Patent classifications
C07C229/42
COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION
The disclosures herein provide compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These compounds may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, intravenous, spray, parenteral, lozenge, solution, syrup, sachet, transdermal administration, or injection. Such compositions may be used to treatment of inflammation or its associated complications.
IDO INHIBITORS
- James Aaron Balog ,
- Emily Charlotte Cherney ,
- Weiwei Guo ,
- Audris Huang ,
- Jay A. Markwalder ,
- Steven P. Seitz ,
- Weifang Shan ,
- David K. Williams ,
- Natesan Murugesan ,
- Susheel Jethanand Nara ,
- Saumya Roy ,
- Soodamani Thangavel ,
- Ramesh Kumar Sistla ,
- Srinivas Cheruku ,
- Srinivasan Thangathirupathy ,
- Yadagiri Kanyaboina ,
- Nagalakshmi Pulicharla
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
ADDITION-FRAGMENTATION AGENT WITH PENDENT AMINE GROUPS
Provided is an addition-fragmentation agent of the formula (I) where R.sup.amine comprises a tertiary amine group; R.sup.2 linking group of valence a+2; Z is an ethylenically unsaturated polymerizable group; and subscript a is 0 or 1.
##STR00001##
ADDITION-FRAGMENTATION AGENT WITH PENDENT AMINE GROUPS
Provided is an addition-fragmentation agent of the formula (I) where R.sup.amine comprises a tertiary amine group; R.sup.2 linking group of valence a+2; Z is an ethylenically unsaturated polymerizable group; and subscript a is 0 or 1.
##STR00001##
Synthesis of 4-chlorokynurenines and intermediates
The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
Synthesis of 4-chlorokynurenines and intermediates
The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
Synthesis of 4-chlorokynurenines and intermediates
The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
Prodrugs of non-steroid anti-inflammatory agents (NSAIDS)
The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.
Prodrugs of non-steroid anti-inflammatory agents (NSAIDS)
The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.
PROCESS OF MAKING 3-(4'-AMINOPHENYL)-2-METHOXYPROPIONIC ACID, AND ANALOGS AND INTERMEDIATES THEREOF
The disclosure provides a process for the preparation of 3-(4′-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.