Abstract: The invention relates to the combined use of the PDE4 inhibitor N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide, its pharmacologically tolerable salts or its N-oxide with a PDE3 inhibitor for the treatment of certain disease conditions such as, for example, acute or chronic obstructions of the bronchi.
Thomas Bär, Thomas Martin, Josef Stadlwieser, Wolf-Rüdiger Ulrich, Andreas Dominik, Ulrich Thibaut, Daniela Bundschuh, Rolf Beume, Karl-Josef Goebel, Wolfram Bode, Luis Moroder, Pedro Jose Barbosa Pereira, Andreas Bergner, Robert Huber, Christian Sommerhoff, Norbert Schaschke
Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, and R3 are hydrogen, 1-4C-alkyl, or halogen; R4, R5, R6, and R9 are hydrogen or 1-4C-alkyl; R7 and R8 are hydrogen, 1-4C-alkyl, 1-4C-alkoxy, or halogen; A is 1-7C-alkylene, 2-7C-alkenylene, 3-7C-cycloalkylene, or phenylene; G is hydrogen, hydroxyl, 1-7C-alkyl, 1-4C-alkyl substituted by fluorine, 2-7C-alkenyl, 3-7C-cycloalkyl, a mono- or di-1-4C-alkylcarbamoyl or -thiocarbamoyl, N-1-4C-alkyl-N′-cyanoamidino, 1-N-1-4C-alkylamino-2-nitroethylene, N-2-propynyl-N′-cyanoamidino, aminosulfonylamidino, —N(R10)R11, the part of the compound of formula (I) bonded to A, glucopyranoside, or a cyclic system or bicyclic system which is optionally substituted by R12 and R13; X is oxygen, N-1-4C-alkyl, NH, or S; Y is oxygen, N-1-4C-alkyl, NH, S, 1,4-piperazinylene, or 1,4-piperidinylene; Z is oxygen, N-1-4C-alkyl, NH, S, or CO; m is from 1 to 7; n is from 0 to 4; t is 0, 1, or 2; and u is 0 or 1, and their salts suitable for controllin
Abstract: Compounds 8,9-diethoxy-2-methyl-6-[4(p-toluenesulfonamide) phenyl]-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridine and 9-ethoxy-8-methoxy-2-methyl-6-[4-(p-toluenesulfonamido)phenyl]-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridine and medicament compositions based thereon are useful for treating airway disorders, high blood pressure disorders and concomitant disorders connected therewith.
Abstract: Compounds of formula I,
wherein Het represents a heterocycle having the meaning
and R1, R2, R3 and R4 have the meanings as given in the description are novel effective bronchial therapeutics.
Abstract: Compounds of formula I
in which R1, R2, R3 and A have the meaning set forth in the specification, are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors useful as therapeutics in human and veterinary medicine. They are distinguished by low toxicity, good enteral absorption (high bioavailability), a wide therapeutic breadth and absence of significant side effects.
Abstract: A diseased state based on acute or chronic obstruction of vessels and/or bronchi, acute or chronic inflammation and/or edema formation is advantageously treated by the combined administration of a PDE inhibitor with either an adenylate cyclase agonist or a guanylate cyclase agonist to a subject in need of such therapy. Administration can be either concurrent or in either order.