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MX2018014168A - Tratamiento de transtornos neurologicos. - Google Patents

Tratamiento de transtornos neurologicos.

Info

Publication number
MX2018014168A
MX2018014168A MX2018014168A MX2018014168A MX2018014168A MX 2018014168 A MX2018014168 A MX 2018014168A MX 2018014168 A MX2018014168 A MX 2018014168A MX 2018014168 A MX2018014168 A MX 2018014168A MX 2018014168 A MX2018014168 A MX 2018014168A
Authority
MX
Mexico
Prior art keywords
formula
optionally substituted
alkyl
independently
alkoxy
Prior art date
Application number
MX2018014168A
Other languages
English (en)
Inventor
Beaufils Florent
Rageot Denise
Hebeisen Paul
Fabbro Doriano
HILLMANN-WULLNER Petra
Huu Phuc Nguyen Hoa
Löscher Wolfgang
BRANDT Claudia
Markus SELE Alexander
Original Assignee
Piqur Therapeutics 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 Piqur Therapeutics Ag filed Critical Piqur Therapeutics Ag
Publication of MX2018014168A publication Critical patent/MX2018014168A/es

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    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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)
  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente invención se refiere a un compuesto de fórmula (I), (VER FORMULA) (I) en donde X1, X2 y X3 son, independientemente de entre sí, N o CH; con la condición de que al menos dos de X1, X2 y X3 son N; Y es N o CH; R1 y R2 son independientemente de entre sí (iii) un morfolinilo de fórmula (II) (VER FORMULA) N O R3 R4 (II) en donde la flecha denota el enlace en la fórmula (I); y en donde R3 y R4 son independientemente de entre sí H, alquilo C1-C3 opcionalmente sustituido con uno o dos OH, fluoroalquilo C1-C2, alcoxi C1-C2, alcoxi C1-C2 alquilo C1-C3, CN, o C(O)Oalquilo C1-C2; o R3 y R4 forman en conjunto un residuo bivalente -R5R6- seleccionado a partir de alquileno C1-C3 opcionalmente sustituido con 1 hasta 4 F, -CH2-O-CH2-, -CH2-NH-CH2-, o cualquiera de las estructuras (VER FORMULA) O ; en donde las flechas denotan los enlaces en la fórmula (II); o (iv) un anillo heterocíclico Z de 6 elementos saturado seleccionado a partir de tiomorfolinilo y piperazinilo, opcionalmente sustituido por 1 hasta 3 R7; en donde R7 es independientemente en cada caso alquilo C1-C3 opcionalmente sustituido con uno o dos OH, fluoroalquilo C1-C2, alcoxi C1-C2 alquilo C1-C3, cicloalquilo C3-C6; o dos sustituyentes R7 forman en conjunto un residuo bivalente -R8R9- seleccionado a partir de alquileno C1-C3 opcionalmente sustituido con 1 hasta 4 F, -CH2-O-CH2- o -O-CH2CH2-O-;con la condición de que al menos uno de R1 y R2 es un morfolinilo de fórmula II; y profármacos, metabolitos, tautómeros, solvatos y sales de los mismos farmacéuticamente aceptables, para uso en la prevención o tratamiento de un trastorno neurológico en un sujeto.
MX2018014168A 2016-05-18 2017-05-17 Tratamiento de transtornos neurologicos. MX2018014168A (es)

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
MX2018014168A true MX2018014168A (es) 2019-04-29

Family

ID=56024138

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018014168A MX2018014168A (es) 2016-05-18 2017-05-17 Tratamiento de transtornos neurologicos.

Country Status (25)

