Pyrazolopyrimidines and their use for the treatment of CNS disorders
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A kind of alkyl, the technology selected from, is applied in the field of preparing these compounds
Inactive Publication Date: 2011-08-03
BOEHRINGER INGELHEIM INT GMBH
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Traditional PDE inhibitors do not inhibit human PDE9A
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[0031] R 1.1 R 1 is a substituent selected from the following:
[0032] C 1-8 Alkyl-, C 2-8 Alkenyl-, C 2-8 Alkynyl-, R 10 -S-C 1-3 Alkyl-, R 10 -O-C 1-3 Alkyl-, C 3-7 Cycloalkyl-, C 3-7 Cycloalkyl-C 1-6 Alkyl-, C 3-7 Cycloalkyl-C 2-6 Alkenyl-, C 3-7 Cycloalkyl-C 2-6 Alkynyl-, C 3-8 Heterocycloalkyl-, C 3-8 Heterocycloalkyl-C 1-6 Alkyl-, C 3-8 Heterocycloalkyl-C 2-6 Alkenyl-, C 3-8 Heterocycloalkyl-C 2-6 Alkynyl-, aryl, aryl-C 1-6 Alkyl-, aryl-C 2-6 alkenyl-, aryl-C 2-6 Alkynyl-, Heteroaryl, Heteroaryl-C 1-6 Alkyl-, Heteroaryl-C 2-6 alkenyl- and heteroaryl-C 2-6 Alkynyl-, wherein the above-mentioned groups are optionally independently selected from each other by one or more groups selected from the group R 1.1.S1 The substituent is substituted, the group R 1.1.S1 From fluorine, chlorine, bromine, iodine, oxo (oxo) (wherein the oxo group is preferably only the substituent of cycloalkyl or heterocycloalkyl), HO-, NC-, O 2 N-, F 3 C-, HF 2 C-, FH 2...
Embodiment
[0359] pharmaceutical composition
[0360] The following examples present pharmaceutical preparations which illustrate the invention but do not limit the scope of the invention:
[0361] The term "active substance" means one or more compounds of the invention (including salts thereof).
Embodiment A
[0363] Tablets containing 100 mg of active substance
[0364] composition:
[0365] One tablet contains:
[0366] Active substance 100.0mg
[0367] Lactose 80.0mg
[0368] Corn starch 34.0mg
[0369] Polyvinylpyrrolidone 4.0mg
[0370] Magnesium stearate 2.0mg
[0371] 220.0 mg
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Abstract
The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein A is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving perception, concentration, learning and / or memory in patients in need thereof. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
Description
[0001] The present invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones. These new compounds are useful for the preparation of medicaments, in particular for improving perception, concentration, learning and / or Drugs for memory. [0002] Chemically, these compounds are characterized as pyrazolopyrimidinones with a cycloalkyl moiety directly bonded to its 1-position and a second cycloalkyl moiety bonded to its 6-position through an optionally substituted methylene bridge. Substituents. Other aspects of the invention relate to processes for the preparation of these compounds and their use as medicaments / for the preparation of medicaments. Background of the invention [0003] Inhibition of phosphodiesterase 9A (PDE9A) is one of the current concepts in finding new and available avenues for the treatment of cognitive impairments attributed to central nervous system disorders (CNS disorders) such as Alzheimer's disease ) or due to any other cra...
Claims
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