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131. 发明专利

HK1035183A1 New hydroxyindoles, their use as phosphodiesterase4 inhibitors and method for producing same. 未知
公开(公告)号：HK1035183A1
公开(公告)日：2001-11-16
申请号：HK01105669
申请日：2001-08-14
申请人： ELBION AG
发明人： HOFGEN NORBERT , EGERLAND UTE , POPPE HILDEGARD , MARX DEGENHARD , SZELENYI STEFAN , KRONBACH THOMAS , POLYMEROPOULOS EMMANUEL , HEER SABINE
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P43/00 , C07D209/22 , C07D209/24 , C07D209/42 , C07D401/06 , C07D401/12 , C07D413/02 , C07D417/02 , C07D , A61K , A61P
摘要： 5- or 6-Hydroxyindole derivatives (I), their optical isomers, racemates and diastereomers, and their acid addition and base salts are new: : 5- or 6-Hydroxyindole derivatives (I), their salts, optical isomers, racemates and diastereomers are new: [Image] A : bond; -(CH 2) m-; -(CH 2) m-(CH=CH) n-(CH 2) p-; -(CHOZ) m-; -C(O)-; -C(S)-; -C(=N-Z)-; -O-; -S-; or -N(Z)-; m, p : 0-3; n : 0-2; Z : H; alkyl; alkenyl; or a heterocycle or carbocycle (both mono-, bi- or tricyclic and saturated or mono- or poly-unsaturated); B : C; S; or S(O); D : O or N-Z or, when B = C, also S or CH 2; E : bond; -(CH 2) m-; -O-; -S-; or -N(Z)-; R 1>, R 5>alkyl, alkenyl, a heterocycle, carbocycle or carbocyclic or heterocyclic spirocycle (all optionally mono- or poly-substituted by Q); Q : OH; SH; NH 2; NH(alkyl); N(alkyl) 2; NH(aryl); N(aryl) 2; N(alkyl)(aryl); NHCOR 6>; NO 2; CN; F; Cl; Br; I; alkoxy; aryloxy; OC(O)R 6>; alkylthio; arylthio; SOR 6>; SO 3H; SO 2R 6>; alkyl-SO 2O; aryl-SO 2O; C(S)R 6>; COOH; C(O)R 6>; or a heterocycle or carbocycle (aryl, heterocycle and carbocycle are optionally mono- or poly-substituted by R 4>); R 2>, R 3>H or OH, but at least one is OH; R 4>H; OH; SH; NH 2; NH(alkyl) N(alkyl) 2; NH(aryl); N(aryl) 2; N(alkyl)(aryl); NHCOR 6>; NO 2; CN; COOH; C(O)R 6>; C(S)R 6>; F: Cl; Br; I; alkoxy; aryloxy; OC(O)R 6>; alkylthio; arylthio; SOR 6>; or SO 2R 6>; R 6>H; NH 2; NH(alkyl); N(alkyl) 2; NH(aryl); N(aryl) 2; N(alkyl)(aryl); alkoxy; aryloxy; alkylthio; arylthio; arylthio-alkyl; alkenyl; or a heterocycle or carbocycle. The full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for the preparation of compounds (I). ACTIVITY : Bronchodilator; neuroprotective. MECHANISM OF ACTION : Phosphodiesterase 4 (PDE 4) inhibitors; TNF-alpha inhibitors. A modification of the method described by Thompson et al. Adv. Cycl. Nucl. Res. 1979, 10, 69-92 was used to determine the inhibition of phosphodiesterase by compounds (I). In this test, compounds (I) exhibited IC 5 0 values of 10 -> 9>-0 -> 5> M. The selectivity over PDE types 2, 3 and 5 was by a factor of 100-10000. Compounds (I) had IC 5 0 values of 10 -> 7>-10 -> 5> M in a test for the inhibition of TNF-alpha release from nasal polyp cells (see Int. Arch. Allergy Immunol., 1993, 101, 308-310). Further, in a test for the inhibition of late phase eosinophilia in ovalubin-sensitized guinea pigs, compounds (I) gave 30-80% inhibition when administered i.p. and 40-70% inhibition when administered p.o. In a test for their effect on allergen-induced vascular permeability in ovalbumin-sensitized rats, compounds (I), administered intranasally exhibited IC 5 0 values of 10 -> 8>-10 -> 5> M.

