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AR088741A1 - Derivados de pirazol - Google Patents

Derivados de pirazol

Info

Publication number
AR088741A1
AR088741A1 ARP120102009A ARP120102009A AR088741A1 AR 088741 A1 AR088741 A1 AR 088741A1 AR P120102009 A ARP120102009 A AR P120102009A AR P120102009 A ARP120102009 A AR P120102009A AR 088741 A1 AR088741 A1 AR 088741A1
Authority
AR
Argentina
Prior art keywords
halogen
disorders
substituted
optionally substituted
lower alkyl
Prior art date
Application number
ARP120102009A
Other languages
English (en)
Inventor
Ghellamallah Cedric
Pflieger Philippe
Norcross Roger
Galley Guido
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 AR088741A1 publication Critical patent/AR088741A1/es

Links

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

Landscapes

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

Abstract

La presente se refiere a compuestos de la fórmula (1) ó (2) en las que: R¹ es hidrógeno o fenilo opcionalmente sustituido por halógeno, 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. Se ha encontrado que los compuestos de las fórmulas (1) y (2) 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.
ARP120102009A 2011-06-09 2012-06-07 Derivados de pirazol AR088741A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR088741A1 true AR088741A1 (es) 2014-07-02

Family

ID=46298390

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120102009A AR088741A1 (es) 2011-06-09 2012-06-07 Derivados de pirazol

Country Status (33)

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)
HK (1) HK1191862A1 (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
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
US9580407B2 (en) * 2012-12-07 2017-02-28 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
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).
AU2018258274C1 (en) 2017-04-24 2021-12-02 Tesaro, Inc. Methods of manufacturing of niraparib
CN112480079B (zh) * 2017-11-08 2022-03-11 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
WO2020064792A1 (en) 2018-09-27 2020-04-02 F. Hoffmann-La Roche Ag Heterocyclyl compounds for the treatment of autoimmune disease
KR102396602B1 (ko) * 2019-02-28 2022-05-11 주식회사 마더스제약 피라졸 아마이드 유도체 화합물 및 이의 용도
CN114008025A (zh) * 2019-05-14 2022-02-01 美特波米德有限公司 Acss2抑制剂和其使用方法
CA3146830A1 (en) * 2019-07-11 2021-01-14 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
CN119654138A (zh) * 2022-08-12 2025-03-18 豪夫迈·罗氏有限公司 包含5-乙基-4-甲基-n-[4-[(2s)吗啉-2-基]苯基]-1h-吡唑-3-甲酰胺的药物组合物

Family Cites Families (10)

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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
US6841684B2 (en) * 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
SK8542000A3 (en) 1997-12-04 2001-03-12 Allergan Sales Inc Substituted imidazole derivatives having agonist-like activity at alpha 2b or 2b/2c adrenergic receptors
RU2460725C2 (ru) 2007-02-15 2012-09-10 Ф. Хоффманн-Ля Рош Аг Новые 2-аминооксазолины в качестве лигандов taar1
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
TW201302727A (zh) 2013-01-16
MA35192B1 (fr) 2014-06-02
ZA201308939B (en) 2014-08-27
CN103596567A (zh) 2014-02-19
NZ617350A (en) 2016-01-29
JP2014516066A (ja) 2014-07-07
RS54183B1 (en) 2015-12-31
CA2837255C (en) 2020-10-27
BR112013031324B1 (pt) 2021-11-03
EP2717873A1 (en) 2014-04-16
EA024648B1 (ru) 2016-10-31
WO2012168260A1 (en) 2012-12-13
EA201391787A1 (ru) 2014-04-30
MY162160A (en) 2017-05-31
HRP20151077T1 (hr) 2015-11-06
UA110525C2 (ru) 2016-01-12
CA2837255A1 (en) 2012-12-13
AU2012266457B2 (en) 2016-09-08
BR112013031324A2 (pt) 2016-11-29
PT2717873E (pt) 2015-09-18
CL2013003484A1 (es) 2014-08-08
JP5914642B2 (ja) 2016-05-11
ECSP13013072A (es) 2014-01-31
MX2013013853A (es) 2014-01-20
US20120316172A1 (en) 2012-12-13
IL229549B (en) 2019-06-30
EP2717873B1 (en) 2015-07-15
KR20140029517A (ko) 2014-03-10
PL2717873T3 (pl) 2015-12-31
PE20140934A1 (es) 2014-08-06
DK2717873T3 (en) 2015-07-27
HK1191862A1 (zh) 2014-08-08
KR101574905B1 (ko) 2015-12-04
US9073911B2 (en) 2015-07-07
CO6801764A2 (es) 2013-11-29
AU2012266457A1 (en) 2013-11-14
SI2717873T1 (sl) 2015-09-30
PH12013502315A1 (en) 2016-05-11
IL229549A0 (en) 2014-01-30
ES2546438T3 (es) 2015-09-23
SG195156A1 (en) 2013-12-30
CN103596567B (zh) 2016-03-16
MX347239B (es) 2017-04-20
TWI440636B (zh) 2014-06-11
CY1116778T1 (el) 2017-03-15

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