- CYCLEN BASED COMPOUNDS, COORDINATION COMPOUNDS, PEPTIDES, PHARMACEUTICAL PREPARATION, AND USE THEREOF
-
The present invention relates to cyclen based compounds of general formula (I), wherein X is nitrogen and Y, Z are –CH-, or X, Z are –CH- and Y is nitrogen, or X, Y are –CH- and Z is nitrogen; R1 is independently selected from H; COOH; benzylox
- -
-
Page/Page column 9-10
(2021/01/23)
-
- 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 0551
(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 0824
(2017/03/14)
-
- PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
-
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
-
- COMPLEMENT PATHWAY MODULATORS AND USES THEREOF
-
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
-
- PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
-
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
-
- COMPLEMENT PATHWAY MODULATORS AND USES THEREOF
-
The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
-
- PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
-
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
-
- Novel Inhibitors of the Amino Acid Transporters ASCT1 and ASCT2
-
The invention features compounds and methods relating to novel hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention can be used in research or clinical applications (e.g., for the treatment of cancer, microbial infection, or ischemia-related central nervous system injury).
- -
-
-
- Synthesis of (2S, 3R, 4S), (2S, 3S, 4R)-epoxyprolines and aminohydroxyprolines
-
25, 3R, 4S- and 25, 38, 4R-epoxy-L-prolines were synthesised from trans- 4-hydroxy-L-proline. Assignment of the stereochemical configurations of the epoxy prolines was achieved by n.O.e. studies and chemical correlation. The synthetic utility of the protected epoxides was investigated briefly by ring opening with NAN3, followed by deprotection to give aminohydroxy prolines.
- Robinson, J. Kenneth,Lee, Victor,Claridge, Timothy D. W.,Baldwin, Jack E.,Schofield, Christopher J.
-
p. 981 - 996
(2007/10/03)
-
- Substrate specificity of proline 4-hydroxylase: Chemical and enzymatic synthesis of 2S,3R,4S-epoxyproline
-
The substrate specificity of L-proline 4-hydroxylase, a 2-oxoglutarate dependent dioxygenase from Streptomyces griseoviridus P8648, was investigated. Preliminary assays measuring turnover of 2-oxyglutarate indicated 3,4-dehydro-L-proline was an efficient
- Baldwin,Field,Lawrence,Lee,Robinson,Schofield
-
p. 4649 - 4652
(2007/10/02)
-