13808-71-4Relevant academic research and scientific papers
Preparation method of pyrazole derivative (by machine translation)
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Paragraph 0121-0125, (2019/12/02)
The preparation method comprises the following steps: mixing an alkyne propyl alcohol derivative, a halogen source, an acid and a solvent, heating and reacting, and reacting to Meyer - Schuster generate the pyrazole derivative. Compared with the prior art, the preparation method disclosed by the invention has 91% the advantages of maximum yield, simple operation, mild conditions, high conversion rate, few byproducts and the like, and provides a brand-new synthetic method for construction of pyrazole compounds. (by machine translation)
Novel Compounds as Autotaxin Inhibitors and Pharmaceutical Compositions Comprising the Same
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Paragraph 1355-1356, (2018/05/17)
The present invention relates to a novel autotaxin inhibitor compound for preventing and treating disease or symptoms due to an increase in concentration of lysophosphatidic acid or activation of autotaxin. The present invention further relates to a pharmaceutical composition containing the same. The novel compound of the present invention is an autotaxin inhibitor which inhibits production of lysophosphatidic acid, and thus is useful for treating or preventing cardiovascular disease, cancer, metabolic disease, kidney disease, liver disease, inflammatory diseases, nervous disease, respiratory disease, desmoid disease, eye disease, cholestatic symptoms, other types of chronic pruritus or acute, or chronic rejection of transplanted organs.COPYRIGHT KIPO 2017
TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE & INFLAMMATORY DISEASES
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Page/Page column 66-67, (2008/06/13)
Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following (formula I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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Page/Page column 22, (2010/11/30)
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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Page 182, (2008/06/13)
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.
Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
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Page/Page column 88-89, (2010/02/06)
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
Process for preparing pyrazoles
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, (2008/06/13)
A process for preparing pyrazoles of the formula I in which R1,R2,R3 independently of one another are C1- to C20-alkyl, C3- to C8-cycloalkyl, or C7- to C20-aralkyl or aryl, unsubstituted or substituted by C1- to C4-alkyl, halogen and/or nitro, R1,R3 are additionally independently of one another hydrogen, by reacting a carbonyl compound of the formula R1-CH2-CO-R2, in which R1 and R2 are as defined above in the presence of a strong base with a) formic esters of the formula H-COOR4, in which R4 is C1- to C8-alkyl at from (-20) to 70 DEG C. and a pressure of from 1 to 50 bar or b) carbon monoxide at from 0 to 100 DEG C. and a pressure of from 1.5 to 150 bar and reacting the resulting intermediate, the hydrazines of the formula R3-NH-NH2, in which R3 is as defined above, and an inorganic or organic acid at from 0 to 90 DEG C. and a pressure of from 1 to 10 bar, which comprises filtering off or centrifuging off the intermediate, is described.
