15865-57-3Relevant articles and documents
Quantum Tunneling Mediated Interfacial Synthesis of a Benzofuran Derivative
Paintner, Tobias,Bj?rk, Jonas,Du, Ping,Klyatskaya, Svetlana,Paszkiewicz, Mateusz,Hellwig, Raphael,Uphoff, Martin,?ner, Murat A.,Cuniberto, Edoardo,Deimel, Peter S.,Zhang, Yi-Qi,Palma, Carlos-Andres,Allegretti, Francesco,Ruben, Mario,Barth, Johannes V.,Klappenberger, Florian
supporting information, p. 11285 - 11290 (2019/07/15)
Reaction pathways involving quantum tunneling of protons are fundamental to chemistry and biology. They are responsible for essential aspects of interstellar synthesis, the degradation and isomerization of compounds, enzymatic activity, and protein dynami
Heavily Substituted Atropisomeric Diarylamines by Unactivated Smiles Rearrangement of N-Aryl Anthranilamides
Costil, Romain,Dale, Harvey J. A.,Fey, Natalie,Whitcombe, George,Matlock, Johnathan V.,Clayden, Jonathan
supporting information, p. 12533 - 12537 (2017/09/13)
Diarylamines find use as metal ligands and as structural components of drug molecules, and are commonly made by metal-catalyzed C?N coupling. However, the limited tolerance to steric hindrance of these couplings restricts the synthetic availability of more substituted diarylamines. Here we report a remarkable variant of the Smiles rearrangement that employs readily accessible N-aryl anthranilamides as precursors to diarylamines. Conformational predisposition of the anthranilamide starting material brings the aryl rings into proximity and allows the rearrangement to take place despite the absence of electron-withdrawing substituents, and even with sterically encumbered doubly ortho-substituted substrates. Some of the diarylamine products are resolvable into atropisomeric enantiomers, and are the first simple diarylamines to display atropisomerism.
Substituted fused pyrimidinone and dihydro-pyrimidone
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Paragraph 0170, (2016/10/08)
The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
ARYL FUSED LACTAMS AS EZH2 MODULATORS
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Page/Page column 77; 78, (2016/04/19)
This invention relates to compounds of Formula (I) in which R1, R2, R3, R4, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
ARYL AND HETEROARYL FUSED LACTAMS
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Paragraph 0838; 0839; 0840, (2014/07/08)
This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Towards the development of chromone-based MEK1/2 modulators
Redwan, Itedale Namro,Dyrager, Christine,Solano, Carlos,Fernández De Trocóniz, Guillermo,Voisin, Laure,Bliman, David,Meloche, Sylvain,Gr?tli, Morten
, p. 127 - 138 (2014/08/18)
Inhibition or allosteric modulation of mitogen-activated protein kinase kinases MEK1 and MEK2 (MEK1/2) represent a promising strategy for the discovery of new specific anticancer agents. In this paper, structure-based design, beginning from the lead compound PD98059, was used to study potential structural modifications on the chromone structure in order to obtain highly potent derivatives that target the allosteric pocket in MEK1. Subsequently, a small series of PD98059 analogs were synthesized to provide a first generation of chromone-based derivatives that inhibit the activation of MEK1 with IC 50 values as low as 30 nM in vitro. Complementary cellular studies also showed that two of the compounds in the series inhibit the activity of MEK1/2 with IC50 values in the nanomolar range (73-97 nM). In addition, compounds in this series were found to inhibit the proliferation of a small panel of human cancer cell lines.
QUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
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Page/Page column 47; 48, (2013/04/24)
This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr
SUBSTITUTED 1-ALKYLCINNOLIN-4(1H)-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION OF SAME
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Page/Page column 8, (2012/06/01)
The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C2-C5)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R1 represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R2 represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO2-Alk, —CO—N(R4)-Alk, —N(R4)SO2-Alk, —N(R4)CO-Alk, —N(R4)SO2—N(Alk)2; R3 represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 represents a hydrogen atom or a (C1-C4)alkyl; Alk represents an unsubstituted or substituted (C1-C4)alkyl. Preparation process and therapeutic application.
SUBSTITUTED 1-BENZYL-CINNOLIN-4(1H)-ONE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
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Page/Page column 6, (2011/06/26)
The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB2 receptors, their preparation and their therapeutic application.
QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 107, (2010/06/15)
The invention is directed to quinazoline compounds that can inhibit the bioactivity of one or more kinase enzymes, including a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Fit kinase, an Aurora kinase, or a Src kinase, or any combination thereof; to methods of use of those compounds; and to methods of preparation of those compounds. The inventive compounds can be used in the treatment of malconditions including cardiovascular disease, neurogenic pain, hypertension, atherosclerosis, angina, stroke, arterial obstruction, peripheral arterial disease, erectile dysfunction, acute and chronic pain, dementia, Alzheimer's disease, Parkinson's disease, neuronal degeneration, asthma, amyotrophic lateral sclerosis, spinal cord injury, rheumatoid arthritis, osteoarthritis, osteoporosis, psoriasis, cerebral vasospasm, open angle glaucoma, multiple sclerosis, pulmonary hypertension, acute respiratory distress syndrome, inflammation, diabetes, urinary organ diseases and benign prostatic hypertrophy (BPH), metastasis, cancer, glaucoma, ocular hypertension, retinopathy, autoimmune disease, viral infection, or myocardial pathology.
