MX2015002900A - Derivados de pirazol carboxamida como moduladores de los receptores asociados con las aminas traza (taar) para uso en el tratamiento de varios trastornos, tales como depresion, diabetes y enfermedades de parkinson. - Google Patents

Derivados de pirazol carboxamida como moduladores de los receptores asociados con las aminas traza (taar) para uso en el tratamiento de varios trastornos, tales como depresion, diabetes y enfermedades de parkinson.

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Publication number
MX2015002900A
MX2015002900A MX2015002900A MX2015002900A MX2015002900A MX 2015002900 A MX2015002900 A MX 2015002900A MX 2015002900 A MX2015002900 A MX 2015002900A MX 2015002900 A MX2015002900 A MX 2015002900A MX 2015002900 A MX2015002900 A MX 2015002900A
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Mexico
Prior art keywords
lower alkyl
halogen
substituted
disorders
hydroxy
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MX2015002900A
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English (en)
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MX363362B (es
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Guido Galley
Roger Norcross
Philippe Pflieger
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Hoffmann La Roche
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Publication of MX2015002900A publication Critical patent/MX2015002900A/es
Publication of MX363362B publication Critical patent/MX363362B/es

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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/16Anti-Parkinson drugs
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    • 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
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
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Abstract

La presente invención se refiere a compuestos de la fórmula (I) en la que R1 es fenilo opcionalmente sustituido por halógeno, alquilo inferior, cicloalquilo inferior, alcoxi inferior, ciano, alquilo inferior sustituido por halógeno, alquilo inferior sustituido por hidroxi, alcoxi inferior sustituido por halógeno o alcoxi inferior sustituido por hidroxi; o es piridin-2-, -3- o -4-ilo opcionalmente sustituido por halógeno, alquilo inferior, cicloalquilo inferior, ciano, alquilo inferior sustituido por halógeno, alquilo inferior sustituido por hidroxi, alcoxi inferior, alcoxi inferior sustituido por halógeno o alcoxi inferior sustituido por hidroxilo; o es pirimidin-2-, -4- o -5-ilo opcionalmente sustituido por halógeno, alquilo inferior, cicloalquilo inferior, alquilo inferior sustituido por hidroxi o alquilo inferior sustituido por halógeno; o es pirazin-2-ilo opcionalmente sustituido por halógeno, alquilo inferior, cicloalquilo inferior, alquilo inferior sustituido por halógeno, alquilo inferior sustituido por hidroxi o ciano; o es 2,2-difluorbenzo[d] [1,3]dioxol-5-ilo, o es tiazolilo opcionalmente sustituido por alquilo inferior sustituido por halógeno; R2 es hidrógeno o alquilo inferior; R3 es hidrógeno, amino o alquilo inferior; Z es un enlace, - CH2- u -O-; o a una sal de adición de ácido farmacéuticamente apropiada de los mismos. Ahora se ha encontrado que los compuestos de las fórmulas I tienen una buena afinidad con los receptores asociados con las aminas traza (TAAR), en especial con el TAAR1. Los compuestos pueden utilizarse para el tratamiento de la depresión, trastornos de ansiedad, trastorno bipolar, trastorno de hiperactividad con déficit de atención (ADHD), los trastornos relacionados con el estrés, trastornos psicóticos, esquizofrenia, enfermedades neurológicas, enfermedad de Parkinson, trastornos neurodegenerativos, enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias, trastornos metabólicos, trastornos de ingestión de comida, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos y malfunción de la homeostasis de la temperatura corporal, trastornos del sueño y del ritmo circadiano y trastornos cardiovasculares.
MX2015002900A 2012-09-14 2013-09-11 Derivados de pirazol carboxamida como moduladores de los receptores asociados con las aminas traza (taar) para uso en el tratamiento de varios trastornos, tales como depresión, diabetes y enfermedades de parkinson. MX363362B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12184360 2012-09-14
PCT/EP2013/068769 WO2014041007A1 (en) 2012-09-14 2013-09-11 Pyrazole carboxamide derivatives as taar modulators for use in the treatment of several disorders, such as depression, diabetes and parkinson's disease

Publications (2)

Publication Number Publication Date
MX2015002900A true MX2015002900A (es) 2015-06-03
MX363362B MX363362B (es) 2019-03-21

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MX2015002900A MX363362B (es) 2012-09-14 2013-09-11 Derivados de pirazol carboxamida como moduladores de los receptores asociados con las aminas traza (taar) para uso en el tratamiento de varios trastornos, tales como depresión, diabetes y enfermedades de parkinson.

