Patent classifications
C07D207/273
SYNTHETIC PROCESSES FOR THE PRODUCTION OF 1-((3S,4R)-4-(2,6-DIFLUORO-4-METHOXYPHENYL)-2-OXOPYRROLIDIN-3-YL)-3-PHENYLUREA
Highly efficient processes are provided for preparing key intermediates in the synthesis of compounds (I). The process are broadly applicable and can provide selected components having a variety of substituents. Some intermediates are claimed.
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SYNTHETIC PROCESSES FOR THE PRODUCTION OF 1-((3S,4R)-4-(2,6-DIFLUORO-4-METHOXYPHENYL)-2-OXOPYRROLIDIN-3-YL)-3-PHENYLUREA
Highly efficient processes are provided for preparing key intermediates in the synthesis of compounds (I). The process are broadly applicable and can provide selected components having a variety of substituents. Some intermediates are claimed.
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NITROXIDE CONTAINING AMYLOID BINDING AGENTS FOR IMAGING AND THERAPEUTIC USES
The present invention provides methods of using nitroxide spin-labeled amyloid beta-binding compounds to image amyloid. The present invention also provides nitroxide spin-labeled amyloid beta-binding compounds.
NITROXIDE CONTAINING AMYLOID BINDING AGENTS FOR IMAGING AND THERAPEUTIC USES
The present invention provides methods of using nitroxide spin-labeled amyloid beta-binding compounds to image amyloid. The present invention also provides nitroxide spin-labeled amyloid beta-binding compounds.
Substituted cyclohexyl compounds as NOP inhibiiors
Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders. ##STR00001##
Substituted cyclohexyl compounds as NOP inhibiiors
Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders. ##STR00001##
PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE
- Burcu Selin Aytar ,
- Alina Borovika ,
- Collin Chan ,
- Joerg Deerberg ,
- Nathan R. Domagalski ,
- Martin D. Eastgate ,
- Yu Fan ,
- Michael David Bengt Fenster ,
- Robert V. Forest ,
- Francisco Gonzalez-Bobes ,
- Rebecca A. Green ,
- Matthew R. Hickey ,
- Nathaniel David Kopp ,
- Thomas E. La Cruz ,
- Kathleen Lauser ,
- Hong Geun Lee ,
- David K. Leahy ,
- Helen Y. Luo ,
- Thomas M. Razler ,
- Scott A. Savage ,
- Chris Sfouggatakis ,
- Maxime C.D. Soumeillant ,
- Serge Zaretsky ,
- Bin Zheng ,
- Ye Zhu
The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide,
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INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
ALKYNE COMPOUNDS AS IRAK INHIBITORS, PREPARATION METHODS AND MEDICINAL USES THEREOF
This application discloses alkyne compounds of formula (I) useful as IRAK inhibitors and therapeutic agents for treatment of IRAK, especially IRAK-4, mediated disease or disorders, including autoimmune diseases, cancers, neurodegenerative disorders, viral diseases, and inflammatory disorders, hereditary disorders, and so on. The application also discloses pharmaceutical compositions containing these compounds, and synthetic methods and medical uses of the compounds.
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