MX347239B - Derivados de pirazol. - Google Patents

Derivados de pirazol.

Info

Publication number
MX347239B
MX347239B MX2013013853A MX2013013853A MX347239B MX 347239 B MX347239 B MX 347239B MX 2013013853 A MX2013013853 A MX 2013013853A MX 2013013853 A MX2013013853 A MX 2013013853A MX 347239 B MX347239 B MX 347239B
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MX
Mexico
Prior art keywords
halogen
disorders
sup
lower alkyl
substituted
Prior art date
Application number
MX2013013853A
Other languages
English (en)
Other versions
MX2013013853A (es
Inventor
Galley Guido
Norcross Roger
Pflieger Philippe
Ghellamallah Cédric
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 MX2013013853A publication Critical patent/MX2013013853A/es
Publication of MX347239B publication Critical patent/MX347239B/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
    • 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)
  • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a compuestos de la fórmula (Ver Formula) en donde: 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 seleccionados 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 lA 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 depresión, trastornos de ansiedad, trastorno bipolar, trastorno de hiperactividad con déficit de atención (por sus siglas en inglés, ADHD), trastornos relacionados con el estrés, trastornos psicóticos como son esquizofrenia, enfermedades neurológicas, por ejemplo enfermedad de Parkinson, trastornos neurodegenerativos, por ejemplo enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias y trastornos metabólicos, por ejemplo trastornos de ingestión de comida, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos y malfunción de la temperatura corporal, homeostasis, trastornos del sueño y ritmo circadiano y trastornos cardiovasculares.
MX2013013853A 2011-06-09 2012-06-06 Derivados de pirazol. MX347239B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11169217 2011-06-09
PCT/EP2012/060627 WO2012168260A1 (en) 2011-06-09 2012-06-06 Pyrazole derivatives

Publications (2)

Publication Number Publication Date
MX2013013853A MX2013013853A (es) 2014-01-20
MX347239B true MX347239B (es) 2017-04-20

Family

ID=46298390

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013013853A MX347239B (es) 2011-06-09 2012-06-06 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 (18)

* 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
KR101631003B1 (ko) * 2012-01-12 2016-06-15 에프. 호프만-라 로슈 아게 미량 아민 결합 수용체(taar)로서 헤테로환형 유도체
MA37944B2 (fr) 2012-09-14 2017-10-31 Hoffmann La Roche Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson
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
JP6814814B2 (ja) 2016-03-17 2021-01-20 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Taarのアゴニストとしての活性を有する5−エチル−4−メチル−ピラゾール−3−カルボキサミド誘導体
CA3060715C (en) 2017-04-24 2024-10-01 Tesaro, Inc. PROCESSES FOR MANUFACTURING 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
WO2020230136A1 (en) * 2019-05-14 2020-11-19 Metabomed Ltd Acss2 inhibitors and methods of use thereof
ES2966457T3 (es) * 2018-06-18 2024-04-22 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
CN112752755A (zh) 2018-09-27 2021-05-04 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的杂环基化合物
KR102396602B1 (ko) * 2019-02-28 2022-05-11 주식회사 마더스제약 피라졸 아마이드 유도체 화합물 및 이의 용도
KR20220035106A (ko) * 2019-07-11 2022-03-21 에프. 호프만-라 로슈 아게 치환된 피라졸 유도체의 제조 방법
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
KR20250176791A (ko) 2024-06-13 2025-12-22 인천대학교 산학협력단 피라졸 유도체를 유효성분으로 포함하는 항노화 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
US6841684B2 (en) * 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
IL136388A0 (en) 1997-12-04 2001-06-14 Allergan Sales Inc Substituted imidazole derivatives having agonist-like activity at alpha 2b or 2b/2c adrenergic receptors
JP5130305B2 (ja) 2007-02-15 2013-01-30 エフ.ホフマン−ラ ロシュ アーゲー Taar1リガンドとしての2−アミノオキサゾリン
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
TWI440636B (zh) 2014-06-11
MY162160A (en) 2017-05-31
TW201302727A (zh) 2013-01-16
PH12013502315A1 (en) 2016-05-11
AU2012266457A1 (en) 2013-11-14
RS54183B1 (sr) 2015-12-31
BR112013031324A2 (pt) 2016-11-29
MA35192B1 (fr) 2014-06-02
IL229549A0 (en) 2014-01-30
JP2014516066A (ja) 2014-07-07
ECSP13013072A (es) 2014-01-31
KR20140029517A (ko) 2014-03-10
EP2717873B1 (en) 2015-07-15
SI2717873T1 (sl) 2015-09-30
UA110525C2 (ru) 2016-01-12
PL2717873T3 (pl) 2015-12-31
KR101574905B1 (ko) 2015-12-04
IL229549B (en) 2019-06-30
EP2717873A1 (en) 2014-04-16
AU2012266457B2 (en) 2016-09-08
JP5914642B2 (ja) 2016-05-11
EA201391787A1 (ru) 2014-04-30
CY1116778T1 (el) 2017-03-15
ZA201308939B (en) 2014-08-27
CN103596567B (zh) 2016-03-16
AR088741A1 (es) 2014-07-02
MX2013013853A (es) 2014-01-20
PE20140934A1 (es) 2014-08-06
ES2546438T3 (es) 2015-09-23
CO6801764A2 (es) 2013-11-29
CL2013003484A1 (es) 2014-08-08
DK2717873T3 (en) 2015-07-27
PT2717873E (pt) 2015-09-18
US9073911B2 (en) 2015-07-07
BR112013031324B1 (pt) 2021-11-03
HK1191862A1 (zh) 2014-08-08
NZ617350A (en) 2016-01-29
WO2012168260A1 (en) 2012-12-13
CA2837255C (en) 2020-10-27
CA2837255A1 (en) 2012-12-13
EA024648B1 (ru) 2016-10-31
US20120316172A1 (en) 2012-12-13
CN103596567A (zh) 2014-02-19
HRP20151077T1 (hr) 2015-11-06
SG195156A1 (en) 2013-12-30

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