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1. WO2020114853 - PRODRUGS OF 4-((1R,3S)-6-CHLORO-3-PHENYL-2,3-DIHYDRO-1H-INDEN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND 4-((1/R,3S)-6-CHLORO-3-(PHENYL-D5)-2,3-DIHYDRO-1H-INDEN-1-YL)-2,2-DIMETHY-1-(METHYL-D3)PIPERAZINE

Publication Number WO/2020/114853
Publication Date 11.06.2020
International Application No. PCT/EP2019/082715
International Filing Date 27.11.2019
IPC
C07D 295/037 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
02containing only hydrogen and carbon atoms in addition to the ring hetero elements
037with quaternary ring nitrogen atoms
A61P 25/18 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61K 31/495 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
CPC
A61K 31/495
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
C07D 295/037
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
02containing only hydrogen and carbon atoms in addition to the ring hetero elements
037with quaternary ring nitrogen atoms
Applicants
  • H. LUNDBECK A/S [DK]/[DK]
Inventors
  • JACOBSEN, Mikkel, Fog
  • JØRGENSEN, Morten
Priority Data
PA20180094703.12.2018DK
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PRODRUGS OF 4-((1R,3S)-6-CHLORO-3-PHENYL-2,3-DIHYDRO-1H-INDEN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND 4-((1/R,3S)-6-CHLORO-3-(PHENYL-D5)-2,3-DIHYDRO-1H-INDEN-1-YL)-2,2-DIMETHY-1-(METHYL-D3)PIPERAZINE
(FR) PROMÉDICAMENTS DE 4-((1R,3S)-6-CHLORO-3-PHÉNYL-2,3-DIHYDRO-1H-INDEN-1-YL)-1,2,2-TRIMÉTHYLPIPÉRAZINE ET 4-((1/R,3S)-6-CHLORO-3-(PHÉNYL-D5)-2,3-DIHYDRO-1H-INDEN-1-YL)-2,2-DIMÉTHY-1-(MÉTHYL-D3)PIPÉRAZINE
Abstract
(EN)
The present invention relates to prodrugs of 4-((1R,3S)-6-chloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)- 1,2,2-trimethylpiperazine in the form of 1a and 1b; and 4-((1R,3S)-6-chloro-3-(phenyl-d5)-2,3-dihydro- 1H-inden-1-yl)-2,2-dimethyl-1-(methyl-d3)piperazine in the form of 2a and 2b, wherein X - is a counter ion, or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising prodrugs, or pharmaceutically acceptable salts thereof, of the invention.
(FR)
La présente invention concerne des promédicaments de 4-((1R,3S)-6-chloro-3-phényl-2,3-dihydro-1H-inden-1-yl)- 1,2,2-triméthylpipérazine sous la forme 1a et 1b; et de 4-((1R,3S)-6-chloro-3-(phényl-d5)-2,3-dihydro- 1H-inden-1-yl)-2,2-diméthyl-1-(méthyl-d3)pipérazine sous la forme 2a et 2b, X étant un contre-ion, ou des sels pharmaceutiquement acceptables de ceux-ci. La présente invention concerne également des compositions pharmaceutiques comprenant des promédicaments, ou des sels pharmaceutiquement acceptables de ceux-ci selon l'invention.
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