- PROCESS FOR PREPARING ATALUREN AND ITS INTERMEDIATES
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The present invention provides processes for the preparation of ataluren. Intermediates for preparing ataluren are also provided.
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Paragraph 0101-0102
(2018/01/18)
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- Novel method for synthesizing Ataluren
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The invention discloses a novel method for synthesizing Ataluren. The method comprises the following steps that 1, a compound 2 reacts with hydroxylamine hydrochloride under the alkaline condition to obtain an intermediate 3; 2, in the presence of a reducing agent diethoxymethylsilane and bis(4-nitrobenzophenone)phosphate, a catalytic amount of triphenylphosphine and an equivalent amount of carbon tetrachloride and compound 4 react to obtain the target compound Ataluren (1). According to the method, the raw materials are easy to obtain, the synthesizing steps are brief, environmental friendliness is achieved, aftertreatment is convenient, and high industrial production value is achieved.
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Paragraph 0020; 0021
(2017/08/25)
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- METHODS OF USE OF A CLASS llA HDAC INHIBITOR
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Novel uses of selective class Ila HDAC inhibitors are described.
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Paragraph 86
(2017/08/01)
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- Optical film, retardation plate, elliptica polarizing plate, liquid crystal display device and compound
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An optical film including at least one compound represented by formula (1) is disclosed. In the formula, Y11, Y12 and Y13 each independently represent methine or a nitrogen atom; R11, R12 and R13
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Paragraph 93; 94
(2016/11/21)
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- COMPOUNDS AND METHODS for the inhibition of HDAC
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Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
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Paragraph 0134-0135
(2015/11/24)
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- COMPOUNDS AND METHODS
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Disclosed are compounds having formula I, wherein X1, X2, X3, R1, R2, R3, R4, R5, Y, A, Z, L, m and n are as defined herein, and methods of making and using the same.
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Page/Page column 39
(2013/03/26)
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- Conformationally restricted analogs of the direct thrombin inhibitor FM 19
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The serine protease thrombin plays several key roles in the clotting cascade within the hemostatic system, such as in fibrin formation and platelet activation. Thus, development of an inhibitor that binds to the enzyme's active site (a direct thrombin inhibitor) offers an approach for the treatment of thrombus-associated diseases. Previous structure-activity relationship studies originally based on the bradykinin breakdown product Arg-Pro-Pro-Gly-Phe (RPPGF) led to the development of lead compound FM 19 (d-Arg-Oic-Pro-d-Ala-Phe(p-Me)- NH2). The recently determined X-ray structure of FM 19 in the active site of thrombin has revealed sites of modification to potentially improve inhibition. In this study, we report the synthesis and biological characterization of nine peptides that replace only the d-Arg residue of the FM 19 sequence, investigating ways to add conformational restriction, modification of the basic moiety at the end of the side chain, and removal of the charge from the N-terminus. Two of these peptides, 6 and 7 (IC50 values of 0.51 and 0.45 μM, respectively), show similar potency to the best compounds in the FM 19 series reported thus far.
- Girnys, Elizabeth A.,Porter, Vanessa R.,Mosberg, Henry I.
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experimental part
p. 7425 - 7434
(2012/01/02)
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- Pyridazinone derivatives
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Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment
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Page/Page column 19-20
(2011/11/12)
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- BENZOTHIAZOLONE DERIVATIVES
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Compounds of the formula I, in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and ca
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Page/Page column 19
(2011/11/12)
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- 2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS
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Compounds of the formula (I), in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
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Page/Page column 39-40
(2010/12/29)
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- 2-BENZYLPYRIDAZINONE DERIVATIVES AS MET KINASE INHIBITORS
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Compounds of the formula I in which R1, R2, R3, R4′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
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Page/Page column 23-24
(2010/12/26)
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- PROPANE-1,3-DION DERIVATIVE OR SALT THEREOF
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It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by -SO2-R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
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Page/Page column 19
(2008/06/13)
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- Benzene compounds
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The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.
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Page/Page column 70
(2010/11/27)
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