Author "Hortala, Laurent"

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1. Oral delivery of diabetes peptides — Comparing standard formulations incorporating functional excipients and nanotechnologies in the translational context [2016]

  • Lakkireddy, Harivardhan Reddy, Urmann, Matthias, Besenius, Melissa, Werner, Ulrich, Haack, Torsten, Brun, Priscilla, Alié, Jean, Illel, Brigitte, Hortala, Laurent, Vogel, Rachel, and Bazile, Didier
  • In Advanced Drug Delivery Reviews 15 November 2016 106 Part B:196-222

2. Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif [2010]

  • HORTALA, Laurent, RINALDI-CARMONA, Murielle, CONGY, Christian, BOULU, Laurent, SADOUN, Freddy, FABRE, Gérard, FINANCE, Olivier, and BARTH, Francis
  • Bioorganic & medicinal chemistry letters (Print). 20(15):4573-4577
Subjects
Biochemistry, molecular biology, biophysics, Biochimie, biologie moléculaire, biophysique, Pharmacology drugs, Pharmacologie, galénique, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Neuropharmacologie, Neuropharmacology, Neuromédiateurs. Neurotransmission. Récepteurs, Neurotransmitters. Neurotransmission. Receptors, Divers, Miscellaneous, Chlore Composé organique, Chlorine Organic compounds, Cloro Compuesto orgánico, Fluor Composé organique, Fluorine Organic compounds, Fluor Compuesto orgánico, Mammalia, Rodentia, Vertebrata, Affinité, Affinity, Afinidad, Animal, Antagoniste, Antagonist, Antagonista, Dérivé du benzène, Benzene derivatives, Benceno derivado, Dérivé du pyrrole, Pyrrole derivatives, Pirrol derivado, Hétérocycle azote, Nitrogen heterocycle, Heterociclo nitrógeno, In vitro, In vivo, Rat, Rata, Relation structure activité, Structure activity relation, Relación estructura actividad, Récepteur cannabinoïde CB1, CB1 cannabinoid receptor, Receptor canabinoide CB1, Sulfonamide, Sulfonamida, Synthèse chimique, Chemical synthesis, Síntesis química, Transit digestif, Digestive transit, Transito digestivo, Voie orale, Oral administration, Vía oral, Pipéridine-4-carboxamide(1-[5-(4-chlorophényl)-4-(2,4-dichlorophényl)-1-(3-[mésylamino]propyl)pyrrole-2-carbonyl]-4-[4,4-difluoropipéridino]), CB1 antagonist, Peripherally-restricted cannabinoid antagonist, and Pyrrole
Abstract
A new series of 2,3-diarylpyrroles have been prepared and evaluated as CB1 antagonists. Modulation of the topological polar surface area allowed the identification of high affinity peripherally-restricted CB1 antagonists. Compound 11, obtained after further optimization of the metabolic profile displayed very low brain penetration, yet was able to reverse CP55940-induced gastrointestinal transit inhibition following oral administration.

3. Pyrrole derivatives, preparation thereof and therapeutic use thereof [2011]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention relates to compounds having the formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7 and R8 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.

4. Pyrrole derivatives, intermediates therefor, preparation and therapeutic use thereof [2011]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention concerns compounds of formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.

5. Derivatives of 4,5-diarylpyrrole, preparation method thereof and use of same in therapeutics [2009]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention relates to compounds having formula (I): [chemical expression included] Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.

6. PYRROLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF [2009]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention relates to compounds having the formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7 and R9 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.

7. 1,5-diarylpyrrole derivatives, preparation method thereof and application of same in therapeutics [2009]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention relates to compounds having formula (I): [chemical expression included] Wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.

8. PYRROLE DERIVATIVES, INTERMEDIATES THEREFOR, PREPARATION AND THERAPEUTIC USE THEREOF [2008]

  • BARTH, Francis, CONGY, Christian, HORTALA, Laurent, and RINALDI-CARMONA, Murielle
Abstract
The invention concerns compounds of formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.

