
(2018/12/13)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Paragraph 0515; 0517-0518
(2017/07/05)
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- Chiral Triazoles in Anion-Binding Catalysis: New Entry to Enantioselective Reissert-Type Reactions
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Easily accessible and tunable chiral triazoles have been introduced as a novel class of C-H bond-based H-donors for anion-binding organocatalysis. They have proven to be effective catalysts for the dearomatization reaction of different N-heteroarenes. Although this dearomatization approach represents a powerful strategy to build chiral heterocycles, to date only a few catalytic methods to this end exist. In this work, the organocatalyzed enantioselective Reissert-type dearomatization of isoquinoline derivatives employing a number of structurally diverse chiral triazoles as anion-binding catalysts was realized. The here presented method was employed to synthesize a number of chiral 1,2-dihydroisoquinoline substrates with an enantioselectivity up to 86:14 e.r. Moreover, a thorough study of the determining parameters affecting the activity of this type of anion- binding catalysts was carried out.
- Zurro, Mercedes,Asmus, S?ren,Bamberger, Julia,Beckendorf, Stephan,García Manche?o, Olga
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supporting information
p. 3785 - 3793
(2016/03/08)
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- HCV NS5A replication complex inhibitors. Part 4.1 optimization for genotype 1a replicon inhibitory activity
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A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging f
- St. Laurent, Denis R.,Serrano-Wu, Michael H.,Belema, Makonen,Ding, Min,Fang, Hua,Gao, Min,Goodrich, Jason T.,Krause, Rudolph G.,Lemm, Julie A.,Liu, Mengping,Lopez, Omar D.,Nguyen, Van N.,Nower, Peter T.,O'Boyle, Donald R.,Pearce, Bradley C.,Romine, Jeffrey L.,Valera, Lourdes,Sun, Jin-Hua,Wang, Ying-Kai,Yang, Fukang,Yang, Xuejie,Meanwell, Nicholas A.,Snyder, Lawrence B.
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p. 1976 - 1994
(2014/04/03)
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- Facile synthesis of substituted isoquinolines
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A facile three-step protocol toward methoxy isoquinolines 7 starting with substituted 2-allylbenzaldehydes 9 was described. The overall synthetic process of skeleton 7 was carried out using the Grignard addition, PCC-oxidation, and one-pot oxidative cleavage of the olefinic group of skeleton 9 with OsO 4-NaIO4 followed by the condensation of the resulting 1,5-dicarbonyl compounds with NH4OAc. Skeleton 9 was prepared in high yield via the known Claisen rearrangement of skeleton 8 and O-methylation. Papaverine 2 is also synthesized via the simple three-step synthetic protocol.
- Chang, Meng-Yang,Wu, Ming-Hao,Lee, Nein-Chia,Lee, Ming-Fang
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p. 2125 - 2128
(2012/07/14)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 104
(2012/02/15)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds
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Page/Page column 255-256
(2012/04/10)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 192-193
(2011/06/16)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
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Page/Page column 105-106
(2011/06/16)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 100-101
(2011/07/07)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 167; 168
(2010/11/04)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 154-155
(2010/12/26)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 112-113
(2010/12/26)
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- Hepatitis C Virus Inhibitors
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 60
(2010/10/19)
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- Hepatitis C Virus Inhibitors
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 51-52
(2009/09/28)
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- Organocatalytic asymmetric destruction of 1-benzylated Reissert compounds catalysed by quaternary cinchona alkaloids
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The enantiomeric enrichment of racemic 1-benzylated Reissert compounds under organocatalytic biphasic conditions is presented. The enrichment is the consequence of an asymmetric destruction of the racemic compounds resulting in the formation of the corres
- Frisch, Kim,Jorgensen, Karl Anker
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p. 2966 - 2974
(2008/03/14)
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- Quinoline and quinazoline compounds useful in therapy, particularly in the treatment of benign prostatic hyperplasia
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Compounds of formula I, STR1whereinR 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms;R 2 represents H or C 1-6 alkoxy optionally substituted by one or more fluorine atoms;R 3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted;R 4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted;X represents CH or N; andL is absent,or represents a cyclic group of formula Ia, STR2or represents a chain of formula Ib, STR3and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
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- AMINOISOQUINOLINE DERIVATIVES
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Aminoisoquinoline derivatives represented by formulae (I and II), analogs thereof or pharmaceutically acceptable salts of the same. Because of having excellent inhibitory effects on activated blood coagulation factor X, these compounds are useful as active ingredients in anticoagulants or preventives/remedies for thrombosis or embolism.
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- Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors
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A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT1A affinity.
- Meagher, Kristin L,Mewshaw, Richard E,Evrard, Deborah A,Zhou, Ping,Smith, Deborah L,Scerni, Rosemary,Spangler, Taylor,Abulhawa, Susan,Shi, Xiaojie,Schechter, Lee E,Andree, Terrance H
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p. 1885 - 1888
(2007/10/03)
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- BICYCLIC NITROGEN HETEROCYCLIC ETHERS AND THIOETHERS, AND THEIR PHARMACEUTICAL USES
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A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H. sub.2-antagonist, anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.
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