cas 158681-13-1, Rimonabant hydrochloride | Articles data

Articles about 158681-13-1Total 12 be found

"Photo-Rimonabant": Synthesis and Biological Evaluation of Novel Photoswitchable Molecules Derived from Rimonabant Lead to a Highly Selective and Nanomolar " Cis-On" CB1R Antagonist
Human cannabinoid receptor type 1 (hCB1R) plays important roles in the regulation of appetite and development of addictive behaviors. Herein, we describe the design, synthesis, photocharacterization, molecular docking, and in vitro characterization of "photo-rimonabant", i.e., azo-derivatives of the selective hCB1R antagonist SR1411716A (rimonabant). By applying azo-extension strategies, we yielded compound 16a, which shows marked affinity for CB1R (Ki (cis form) = 29 nM), whose potency increases by illumination with ultraviolet light (CB1R Kitrans/cis ratio = 15.3). Through radioligand binding, calcium mobilization, and cell luminescence assays, we established that 16a is highly selective for hCB1R over hCB2R. These selective antagonists can be valuable molecular tools for optical modulation of CBRs and better understanding of disorders associated with the endocannabinoid system.
Rodríguez-Soacha, Diego A.,Fender, Julia,Ramírez, Yesid A.,Collado, Juan Antonio,Mu?oz, Eduardo,Maitra, Rangan,Sotriffer, Christoph,Lorenz, Kristina,Decker, Michael
p. 1632 - 1647
(2021/05/10)

Preparation method for rimonabant hydrochloride
The invention discloses a preparation method for rimonabant hydrochloride, belonging to the field of chemical pharmacy. An ester is used as an initial raw material and undergoes hydrolysis, condensation and salt formation so as to obtain the rimonabant hydrochloride. The preparation method is simple and convenient to operate and has low cost and high yield.
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Paragraph 0014

(2016/10/17)

POLYMORPHIC FORM OF RIMONABANT HYDROCHLORIDE AND PROCESSES FOR PREPARATION THEREOF
Provided is a crystalline form of Rimonabant hydrochloride, processes for its preparation and pharmaceutical compositions containing such crystalline form of Rimonabant hydrochloride.
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(2008/12/08)

PROCESS FOR PREPARATION OF PYRAZOLE DERIVATIVES
A process for preparation of Pyrazole derivatives adapted for one pot reaction involving the use of a pyclizing agent and involving the step of amidation in the presence of a catalyst. The steps for isolation and purification of found Pyrazole derivatives are also disclosed.
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(2008/12/08)

Preparation of crystalline polymorphs of rimonabant hydrochloride
This invention relates to three novel solvate forms of crystalline rimonabant hydrochloride (Form A, B, and C) and two novel crystalline polymorphic forms of rimonabant hydrochloride anhydrous (Form D and E), to processes for preparing such polymorphic forms or solvate forms, to pharmaceutical compositions containing them and to the use of them in medicine.
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Page/Page column 11

(2008/06/13)

POLYMORPHS OF RIMONABANT
Crystalline form C of rimonabant and amorphous rimonabant, processes for their preparation and pharmaceutical compositions thereof.
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(2008/06/13)

POLYMORPHS OF RIMONABANT
Crystalline form C of rimonabant and amorphous rimonabant, processes for their preparation and pharmaceutical compositions thereof.
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Page/Page column 12-13

(2008/06/13)

IMPROVED PROCESS FOR RIMONABANT
The present invention provides an improved and commercially viable process for the preparation of rimonabant substantially free of amide impurity, namely 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxamide and its pharmaceutically acceptable acid addition salts thereof. Thus, for example, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxylic acid chloride is reacted with 1-minopiperidine in the presence of a base and optionally using a phase transfer catalyst such as tetra-butylammonium bromide in a biphasic reaction medium containing water and a water-immiscible solvent to obtain pure rimonabant.
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Page/Page column 7

(2008/06/13)

POLYMORPHIC FORMS OF RIMONABANT
Polymorphic crystalline Forms III, IV, V, and VI of rimonabant, amorphous rimonabant, and amorphous rimonabant in an intimate dispersion with a pharmaceutically acceptable carrier.
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Page/Page column 20-21

(2008/06/13)

AN AMORPHOUS AND THREE CRYSTALLINE FORMS OF RIMONABANT HYDROCHLORIDE
The present invention describes novel forms of Rimonabant hydrochloride, processes for their preparation and pharmaceutical compositions containing them. Thus, the present invention discloses three new crystalline forms designated as Form II, Form III and Form IV of Rimonabant hydrochloride and novel amorphous forms of the salt.
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(2008/06/13)