Patent classifications
C07D407/14
4-CARBOXAMIDO-ISOINDOLINONE DERIVATIVES AS SELECTIVE PARP-1 INHIBITORS
There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
NEW PYRAZOLE DERIVATIVES AS NIK INHIBITORS
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
HETEROCYCLIC PAD4 INHIBITORS
- Kumaravel Selvakumar ,
- Venkatram Paidi ,
- Srinivasan Thangathirupathy ,
- Vijaya Kumar Cm ,
- Tirupathi Rao Alajangi ,
- Mallikarjun Reddy Sura ,
- Krishna Mahadevu ,
- Ramesh Kumar Sistla ,
- Piyush Agarwal ,
- Arul Mozhi Subbiah Karuppiah ,
- Jalathi S. Nair ,
- Ooha Morampudi ,
- Manoranjan Panda ,
- Joseph A. Tino ,
- Robert J. Cherney ,
- John V. Duncia ,
- Daniel S. Gardner ,
- T. G. Murali Dhar ,
- Audrey Graham Ross ,
- Paul E. Gormisky ,
- Xiao Zhu ,
- Boris M. Seletsky ,
- Alyssa H. Antropow ,
- Deqiang Niu ,
- Zhengdong Zhu ,
- Guobin Miao ,
- Julio Herman Cuervo
The disclosure generally relates to substituted heterocyclic compounds of Formula (Ia), which are inhibitors of PAD4, method for preparing these compounds, pharmaceutical compositions comprising these compounds and use of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.
##STR00001## ##STR00002##
Isoindolinone inhibitors of the MDM2-P53 interaction having anticancer activity
- Gianni Chessari ,
- Steven Howard ,
- Ildiko Maria Buck ,
- Benjamin David Cons ,
- Christopher Norbert Johnson ,
- Rhian Sara Holvey ,
- David Charles Rees ,
- Jeffrey David St. Denis ,
- Emiliano Tamanini ,
- Bernard Thomas Golding ,
- Ian Robert Hardcastle ,
- Celine Florence Cano ,
- Duncan Charles Miller ,
- Martin Edward Mäntylä Noble ,
- Roger John Griffin ,
- James Daniel Osborne ,
- Joanne Peach ,
- Arwel Lewis ,
- Kim Louise Hirst ,
- Benjamin Paul Whittaker ,
- David Wyn Watson ,
- Dale Robert Mitchell
The invention provides a compound of formula (I): ##STR00001##
or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
Isoindolinone inhibitors of the MDM2-P53 interaction having anticancer activity
- Gianni Chessari ,
- Steven Howard ,
- Ildiko Maria Buck ,
- Benjamin David Cons ,
- Christopher Norbert Johnson ,
- Rhian Sara Holvey ,
- David Charles Rees ,
- Jeffrey David St. Denis ,
- Emiliano Tamanini ,
- Bernard Thomas Golding ,
- Ian Robert Hardcastle ,
- Celine Florence Cano ,
- Duncan Charles Miller ,
- Martin Edward Mäntylä Noble ,
- Roger John Griffin ,
- James Daniel Osborne ,
- Joanne Peach ,
- Arwel Lewis ,
- Kim Louise Hirst ,
- Benjamin Paul Whittaker ,
- David Wyn Watson ,
- Dale Robert Mitchell
The invention provides a compound of formula (I): ##STR00001##
or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.
Compounds and methods of use
Compounds are provided according to Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8 and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Benzoimidazole Derivatives As Anticancer Agents
The disclosure relates to benzoimidazole derivatives, acting as anticancer drugs, as well as pharmaceutical composition containing the compounds. These compounds are able to firstly inhibit the protein/protein interactions of the MAP Kinase Erk, leading to inhibition of proliferation and secondly to induce apoptosis in human cancer cell lines.
ORGANIC ELECTRONIC DEVICE AND DISPLAY APPARATUS USING COMPOSITION FOR ORGANIC ELECTRONIC DEVICE
The present invention relates to an organic electric element and a display device using the same as a hole transport layer comprising a composition composed of two or more compounds having similar structures to improve luminous efficiency, stability and life span of an electric element, and an electronic device including the same.
ORGANIC ELECTRONIC DEVICE AND DISPLAY APPARATUS USING COMPOSITION FOR ORGANIC ELECTRONIC DEVICE
The present invention relates to an organic electric element and a display device using the same as a hole transport layer comprising a composition composed of two or more compounds having similar structures to improve luminous efficiency, stability and life span of an electric element, and an electronic device including the same.