- PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS
-
This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl -mediated disorders.
- -
-
Page/Page column 365-366
(2020/10/18)
-
- 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 0499
(2017/03/14)
-
- PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV
-
A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(-)- ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(-)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(-)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis- (1R,2S)-(-)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(-)-ephedrine from the precipitated salt obtained in step (b).
- -
-
Page/Page column 21-22
(2011/10/10)
-
- PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV
-
The present invention relates to synthesis procedures and intermediates of a compound offormula: (XVII) and the salts thereof.
- -
-
Page/Page column 24
(2008/12/07)
-
- Novel antifungal β-amino acids: Synthesis and activity against Candida albicans
-
A series of novel β-amino acids has been synthesized and tested for their in vitro antifungal activity against Candida albicans. A steep SAR was observed. β-Amino acid 21 (BAY 10-8888/PLD-118) revealed the most favourable activity-tolerability profile and was selected for clinical studies as a novel antifungal for the oral treatment of yeast infections.
- Mittendorf, Joachim,Kunisch, Franz,Matzke, Michael,Militzer, Hans-Christian,Schmidt, Axel,Schoenfeld, Wolfgang
-
p. 433 - 436
(2007/10/03)
-
- Efficient asymmetric synthesis of β-amino acid BAY 10-8888/PLD-118, a novel antifungal for the treatment of yeast infections
-
The β-amino acid BAY 10-8888/PLD-118 is currently being investigated in phase II clinical studies as a novel antifungal for the treatment of yeast infections. An efficient asymmetric synthesis of this compound is described. The key step employed a highly enantioselective, quinine-mediated alcoholysis of a mesoanhydride intermediate.
- Mittendorf, Joachim,Benet-Buchholz, Jordi,Fey, Peter,Mohrs, Klaus-Helmut
-
p. 136 - 140
(2007/10/03)
-
- The Synthesis of Novel Trans-Oxabicyclo[3,3,0]octane Systems as Potential Inhibitors of HIV Protease
-
The novel trans-3-oxabicyclo[3,3.0]octan-7-one system has been prepared by intramolecular ring closure of the corresponding cyclopentane diol. Peralkylation and benzylidene substitution of the octanone has allowed the preparation of tetra-alkylated potential inhibitors of HIV protease. Weak activity against HIV protease (IC50's 70-100μM) was observed.
- Mahler, Mikael E.,Palmer, Michael J.
-
p. 193 - 194
(2007/10/03)
-