Country Link
US (3) US20190284178A1 (es)
EP (1) EP3458067B1 (es)
JP (1) JP6991158B2 (es)
KR (1) KR102472461B1 (es)
CN (1) CN109475560B (es)
AU (1) AU2017265383B2 (es)
CA (1) CA3022753C (es)
CY (1) CY1124051T1 (es)
DK (1) DK3458067T3 (es)
ES (1) ES2863250T3 (es)
HR (1) HRP20210477T1 (es)
HU (1) HUE053494T2 (es)
IL (1) IL263080B (es)
LT (1) LT3458067T (es)
MX (1) MX2018014168A (es)
PL (1) PL3458067T3 (es)
PT (1) PT3458067T (es)
RS (1) RS61655B1 (es)
RU (1) RU2765868C2 (es)
SG (1) SG11201809792TA (es)
SI (1) SI3458067T1 (es)
SM (1) SMT202100177T1 (es)
TW (1) TWI753912B (es)
WO (1) WO2017198346A1 (es)
ZA (1) ZA201807393B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7118509B2 (ja) 2016-05-18 2022-08-16 トルク アーゲー 皮膚病変の治療
SG11202004589SA (en) * 2017-11-23 2020-06-29 Piqur Therapeutics Ag Treatment of skin disorders
IL307565A (en) * 2021-04-09 2023-12-01 Universit?T Basel Triazine derivatives as reversible and irreversible covalent inhibitors of PI3K
CN117396470A (zh) * 2021-04-09 2024-01-12 巴塞尔大学 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物

Family Cites Families (11)

* Cited by examiner, † Cited by third party
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
EP1993357B1 (en) * 2006-02-09 2014-01-22 Alba Therapeutics Corporation Formulations for a tight junction effector
PL2041139T3 (pl) 2006-04-26 2012-05-31 Hoffmann La Roche Związki farmaceutyczne
RU2448109C2 (ru) 2006-08-08 2012-04-20 Чугаи Сейяку Кабусики Кайся Производное пиримидина в качестве ингибитора pi3k и его применение
KR20090108124A (ko) * 2007-02-06 2009-10-14 노파르티스 아게 Ｐｉ 3-키나제 억제제 및 그의 사용 방법
DK3216793T3 (da) * 2008-05-23 2019-05-06 Wyeth Llc Triazinforbindelser som p13-kinase- og mtor-inhibitorer
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
JP6426745B2 (ja) 2013-10-04 2018-11-21 ウニヴェルズィテート バーゼル 配座固定されたＰＩ３Ｋ及びｍＴＯＲ阻害剤
MA40933A (fr) * 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
JP7118509B2 (ja) * 2016-05-18 2022-08-16 トルク アーゲー 皮膚病変の治療
AU2017265384B2 (en) 2016-05-18 2023-02-23 The Trustees Of The University Of Pennsylvania Treatment of skin lesions

Also Published As

Publication number Publication date
KR20190008294A (ko) 2019-01-23
RS61655B1 (sr) 2021-04-29
AU2017265383A1 (en) 2018-12-13
RU2765868C2 (ru) 2022-02-04
HRP20210477T1 (hr) 2021-05-14
US20240343718A1 (en) 2024-10-17
RU2018140013A3 (es) 2020-07-09
JP2019519507A (ja) 2019-07-11
EP3458067A1 (en) 2019-03-27
NZ748601A (en) 2024-12-20
BR112018073579A2 (pt) 2019-03-19
TW201808944A (zh) 2018-03-16
DK3458067T3 (da) 2021-04-06
US11878972B2 (en) 2024-01-23
TWI753912B (zh) 2022-02-01
KR102472461B1 (ko) 2022-11-30
EP3458067B1 (en) 2020-12-30
IL263080A (en) 2018-12-31
CA3022753A1 (en) 2017-11-23
SMT202100177T1 (it) 2021-05-07
PL3458067T3 (pl) 2021-12-13
SG11201809792TA (en) 2018-12-28
BR112018073579A8 (pt) 2023-01-10
SI3458067T1 (sl) 2021-07-30
WO2017198346A1 (en) 2017-11-23
RU2018140013A (ru) 2020-06-18
ES2863250T3 (es) 2021-10-11
CA3022753C (en) 2024-09-24
US20190284178A1 (en) 2019-09-19
CY1124051T1 (el) 2022-05-27
PT3458067T (pt) 2021-04-07
ZA201807393B (en) 2023-10-25
CN109475560A (zh) 2019-03-15
JP6991158B2 (ja) 2022-02-10
AU2017265383B2 (en) 2022-07-28
US20220135551A1 (en) 2022-05-05
HUE053494T2 (hu) 2021-06-28
IL263080B (en) 2022-02-01
CN109475560B (zh) 2023-05-02
LT3458067T (lt) 2021-04-26

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