- COMPOUNDS TARGETING RNA-BINDING PROTEINS OR RNA-MODIFYING PROTEINS
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The invention relates to a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising the same and methods of preparing and using the same. The variables are described herein.
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Page/Page column 189; 190
(2021/09/11)
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- A Novel One-Pot Synthesis of N,N-Dimethylaminopyridines by Diazotization of Aminopyridines in Dimethylformamide in the Presence of Trifluoromethanesulfonic Acid
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Abstract: Diazotization of aminopyridines in the presence of trifluoromethanesulfonic acid gives the corresponding pyridinyl trifluoromethanesulfonates instead of expected diazonium salts. Pyridinyl trifluoromethanesulfonates can be converted to N,N-dimethylaminopyridines on heating in dimethylformamide via replacement of the trifluoromethanesulfonyloxy group. The reaction is accelerated under microwave irradiation. A novel one-pot procedure has been proposed for the synthesis of 2- and 4-(dimethylamino)pyridines from commercially available aminopyridines. The procedure provides high yields of the target products, and it can be regarded as an alternative to the known methods of synthesis of N,N-dimethylpyridin-4-amine (DMAP) widely used as base catalyst in organic synthesis.
- Filimonov, V. D.,Krasnokutskaya, E. A.,Potapova, M. I.,Sanzhiev, A. N.
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p. 1023 - 1028
(2020/07/25)
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- As tyrosine kinase inhibitors of the nitrogen-containing heteroaromatic ring derivatives
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The present invention relates to compounds as represented by general formula (I) as tyrosine kinase inhibitors, preparation method thereof, pharmaceutical compositions containing the compounds, and uses thereof for preventing and/or treating instances of B-cell related leukemia, inflammatory diseases and autoimmune diseases, wherein A, ring B, L1, L2, R1, R2, R3, a, b, c, d, e, p and q are as defined in the specification.
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Paragraph 0524; 0525; 0526; 0527; 0528
(2018/09/02)
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- Discovery of potent transient receptor potential vanilloid 1 antagonists: Design and synthesis of phenoxyacetamide derivatives
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We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50 = 411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC50 = 33 nM). In addition, 15d ameliorated bladder overactivity in rats in vivo.
- Takahashi, Eiki,Hirano, Noriyuki,Nagahara, Takashi,Yoshikawa, Satoru,Momen, Shinobu,Yokokawa, Hiroshi,Hayashi, Ryoji
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p. 3154 - 3156
(2013/06/26)
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- PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY
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Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
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Page/Page column 55
(2011/02/15)
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- Anti-Viral Compounds
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Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
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- A simple synthesis of aminopyridines: Use of amides as amine source
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A transition metal/microwave irradiation (or base) free synthesis of aminopyridines has been accomplished via C-N bond forming reaction between chloropyridine and a variety of simple amides under refuxing conditions.
- Kodimuthali, Arumugam,Mungara, Anitha,Prasunamba, Padala Lakshmi,Pal, Manojit
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experimental part
p. 1439 - 1445
(2010/11/04)
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- Organic compounds
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.
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Page/Page column 26
(2009/05/29)
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- NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula (I): in which the substitutents are as defined in claim 1 and and salts, solvates, hydrates and N- oxides thereof.
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Page/Page column 60
(2008/12/08)
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- SELECTIVE AZOLE PDE10A INHIBITOR COMPOUNDS
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The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
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Page/Page column 112
(2010/11/29)
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- ANTHRANILAMIDES
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The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof wherein R1, R2, and Het are as defined herein. Compounds of the present invention are useful as Aurora kinase inhibitors.
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Page/Page column 22
(2009/01/20)
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- INDOLINONE DERIVATIVES AND THEIR USE IN TREATING DISEASE-STATES SUCH AS CANCER
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The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 21
(2009/01/24)
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- Diacylglycerol acyltransferase inhibitors
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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 diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 15
(2010/11/27)
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- COMPOUNDS AND THERAPEUTICAL USE THEREOF
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Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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Page/Page column 76 - 77
(2008/06/13)
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- N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.
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- Substituted benzazoles and methods of their use as inhibitors of Raf kinase
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New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
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- Neuropeptide Y antagonists
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The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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Page column 33
(2010/02/05)
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- Intermediates from ring-opening reactions. Reactions of 2-chloro-5-nitropyridine and 2-chloro-3-nitropyridine with deuteroxide ion in selected solvents
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Open chain intermediates from the ring-opening reaction of aqueous sodium deuteroxide (2 mol) with 2-chloro-5-nitropyridine (1 mol) and 2-chloro-3-nitropyridine (1 mol) were isolated.These intermediates were purified, analyzed for elemental composition, and characterized by various spectrophotometric techniques.The intermediate formed from 2-chloro-5-nitropyridine and two equivalents of deuteroxide ion reacts with additional deutroxide in D2O in various polar solvents to reclose the pyridine ring.The kinetics of the ring closure reaction are reported and are supplemented with observations of salt and solvent effects upon the rate of closure.In addition, a mechanism for the ring closure is presented.The intermediate formed from 2-chloro-3-nitropyridine did not undergo a similar ring closure when reacted with additional deuteroxide, but instead formed various decomposition products.A reason for failure of this ring closure is suggested.
- Reinheimer, John D.,Sourbatis, Nicolas,Lavallee, Robert L.,Goodwin, Douglas,Gould, George L.
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p. 1120 - 1123
(2007/10/02)
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