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Ep 2401275 B1 (19) TZZ Z_ _T (11) EP 2 401 275 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: C07D 471/04 (2006.01) C07D 519/00 (2006.01) of the grant of the patent: A61K 31/4375 (2006.01) A61P 11/00 (2006.01) 24.07.2013 Bulletin 2013/30 (86) International application number: (21) Application number: 10707251.4 PCT/EP2010/052343 (22) Date of filing: 24.02.2010 (87) International publication number: WO 2010/097410 (02.09.2010 Gazette 2010/35) (54) NAPHTHYRIDINE DERIVATIVES HAVING BRONCHODILATING ACTIVITY NAPHTHYRIDIN-DERIVATE MIT BRONCHENERWEITERNDER WIRKUNG DÉRIVÉS DE NAPHTHYRIDINE À ACTIVITÉ BRONCHODILATATOIRE (84) Designated Contracting States: • THORNQVIST-OLTNER, Viveca AT BE BG CH CY CZ DE DK EE ES FI FR GB GR S-261 40 Landskrona (SE) HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL • TOFTERED, Jörgen PT RO SE SI SK SM TR S-224 72 Lund (SE) • WENSBO, David (30) Priority: 24.02.2009 US 155027 P S-260 21 Billeberga (SE) 28.08.2009 SE 0950620 • DALENCE, Maria S-224 71 Lund (SE) (43) Date of publication of application: 04.01.2012 Bulletin 2012/01 (74) Representative: Ström & Gulliksson AB Box 4188 (73) Proprietor: Respiratorius AB 203 13 Malmö (SE) 22643 Lund (SE) (56) References cited: (72) Inventors: EP-A1- 1 669 348 US-A- 4 031 103 • JOHANSSON, Martin US-A- 5 753 666 S-216 22 Limhamn (SE) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 2 401 275 B1 Printed by Jouve, 75001 PARIS (FR) EP 2 401 275 B1 Description Technical field 5 [0001] The present invention relates to novel bronchorelaxing compounds, pharmaceutical compositions comprising such compounds, and a method of treating or alleviating conditions accompanied by bronchoconstriction and/or vaso- constriction, by use of such compounds. Background 10 [0002] Asthma and chronic obstructive pulmonary disease (COPD) are diseases affecting the respiratory system, which millions of people suffer from. These diseases are today regarded as inflammatory diseases and the symptoms comprise constriction of the airways. Common treatment of the associated bronchoconstriction involves use of beta- agonists, such as terbutalin and formoterol, and anticholinergics, such as ipratropium bromide and tiotropium bromide. 15 [0003] Hypertension, i.e. high blood pressure, increases the risk of stroke, heart attacks, heart failure and kidney disease. Medications presentlyused for thetreatment of hypertension include theadministration of beta- blockers, calcium channel blockers, diuretics, angiotensin- converting enzyme inhibitors and angiotensin II receptor antagonists. Vasocon- striction results in an increase in the blood pressure. [0004] The treatments for prevention, revocation or reduction of bronchoconstricion and vasoconstriction are in many 20 ways insufficient and there is a need for alternative treatments. [0005] More specifically, there is a need of compounds also being effective in preventing or revoking bronchoconstric- tion within the small airways, such as human airways having a diameter of less than 2.0 mm. It is believed that a bronchodilating effect on small airways (noncartilaginous airways of 2.0 mm or less in inner diameter) is of greater relevance for clinically observed relief of symptoms in COPD (i.e. shortness of breath), and maybe even in severe 25 asthma, as compared to bronchodilation of larger bronchi (more than 2 mm in inner diameter), due to the greater total surface area associated with the former. [0006] Furthermore, there is a need for compounds being effective in preventing or revoking bronchoconstriction, whose mechanisms differs from pharmacological established mechanisms of bronchodilation and preferably being ef- fective in preventing or revoking bronchoconstriction within the small airways. Accordingly, there is a need for compounds 30 being effective in preventing or revoking bronchoconstriction and which neither affect adrenergic or muscarinic receptors nor increasing the levels of cAMP through inhibition of phosphodiesterase enzymes, such as PDE3A enzyme. US 4,031,103 discloses 2-amino-5,7-disubstituted-naphthyridine and 5,7-disubstituted-naphthyridin-2(1H)-one deriva- tives with bronchodilating and hypotensive properties prepared by the reaction of 2,6- diaminopyridine with an appropriate beta-diketone providing the 2-amino products. 