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1. 发明专利

AT370149T 未知
公开(公告)号：AT370149T
公开(公告)日：2007-09-15
申请号：AT02803410
申请日：2002-11-22
申请人： JANSSEN PHARMACEUTICA NV
发明人： TEGTMEIER FRANK , JANSSENS FRANS , LEENAERTS JOSEPH , VAN ROSSEM KOENRAAD , ALCAZAR-VACA MANUEL , MARTINEZ-JIMENEZ PEDRO , BARTOLOME-NEBREDA JOSE , GOMEZ-SANCHEZ ANTONIO , FERNANDEZ-GADEA FRANCISCO , VAN REEMPTS JOZEF
IPC分类号： 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
摘要： 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.

2. 发明专利

ES2927355T3 Compuestos inhibidores de OGA 未知
公开(公告)号：ES2927355T3
公开(公告)日：2022-11-04
申请号：ES19732991
申请日：2019-06-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： BARTOLOME-NEBREDA JOSÉ MANUEL , TRABANCO-SUAREZ ANDRÉS , LEENAERTS JOSEPH , OEHLRICH DANIEL , BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS , MARTINEZ LAMENCA CAROLINA , VELTER ADRIANA , VAN ROOSBROECK YVES
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/501 , A61P25/28
摘要： La presente invención se refiere a inhibidores de O-GIcNAc hidrolasa (OGA). La invención también está dirigida a composiciones farmacéuticas que comprenden tales compuestos, a procesos para preparar tales compuestos y composiciones, y al uso de tales compuestos y composiciones para la prevención y tratamiento de trastornos en los que la inhibición de OGA es beneficiosa, como tauopatías, en particular enfermedad de Alzheimer o parálisis supranuclear progresiva; y enfermedades neurodegenerativas acompañadas de una patología tau, en particular esclerosis lateral amiotrófica o demencia del lóbulo frontotemporal causada por mutaciones C90RF72. (Traducción automática con Google Translate, sin valor legal)

3. 发明专利

AT533762T 未知
公开(公告)号：AT533762T
公开(公告)日：2011-12-15
申请号：AT09735472
申请日：2009-04-21
申请人： JANSSEN PHARMACEUTICA NV
发明人： LOVE CHRISTOPHER , LEENAERTS JOSEPH , COOYMANS LUDWIG , LEBSACK ALEC , BRANSTETTER BRYAN , RECH JASON , GLEASON ELIZABETH , VENABLE JENNIFER , WIENER DANIELLE , SMITH DEBORAH , BREITENBUCHER JAMES
IPC分类号： C07D401/14 , A61K31/4427 , C07D405/14 , C07D413/14
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I).

4. 发明专利

ES2376092T3 ANTAGONISTAS DE P2X7 SUSTITUIDOS CON QUINOLINA O ISOQUINOLINA. 未知
公开(公告)号：ES2376092T3
公开(公告)日：2012-03-08
申请号：ES09735472
申请日：2009-04-21
申请人： JANSSEN PHARMACEUTICA NV
发明人： LOVE CHRISTOPHER , LEENAERTS JOSEPH , COOYMANS LUDWIG , LEBSACK ALEC , BRANSTETTER BRYAN , RECH JASON , GLEASON ELIZABETH , VENABLE JENNIFER , WIENER DANIELLE , SMITH DEBORAH , BREITENBUCHER JAMES
IPC分类号： C07D401/14 , A61K31/4427 , C07D405/14 , C07D413/14
摘要： Compuesto de fórmula (I) incluyendo cualquier forma estereoquímicamente isomérica del mismo, en la que n es un número entero 1, 2 ó 3; m es un número entero 1, 2 ó 3; p es un número entero 1 ó 2; R3 es hidrógeno, halo, alquilo C1-4 o alquiloxilo C1-4; X representa O, S, SO2, CR4R5 o NR6; en el que R4 y R5 se seleccionan cada uno independientemente del otro entre hidrógeno, halo, hidroxilo, alquilo C1-4, alquiloxilo C1-4 o arilo; en el que R6 es hidrógeno, fenilo, -CO-R7 o -CO-O-R7, en los que R7 es alquilo C1-6 o amino; R1 es un heterociclo seleccionado entre piridinilo o pirimidinilo, en el que dicho heterociclo está sustituido con uno o dos sustituyentes seleccionados cada uno independientemente del otro entre hidrógeno, halo, hidroxilo, alquilo C1-6, alquiloxilo C1-6, polihaloalquilo C1-4, fenilo, cicloalquilo C3-6, cicloalquiloxilo C3-6, cicloalquil C3-6-alquiloxilo C1-4 o NR8R9; en el que R8 y R9 se seleccionan independientemente uno del otro entre hidrógeno, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-6, y en el que R8 y R9 pueden tomarse junto con el átomo de nitrógeno al que están unidos para formar un anillo de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo o morfolinilo que puede estar opcionalmente sustituido con uno o dos sustituyentes seleccionados cada uno independientemente del otro entre alquilo C1-4, alquiloxilo C1-4, halo, hidroxilo o alquilcarbonilo C1-4; R2 es un heterociclo seleccionado entre quinolinilo o isoquinolinilo, en el que dicho heterociclo está sustituido con uno o dos sustituyentes seleccionados cada uno independientemente del otro entre hidrógeno, halo, hidroxilo, alquilo C1-6, alquiloxilo C1-6, cicloalquilo C3-6, cicloalquiloxilo C1-6, polihaloalquilo C1-4, NR10R11 y OR12; en el que R10 y R11 se seleccionan independientemente uno del otro entre hidrógeno, alquilo C1-6, cicloalquilo C3-6, polihaloalquilo C1-4, tetrahidrofuranilo, tetrahidropiranilo, piperidinilo, N- (1, 5-dioxa-9-azaespiro[5.5]undec-9-ilo) , N- (1, 7-diaza-espiro[4.4]non-7-ilo) , N- (2, 6-diaza-espiro[4.5]dec-2-ilo) y alquilo C1-6 sustituido con uno o dos sustituyentes seleccionados entre hidroxilo, halo, arilo1, alquiloxilo C1-4, cicloalquilo C3-6, hidroxicarbonilo, alquilsulfonilamino C1-4, cicloalquilsulfonilamino C3-6, tetrahidrofuranilo, tetrahidropiranilo, pirrolidinilo, piridinilo, morfolinilo, amino, mono- o di (alquil C1-4) amino, amino sustituido con alquilo C1-4 sustituido con hidroxilo; y en el que R10 y R11 pueden tomarse junto con el átomo de nitrógeno al que están unidos para formar un anillo de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, azepanilo, N-[1, 4]-oxazepanilo, morfolinilo, N- (2, 6diaza-espiro[3.3]hept-2-ilo) , 6-acetil-2, 6-diaza-biciclo[

