38789-75-2Relevant academic research and scientific papers
PYRAZOLOPYRIDINE COMPOUND AS RET INHIBITOR AND APPLICATION THEREOF
-
Paragraph 0464-0466, (2022/02/19)
Disclosed is a series of pyrazolopyridine compounds, and application thereof in the preparation of RET kinase inhibitors for treatment. Specifically disclosed is the compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
Novel indirect AMP-activated protein kinase activators: Identification of a second-generation clinical candidate with improved physicochemical properties and reduced hERG inhibitory activity
Kuramoto, Kazuyuki,Sawada, Yuki,Yamada, Tomohiro,Nagashima, Takeyuki,Ohnuki, Kei,Shin, Takashi
, p. 452 - 465 (2020/09/09)
This study reports the synthesis and evaluation of novel indirect AMP-activated protein kinase (AMPK) activators. The series of compounds selectively inhibited cell growth in several human breast cancer cell lines by activating AMPK. We performed back-up medicinal chemistry synthetic research on ASP4132, a previously reported as a compound for clinical development that acts as an indirect AMPK activator. This led to the successful identification of 4-({4-[5-({1-[(5-ethoxypyrazin-2-yl)methyl]-4-fluoropiperidin-4-yl}methoxy)-3-methylpyridine-2-carbonyl]piperazin-1-yl}methyl)benzonitrile succinate (27b), a potent, highly aqueous soluble and metabolically stable compound in human hepatocytes. Compound 27b also showed weaker human Ether-a-go-go Related Gene (hERG) inhibitory activity than that of compound 13 and ASP4132. Therefore, 27b was a promising AMPK activator and a second-generation clinical candidate for treatment for human cancer.
COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
-
Page/Page column 117; 118, (2019/07/19)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
-
Paragraph 0556-0557, (2019/07/10)
The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
-
Page/Page column 114-115, (2019/07/19)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.
1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
-
Page/Page column 108; 109, (2018/09/25)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
Ruf, Sven,Hallur, Mahanandeesha Siddappa,Anchan, Nisha K.,Swamy, Indu N.,Murugesan, Karthikai Raj,Sarkar, Sayantani,Narasimhulu, Lokesh Kananti,Putta, V.P. Rama Kishore,Shaik, Shama,Chandrasekar, Devaraj Venkatapura,Mane, Vishal Subhash,Kadnur, Sanjay Venkatachalapathi,Suresh, Juluri,Bhamidipati, Ravi Kanth,Singh, Manvi,Burri, Raghunadha Reddy,Kristam, Rajendra,Schreuder, Herman,Czech, Joerg,Rudolph, Christine,Marker, Alexander,Langer, Thomas,Mullangi, Ramesh,Yura, Takeshi,Gosu, Ramachandraiah,Kannt, Aimo,Dhakshinamoorthy, Saravanakumar,Rajagopal, Sridharan
supporting information, p. 922 - 925 (2018/02/14)
Nicotinamide N-methyltransferase (NNMT) has been linked to obesity and diabetes. We have identified a novel nicotinamide (NA) analog, compound 12 that inhibited NNMT enzymatic activity and reduced the formation of 1-methyl-nicotinamide (MNA), the primary metabolite of NA by ～80% at 2 h when dosed in mice orally at 50 mg/kg.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
-
Paragraph 0202, (2016/03/22)
Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
-
Paragraph 0119, (2016/03/22)
Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
-
Paragraph 0167, (2016/03/22)
Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use. Formula (I)
