公开(公告)号：WO02100862A3

公开(公告)日：2003-02-27

申请号：PCT/EP0206576

申请日：2002-06-11

Applicant: JANSSEN PHARMACEUTICA NV ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  VAN REEMPTS JOS

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  VAN REEMPTS JOS

IPC: A61K9/10 ,  A61K31/00 ,  A61K31/519 ,  A61K31/55 ,  A61P3/00 ,  A61P7/10 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro- 6 H - benzimidazo[2,1 -b][3]benzazepin-6-yl) -2-(phenylmethyl)- 1-piperidinyl]ethyl] -2,10-dimethyl pyrimido[1, 2- a ]benzimidazol- 4(10 H )-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof.

Abstract translation: 本发明涉及可用于治疗升高的颅内压（ICP）和/或继发性缺血的新型取代的四环咪唑衍生物，特别是由脑损伤引起的，特别是由创伤性（TBI）和非创伤性脑损伤引起的 其制备方法，包含它们的药物组合物及其作为药物的用途。 新化合物包括根据通式（I）的化合物，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。 特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基）-2-（苯基甲基） - 哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和N-氧化物形式 它们。

公开(公告)号：CY1107472T1

公开(公告)日：2012-12-19

申请号：CY071101471

申请日：2007-11-14

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TEGTMEIER FRANK ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  VAN REEMPTS JOZEF LEO HENRI

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00

Abstract: Ηεφεύρεσηαφοράένανέοανταγωνιστήυποδοχέαισταμίνηςκαιτηχρήσηενόςανταγωνιστήυποδοχέαισταμίνηςγιατημείωσητηςενδοκρανιακήςπίεσης (ΕΚΠ), συγκεκριμέναγιατηπρόληψηκαιτηθεραπείατηςαυξημένηςενδοκρανιακήςπίεσηςκαι/ήδευτερεύουσαςισχαιμίας, πουπροκαλείταισυγκεκριμένααπόεγκεφαλικότραυματισμό, πιοσυγκεκριμέναπροκαλείταιαπότραυματικό (ΤΕΤ) καιμητραυματικόεγκεφαλικότραυματισμό. ΟινέεςενώσειςπεριλαμβάνουνενώσειςσύμφωναμετογενικόΤύπο (I) ταφαρμακευτικάαποδεκτάάλαταπρόσθεσηςοξέοςή βάσεωςαυτού, τιςστερεοχημικάισομερείςμορφέςαυτούκαιτημορφήΝ-οξειδίουαυτού. Συγκεκριμένα, ηπροτιμώμενηένωσηείναι 3-[2-[4-(11,12-διυδρο-6H-βενζιμιδαζο[2,1-b][3]βενζαζεπιν-6-υλ)-2-(φαινυλ-μεθυλ)-1-πιπεριδινυλ]αιθυλ]-2,10-διμεθυλπυριμιδο[1,2-α]βενζιμιδαζολ-4(10H)-όνη, ταφαρμακευτικάαποδεκτάάλαταπρόσθεσηςοξέοςή βάσεωςαυτής, οιστερεοχημικάισομερείςμορφέςαυτήςκαιη μορφήΝ-οξειδίουαυτής. Επίσηςαξιώνεταιη νέαχρήσηεμπορικάδιαθέσιμωνανταγωνιστώνυποδοχέαισταμίνης H1-καιΗ2 γιατημείωσητηςενδοκρανιακήςπίεσης (ΕΚΠ).

公开(公告)号：PT1832287E

公开(公告)日：2009-05-05

申请号：PT07107669

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  TEGTMEIER FRANK ,  ROSSEM KOENRAAD ARTHUR VAN ,  REEMPTS JOZEF LEO HENRI VAN ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  FERNANDEZ-GADEA FRANCISCO JAVI

IPC: A61P9/10 ,  C07D487/04 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00 ,  C07D519/00

公开(公告)号：PL369864A1

公开(公告)日：2005-05-02

申请号：PL36986402

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TEGTMEIER FRANK ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  VAN REEMPTS JOZEF LEO HENRI

IPC: C07D487/04 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00 ,  C07D519/00

