MX2016016190A - Derivados de pirazino[2,1-a]isoquinolina sustituida para el tratamiento de trastornos del sistema nervioso central. - Google Patents

Derivados de pirazino[2,1-a]isoquinolina sustituida para el tratamiento de trastornos del sistema nervioso central.

Info

Publication number
MX2016016190A
MX2016016190A MX2016016190A MX2016016190A MX2016016190A MX 2016016190 A MX2016016190 A MX 2016016190A MX 2016016190 A MX2016016190 A MX 2016016190A MX 2016016190 A MX2016016190 A MX 2016016190A MX 2016016190 A MX2016016190 A MX 2016016190A
Authority
MX
Mexico
Prior art keywords
disorders
halogen
lower alkyl
substituted
treatment
Prior art date
Application number
MX2016016190A
Other languages
English (en)
Inventor
Galley Guido
Norcross Roger
Pflieger Philippe
Cecere Giuseppe
Patiny-Adam Angélique
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 MX2016016190A publication Critical patent/MX2016016190A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

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

Abstract

La presente invención se refiere a un compuesto de fórmula (I) en donde R1/R2 son independientemente uno de otro hidrógeno o halógeno; L es un enlace, -NH-, -C(O)NH-, -NHC(O) - o NHC(O)NH-; R es hidrógeno, alquilo inferior, cicloalquilo, bencilo, fenilo o un grupo heteroarilo de cinco o seis miembros, en donde los grupos fenilo y heteroarilo están opcionalmente sustituidos por uno o dos sustituyentes, seleccionados de halógeno, alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halógeno, alcoxi inferior sustituido por halógeno, cicloalquilo o di-alquil amino inferior o R es halógeno si L es un enlace o a una sal de adición de ácido farmacéuticamente apropiada del mismo, a todas las mezclas racémicas, todos sus enantiómeros correspondientes y/o isómeros ópticos. Los compuestos de fórmulas (I) tienen una buena afinidad por los receptores asociados con las amina traza (TAAR), en especial para TAAR1 y se pueden usar para el tratamiento de depresión, trastorno de ansiedad, trastorno bipolar, trastorno de déficit de atención con hiperactividad (ADHD), trastornos relacionados con el estrés, trastornos psicóticos como esquizofrenia, enfermedades neurológicas tales como enfermedad de Parkinson, trastornos neurodegenerativos tales como la enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias y trastornos metabólicos tales como trastornos de alimentación, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos y mal funcionamiento de la homeostasis de la temperatura corporal, trastornos del sueño y de ritmo circadiano, y trastornos cardiovasculares.
MX2016016190A 2014-08-27 2015-08-24 Derivados de pirazino[2,1-a]isoquinolina sustituida para el tratamiento de trastornos del sistema nervioso central. MX2016016190A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14182460 2014-08-27
PCT/EP2015/069309 WO2016030306A1 (en) 2014-08-27 2015-08-24 Substituted pyrazino[2,1-a]isoquinoline derivatives for the treatment of cns disorders

Publications (1)

Publication Number Publication Date
MX2016016190A true MX2016016190A (es) 2017-03-08

Family

ID=51398569

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016016190A MX2016016190A (es) 2014-08-27 2015-08-24 Derivados de pirazino[2,1-a]isoquinolina sustituida para el tratamiento de trastornos del sistema nervioso central.

Country Status (9)

Country Link
US (2) US9828374B2 (es)
EP (1) EP3186250B1 (es)
JP (1) JP6364122B2 (es)
KR (1) KR101909845B1 (es)
CN (1) CN106470994B (es)
CA (1) CA2953040A1 (es)
MX (1) MX2016016190A (es)
RU (1) RU2017106928A (es)
WO (1) WO2016030306A1 (es)

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4517187A (en) * 1982-10-18 1985-05-14 Pennwalt Corporation 1,3,4,6,7-11b-Hexahydro-7-phenyl-2H-pyrazino[2,1-a]isoquinolines methods of preparation, and use as antidepressants
GB9425211D0 (en) 1994-12-14 1995-02-15 Ucb Sa Substituted 1H-imidazoles
GB9520150D0 (en) 1995-10-03 1995-12-06 Orion Yhtymae Oy New imidazole derivatives
US6841684B2 (en) 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
CA2446795A1 (en) * 2001-05-10 2002-11-14 Agouron Pharmaceuticals, Inc. Sulfamide, sulfamate, sulfonamide, urea, amide, alpha, alpha-difluoro amide oxalyl diamide, and heterobicycles fkbp-binding ligands
KR100682506B1 (ko) * 2005-01-18 2007-02-15 (주)젠크로스 프라지콴텔, 또는 이의 염을 포함하는 약학 조성물
CA2612495A1 (en) * 2005-06-17 2006-12-28 Janssen Pharmaceutica N.V. Hexahydro-pyrrolo-isoquinoline compounds for the treatment of cns disorders
TW200813015A (en) * 2006-03-15 2008-03-16 Mitsubishi Pharma Corp 2-(cyclic amino)-pyrimidone derivatives
KR100799020B1 (ko) * 2006-06-30 2008-01-28 주식회사 하이닉스반도체 반도체 메모리 소자의 제조방법
RU2456281C2 (ru) * 2006-11-16 2012-07-20 Ф. Хоффманн-Ля Рош Аг Замещенные 4-имидазолы, способ их получения и их применение
RU2460725C2 (ru) 2007-02-15 2012-09-10 Ф. Хоффманн-Ля Рош Аг Новые 2-аминооксазолины в качестве лигандов taar1
WO2009124755A1 (en) * 2008-04-08 2009-10-15 European Molecular Biology Laboratory (Embl) Compounds with novel medical uses and method of identifying such compounds
CN103910725B (zh) * 2013-01-09 2015-12-02 江南大学 一类吡喹酮类似物、其制备方法和用途

Also Published As

Publication number Publication date
WO2016030306A1 (en) 2016-03-03
JP6364122B2 (ja) 2018-07-25
US20170145010A1 (en) 2017-05-25
CA2953040A1 (en) 2016-03-03
RU2017106928A3 (es) 2019-03-18
RU2017106928A (ru) 2018-10-01
KR20170029634A (ko) 2017-03-15
CN106470994B (zh) 2019-09-24
EP3186250A1 (en) 2017-07-05
JP2017523990A (ja) 2017-08-24
US10316036B2 (en) 2019-06-11
CN106470994A (zh) 2017-03-01
EP3186250B1 (en) 2018-04-18
US20180037582A1 (en) 2018-02-08
US9828374B2 (en) 2017-11-28
KR101909845B1 (ko) 2018-10-18

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