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91. 发明专利

EE05271B1 未知
公开(公告)号：EE05271B1
公开(公告)日：2010-02-15
申请号：EEP200300166
申请日：2001-10-25
申请人： ELBION AG
发明人： HOEFGEN NORBERT , EGERLAND UTE , KRONBACH THOMAS , MARX DEGENHARD , SZELENYI STEFAN , KUSS HILDEGARD , POLYMEROPOULOS EMMANUEL
IPC分类号： A61K31/40 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P3/10 , A61P5/48 , A61P7/12 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/04 , A61P13/08 , A61P13/12 , A61P15/10 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/30 , A61P27/14 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P33/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D471/04
摘要： 7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds and methods of treating arthritis and other conditions with the compounds are also provided.

92. 发明专利

AR061206A1 PIRIDO[3,2-E]PIRAZINAS, SU USO COMO INHIBIDORES DE LA FOSFODIESTERASA 10, Y PROCESOS PARA PREPARARLAS 未知
公开(公告)号：AR061206A1
公开(公告)日：2008-08-13
申请号：ARP070102310
申请日：2007-05-29
申请人： ELBION AG
IPC分类号： C07D471/14 , A61K31/4353 , A61P25/00
摘要： Pirido[3,2-e]pirazinas, procesos para prepararlas, preparaciones farmacéuticas que comprenden estos compuestos y al uso farmacéutico de estos compuestos, que son inhibidores de la fosfodiesterasa 10, como compuestos activos para tratar enfermedades de mamíferos, que incluyen a un ser humano, que pueden ser influidos por el uso de los compuesto para inhibir la actividad de la fosfodiesterasa 10 en el sistema nervioso central. Más particularmente, tratamiento de trastornos neurologicos y psiquiátricos, por ejemplo psicosis y trastornos que comprenden déficits cognitivos como síntomas. Reivindicacion 1: Compuestos caracterizados porque formula (1) donde el enlace entre A y N es un enlace simple o un doble enlace, A es C cuando el enlace es un doble enlace y CH cuando el enlace es un enlace simple, m es 0 o 1, n es 0 o 1, donde R1 es R2 se seleccionan independientemente de H, un radical cíclico, alquilo C1-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, alquenilo C2-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, alquilinilo C2-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, un sistema anular carbocíclico saturado, monoinsaturado o poliinsaturado con 3 a 8 átomos o un sistema anular heterocíclico con 5 a 15 átomos anulares, cada uno opcionalmente mono- o poliinsaturado con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico y R3 se selecciona de H, un radical cíclico, N3, CN, R6, OR6, SR6, SOR6, SO2R6, NH(CO)OR6, N((CO)OR6)2, NR6 ((CO)OR6), NH-(C=O)-NH2, NR6-(C=O)-NH2, NR6-(C=O)-NH2, NH-(C=O)-NHR6, NR6-(C=O)-NHR6, NH- SO2R6, N(SO2R6)2 y NR6(SO2R6), donde R6 es en cada caso independientemente, un radical cíclico, alquilo C1-8 ciclo(hetero)alquilo C3-8, alquenilo C2-8, ciclo(hetero)alquenilo C3-8, o alquinilo C2-8, cada uno opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, R7, OR7, SR7, NHSO2R7, N(SO2R7) o N(R8)SO2R7, donde R7 es arilo, heteroarilo, arilalquilo C1-5, heteroarilalquilo C1-5, donde arilo es fenilo o naftilo, heteroarilo es un sistema anular heterocíclico aromático de 5 a 5 átomos en el anillo que contiene por lo menos un átomo seleccionado de N, que incluye N-oxido, s y O y donde arilo y heteroarilo están opcionalmente mono- o polisustituidos, con halo, amino, alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico y R8 es alquilo C1-5, opcionalmente mono- o polisustituido con halo, OH, O-C1-3 alquilo y/o un radical cíclico, R4 se selecciona de H, halo, un radical cíclico, R9, OH u OR9, NH(C=O)-alquilo C1-3, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 o/y un radical cíclico, NH2, NHR9 o NR9R10, donde R9 y R10 se seleccionan independientemente de - un radical cíclico, - alquilo C1-6 o ciclo(hetero)alquilo C3-6, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, - arilalquilo-C1-5, donde arilo es fenilo, opcionalmente mono- o polisustituido con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o radical cíclico o -NR9R10 juntos forman un anillo de cinco, seis o siete miembros saturado o insaturado que puede contener hasta 3 heteroátomos, con preferencia N, que incluye N-oxido, Sy/u O, opcionalmente mono- o polisustituido con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o aril-alquilo C1-5, donde arilo es fenilo, opcionalmente mono- o polisustituido con halo, amino, alquilamino c1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico, y R5 se selecciona de H, alquilo C1-5, cicloalquilo C3-6 o (CO)-alquilo C1-5, opcionalmente mono- o poli sustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, o sales y derivados aceptables para uso farmacéutico de los mismos.