132. 发明专利

HU9802941A3 NOVEL 1-AR(ALK)YL-IMIDAZOLIN-2-ONES CONTAINING A DISUBSTITUTED AMINE RADICAL IN THE 4TH POSITION, HAVING AN ANTI-CONVULSIVE EFFECT AND PROCESS FOR THEIR PRODUCTION, THEIR USE AND PHARMACEUTICALS CONTAINING THE SAME 未知
公开(公告)号：HU9802941A3
公开(公告)日：1999-10-28
申请号：HU9802941
申请日：1996-07-26
申请人： ELBION AG
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61P21/00 , A61P21/02 , C07D233/88
摘要： Compounds with an anti-convulsive effect of general formula (1) in which X = hydrogen, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, halogen and R or R = C1-C4 alkyl, cycloalkyl or heteroalkyl.

134. 发明专利

BRPI0606897A2 未知
公开(公告)号：BRPI0606897A2
公开(公告)日：2009-07-21
申请号：BRPI0606897
申请日：2006-01-31
申请人： ELBION AG
发明人： RUNDFELDT CHRIS , KUSS HILDEGARD , DRAHEIM REGINA , BERNOESTER KATRIN
IPC分类号： A61K31/44 , A61P13/10
摘要： The present invention is directed to the prevention, reversal and medical treatment of lower urinary tract dysfunction including bladder instability and other related diseases as described below including urinary flow problems, urgency and incontinence as a result of prostate hyperplasia (BPH) and to the prevention, reversal and medical treatment of irritable bowel syndrome (IBS) with special focus on the diarrhea-predominant and mixed diarrhea-constipation type IBS, both in human beings and animals.

136. 发明专利

PE20080711A1 PIRIDO[3,2-E] PIRAZINAS, SU USO COMO INHIBIDORES DE LA FOSFODIESTERASA 10 Y PROCESOS PARA PREPARLAS 未知
公开(公告)号：PE20080711A1
公开(公告)日：2008-06-14
申请号：PE2007000674
申请日：2007-05-30
申请人： ELBION AG
发明人： HOFGEN NORBERT , STANGE HANS , EGERLAND UTE , SCHINDLER RUDOLF , PFEIFER THOMAS , RUNDFELDT CHRIS , LANGEN BARBARA
IPC分类号： A61K31/4985 , A61P25/18 , C07D471/14
摘要： SE REFIERE A COMPUESTOS PIRIDO[3,2-e]PIRAZINAS DE FORMULA (I), EN DONDE A Y N ES UN ENLACE SIMPLE O DOBLE; A ES C CUANDO ES DOBLE ENLACE Y CH CUANDO ES ENLACE SIMPLE; m ES 0 O 1; n ES 0 O 1; R1 Y R2 SON INDEPENDIENTEMENTE H, , ALQUILO(C1-C8), ALQUENILO(C2-C8), ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS; R3 ES H, UN RADICAL CICLICO, N3, R6, NH-(C=O)-OR6; NR6(SO2R6), ENTRE OTROS, DONDE R6 ES ALQUILO(C1-C8), ALQUENILO(C2-C8), ENTRE OTROS; R4 ES H, HALO, R9, OH, OR9, NR9R10, ENTRE OTROS, SON COMPUESTOS PREFERIDOS: 4,8-DIMETOXI-3-METIL-1-PROPIL-IMIDAZO[1,5-a]PIRIDO[3,2-e]PIRAZINA, 4,8-DIMETOXI-1-PROPIL-IMIDAZO[1,5-a]PIRIDO[3,2-e]PIRAZINA, 1-ETIL-4-ISOPROPILOXI-8-METOXI-3-METIL-IMIDAZO[1,5-a]PIRIDO[3,2-e]PIRAZINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE PREPARACION Y COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA FOSFODIESTERASA 10 EN EL SISTEMA NERVIOSO CENTRAL, SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS Y PSIQUIATRICOS, COMO LA ESQUIZOFRENIA

