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1. WO2020109354 - NOVEL DUAL MODE OF ACTION SOLUBLE GUANYLATE CYCLASE ACTIVATORS AND PHOSPHODIESTERASE INHIBITORS AND USES THEREOF

Publication Number WO/2020/109354
Publication Date 04.06.2020
International Application No. PCT/EP2019/082668
International Filing Date 27.11.2019
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/5365 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365ortho- or peri-condensed with heterocyclic ring systems
A61P 7/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
08Vasodilators for multiple indications
A61P 3/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
CPC
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
08Vasodilators for multiple indications
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • TOPADUR PHARMA AG [CH]/[CH]
Inventors
  • KOCH, Guido
  • LONE, Esra
  • DI MAIO, Selena
  • NAEF, Reto
  • PETERKE, Jeanette
  • SPOERRI, Michael
  • TENOR, Hermann
  • MARTINI, Elia
Agents
  • SPERRLE, Martin
Priority Data
18208939.128.11.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL DUAL MODE OF ACTION SOLUBLE GUANYLATE CYCLASE ACTIVATORS AND PHOSPHODIESTERASE INHIBITORS AND USES THEREOF
(FR) NOUVEAUX ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLES À DOUBLE MODE D'ACTION, INHIBITEURS DE PHOSPHODIESTÉRASE ET LEURS UTILISATIONS
Abstract
(EN)
The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) and said compound of formula II each comprises at least one ONO2 or ONO moiety; R1 is C1-C3alkyl; R2 is H, C1-C6alkyl, C3-C6cycloalkyl, C1-C2alkoxy, C2-C4alkenyl; R3 is C1-C4alkyl optionally substituted with C1-C2alkoxy, C3-C4cycloalkyl, C2-C4alkenyl; R4 and R5 are each independently H or C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, COOH, C1-C3alkoxy, C3-C6cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homo-piperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with independently one or more R6; R6 is C1-C6alkyl optionally substituted with independently one or more halogen, OH, ONO, ONO2, C1-C3alkoxy, C1-C3haloalkoxy, COOR7, NR8R9, C=NR10; R7 is H, or C1-C4alkyl optionally substituted with F, OH, ONO, ONO2, NR8R9; R8 and R9 are independently H, or C1-C4alkyl optionally substituted with ONO, ONO2; R10 is C1-C4alkyl optionally substituted with F, ONO, ONO2; C3-C6cycloalkyl; pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.
(FR)
La présente invention concerne des composés de formule (I) ou de formule (II) ou un sel, un solvate ou un hydrate pharmaceutiquement acceptable de ceux-ci, ledit composé de formule (I) et ledit composé de formule II comprenant chacun au moins une fraction ONO2 ou ONO ; R1 représente alkyle en C1-C3 ; R2 représente H, alkyle en C1-C6, cycloalkyle en C3-C6, alcoxy en C1-C2, alcényle en C2-C4 ; R3 représente alkyle en C1-C4 éventuellement substitué par alcoxy en C1-C2, cycloalkyle en C3-C4, alcényle en C2-C4 ; R4 et R5 représentent chacun indépendamment H ou alkyle en C1-C6 éventuellement substitué par F, OH, ONO, ONO2, COOH, alcoxy en C1-C3, cycloalkyle en C3-C6 ; ou conjointement avec l'atome d'azote auquel ils sont attachés forment un cycle hétérocyclique, de préférence ledit cycle hétérocyclique étant choisi parmi aziridine, azétidine, pyrollidine, pipéridine, morpholine, pipérazine, homo-pipérazine, 2,5-diazabicyclo[2,2,1]heptane et 3,7-diazabicyclo[3,3,0]octane, ledit cycle hétérocyclique étant éventuellement substitué par un ou plusieurs R6 ; R6 représente alkyle en C1-C6 éventuellement substitué par un ou plusieurs halogène, OH, ONO, ONO2, alcoxy en C1-C3, haloalcoxy en C1-C3, COOR7, NR8R9, C=NR10 ; R7 représente H, ou alkyle en C1-C4 éventuellement substitué par F, OH, ONO, ONO2, NR8R9 ; R8 et R9 représentent indépendamment H, ou alkyle en C1-C4 éventuellement substitué par ONO, ONO2; R10 représente alkyle en C1-C4 éventuellement substitué par F, ONO, ONO2 ; cycloalkyle en C3-C6 ; l'invention concerne également des compositions pharmaceutiques de ceux-ci, et leur utilisation dans des méthodes de traitement ou de prévention d'une maladie atténuée par l'inhibition de PDE5 chez un être humain ou chez un mammifère non humain.
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