Abstract: The invention concerns the use of an H1- and/or H2-histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. In particular, the histamine antagonist is selected from the group of acrivastine, alimemazine, antazoline, astemizole, azatadine, azelastine, brompheniramine, buclizine, carbinoxamine, carebastine, cetirizine, chlorcyclizine, chlorpheniramine, cinnarizine, clemastine, clemizole, clocinizine, clonidine, cyclizine, cyproheptadine, descarboethoxyloratidine, dexchlorpheniramine, dimenhydrinate, dimethindene, dimethothiazine, diphenhydramine, diphenylpyraline, doxylamine, ebastine, efletirizine, epinastine, fexofenadine, hydroxyzine, ketotifen, levocabastine, loratidine, meclizine, mequitazine, methdilazine, mianserin, mizolastine, niaprazine, noberastine, norastemizole, oxatomide, oxomemazine, phenbenzamine, pheniramine, picumast, promethazine, pyrilamine, temelastine, terfenadine, trimeprazine, tripelennamine, triprolidine, ranitidine, cimetidine, famotidine, nizatidine, tiotidine, zolantidine, ritanserine, and derivatives thereof and mixtures of any two or more of the foregoing.

公开(公告)号：NO20042618L

公开(公告)日：2004-06-22

申请号：NO20042618

申请日：2004-06-22

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ALCAZAR-VACA MANUEL JESUS ,  BARTOLOME-NEBREDA JOSE MANUEL ,  MARTINEZ-JIMENEZ PEDRO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  TEGTMEIER FRANK ,  ROSSEM KOENRAAD ARTHUR VAN ,  REEMPTS JOZEF LEO HENRI VAN

IPC: C07D487/04 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00 ,  C07D519/00

Abstract: The invention concerns the use of an H1- and/or H2-histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. In particular, the histamine antagonist is selected from the group of acrivastine, alimemazine, antazoline, astemizole, azatadine, azelastine, brompheniramine, buclizine, carbinoxamine, carebastine, cetirizine, chlorcyclizine, chlorpheniramine, cinnarizine, clemastine, clemizole, clocinizine, clonidine, cyclizine, cyproheptadine, descarboethoxyloratidine, dexchlorpheniramine, dimenhydrinate, dimethindene, dimethothiazine, diphenhydramine, diphenylpyraline, doxylamine, ebastine, efletirizine, epinastine, fexofenadine, hydroxyzine, ketotifen, levocabastine, loratidine, meclizine, mequitazine, methdilazine, mianserin, mizolastine, niaprazine, noberastine, norastemizole, oxatomide, oxomemazine, phenbenzamine, pheniramine, picumast, promethazine, pyrilamine, temelastine, terfenadine, trimeprazine, tripelennamine, triprolidine, ranitidine, cimetidine, famotidine, nizatidine, tiotidine, zolantidine, ritanserine, and derivatives thereof and mixtures of any two or more of the foregoing.

公开(公告)号：PL186541B1

公开(公告)日：2004-01-30

申请号：PL32687197

申请日：1997-04-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE I ,  MARTINEZ-JIMENEZ PEDRO ,  FERNANDEZ-GADEA FRANCISCO J ,  SIPIDO VICTOR K

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/553 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/16 ,  A61K31/424 ,  A61P25/30

Abstract: PCT No. PCT/EP97/01830 Sec. 371 Date Oct. 6, 1998 Sec. 102(e) Date Oct. 6, 1998 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/39001 PCT Pub. Date Oct. 23, 1997This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or trihalomethyl; X is CR6R7, NR8, O, S, S(=O) or S(=O)2; each independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

公开(公告)号：ES2182064T3

公开(公告)日：2003-03-01

申请号：ES97919344

申请日：1997-04-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  MARTINEZ-JIMENEZ PEDRO ,  FERNANDEZ-GADEA FRANCISCO ,  SIPIDO VICTOR KAREL

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/553 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/16

Abstract: PCT No. PCT/EP97/01830 Sec. 371 Date Oct. 6, 1998 Sec. 102(e) Date Oct. 6, 1998 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/39001 PCT Pub. Date Oct. 23, 1997This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or trihalomethyl; X is CR6R7, NR8, O, S, S(=O) or S(=O)2; each independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

