- RECEPTOR INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND USE THEREOF
-
The present invention discloses a receptor inhibitor of formula (I), a pharmaceutical composition comprising the same and the use thereof.
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Paragraph 0137-0138
(2021/01/28)
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- As hepatitis c inhibitor spiro compound and its use in medicine
-
The invention provides a spiro compound serving as a hepatitis c inhibitor and application thereof in a medicine. The compound is a compound as shown in a formula (I) or a stereisomer, a geometric isomer, a tautomer, nitric oxide, an aquo-complex, a solvate, a metabolite, pharmaceutically acceptable salt or prodrug of the compound as shown in the formula (I). The invention also provides a pharmaceutical composition containing the compound, application of the compound and the pharmaceutical composition in inhibition of HCV (Hepatitis C Virus) copy and HCV virus protein, as well as the application of the compound and the pharmaceutical composition in prevention, handling, treatment or relieving of HCV infection or hepatitis c disease for a patient. The formula I is as shown in the specification.
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Paragraph 1467-1469
(2017/12/28)
-
- ALKYNE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is alkyne substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein can reduce the excessive activation of complement.
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Paragraph 0578
(2017/03/14)
-
- ETHER COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
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Paragraph 0658
(2017/03/14)
-
- Substituted piperidine amide derivative, preparation method thereof, and application of derivative to pharmacy
-
The invention relates to a substituted piperidine amide derivative as shown in a general formula (I) or a stereisomer and pharmaceutically acceptable salt thereof, a preparation method of the derivative, medicinal combination as well as application of the derivative to the aspects of local anaesthesia or analgesia. The definition of each group of the general formula (I) is consistent with that of the description. (The general formula (I) is as shown in the description).
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Paragraph 0334; 0335; 0336; 0337
(2017/08/30)
-
- SUBSTITUTED OXETANES AND THEIR USE AS INHIBITORS OF CATHEPSIN C
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This invention relates to a compound of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
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Page/Page column 45
(2016/03/04)
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- NOVEL SUBSTITUTED SPIROCYCLES
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This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agen
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Paragraph 0221
(2016/04/09)
-
- 2-Azanorbornane-based amine organocatalyst for enantioselective aldol reaction of isatins with ketones
-
Optically active 2-azanorbornane-based organocatalysts were designed and synthesized, and the catalytic activity of these catalysts in enantioselective aldol reactions of isatins with ketones was investigated. Among these catalysts, 2-azanorbornylmethanol
- Ogasawara, Ayumi,Subba Reddy,Seki, Chigusa,Okuyama, Yuko,Uwai, Koji,Tokiwa, Michio,Takeshita, Mitsuhiro,Nakano, Hiroto
-
p. 1062 - 1068
(2016/10/11)
-
- Intermediate reddy handkerchief Wei method of preparation
-
The invention relates to a method for preparing (1R,3S,4S)-N-tert-butyloxycarbonyl-2-azabicyclo[2,2,1]heptane-3-carboxylic acid (formula V), wherein the formula V is defined in the instruction. The method comprises: dissolving glyoxylate in a solvent, coo
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Paragraph 0009; 0034-0039
(2020/02/08)
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- SPIRO COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
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Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
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Paragraph 0649
(2015/11/09)
-
- Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
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Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
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Paragraph 0679; 0680; 0681
(2015/03/28)
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- FUSED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X', Y, Y', A, A',Q1, Q2, R1-R4, X4, R5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof.
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Paragraph 00338; 00339
(2014/06/23)
-
- SPIRO RING COMPOUND AS HEPATITIS C VIRUS (HCV) INHIBITOR AND USES THEREOF FIELD OF THE INVENTION
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A compound of formula (I) or a stereoisomer, a geometric isomer. a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof is provided, which can be used for treating HCV infection or a HCV disorder. Also a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof are provided, which can also be used for treating HCV infection or a HCV disorder.
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Page/Page column 194; 195
(2014/06/23)
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- BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided herein is a compound of formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof, which can also be used for treating HCV infection or a HCV disorder.
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Page/Page column 168
(2014/09/16)
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- BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS AND PHARMACEUTICAL APPLICATIONS THEREOF
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Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
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Paragraph 00327
(2014/02/16)
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- SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C
-
This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)- amides of formula (1) and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
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Page/Page column 198-199
(2014/09/29)
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- SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C
-
This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula (1) and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
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Page/Page column 73
(2014/09/29)
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- HEPATITIS C VIRUS INHIBITORS
-
The invention provides compounds of formulas (I) or (II): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
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Paragraph 0309; 0310
(2013/11/06)
-
- SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, D and R2 are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
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Page/Page column 61; 62
(2013/03/28)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS FOR TREATING HEPATITIS C VIRAL INFECTION
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Tetracyclic heterocycle compounds of formula (I) and pharmaceutically acceptable salts thereof are provided, wherein A, A', G, R1, R15, U, V, V', W, W, X, X', Y and Y' are as defined in the invention. The pharmaceutical compositions comprising these compounds and the use of the compounds for treating hepatitis C virus (HCV) infection are also provided.
