DR. MAIER THOMAS,DR. VIERTELHAUS MARTIN,DR. STENGEL THOMAS,PROF. DR. PAHL ANDREAS,DR. HOLST HANS CHRISTOF,DR. HUMMEL ROLF,PETER - DR. TENOR HERMANN,DR. FLOCKERZI DIETER,DR. MANN ALEXANDER,DR. DUNKERN
申请号：
ARP120102088
公开号：
AR086915A1
申请日:
2012.06.12
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
Are effective inhibitors of phosphodiesterase type 4 and 5.Claim 1: a compound of formula (1), wherein R1 represents a phenyl Derivative of the formula (2) or (3), where R2 is c1-4 alkoxy or c1-4 alkoxy substituted predominantly or entirely by Fluorine； R3 is c1-4 alkoxy, cicloalcoxi C3 - 5Cicloalcoxi methoxy c3-5 or c1-4 alkoxy substituted predominantly or entirely by Fluorine； R4 is c1-4 alkoxy or c1-4 alkoxy substituted predominantly or entirely by Fluorine is c1-4 alkyl； R5, R6 is Hydrogen or alkyl or c1-4, where together with R5 and R6 the inclusion of the d You carbon ATOMS, which are United to form a Hydrocarbon Ring 5.6 - or 7 - members linked by Spiro, optionally interrupted by one Oxygen Atom is Hydrogen or Sulfur； R7, R8 is c1-4 alkyl； and R7 and R8 together form a group alquileno c3-5； R9 is Hydrogen or alkyl or c1-4, R8 and R9 and where together with the inclusion of the carbon Atom, the Which together form a Hydrocarbon Ring 5.6 - or 7 - members linked by Spiro； M is 1 or 2； R10 is independently Hydrogen, alkyl, cycloalkyl C1 - C5 - 6, 7 - ch (CH3) - R11 and R12 - CH2 -, where is not replaced or Hydroxy phenyl R11, R12 is hydroxyl, cycloalkyl C5 - 7, - n - (alkyl c1-2) 2, - CH2 - S - (c1-2 alkyl phenyl), not s Ustituido, phenyl substituted by phenyl substituted by R13, R13 and R14, where R13 is Hydrogen,C1-4 alkoxy, c1-4 alkyl, fluoroalquilo c1-4, phenyl, hydroxyl, - C (o) NH2 - CN, - 1 - 2 - oxoazetidin yl - 1 - or 2 - oxopirrolidin ILO R14 is Hydrogen； c1-4 alkyl, alkoxy, c1-4, fluoroalquilo c1-4, hydroxyl phenyl, - C (o) NH2 or - ns； or R12 is a Heterocyclic Ring of five or six members Selected imidazole - yl - 2 - 4 - ILO, imidazole, pyrazole - 1 - 2 - tiofen - ILO, ILO, ILO thiophene-3 thiazole thiocyanatoacetate,Thiazole - 4 - 5 - thiazole - ILO, ILO, ILO pyridin - pyridin - 2, - 3 - 4 - pyridin - ILO, ILO, indole thiocyanatoacetate, indole - 3 - ILO, 1 - methyl - 2 - ilo indole or indole - 3 - methyl - 1 - ilo； or R12 is - CH2 - C (o) - R15, whe
