204972-81-6Relevant articles and documents
New method for preparing dabigatran etexilate intermediate
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Paragraph 0008; 0021, (2016/11/24)
The invention discloses a new method for preparing a dabigatran etexilate intermediate. The new method includes the steps that 3-methoxy-4-aminobenzoate serves as a starting raw material firstly, and then the dabigatran etexilate key intermediate 3-[[[2-[[(4-cyanophenyl)amino]methyl]-1-methyl-1H-benzimidazole-5-yl]carbonyl]-pyridine-2-yl amino]ethyl propionate is prepared through the steps of substitution, condensation, cyclization and the like. Reaction conditions in all the steps of the synthetic process are mild, the reaction yield is high, the purity of the end product is higher than 99.0%, and the new method is suitable for industrialized production.
Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents
Zhang, Qin,Zhong, Ying,Yan, Lin-Na,Sun, Xun,Gong, Tao,Zhang, Zhi-Rong
, p. 1010 - 1014 (2011/03/21)
A series of curcumin analogues with different substituents at the 4-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines. Several novel curcumin analogues, especially 32 and 34, exhibited selective and potent cytotoxic activity against human epidermoid carcinoma cell line A-431 and human glioblastoma cell line U-251, implying their specific potential in the chemoprevention and chemotherapy of skin cancer and glioma. The preliminary SAR information extracted from the results suggested that introduction of appropriate substituents to the 4′-positions could be a promising approach for the development of new cytotoxic curcumin analogues with special selectivity for A-431 and U-251 cell lines.
THERAPEUTIC AGENT FOR RESPIRATORY DISEASE CONTAINING 4-HYDROXYPIPERIDINE DERIVATIVE AS ACTIVE INGREDIENT
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Page/Page column 31, (2008/06/13)
An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or -NR7-(wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that when n is 1, G1 and G2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R1 is, for example, NO2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R2and R3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO2; each of R4 and R5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.
Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
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, (2008/06/13)
A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1is optionally substituted phenyl; Ar2is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1is hydrogen, hydroxy, or C1-C4alkyl; and R2and R3are independently selected from optionally substituted C1-C7alkyl, C3-C6cycloalkyl, C2-C6alkenyl, C2-C6alkynyl, or R2and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.