5. 发明专利

AT423599T 未知
公开(公告)号：AT423599T
公开(公告)日：2009-03-15
申请号：AT07107669
申请日：2002-11-22
申请人： JANSSEN PHARMACEUTICA NV
发明人： TEGTMEIER FRANK , JANSSENS FRANS , LEENAERTS JOSEPH , VAN ROSSEM KOENRAAD , ALCAZAR-VACA MANUEL , MARTINEZ-JIMENEZ PEDRO , BARTOLOME-NEBREDA JOSE MANUEL , GOMEZ-SANCHEZ ANTONIO , FERNANDEZ-GADEA FRANCISCO , VAN REEMPTS JOZEF
IPC分类号： 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
摘要： 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.

6. 发明专利

BG65133B1 ANTIHISTAMINIC SPIRO COMPOUNDS 未知
公开(公告)号：BG65133B1
公开(公告)日：2007-03-30
申请号：BG10554601
申请日：2001-05-29
申请人： JANSSEN PHARMACEUTICA NV
发明人： JANSSENS FRANS , LEENAERTS JOSEPH
IPC分类号： C07D471/20 , A61K31/438 , A61K31/55 , A61P11/06 , A61P17/00 , A61P17/04 , A61P27/14 , A61P27/16 , A61P37/00 , A61P37/08 , A61P43/00 , C07D487/20 , C07D495/22 , C07D498/20 , C07D519/00
摘要： The invention concerns the applicable in medicine compounds of formula a prodrug, a N-oxide, an addition salt, and quaternary amine or a stereochemically isomeric form thereof therein R1 is hydrogen, C1-C6 alkyl, halo, formyl, carboxyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, N(R3R4)C(=O)-, N(R3R4)C(=O)N(R5)-, ethenyl substituted with carboxyl or C1-6 alkyloxycarbonyl, or C1-6 alkyl substitutedwith hydroxy, carboxyl, C1-6 alkyloxy, C1-6alkyloxycarnonyl, N(R3R4)C(=O)-, C1-6 alkylC(=O)N(R5)-, C1-6 alkylS(=O)2N(R5)-, or N(R3R4)C(=O))N(R5)-, wherein each R3 and each R4 independently are hydrogen or C1-4 alkyl and R5 is hydrogen or hydroxy; R2 is hydrogen, C1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkyloxyC1-6alkyl, N(R3R4)C(=O)-, aryl or halo; n is1 or 2; -A-B- represents a bivalent radical of formula -Y-CH=CH-, -CH=CH-Y-, or -CH=CH-CH=CH-, wherein each hydrogen atom may independently be replaced by R6 wherein R6 is C1-4 alkyl, halo, hydroxy, C1-6 alkoxy, ethenyl substituted wi5th carboxyl or C1-6 alkyloxycarbonyl or C1-6 alkyloxycarbonyl, hydroxy C1-6 alkyl, formyl, carboxyl or hydroxycarbonyl C1-6 alkyl, and each Y independently is a bivalent radical of formula -O-, -S-, or NR7-, wherein R7 is hydrogen, C1-6 alkyl or C1-6 alkylcarbonyl; Z is a bivalent radical of formula -(CH2)p-, -CH=CH-, -CH2-CHOH-, -CH2-O-, -CH2-O-, -CH2-C(=O), or -CH2-C(=NOH)-, provided that the bivalent radicals are connected to the nitrogen of the imidazole ring via their -CH2- moiety; and wherein p is 1, 2, 3 or 4; L is hydrogen; C-16 alkyl; C2-6 aslkenyl;C1-6 alkylcarbonyl; C1-6 alkyloxycarbonyl; C1-6 alkyl substituted with hydroxy, carboxyl, C1-6 alkyloxy, C1-6 alkyloxycabonyl, aryl, aryloxy, cyano or R8NH- wherein R8 is hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, C1-6 alkylcarbonyl; or L represents a radical of formula -Alk-Y-Het1, -Alk-NH-CO-Het2 or -Alk-Het3 wherein Alk represents C1-4 alkanediyl; Y represents O, S or NH; Het1 and Het2each represent an optionally substituted heterocycle; for use as a medicine.

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