Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

4, 5-Dihydro-Thiazo-2-Ylamine Derivatives and their Use as NO-Synthase Inhibitors.

The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (1) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (1) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved arbnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2) ...

2-Aminothiazoline derivatives and their use as no-synthase inhibitors.

The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, -CH-R3, -CH2-S-R4 or phenyl radical substituted by a nitro or NH-C(=NH)CH3 radical; or R1 is an alkyl radical and R2 is a hydrogen atom; R3 is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R4 represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.

IMIDAZO (1,2-A>INDENO (1,2-E>PYRAZIN-2-CARBONSÄUR of DERIVATIVES, YOUR PRODUCTION AND IT CONTAINING DRUGS

2-AMINOTHIAZOLINDERIVATE AND YOUR USE AS NO-SYNTHASE INHIBITORS

IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZIN-4-ONDERIVATE AND THESE CONTAINING PHARMACEUTICAL PREPARATIONS

Tryptamine derivatives, preparation thereof and medicaments containing them

4,5-dihydro-thiazo-2-ylamine derivatives and their use as no-synthase inhibitors

Indazoles substituted with an anti-cancerous activity

INDAZOLES SUBSTITUTED WITH AN ANTI-CANCEROUS ACTIVITY

SpiroÝheterocycle-imidazoÝ1,2-a¨indenoÝ1,2-e¨pyrazine¨-4'-on es, preparation thereof and drugs containing same

Derived from 1,2,4-triazolo (4,3-a) pyrazine-4-one, their preparation and drugs the container

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle R, R1 et R2 sont tels que définis dans la description, leurs sels, leur préparation et les médicaments les contenant.

Medicaments containing derivatives of 7:00-imidazol [1,2-a] pyrazin-8-one, the novel compounds and [...]

Médicaments contenant en tant que principe actif au moins un composé de formule: (CF DESSIN DANS BOPI) dans laquelle R1 représente un atome d'hydrogène ou un radical alkyle ou phényle, R2 représente (a) un radical phényle, (b) un radical phényle substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy, polyfluoroalkyle, polyfluoroalcoxy, phényle, nitro ou cyano, (c) un radical naphtyle, (d) un radical naphtyle substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy, polyfluoroalkyle, polyfluoroalcoxy, phényle, nitro ou cyano, (e) un radical 2-, 3- ou 4-pyridyle, (f) un radical 2-, 3- ou 4-pyridyle substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy, polyfluoroalkyle, poly, fluoroalcoxy, phényle, nitro ou cyano, (g) un radical 2- ou 3-furyle, (h) un radical 2- ou 3-furyle substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy, polyfluoroalkyle, polyfluoroalcoxy, phényle, nitro ou cyano ou un sel d'un tel composé, les composés de formule (1) nouveaux et leur préparation. Medicines containing as active principle at least one compound of formula: (CF DRAWING IN BOPI) in which R1 represents a hydrogen atom or an alkyl or phenyl radical, R2 represents (a) a phenyl radical, (b) a radical phenyl substituted with one or more substituents chosen from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals, (c) a naphthyl radical, (d) a naphthyl radical substituted by one or more substituents chosen from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals, (e) a 2-, 3- or 4-pyridyl radical, (f) a 2-, 3- or 4-pyridyl substituted by one or more substituents chosen from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, poly, fluoroalkoxy, phenyl, ...

5H-INDENO (1,2-B>PYRAZIN-2,3-DION-DERIVATE ANTAGONIST of the AMPA AND NMDA RECEPTORS

Derivatives of 5h,10h-imidazoÝ1,2-a¨indenoÝ1,2-e¨pyrazine-4-one, preparation thereof and medicaments containing them

5h,10h-imidazo{1,2-a}indeno{1,2-e}pyrazine-4-one derivatives, preparation thereof and drugs containing same

NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS

L'invention concerne les nouveaux produits de formule (I): dans laquelle : Ra représente H, HaI, aryle ou hétéroaryle éventuellement substitués; Rb représente H, Rc, -COORc,-CO-Rc ou -CO-NRcRd; avec Rc représente alkyle, cycloalkyle, hétérocycloalkyle, aryle et hétéroaryle, tous éventuellement substitués; Rd représente H, alk ou cycloalkyle; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET. The invention relates to novel products of formula (I): in which: Ra represents H, HaI, aryl or optionally substituted heteroaryl; Rb is H, Rc, -COORc, -CO-Rc or -CO-NRcRd; with Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all isomeric forms and salts, as medicaments especially as MET inhibitors.

DERIVATIVES OF 6-(6-O-CYCLOALKYL OR 6-NH-CYCLOALKYL-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS

L'invention concerne les nouveaux produits de formule (I) dans laquelle - - - - représente une liaison simple ou double; Ra représente -O-cycloalkyle ou -NH-cycloalkyle; X représente S, SO ou SO2, A représente NH ou S; W représente H, alkyle ou COR avec R représente cycloalkyle; alkyle; alcoxy; O-phényle; -O-(CH2)n-phényle avec n= 1 à 4; ou NR1 R2 avec R1 représente H ou alk et R2 représente H, cycloalkyle, hétérocycloalkyle, ou alkyle; ou bien R1, R2 forment avec N un cycle renfermant éventuellement O, S, N et/ou NH; tous ces radicaux étant éventuellement substitués; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET. The invention relates to novel products of formula (I) wherein - - - - represents a single or double bond; Ra represents -O-cycloalkyl or -NH-cycloalkyl; X is S, SO or SO 2, A is NH or S; W is H, alkyl or COR with R is cycloalkyl; alkyl; alkoxy; O-phenyl; -O- (CH 2) n-phenyl with n = 1 to 4; or NR1 R2 with R1 is H or alk and R2 is H, cycloalkyl, heterocycloalkyl, or alkyl; or R1, R2 together with N form a ring optionally containing O, S, N and / or NH; all these radicals being optionally substituted; these products being in all isomeric forms and salts, as medicaments especially as MET inhibitors.

2H-1,2,4-BENZOTHIADIAZINE-1,1-DIOXIDE-3-CARBOXYLIC ACID DERIVATIVES USED FOR PREPARING THERAPEUTIC COMPOUNDS; NEW PRODUCTS OBTAINED; PROCESS FOR PREPARING THEM AND THERAPEUTIC AGENTS CONTAINING THE SAME

... 2130095 9321171 Application de dérivés d'acide 2H-1,2,4-benzothiadiazine-1,1-dioxyde-3-carboxylique de formule (I), un sel d'un tel composé ou un précurseur d'un tel composé à la préparation de médicaments antagonistes du récepteur NMDA et/ou du récepteur AMPA, les nouveaux composés de formule (I), leur préparation et les médicaments les contenant.

3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE-1,1-DIOXIDE-3-CARBOXYLIC ACID DERIVATIVES; PROCESS FOR PREPARING THE SAME AND THERAPEUTIC AGENTS CONTAINING THEM

Compounds of formula (I), wherein R is (a) a hydrogen atom, (b) an alkyl radical, (c) an allyl radical, (d) a phenyl radical, (e) a 2-or-3-pyridyl alkyl radical, (f) a 2-quinolylalkyl radical, (g) a naphthylalkyl radical, (h) a cycloalkylalkyl radical, (i) a 2H-3-naphtho[1,8-cd]isothiazol-2-yl-1,1-dioxide)alkyl radical, (j) a (5,6-dihydro 1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolyl-2,2-dioxide)alkyl, (k) an -alk-CO-R5 radical, (l) an -alk-R6-R7 radical, (m) a 4-phenylpirerazinyl-alkyl radical wherein the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl or alkoxy radicals, (n) a 10-phenothiazinylalkyl radical (o) a (10-alkyl-2-phenothiazinyl)alkyl radical, (p) a 3-indolylalkyl radical, (q) a phenylalkyloxy radical, (r) a 1-phenylalkyl-4-piperidyl radical, (s) a 2-thienylalkyl radical, or (t) a phenylalkyl radical wherein the phenyl is unsubstituted or substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, amino, nitro, cyano, phenyl, vinyl, polyfluoroalkoxy, alkoxycarbonyl, carboxy, phenylalkyloxy, phenylalkyl, benzoylamino, phenylcarbonyl and phenoxy radicals in which the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy or polyfluoroalkyl radicals; R1 is a carboxy, alkoxycarbonyl, tetrazolyl, -CO-NH2, -CO-NH-alk, -CO-N(alk)2, -CO-NHOH, -CO-N(alk)OH, -CO-NH-O-R8, -CO-N(alk)-OR8 or a group which is convertible in vivo into a carboxy radical; each of R2, R3 and R4, which are the same or different, is a hydrogen or halogen atom or an alkyl or alkoxy radical; R5 is a hydroxy, alkoxy, phenyl or -NR9R10 radical; R6 is an oxygen, sulphur or nitrogen atom or a SO, SO2 or -N-alk radical, R7 is an alkyl, phenylalkyl or phenyl radical optionally substituted by one or more hydrogen atoms; R8 is an alkyl or phenylalkyl radical; each of R9 and R10, which are the same or different, is a hydrogen atom or an alkyl ...

Piperidines, their preparation and the medicaments containing them

Compounds of formula: in which R1 represents a hydroxyl or optionally substituted phenyl radical, a heterocycle or a residue of formula: R2 represents a methylene or ethylene radical or an NH or N-alkyl residue, R3 represents a hydrogen or halogen atom, R4 represents a phenyl or quinloyl radical, R5 represents a hydrogen atom or an alkyl radical, R8 represents an alkyl radical, n is equal to 1, 2 or 3, and the dashes represent an optional carbon-carbon double bond, it being understood that, when R2 represents an NH residue, the dashes necessarily represent a double bond and that, when R2 represents an ethylene radical, the dashes never represent a double bond, and their racemates and their enantiomers when they contain at least one asymmetric centre and their salts with inorganic and organic acids.

New 4-substd. 1,4-di:phenyl-1-sila:cyclopentane derivs. - used as serotonin antagonists e.g. for treating anxiety, migraine, asthma or hypertension

1,1-Diphenyl-3-(piperidino or piperazino)-1-silacyclopentane derivs. of formula (I) and their racemates, enantiomers, diastereoisomers and salts are new. Where R1, R2 = phenyl (opt. substd. by one or more of halogen, alkyl, alkoxy, alkylthio and CF2); or SiR1R2 = sila-dibenzocycloheptadiene gp. of formula (i): R3 = N or CH and the dotted bond is absent; or R3 = C and the dotted bond is present; R4 = phenyl (opt. substd. by one or more of halogen, alkyl and OH), pyridyl or pyrimidinyl; alkyl moieties have 1-4C. 9 Cpds. are specifically claimed, including, (RS)-1,1-diphenyl- 3-(4-phenyl-1-piperaziyl) -1-sila-cyclopentane. USE/ADVANTAGE - (I) are serotonin antagonists (claimed), effective against 5HT-2 receptors. They are useful for treating CNS, cardiovascular or gastrointestinal disorders involving serotonin, esp. anxiety, sleep and memory disorders, ischaemia, depression, psychosis (esp. schizophrenia), migraine, asthma, hypertension or urticaria, or as analgesics or platelet aggregation inhibitors. (I) generally have central 5HT-2 receptor antagonist IC50 less than 100 mM, and have low toxicity (no-toxic to mice at 300 mg/kg p.o.). Daily oral dose for adults is 10-300 mg.