137. 发明专利

PE02662008A1 4-AMINO-PIRIDO[3,2-E]PIRAZINAS, SU USO COMO INHIBIDORES DE FOSFODIESTERASA 10 Y PROCESOS PARA SU PREPARACION 未知
公开(公告)号：PE02662008A1
公开(公告)日：2008-04-10
申请号：PE0006752007
申请日：2007-05-30
申请人： ELBION AG
发明人： HOFGEN NORBERT , STANGE HANS , LANGEN BARBARA , EGERLAND UTE , SCHINDLER RUDOLF , GASPARIC ANTJE , RUNDFELDT CHRIS
IPC分类号： A61K31/4985 , A61P25/00 , C07D471/14
CPC分类号： C07D471/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA II DONDE R1 y R2 SON CADA UNO H, RADICAL CICLICO, ALQUILO C1-C8, ENTRE OTROS; R3 ES NH2, NHR5, NR5R6; R5 y R6 SON CADA UNO RADICAL CICLICO, ALQUILO C1-C5, (C=O) ARIL-ALQUILO C1-C5, ENTRE OTROS; R4 ES H, HALO, RADICAL CICLICO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-AMINO-8-METOXI-3-METIL-1-PROPIL-IMIDAZO[1,5-a]PIRIDO[3,2-e]PIRAZINA; 4-AMINO-1-ETIL-8-METOXI-3-METIL-IMIDAZO[1,5-a]PIRIDO[3,2-e]PIRAZINA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. LOS COMPUESTOS INHIBIDORES DE FOSFODIESTERASA 10 EN EL SISTEMA NERVIOSO CENTRAL. SON UTILES EN EL TRATAMIENTO DE DE TRANSTORNOS NEUROLOGICOS Y PSIQUIATRICOS

138. 发明专利

NO325346B1 未知
公开(公告)号：NO325346B1
公开(公告)日：2008-04-07
申请号：NO995300
申请日：1999-10-29
申请人： ELBION AG
发明人： DOST RITA , ROSTOCK ANGELIKA , UNVERFERTH KLAUS , TOBER CHRISTINE , RUNDFELDT CHRIS , BARTSCH RENI
IPC分类号： A61K31/4166 , C07D233/88 , A61K20060101 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/416 , A61K31/4174 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5377 , A61P25/00 , A61P25/22
摘要： A process for the treatment of anxiety and tension, which comprises administering to a patient in need therefor an anxiolytically effective amount of a compound of the formula wherein X is hydrogen, a C1-4 alkyl, C1-4 alkoxy, trifluoromethyl residue, or halogen; R1 and R2 are independently of each other a C1-4 alkyl, cycloalkyl, C2-4 hydroxyalkyl, or heteroalkyl residue, or R1 and R2 together form a C2-6 alkylene residue in which one -CH2- group can be replaced by oxygen, nitrogen or sulfur; n is 0 or 1, and m is 0 or a cardinal number from 1-5, or a pharmaceutically acceptable salt of the compound.

139. 发明专利

CL2007001554A1 Compuestos derivados de pirido [3,2-e]pirazinas;inhibidoras de pde10;procedimiento de preparacion;composicion farmaceutica que comprende; kit farmaceutico; uso para preparar de un medicamento para tratar o prevenir trastornos asociados a la hiperactividad de pde10 y/o trastornos en los que inhibir la pde10 es de valor. 未知
公开(公告)号：CL2007001554A1
公开(公告)日：2008-01-18
申请号：CL2007001554
申请日：2007-05-30
申请人： ELBION AG
发明人： HOFGEN NORBERT , STANGE HANS , LANGEN BARBARA , EGERLAND UTE , SCHINDLER RUDOLF , PFEIFER THOMAS , RUNDFELDT CHRIS
IPC分类号： A61K31/4985 , A61P25/00 , C07D233/06 , C07D471/14 , C07D487/14
摘要： Compuestos derivados de pirido [3,2-e]pirazinas; procedimiento de preparación; composición farmacéutica que comprende a dichos compuestos; kit farmacéutico; y uso de los compuestos para el tratamiento de trastornos del sistema nervioso central.

140. 发明专利

MX2007009187A EL USO DE FLUPIRTINA PARA EL TRATAMIENTO DE VEJIGA SUPERACTIVA Y ENFERMEDADES ASOCIADAS, Y PARA EL TRATAMIENTO DEL SINDROME DEL INTESTINO IRRITABLE. 未知
公开(公告)号：MX2007009187A
公开(公告)日：2007-09-21
申请号：MX2007009187
申请日：2006-01-31
申请人： ELBION AG
发明人： KUSS HILDEGARD , RUNDFELDT CHRIS , DRAHEIM REGINA , BERNOESTER KATRIN
IPC分类号： A61K31/44 , A61P13/10
摘要： La presente invencion esta dirigida a la prevencion, reversion y tratamiento medico de disfuncion del tracto urinario inferior, incluyendo la inestabilidad de la vejiga y otras enfermedades relacionadas como se describe mas adelante, incluyendo problemas de flujo urinario, urgencia e incontinencia como resultado de hiperplasia prostatica (BPH) y con la prevencion, reversion y tratamiento medico del sindrome del intestino irritable (IBS) con enfoque especial sobre diarrea predominante y constipacion por diarrea mezclada tipo IBS, tanto en seres humanos como en animales.

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