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US (1) US9487501B2 (es)
EP (1) EP2895477B1 (es)
JP (2) JP2015531782A (es)
KR (1) KR101706486B1 (es)
CN (2) CN107903251A (es)
AR (1) AR092537A1 (es)
AU (1) AU2013314388B2 (es)
BR (1) BR112015004511B1 (es)
CA (1) CA2882821C (es)
CL (1) CL2015000580A1 (es)
CR (1) CR20150087A (es)
DK (1) DK2895477T3 (es)
EA (1) EA026062B1 (es)
ES (1) ES2654653T3 (es)
HK (2) HK1206720A1 (es)
HR (1) HRP20171981T1 (es)
HU (1) HUE037689T2 (es)
IL (1) IL237332B (es)
LT (1) LT2895477T (es)
MA (1) MA37944B2 (es)
MX (1) MX363362B (es)
MY (1) MY178667A (es)
NO (1) NO2895477T3 (es)
NZ (1) NZ705154A (es)
PE (1) PE20150735A1 (es)
PH (1) PH12015500489B1 (es)
PL (1) PL2895477T3 (es)
PT (1) PT2895477T (es)
RS (1) RS56747B1 (es)
SG (1) SG11201501958QA (es)
SI (1) SI2895477T1 (es)
TW (1) TWI610926B (es)
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Publication number Priority date Publication date Assignee Title
CN106715395B (zh) * 2014-07-30 2020-05-12 豪夫迈·罗氏有限公司 作为taar调节剂的6-氨基-5,6,7,8-四氢萘-2-基或3-氨基色满-7-基衍生物
SG10201913878YA (en) 2016-03-17 2020-03-30 Hoffmann La Roche 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar
JP7191828B2 (ja) * 2016-12-15 2022-12-19 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア がん治療のための組成物および方法
SG11202110401WA (en) 2019-04-09 2021-10-28 Hoffmann La Roche Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease
WO2022262855A1 (zh) * 2021-06-18 2022-12-22 上海拓界生物医药科技有限公司 一种malt1抑制剂及其制备方法和用途

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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
CN101616902B (zh) 2007-02-15 2013-03-27 弗·哈夫曼-拉罗切有限公司 作为taar1配体的2-氨基*唑啉类化合物
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
TW201236685A (en) * 2010-11-11 2012-09-16 Daiichi Sankyo Co Ltd New pyrazole amide derivatives
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

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US9487501B2 (en) 2016-11-08
AU2013314388A1 (en) 2015-03-05
CN107903251A (zh) 2018-04-13
ZA201501126B (en) 2016-01-27
UA113776C2 (xx) 2017-03-10
CA2882821C (en) 2018-05-22
CA2882821A1 (en) 2014-03-20
KR101706486B1 (ko) 2017-02-13
BR112015004511B1 (pt) 2022-08-02
AU2013314388B2 (en) 2016-07-14
HRP20171981T1 (hr) 2018-02-09
CR20150087A (es) 2015-04-06
PH12015500489A1 (en) 2015-04-20
PH12015500489B1 (en) 2015-04-20
EA026062B1 (ru) 2017-02-28
HK1206720A1 (en) 2016-01-15
BR112015004511A8 (pt) 2021-11-03
US20150218131A1 (en) 2015-08-06
PT2895477T (pt) 2017-12-29
RS56747B1 (sr) 2018-03-30
CL2015000580A1 (es) 2015-07-10
TW201425308A (zh) 2014-07-01
WO2014041007A1 (en) 2014-03-20
EA201590454A1 (ru) 2015-09-30
HUE037689T2 (hu) 2018-09-28
MA37944A1 (fr) 2016-04-29
EP2895477B1 (en) 2017-11-01
IL237332B (en) 2018-07-31
TWI610926B (zh) 2018-01-11
PL2895477T3 (pl) 2018-03-30
ES2654653T3 (es) 2018-02-14
NZ705154A (en) 2018-03-23
IL237332A0 (en) 2015-04-30
DK2895477T3 (en) 2018-01-15
SI2895477T1 (en) 2018-02-28
EP2895477A1 (en) 2015-07-22
MA37944B2 (fr) 2017-10-31
JP2015531782A (ja) 2015-11-05
AR092537A1 (es) 2015-04-22
KR20150054947A (ko) 2015-05-20
MY178667A (en) 2020-10-20
NO2895477T3 (es) 2018-03-31
SG11201501958QA (en) 2015-04-29
LT2895477T (lt) 2018-01-25
CN104619700A (zh) 2015-05-13
JP2017122103A (ja) 2017-07-13
JP6529998B2 (ja) 2019-06-12
BR112015004511A2 (pt) 2017-07-04
MX363362B (es) 2019-03-21
PE20150735A1 (es) 2015-05-17
HK1252981A1 (zh) 2019-06-06

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