25724-79-2Relevant articles and documents
INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
-
Page/Page column 128, (2021/09/11)
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy
Ashcraft, Luke,Chin, Eva R.,Chuang, Chihyuan,Collibee, Scott,Cremin, Peadar,Hartman, James,Hwee, Darren T.,Malik, Fady I.,Morgan, Bradley P.,Robertson, Laura A.,Schaletzky, Julia,Vander Wal, Mark,Wang, Jingying,Wang, Wenyue,Wang, Xiaolin,Wehri, Eddie,Wu, Yangsong,Zamora, Jeanelle
supporting information, p. 14142 - 14152 (2021/10/20)
Hypercontractility of the cardiac sarcomere may be essential for the underlying pathological hypertrophy and fibrosis in genetic hypertrophic cardiomyopathies. Aficamten (CK-274) is a novel cardiac myosin inhibitor that was discovered from the optimization of indoline compound 1. The important advancement of the optimization was discovery of an Indane analogue (12) with a less restrictive structure-activity relationship that allowed for the rapid improvement of drug-like properties. Aficamten was designed to provide a predicted human half-life (t1/2) appropriate for once a day (qd) dosing, to reach steady state within two weeks, to have no substantial cytochrome P450 induction or inhibition, and to have a wide therapeutic window in vivo with a clear pharmacokinetic/pharmacodynamic relationship. In a phase I clinical trial, aficamten demonstrated a human t1/2 similar to predictions and was able to reach steady state concentration within the desired two-week window.
CARDIAC SARCOMERE INHIBITORS
-
Paragraph 0245, (2020/01/24)
Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, Y1, Y2, L1, and G1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
DIHYDROBENZOFURAN AND INDEN ANALOGS AS CARDIAC SARCOMERE INHIBITORS
-
Paragraph 0377, (2019/08/08)
Provided are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, Z, B, R1, R2, R3, G1, G2, and G3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt, thereof for use in methods of treatment heart diseases through cardiac sarcomere inhibtion.
Aromatic ring functionalization of benzolactam derivatives: New potent dopamine D3 receptor ligands
Ortega, Raquel,Hübner, Harald,Gmeiner, Peter,Masaguer, Christian F.
supporting information; experimental part, p. 2670 - 2674 (2011/06/20)
Since the discovery of the dopamine D3 receptor, an intensive effort has been directed toward the development of potent and selective ligands in order to elucidate the function and potential therapeutic advantages of targeting D3 rec
PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
-
Page/Page column 11-12, (2011/11/13)
The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR,
HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS
-
Page/Page column 21, (2009/04/24)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
AMINO ACID COMPOUNDS
-
Page/Page column 47, (2009/12/23)
[Problem] To provide novel compounds that are S1P1 receptor agonists and exhibit an immunosuppressive activities by inducing lymphocyte sequestration in secondary lymphoid tissues. In addition, to provide a pharmaceutical agent which comprises the compounds as an effective component, in particular to provide a therapeutic and/or prophylactic agent for an autoimmune disease and the like. [Solving Means] Amino acid compounds that are represented by the following Formula (1) are provided
PESTICIDAL CONDENSED - RING ARYL COMPOUNDS
-
Page/Page column 139, (2009/10/22)
Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping -W1-W2-W3-W4- are as defined herein.
Organocatalytic enantioselective synthesis of metabotropic glutamate receptor ligands
Suri, Jeff T.,Steiner, Derek D.,Barbas III, Carlos F.
, p. 3885 - 3888 (2007/10/03)
(Chemical Equation Presented) (R)-Proline catalyzes the amination reaction of functionalized indane carboxaldehydes and allows for the efficient enantioselective synthesis (>99% ee) of the metabotropic glutamate receptor ligands (S)-AIDA and (S)-APICA.
