197080-73-2Relevant academic research and scientific papers
A New Lead Identification Strategy: Screening an sp3-rich and Lead-like Compound Library Composed of 7-Azanorbornane Derivatives
Karaki, Fumika,Umemoto, Sho,Ashizawa, Karin,Oki, Tomoya,Sato, Noriko,Ogino, Takumi,Ishibashi, Naoto,Someya, Ryoto,Miyano, Kanako,Hirayama, Shigeto,Uezono, Yasuhito,Fujii, Hideaki
, p. 1840 - 1848 (2019)
Although the advantages of sp3-rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2-rich components. Compounds that are sp3-rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp3-rich libraries. By modifying sp3-rich 7-azanorbornane scaffolds through click chemistry, we efficiently prepared a small set of compounds. These compounds were not only sp3-rich, but also had sufficient “lead-like” properties in view of molecular weights and hydrophobicity. Screening assays of this library provided weak κ opioid receptor agonists and growth hormone secretagogue receptor agonists with high hit rates. These results indicate that the 7-azanorbornane scaffold may be a “privileged structure” for lead identification in drug discovery.
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
-
Paragraph 001667; 001670, (2018/07/29)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
PYRROLOPYRIDINE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
-
Paragraph 0140; 0141, (2017/11/06)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
BENZIMIDAZOLE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
-
Paragraph 139; 140, (2016/02/12)
Provided herein are compounds of the formulas (I) and (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN
-
Paragraph 0344, (2015/05/26)
Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
Visible-light-triggered release of nitric oxide from N-pyramidal nitrosamines
Karaki, Fumika,Kabasawa, Yoji,Yanagimoto, Takahiro,Umeda, Nobuhiro,Firman,Urano, Yasuteru,Nagano, Tetsuo,Otani, Yuko,Ohwada, Tomohiko
experimental part, p. 1127 - 1141 (2012/03/26)
Although many organic/inorganic compounds that release nitric oxide (NO) upon photoirradiation (phototriggered caged-NOs) have been reported, their photoabsorption wavelengths mostly lie in the UV region, because X - NO bonds (X=heteroatom and metal) generally have rather strong π-bond character. Thus, it is intrinsically difficult to generate organic compounds that release NO under visible light irradiation. Herein, the structures and properties of N-pyramidal nitrosamine derivatives of 7-azabicyclo[2.2.1]heptanes that release NO under visible light irradiation are described. Bathochromic shifts of the absorptions of these nitrosamines, attributed to HOMO (n)-LUMO (π*) transitions associated with the nonplanar structure of the N - NO moiety, enable the molecules to absorb visible light, which results in N - NO bond cleavage. Thus, these compounds are innate organic caged-NOs that are uncaged by visible light. A visible difference: Nitrosamine derivatives of 7-azabicyclo[2.2.1]heptanes undergo N - NO bond cleavage upon exposure to visible light at wavelengths longer than 420a nm, thereby releasing NO. Bathochromic shifts of the absorptions of these nitrosamines are attributed to HOMO (n)-LUMO (π*) transitions associated with the nonplanar structure of the N - NO moiety (see figure). Copyright
BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
-
Page/Page column 106-107, (2010/07/09)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
Oligomers of β-amino acid bearing non-planar amides form ordered structures
Otani, Yuko,Futaki, Shiroh,Kiwada, Tatsuto,Sugiura, Yukio,Muranaka, Atsuya,Kobayashi, Nagao,Uchiyama, Masanobu,Yamaguchi, Kentaro,Ohwada, Tomohiko
, p. 11635 - 11644 (2007/10/03)
In this report, we explore the feasibility of using bicyclic chiral β-amino acids, (1R,2R,4S)- and (1S,2S,4R)-7-azabicyclo[2.2.1]heptane-2-carboxylic acid (R-Ah2c and S-Ah2c, respectively), to prepare novel peptides with unique properties. Facile cis-trans isomerization of the non-planar amide bonds of these β-amino acids should result in great flexibility of the backbone structure of β-peptides containing them. Indeed, oligomers of these amino acids showed thermostability and characteristic CD absorptions, which were not concentration-dependent, suggesting that the oligomers remained monomeric. The results indicated the formation of self-organized monomeric structures with chain-length-dependent stabilization. Energy calculations suggested that the peptides can take helical structures in which the energy barriers to cis-trans isomerization are greater for the central amide bonds than for the terminal amides.
COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES
-
Page 45, (2010/02/06)
The invention discloses compounds that are selective α7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.
1H-PYRAZOLE AND 1H-PYRROLE-AZABICYCLIC COMPOUNDS WITH ALFA-7 NACHR ACTIVITY
-
Page 76-77, (2010/02/06)
The invention provides compounds of Formula (I), wherein Azabicyclo is Formula (I, II, III, IV, V, VI, VII); W is Formula (m); where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which α7 is known to be involved.
