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1. WO2010094609 - PHARMACEUTICAL COMPOSITION CONTAINING INHIBITING AGENTS OF PROTEIN METHYLTRANSFERASE I AND USE THEREOF TO TREAT TUMOR DISEASES

Publication Number WO/2010/094609
Publication Date 26.08.2010
International Application No. PCT/EP2010/051671
International Filing Date 11.02.2010
IPC
A61K 31/415 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
A61K 31/4196 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/4245 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4245Oxadiazoles
A61K 31/426 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
4261,3-Thiazoles
A61K 31/433 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
433Thiadiazoles
A61K 31/444 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
CPC
A61K 31/165
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
165having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/415
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
A61K 31/4196
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/4245
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4245Oxadiazoles
A61K 31/426
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
4261,3-Thiazoles
A61K 31/433
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
433Thidiazoles
Applicants
  • ALBERT-LUDWIGS-UNIVERSITÄT FREIBURG [DE]/[DE] (AllExceptUS)
  • MARTIN-LUTHER-UNIVERSITÄT HALLE-WITTENBERG [DE]/[DE] (AllExceptUS)
  • JUNG, Manfred [DE]/[DE] (UsOnly)
  • SCHÜLE, Roland [DE]/[DE] (UsOnly)
  • METZGER, Eric [DE]/[FR] (UsOnly)
  • SPANNHOFF, Astrid [DE]/[DE] (UsOnly)
  • LIEBSCHER, Jürgen [DE]/[DE] (UsOnly)
  • PÄTZEL, Michael [DE]/[DE] (UsOnly)
  • SIPPL, Wolfgang [DE]/[DE] (UsOnly)
Inventors
  • JUNG, Manfred
  • SCHÜLE, Roland
  • METZGER, Eric
  • SPANNHOFF, Astrid
  • LIEBSCHER, Jürgen
  • PÄTZEL, Michael
  • SIPPL, Wolfgang
Agents
  • KELLER, G.
Priority Data
09002395.320.02.2009EP
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) PHARMAZEUTISCHE ZUSAMMENSETZUNG ENTHALTEND HEMMSTOFFE DER PROTEINMETHYLTRANSFERASE I UND DEREN VERWENDUNG ZUR BEHANDLUNG VON TUMORERKRANKUNGEN
(EN) PHARMACEUTICAL COMPOSITION CONTAINING INHIBITING AGENTS OF PROTEIN METHYLTRANSFERASE I AND USE THEREOF TO TREAT TUMOR DISEASES
(FR) COMPOSITIONS PHARMACEUTIQUES COMPRENANT DES ANTAGONISTES DE LA PROTÉINE MÉTHYLTRANSFÉRASE I ET SON UTILISATION POUR LE TRAITEMENT DE MALADIES TUMORALES
Abstract
(DE)
Offenbart werden Inhibitoren der PMRT-Typ I-Methyltransferase und deren Verwendung in pharmazeutischen Zusammensetzungen, die eine Verbindung der allgemeinen Formel I enthalten, worin die Reste R1 und R2 gleich oder unterschiedlich sind und ausgewählt sind aus den Bedeutungen Wasserstoff, gerad- oder verzweigtkettiges C1-5-Alkyl, oder n eine ganze Zahl zwischen 3 und 5 ist, X ein Heteroatom ist, ausgewählt aus O, S, N-R1 oder die Bedeutung -CH2- hat und der Rest Het ein 5-, 6- oder 7-gliedriger aromatischer oder nicht aromatischer Ring ist, der 1 bis 5 Heteroatome, ausgewählt aus N, S und O ist, wobei der Ring gegebenenfalls substituiert sein kann und ein substituierter oder nicht substituierter polycyclischer Ring sein kann sowie dessen pharmazeutisch annehmbare Salze. Die Zusammensetzungen dienen der Verwendung als Arzneimittel gegen Tumorerkrankungen.
(EN)
The invention relates to inhibitors of PMRT type I methyltransferase and to the use thereof in pharmaceutical compositions, which contain a compound of the general formula I, wherein the groups R1 and R2 are the same or different and are selected from among the meanings hydrogen, straight-chain or branched-chain C1-5 alkyl, or n is an integer between 3 and 5, X is a heteroatom selected from among O, S, N-R1 or has the meaning -CH2-, and the group Het is a 5-, 6-, or 7-membered aromatic or non-aromatic ring that is 1 to 5 heteroatoms selected from among N, S, and O, wherein the ring can optionally be substituted and can be a substituted or unsubstituted polycyclic ring, and to pharmaceutically acceptable salts of thereof. The compositions are used as drugs against tumor diseases.
(FR)
L'invention porte sur des inhibiteurs de la méthyltransférase PMRT de type I et sur leur utilisation dans des compositions pharmaceutiques qui contiennent un composé de Formule générale I, dans laquelle les restes R1 et R2 sont identiques ou différents et sont choisis parmi les significations hydrogène, alkyle en C1-5 à chaîne droite ou ramifiée, n est un nombre entier entre 3 et 5, X est un hétéroatome choisi parmi O, S, N-R1 ou a la signification -CH2-, et le reste Het est un cycle aromatique ou non aromatique à 5, 6 ou 7 chaînons, qui comporte 1 à 5 hétéroatomes, choisis parmi N, S et O, le cycle pouvant être le cas échéant substitué et pouvant être un noyau polycyclique substitué ou non substitué, ainsi que sur les sels pharmaceutiquement acceptables de ce composé. Les compositions sont destinées à être utilisées en tant que médicament contre les maladies tumorales.
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