4,5-DIHYDRO-THIAZO-2-YLAMINE DERIVATIVES AND THEIR USE AS NO-SYNTHASE INHIBITORS

The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2- ylamine of formula (I) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (I) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved abnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2). © KIPO & WIPO 2007 ...

IMIDAZO (1,2-A>INDENO (1,2-E> PYRAZINONE ANTAGONISTS of the AMPA AND NMDA RECEPTORS

5H, 10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZIN -4-ONE of DERIVATIVES YOUR PRODUCTION AND THESE CONTAINING DRUGS

5H, 10H-IMIDAZO (1,2-A>INDENO (1,2-E>PYRAZIN-4-ONE of DERIVATIVES, YOUR PRODUCTION AND IT CONTAINING DRUGS

DERIVED FROM 4,5-DIHYDRO-1,3-THIAZOL-2-YLAMINE, THEIR PREPARATION AND COMPOSITIONSPHAMARCEUTIQUES the CONTAINER

IMIDAZO (1,2-A>PYRAZIN-4-ON-DERIVATE ANTAGONIST of the AMPA AND NMDA RECEPTORS

SPIRO (HETEROZYCLISCHE IMIDAZO (1,2-A>INDENO (1,2E>PYRAZIN>-4' ONE, THEIR PRODUCTION AND THESE CONTAINING DRUGS

5H, 10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZIN-4-ONE of DERIVATIVES ANTAGONISTS of the RECEPTORS AMPA AND NMDA, YOUR PRODUCTION AND INTERMEDIATE PRODUCTS AND IT CONTAINING DRUGS

4,5-DIHYDRO-2-THIAZOLYLAMINDERIVATE AND YOUR USE AS NO-SYNTHASE INHIBITORS

7h-imidazo(1,2-a)pyrazine-8-one nmda receptor antagonists

3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide-3-carboxyl ic acid derivatives, preparation thereof and drugs containing same

IMIDAZO [1, 2-A] PYRIMIDINE DERIVATIVES METHOD FOR THE PRODUCTION THEREOF APPLICATION THEREOF AS MEDICAMENTS PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS MET INHIBITORS

L'invention concerne les nouveaux produits de formule (I): dans laquelle : n = 0,1 ou 2; X représente H, HaI ou alk; R représente H, NH2, NHaIk, N(alk)2; Ra représente H; HaI; -O-cycloalkyle; -O-alkyle, -O-aryle; -O-hétéroaryle; - NRd(cycloalkyle); -NRd(alkyle); -NRd(aryle); -NRd(hétéroaryle); alkyle; cycloalkyle; hétérocycloalkyle; aryle ou hétéroaryle; tous éventuellement substitués; Rb représente H, Rc, -COORc-CO-Rc ou -CO-NRcRd; avec Rc représente alkyle, cycloalkyle, hétérocycloalkyle, aryle et hétéroaryle, tous éventuellement substitués; Rd représente H, alk ou cycloalkyle; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET.

Antisérotonines, their preparation and drugs the container

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle -R1 représente un reste de formule: (CF DESSIN DANS BOPI) -Het représente . un radical phényl-4 tétrahydro-1,2,3,6 pyridyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, . un radical phényl-4 pipéridino dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, . un radical phényl-4 pipérazinyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, -R2 représente un radical alkyle ou phényle, -R3 représente un atome d'hydrogène ou un radical phényle -R4 représente un atome d'hydrogène ou d'halogène ou un radical phényl-4 pipérazinyl-1, -R5 représente un radical carbonyle ou sulfonyle, -R6 représente un radical Si(CH3 )2 ou C(CH3 )2 , -n est égal à 1, 2, 3 ou 4, leurs sels, leur préparation et les médicaments les contenant. Compounds of formula: (CF DRAWING IN BOPI) in which -R1 represents a residue of formula: (CF DRAWING IN BOPI) -Het represents. a phenyl-4-tetrahydro-1,2,3,6-pyridyl-1 radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical ,. a phenyl-4 piperidino radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical ,. a phenyl-4 piperazinyl-1 radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical, -R2 represents an alkyl or phenyl radical, -R3 represents a hydrogen atom or a radical phenyl -R4 represents a hydrogen or halogen atom or a phenyl-4 piperazinyl-1 radical, -R5 represents a carbonyl or sulfonyl radical, -R6 represents an Si (CH3) 2 or C (CH3) 2 radical, - n is equal to 1, 2, 3 or 4, their salts, their preparation and the drugs containing them.

New substituted indazoles are kinase inhibitors, useful in the treatment of cancers

Indazoles substitués, compositions les contenant, procédé de fabrication et utilisation. La présente invention concerne en particulier de nouveaux indazoles substitués spécifiques présentant une activité inhibitrice de kinases, ayant une activité thérapeutique, en particulier en oncologie.

New di:hydro-benzothiadiazine di:oxide carboxylic acid derivs.

La présente invention concerne des composés de formule: (CF DESSIN DANS BOPI) dans laquelle R représente un atome d'hydrogène ou un radical alkyle, -alk-CO-R5 , -alk-R6 -R7 ou phénylalkyle dans lequel le phényle est non substitué ou substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les radicaux alkyle et alcoxy, R1 représente un radical carboxy, alcoxycarbonyle, tétrazolyle, -CO-NHOH, -CO-N(alk)OH, -CO-NH-O-alk, -CO-N(alk)-OR8 ou un groupe convertible en radical carboxy in vivo, R2 , R3 et R4 , identiques ou différents, représentent chacun un atome d'hydrogène ou d'halogène ou un radical alkyle, R5 représente un radical hydroxy, alcoxy, phényle, ou -NR9 R1 0 , R6 représente un atome d'oxygène, de soufre ou d'azote ou un radical SO, SO2 ou N-alk, R7 représente un radical alkyle, phénylalkyle ou phényle éventuellement substitué par un ou plusieurs atomes d'halogène, R8 représente un radical alkyle ou phénylalkyle, R9 et R1 0 , identiques ou différents, représentent ...

Imidazo(1,2-a)pyrazine-4-one, preparation thereof and drugs containing same

NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS

L'invention concerne les nouveaux produits de formule (I): dans laquelle: Ra représente H, HaI, aryle ou hétéroaryle éventuellement substitués; Rb représente H, Rc, -COORc-CO-Rc ou -CO-NRcRd; avec Rc représente alkyle, cycloalkyle, hétérocycloalkyle, aryle et hétéroaryle, tous éventuellement substitués; Rd représente H, alk ou cycloalkyle; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET.

5H,10H-IMIDAZO[1,2-A]INDENO[1,2-E]PYRAZIN-4-ONE DERIVATIVES,PREPARATION THEREOF, AND DRUGS CONTAINING SAID DERIVATIVES

Composés de formule (I), dans laquelle: R représente un atome d'hydrogène ou un radical carboxy, alcoxycarbonyle, -CO-NR4R5, -PO3H2 ou -CH2OH, et R1 représente un radical -alk-NH2, -alk-NH-CO-R3, -alk-COOR4, -alk-CO-NR5R6 ou CO-NH-R7. Les composés de formule (I) présentent des propriétés pharmacologiques intéressantes. Ces composés sont des antagonistes du récepteur de l'acide .alpha.-amino-3-hydroxy-5-méthyl-4-isoxazolepropionique (AMPA), connu aussi sous le nom de récepteur du quisqualate. Par ailleurs, les composés de formule (I) sont des antagonistes non compétitifs du récepteur Nméthyl-D-aspartate (NMDA) et, plus particulièrement, ce sont des ligands pour les sites modulateurs de la glycine du récepteur NMDA.

5H-INDENO[1,2-B]PYRAZINE-2,3-DIONE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME

Composés de formule (I) dans laquelle R, R1, R2 et R3 sont tels que définis dans la description, leurs sels, leur préparation et les médicaments les contenant. Les composés de formule (I) présentent des propriétés pharmacologiques intéressantes. Ces composés sont des antagonistes du récepteur de l'acide .alpha.-amino-3-hydroxy-5-méthyl-4-isoxazol epropionique (AMPA), connu aussi sous le nom de récepteur du quisqualate. Par ailleurs, les composés de formule (I) sont des antagonistes non compétitifs du récepteur N-méthyl-D-aspartate (NMDA) et, plus particulièrement, ce sont des ligands pour les sites modulateurs de la glycine du récepteur NMDA.

Imidazo[1,2-a]pyrimidine derivatives, method for preparation thereof, use thereof as medicaments, pharmaceutical compositions and met inhibitors

The invention relates to the novel products of formula (I): in which: n = 0,1 or 2; X is H, Hal or alkyl; R is H, NH2, NH alkyl or N(alkyl)2; Ra is H, Hal, -O-cycloalkyl, -O-alkyl, -O-aryl, -O-heteroaryl, -NRd(cycloalkyl), -NRd(alkyl), -NRd(aryl), -NRd(heteroaryl), alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, all optionally substituted; Rb is H, Rc, -COORc-CO-Rc or -CO-NRcRd; wherein Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted, and Rd is H, alk or cycloalkyl. These products are in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.

DERIVED FROM 5:00, 10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE-4-ONE, THEIR PREPARATION, THEIR INTERMEDIARIES AND DRUGS the CONTAINER

La présente invention concerne des composés de formule: (CF DESSIN DANS BOPI) dans laquelle R représente un atome d'hydrogène ou un radical -COOH, -alk-COOH, -PO3 H2 , -CH2 -PO3 H2 , -CH=CH-COOH ou phényle substitué par un radical carboxy, R1 représente un radical -alk-CN, -alk-COOH, -alk-Het, -alk-PO3 H2 ou -alk-CO-NH-SO2 R2 , R2 représente un radical alkyle ou phényle, alk représente un radical alkyle, Het représente un hétérocycle mono ou polycyclique saturé ou insaturé contenant 1 à 9 atomes de carbone et un ou plusieurs hétéroatomes choisi parmi O, S, N, l'hétérocycle étant éventuellement substitué par un ou plusieurs radicaux alkyle, phényle ou phénylalkyle, étant entendu que lorsque R représente un atome d'hydrogène ou un radical -COOH ou -PO3 H2 , R1 ne peut pas représenter -alk-COOH, leurs isomères, racémiques, énantiomères et diastéréoisomères, leurs sels, leur préparation, leurs intermédiaires et les médicaments les contenant.

DERIVED From ACID IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE-2-CARBOXYLIQUE, THEIR PREPARATION AND DRUGS the CONTAINER

Composés de formule : (CF DESSIN DANS BOPI) dans laquelle R, R1 , R2 et R3 sont tels que définis dans la description, leurs sels, leur préparation et les médicaments les contenant.

USE OF DERIVED FROM 2-AMINOTHIAZOLINE LIKE INHIBITORS FROM NO-SYNTHASEINDUCTIBLE

Derived from imidazo [1,2-a] pyrazine-4-one, their preparation and drugs the container

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle le cycle A est choisi parmi les cycles suivants: (CF DESSIN DANS BOPI) dans lesquels R représente un radical CH2 ou un atome de soufre, d'oxygène ou d'azote substitué par un radical alkyle, leurs sels, leur préparation et les médicaments les contenant.

