Patent classifications
C07D233/30
SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure:
##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure:
##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Heather Sharron Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure: ##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Heather Sharron Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure: ##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
DISCRETE PEG CONSTRUCTS
Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEG.sub.x can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and hidden; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of -amino--carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Heather Sharron Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure:
##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Heather Sharron Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure:
##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
SMALL MOLECULE INHIBITORS OF PR3 AND HNE AND USES THEREOF
Disclosed herein are novel small molecules that can be used therapeutically to treat ailments and diseases associated with an over-active or undesired immune response. Specific embodiments include inhibitors of Proteinase 3 (PR3) and Human Neutrophil Elastase (HNE) and methods for their synthesis and use. The agents can be used to treat alpha-1 antitrypsin deficiency and other ailments related to neutrophil activity.
Inhibition of cell proliferation
The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC.sub.50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.