C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
260/235.01
C07F 7/08 (2006.01) C07C 405/00 (2006.01) C07D 295/18 (2006.01) C07H 13/04 (2006.01)
Patent
CA 1246558
ABSTRACT OF THE DISCLOSURE Novel carbacyclin amides of the general formula Image wherein R1 is NHR4, wherein R4 is (a) -(CH2)n-R8' (b) C2-10- alkenyl, (c) C1-10-alkyl or C2-10-alkenyl each substituted by C6- 10-aryl or by C6-10-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluo- romethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; (d) C3-10-cycloalkyl (e) C3-10-cycloalkyl substituted by C1-4- alkyl, (f) C6-10-aryl, (g) C6-l0-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4-alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; or (h) C2-8-alkyl substituted by 1-5 hydroxy groups, or R1 is -NR4R5, wherein R4 and R5 each is C2-8-alkyl substituted by 1-5 hydroxy groups or R4 and R5 together with the N-atom form a 5- or 6- membered heterocycle containing up to 1 additional O, S, or N atom wherein an additional N-atom can be substituted by C1- 4-alkyl, or R1 is -NR4R5 wherein R4 is (a) C1-10-alkyl, (b) C2- 10-alkenyl, (c) C1-10-alkyl or C2-10-alkenyl each substituted by C6-10-aryl or C6-10-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4-alkoxy group; (d) C3-10-cycloalkyl or (e) C3-10-cycloalkyl substituted by C1-4-alkyl, and R5 is (a) C2-10-alkenyl, (b) C1-10-alkyl or C2-10-alkenyl each substituted by C6-10-aryl or by C6-10-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4-alkoxy group; (c) C3-10-cycloalkyl, (d) C3-10- cycloalkyl substituted by C1-4-alkyl, (e) C6-10-aryl, (f) C6-10- aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4-alkoxy group; or (g) C2-8-alkyl substituted by 1-5 hydroxy groups, n is 1, 2, 3 or 4, R8 is - CONH2 or -N(C1-C4-alkyl)2; R2 is OR: R3 is (a) C1-10-alkyl, (b) C2-10 alkenyl, (c) C1-10-alkyl or C2-10-alkenyl each substituted by C6-10-aryl or by C6-10-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; (d) C3-10-cycloalkyl, (e) C3-10-cycloalkyl substituted by C1-4 alkyl, (f) C6-10-aryl, (g) C6-10-aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S the remainder being carbon atoms; X is -O- or -CH2-; A-W-D-E-R3 is Image Y is H or CH3;? represents .alpha.- or .beta. -bond; represents a single, double or triple bond, the double bond in the 13-position being in the trans-configuration; Image C1-3-alkyl; di-C1-3-alkyl; H, H; H, F; or CH2(CH2)mCH2; Z and Z' each is H or C1-5-alkyl; m is 1, 2 or 3 and R is H, tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, trimethylsilyl, dimethyl-tert-butyl-silyl, tribenzylsilyl acetyl, propionyl, butynyl and benzoyl.The novel carbacyclin amides have inter alia a hypotensive and brochodilative action and may accordingly be made up into pharmaceutical preparations with suitable carriers.
431617
Mannesmann Gerda
Nieuweboer Bob
Raduchel Bernd
Skuballa Werner
Town Michael H.
Marks & Clerk
Schering Aktiengesellschaft
LandOfFree
Carbacyclin amides, process for their manufacture and their... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Carbacyclin amides, process for their manufacture and their..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Carbacyclin amides, process for their manufacture and their... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1201080