Heterocyclic [...] the preparation thereof and drugs containing

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle -R1 représente un reste de formule: (CF DESSIN DANS BOPI) Het représente: . un radical phényl-4 tétrahydro-1,2,3,6 pyridyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, . un radical phényl-4 pipéridino dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, . un radical phényl-4 pipérazinyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, -R2 représente un atome d'hydrogène ou un radical alkyle, -n est égal à 1, 2, 3 ou 4, leurs sels, leur préparation et les médicaments les contenant. Compounds of formula: (CF DRAWING IN BOPI) in which -R1 represents a residue of formula: (CF DRAWING IN BOPI) Het represents:. a phenyl-4-tetrahydro-1,2,3,6-pyridyl-1 radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical ,. a phenyl-4 piperidino radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical ,. a phenyl-4 piperazinyl-1 radical in which the phenyl ring is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical, -R2 represents a hydrogen atom or an alkyl radical, -n is equal to 1, 2, 3 or 4, their salts, their preparation and the medicaments containing them.

TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND DRUGS CONTAINING

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle Het est tel que défini dans la description, leurs sels, leur préparation et les médicaments les contenant.

REPLACED INDAZOLES, COMPOSITIONS CONTAIN THAT THEM, PROCEDURE OF MANUFACTURE AND USE

INDAZOLES SUBSTITUIDOS, COMPOSICIONES QUE LOS CONTIENEN, PROCEDIMIENTO PARA LA FABRICACION Y UTILIZACION. LA PRESENTE INVENCION SE REFIERE, EN PARTICULAR, A NUEVOS INDAZOLES SUBSTITUIDOS ESPECIFICOS, QUE PRESENTAN UNA ACTIVIDAD INHIBIDORA DE KINASAS, QUE TIENEN UNA ACTIVIDAD TERAPEUTICA , EN PARTICULAR EN ONCOLOGIA.

4,5-dihydro-thiazo-2-ylamine derivatives and their use as no-synthase inhibitors

ImidazoÝ1,2-a¨indenoÝ1,2-e¨pyrazine-2-carboxylic acid derivatives, preparation thereof and drugs containing same

5H,10H-IMIDAZO[1,2-A]INDENO[1,2-E]PYRAZIN-4-ONE DERIVATIVES; PROCESS FOR PREPARING THE SAME AND DRUGS CONTAINING THEM

Composés de formule (I) dans laquelle R et R1, identiques ou différents, représentent un atome d'hydrogène ou d'halogène ou un radical alkyle, alcoxy, amino, acylamino, phényluréido, -N=CH-N(R2R3, nitro, imidazolyle, phényle, SO3H ou cyano, R2 et R3, identiques ou différents, représentent chacun un radical alkyle, leurs sels, leur préparation, les intermédiaires pour les préparer et les médicaments les contenant.

ANTISEROTONINS, PREPARATION THEREOF AND MEDICAMENTS CONTAINING THEM

2103562 9219624 PCTABS00160 Composés de formule R1-(CH2)n-Het dans laquelle R1 représente un reste de formule (B), (C), (D); Het représente un radical phényl-4 tétrahydro-1,2,3,6 pyridyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy, un radical phényl-4 pipéridino dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy; un radical phényl-4 pipérazinyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy; R3 représente un atome d'hydrogène ou un radical phényle; R4 représente un atome d'hydrogène ou d'halogène ou un reste Het; R5 représente un radical carbonyle ou sulfonyle; R6 représente un radical Si(CH3)2 ou C(CH3)2; n est égal à 1, 2, 3 ou 4, à l'exception du ¢(phényl-4 tétrahydro-1,2,3,6 pyridyl-1)-2 éthyl! amino -3 benzisothiazole-1,2 dioxyde-1,1; leurs sels, leur préparation et les médicaments les contenant. 2103562 9219624 PCTABS00160 Compounds of formula R1- (CH2) n-Het in which R1 represents a residue of formula (B), (C), (D); Het represents a 4-phenyl-1,2,3,6-pyridyl-1 radical, the phenyl ring of which is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical, a 4-phenyl piperidino radical, the ring of which phenyl is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a 4-phenyl-piperazinyl-1 radical, the phenyl ring of which is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R3 represents a hydrogen atom or a phenyl radical; R4 represents a hydrogen or halogen atom or a Het residue; R5 represents a carbonyl or sulfonyl radical; R6 represents an Si (CH3) 2 or C (CH3) 2 radical; n is 1, 2, 3 or 4, with the exception of ¢ (4-phenyl-1,2,3,6-tetrahydro-pyridyl-1) -2 ethyl! amino -3 benzisothiazole-1,2 dioxide-1,1; their salts, their preparation and the ...

New 1,1-di:phenyl-3-hydroxy-(sila)cyclopentane derivs. - used as serotonin antagonists e.g. for treating anxiety, migraine, asthma or hypertension

Dérivés de diphényl-1,1 hydroxy-3 (sila)cyclopentane de formule: (CF DESSIN DANS BOPI) dans laquelle R représente un atome de carbone ou de silicium, soit (CF DESSIN DANS BOPI) atome de carbone, R2 représente un radical phényle ou phényle substitué par un ou plusieurs substituants, identiques ou différents, choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy et alkylthio, R3 représente un atome d'hydrogène ou un radical alkyle ou acyle, R4 et R5 , identiques ou différents, représentent chacun un radical phényle éventuellement substitué par un ou plusieurs substituants, identiques ou différents, choisis parmi les atomes d'halogène et les radicaux alkyle, alcoxy, alkylthio et trifluorométhyle, leurs sels, leur préparation et les médicaments les contenant.

Inducible nitrogen monoxide synthase inhibitors comprising new or known 4- and/or 5-substituted 4,5-dihydro-thiazol-2-ylamine compounds, useful e.g. for treating neurodegenerative or inflammatory diseases

La présente invention concerne l'utilisation de dérivés de 2-aminothiazoline de formule : dans laquelle soit R1 est un atome d'hydrogène ou un radical alkyle et R2 est un radical alkyle, -alk-NH2 , -CH2-R3 ou phényle substitué par un radical nitro ou -NH-C (=NH) CH3 , soit R, est un radical alkyle et R2 est un atome d'hydrogène, R3 est un radical cycloalkyle (3-6C), pyridyle, thiényle, phényle ou phényle substitué par un radical nitro ou carboxy, alk représente un radical alkylène ou leurs sels pharmaceutiquement acceptables comme inhibiteurs de NO-synthase inductible.

New 1,1--di:phenyl-4-amino-sila:cyclopentene derivs. - used as serotonin antagonists, e.g. for treating anxiety, migraine, asthma or hypertension

4-Amino-1,1-diphenyl -1-sila-cyclopent-2-ene derivs. of formula (I) and their racemates, enantiomers, diastereo-isomers and salts are new. Where R1, R2 = phenyl (opt. substd. by one or more of halogen, alkyl, alkoxy, alkylthio and CF3); R3, R4 = alkyl; or NR3R4 = heterocyclic gp. of formula (a): R5 = N, CH or C(OH) and the dotted bond is present; or R5 = C and the dotted bond is absent; R6 = phenyl (opt. substd. by one or more of halogen, alkyl and OH); alkyl moieties have 1-4C. USE/ADVANTAGE - (I) are serotonin antagonists (claimed), effective against 5HT-2 receptors. They are useful for treating CNS, cardiovascular or gastrointestinal disorders involving serotoninn, esp. anxiety, sleep and memory disorders, ischaemia, depression, psychosis (esp. schizophrenia), migraine, asthma, hypertension or asthma, or as analgesics or platelet aggregation inhibitors. (I) generally have central 5HT-2 receptor antagonist IC50 less than 100 nM, and have low toxicity (non-toxic to mice at 300 mg/kg p.o.). Daily oral dose for adults is 10-300 mg.

Derivatives imidazo [1,2-a] indeno [1,2-e] pyrazine-4-one, the preparation thereof and drugs containing

Pharmaceutical compositions containing, as the active principle, compounds of formula (I), wherein R, R1 and R2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

5H-indeno(1,2-b)pyrazine-2,3-dione derivatives, preparation thereof and drugs containing same

ImidazoÝ1,2-a¨pyrazine-4-one, preparation thereof and drugs containing same

Indeno{1,2-e}pyrazin-4-ones, preparation thereof and medicaments containing same

Azaindoles

ANTISEROTONIN HETEROCYCLIC DERIVATIVES, PREPARATION THEREOF AND MEDICAMENTS CONTAINING THEM

... 2103561 9219606 PCTABS00160 Composés de formule (I) R1-(CH2)n-Het, dans laquelle R1 représente un reste des formules (A), (B) et (C), Het représente: un radical phényl-4 tétrahydro-1,2,3,6 pyridyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy; un radical phényl-4 pipéridino dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy; un radical phényl-4 pipérazinyl-1 dont le cycle phényle est éventuellement substitué par un atome d'halogène ou un radical alkyle, alcoxy ou hydroxy; R2 représente un atome d'hydrogène ou un radical alkyle, n est égal à 1, 2, 3 ou 4, leurs sels, leur préparation et les médicaments les contenant.

DERIVED FROM 10:00 - IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZIN-4-ONE, THEIR PREPARATION AND DRUGS the CONTAINER

Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, -CO-NR4R5, -PO3H2 or -CH2OH radical, and R1 is an -alk-NH2, -alk-NH-CO-R3, -alk-COOR4, -alk-CO-NR5R6 or -CO-NH-R7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.

Derived from 5:00 - indeno [1,2-b] pyrazine-2,3-dione, their preparation and drugs the container

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle R, R1 et R2 sont tels que définis dans la description, leurs sels, leur préparation et les médicaments les contenant.

Indeno [1,2-e] pyrazine-4-ones, their preparation and drugs the container

Compounds of formula (I), wherein R is a substituted nitrogen, oxygen or sulphur atom or a radical C=R3, C(R4)R5 or CH-R6; R1 is a hydroxy radical, polyfluoroalkoxy, carboxy, alkoxycarbonyl, -NH-CHO or -NH-CO-N(alk)Ar where Ar is optionally substituted, -N(alk)-CO-NR8R9, -N(alk-Ar)-CO-NR8R9, -NH-CO-NR9R12, -NH-CS-NR8R9, -N(alk)-CS-NR8R9, -NH-CO-R10, -NH-CS-R20, -NH-C(=NR21)-NR7R9, -N(alk)-C(=NR21)-NR7R9, -NH-SO2-NR7R9, -N(alk)-SO2-NR7R9, -CO-NR7R9, -NH-SO2-CF3, -NH-SO2-alk, -NR9R11, -S(O)m-alk-Ar, -SO2-NR7R9, optionally 3-substituted 2-oxo-1-imidazolidinyl or optionally 3-substituted 2-oxo-1 perhydropyrimidinyl; R2 is a hydrogen or halogen atom or an akyl radical, alkoxy, amino, -NH-CO-NH-Ar, N=CH-N(alk)alk', nitro, cyano, phenyl, imidazolyl, acylamino, SO3H, hydroxy, polyfluoroalkoxy, carboxy, alkoxycarbonyl, -NH-CHO, -NH-CO-N(alk)Ar where Ar is optionally substituted, -N(alk)-CO-NR8R9, -N(alk-Ar)-CO-NR8R9, -NH-CO-NR9R12, -NH-CS-NR8R9, -N(alk)-CS-NR8R9, -NH-CO-R10, -NH-CS-R20, -NH-C(=NR21)-NR7R9, -N(alk)-C(=NR21)-NR7R9, -NH-SO2-NR7R9, -N(alk)-SO2-NR7R9, -CO-NR7R9, -NH-SO2-CF3, -NH-SO2-alk, -NR9R11, -S(O)m-alk-Ar, -SO2-NR7R9, optionally 3-substituted 2-oxo-1-imidazolidinyl or optionally 3-substituted 2-oxo-1-perhydropyrimidinyl; R3 is an oxygen atom or a NOH, NO-alk-COOX or CH-R13 radical; R4 is an alkyl radical, -alk-Het or -alk-Ar; R5 is a straight or branched C1-11 alkyl radical, -alk-Het or -alk-Ar, or R4 and R5, taken together with the carbon atom to which they are attached, form a cycloalkyl radical; R6 is a hydrogen atom radical or a hydroxy radical, straight or branched C1-11 alkyl, -NR14R15, -alk-OH, -alk-NR14R15, -alk-Ar or -alk-Het; and salts thereof. The compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, particularly NMDA receptor glycine modulation site ligands, and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate ...

