CY1124051T1 - Θεραπεια νευρολογικων διαταραχων - Google Patents

Θεραπεια νευρολογικων διαταραχων

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Publication number
CY1124051T1
CY1124051T1 CY20211100267T CY211100267T CY1124051T1 CY 1124051 T1 CY1124051 T1 CY 1124051T1 CY 20211100267 T CY20211100267 T CY 20211100267T CY 211100267 T CY211100267 T CY 211100267T CY 1124051 T1 CY1124051 T1 CY 1124051T1
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CY
Cyprus
Prior art keywords
formula
optionally substituted
alkyl
treatment
morpholinyl
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CY20211100267T
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English (en)
Inventor
Denise RAGEOT
Paul Hebeisen
Florent Beaufils
Doriano Fabbro
Petra HILLMANN-WULLNER
Wolfgang Löscher
Claudia BRANDT
Alexander Markus SELE
Hoa Huu Phuc NGUYEN
Original Assignee
Torqur Ag
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Publication of CY1124051T1 publication Critical patent/CY1124051T1/el

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/153Ortho-condensed systems the condensed system containing two rings with oxygen as ring hetero atom and one ring with nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Η παρούσα εφεύρεση αφορά μία ένωση του τύπου (Ι), όπου τα Χ1, Χ2 και Χ3 είναι, ανεξάρτητα το ένα από το άλλο, Ν ή CH· με την προϋπόθεση ότι τουλάχιστον δύο από τα Χ1, Χ2 και Χ3 είναι Ν· το Υ είναι Ν ή CH· τα R1 και R2 είναι ανεξάρτητα το ένα από το άλλο (iii) ένα μορφολινύλιο του τύπου (II) όπου το βέλος δηλώνει τον δεσμό στον τύπο (I)· και όπου τα R3 και R4 είναι ανεξάρτητα το ένα από το άλλο Η, C1-C3αλκύλιο ενδεχομένως υποκατεστημένο με ένα ή δύο ΟΗ, C1-C2φθοροαλκύλιο, C1-C2αλκοξυ, C1-C2αλκοξυC1-C3αλκύλιο, CN, ή C(Ο)Ο-C1-C2αλκύλιο· ή τα R3 και R4 σχηματίζουν μαζί ένα δισθενές υπόλοιπο -R5R6- που επιλέγεται από C1-C3αλκυλένιο, ενδεχομένως υποκατεστημένο με 1 έως 4 F, -CH2-O-CH2-, -CH2-NH-CH2-, ή οποιαδήποτε από τις δομές όπου τα βέλη δηλώνουν τους δεσμούς στον τύπο (II)· ή (iv) ένας κορεσμένος 6-μελής ετεροκυκλικός δακτύλιος Ζ που επιλέγεται από θειομορφολινύλιο και πιπεραζινύλιο, ενδεχομένως υποκατεστημένο με 1 έως 3 R7· όπου το R7 είναι ανεξάρτητα σε κάθε εμφάνιση C1-C3αλκύλιο ενδεχομένως υποκατεστημένο με ένα ή δύο ΟΗ, C1-C2φθοροαλκύλιο, C1-C2αλκοξυC1-C3αλκύλιο, C3-C6κυκλοαλκύλιο· ή δύο R7 υποκαταστάτες σχηματίζουν μαζί ένα δισθενές υπόλοιπο -R8R9-που επιλέγεται από C1-C3αλκυλένιο ενδεχομένως υποκατεστημένο με 1 έως 4 F, -CH2-O-CH2- ή -Ο-CH2CH2-O-· με την προϋπόθεση ότι τουλάχιστον ένα από τα R1 και R2 είναι ένα μορφολινύλιο του τύπου II· και προφάρμα, μεταβολίτες, ταυτομερή, επιδιαλυτώματα και φαρμακευτικά αποδεκτά άλατα αυτής, για χρήση στην πρόληψη ή θεραπεία μιας νευρολογικής διαταραχής σε ένα υποκείμενο.
CY20211100267T 2016-05-18 2021-03-26 Θεραπεια νευρολογικων διαταραχων CY1124051T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16170107 2016-05-18
PCT/EP2017/025136 WO2017198346A1 (en) 2016-05-18 2017-05-17 Treatment of neurological disorders

Publications (1)

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CY1124051T1 true CY1124051T1 (el) 2022-05-27

