Sanofi

Adir Et Compagnie

Societe Anonyme Sanofi

Cnrs

Elf Sanofi

Virbac Corporation

Via Pharmaceuticals, Inc.

Université Louis Pasteur

Jean-Jacques Bourguignon

Camille G Wermuth

Paul Worms

Camille-Georges Wermuth

Roger Brodin

Robert Boigegrain

Dominique Olliero

Michele Calas

Marie-Laure Ancelin

Jean P Kan

Pierre Renard

Gerard Adam

Kathleen Biziere

Michelle Devissaguet

Catherine Thollon

Louis Giral

Jean-Paul Kan

Jean-Pierre Chambon

Henri Joseph Vial

Martine Schmitt

Henri Vial

Alain Lombet

Valerie Vidal

Eric Rubi

Yan Lagouge

Claire Lugnier

Eveline Klotz

Jean-Paul Macher

Pierre Raboisson

Dominique Schultz

De La Renaud

Serge Gobaille

Jean-Francois R De La Faverie

Michel Maitre

Isabelle Morin

Evelyne Klotz

The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates. The inventive compounds more particularly correspond to general formula (I): 

Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof

The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A', identical or different, are respectively either a group A1 and A&#x2032;1 of formula (1) wherein n=2 to 4; R&#x2032;1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3. B and B&#x2032;, identical or different, represent respectively either the group B1 and B&#x2032;1, if A and A&#x2032; respectively represent A1, A&#x2032;1, B1, B&#x2032;1 representing a group R1 which has the same definition as R&#x2032;1 above, but cannot be a hydrogen atom; or respectively the groups B2 and B&#x2032;2, if A and A&#x2032; represent A2, B2 or B&#x2032;2 being the group R1 as defined above, or a group of formula (2) wherein &#x2014;Ra is RS&#x2014; or RCO&#x2014;, wherein R is a C1-C6 alkyl, substituted if required, a phenyl or benzyl, wherein the phenyl is substituted if required, the latter being optionally substituted; R2 is hydrogen, C1-C5 alkyl, or a &#x2014;CH2-COO&#x2014; (C1-C5)alkyl group; and R3 is hydrogen, C1-C5 alkyl or alkenyl, substituted if required, a phosphate, an alkoxy wherein the alkyl is a C1-C3 alkyl, or aryloxy; or an alkyl (or arylcarbonyloxy; or R2 and R3 form together a cycle with 5 or 6 C; R and R3 can be bound to form a cycle. &#xb1; represents: either a single bond when A and A&#x2032; represent A1 and A&#x2032;1: or when A and A&#x2032; represent A2, and B2 and B&#x2032;2 Represent (3) either, when A and A&#x2032; are &#x2014;CHO or &#x2014;COCH3 and B2 and B&#x2032;2 are R1, a group of formula (4) or a group of formula (5) wherein (a) represents a bond towards Z and (b) a bond towards the nitrogen atom. Z is a C9-C21 alkyl, if required with insertion of one or several bonds, and/or one or several heteroatoms O and/or S and/or several aromatic cycles, and the pharmaceutically acceptable salts of said compounds. Said precursors and cyclized thiazolium derivatives are useful as antiparasitic medicines in particular antimalarial and antibabesiosis.

Quaternary bis-ammonium salt precursors and their uses as prodrugs having an antiparasitic activity

Bis(2-aminopyridine)s, preparation method therefor and use thereof for

The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.

Pyridazine derivatives

The invention relates to 3-aminopyridazine derivatives. These compounds have the formula ##STR1## in which: R.sub.V is a linear or branched C.sub.1 -C.sub.4 alkyl group;

3-(N-azabicycloalkyl)aminopyridazine derivatives and pharmaceutical

A compound having an aryltriazine structure selected from those of formula (I): ##STR1## for which the meaning of the substituents Ar, R.sub.1, R.sub.5, R.sub.6, and R.sub.6 ' is given in the description. The compound of the invention is useful as medicinal product for disorders associated with a cholinergic dysfunction.

Compounds having an aryltriazine structure

New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;

Imidazo [1,2-c] quinazoline compounds

The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors. These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.

Tricyclic cholinergic receptor agonists

The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them. These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;

Novel tricyclic derivatives which are agonists of cholinergic receptors,

The present invention relates to imidazo[1,2-b]-pyridazines having the formula: ##STR1## in which: R.sub.1 represents hydrogen, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.1 -C.sub.4 alkyl group occupying one of the free positions of the benzene ring; R.sub.2 represents hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; and R.sub.4 R.sub.5 represent hydrogen or a C.sub.1 -C.sub.4 alkyl group, or R.sub.4 and R.sub.5 form, together with the nitrogen atom to which they are bonded, a 5-membered or 6-membered heterocycle optionally containing a second heteroatom. Application: drugs, especially for the treatment of cortical cholinergic deficiencies.

Imidazo[1,2-]pyridazines for cortical cholinergic deficiencies

The invention relates to 1,2,4-triazolo [4,3-b]pyridazines substituted in the 7-position of formula: ##STR1## in which R represents hydrogen, a lower alkyl group, a phenyl group, a chlorophenyl group or a benzyl group and R.sub.1 represents a phenyl, halogenophenyl, trifluoromethylphenyl, lower alkyl-phenyl or lower alkoxy-phenyl group or a phenyl-lower alkyl group, or one of its pharmaceutically acceptable salts. Said compounds antagonize the effects of benzodiazepines and therefore are useful as antidotes in the abuse of benzodiazepines and compounds acting on benzodiazepine receptors.

Triazolo [3,4-b]pyridazines, process for their preparation and

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Hipsheim, France

Jean-Jacques Bourguignon