- OXOACRIDINYL ACETIC ACID DERIVATIVES AND METHODS OF USE
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Compounds of Formulae I, II, their pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein are provided. Methods involving compounds of Formulae I or II as effective modulators of STING are also provided.
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Page/Page column 99-100
(2020/11/30)
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- Dioxolone structure containing 4 - N substituted quinazoline derivatives and its preparation and use (by machine translation)
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The invention discloses a dioxolone structure containing 4 -NSubstituted quinazoline derivatives, its structure such as shown in I. This invention has introduced to substituted benzoic acid, methanol, nitric acid, formamide, trichloro oxygen phosphorus chlorine, nitrobenzene formaldehyde, acetone, stannous chloride, substituted aromatic aldehyde as raw material, by the multi-step reaction to synthesize the target compound. The compounds can be used as anti-tumor, anti-bacterial plant and anti-plant-virus of the drug. (1 E, 4 E) - 1 - substituted phenyl - 5 - (4 - (substituted quinazoline - 4 - amino) phenyl) - 1, 4 - pentadiene - 3 - one. (by machine translation)
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Paragraph 0045; 0046
(2017/11/16)
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- Method of Synthesizing 6,7-Substituted 4-Anilino Quinazoline
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A method of synthesizing 6,7-substituted 4-anilino quinazoline employs 3,4-substituted benzoic acid as an initial reactant, and the 6,7-substituted 4-anilino quinazoline is obtained by an esterifying step, a nitrating step, a reducing step, a cyclizing step, and an one-pot reaction. In the above method, the initial reactant has low cost and yield. of the 6,7-substituted 4-anilino quinazoline is high, therefore, production cost can be reduced effectively, and competitive power of the product of the 6,7-substituted 4-anilino quinazoline can be improved.
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Page/Page column 6
(2010/11/03)
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- Benzamides and benzamidines as specific inhibitors of epidermal growth factor receptor and v-Src protein tyrosine kinases
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The benzamides 1 and the benzamidines 2 as well as the cyclic benzamidines 3 were designed and synthesized as the mimics of 4-anilinoquinazolines for an inhibitor of EGFR tyrosine kinase. The specific inhibitions of EGFR tyrosine kinase were observed in the benzamides 1c and 1d, and the benzamidine 2a, whereas the specific inhibitions of v-Src kinase were observed in the benzamide 1j and the benzamidine 2d at a 10μg/mL concentration of compounds. The cyclic benzamidines 3a and 3b showed potent kinase inhibition of EGFR at a 1.0μg/mL concentration. According to the docking simulation using the X-ray structure of EGFR kinase domain in complex with erlotinib, the LigScore2 scoring function value of erlotinib was calculated as 5.61, whereas that of the benzamide 1c was 5.05. In a similar manner, the LigScore2 value of the cyclic benzamidine 3a was calculated as 5.10.
- Asano, Toru,Yoshikawa, Tomohiro,Usui, Taikou,Yamamoto, Hiroshi,Yamamoto, Yoshinori,Uehara, Yoshimasa,Nakamura, Hiroyuki
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p. 3529 - 3542
(2007/10/03)
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- Synthesis of 3,4-dihydroxy-6-(N-ethylamino)benzamide, a new phenolic compound isolated from green pepper (Piper nigrum L.) berries
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The synthesis of 3,4-dihydroxy-6-(N-ethylamino)benzamide (9), a novel phenolic constittuent of green pepper berries, responsible for its blackening during drying process has been developed from vanillic acid (1) in eight steps.Use of mild reaction conditions such as employing anhydrous ammonium formate as hydrogen transfer agent during reduction of 3 at room temperature (Step III), reductive alkylation of 4 with sodium borohydride and acetic acid (Step IV) and protecting the amino group using acetic acid (Step IV) and protecting the amino group using trifluoroacetic acid prior to demethylation (Step VII) and hydrolysis (Step VIII) results in an acceptable yield of the final product (9) despite its highly unstable nature.
- Variyar, Prasad S.,Bandyopadhyay, Chiranjib
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p. 911 - 913
(2007/10/03)
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- 6-NITRO-ISO-VANILLIC ACID, AN UNUSUAL CHROMOGEN FROM THE GENUS CORTINARIUS
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Key Word Index-Cortinarius; Sericeocybe; Agaricales; pigment; 6-nitro-iso-vanillic acid. 6-Nitro-iso-vanillic acid, a new natural product, has been isolated from the fruit bodies of an Australian toadstool belonging to Cortinarius (Sericeocybe).
- Gill, Melvyn,Gimenez, Alberto,Strauch, Richard J.
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p. 2815 - 2818
(2007/10/02)
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- 3-Alkoxy-thianapthene-2-carboxamides
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The 3-alkoxy-thianaphthene-2-carboxamides of this invention are effective for the treatment of mammals afflicted with emesis. When administered to dogs in dosages of 250 μg/kg, compounds of this invention give 100% protection against vomiting normally induced by subcutaneous administration of apomorphine. The compounds of this invention also favorably modify behavior disturbances in mammals.
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