5:00, 10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE-A-ONES SUBSTITUEES IN POSITION 2, THEIR PREPARATION AND the DRUGS the CONTAINER

La présente invention concerne des composés de formule: (CF DESSIN DANS BOPI) dans laquelle R représente un radical -CO-CH2 -PO3 H2 , -CO-NH-tétrazole-5-yle, -CO-NHOH, -CO-NH-NH2 , -alk-COOH, -CH2 -PO3 H2 , -CO-NH-SO2 R1 , -CH=CH-COOH ou phényle substitué par un radical carboxy, alk représente un radical alkyle et R 1 représente un radical alkyle ou phényle, leurs racémiques, isomères, énantiomères et diastéréoisomères, leurs sels, leur préparation et les médicaments les contenant.

ImidazoÝ1,2-a¨pyrazine-4-one derivatives, preparation thereof and drugs containing same

IndenoÝ1,2-e¨pyrazine-4-ones, preparation thereof and drugs containing same

1,2,4-triazoloÝ4,3-a¨pyrazine-4-one derivatives, preparation thereof and drugs containing same

IMIDAZO[1,2-A]PYRAZIN-4-ONE, PREPARATION THEREOF AND DRUGS CONTAINING SAME

Composés de formule (I) dans laquelle soit R représente C=R3, C(R4)R5 ou CH-R6, R1 et R2 représentent hydrogène, halogène, alkyle, alcoxy, amino, acylamino, -NH-CO-NH-Ar, -N=CH-N(alk)alk', nitro, cyano, phényle, imidazolyle ou SO3H, R3 représente oxygène, NOH, NO-alk-COOX ou CH-R7, R4 représente alkyle, -alk-Het ou alk-Ar, R5 représente alkyle, -alk-Het ou -alk-Ar ou bien C(R4)R5 représente cycloalkyle, R6 représente hydroxy, alkyle, -NR8R9, -alk-OH, -alk-NR8R9, -alk-Ar ou -alk-Het, R7 représente hydroxy, alkyle, phényle, -alk-Ar, -alk-Het, -NR10R11 ou un hétérocycle, R8 et R9 représente alkyle, ou bien R8 représente hydrogène et R9 représente hydrogène ou alkyle, -COR12, -CSR30 ou -SO2R13, R10 et R11 représentent alkyle ou cycloalkyle, R12 représente alkyle, cycloalkyle, phényle, -COO-alk, -CH2-COOX, -CH2-NH2, -NH-alk, -NH-Ar, -NH2 ou -NH-Het, R13 représente alkyle ou phényle, R30 représente -NH-alk, -NH-Ar, -NH2 ou -NH-Het, soit R représente un radical 2-imidazolylméthyle et R1 et R2 ...

DERIVED FROM 4-HYDROXY-3-PHENYL-INDENO (1,2-B) PYRIDINE-2 (1H) - ONE, THEIR PREPARATION AND DRUGS the CONTAINER

Derivatives of formula (I), wherein R is a methylene radical, N-alk, NH or an oxygen or sulphur atom, R1 and R2, which are the same or different, are a hydrogen or halogen atom or a hydroxy, alkoxy, alkyl, nitro, amino, monoalkylamino, dialkylamino, cyano, polyfluoroalkyl, polyfluoroalkoxy or phenoxy radical, R3 and R4, which are the same or different, are a hydrogen or halogen atom or an alkyl radical; tautomeric forms thereof, salts thereof, preparation thereof and drugs containing said derivatives.

5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN-4-ONE DERIVATE, IHRE HERSTELLUNG UND DIE SIE ENTHALTENDEN ARZNEIMITTEL

2-AMINOTHIAZOLINDERIVATE UND IHRE VERWENDUNG ALS NO-SYNTHASE INHIBITOREN

5h-indenoÝ1,2-b¨pyrazine-2,3-dione derivatives, preparation thereof and drugs containing same

Novel triazolo(4,3-a)pyridine derivatives, process for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use, in particular as MET inhibitors

2-substituted 5h,10h-imidazo{1,2-a}indeno{1,2-e}pyrazine-4-ones, preparation thereof and drugs containing same

DERIVATIVES OF 6-(6-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) 5-FLUORO-BENZOTHIAZOLES AND 5-FLUORO-BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS METINHIBITORS

L'invention concerne les nouveaux produits de formule (I): dans laquelle (II) représente une liaison simple ou double; F représente un atome de fluor, Ra représente H, HaI, alcoxy, O-cycloalkyle, -O- hétérocycloalkyle; -NH-cycloalkyle, -NH-hétérocycloalkyle, hétéroaryle,phényle, NHCOaIk, NHCOcycloalk ou NR1 R2; X représente S, SO ou SO2, A représente NH ou S; W représente H, alkyle ou COR avec R représente cycloalkyle; alkyle éventuellement substitué par NR3R4, alcoxy, hydroxy, phényle, hétéroaryle, ou hétérocycloalkyle; alcoxy éventuellement substitué par NR3R4, càd un radical O-(CH2)n-NR3R4, un radical O-phényle ou O-(CH2)n-phényle, avec phényle éventuellement substitué et n= 1 à 4; ou le radical NR1 R2; R1 représente H ou al k et R2 représente H, cycloalkyle ou alkyle; R3 et R4 représentent H, alk, cycloalkyle, hétéroaryle ou phényle; R1, R2 et/ou R3,R4 forment avec N un cycle renfermant éventuellement O, S, N et/ou NH; tous hétérocycloalkyle, hétéroaryle et phényle et cycliques étant ...

SPIRO HETEROCYCLE-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE) - 4 ' - ONES, THEIR PREPARATION AND DRUGS CONTAINERS

Compounds of formula (I), wherein R3 and R4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl radical, -CHO, -COOR11, -CO-alk-COOR6, -CO-alk-NR6R12, -CO-alk-CONR6R8, -CO-COOR6, -CO-CH2-O-CH2-COOR6, -CO-CH2-S-CH2-COOR6, -CO-CH=CH-COOR6, -CO-alk, -CO-Ar". -CO-alk-Ar", -CO-NH-Ar", -CO-NH-alk-Ar", -CO-Het, -CO-alk-Het, -CO-NH-Het, -CO-NH-alk-Het, -CO-NH2, -CO-NH-alk, -CO-N(alk)alk', -CS-NH2, -CS-NH-alk, -CS-NH-Ar", -CS-NH-Het, -alk-Het, -alk-NR6R8, -alk-COOR6, -alk-CO-NR6R8, -alk-Ar", -SO2-alk, -SO2-Ar or -CO-cycloalkyl, where the cycloalkyl is optionally 2-substituted by a carboxy radical; or (b) a 2-pyrrolidine-5-one ring. The compounds of formula (I) have useful pharmacological properties and are alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.

INDENO [1,2-E] PYRAZIN-4-ONES, THEIR PREPARATION AND DRUGS the CONTAINER

Compounds of formula (I), wherein R is a C=CH-R2, C(R3)R4, CH-NH2, CH-CH(OH)-COOH or CH-CH(OH)-COOalk radical, R1 is an -alk-NH2 or alk-NH-CO-R5 radical, R2 is a -COOH or -COOalk radical, R3 is an alkyl, -alk-Ar or -alk-Het radical, R4 is an -NH2, -NH-alk, -N(alk)-alk', -NH-CO-alk, -NH-CO-Ar', -NH-CO-ALK-Ar', -NH-CO-Het, -NH-CO-alk-Het, -NH-CO-alk-COOH, -NH-CO-alk-COOalk', -alk-COOH, -alk-COOalk', -NH-CO-NH2, -NH-CO-NH-alk, -NH-CO-NH-Ar' or -NH-CO-NH-alk-Ar' radical, or R3 and R4, together with the carbon atom to which they are attached, form a 2- or 3-pyrrolidine, 2- or 4-piperidine or 2-azacycloheptane substituted or unsubstituted ring, R5 is an -NH2, -NH-alk, -NH-Ar', -NH-cycloalkyl, -NH-alk-Ar' or -N(alk)-alk' radical, the salts thereof, the preparation thereof and medicaments containing same are described.

DERIVED FROM 5:00, 10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE-4-ONE, THEIR PREPARATION AND DRUGS the CONTAINER

Compounds of formula (I), wherein R is a hydrogen atom or a -COOH or CH2OH radical, R1 is a -CH-R2 radical, R2 is a 3-dimethyl-1H-pyrazole-4-yl, 4-chloro-1-methylimidazole-5-yl or 3-hydroxy-isoxazole-5-yl radical, except for 10-(1,3-dimethyl-1H-pyrazole-4-methylene)-5H,10H-imidazo[1,2-a]indeno[ 1,2-e]pyrazine-4-one, isomers thereof, salts thereof, the preparation thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites.

5h,10h-imidazo{1,2-a}indeno{1,2-e}pyrazine-4-one derivatives, preparation thereof, intermediates thereof and drugs containing same

5H,10H-IMIDAZO[1,2-A]INDENO[1,2-E]PYRAZINE-4-ONE DERIVATIVES, PREPARATION THEREOF, INTERMEDIATES THEREOF AND DRUGS CONTAINING SAME

Compounds of formula (I), wherein R is a hydrogen atom or a -COOH, -alk-COOH, -PO¿3?H¿2?, -CH¿2?-PO¿3?H¿2?, or -CH=CH-COOH radical, or a phenyl radical substituted by a carboxy radical, R¿1? is an alk-CN, -alk-COOH, -alk-Het, alk-PO¿3?H¿2? or -alk-CO-NH-SO¿2?R¿2? radical, R¿2? is an alkyl or phenyl radical, alk is an alkyl radical, Het is a saturated or unsaturated mono- or polycyclic heterocyclic ring containing 1-9 carbon atoms and one or more heteroatoms selected from O, S and N, said heterocyclic ring optionally being substituted by one or more alkyl, phenyl or phenylalkyl radicals, with the proviso that when R is a hydrogen atom or a -COOH or -PO¿3?H¿2? radical, R¿1? cannot be -alk-COOH, isomers, racemic mixtures, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof, intermediates thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites.

