- Pyrazole alcohol compound, pharmaceutical composition thereof and application thereof to drugs
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The invention discloses a 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound, a tautomer thereof, a pharmaceutical composition thereof and application thereof to drugs. The 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound has double effects of resisting platelet aggregation and protecting nerve cells, and comprises a compound as shown in the formula (I), a tautomer (Ia) thereof, or a stereoisomer, a geometrical isomer, a hydrate or a solvate thereof, or a pharmaceutically acceptable salt or prodrug as shown in the description. The 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound and the pharmaceutical composition thereof provided by the invention can be used for preparing drugs for prevention and/or treatment and/or auxiliary treatment of cerebral apoplexy, cardiovascular and cerebrovascular diseases, senile dementia and complications thereof caused by thrombosis and excessive free radicals.
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Paragraph 0128; 0139
(2018/10/19)
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- A novel synthetic method for β-keto esters
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A novel synthetic method for the preparation of β-keto esters has been developed. α-Phenylseleno acetate was treated with LDA to produce a selenium-stabilised carbanion, which reacted with aldehydes, followed by selenoxide syn-elimination, to give β-keto esters.
- Qian, Hao,Ge, Chunrong,Huang, Xian
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p. 160 - 161
(2008/02/03)
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- Preparation of polystyrene-supported α-seleno acetate and application to solid-phase synthesis of β-keto esters
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A novel polystyrene-supported α-seleno acetate has been developed. This novel resin was treated with LDA to produce a selenium-stabilized carbanion, which reacted with aldehydes, followed by selenoxide syn-elimination to give β-keto esters. Georg Thieme Verlag Stuttgart.
- Qian, Hao,Huang, Xian
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p. 1547 - 1548
(2007/10/03)
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- Ether linked macrolides useful for the treatment of microbial infections
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The present invention relates to 14- or 15-membered macrolides substituted at the 4″ position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or top
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Page/Page column 15-16
(2008/06/13)
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- 4" AMINO LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS
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The present invention relates to 15-membered macrolides substituted at the 4" position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical mi
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Page/Page column 34; 35
(2008/06/13)
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- ESTER LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS
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The present invention relates to 14- or 15-membered macrolides substituted at the 4” position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or top
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Page/Page column 41-42
(2008/06/13)
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- CARBAMATE LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS
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The present invention relates to 14- or 15-membered macrolides substituted at the 4" position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.
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Page/Page column 35-36
(2010/02/14)
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- Synthesis and Antibacterial Activity of Some Novel 1-Substituted 1,4-Dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic Acids. Potent Antistaphylococcal Agents
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The palladium-catalyzed coupling of 3- and 4-(trialkylstannyl)pyridines with 7-bromo or 7-chloro 1-substituted 1,4-dihydro-4-oxo-3-quinolinecarboxylates has provided access to the corresponding 1-substituted 1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarbox
- Reuman, Michael,Daum, Sol J.,Singh, Baldev,Wentland, Mark P.,Perni, Robert B.,et al.
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p. 2531 - 2540
(2007/10/02)
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- A process for producing a substituted benzoyl fatty acid derivative
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A process for producing a substituted benzoyl fatty acid derivative of the general formula (I) which is represented by the following reaction formula: [wherein R is H or -OC(R3)(R4)-R5(wherein each of R3and R4is H or a C1-6alkyl group, R5is a cyano group, -CON(R6)R7(wherein each of R6and R7is H or a C1-6alkyl group) or -COAR8(wherein R8is H or a C1-6alkyl group, and A is O or S)), each of R1and R2is H or a C1-6alkyl group, each of X's is a halogen atom, n is an integer of 1 to 3, Hal is a halogen atom, and R9is a C1-6alkyl group, an unsubstituted phenyl group, or a substituted phenyl group having one or more substituents selected from the group consisting of halogen atoms, C1-6alkyl groups, halo-C1-6alkyl groups, C1-6alkoxy groups, halo-C1-6alkoxy groups, C1-6alkylthio groups and halo-C1-6alkylthio groups] and makes it possible to produce the substituted benzoyl fatty acid derivative in high yield from inexpensive materials in the presense of a reusable catalyst.
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- Synthesis and pharmacological evaluation of a new series of substituted benzoyl-γ-butyrolactone derivatives
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A series of substituted benzoyl-γ-butyrolactones (1-3) has been synthesized and tested for their ability to affect central dopaminergic and GABAergic function in comparison to γ-butyrolactone (GBL).Similarly to GBL, α-, β- and γ-substituted GBLs 1-3 with one or more chlorine on the phenyl ring were found to induce central depressant effects in rats, though at different degrees.However, the test compounds modified dopamine (DA) metabolism in rat striatum differently from GBL.In fact, whereas GBL increased both DA and dihydroxyphenylacetic acid (DOPAC) content, GBL derivatives 1-3 increased DA levels, but reduced the DOPAC concentration.Moreover, some of them, unlike GBL, effectively antagonized pentylenetetrazole (PTZ)-induced seizures in mice.In particular, α-3,5-dichlorobenzoyl-GBL (1g) was effective at a dose as low a 36 mg/kg in decressing the number of animals having convulsions.However, in vitro addition and in vivo administration of the test compounds failed to modify -t-butylbicyclophosphorothionate (-TBPS) binding, which is a very sensitive tool for revealing changes in the GABAergic function. γ-butyrolactone / benzoyl-γ-butyrolactone / dopamine / anticonvulsant effect
- Cignarella, G.,Barlocco, D.,Pocar, D.,Clerici, F.,Curzu, M. M.,et al.
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p. 721 - 726
(2007/10/03)
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- 2-Amino-4-substituted-thiazolecarboxylic acids and their derivatives
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2-Amino-4-substituted-5-thiazolecarboxylic acids and derivatives thereof, are intermediates for the preparation of 2-substituted-4-substituted-5-thiazolecarboxylic acid derivatives which are herbicidal safeners.
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