153034-78-7Relevant articles and documents
HETEROARYL COMPOUNDS AS INHIBITORS OF PROGRAMMED NECROSIS PATHWAY, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00231-00233, (2021/07/10)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the programmed necrosis pathway.
PYRIDINYLPYRAZOLOQUINOLINE COMPOUND
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Paragraph 0061; 0062, (2016/04/08)
A compound represented by formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 represents a group represented by the formula: a group represented by the formula: or a group represented by the formula: and R2 represe
Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma
Billaud, Emilie M.F.,Maisonial-Besset, Aurélie,Rbah-Vidal, Latifa,Vidal, Aurélien,Besse, Sophie,Béquignat, Jean-Baptiste,Decombat, Caroline,Degoul, Fran?oise,Audin, Laurent,Deloye, Jean-Bernard,Dollé, Frédéric,Kuhnast, Bertrand,Madelmont, Jean-Claude,Tarrit, Sébastien,Galmier, Marie-Josèphe,Borel, Michèle,Auzeloux, Philippe,Miot-Noirault, Elisabeth,Chezal, Jean-Michel
, p. 818 - 838 (2015/03/05)
Melanin pigment represents an attractive target to address specific treatment to melanoma cells, such as cytotoxic radionuclides. However, less than half of the patients have pigmented metastases. Hence, specific marker is required to stratify this patient population before proceeding with melanin-targeted radionuclide therapy. In such a context, we developed fluorinated analogues of a previously studied melanin-targeting ligand, N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide (ICF01012). These latter can be labeled either with 18F or 131I/125I for positron emission tomography imaging (melanin-positive patient selection) and targeted radionuclide therapy purposes. Here we describe the syntheses, radiosyntheses and preclinical evaluations on melanoma-bearing mice model of several iodo- and fluoro(hetero)aromatic derivatives of the ICF01012 scaffold. After preliminary planar gamma scintigraphic and positron emission tomography imaging evaluations, [125I]- and [18F]-N-[2-(diethylamino)ethyl]-4-fluoro-3-iodobenzamides ([125I]4, [18F]4) were found to be chemically and biologically stable with quite similar tumor uptakes at 1 h p.i. (9.7 ± 2.6% ID/g and 6.8 ± 1.9% ID/g, respectively).
PYRAZOLOQUINOLINE DERIVATIVES
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Paragraph 0426; 0427; 0428, (2013/06/26)
A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.
[1H- PYRAZOLO [3, 4-B] PYRIDINE-4-YL] -PHENYLE OR -PYRIDIN-2-YLE DERIVATIVES AS PROTEIN KINASE C-THETA
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Page/Page column 169, (2009/07/17)
The present invention relates to compounds of formula (I) and (IA) useful as inhibitors of protein kinase (1a). The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. (a) : in particular protein kinase C theta, wherein A and A' are independently -N- or -C(R+) -. Ring B is five- or six-membered saturated carbocyclic or heterocyclic R1, R2, R3, R4, R5, R6, R7, x and y are as described herein.
BACTERICIDE COMPOSITION AND METHOD OF CONTROLLING PLANT DISEASE
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Page/Page column 13-14, (2008/06/13)
It is to provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing as active ingredients (a) a benzoylpyridine derivative represented by the formula (I) or its salt: (wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2' is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2" is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2' and R2" may form a condensed ring containing an oxygen atom) and (b) at least one another fungicide.
3-BENZOYL-2,4,5-SUBSTITUTED PYRIDINE DERIVATIVES OR SALTS THEREOF AND BACTERICIDES CONTAINING THE SAME
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Page/Page column 7, (2010/02/13)
To provide 3-benzoyl-2,4,5-substituted pyridine derivatives or their salts, fungicides containing them, and intermediates for producing them. By providing a group of compounds comprising specific 3-benzoyl-2,4,5-substituted pyridine derivatives or their s
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors
Wang, Le,Lin, Nan-Horng,Li, Qun,Henry, Rodger F.,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan C.,Bauch, Joy L.,Rosenberg, Saul H.,Sham, Hing L.
, p. 4603 - 4606 (2007/10/03)
The synthesis and biological evaluation of two novel series of potent and selective FTase inhibitors are described. Two novel series of potent and selective FTase inhibitors have been synthesized using structure-based design. Medicinal chemistry efforts led to the discovery of compound 4e with potent cellular activity and good oral bioavailability in dog. A synthetic route toward novel heterocycles 1,5-dimethyl-6-oxo-4-aryl-1,6-dihydro-pyridine-2- carbonitrile was established. The structure of compound 5c was confirmed by X-ray crystallography.
HETEROCYCLIC KINASE INHIBITORS
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Page 89, (2010/02/08)
Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Farnesyltransferase inhibitors
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, (2008/06/13)
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.