公开(公告)号：DK0892804T3

公开(公告)日：2002-12-02

申请号：DK97919344

申请日：1997-04-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  MARTINEZ-JIMENEZ PEDRO ,  FERNANDEZ-GADEA FRANCISCO ,  SIPIDO VICTOR KAREL

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/553 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/16

Abstract: PCT No. PCT/EP97/01830 Sec. 371 Date Oct. 6, 1998 Sec. 102(e) Date Oct. 6, 1998 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/39001 PCT Pub. Date Oct. 23, 1997This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or trihalomethyl; X is CR6R7, NR8, O, S, S(=O) or S(=O)2; each independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

公开(公告)号：CY1115353T1

公开(公告)日：2017-01-04

申请号：CY141100471

申请日：2014-06-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSÉ MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  VAN REEMPTS JOS

IPC: C07D471/04 ,  A61K9/10 ,  A61K31/00 ,  A61K31/519 ,  A61K31/55 ,  A61P3/00 ,  A61P7/10 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D519/00

Abstract: Ηεφεύρεσηαφοράσενέαπαράγωγαυποκατεστημένηςτετρακυκλικήςιμιδαζόληςχρήσιμαγιατηθεραπευτικήαντιμετώπισητηςαυξημένηςενδοκρανιακήςπίεσης (ICP) και/ήτηςδευτερογενούςισχαιμίας, συγκεκριμέναεκείνηςπουπροκαλείταιαπόεγκεφαλικήβλάβη, πιοσυγκεκριμέναεκείνηςπουπροκαλείταιαπότραυματική (TBI) καιμητραυματικήεγκεφαλικήβλάβη, διαδικασίεςγιατηνπαρασκευήτους, φαρμακευτικέςσυνθέσειςπουταπεριέχουνκαιτηχρήσητουςωςφάρμακο. ΟινέεςενώσειςπεριλαμβάνουνενώσειςσύμφωναμετογενικόΤύπο (I), ταφαρμακευτικώςαποδεκτάάλαταπρόσθεσηςοξέοςή βάσηςαυτών, τιςστερεοχημικάισομερείςμορφέςαυτώνκαιτιςμορφέςΝ-οξειδίουαυτών. Συγκεκριμένα, ηπροτιμώμενηένωσηείναι 3-[2-[4-(11,12-διυδρο-6Η-βενζιμιδαζο[2,1- b][3]βενζαζεπιν-6-υλ)-2-(φαινυλμεθυλ)-1-πιπεριδινυλ]αιθυλ]-2,10-διμεθυλπυριμιδο[1,2-α]βενζιμιδαζολ-4(10Η)-όνη, ταφαρμακευτικώςαποδεκτάάλαταπρόσθεσηςοξέοςή βάσηςαυτής, οιστερεοχημικώςισομερείςμορφέςαυτήςκαιη μορφήΝ-οξειδίουαυτής.

公开(公告)号：ES2475240T3

公开(公告)日：2014-07-10

申请号：ES02748780

申请日：2002-06-11

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESÚS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSÉ MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  VAN REEMPTS JOS

IPC: C07D471/04 ,  A61K9/10 ,  A61K31/00 ,  A61K31/519 ,  A61K31/55 ,  A61P3/00 ,  A61P7/10 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D519/00

Abstract: Compuesto según la fórmula general (I), **Fórmula** las sales de adición de ácido o base farmacéuticamente aceptables del mismo, las formas estereoquímicamente isoméricas del mismo y la forma de N-óxido del mismo, en la que: m es 1; n es 1; a, b, c son independientemente un enlace sencillo o uno doble; X es un radical alcanodiilo C1-5 bivalente en el que uno o más grupos -CH2- pueden estar opcionalmente sustituidos con -CO-, o -NR7- en el que R7 es alquilcarbonilo Y es -CH2-, -CH2-CH2- o -CH>=CH-; Z es N, en cuyo caso a es un doble enlace y b es un enlace sencillo, o es NR7 en cuyo caso a es un enlace sencillo y R7 se selecciona del grupo de alquilo, piridinilalquilo, fenilalquilo y pirazinilalquilo; R1, R2 son independientemente hidrógeno, alquilo, bencilo, naftilmetilo, isoindolilo y fenilo; -A-B- es independientemente un radical bivalente de fórmula