- Method for preparing 1-(4-chlorphenyl)-pyrazolidine-3-one
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The invention relates to the field of bactericide synthesis, and discloses a method for preparing 1-(4-chlorphenyl)-pyrazolidine-3-one. The method comprises the following steps: 1) reacting parachloroaniline with acrylic acid to obtain an addition reactio
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Paragraph 0064; 0065-0067; 0079-0081; 0091-0094
(2021/02/10)
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- 2,3-dihydro-1H-quinoline-4-ketone thiosemicarbazone derivatives as well as preparation method and application thereof
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The invention discloses 2,3-dihydro-1H-quinoline-4-ketone thiosemicarbazone derivatives as well as a preparation method and application thereof. The structural formula of the derivatives is as shown in a formula (I): (the formula is as shown in the description), wherein R1 is halogen, alkyl or alkoxy; R2 is hydrogen, halogen or alkoxy; R3 is hydrogen or halogen; R4 is hydrogen or halogen; X is hydrogen, acetyl or nitryl; and Y is hydrogen or phenyl. The derivatives can obviously inhibit proliferation of tumor cells, and has significant inhibition effect on multiple cancer cell strains such asbreast cancer cells, melanoma cells and prostatic cancer cells; and the anti-tumor activity is obviously better than that of a broad-spectrum anti-cancer medicine cis-platinum. In addition, the preparation process of the derivatives is simple, the conditions are mild, the sources of the raw materials are rich, the production cost is low, and potential medicinal value and good application prospectin the aspect of preparing a novel anti-tumor medicine are achieved.
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Paragraph 0076-0079; 0185-0188
(2019/04/04)
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- Fused, Tricyclic Sulfonamide Inhibitors of Gamma Secretase
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The invention provides compounds of formula I: or pharmaceutically salts thereof where R1, R2, and the A, B, and C-rings are as defined herein. Compounds of formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds or salts of formula I, methods of preparing the desired compounds, and methods of treating cognitive disorders, such as Alzheimer's disease, using the compounds or salts of formula I.
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Page/Page column 78; 79
(2008/06/13)
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- Kinetics and mechanism of thermal gas-phase elimination of α- and β- (N-arylamino)propanoic acid: Experimental and theoretical analysis
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2-(N-Phenylamino)propanoic acid 1a and 3-(N-phenylamino)-propanoic acid 2a together with four of their aryl analogues were pyrolysed in the gas-phase. The reactions were homogeneous and free from catalytic and radical pathways. Analysis of the pyrolysate of 1 showed the elimination products to be carbon monoxide, acetaldehyde and aniline, while the pyrolysate of 2 reveals the formation of acrylic acid in addition to aniline. Theoretical study of the pyrolysis of 2 using an ab initio SCF method lend support to a reaction pathway involving a 4-membered cyclic transition state.
- Al-Awadi, Sundus A.,Abdallah, Mariam R.,Hasan, Mohamad A.,Al-Awadi, Nouria A.
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p. 3045 - 3049
(2007/10/03)
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- Pyridocarbazole derivatives having cGMP-PDE inhibitory activity
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PCT No. PCT/JP97/01829 Sec. 371 Date Jan. 29, 1998 Sec. 102(e) Date Jan. 29, 1998 PCT Filed May 29, 1997 PCT Pub. No. WO97/45427 PCT Pub. Date Dec. 4, 1997The invention relates to novel pyridocarbazole derivatives having highly selective action in inhibiting cyclic GMP-phosphodiesterase (hereinafter abbreviated as cGMP-PDE), processes for producing such derivatives, agents containing at least one of such derivatives as an active ingredient for preventing and/or treating pulmonary hypertension, ischemic heart diseases or diseases against which the cGMP-PDE inhibitory action is effective, and intermediates useful for the production of pyridocarbazole derivatives.
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