62516-08-9Relevant articles and documents
DO3A type highly stable paramagnetic probe capable of being used for intracellular magnetic resonance research and preparation method of DO3A type highly stable paramagnetic probe
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Paragraph 0055; 0058; 0061-0062, (2019/01/15)
The invention provides a DO3A type highly stable paramagnetic probe T1 capable of being used for intracellular magnetic resonance research and a preparation method of the DO3A type highly stable paramagnetic probe T1. The structural formula of the paramag
A Reactive, Rigid GdIII Labeling Tag for In-Cell EPR Distance Measurements in Proteins
Yang, Yin,Yang, Feng,Gong, Yan-Jun,Chen, Jia-Liang,Goldfarb, Daniella,Su, Xun-Cheng
supporting information, p. 2914 - 2918 (2017/03/14)
The cellular environment of proteins differs considerably from in vitro conditions under which most studies of protein structures are carried out. Therefore, there is a growing interest in determining dynamics and structures of proteins in the cell. A key factor for in-cell distance measurements by the double electron–electron resonance (DEER) method in proteins is the nature of the used spin label. Here we present a newly designed GdIII spin label, a thiol-specific DOTA-derivative (DO3MA-3BrPy), which features chemical stability and kinetic inertness, high efficiency in protein labelling, a short rigid tether, as well as favorable spectroscopic properties, all are particularly suitable for in-cell distance measurements by the DEER method carried out at W-band frequencies. The high performance of DO3MA-3BrPy-GdIII is demonstrated on doubly labelled ubiquitin D39C/E64C, both in vitro and in HeLa cells. High-quality DEER data could be obtained in HeLa cells up to 12 h after protein delivery at in-cell protein concentrations as low as 5–10 μm.
INDOLE AND AZAINDOLE HALOALLYLAMINE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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Paragraph 0318, (2017/09/05)
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
AROMATIC RING COMPOUND
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Paragraph 0296, (2015/01/18)
Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
Discovery of potent and selective pyrazolopyrimidine Janus kinase 2 inhibitors
Hanan, Emily J.,Van Abbema, Anne,Barrett, Kathy,Blair, Wade S.,Blaney, Jeff,Chang, Christine,Eigenbrot, Charles,Flynn, Sean,Gibbons, Paul,Hurley, Christopher A.,Kenny, Jane R.,Kulagowski, Janusz,Lee, Leslie,Magnuson, Steven R.,Morris, Claire,Murray, Jeremy,Pastor, Richard M.,Rawson, Tom,Siu, Michael,Ultsch, Mark,Zhou, Aihe,Sampath, Deepak,Lyssikatos, Joseph P.
, p. 10090 - 10107 (2013/01/16)
The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the p
PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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Page/Page column 83-84, (2011/02/24)
A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical
INHIBITORS OF AKT ACTIVITY
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Page/Page column 55-56, (2008/12/04)
Invented are novel pyrazole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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Page/Page column 48, (2008/12/04)
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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Page/Page column 40, (2008/12/04)
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
MCH receptor antagonists
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Page/Page column 11-12; 18-19, (2008/06/13)
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 obesity, hyperphagia, anxiety, depression and related disorders and diseases.