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US (3) US20190284178A1 (el)
EP (1) EP3458067B1 (el)
JP (1) JP6991158B2 (el)
KR (1) KR102472461B1 (el)
CN (1) CN109475560B (el)
AU (1) AU2017265383B2 (el)
BR (1) BR112018073579A8 (el)
CA (1) CA3022753A1 (el)
CY (1) CY1124051T1 (el)
DK (1) DK3458067T3 (el)
ES (1) ES2863250T3 (el)
HR (1) HRP20210477T1 (el)
HU (1) HUE053494T2 (el)
IL (1) IL263080B (el)
LT (1) LT3458067T (el)
MX (1) MX2018014168A (el)
PL (1) PL3458067T3 (el)
PT (1) PT3458067T (el)
RS (1) RS61655B1 (el)
RU (1) RU2765868C2 (el)
SG (1) SG11201809792TA (el)
SI (1) SI3458067T1 (el)
TW (1) TWI753912B (el)
WO (1) WO2017198346A1 (el)
ZA (1) ZA201807393B (el)

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Publication number Priority date Publication date Assignee Title
KR102483630B1 (ko) 2016-05-18 2023-01-02 토르쿠르 아게 피부 병변의 치료
RU2020115351A (ru) * 2017-11-23 2021-12-23 Пикур Терапьютикс Аг Лечение кожных заболеваний
BR112023020804A2 (pt) * 2021-04-09 2023-12-19 Univ Basel Derivado de triazina como inibidores covalentes reversíveis e irreversíveis de pi3k

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Publication number Priority date Publication date Assignee Title
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CA2838399C (en) * 2006-02-09 2017-03-07 Alba Therapeutics Corporation Formulations for a tight junction effector
JP5546240B2 (ja) * 2006-04-26 2014-07-09 ジェネンテック, インコーポレイテッド 医薬化合物
PL2050749T3 (pl) 2006-08-08 2018-03-30 Chugai Seiyaku Kabushiki Kaisha Pochodna pirymidyny jako inhibitor pi3k i jej zastosowanie
JP2010518107A (ja) * 2007-02-06 2010-05-27 ノバルティス アーゲー Pi3−キナーゼ阻害剤およびその使用方法
NZ588526A (en) 2008-05-23 2012-08-31 Wyeth Llc Triazine compounds as pi3 kinase and mtor inhibitors
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
SG11201602602RA (en) 2013-10-04 2016-04-28 Univ Basel Conformationally restricted pi3k and mtor inhibitors
MA40933A (fr) * 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
WO2017198347A1 (en) 2016-05-18 2017-11-23 Piqur Therapeutics Ag Treatment of skin lesions
KR102483630B1 (ko) * 2016-05-18 2023-01-02 토르쿠르 아게 피부 병변의 치료

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EP3458067A1 (en) 2019-03-27
JP6991158B2 (ja) 2022-02-10
WO2017198346A1 (en) 2017-11-23
US20220135551A1 (en) 2022-05-05
TW201808944A (zh) 2018-03-16
RU2018140013A3 (el) 2020-07-09
BR112018073579A8 (pt) 2023-01-10
RS61655B1 (sr) 2021-04-29
MX2018014168A (es) 2019-04-29
RU2018140013A (ru) 2020-06-18
HUE053494T2 (hu) 2021-06-28
CN109475560B (zh) 2023-05-02
AU2017265383A1 (en) 2018-12-13
US20240343718A1 (en) 2024-10-17
SI3458067T1 (sl) 2021-07-30
HRP20210477T1 (hr) 2021-05-14
BR112018073579A2 (pt) 2019-03-19
TWI753912B (zh) 2022-02-01
US11878972B2 (en) 2024-01-23
DK3458067T3 (da) 2021-04-06
PL3458067T3 (pl) 2021-12-13
IL263080A (en) 2018-12-31
ES2863250T3 (es) 2021-10-11
KR20190008294A (ko) 2019-01-23
IL263080B (en) 2022-02-01
US20190284178A1 (en) 2019-09-19
KR102472461B1 (ko) 2022-11-30
PT3458067T (pt) 2021-04-07
EP3458067B1 (en) 2020-12-30
SG11201809792TA (en) 2018-12-28
JP2019519507A (ja) 2019-07-11
CA3022753A1 (en) 2017-11-23
ZA201807393B (en) 2023-10-25
LT3458067T (lt) 2021-04-26
CN109475560A (zh) 2019-03-15
AU2017265383B2 (en) 2022-07-28
RU2765868C2 (ru) 2022-02-04

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