MX366840B - Pirimidinas novedosas 2,5-sustituidas como inhibidores de pde. - Google Patents

Pirimidinas novedosas 2,5-sustituidas como inhibidores de pde.

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Publication number
MX366840B
MX366840B MX2017000522A MX2017000522A MX366840B MX 366840 B MX366840 B MX 366840B MX 2017000522 A MX2017000522 A MX 2017000522A MX 2017000522 A MX2017000522 A MX 2017000522A MX 366840 B MX366840 B MX 366840B
Authority
MX
Mexico
Prior art keywords
novel
substituted pyrimidines
pde inhibitors
medicaments
indices
Prior art date
Application number
MX2017000522A
Other languages
English (en)
Other versions
MX2017000522A (es
Inventor
Konetzki Ingo
Hesslinger Christian
Jakob Florian
Craan Tobias
Nardi Antonio
Welbers Andre
Original Assignee
Gruenenthal Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of MX2017000522A publication Critical patent/MX2017000522A/es
Publication of MX366840B publication Critical patent/MX366840B/es

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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

La invención se relaciona con compuestos novedosos de pirimidina condensada de la fórmula general (I) en los cuales los agrupamientos químicos, sustituyentes e índices son como se define en la descripción, y con su uso como medicamentos, en particular como medicamentos para el tratamiento de condiciones y enfermedades que se puedan tratar mediante la inhibición de la enzima de PDE4.
MX2017000522A 2014-07-16 2015-07-16 Pirimidinas novedosas 2,5-sustituidas como inhibidores de pde. MX366840B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14002451 2014-07-16
PCT/EP2015/001475 WO2016008592A1 (en) 2014-07-16 2015-07-16 Novel 2,5-substituted pyrimidines as pde inhibitors

Publications (2)

Publication Number Publication Date
MX2017000522A MX2017000522A (es) 2017-05-01
MX366840B true MX366840B (es) 2019-07-26

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MX2017000522A MX366840B (es) 2014-07-16 2015-07-16 Pirimidinas novedosas 2,5-sustituidas como inhibidores de pde.

Country Status (19)

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US (1) US9315490B2 (es)
EP (2) EP3169680A1 (es)
JP (1) JP6726655B2 (es)
KR (1) KR20170032420A (es)
CN (1) CN106488916A (es)
AR (1) AR101197A1 (es)
AU (1) AU2015291477B2 (es)
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AR101196A1 (es) * 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
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