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ECSP13013072A - Derivados de pirazol - Google Patents

Derivados de pirazol

Info

Publication number
ECSP13013072A
ECSP13013072A ECSP13013072A ECSP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A
Authority
EC
Ecuador
Prior art keywords
halogen
disorders
lower alkyl
optionally substituted
substituted
Prior art date
Application number
Other languages
English (en)
Inventor
Roger David Norcross
Guido Galley
Philippe Pflieger
Cédric Ghellamallah
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 ECSP13013072A publication Critical patent/ECSP13013072A/es

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Classifications

    • 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
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Addiction (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invención se refiere a compuestos de la fórmula IA o IBen las que:R1 es hidrógeno o fenilo opcionalmente sustituido por haló-geno, CN o alcoxi inferior o alcoxi inferior sustituido por halógeno; R2 es hidrógeno o alquilo inferior;R3 es hidrógeno o alquilo inferior o es fenilo opcionalmente sustituido por uno o más sustituyentes elegidos entre halógeno, ciano o alcoxi inferior sustituido por halógeno, o es piridinilo opcionalmente sustituido por halógeno o alquilo inferior sustituido por halógeno, o es pirimidinilo, opcionalmente sustituido por alquilo inferior sustituido por halógeno, o es pirazinilo, opcionalmente sustituido por halógeno, ciano o alquilo inferior sustituido por halógeno;R4 es hidrógeno, alquilo inferior o fenilo;Z es un enlace, -CH2- u -O-;o a una sal de adición de ácido farmacéuticamente aceptable de los mismos.Ahora se ha encontrado que los compuestos de las fórmulas IA e IB tienen buena afinidad con los receptores asociados con las aminas traza (TAARs), en especial con el TAAR1.Estos compuestos 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 como son la esquizofrenia, las enfermedades neurológicas, por ejemplo la enfermedad de Parkinson, los trastornos neurodegenerativos, por ejemplo la enfermedad de Alzheimer, la epilepsia, la migraña, la hipertensión, el abuso de sustancias y los trastornos metabólicos, por ejemplo 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 malfunción de la temperatura corporal, la homeostasis, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.
ECSP13013072 2011-06-09 2013-12-09 Derivados de pirazol ECSP13013072A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11169217 2011-06-09

Publications (1)

Publication Number Publication Date
ECSP13013072A true ECSP13013072A (es) 2014-01-31

Family

ID=46298390

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13013072 ECSP13013072A (es) 2011-06-09 2013-12-09 Derivados de pirazol

Country Status (32)

Country Link
US (1) US9073911B2 (es)
EP (1) EP2717873B1 (es)
JP (1) JP5914642B2 (es)
KR (1) KR101574905B1 (es)
CN (1) CN103596567B (es)
AR (1) AR088741A1 (es)
AU (1) AU2012266457B2 (es)
BR (1) BR112013031324B1 (es)
CA (1) CA2837255C (es)
CL (1) CL2013003484A1 (es)
CO (1) CO6801764A2 (es)
CY (1) CY1116778T1 (es)
DK (1) DK2717873T3 (es)
EA (1) EA024648B1 (es)
EC (1) ECSP13013072A (es)
ES (1) ES2546438T3 (es)
HR (1) HRP20151077T1 (es)
IL (1) IL229549B (es)
MA (1) MA35192B1 (es)
MX (1) MX347239B (es)
MY (1) MY162160A (es)
PE (1) PE20140934A1 (es)
PH (1) PH12013502315A1 (es)
PL (1) PL2717873T3 (es)
PT (1) PT2717873E (es)
RS (1) RS54183B1 (es)
SG (1) SG195156A1 (es)
SI (1) SI2717873T1 (es)
TW (1) TWI440636B (es)
UA (1) UA110525C2 (es)
WO (1) WO2012168260A1 (es)
ZA (1) ZA201308939B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029370B2 (en) 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
WO2013104591A1 (en) 2012-01-12 2013-07-18 F. Hoffmann-La Roche Ag Heterocyclic derivatives as trace amine associated receptors (taars)
EP2895477B1 (en) * 2012-09-14 2017-11-01 F. Hoffmann-La Roche AG Pyrazole carboxamide derivatives as taar modulators for use in the treatment of several disorders, such as depression, diabetes and parkinson's disease.
WO2014088983A1 (en) * 2012-12-07 2014-06-12 Merck Sharp & Dohme Corp. Regioselective n-2 arylation of indazoles
WO2015165085A1 (en) * 2014-04-30 2015-11-05 F.Hoffmann-La Roche Ag Morpholin-pyridine derivatives
BR112018015389B1 (pt) 2016-03-17 2023-12-19 F. Hoffmann-La Roche Ag Derivado de 5-etil-4-metil-pirazol-3-carboxamida, seu processo de fabricação, preparação farmacêutica oral e uso
AU2018258274C1 (en) 2017-04-24 2021-12-02 Tesaro, Inc. Methods of manufacturing of niraparib
CN112480005B (zh) * 2017-11-08 2022-08-19 北京嘉林药业股份有限公司 化合物及其治疗癌症的用途
MX2020013899A (es) * 2018-06-18 2021-05-27 Janssen Pharmaceutica Nv Derivados de pirazol como inhibidores de malt1.
KR102161787B1 (ko) * 2018-07-02 2020-10-06 한국기초과학지원연구원 수면 장애의 예방 또는 치료용 약학적 조성물
US20210395239A1 (en) 2018-09-27 2021-12-23 Hoffmann-La Roche Inc. Heterocyclyl compounds for the treatment of autoimmune disease
WO2020175957A1 (ko) * 2019-02-28 2020-09-03 주식회사 마더스제약 피라졸 아마이드 유도체 화합물 및 이의 용도
EP3983386A4 (en) * 2019-05-14 2023-01-11 Metabomed Ltd ACSS2 INHIBITORS AND METHODS OF USE THEREOF
AU2020310539A1 (en) * 2019-07-11 2022-01-06 F. Hoffmann-La Roche Ag Process for the preparation of substituted pyrazole derivatives
WO2023283369A1 (en) * 2021-07-08 2023-01-12 Vibliome Therapeutics, Llc Modulators of protein kinases
WO2023183444A1 (en) * 2022-03-24 2023-09-28 Vibliome Therapeutics, Llc Modulators of protein kinases
KR20250044870A (ko) * 2022-08-12 2025-04-01 에프. 호프만-라 로슈 아게 5-에틸-4-메틸-n-[4-[(2s) 모르폴린-2-일]페닐]-1h-피라졸-3-카르복스아미드를 포함하는 약제학적 조성물