DERIVATIVES OF 6-(6-O-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS

L'invention concerne les nouveaux produits de formule (I): (I) dans laquelle (II) représente une liaison simple ou double; Ra représente -O-Z-Rc avec Z simple liaison ou alkylène éventuellement substitué et Rc représente cycloalkyle, hétérocycloalkyle, aryle ou hétéroaryle éventuellement substitués; Rb représente H ou F; avec si Rb est H, alors Rc n'est pas cycloalkyle quand Z est simple liaison et Rc n'est pas hétérocycloalkyle quand Z est alkylène; X représente S, SO ou SO2, A représente NH ou S; W représente H, alkyle, cycloalkyle ou COR avec R représente cycloalkyle; alkyle; alcoxy; O- phényle; -O-(CH2)n-phényle avec n= 1 à 4; ou NR1 R2 avec R1 représente H ou alk et R2 représente H, cycloalkyle ou alkyle; ou bien R1, R2 forment avec N un cycle renfermant éventuellement O, S, N et/ou NH; tous ces radicaux étant éventuellement substitués; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET. The invention relates to novel products of formula (I): (I) wherein (II) represents a single or double bond; Ra represents -O-Z-Rc with Z single bond or optionally substituted alkylene and Rc represents optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Rb is H or F; with if Rb is H, then Rc is not cycloalkyl when Z is single bond and Rc is not heterocycloalkyl when Z is alkylene; X is S, SO or SO 2, A is NH or S; W is H, alkyl, cycloalkyl or COR with R is cycloalkyl; alkyl; alkoxy; O-phenyl; -O- (CH 2) n-phenyl with n = 1 to 4; or NR1 R2 with R1 is H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 together with N form a ring optionally containing O, S, N and / or NH; all these radicals being optionally substituted; these products being in all isomeric forms and salts, as medicaments especially as MET inhibitors.

Application of derived from acid 2:00 - 1,2,4-benzothiadiazine-1,1-dioxide-3-carboxylic to the demédicaments preparation, new products, their preparation and drugs the container

The use of 2H-1,2,4-benzothiadiazine-1,1-dioxide-3-carboxylic acid derivatives of formula (I), a salt thereof or a precursor thereof, for preparing NMDA and/or AMPA receptor antagonist drugs, the novel compounds of formula (I), preparation thereof, and drugs containing same, are disclosed.

Compositions containing new or known 4-substituted 4,5-dihydro-thiazol-2-ylamines, as inducible nitrogen monoxide synthase inhibitors useful e.g. for treating neurodegenerative or inflammatory diseases

La présente invention concerne des dérivés de 4, 5-dihydro-1, 3-thiazol-2-ylamine de formule : dans laquelle R représente un radical phényle ou phényle substitué par alcoxy ou halogène, leurs sels pharmaceutiquement acceptables, leur préparation et les compositions pharmaceutiques les contenant.

Epoxydes, leur préparation et leur emploi.

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle R1 et R2 identiques ou différents représentent des atomes d'hydrogène ou de fluor ou des radicaux alkyle, alkoxy ou dialkylamino, procédé pour leur préparation et leur utilisation.

Derivatives imidazo [1,2-a] pyrazine-4-one, the preparation thereof and drugs containing

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle R représente C=R3 , C(R4 )R5 ou CH-R6 , R1 et R2 représentent hydrogène, halogène, alkyle, alcoxy, amino, acylamino, -NH-CO-NH-Ar, -N=CH-N(alk)alk', nitro, cyano, phényle, imidazolyle ou SO3 H, R3 représente oxygène, NOH, NO-alk-COOX ou CH-R7 , R4 représente alkyle, -alk-Het ou -alk-Ar, R5 représente alkyle, -alk-Het ou -alk-Ar ou bien C(R4 )R5 représente cycloalkyle, R6 représente hydroxy, alkyle, -NR8 R9 , -alk-OH, -alk-NR8 R9 , -alk-Ar ou -alk-Het, R7 représente hydroxy, alkyle, phényle, -alk-Ar, -alk-Het, -NR1 0 R1 1 ou un hétérocycle, R8 et R9 , représentent alkyle, ou bien R8 représente hydrogène et R9 représente hydrogène ou alkyle, -COR1 2 , -CSR3 0 ou -SO2 R1 3 , R1 0 et R1 1 représentent alkyle ou cycloalkyle, R1 2 représente alkyle, cycloalkyle, phényle, -COO-alk, -CH2 -COOX, -CH2 -NH2 , -NH-alk, -NH-Ar, -NH2 ou -NH-Het, R1 3 représente alkyle ou phényle, R3 0 représente -NH-alk, -NH-Ar, -NH2 ou -NH-Het, leurs sels, leur ...

5H,10H-imidazo{1,2-a}indeno{1,2-e}pyrazin-4-one derivatives, preparation thereof, and drugs containing said derivatives

Imidazo(1,2-a)indeno(1,2-e)pyrazine-4-one derivatives and pharmaceutical compositions containing same

Azaindoles

The invention is directed to physiologically active compounds of general formula (I):- and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Derivatives of 5H,10H-imidazo(1,2-a)indeno(1,2-e)pyrazine-4-one, preparation thereof and medicaments containing them

2-aminothiazoline derivatives and their use as no-synthase inhibitors

Use of 2H-1,2,4-benzothiadiazine-1,1-dioxide-3-carboxylic acid derivatives for preparing NMDA/AMPA receptor antagonist drugs, novel products, preparation thereof and drugs containing same

5h,10h-imidazoÝ1,2-a¨indenoÝ1,2-e¨pyrazin-4-one derivatives, preparation thereof, and drugs containing said derivatives

DERIVATIVES OF 5H, 1OH-IMIDAZO[1,2-A)INDEN[1,2-E]PYRAZIN-4-ON, THEIR PREPARATION AND THEIR INTERMEDIATE PRODUCTS AND MEDICAMENTS CONTAINING THEM

The invention relates to compounds with the formulawhere R is hydrogen atom or -COOH, -alk-COOH, -PO3H2, -CH2-PO3H2,-CH=CH-COOH or phenyl radical substituted by carboxyradical, R1being -alk-CN, -alk-COOH, -alk-Het, -alk-PO3H2 or-alk-CO-NH-SO2R2, R2 meaning alkyl or phenyl radical, alk is alkylradical, Het is saturated or unsaturated mono- or polycyclicheterocycle containing from 1 to 9 carbon atoms and one or moreheteroatoms selected amongst O, S & N, the heterocycle beingoptionally substituted by one or more alkyl, phenyl or phenylalkylradicals, and when R is hydrogen atim or -COOH, or -PO3H2, R1cannot be -alk-COOH. The invention also relates to isomers,racemates, enantiomers and diasteroisomers of the above compiunds,to their salts, to their preparation, as well as to intermediateproducts and medicaments containing them.15 claims ...

IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN-2-CARBONSÄURE DERIVATE, IHRE HERSTELLUNG UND SIE ENTHALTENDE ARZNEIMITTEL

Novel imidazo[1,2-a]pyridine derivatives, method for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use in particular as MET inhibitors

IMIDAZO DERIVATIVES [1,2-A] PYRIMIDINE, PROCEDURE OF PREPARATION, INTERMEDIARIES OF THIS PROCESS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE/UNDERSTAND AND USE OF The same, LIKE INHIBITORS OF PROTEINQUINASA MET, FOR the TREATMENT OF CANCERS, PSORIASIS, DISEASES OF the CENTRAL NERVOUS SYSTEM AND OTHERS

Reivindicacion 1: Productos de formula (1), en la que n es = 0, 1 o 2; X representa un átomo de hidrogeno, un átomo de halogeno o un radical alquilo; R representa un átomo de hidrogeno, un radical NH2, NHalk o N(alk)2; Ra representa un átomo de hidrogeno, un átomo de halogeno, o un radical -O-cicloalquilo, -O-alquilo, -O-arilo, -O-heteroarilo, -NRd(cicloalquilo), -NRd(alquilo), -NRd(arilo), -NRd(heteroarilo), alquilo, cicloalquilo, heterocicloalquilo, un radical arilo, o un radical heteroarilo; en todos estos radicales, los radicales cicloalquilo, alquilo, arilo y heteroarilo estando opcionalmente sustituidos como se indica a continuacion; Rb representa un átomo de hidrogeno, un radical Rc, -COORc, -CO-Rc o un radical -CO-NRcRd; con Rc representando un radical alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo, estando todos estos radicales opcionalmente substituidos como se indica a continuacion; Rd representa un átomo de hidrogeno o un radical alquilo o cicloalquilo; estando ...

5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN-4-ONE DERIVATE ANTAGONISTEN DER REZEPTOREN AMPA UND NMDA, IHRE HERSTELLUNG UND ZWISCHENPRODUKTE UND SIE ENTHALTENDE ARZNEIMITTEL

4-hydroxy-3-phenyl-indeno(1,2-b)pyridine-2(1h)-one derivatives as nmda antagonists

IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZINE-2-CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

DERIVATIVES OF 4-HYDROXY-3-PHENYL-INDENO (1,2-B) PYRIDINE-2 (1H) - ONE, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

5H, 10H-imidazo [1,2-a] indeno [1,2-e] pyrazine-4-one derivatives, their preparation and the medicaments containing them.

Indeno [1,2-e] pyrazine-4-ones, their preparation and the drugs containing them.

NEW SUBSTITUTED INDAZOLES, THEIR PREPARATION AND THEIR THERAPEUTIC USE

L'invention est relative à des composés de formule (1) dans laquelle : . E désigne un graupement :(i) de formule -NT-CO-O- ou -NT-CX-NT'- dans laquelle X désigne =0 ou =S et T et T', pouvant être identiques ou différents, sont choisis indépendamment parmi H ou un groupe alkyle ou(ii) formant un cycle à 5 ou 6 chaînonsqui est rattaché en position 5 ou 6 au noyau indazole par -NT- ou par l'atome d'azote N1;. R1représente un ou plusieurs substituant(s), choisis indépendamment l'un de l'autre lorsqu'il y en a plusieurs, pouvant être : un atome d'halogène, un groupe alkyle, alkényle, alkynyle, halogénoalkyle, halogénoalcoxy, aryle, hétéroaryle, hétérocycloalkyle, cycloalkyle, CN, NRR', OR, NOz, COOR, CONRR', NRCOR' ;. R2représente un atome d'hydrogène, un groupe alkyle, alkényle ou alkynyle ;. R3représente un ou plusieurs substituant(s), choisis indépendamment l'un de l'autre lorsqu'il y en a plusieurs et pouvant être : un atome d'halogène, un groupe alkyle, alkényle, alkynyle, halogénoalcoxy, aryle, hétéroaryle, cycloalkyle, hétérocycloalkyle, CN, NRR', CF3, OR, NO2, COOR, CONRR', NRCOR' ;. R4désigne un atome d'hydrogène ou d'halogène, un groupe alkyle, alkényle, alkynyle, aryle, hétéroaryle, hétérocycloalkyle, -NR-CO-R', COOR, NRR', CHO, CONR(OR') ;. R et R', pouvant être identiques ou différents, désignent indépendamment l'un de l'autre : un atome d'hydrogène, un groupe alkyle, aryle, hétérocycloalkyle, cycloalkyle ou hétéroaryle ;. n1représente un nombre entier allant de 0 à 5 et n3un nombre entier allant de 0 à 3. The invention relates to compounds of formula (1) in which: E denotes a graupement: (i) of formula -NT-CO-O- or -NT-CX-NT'- in which X denotes = 0 or = S and T and T ', which may be identical or different, are chosen independently from H or an alkyl group or (ii) forming a 5- or 6-membered ring which is attached in position 5 or 6 to ...

