MA37944B2 - 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 - Google Patents

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

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Publication number
MA37944B2
MA37944B2 MA37944A MA37944A MA37944B2 MA 37944 B2 MA37944 B2 MA 37944B2 MA 37944 A MA37944 A MA 37944A MA 37944 A MA37944 A MA 37944A MA 37944 B2 MA37944 B2 MA 37944B2
Authority
MA
Morocco
Prior art keywords
lower alkyl
halogen
substituted
disorders
hydroxy
Prior art date
Application number
MA37944A
Other languages
English (en)
Other versions
MA37944A1 (fr
Inventor
Guido Galley
Roger Norcross
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 MA37944A1 publication Critical patent/MA37944A1/fr
Publication of MA37944B2 publication Critical patent/MA37944B2/fr

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    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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

Abstract

La présente invention concerne des composés de formule (i) dans laquelle r1 est phényle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alcoxy inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxy ; ou est pyridine-2, 3 ou 4-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxyle ; ou est pyrimidin-2, 4 ou 5-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par hydroxy ou alkyle inférieur substitué par halogène ; ou est pyrazin-2-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy ou cyano ; ou est 2,2-difluorobenzo[d][1,3]dioxol-5-yle, ou est thiazolyle, facultativement substitué par alkyle inférieur substitué par halogène ; r2 est hydrogène ou alkyle inférieur ; r3 est hydrogène, amino ou alkyle inférieur ; z est une liaison, -ch2- ou -o- ; ou un sel d'addition d’acide pharmaceutiquement adapté. Il a maintenant été découvert que les composés de formule i ont une bonne affinité pour les récepteurs associés aux amines traces (taar), notamment taar1. Les composés peuvent être utilisés pour le traitement de la dépression, des troubles anxieux, du trouble bipolaire, de l'hyperactivité avec déficit de l'attention (adhd), des troubles relatifs au stress, des troubles psychotiques tels que la schizophrénie, des maladies neurologiques telles que la maladie de parkinson, des maladies neurodégénératives telles que la maladie d'alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus d'alcool ou d'autres drogues et de troubles métaboliques tels que les troubles de l'alimentation, le diabète, les complications diabétiques, l'obésité, la dyslipidémie, les troubles de la consommation d'énergie et de l'assimilation, les troubles et le mauvais fonctionnement de l'homéostasie de la température corporelle, les troubles du sommeil et du rythme circadien, et les troubles cardiovasculaires.
MA37944A 2012-09-14 2013-09-11 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 MA37944B2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12184360 2012-09-14
PCT/EP2013/068769 WO2014041007A1 (fr) 2012-09-14 2013-09-11 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

Publications (2)

Publication Number Publication Date
MA37944A1 MA37944A1 (fr) 2016-04-29
MA37944B2 true MA37944B2 (fr) 2017-10-31

Family

ID=47044779

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37944A MA37944B2 (fr) 2012-09-14 2013-09-11 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

Country Status (35)