9. DERIVATIVES OF 4,5-DIARYLPYRROLE, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS [2008]

  • BARTH, Francis, CONGY, Christian, HORTALA, Laurent, and RINALDI-CARMONA, Murielle
Abstract
The invention relates to compounds having formula (I): [chemical expression included] Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.

10. Pyrrole derivatives, their preparation and their therapeutic use [2008]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention concerns compounds of formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.

11. Diphenylpyridine derivatives, preparation and therapeutic application thereof [2008]

  • Barth, Francis, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): [chemical expression included] where: R1 represents hydrogen or a (C1-C4)alkyl; R2 represents: a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1-C4)alkanoyl; NR10R11; a nonaromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4)alkyl; a nonaromatic (C11-C12) carbocycle unsubstituted or mono- or polysubstituted with (C1-C4)alkyl; a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4)alkyl; or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin-1-yl group; the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.

12. 1,5-DIARYLPYRROLE DERIVATIVES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS [2008]

  • BARTH, Francis, CONGY, Christian, HORTALA, Laurent, and RINALDI-CARMONA, Murielle
Abstract
The invention relates to compounds having formula (I): [chemical expression included] Wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.

13. PYRROLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE [2007]

  • Barth, Francis, Congy, Christian, Hortala, Laurent, and Rinaldi-Carmona, Murielle
Abstract
The invention concerns compounds of formula (I): [chemical expression included] Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.

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16. Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif [2010]

  • Hortala, Laurent, Rinaldi-Carmona, Murielle, Congy, Christian, Boulu, Laurent, Sadoun, Freddy, Fabre, Gérard, Finance, Olivier, and Barth, Francis
  • Bioorganic & Medicinal Chemistry Letters. Aug2010, Vol. 20 Issue 15, p4573-4577. 5p.
Subjects
DRUG design, CANNABINOIDS, DRUG receptors, ORAL drug administration, CHEMICAL inhibitors, PYRROLES, and METABOLISM
Abstract
Abstract: A new series of 2,3-diarylpyrroles have been prepared and evaluated as CB1 antagonists. Modulation of the topological polar surface area allowed the identification of high affinity peripherally-restricted CB1 antagonists. Compound 11, obtained after further optimization of the metabolic profile displayed very low brain penetration, yet was able to reverse CP55940-induced gastrointestinal transit inhibition following oral administration. [Copyright &y& Elsevier]

17. Acyl transfer of 8-acetoxy-2-oxazolinylquinoline assisted by hydrogen bonding formation [2002]

  • Hortala, Laurent, Moberg, Christina, Levacher, Vincent, Bourguignon, Jean, and Dupas, Georges
  • In Tetrahedron Letters 2002 43(6):1027-1029

18. Synthesis and antiproliferative activity of a cyclic analog of dolastatin 10 [1998]

  • Poncet, Joël, Hortala, Laurent, Busquet, Magali, Guéritte-Voegelein, Françoise, Thoret, Sylvie, Pierré, Alain, Atassi, Ghanem, and Jouin, Patrick
  • In Bioorganic & Medicinal Chemistry Letters 1998 8(20):2855-2858

19. Chiral ditopic receptors. Application to palladium-catalyzed allylic alkylation [2003]

  • Bourguignon, Jean, Bremberg, Ulf, Dupas, Georges, Hallman, Kristina, Hagberg, Lars, Hortala, Laurent, Levacher, Vincent, Lutsenko, Serghey, Macedo, Emmanuel, Moberg, Christina, Quéguiner, Guy, and Rahm, Fredrik
  • Tetrahedron. Nov2003, Vol. 59 Issue 48, p9583. 7p.
Subjects
PALLADIUM, HYDROCARBONS, ORGANIC compounds, and PYRIDINE
Abstract
Chiral pyridinooxazoline, quinolinooxazoline, bis(oxazolino)pyridine (pybox), and bisoxazoline (box) derivatives containing crown ether residues were prepared. Some of the ligands were assessed in substrate binding studies and in palladium catalyzed allylic alkylations. [Copyright &y& Elsevier]

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