New triazolo(4,3-a)pyridine derivatives are mesenchymal-epithelial transition protein kinase inhibitors useful in a pharmaceutical composition for preparing a medicament to treat/prevent e.g. fibrotic disorders, allergies and asthma

Triazolo[4,3-a]pyridine derivatives (I) and their isomers, racemic isomers, enantiomers, diastereomers and inorganic and organic acid or base addition salts are new. Triazolo[4,3-a]pyridine derivatives of formula (I) and their isomers, racemic isomers, enantiomers, diastereomers and inorganic and organic acid or base addition salts are new. Ra1 : aryl, heteroaryl (both optionally substituted), H or halo; Rb : H, Rc, -COORc, -CO-Rc or -CO-NRcRd; Rc : alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted); Rd : H, alkyl or cycloalkyl; either R1R2 : alkyl (optionally substituted by OH, alkoxy, NR3R4, heterocycloalkyl, heteroaryl or phenyl (optionally substituted)), cycloalkyl or H, where alkyl(alk) or alkoxy comprising 1-6C; and R3R4 : alkyl (optionally substituted by OH, alkoxy, heterocycloalkyl, heteroaryl or phenyl (optionally substituted)), cycloalkyl or H; or NR1R2 : 3-10 membered cyclic radical or optionally heteroatoms of O, S, N or NH; or NR3R4 : 3-10 membered cyclic radical or optionally heteroatoms of O, S, N or NH; or NR1R2, NR3R4 : cyclic radical optionally substituted by halo, OH, oxo, alkoxy, NH 2, NHalk, N(alk) 2, alkyl, phenyl, CH 2-phenyl or heteroaryl, such as alkyl, phenyl or heteroaryl optionally substituted by halo, OH, alkyl, 1-4C alkoxy, NH 2, NHalk or N(alk) 2. Provided that when: Rc is cycloalkyl, then it is optionally substituted by aryl or heteroaryl (both optionally substituted) or heterocycloalkyl; and Rc is alkyl, then it is optionally substituted by optionally substituted heterocycloalkyl. Where the: alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted by halo, OH, alkoxy, CN, CF 3, -NR1R2, -COOH, -COOalk, -CONR1R2 or -NR1COR2; alkyl is optionally substituted by a radical, aryl or heteroaryl, which is optionally substituted by halo, OH, alkyl or NR3R4; and cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted by alkyl, which is optionally substituted by halo, ...

5H-indeno [1,2-b] pyrazine-2,3-dione derivatives, their preparation and drugs containing them.

5H, 10H-imidazo [1,2-a] indeno [1,2-e] pyrazine-4-one derivatives, their preparation and the medicaments containing them.

Composés de formule: (CF DESSIN DANS BOPI) dans laquelle R représente un atome d'hydrogène ou d'halogène ou un radical alkyle, nitro, imidazolyle ou cyano, leur préparation, les intermédiaires pour les préparer et les médicaments les contenant.

Imidazo [1,2-a] pyrazine-4-one derivatives, their preparation and drugs containing them.

ANTISEROTONINS, THEIR PREPARATION AND THE MEDICINES CONTAINING THEM.

1,2,4-Triazolo (4,3-a) pyrazine-4-one derivatives, their preparation and the medicaments containing them.

New 6-triazolopyridazine-sulfanyl benzothiazole compounds are met kinase inhibitors useful for treating e.g. metabolic disorders, allergies, asthma, thrombosis, nervous system diseases, retinopathy, psoriasis, diabetes and cancers

L'invention concerne les nouveaux produits de formule (I): avec R1 représente alkyle, cycloalkyle ou cycloalkylalkyle ; Rb représente un atome d'hydrogène ou bien atome de fluor W représente H; alkyle, cycloalkyle, hétérocycloalkyle ou COR avec R représente cycloalkyle, hétérocycloalkyle, alkyle ; alcoxy, -O-hétérocycloalkyle ; ou NHR2 avec R2 représente H, cycloalkyle, hétérocycloalkyle ou alkyle ; tous éventuellement substitués ; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de MET.

Epoxides, their preparation and their use

Compounds of formula: in which R1 and R2, which are identical or different, represent hydrogen or fluorine atoms or alkyl, alkoxy or dialkylamino radicals, process for their preparation and their use.

NOVEL TRIAZOLO®4,3-A! PYRIDINE DERIVATIVES, PROCESS FOR THEIR PREPARATION, THEIR USE AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS

New 6-triazolopyridazine-sulfanyl benzothiazole compounds are met kinase inhibitors useful for treating e.g. metabolic disorders, allergies, asthma, thrombosis, nervous system diseases, retinopathy, psoriasis, diabetes and cancers

6-Triazolopyridazine-sulfanyl benzothiazole compounds (I) and their isomeric forms, racemates, enantiomers, diastereoisomers, or addition salts with inorganic or organic acids or bases, are new. 6-Triazolopyridazine-sulfanyl benzothiazole compounds of formula (I) and their isomeric forms, racemates, enantiomers, diastereoisomers, or addition salts with inorganic or organic acids or bases, are new. R1 : alkyl, cycloalkyl or cycloalkylalkyl (al optionally substituted); R1b : H or F; W1 : alkyl, cycloalkyl or heterocycloalkyl (all optionally substituted by optionally substituted alkoxy, optionally substituted heterocycloalkyl or NR3R4), H or COR; R : cycloalkyl, heterocycloalkyl or alkyl (all optionally substituted by one or more cycloalkyl, heterocycloalkyl, heteroaryl, phenyl or NR3R4 (all optionally substituted), halo, OH or alkoxy), alkoxy (optionally substituted by optionally substituted alkyl, heterocycloalkyl or NR3R4), -O-heterocycloalkyl (optionally substituted), or NHR2; R2 : heterocycloalkyl, heteroaryl, phenyl or NR3R4 (all optionally substituted), cycloalkyl, heterocycloalkyl or alkyl (all optionally substituted by OH or alkoxy); either R3, R4 : alkyl, cycloalkyl, heterocycloalkyl, phenyl or heteroaryl (all optionally substituted by one or more OH, alkoxy, NH 2, NHAlk, N(Alk) 2or heterocycloalkyl), or heteroaryl or phenyl (both optionally substituted), or H; or NR3R4 : 3-10 membered ring containing optionally one or more other heteroatoms of O, S, N or NH, optionally S, optionally in the form of SO or SO 2, where the ring includes optional -NH- , which is optionally substituted; R5, R5a : alkyl or cycloalkyl (both optionally substituted by one or more halo or OH), 1-4C alkyl, 1-4C alkoxy, NH 2, NHAlk or N(Alk) 2group; and Alk, alkyl : 1-10C alkyl, where all the cycloalkyl groups are not more than 3-7C cycloalkyl groups. Where all the alkyl, cycloalkyl, heterocycloalkyl, -O-heterocycloalkyl, heteroaryl and phenyl groups in R3 and R4 may form with the ...

INDENO [1,2-E] PYRAZIN-4-ONES, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

HYDRAZINOCARBONYL-THIENO [2,3-C] PYRAZOLES, PROCESS FOR THEIR PREPARATION, COMPOSITIONS CONTAINING SAME AND USE THEREOF

Hydrazinocarbonyl-thiéno[2,3-c]pyrazoles, procédé de préparation, compositions les contenant, et utilisation. La présente invention concerne notamment la préparation d'hydrazinocarbonyl-thiéno[2,3-c]pyrazoles, leur procédé de préparation, des compositions les contenant, et leur utilisation comme médicament, en particulier en tant qu'agents anticancéreux. Hydrazinocarbonyl-thieno [2,3-c] pyrazoles, process for their preparation, compositions containing them, and use. The present invention relates in particular to the preparation of hydrazinocarbonyl-thieno [2,3-c] pyrazoles, to a process for their preparation, to compositions containing them, and to their use as a medicament, particularly as anti-cancer agents.

EPOXIDES, THEIR PREPARATION AND THEIR USE.

6-(alkyl- or cycloalkyl-triazolopyridazine-sulfanyl) benzothiazole derivatives: preparation, application as medicaments and use as met inhibitors

The invention relates to the novel products of formula (I); where R 1 represents alkyl, cycloalkyl or cycloalkylalkyl; Rb represents a hydrogen atom or else a fluorine atom; W represents H; alkyl, cycloalkyl, heterocycloalkyl or COR where R represents cycloalkyl, heterocycloalkyl, alkyl; alkoxy, -O-heterocycloalkyl; or NHR 2 where R 2 represents H, cycloalkyl, heterocycloalkyl or alkyl; all optionally substituted; these products being in any isomer form, and the salts thereof, as medicaments, especially as MET inhibitors.

Azaindoles.

Azaindoles for inhibiting aurora2 and other kinases

The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

10H-IMIDAZO (1,2-A) INDENO (1,2-E) PYRAZIN-4-ONE DERIVATIVES, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

5h-indeno[1,2-b]pyrazine-2,3-dione derivaties, preparation thereof and drugs containing same

Novel substituted indazoles, the preparation thereof and use of same in therapeutics

This disclosure relates to compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , E, and n 1 are as defined in the disclosure, to compositions containing them, to processes for preparing them, and the use thereof.

New di:hydro-benzothiadiazine di:oxide carboxylic acid derivs.

3,4-Dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide- 3-carboxylic acid derivs. of formula (I), their racemates, enantiomers and metal or nitrogen contg. base addn. salts are new. R = H, alkyl, allyl, phenyl, 2- or 3-pyridylalkyl, 2-quinolylalkyl, naphthylalkyl, cycloalkylalkyl, 2H-3-naphtho-(1,8-ca)-isothiazl-2-yl-1,1-dioxide)alkyl, 15,6-dihydro- 1H,4H-1,2,5-thiadiazolo(4,3,2-ij)quinolyl- 2,2-dioxide)alkyl, alk-COR5, alkR6R7, 4-phenyl- piperazinylalkyl (opt. phenyl ring. subsd. by halo, alkyl and.or alkoxy), 10-phenothiazinylalkyl, (10-alkyl-2-phenothiazinyl)alkyl, 3-indolylalkyl, phenylalkyloxy, 1-phenylalkyl-4-piperidyl, 2-thienylalkyl or phenyalkyl (opt. ring substd.); R1 = COOH, alkoxycarbonyl, tetrazolyl, CONH2, CONHalk, CON(alk)2, CONHOH, CON(alk)OH, CONHOR8, CON(alk)OR8 or a gp. convertible in vivo to carboxy; R2-R4 = H, halo, alkyl or alkoxy; R5 = OH, alkoxy, phgenyl or NR9R10; R6 = O, S, N, S, SO2 or Nalk; R7 = alkyl, phenylalkyl, or phenyl opt. substd. by one or more halo; R89 = alkyl or phenylalkyl; R9, R10 = H, alkyl or phenyl; alk = alkyl or alkylene; alkyl, alkoxy or alkylene contain 1-10C.

NOVEL IMIDAZO [1,2-A] PYRIDINE DERIVATIVES, PREPARATION METHOD, MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND USE IN PARTICULAR AS MET INHIBITORS

2-Aminothiazoline derivatives and their use as no-synthase inhibitors.

5H, 10H-imidazo(1,2-a)indeno(1,2-e)pyrazin-4-one derivatives their preparation and the medicaments containing them

5H-indeno [1,2-b] pyrazine-2,3-dione derivatives, as well as medicaments containing the compounds

Imidazole [1,2-αApyrazin-4-one, preparation thereof and drug containing the compound

AMP AND NMDA RECEPTOR ANTAGONISTS, THEIR NTERMEDIARY PREPARATION AND MEDICINES THAT CONTAIN THEM

Substituted indazoles, compositions containing them, method of production and use

Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology.