Country Link
US (1) US9487501B2 (fr)
EP (1) EP2895477B1 (fr)
JP (2) JP2015531782A (fr)
KR (1) KR101706486B1 (fr)
CN (2) CN107903251A (fr)
AR (1) AR092537A1 (fr)
AU (1) AU2013314388B2 (fr)
BR (1) BR112015004511B1 (fr)
CA (1) CA2882821C (fr)
CL (1) CL2015000580A1 (fr)
CR (1) CR20150087A (fr)
DK (1) DK2895477T3 (fr)
EA (1) EA026062B1 (fr)
ES (1) ES2654653T3 (fr)
HK (2) HK1252981A1 (fr)
HR (1) HRP20171981T1 (fr)
HU (1) HUE037689T2 (fr)
IL (1) IL237332B (fr)
LT (1) LT2895477T (fr)
MA (1) MA37944B2 (fr)
MX (1) MX363362B (fr)
MY (1) MY178667A (fr)
NO (1) NO2895477T3 (fr)
NZ (1) NZ705154A (fr)
PE (1) PE20150735A1 (fr)
PH (1) PH12015500489B1 (fr)
PL (1) PL2895477T3 (fr)
PT (1) PT2895477T (fr)
RS (1) RS56747B1 (fr)
SG (1) SG11201501958QA (fr)
SI (1) SI2895477T1 (fr)
TW (1) TWI610926B (fr)
UA (1) UA113776C2 (fr)
WO (1) WO2014041007A1 (fr)
ZA (1) ZA201501126B (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016016162A1 (fr) * 2014-07-30 2016-02-04 F. Hoffmann-La Roche Ag Dérivés 6-amino -5,6,7,8-tétrahydronaphtalène -2-yle ou 3-aminochroman -7-yl comme modulateurs de taar
MY195528A (en) 2016-03-17 2023-01-30 Hoffmann La Roche 5-Ethyl-4-Methyl-Pyrazole-3-Carboxamide Derivative Having Activity as Agonist of Taar
RU2019121922A (ru) * 2016-12-15 2021-01-18 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Композиции и способы лечения рака
KR20210149163A (ko) 2019-04-09 2021-12-08 에프. 호프만-라 로슈 아게 자가면역 질환의 치료를 위한 헥사하이드로-1H-피라지노[1,2-a]피라진 화합물
WO2022262855A1 (fr) * 2021-06-18 2022-12-22 上海拓界生物医药科技有限公司 Inhibiteur de malt1, son procédé de préparation et son utilisation

Family Cites Families (8)

* 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
KR101335845B1 (ko) 2007-02-15 2013-12-02 에프. 호프만-라 로슈 아게 Taar1 리간드로서의 2-아미노옥사졸린
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
WO2012063896A1 (fr) * 2010-11-11 2012-05-18 第一三共株式会社 Nouveau dérivé de pyrazole amide
US9073911B2 (en) * 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
US9029370B2 (en) * 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives

Also Published As

Publication number Publication date
ES2654653T3 (es) 2018-02-14
KR101706486B1 (ko) 2017-02-13
EA201590454A1 (ru) 2015-09-30
HUE037689T2 (hu) 2018-09-28
IL237332A0 (en) 2015-04-30
CA2882821A1 (fr) 2014-03-20
PH12015500489A1 (en) 2015-04-20
JP6529998B2 (ja) 2019-06-12
SI2895477T1 (en) 2018-02-28
EA026062B1 (ru) 2017-02-28
HK1206720A1 (en) 2016-01-15
CR20150087A (es) 2015-04-06
BR112015004511A2 (pt) 2017-07-04
CN104619700A (zh) 2015-05-13
CN107903251A (zh) 2018-04-13
AU2013314388B2 (en) 2016-07-14
BR112015004511B1 (pt) 2022-08-02
CA2882821C (fr) 2018-05-22
HK1252981A1 (zh) 2019-06-06
AU2013314388A1 (en) 2015-03-05
US9487501B2 (en) 2016-11-08
UA113776C2 (xx) 2017-03-10
PH12015500489B1 (en) 2015-04-20
ZA201501126B (en) 2016-01-27
SG11201501958QA (en) 2015-04-29
PL2895477T3 (pl) 2018-03-30
JP2017122103A (ja) 2017-07-13
LT2895477T (lt) 2018-01-25
MX363362B (es) 2019-03-21
JP2015531782A (ja) 2015-11-05
NZ705154A (en) 2018-03-23
HRP20171981T1 (hr) 2018-02-09
IL237332B (en) 2018-07-31
CL2015000580A1 (es) 2015-07-10
TWI610926B (zh) 2018-01-11
AR092537A1 (es) 2015-04-22
RS56747B1 (sr) 2018-03-30
EP2895477A1 (fr) 2015-07-22
EP2895477B1 (fr) 2017-11-01
MA37944A1 (fr) 2016-04-29
MX2015002900A (es) 2015-06-03
MY178667A (en) 2020-10-20
NO2895477T3 (fr) 2018-03-31
DK2895477T3 (en) 2018-01-15
PE20150735A1 (es) 2015-05-17
BR112015004511A8 (pt) 2021-11-03
PT2895477T (pt) 2017-12-29
TW201425308A (zh) 2014-07-01
WO2014041007A1 (fr) 2014-03-20
US20150218131A1 (en) 2015-08-06
KR20150054947A (ko) 2015-05-20

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