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AR086880A1 - Derivados de morfolin-benzamidas sustituidas, composiciones farmaceuticas que los contienen y uso de las mismas para tratar enfermedades asociadas fundamentalmente al sistema nervioso central - Google Patents

Derivados de morfolin-benzamidas sustituidas, composiciones farmaceuticas que los contienen y uso de las mismas para tratar enfermedades asociadas fundamentalmente al sistema nervioso central

Info

Publication number
AR086880A1
AR086880A1 ARP120102045A ARP120102045A AR086880A1 AR 086880 A1 AR086880 A1 AR 086880A1 AR P120102045 A ARP120102045 A AR P120102045A AR P120102045 A ARP120102045 A AR P120102045A AR 086880 A1 AR086880 A1 AR 086880A1
Authority
AR
Argentina
Prior art keywords
disorders
halogen
trifluoromethyl
lower alkyl
pyridin
Prior art date
Application number
ARP120102045A
Other languages
English (en)
Inventor
Roger Norcross
Guido Galley
Philippe Pflieger
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR086880A1 publication Critical patent/AR086880A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Addiction (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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

La presente se refiere a compuestos de la fórmula (1) en la que: R1 es hidrógeno, halógeno, ciano, alquilo inferior, alquilo inferior sustituido por halógeno, alcoxi inferior, alcoxi inferior sustituido por halógeno o C(O)NH2, o es fenilo opcionalmente sustituido por halógeno, ciano o alcoxi inferior sustituido por halógeno, o es 2,2-difluorobenzo[d][1,3]dioxol-5-ilo, o es 6-(trifluorometil)-pirazin-2-ilo o 5-(trifluorometil)-pirazin-2-ilo o es 6-(trifluorometil)-pirimidin-4-ilo, o es 6-(trifluorometil)-piridin-3-ilo, o es 5-cianopirazin-2-ilo o es 2-(trifluorometil)pirimidin-4-ilo; n es el número 1 ó 2; R2 es halógeno, alquilo inferior o ciano y R3 es hidrógeno, o R2 es hidrógeno y R3 es halógeno, alquilo inferior o ciano; X es un enlace, -NR’-, -CH2NH- o -CHR’-; R’ es hidrógeno o alquilo inferior; Z es un enlace, -CH2- u -O-; Ar es fenilo o es heteroarilo elegido entre el grupo formado por 1H-indazol-3-ilo, piridin-2-ilo, piridin-3-ilo, piridin-4-ilo, pirimidin-5-ilo, 1H-pirazol-3-ilo, 1H-pirazol-4-ilo y 1H-pirazol-5-ilo; o una sal de adición de ácido farmacéuticamente apropiada de los mismos; que pueden utilizarse para el tratamiento de la depresión, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atención (ADHD), los trastornos relacionados con el estrés, los trastornos psicóticos, la esquizofrenia, las enfermedades neurológicas, la enfermedad de Parkinson, los trastornos neurodegenerativos, la enfermedad de Alzheimer, la epilepsia, la migraña, la hipertensión, el abuso de sustancias, los trastornos metabólicos, los trastornos de ingestión de comida, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos de consumo y asimilación de energía, los trastornos y mal función de la homeostasis de la temperatura corporal, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.
ARP120102045A 2011-06-10 2012-06-08 Derivados de morfolin-benzamidas sustituidas, composiciones farmaceuticas que los contienen y uso de las mismas para tratar enfermedades asociadas fundamentalmente al sistema nervioso central AR086880A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11169441 2011-06-10

Publications (1)

Publication Number Publication Date
AR086880A1 true AR086880A1 (es) 2014-01-29

Family

ID=46298391

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120102045A AR086880A1 (es) 2011-06-10 2012-06-08 Derivados de morfolin-benzamidas sustituidas, composiciones farmaceuticas que los contienen y uso de las mismas para tratar enfermedades asociadas fundamentalmente al sistema nervioso central

Country Status (33)

Country Link
US (1) US9029370B2 (es)
EP (1) EP2718271B1 (es)
JP (1) JP5788087B2 (es)
KR (1) KR101574906B1 (es)
CN (1) CN103596937B (es)
AR (1) AR086880A1 (es)
AU (1) AU2012266462B2 (es)
BR (1) BR112013030698B1 (es)
CA (1) CA2834675C (es)
CL (1) CL2013003485A1 (es)
CO (1) CO6811866A2 (es)
CY (1) CY1116769T1 (es)
DK (1) DK2718271T3 (es)
EA (1) EA022376B1 (es)
EC (1) ECSP13013073A (es)
ES (1) ES2546529T3 (es)
HK (1) HK1192562A1 (es)
HR (1) HRP20151201T1 (es)
IL (1) IL229335A (es)
MA (1) MA35194B1 (es)
MX (1) MX354410B (es)
MY (1) MY162461A (es)
PE (1) PE20140968A1 (es)
PH (1) PH12013502263A1 (es)
PL (1) PL2718271T3 (es)
PT (1) PT2718271E (es)
RS (1) RS54415B1 (es)
SG (1) SG194840A1 (es)
SI (1) SI2718271T1 (es)
TW (1) TWI445701B (es)
UA (1) UA110388C2 (es)
WO (1) WO2012168265A1 (es)
ZA (1) ZA201308401B (es)