Substituted indazoles, the preparation thereof, and use of same in therapeutics

The invention relates to compounds of formula (I) wherein: E is a grouping (i) of formula -NT-CO-O- or -NT-CX-NT'- wherein X is =O or =S and T and T', that can be identical or different and selected independently, from H or an alkyl group, or (ii) forming a five-membered or six-membered ring bound in position 5 or 6 of the indazole nucleus by -NT- or by the nitrogen atom N1; R1 is at least one substituent selected independently when there are several, and being a halogen atom, an alkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalcoxy, aryl, heteroaryl, heterocycloalkyl, cycloalkyl, CN, NRR', OR, NO2, COOR, CONRR', or NRCOR' group; R2 is a hydrogen atom, or an alkyl, alkenyl or alkynyl group; R3 is at least one substituent selected independently when there are several, and being a hydrogen atom, an alkyl, alkenyl, alkynyl, halogenoalcoxy, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, CN, NRR', CF3, OR, NO2, COOR, CONRR', or NRCOR' group; R4 is a hydrogen atom or a halogen atom, an alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycloalkyl, -NR-CO-R', COOR, NRR', CHO, or CONR(OR') group; R and R' are identical or different and are independently a hydrogen atom, or an alkyl, aryl, heterocycloalkyl, cycloalkyl or heteroaryl group; and n1 is a whole number between 0 and 5, and n3 is a whole number between 0 and 3.

Imidazo [1,2-a] pyrazin-4-one derivatives, their preparation and medicines containing them

2-aminothiazoline derivatives and their use as no-synthase inhibitors.

3,4-dihydro-2h-1,2,4-benzothiadiazine-1,1-dioxide-3-carboxylic acid derivatives, preparation thereof and drugs containing same

Compounds of formula (I), wherein R is (a) a hydrogen atom, (b) an alkyl radical, (c) an allyl radical, (d) a phenyl radical, (e) a 2-or-3-pyridyl alkyl radical, (f) a 2-quinolylalkyl radical, (g) a naphthylalkyl radical, (h) a cycloalkylalkyl radical, (i) a 2H-3-naphtho[1,8-cd]isothiazol-2-yl-1,1-dioxide)alkyl radical, (j) a (5,6-dihydro 1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolyl-2,2-dioxide)alkyl, (k) an -alk-CO-R5 radical, (l) an -alk-R6-R7 radical, (m) a 4-phenylpirerazinyl-alkyl radical wherein the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl or alkoxy radicals, (n) a 10-phenothiazinylalkyl radical (o) a (10-alkyl-2-phenothiazinyl)alkyl radical, (p) a 3-indolylalkyl radical, (q) a phenylalkyloxy radical, (r) a 1-phenylalkyl-4-piperidyl radical, (s) a 2-thienylalkyl radical, or (t) a phenylalkyl radical wherein the phenyl is unsubstituted or substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, amino, nitro, cyano, phenyl, vinyl, polyfluoroalkoxy, alkoxycarbonyl, carboxy, phenylalkyloxy, phenylalkyl, benzoylamino, phenylcarbonyl and phenoxy radicals in which the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy or polyfluoroalkyl radicals; R1 is a carboxy, alkoxycarbonyl, tetrazolyl, -CO-NH2, -CO-NH-alk, -CO-N(alk)2, -CO-NHOH, -CO-N(alk)OH, -CO-NH-O-R8, -CO-N(alk)-OR8 or a group which is convertible in vivo into a carboxy radical; each of R2, R3 and R4, which are the same or different, is a hydrogen or halogen atom or an alkyl or alkoxy radical; R5 is a hydroxy, alkoxy, phenyl or -NR9R10 radical; R6 is an oxygen, sulphur or nitrogen atom or a SO, SO2 or -N-alk radical, R7 is an alkyl, phenylalkyl or phenyl radical optionally substituted by one or more hydrogen atoms; R8 is an alkyl or phenylalkyl radical; each of R9 and R10, which are the same or different, is a hydrogen atom or an alkyl ...

DERIVATIVES OF 5H-INDENO (1,2-B) -PIRAZINE-2,3-DIONA, ITS PREPARATION AND THE MEDICINES THAT CONTAIN THEM.

COMPUESTO DE FORMULA (I) EN LA QUE R, R 1 , R 2 Y R{SUB,3} SON TALES COMO SE DEFINEN EN LA DESCRIPCION, SUS SALES, SU PREPARACION Y LOS MEDICAMENTOS QUE LOS CONTIENEN. LOS COMPUESTOS DE FORMULA (I) PRESENTAN PROPIEDADES FARMACOLOGICAS INTERESANTES. ESTOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE ACIDO {AL}-AMINO-3-HIDROXI-5-METIL-4-ISOXAZOLEPROPIONICO (AMPA), TAMBIEN CONOCIDO BAJO EL NOMBRE DE RECEPTOR DE QUISCALATO. POR OTRA PARTE, LOS COMPUESTOS DE FORMULA (I) SON ANTAGONISTAS NO COMPETITIVOS DEL RECEPTOR N-METIL-D-ASPARTATO (NMDA) Y, MAS EN PARTICULAR, SON LIGANDOS PARA SITIOS MODULADORES DE LA GLICINA DEL RECEPTOR NMDA. COMPOSED OF FORMULA (I) IN WHICH R, R 1, R 2 AND R {SUB, 3} ARE SUCH AS DEFINED IN THE DESCRIPTION, THEIR SALTS, THEIR PREPARATION AND THE MEDICINES CONTAINING THEM. THE COMPOUNDS OF FORMULA (I) PRESENT INTERESTING PHARMACOLOGICAL PROPERTIES. THESE COMPOUNDS ARE ANTAGONISTS OF THE ACID RECEPTOR {AL} -AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONICO (AMPA), ALSO KNOWN UNDER THE NAME OF RECEIVER OF CHYSCALATE. ON THE OTHER HAND, THE FORMULA (I) COMPOUNDS ARE NON-COMPETITIVE ANTAGONISTS OF THE N-METHYL-D-ASPARTATE (NMDA) RECEPTOR AND, MORE IN PARTICULAR, ARE LIGENDOUS FOR MODULATOR SITES OF THE GLYCINE OF THE NMDA RECEPTOR.

Azaindoles

THE INVENTION IS DIRECTED TO PHYSIOLOGICALLY ACTIVE COMPOUNDS OF GENERAL FORMULA (I):- AND COMPOSITIONS CONTAINING SUCH COMPOUNDS; AND THEIR PRODRUGS, AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES OF SUCH COMPOUNDS AND THEIR PRODRUGS, AS WELL AS TO NOVEL COMPOUNDS WITHIN THE SCOPE OF FORMULA (I). SUCH COMPOUNDS AND COMPOSITIONS HAVE VALUABLE PHARMACEUTICAL PROPERTIES, IN PARTICULAR THE ABILITY TO INHIBIT KINASES.

Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, preparation method, compositions containing same and use

The invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles, their preparation method, compositions containing same and use thereof. In particular, the invention concerns the preparation of hydrazinocarbonyl-thieno[2,3-c]pyrazoles, their preparation method, compositions containing same, and their use as medicine, in particular as anticancer agents.

Imidazo(1,2-a)indeno(1,2-e)pyrazine-4-one derivatives and pharmaceutical compositions containing same

Pharmaceutical compositions containing, as the active principle, compounds of formula (I), wherein R, R1 and R2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

Antiserotonines, prepartion thereof and medicaments containing them

Compounds having the formula R1-(CH2)n-Het wherein R1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy ou hydroxy radical; a radical phenyl-4 piperidino whose phenyl cyle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical. R3 is a hydrogen atom or a phenyl radical; R4 is a hydrogen or halogen atom or a residue Het; R5 is a carbonyl or sulfonyl radical; R6 is a radical Si(CH3)2 or C(CH3)2; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.

Derivatives of 6-(6-o-substituted-triazolopyridazine-sulfanyl) benzothiazoles and benzimidazoles, preparation thereof, use thereof as drugs, and use thereof as met inhibitors.

La invención se refiere a los nuevos productos de fórmula (I) en la que representa un enlace sencillo o doble; Ra representa -O-Z-Rc en el que Z es un enlace sencillo o alquileno opcionalmente sustituido y Rc representa cicloalquilo, heterocicloalquilo, arilo o heteroarilo opcionalmente sustituidos; Rb representa H o F; de forma que si Rb es H, entonces Rc no es cicloalquilo cuando Z es un enlace sencillo y Rc no es heterocicloalquilo cuando Z es alquileno X representa S, SO o SO2. A representa NH o S; W representa H, alquilo, cicloalquilo o COR en el que R representa cicloalquilo; alquilo; alcoxi; O-fenilo ; -O-(CH2)n-fenilo con n= 1 a 4 ; o NR1 R2 en el que R1 representa H o alk y R2 representa H, cicloalquilo o alquilo; o bien R1, R2 forman con N un ciclo que tiene opcionalmente O, S, N y/o NH; estando todos estos radicales opcionalmente sustituidos; estando estos productos en todas las formas de isómeros y sales, como medicamentos, principalmente como inhibidores de MET.

5h,10h-imidazo[1,2-a]indeno[1,2-e]pyrazin-4-one derivatives, intermediates,preparation and use thereof, and drugs containing said derivatives

4-hydroxy-3-phenylindeno[1,2-b]pyridin-2(1H)-one derivatives their preparation and the medicaments containing them

Azaindoles

Substituted indazoles, compositions containing them, method of production and use

Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology.

2-Aminothiazoline derivatives and their use as no-synthase inhibitors.

New triazolo(4,3-a)pyridine derivatives are Met protein kinase inhibitors useful to treat e.g. fibrotic disorders, metabolic disorders, allergies, asthma, thrombosis, retinopathy, psoriasis, rheumatoid arthritis, diabetes and cancer

Triazolo(4,3-a)pyridine derivatives (I) and their all possible isomeric forms, racemates, enantiomers and diastereoisomers, and addition salts with organic or inorganic acid and bases, are new. Triazolo(4,3-a)pyridine derivatives of formula (I) and their all possible isomeric forms, racemates, enantiomers and diastereoisomers, and addition salts with organic or inorganic acid and bases, are new. R1a : aryl or heteroaryl (both optionally substituted), H or halo; R1b : H, R1c, -COOR1c, CO-R1c or CO-NR1cR1d; R1c : alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted); one of R 1> and R 2> : H or alkyl; and other of R 1> and R 2> : cycloalkyl or alkyl (both optionally substituted by one or more OH, alkoxy, NR 3>R 4>, heterocycloalkyl, heteroaryl or phenyl (all optionally substituted)) or H; or NR 1>R 2> : 3-10 membered ring optionally containing one or more other heteroatoms(s) comprising O, S, N or NH, and including the possible substituted NH group; one of R 3> and R 4> : H or alkyl; and other of R 3> and R 4> : H, cycloalkyl or alkyl (optionally substituted by one or more OH, alkoxy, heterocycloalkyl, heteroaryl or phenyl (all optionally substituted)); or NR 1>R 2> : 3-10 membered ring optionally containing one or more other heteroatoms(s) comprising O, S, N or NH, and including the possible substituted NH group; and R1d : alkyl, cycloalkyl or H, where the cycloalkyl, heterocycloalkyl, heteroaryl or aryl being optionally substituted by halo, OH, alkoxy, CN, CF 3, -NR 1>R 2>, COOH, -COOalk, -CONR 1>R 2>, -NR 1>COR 2> or heterocycloalkyl, alkyl and cycloalkyl being optionally substituted by one or more aryl or heteroaryl (both optionally substituted by one or more radicals of halo or OH, alkyl, alkoxy or NR 3>R 4>), alkyl and cycloalkyl being optionally substituted by one or more aryl or heteroaryl (both optionally substituted by one or more radicals of halo or OH, alkyl, ...