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
BR9813381A (pt) 1997-12-04 2000-10-03 Allergan Sales Inc "derivados de imidazol substituìdo possuindo atividade semelhante a agonista em receptores adrenérgicos alfa 2b ou 2b/2c"
US6841684B2 (en) 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
EP2121641B1 (en) 2007-02-15 2014-09-24 F. Hoffmann-La Roche AG 2-aminooxazolines as taar1 ligands
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
US9132136B2 (en) * 2010-08-02 2015-09-15 Hoffmann-La Roche Inc. Pharmaceutical combination
US9029370B2 (en) 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
CN102899314A (zh) 2011-07-29 2013-01-30 江汉大学 一种批量基因克隆的方法

Also Published As

Publication number Publication date
SG195156A1 (en) 2013-12-30
KR20140029517A (ko) 2014-03-10
RS54183B1 (sr) 2015-12-31
PT2717873E (pt) 2015-09-18
CN103596567B (zh) 2016-03-16
MX2013013853A (es) 2014-01-20
WO2012168260A1 (en) 2012-12-13
UA110525C2 (ru) 2016-01-12
MY162160A (en) 2017-05-31
BR112013031324B1 (pt) 2021-11-03
HRP20151077T1 (hr) 2015-11-06
IL229549A0 (en) 2014-01-30
AU2012266457A1 (en) 2013-11-14
BR112013031324A2 (pt) 2016-11-29
AU2012266457B2 (en) 2016-09-08
EP2717873B1 (en) 2015-07-15
SI2717873T1 (sl) 2015-09-30
CN103596567A (zh) 2014-02-19
AR088741A1 (es) 2014-07-02
JP2014516066A (ja) 2014-07-07
PL2717873T3 (pl) 2015-12-31
DK2717873T3 (en) 2015-07-27
US20120316172A1 (en) 2012-12-13
CA2837255A1 (en) 2012-12-13
EA024648B1 (ru) 2016-10-31
CO6801764A2 (es) 2013-11-29
US9073911B2 (en) 2015-07-07
MX347239B (es) 2017-04-20
ES2546438T3 (es) 2015-09-23
KR101574905B1 (ko) 2015-12-04
CA2837255C (en) 2020-10-27
TW201302727A (zh) 2013-01-16
MA35192B1 (fr) 2014-06-02
PH12013502315A1 (en) 2016-05-11
ZA201308939B (en) 2014-08-27
IL229549B (en) 2019-06-30
JP5914642B2 (ja) 2016-05-11
EP2717873A1 (en) 2014-04-16
HK1191862A1 (zh) 2014-08-08
TWI440636B (zh) 2014-06-11
CY1116778T1 (el) 2017-03-15
PE20140934A1 (es) 2014-08-06
EA201391787A1 (ru) 2014-04-30
CL2013003484A1 (es) 2014-08-08
NZ617350A (en) 2016-01-29

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