- RECEPTOR INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND USE THEREOF
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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; 0139
(2021/01/28)
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- OPTICALLY ACTIVE CROSSLINKED CYCLIC SECONDARY AMINE DERIVATIVE
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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
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- OPTICALLY ACTIVE BRIDGED PIPERIDINE DERIVATIVE
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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
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- ARYL, HETEROARYL, AND HETEROCYCLIC 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 aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
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- 2-Azanorbornane-based amine organocatalyst for enantioselective aldol reaction of isatins with ketones
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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
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p. 1062 - 1068
(2016/10/11)
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- A short stereoselective synthesis of disubstituted cyclic amino acids
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A new synthetic route to enantiomerically pure disubstituted derivatives of cyclic amino acids is reported. Key step of this synthesis is an oxidative cleavage of azabicycloalkene precursors that are synthesized in enantiomerically pure form via aza-Diels
- Maison, Wolfgang,Adiwidjaja, Gunadi
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p. 5957 - 5960
(2007/10/03)
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- Bridged bicyclic vasopressin receptor antagonists with V2-selective or dual V1a/V2 activity
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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)
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- Asymmetric Synthesis of Pipecolic Acid Derivatives Using the Aza-Diels-Alder Reaction
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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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- Enantio- and Diastereo-selective Synthesis of Pipecolic Acid Derivatives using the Aza-Diels-Alder Reaction of Imines with Dienes
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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.
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p. 1337 - 1340
(2007/10/02)
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