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Page/Page column 70-71
(2012/04/17)
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- TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Tetracyclic Indole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprisingat least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 77
(2012/04/17)
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- FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', B, G, R1, U, V, W, W', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 77
(2012/05/04)
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- FUSED TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
-
The present invention discloses novel Fused Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', W, W', X, X', Y and Y' are as defined herein. The present invention also discloses compositions comprising at least one Fused Tetracyclic Heterocycle Compound, and methods of using the Fused Tetracyclic Heterocycle Compounds for treating or preventing HCV infection in a patient.
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-
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- TETRACYCLIC INDOLE DERIVATIVES FOR TREATING HEPATITIS C VIRUS INFECTION
-
Tetracyclic indole derivatives of formula (I), pharmaceutically acceptable salts and the pharmaceutical compositions thereof are provided, wherein A, A', G, R1, R15, U, V, V, W, W, X, X', Y, Y' are as defined in the invention. Use of these derivatives for treating hepatitis C virus (HCV) infection is also provided.
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Page/Page column 88-89
(2012/04/17)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of Formula (I): wherein R1, R2, RA, RB, Z1, Z2, Z3, Z4, Z5 and Z6 are defined herein. The compounds are useful as inhibitors of the function of NS5A protein encoded by HCV for the treatment of hepatitis C viral infection.
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Page/Page column 28
(2011/08/21)
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- FUSED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 99
(2011/08/04)
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- Aza-Diels - Alder reaction of methyl 2-[(R)-1-phenylethyl]iminoethanoate with cyclopentadiene using practical and environmentally friendly biphasic solvent system
-
Aza-Diels - Alder reaction between 2-[(R)-1-phenylethyl]imino-ethanoate (1) and cyclopentadiene using the biphasic solvent system (TMSCl-CH 3OH/toluene) gave (1S,3S,4R)-2-[(R)-1-phenylethyl]-2-aza-bicyclo[2.2. 1]hept-5-ene-3-carboxylates (3a) i
- Hashimoto, Norio,Yasuda, Hironobu,Hayashi, Masaru,Tanabe, Yoo
-
p. 105 - 109
(2012/12/24)
-
- Bridged bicyclic vasopressin receptor antagonists with V2-selective or dual V1a/V2 activity
-
The synthesis and biological testing of a novel series of nonpeptide vasopressin receptor antagonists, containing a bridged bicyclic nucleus, are reported. Variation of substituents (R1-R3) in general formula 3, and the configuration
- Dyatkin, Alexey B.,Hoekstra, William J.,Hlasta, Dennis J.,Andrade-Gordon, Patricia,De Garavilla, Lawrence,Demarest, Keith T.,Gunnet, Joseph W.,Hageman, William,Look, Richard,Maryanoff, Bruce E.
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p. 3081 - 3084
(2007/10/03)
-
- Enantio- and Diastereo-selective Synthesis of Pipecolic Acid Derivatives using the Aza-Diels-Alder Reaction of Imines with Dienes
-
Optically active pipecolic acid derivatives can be prepared by the aza-Diels-Alder reaction of simple dienes with the imine derived from ethyl glyoxylate and chiral 1-phenylethylamine; the cycloadditions are regiospecific, highly diastereoselective within the heterocyclic ring (>92percent exo with cyclic dienes, and 100percent endo with acyclic dienes), and lead to high asymmetric induction in most cases (average d.e. = 72percent).
- Bailey, Patrick D.,Wilson, Robert D.,Brown, George R.
-
p. 1337 - 1340
(2007/10/02)
-
- Asymmetric Synthesis of Pipecolic Acid Derivatives Using the Aza-Diels-Alder Reaction
-
Imines of the type R-N=CHCO2Et can be coerced into undergoing a (4+2) cycloaddition with substituted dienes if the reaction is carried out in DMF in the presence of both water and acid; these reactions show extremely high regio- and diastereoselectivity.U
- Bailey, Patrick D.,Brown, George R.,Korber, Fritjof,Reed, Amanda,Wilson, Robert D.
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p. 1263 - 1282
(2007/10/02)
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