93. 发明专利

NO324947B1 未知
公开(公告)号：NO324947B1
公开(公告)日：2008-01-07
申请号：NO20031722
申请日：2003-04-14
申请人： ELBION AG
发明人： SZELENYI STEFAN , EGERLAND UTE , KRONBACH THOMAS , POLYMEROPOULOS EMMANUEL , KUSS HILDEGARD , HOFGREN NORBERT , MARX DEGENHARD
IPC分类号： C07D471/04 , A61K31/40 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P3/10 , A61P5/48 , A61P7/12 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/04 , A61P13/08 , A61P13/12 , A61P15/10 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/30 , A61P27/14 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P33/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00
摘要： 7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds and methods of treating arthritis and other conditions with the compounds are also provided.

94. 发明专利

UA80711C2 TOPICAL TREATMENT OF SKIN DISEASES 未知
公开(公告)号：UA80711C2
公开(公告)日：2007-10-25
申请号：UA2005000163
申请日：2003-07-10
申请人： ELBION AG
发明人： RUNDFELDT CHRIS , KUSS HILDEGARD , HOEFGEN NORBERT
IPC分类号： A61K31/443 , C07D401/12 , A61K31/4439 , A61K38/22 , A61K45/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D207/00
摘要： The present invention relates to a method for the treatment of an inflammatory and/or allergic skin diseases comprising topically administering a substituted hydroxy indol.

96. 发明专利

ZA200508321B 7-azaindoles and use thereof as therapeutic agents 未知
公开(公告)号：ZA200508321B
公开(公告)日：2006-10-25
申请号：ZA200508321
申请日：2005-10-14
申请人： ELBION AG
发明人： NORBERT H FGEN , HILDEGARD KUSS , MATTHIAS OLBRICH , UTE EGERLAND , CHRIS RUNDFELDT , KARIN STEINIKE , RUDOLF SCHINDLER
IPC分类号： A61K20090101 , A61P20090101 , A61P35/00 , C07D20090101 , C07D471/04
摘要： The invention relates to substituted 7-azaindoles, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.

97. 发明专利

DK1475377T3 未知
公开(公告)号：DK1475377T3
公开(公告)日：2006-10-23
申请号：DK04018391
申请日：1999-04-24
申请人： ELBION AG
发明人： POPPE HILDEGARD , KRONBACH THOMAS , HOEFGEN NORBERT , EGERLAND UTE , MARX DEGENHARD , SZELENYI STEFAN , POLYMEROPOULOS EMMANUEL , HEER SABINE
IPC分类号： C07D401/12 , 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 , C07D413/02 , C07D417/02
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.

98. 发明专利

ZA200507002B Novel hydroxyindoles, use as inhibitors of phosphodiesterase 4 and method for production thereof 未知
公开(公告)号：ZA200507002B
公开(公告)日：2006-06-28
申请号：ZA200507002
申请日：2005-09-01
申请人： ELBION AG
发明人： HOEFGEN NORBERT , KUSS HILDEGARD , EGERLAND UTE , RUNDFELT CHRIS , HARTEN-HAUER HELGE , GASPARIC ANTJE
IPC分类号： A61K20060101 , A61P20060101 , A61P11/00 , C07D20060101 , C07D209/22 , C07D209/42
摘要： The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lympho-cytes).

99. 发明专利

ZA200503399B Novel hydroxyindoles, use as inhibitors of phosphodiesterase 4 and method for production thereof 未知
公开(公告)号：ZA200503399B
公开(公告)日：2006-06-28
申请号：ZA200503399
申请日：2005-04-28
申请人： ELBION AG
发明人： HOEFGEN NORBERT , KUSS HILDEGARD , EGERLAND UTE , RUNDFELDT CHRIS , HARTEN-HAUER HELGE , CASPARIC ANTJE
IPC分类号： A61K20060101 , A61P20060101 , A61P11/00 , C07D20060101 , C07D209/22 , C07D209/42
摘要： The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lympho-cytes).

100. 发明专利

BRPI0409793A 未知
公开(公告)号：BRPI0409793A
公开(公告)日：2006-05-30
申请号：BRPI0409793
申请日：2004-04-23
申请人： ELBION AG
发明人： HOEFGEN NORBERT , KUSS HILDEGARD , STEINIKE KARIN , EGERLAND UTE , RUNDFELDT CHRIS
IPC分类号： A61P11/00 , C07D401/12 , A61K31/4439
摘要： The invention relates to substituted 4-, 6- or 7-hydroxyindoles with N-oxide groups, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.

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