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US9073911B2 (en) 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
MX354815B (es) * 2012-01-12 2018-03-22 Hoffmann La Roche Derivados heterociclicos como receptores asociados con las aminas traza (taars).
PE20150735A1 (es) * 2012-09-14 2015-05-17 Hoffmann La Roche Derivados de pirazol-carboxamida como moduladores de taar para uso en el tratamiento de numerosos desordenes, tales como depresion, diabetes y enfermedad de parkinson
ES2605632T3 (es) * 2012-09-17 2017-03-15 F. Hoffmann-La Roche Ag Derivados triazol carboxamida
WO2014072257A1 (en) * 2012-11-07 2014-05-15 F. Hoffmann-La Roche Ag Pyrazine derivatives
WO2015165085A1 (en) * 2014-04-30 2015-11-05 F.Hoffmann-La Roche Ag Morpholin-pyridine derivatives
RU2016149984A (ru) * 2014-05-28 2018-07-02 Ф. Хоффманн-Ля Рош Аг Производные 5-окса-2-азабицикло[2.2.2]октан-4-ила и 5-окса-2-азабицикло[2.2.1]гептан-4-ила в качестве модуляторов taar1
CN104478798B (zh) * 2014-12-18 2017-01-18 武汉华纳联合药业有限公司 N‑氨基烷基磺酰基‑3‑吡啶甲酰胺衍生物及其在制备治疗心脑血管病药物中的应用
MX377836B (es) * 2016-03-17 2025-03-11 F Hoffmann La Roche Ag Derivado de 5-etil-4-metil-pirazol-3-carboxamida teniendo actividad como agonista de receptor asociado con aminas trazas (taar).
CA3146830A1 (en) * 2019-07-11 2021-01-14 F. Hoffmann-La Roche Ag Process for the preparation of substituted pyrazole derivatives
AU2021225921A1 (en) * 2020-02-28 2022-09-22 Board Of Regents, The University Of Texas System Inhibitors of Receptor Interacting Protein Kinase I for the treatment of disease
TW202440563A (zh) * 2022-11-28 2024-10-16 美商住友製藥美國公司 2-苯基嗎啉與2-苯基(硫代)嗎啉化合物及其用途

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Also Published As

Publication number Publication date
CL2013003485A1 (es) 2014-09-12
ES2546529T3 (es) 2015-09-24
IL229335A (en) 2016-11-30
CO6811866A2 (es) 2013-12-16
CN103596937A (zh) 2014-02-19
MX2013014371A (es) 2014-01-31
SI2718271T1 (sl) 2015-11-30
PT2718271E (pt) 2015-10-29
WO2012168265A1 (en) 2012-12-13
CA2834675A1 (en) 2012-12-13
JP2014516067A (ja) 2014-07-07
CY1116769T1 (el) 2017-03-15
CA2834675C (en) 2019-09-03
PH12013502263A1 (en) 2016-06-29
MX354410B (es) 2018-03-05
EP2718271B1 (en) 2015-08-12
RS54415B1 (en) 2016-04-28
JP5788087B2 (ja) 2015-09-30
BR112013030698B1 (pt) 2022-05-31
CN103596937B (zh) 2016-06-29
DK2718271T3 (en) 2015-08-24
AU2012266462B2 (en) 2016-09-22
ECSP13013073A (es) 2014-01-31
UA110388C2 (xx) 2015-12-25
PL2718271T3 (pl) 2016-01-29
HK1192562A1 (zh) 2014-08-22
MA35194B1 (fr) 2014-06-02
EA201391815A1 (ru) 2014-04-30
PE20140968A1 (es) 2014-08-06
US20120316165A1 (en) 2012-12-13
IL229335A0 (en) 2014-01-30
KR101574906B1 (ko) 2015-12-04
TWI445701B (zh) 2014-07-21
NZ616820A (en) 2015-11-27
ZA201308401B (en) 2014-08-27
BR112013030698A2 (pt) 2016-12-06
SG194840A1 (en) 2013-12-30
US9029370B2 (en) 2015-05-12
HRP20151201T1 (hr) 2015-12-04
EA022376B1 (ru) 2015-12-30
EP2718271A1 (en) 2014-04-16
KR20140028102A (ko) 2014-03-07
MY162461A (en) 2017-06-15
TW201307308A (zh) 2013-02-16
AU2012266462A1 (en) 2013-10-31

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