35 US 5,753,666 discloses 1-Alkyl-substituted-quinolone-3-carboxamides having therapeutic utility via their inhibition of Phosphodiesterase IV esterase and/or Tumor Necrosis Factor activity. Summary 40 [0007] The present invention seeks to mitigate, alleviate, circumvent, or eliminate at least one, such as one or more, of the above-identified deficiencies. [0008] Accordingly there is provided, according to one aspect of the invention, a compound, which may be represented with the general formula (I) 45 50 wherein R1 is selected from the group consisting of C1- C3 alkyl, NH2, NH (C1-C3 alkyl), C1-3 fluoroalkyl, OC1- C3 alkyl, OC1-3 fluoroalkyl, N(C1-C3 alkyl)2 in which the C1-3 alkyl may be the same or different, C(O)C0-C3 alkyl, C(O)OC0- C3 alkyl, C (O)N(C0-C3 alkyl)2 in which the C0-3 alkyl may be the same or different and N (C0-C3 alkyl)C(O)C1-C3 alkyl; A is NR2, O, or S, wherein R2 is selected from the group consisting of H and C1- C3 alkyl; E is selected from the group 55 consisting of C1- C3 alkylene, ethene-1,2-diyl, 1-propene-1,3-diyl and 2-propene-1,3-diyl; if E is selected from the group consisting of ethene-1,2-diyl, 1-propene-1,3-diyl and 2-propene-1,3-diyl, then the stereochemistry of the double-bond may be either E or Z; the integer "p" is 0 (zero), 1 or 2; R3 is independently selected from the group consisting of C1- C3 alkyl, C1-C3 alkyleneOC0-C3 alkyl, OMe, C1-5 fluoroalkyle, C0-C3 alkyleneOC1-3 fluoroalkyl, C(O)OCO-C3 alkyl, 2 EP 2 401 275 B1 and C(O)N(C0-C3 alkyl)2, in which the C0-3 alkyl may be the same or different; R3 may, if present, be connected to any of the carbon atom (s) in E; if "p" is 2, then the two R3 may be the connected to the same carbon atom or to different carbon atoms; Cy1 is a 5-membered heteroaryl, a 6-membered heteroaryl, or phenyl; the integer "n" is 0 (zero), 1 or 2; R4 is independently selected from the group consisting of C1-8 alkyl, C1-5 fluoroalkyl, halo, C0-1 alkylene cyano, C0-8 5 alkyleneOC0-5 alkyl, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, C0-3 alkyleneOC0-3 fluroroalkyl, C0-3 alkyleneNHC0-3 alkyl, C0-3 alkyleneN(C1-5 alkyl)2, in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC (O)OC0-5 alkyl, C0-3 alkyleneOC(O)C0-5 alkyl, C0-3 alkyleneN(C0-3 alkyl)C(O)C0-3 alkyl, C0-3 alkyleneC(O)NHC0-3 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2, in which the C1-5 alkyl may be the same or different, nitro, C (O)C0-C5 alkyl, N (C0-C3 alkyl) SO2C1-C3 alkyl, N(C0-C3 alkyl)SO2C1-C3 fluoroalkyl, OC2-C3alkyleneN(C0-C3 alkyl)2, in which the C0-3 alkyl may 10 be the same or different, and 15 wherein D is selected from the group consisting of C0-C3 alkylene, C0-1 alkylene OC0-1 alkylene, C0-1 alkylene OC (O) C0-1 alkylene, C0-1 alkylene C(O)O C0-1 alkylene, C0-1 alkylene C(O)N(C0-3 alkyl) C0-1 alkylene, C0-1 alkylene N(C0-3 alkyl)C(O) C0-1 alkylene, NHSO2, SO2NH, SO2, SO, C0-1 alkylene C(O) C0-1 alkylene, C0-1 alkylene N (C0-3 alkyl)C0-1 alkylene and S; Cy2 is a 5- membered heteroaryl, a 6- membered heteroaryl, phenyl, a 3- to 8- membered non- 20 aromatic heterocycle or a C3-8 non- aromatic carbocycle; the integer "m" is 0 (zero), 1, 2 3, 4, or 5; and R5 is independently selected from C-5 alkyl, C1-5 fluoroalkyl, halo, C0-1 alkylene cyano, C0-5 alkyleneOC0-5 alkyl, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, C0-3 alkyleneOC1-3 fluoroalkyl, C0-3 alkyleneNHC0-3 alkyl, C0-3 alkyleneN(C1-5 alkyl)2, in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC (O)OC0-5 alkyl, C0-3 alkyleneOC (O)C0-5 alkyl, C0-3 alkyleneN(C0-3 alkyl)C(O)C0-3 alkyl, C0-3 alkyleneC(O)NHC0-3 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2, in which the 25 C1-5 alkyl may be the same or different, C0-3 alkyleneC (O)N(C4-5 alkylene), nitro, C(O)C0-C5 alkyl, C(O)C1-C3 fluor- oalkyl, N(CO-C3 alkyl)SO2C1-C3 alkyl, N(C0-C3 alkyl)SO2C1-C3 fluoroalkyl, and OC2-C3alkyleneN(C0-C3 alkyl)2, in which the C0-3 alkyl may be the same or different; if Cy2 is a 3- to 8-membered non-aromatic heterocycle or a C3-8 non-aromatic carbocycle and "m" is at least 2, then two R5, being attached to the same carbon atom on said 3- to 8- membered non-aromatic heterocycle or said C3-8 non-aromatic carbocycle, may be connected to each other to form a 30 3-, 4- or 5-membered spiro ring; said spiro ring being a non-aromatic carbocycle or a non-aromatic heterocycle; if Cy2 is a 3- to 8-membered non-aromatic heterocycle or a C3-8 non-aromatic carbocycle and "m" is at least 2, then two R5, being attached to different atoms in said 3- to 8- membered non-aromatic heterocycle or said C3-8 non-aromatic carbo- cycle, may be connected to each other to form a C0-3 alkylene bridge; Cy2 thus being a bicyclic residue; if Cy2 is a 3- to 8-membered non-aromatic heterocycle or a C3-8 non- aromatic carbocycle, then R5 may be a double bonded oxygen 35 (=O), being attached to a carbon or sulfur atom in said cycle; R6, R7, and R8 are independently selected from the group consisting
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