The invention relates to compounds of the formula (I) in which Ar1 is an aryl, heteroaryl or heterocyclic group; Ar2 is an aryl or heteroaryl group of the formula (Ia) in which A is a nitrogen or carbon atom optionally substituted by M4; and M1, M2, M3 or M4, are identical or different and represent a hydrogen atom, a halogen atom, a (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, cyano, (C1-C6)haloalkyl, (C1-C6)haloalkoxy, amino, N-(C1-C6)alkylamino, N,N-(C1-C6)dialkylamino, amino(C1-C6)alkyl, N-(C1-C6)alkylamino(C1-C6)alkyl or N,N-(C1-C6)dialkylamino(C1-C6)alkyl radical; Y is an oxgen atom or a NR group; R is a hydrogen atom, a (C1-C6) alkyl, (C1-C6)alkylcarbonyl group; n is an integer between 4 and 6; and D is a carbon or nitrogen atom. The invention also relates to their pharmaceutically acceptable salts, to a method for preparing the same, to pharmaceutical compositions containing the same and to their use as anti-neoplasic agents and/or cell proliferation inhibitors..
C07D 211/08 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
2.
HETEROCYCLIC COMPOUNDS USED AS ANTI-NEOPLASIC AGENTS OR CELL PROLIFERATION INHIBITORS
The invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salts thereof, in which : A is an alkyl or cycloalkyl group, an aryl(C1-C6)alkyl, an aryl, a heteroaryl or a heterocycle; X is a nitrogen atom, a CR5 group in which R5 is hydrogen atom, an alkyl group, a N-(C1- C6)alkylaminoalkyl group, a N,N-(C1-C6)dialkylaminoalkyl group, a hydroxy(C1-C6)alkyl group, a alkoxy(C1-C6)alkyl group or a carbonylaminoalkyl group; Y is a CH2 group, an oxygen atom, a sulphur atom, a sulphoxide group, a sulphonyl group, a CO group or a NR6 group in which R6 is a hydrogen atom, an alkyl group or a (C1-C6)alkylcarbonyle group; B is a (C2- C6)alkylene group; and D is a carbon atom or a nitrogen atom. The invention also relates to methods for preparing the same, to pharmaceutical compositions containing the same and to their use as anti-neoplasic agents and/or cell proliferation inhibitors.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
3.
INDOLE, BENZIMIDAZOLE OR BENZOTRIAZOLE DERIVATIVES INCLUDING A PIPERIDINE OR PIPERAZINE CORE AS ANTI-NEOPLASIC AGENTS OR CELL PROLIFERATION INHIBITORS
The invention relates to compounds of the formula (I), as well as to their pharmaceutically acceptable salts, in which: Ar1 is an aryl or heteroaryl group, each optionally substituted; X and Y are identical or different and represent a nitrogen atom of a CH group; n is an integer between 4 and 6; D is a carbon or nitrogen atom. The invention also relates to a manufacturing method, to pharmaceutical compositions containing the same, and to their use as anti-neoplasic agents and/or cell proliferation inhibitors.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The invention relates to processes for preparing desmethylsertraline, or a pharmaceutically acceptable salt thereof, from (+/-) sertraline or from a cis/trans or cis 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine mixture.
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
C07C 209/82 - PurificationSeparationStabilisationUse of additives
C07C 209/24 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds
C07C 209/52 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of imines or imino-ethers
5.
COMBINATION PRODUCT CONTAINING N-DESMETHYLSERTRALINE, OR A SALT THEREOF, AND AN ANTINEOPLASTIC AGENT FOR THE TREATMENT OF CANCER
The invention relates to a product comprising N-desmethylsertraline ((1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine), or a pharmaceutically acceptable salt thereof, and at least one antineoplastic agent, as a combination product for simultaneous, separate or sequential use in anticancer therapy.
A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
A61K 33/14 - Alkali metal chloridesAlkaline earth metal chlorides
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
6.
IN VITRO ASSAY BASED ON cAMP LEVELS MODULATED BY Gi-COUPLED RECEPTORS
The present invention relates to a reliable and effective in vitro assay based on cAMP levels modulated by Gi-coupled receptors expressed in a selected cell for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor.
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