- Preparation method of m-cyanomethyl methyl benzoate
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The invention discloses a preparation method of m-cyanomethyl methyl benzoate. According to the method, m-bromobenzoic acid is used as a starting raw material; the m-bromine methyl methyl benzoate is prepared through esterification; m-methoxy formyl phenethyl alcohol is obtained and prepared through Grignard reaction; through oxidization, the m-methoxy formyl phenylacetic acid is prepared; through amidation and dewatering, the m-cyanomethyl methyl benzoate is finally prepared. The preparation method provided by the invention has the advantages that the design is ingenious; the route is novel; the raw materials have low price and can be easily obtained; the process is simple; the implementation is easy; the yield is high; the purity of the obtained final product is high; the quality is high; no dangerous process exists; the extremely toxic substances of cyanides and expensive cyaniding reagents used in the conventional synthesis are avoided; the requirements on the equipment are simple; the production difficulty and the production cost investment are reduced; the industrial production can be favorably realized; the economic benefits are good.
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Paragraph 0005; 0012
(2017/08/30)
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- PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
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Paragraph 0099
(2017/07/29)
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- Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)
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Page/Page column 46; 47
(2017/07/31)
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- BICYCLOR [2.2.1] HEPT-7-YLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASES AND CONDITIONS IN WHICH M3 MUSCARINIC RECEPTOR ACTIVITY AND BETA-ADRENERGIC ACTIVITY ARE IMPLICATED
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The present invention relates to compounds of formula (I) having muscarinic M3 receptor and β-adrenergic receptor modulating activity; wherein R1, R2, R3 and X are as defined herein.
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Page/Page column 101
(2009/01/24)
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- 8-OXOADENINE COMPOUND
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An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral siseases and cancers, which is represented by the following formula (1): , wherein A is a group of a formula represented by the formula (2): , wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0-2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.
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Page/Page column 123
(2010/11/24)
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- TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues
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N3-Substituted coformycin aglycon analogues with improved AMP deaminase (AMPDA) inhibitory potency are described. Replacement of the 5-carboxypentyl substituent in the lead AMPDA inhibitor 3-(5-carboxypentyl)-3,6,7,8- tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (2) described in the previous article with various carboxyarylalkyl groups resulted in compounds with 10- 100-fold improved AMPDA inhibitory potencies. The optimal N3 substituent had m-carboxyphenyl with a two-carbon alkyl tether. For example, 3-[2-(3-carboxy- 5-ethylphenyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (43g) inhibited human AMPDA with a K(i) = 0.06 μM. The compounds within the series also exhibited > 1000-fold specificity for AMPDA relative to adenosine deaminase.
- Kasibhatla, Srinivas Rao,Bookser, Brett C.,Probst, Gary,Appleman, James R.,Erion, Mark D.
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p. 1508 - 1518
(2007/10/03)
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