NEW IMIDAZO DERIVATIVES [1,2-A] PYRIMIDINE, ITS PREPARATION PROCEDURE, ITS APPLICATION AS MEDICINES, PHARMACEUTICAL COMPOSITIONS AND NEW USE IN PARTICULARLY AS MET INHIBITORS

LA INVENCIÓN SE REFIERE A LOS PRODUCTOS NUEVOS DE FORMULA (I): EN LA QUE: N = 0,1 Ó 2; X REPRESENTA H, HAL O ALK; R REPRESENTA H, NH2, NHALK, N(ALK)2; RA REPRESENTA H; HAL; -O-CICLOALQUILO; -O-ALQUILO, -O-ARILO; -O-HETEROARILO; -NRD(CICLOALQUILO); -NRD(ALQUILO); -NRD(ARILO); -NRD(HETEROARILO); ALQUILO; CICLOALQUILO; HETEROCICLOALQUILO; ARILO O HETEROARILO; TODOS OPCIONALMENTE SUSTITUIDOS; RB REPRESENTA H, RC, -COORC,-CO-RC O -CO-NRCRD; CON RC REPRESENTANDO ALQUILO, CICLOALQUILO, HETEROCICLOALQUILO, ARILO Y HETEROARILO, TODOS OPCIONALMENTE SUSTITUIDOS; RD REPRESENTA H, ALK O CICLOALQUILO; ESTANDO ESTOS PRODUCTOS EN TODAS LAS FORMAS ISÓMERAS Y LAS SALES, COMO MEDICAMENTOS PRINCIPALMENTE COMO INHIBIDORES DE MET

5H-INDENO[1,2-b]PYRAZINE-2,3-DIONE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME

Compounds of formula (I), wherein R, R1, R2 and R3 are as defined in the description, salts thereof, the preparation thereof and drugs containing same, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

5H, 10H-imidazole £ 1,2-a | indeno £ 1,2-epyrazin-4-one derivatives, drugs containing the compounds and intermediates for the preparation

NOVEL TRIAZOLO®4,3-A! PYRIDINE DERIVATIVES, PROCESS FOR THEIR PREPARATION, THEIR USE AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS

Imidazo [1,2-a] indeno [1,2-e] pyrazine-4-one derivatives, their preparation and drugs containing them.

Imidazo (1,2-A)-Indeno (1,2-E) pyrazin-4-one derivatives and pharmaceutical compositions containing same

Pharmaceutical compositions containing, as the active principle, compounds of formula (I): ##STR1## wherein R, R 1 and R 2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NDMA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

PHARMACEUTICAL COMPOUNDS AND COMPOSITIONS BASED ON AZAINDOLOS FOR INHIBITION OF KINASES

1.- Una composición farmacéutica que comprende compuestos de fórmula general (I): en la cual:R1 representa a arilo o heteroarilo, cada uno opcionalmente sustituido por uno o más grupos seleccionados entre alquilendioxi, alquenilo, alqueniloxi, alquinilo, arilo, ciano, halo, hidroxi, heteroarilo, heterocicloalquilo, nitro, R4, -C(=O)-R, -C(=O)-OR5, -C(=O)-NY1Y2, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, --N(R6)-SO2-R7, -SO2-NY1Y2 y -Z2R;R2 representa a hidrógeno, acilo, ciano, halo, alquenilo inferior, -Z2R4, -SO2-NY3Y4, -NY1Y2 o alquilo inferior opcionalmente sustituido por un sustituyente seleccionado entre arilo, ciano, heteroarilo, heterocicloalquilo, hidroxi, -Z2R4, -C(=O)-NY1Y2, -C(=O)-R, -CO2OR8, -NY3Y4, -N(R6)-C(=O)-R, -N(R6)-C(=O)-NY1Y2, -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -SO2-NY1Y2, y uno o más átomos de halógeno;R3 representa a hidrógeno, arilo, ciano, halo, heteroarilo, alquilo inferior, -Z2R4, -C(=O)-OR5 ó -C(=O)-NY3Y4;R4 representa a alquilo, cicloalquilo, heterocicloalquilo o heterocicloalquilalquilo, cada uno opcionalmente sustituido por un sustituyente seleccionado entre arilo, cicloalquilo, ciano, halo, heteroarilo, heterocicloalquilo, -CHO (o un acetal cíclico de 5, 6 ó 7 elementos derivado del mismo), -C(=O)-NY1Y2, -C(=O)-OR5, -NY1Y2, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4, -Z3R7 y uno o más grupos seleccionados entre hidroxi, alcoxi y carboxi;R5 representa a hidrógeno, alquilo, alquenilo, arilo, arilalquilo, heteroarilo o heteroarilalquilo;R6 representa a hidrógeno o alquilo inferior;R7 representa a alquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heteroarilo heteroarilalquilo;R8 representa a hidrógeno o alquilo inferior;R representa a arilo o heteroarilo; alquenilo; o alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo o heterocicloalquilalquilo, ... 1. A pharmaceutical composition comprising compounds of general formula (I ...

TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

5H-Indeno [1,2-b] pyrazine-2,3-dione derivatives, their preparation and medicines containing them

Derivatives of 5h, 10h-imodazo [1,2-a]indene [1,2-e]pyrazin-4-one, thir production and drugs containing them

HETEROCYCLIC ANTISEROTONIN DERIVATIVES, THEIR PREPARATION AND USE IN MEDICINES

4,5-dihydro-thiazo-2-ylamine derivatives and their use as no-synthase inhibitors

The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (I) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (I) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved abnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2).

IMIDAZO [1,2-a] INDENO [1,2-e] PYRAZIN-4-ONER DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM

triazolo (4,3-a) pyridine derivatives, their preparation process, their application as medicaments, pharmaceutical compositions and use notably as metal inhibitors

The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.

NEW IMIDAZO DERIVATIVES [1,2-a] PYRIMIDINE, ITS PREPARATION PROCEDURE, ITS APPLICATION AS MEDICINES, PHARMACEUTICAL COMPOSITIONS AND NEW USE IN PARTICULARLY AS MET INHIBITORS

La invención se refiere a los productos nuevos de fórmula (I): en la que: n = 0,1 ó 2; X representa H, Hal o alk; R representa H, NH2, NHalk, N(alk)2; Ra representa H; Hal; -O-cicloalquilo; -O-alquilo, -O-arilo; -O-heteroarilo; -NRd(cicloalquilo); -NRd(alquilo); -NRd(arilo); -NRd(heteroarilo); alquilo; cicloalquilo; heterocicloalquilo; arilo o heteroarilo; todos opcionalmente sustituidos; Rb representa H, Rc, -COORc,-CO-Rc o -CO-NRcRd; con Rc representando alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo, todos opcionalmente sustituidos; Rd representa H, alk o cicloalquilo; estando estos productos en todas las formas isómeras y las sales, como medicamentos principalmente como inhibidores de MET.

IMIDAZO DERIVATIVES (1,2-A) INDENO (1,2-E) PIRAZINA-4-ONA AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

COMPOSICIONES FARMACEUTICAS QUE CONTIENEN COMO PRINCIPIO ACTIVO COMPUESTOS DE FORMULA: (I) EN LA QUE R, R{SUB,1} Y R{SUB,2} SON TALES COMO SE DEFINEN EN LA DESCRIPCION O SUS SALES, LOS NUEVOS COMPUESTOS DE FORMULA (I) Y SU PREPARACION. LOS COMPUESTOS DE FORMULA (I) PRESENTAN PROPIEDADES FARMACOLOGICAS INTERESANTES. ESTOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DEL ACIDO {AL}AMINO-3-HIDROXI-5-METIL-4-ISOXAZOLEPROPIONICO (AMPA), TAMBIEN CONOCIDO BAO EL NOMBRE DE RECEPTOR DE QUISCALATO. POR OTRA PARTE, LOS COMPUESTOS DE FORMULA (I) SON ANTAGONISTAS NO COMPETITIVOS DEL RECEPTOR N-METIL-D-ASPARTATO (NMDA), Y MAS EN PARTICULAR, SON LIGANDOS PARA LOS SITIOS MODULADORES DE LA GLICINA DEL RECEPTOR NMDA. PHARMACEUTICAL COMPOSITIONS CONTAINING THE FORMULA COMPOUNDS AS ACTIVE PRINCIPLE: (I) IN WHICH R, R {SUB, 1} YR {SUB, 2} ARE SUCH AS DEFINED IN THE DESCRIPTION OR ITS SALTS, THE NEW FORMULA COMPOUNDS (I ) AND HIS PREPARATION. THE FORMULA COMPOUNDS (I) PRESENT INTERESTING PHARMACOLOGICAL PROPERTIES. THESE COMPOUNDS ARE ANTAGONISTS OF THE ACID RECEIVER {AL} AMINO-3-HYDROXI-5-METHYL-4-ISOXAZOLEPROPIONIC (AMPA), ALSO KNOWN BY THE QUISCALATE RECEIVER NAME. On the other hand, the FORMULA COMPOUNDS (I) ARE NON-COMPETITIVE ANTAGONISTS OF THE N-METHYL-D-ASPARTATE RECEIVER (NMDA), AND MORE IN PARTICULAR, ARE LIGHTING FOR THE MODULATING SITES OF THE NMDA RECEIVER GLICINE.

NEW IMIDAZO DERIVATIVES [1,2-a] PYRIMIDINE, ITS PREPARATION PROCEDURE, ITS APPLICATION AS MEDICINES, PHARMACEUTICAL COMPOSITIONS AND NEW USE IN PARTICULARLY AS MET INHIBITORS

La invención se refiere a los productos nuevos de fórmula (I): en la que:n =0,1 ó 2; x representa H, Hal o alk; R representa H, NH2, NHalk, N(alk)2; Ra representa H; Hal; -O-cicloalquilo; -O-alquilo, -O-arilo; -O-heteroarilo; -NRd(cicloalquilo); -NRd(alquilo); -NRd(arilo); -NRd(heteroarilo); alquilo; cicloalquilo; heterocicloalquilo; arilo o heteroarilo; todos opcionalmente sustituidos.

2-aminothiazoline derivatives and their use as NO synthase inhibitors

1,2,4-benzothiadiazine-3-carboxylic acid derivatives, their preparation and their use

Substituted azaindoles as inhibitors of protein kinases, and process for their preparation

Physiologically active substituted azaindole compounds of general formula (I); compositions containing such compounds; their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs are disclosed, wherein the variables shown in formula (I) are as defined in the specification. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases, whereby these compounds are suitable for use in the treatment of disease states capable of being modulated by the inhibition of the protein kinases.

Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and the ir prodrugs, as well as to novel compounds within the scope of formula (I). Suc h compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles

The invention is directed to compounds of general formula (I):- and pharmaceutically acceptable salts and solvates of such compounds. Such compounds have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

5H-indeno 1,2-b!pyrazine-2,3-dione derivatives, their preparation and medicinal products containing them

Compounds of formula (I): ##STR1## wherein R represents a CR 4 R 5 , CHR 6 , or C═R 7 radical and R 3 represents an oxygen atom, salts thereof, the preparation thereof and drugs containing same. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-osoxaziepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

Novel imidazo[1,2-a]pyridine derivatives, process for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use, in particular as MET inhibitors