- INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Compounds and pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth.
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Page/Page column 41
(2020/06/01)
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- Preparation technology of 3-cyclopropyl-1-methyl-1H-pyrazole-4-formaldehyde
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The invention provides a preparation technology of 3-cyclopropyl-1-methyl-1H-pyrazole-4-formaldehyde (compound 1). The preparation technology comprises the following steps: 1) 1-cyclopropyl methyl ketone reacts with N,N-dimethylformamide dimethylacetal in N,N-dimethylformamide solvent at a proper temperature to obtain a compound 2; 2) the compound 2 reacts with hydrazine hydrate react in an alcohol solvent at a reflux temperature to obtain a compound 3; 3) the compound 3 reacts with a methylation reagent at room temperature to obtain a compound 4; 4) the compound 3 reacts with N,N-dimethylformamide in a halohydrocarbon solvent in an ice-water bath, to obtain the 3-cyclopropyl-1-methyl-1H-pyrazole-4-formaldehyde (compound 1). The synthesis route is shown in the description. According to thepreparation technology provided by the invention, the adopted raw materials, reagents and solvents are conventional synthetic reagents which are cheap and easily available; the reaction conditions inall steps are mild, the aftertreatment is simple, the reaction yield is relatively high, and the product purity is high. Overall preparation cost of the product is low, and the requirements of industrial production are met.
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Paragraph 0014; 0027-0028
(2019/01/14)
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- PYRAZOLE DERIVATIVES
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Provided herein are compounds of the formula I: as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.
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Page/Page column 85; 86
(2017/08/01)
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- PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
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Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the com
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Page/Page column 84
(2012/05/31)
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- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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- Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS. The compounds of the invention for the general Formula I: wherein: Z is Q is selected from the group consisting of: —W— is
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Page/Page column 89
(2010/02/06)
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- Generation and intermolecular capture of cyclopropylacyl radicals
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(Chemical Equation Presented) Cyclopropylacyl radicals derived from S-cyclopropylacyl xanthates (dithiocarbonates) undergo intermolecular additions to olefins without loss of CO or ring opening. In the presence of a phenyl ring on carbon C-1 of the cyclopropane ring, loss can be made to occur in the absence of an olefinic trap. The adducts from the cyclopropylacyl radical additions are easily converted into enones by base-induced β-elimination of the xanthate group.
- Heinrich, Markus R.,Zard, Samir Z.
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p. 4969 - 4972
(2007/10/03)
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