- OPTICALLY ACTIVE CROSSLINKED CYCLIC SECONDARY AMINE DERIVATIVE
-
The present invention relates to the compound of formula (I) wherein p is 1 or 2, R1 is —CF3 or the like, R2a, R2b, R3a, and R3b are hydrogen atom or the like, X is —C(═O)—or the like, or a
- -
-
Paragraph 0277; 0285
(2021/01/29)
-
- OPTICALLY ACTIVE BRIDGED PIPERIDINE DERIVATIVE
-
The present invention relates to the compound of formula (1a) wherein a - d and p are 1 or 2, R1 - R4 are hydrogen atom or the like, and R18 is -CF3 or the like, or a pharmaceutically acceptable salt thereof, wh
- -
-
Paragraph 0190; 0192; 0198-0199
(2021/06/21)
-
- COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
-
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof 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.
- -
-
Paragraph 0526
(2017/03/14)
-
- AMIDE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
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 amide 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 are capable of reducing the excessive activation of complement.
- -
-
Paragraph 0631
(2017/03/14)
-
- ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
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 aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
- -
-
Paragraph 0718
(2017/03/14)
-
- ALKYNE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
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.
- -
-
Paragraph 0579
(2017/03/14)
-
- ETHER COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
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.
- -
-
Paragraph 0659
(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).
- -
-
Paragraph 0334; 0338; 0339; 0340; 0341; 0342
(2017/08/30)
-
- SUBSTITUTED OXETANES AND THEIR USE AS INHIBITORS OF CATHEPSIN C
-
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.
- -
-
Page/Page column 45; 46
(2016/03/04)
-
- NOVEL SUBSTITUTED SPIROCYCLES
-
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
- -
-
Paragraph 0222
(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
- -
-
Paragraph 0009; 0034-0039
(2020/02/08)
-
- SPIRO COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Paragraph 0650
(2015/11/09)
-
- 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.
- -
-
Page/Page column 198-199
(2014/09/29)
-
- 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.
- -
-
Page/Page column 73; 74
(2014/09/29)
-
- 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.
- -
-
Paragraph 0503; 0504
(2014/09/29)
-
- FUSED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
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.
- -
-
Paragraph 00338; 00340
(2014/06/23)
-
- SPIRO RING COMPOUND AS HEPATITIS C VIRUS (HCV) INHIBITOR AND USES THEREOF FIELD OF THE INVENTION
-
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.
- -
-
Page/Page column 194; 195; 196
(2014/06/23)
-
- SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
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.
- -
-
Page/Page column 62; 63
(2013/03/28)
-
- SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, E, F and L 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.
- -
-
Page/Page column 66-67
(2013/03/28)
-
- 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.
- -
-
Paragraph 0309; 0310
(2013/11/06)
-
- TETRACYCLIC HETEROCYCLE COMPOUNDS FOR TREATING HEPATITIS C VIRAL INFECTION
-
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.
- -
-
Page/Page column 70-71
(2012/04/17)
-
- TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
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.
- -
-
Page/Page column 77-78
(2012/04/17)
-
- FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
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.
- -
-
Page/Page column 77
(2012/05/04)
-
- 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.
- -
-
-
- 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.
- -
-
Page/Page column 88-89
(2012/04/17)
-
- HEPATITIS C INHIBITOR COMPOUNDS
-
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.
- -
-
Page/Page column 28; 29
(2011/08/21)
-
- Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid
-
Prolonged hepatitis C infection is the leading cause for cirrhosis of the liver and hepatocellular carcinoma. The etiological agent HCV virus codes a single polyprotein of ~3000 amino acids that is processed with the help of a serine protease NS3A to prod
- Venkatraman, Srikanth,Njoroge, F. George,Wu, Wanli,Girijavallabhan, Viyyoor,Prongay, Andrew J.,Butkiewicz, Nancy,Pichardo, John
-
p. 1628 - 1632
(2007/10/03)
-
- 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)
-
- AZABICYCLO COMPOUND, MATRIX METALLOPROTEASE INHIBITOR, AND SKIN PREPARATION
-
An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H,
- -
-
-
- Synthesis and evaluation of chiral bicyclic proline FKBP12 ligands
-
As part of our ongoing program to explore novel structural classes of FKBP12 ligands, we herein wish to report a new class of FKBP12 ligands containing chiral bicyclic proline analogues. Details of the synthetic routes, together with preliminary biologica
- Limburg, David C.,Thomas IV, Bert E.,Li, Jia-He,Fuller, Mike,Spicer, Dawn,Chen, Yi,Guo, Hongzhi,Steiner, Joseph P.,Hamilton, Gregory S.,Wu, Yong-Qian
-
p. 3867 - 3870
(2007/10/03)
-
- An improved synthesis of enantiopure 2-azabicyclo[2.2.1]heptane-3-carboxylic acid
-
A facile multigram scale preparation of (1R,3S,4S)-2-azabicyclo[2.2.1]heptane-3-carboxylic acid via stereoselective synthesis of the corresponding α-amino ester hydrochloride is detailed. Hitherto applied protocols for the synthesis of this cyclic proline
- Tararov, Vitali I.,Kadyrov, Renat,Kadyrova, Zenfira,Dubrovina, Natalia,Boerner, Armin
-
-
- 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.
-
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.
-
p. 1263 - 1282
(2007/10/02)
-
- Asymmetric Synthesis of Bicyclic Amino Acid Derivatives by Aza-Diels-Alder Reactions in Aqueous Solution
-
Derivatives 7-10 and 13-16 of methyl and ethyl 2-azabicycloheptane-3-carboxylates are synthesized by Aza-Diels-Alder reactions of chiral iminium ions, formed in situ from glyoxylic acid and chiral amines, with cyclopentadiene.Whereas the heterodienophiles derived from phenylglycinol and esters of sterically more demanding amino acids fail to undergo asymmetric cycloadditions, with alanine methyl ester and (R)-1-phenylethylamine hydrochloride the cycloadducts are formed in yields of 15 and 52percent, respectively, reaching the values of up to 90:10 for the exo isomer. Key Words: Asymmetric synthesis / Aza-Diels-Alder reaction / Amino acids, bicyclic
- Waldmann, Herbert,Braun, Matthias
-
p. 1045 - 1048
(2007/10/02)
-