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
Authority
CY
Cyprus
Prior art keywords
formula
optionally substituted
alkyl
treatment
morpholinyl
Prior art date
Application number
CY20211100267T
Other languages
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
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 Torqur Ag filed Critical Torqur Ag
Publication of CY1124051T1 publication Critical patent/CY1124051T1/el

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/14—Ortho-condensed systems
    • C07D491/153—Ortho-condensed systems the condensed system containing two rings with oxygen as ring hetero atom and one ring with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

Landscapes

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

Publication Number Publication Date
CY1124051T1 true CY1124051T1 (el) 2022-05-27

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US (2) 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
RU2018140001A (ru) 2016-05-18 2020-06-18 Пикур Терапьютикс Аг Лечение повреждений кожи
CN111315384A (zh) * 2017-11-23 2020-06-19 皮奎尔治疗公司 皮肤病的治疗
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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JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2007095092A2 (en) * 2006-02-09 2007-08-23 Alba Therapeutics Corporation Formulations for a tight junction effector
EP2402347A1 (en) 2006-04-26 2012-01-04 F. Hoffmann-La Roche AG Pharmaceutical compounds
NZ575274A (en) * 2006-08-08 2010-11-26 Chugai Pharmaceutical Co Ltd Pyrimidine derivative as pi3k inhibitor and use thereof
CN101711241A (zh) * 2007-02-06 2010-05-19 诺瓦提斯公司 Pi3-激酶抑制剂和它们的使用方法
CA2721710A1 (en) * 2008-05-23 2009-11-26 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
BR112016007122A2 (pt) 2013-10-04 2017-08-01 Piqur Therapeutics Ag inibidores de pi3k e mtor conformacionalmente restritos
MA40933A (fr) * 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
RU2018140001A (ru) * 2016-05-18 2020-06-18 Пикур Терапьютикс Аг Лечение повреждений кожи
AU2017265384B2 (en) 2016-05-18 2023-02-23 The Trustees Of The University Of Pennsylvania Treatment of skin lesions

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

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