919475-78-8Relevant academic research and scientific papers
Active substance combination for the treatment of diabetes
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Page/Page column 99, (2008/12/07)
The present invention relates to an active substance combination comprising at least one substituted pyrazoline compound and at least one drug, used to treat diabetes, a medicament comprising said active substance combination, a pharmaceutical formulation
Substituted pyrazoline for preventing weight gain
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Page/Page column 99, (2008/12/07)
The present invention relates to an active substance combination comprising at least one substituted pyrazoline compound and at least one drug, known to produce weight-gain as a side effect, a medicament comprising said active substance combination, a pharmaceutical formulation comprising said active substance combination and the use of said active substance combination for the manufacture of a medicament.
HETEROCYCLYL-SUBSTITUTED PYRAZOLINE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS
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Page/Page column 127; 132; 134, (2008/06/13)
The present invention relates to heterocyclyl-substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
Heterocyclyl-substituted pyrazoline compounds, their preparation and use as medicaments
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Page/Page column 51, (2008/06/13)
The present invention relates to heterocyclyl-substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: Synthesis, biological evaluation, and molecular modeling in the homology model
Srivastava, Brijesh Kumar,Joharapurkar, Amit,Raval, Saurin,Patel, Jayendra Z.,Soni, Rina,Raval, Preeti,Gite, Archana,Goswami, Amitgiri,Sadhwani, Nisha,Gandhi, Neha,Patel, Harilal,Mishra, Bhupendra,Solanki, Manish,Pandey, Bipin,Jain, Mukul R.,Patel, Pankaj R.
, p. 5951 - 5966 (2008/04/12)
A number of analogues of diaryl dihydropyrazole-3-carboxamides have been synthesized. Their activities were evaluated for appetite suppression and body weight reduction in animal models. Depending on the chemical modification of the selected dihydropyrazole scaffold, the lead compounds - the bisulfate salt of (±)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid morpholin-4-ylamide 26 and the bisulfate salt of (-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid morpholin-4-ylamide 30-showed significant body weight reduction in vivo, which is attributed to their CB1 antagonistic activity and exhibited a favorable pharmacokinetic profile. The molecular modeling studies also showed interactions of two isomers of (±)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide 9 with CB1 receptor in the homology model similar to those of N-piperidino-5-(4- chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole-carboxamide (rimonabant) 1 and 4S-(-)-3-(4-chlorophenyl)-N-methyl-N′-[(4-chlorophenyl) -sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine (SLV-319) 2.
