AR093576A1 - SUBSTITUTED HETEROCICLIC DERIVATIVES - Google Patents

SUBSTITUTED HETEROCICLIC DERIVATIVES

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Publication number
AR093576A1
AR093576A1 ARP130104296A ARP130104296A AR093576A1 AR 093576 A1 AR093576 A1 AR 093576A1 AR P130104296 A ARP130104296 A AR P130104296A AR P130104296 A ARP130104296 A AR P130104296A AR 093576 A1 AR093576 A1 AR 093576A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
lower alkoxy
halogen
optionally substituted
crr
Prior art date
Application number
ARP130104296A
Other languages
Spanish (es)
Inventor
M Ceccarelli Simona
Jagasia Ravi
Jakol-Roetne Roland
Peters Jens
Uwe - Wichmann Juergen
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 AR093576A1 publication Critical patent/AR093576A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a compuestos de fórmula general (1) y (2) útiles en tratamiento de enfermedades neurodegenerativas y neuropsiquiátricas. Los compuestos pueden utilizarse para el tratamiento o profilaxis de la esquizofrenia, el trastorno de personalidad obsesiva-compulsiva, la depresión mayor, los trastornos bipolares, los trastornos de ansiedad, el envejecimiento normal, la epilepsia, la degeneración retiniana, el daño cerebral traumático, la lesión de la médula espinal, el trastorno de estrés post-traumático, el trastorno de pánico la enfermedad de Parkinson la demencia la enfermedad de Alzheimer la alteración cognitiva leve, la disfunción cognitiva inducida por quimioterapia (quimocerebro), el síndrome de Down, los trastornos del espectro autista, la pérdida de audición, el tinitus, la ataxia espinocerebelar, la esclerosis lateral amiotrófica, la esclerosis múltiple, la enfermedad de Huntington, el ictus y las alteraciones debidas a la terapia de radiación, el estrés crónico, la neuropatía óptica o la degeneración macular o el abuso de fármacos neuroactivos, tales como el alcohol, los opiáceos, la metanfetamina, la fenciclidina y la cocaína. Reivindicación 1: Compuesto de la fórmula (1) ó (2) en las que R¹ es hidrógeno, alquilo inferior, alcoxi inferior, halógeno, O(CH₂)₂-alcoxi inferior, O(CH₂)₂N(CH₃)₂ ó O(CH₂)-morfolinilo, R¹ es hidrógeno, alquilo inferior, alcoxi inferior, halógeno, O(CH₂)₂-alcoxi inferior, O(CH₂)₂N(CH₃)₂ ó O(CH₂)-morfolinilo, con la condición de que tanto R¹ como R¹ sean simultáneamente hidrógenos, aunque sólo uno de entre R¹ y R¹ es alquilo inferior, alcoxi inferior, halógeno, O(CH₂)₂-alcoxi inferior, O(CH₂)₂N(CH₃)₂ ó O(CH₂)-morfolinilo; Het es un grupo heteroarilo de 5 ó 6 elementos, en el que los heteroátomos se seleccionan de entre N, O ó S; X es -CRR-, -CRR-NR-, -C(O)-, -CH₂-S-, -CH₂-S(O)₂-, CH₂-O- ó -CH₂-CRR-; R / R son, independientemente, hidrógeno, alquilo inferior, hidroxi o fenilo, o R y R pueden formar conjuntamente con el átomo de carbono al que se encuentran unidos un anillo ciclopropilo; R² es alquilo inferior, -C(O)O-alquilo inferior, cicloalquilo C₃₋₆ sustituido opcionalmente con alquilo inferior o =O, ciclohexilo puenteado o cicloalquenilo C₃₋₆, o es un grupo heteroarilo de 5 elementos, en el que el heteroátomo se selecciona de entre N, O ó S y que se sustituye opcionalmente con uno o más alquilos inferiores, o es piridinilo, sustituido opcionalmente con halógeno o alcoxi inferior, o es fenilo, sustituido opcionalmente con uno o más R², seleccionado de entre halógeno, ciano, S(O)₂-alquilo inferior, alquilo inferior, alquilo inferior sustituido con halógeno, alcoxi inferior, alcoxi inferior sustituido con halógeno o amino, o es benzo[1,3]dioxolilo, naftilo, indolilo, benzo-isoxazolilo, 2,3-dihidro-1H-indenilo, sustituido opcionalmente con alcoxi inferior o con un grupo oxo, o es 3,4-dihidro-2H-[1,4]oxazinilo, sustituido opcionalmente con un grupo oxo, o es un grupo heterocicloalquilo de cinco o seis elementos; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a su enantiómero correspondiente y/o isómeros ópticos de los mismos.This refers to compounds of general formula (1) and (2) useful in the treatment of neurodegenerative and neuropsychiatric diseases. The compounds can be used for the treatment or prophylaxis of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain damage, spinal cord injury, post-traumatic stress disorder, panic disorder Parkinson's disease dementia Alzheimer's disease mild cognitive impairment, chemotherapy-induced cognitive dysfunction (chemobrain), Down syndrome, Autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke and alterations due to radiation therapy, chronic stress, optic neuropathy or macular degeneration or abuse of neuroactive drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine. Claim 1: Compound of the formula (1) or (2) wherein R¹ is hydrogen, lower alkyl, lower alkoxy, halogen, O (CH₂) ₂-lower alkoxy, O (CH₂) ₂N (CH₃) ₂ or O ( CH₂) -morpholinyl, R¹ is hydrogen, lower alkyl, lower alkoxy, halogen, O (CH₂) ₂-lower alkoxy, O (CH₂) ₂N (CH₃) ₂ or O (CH₂) -morpholinyl, with the condition that both R¹ as R¹ are simultaneously hydrogens, although only one of R¹ and R¹ is lower alkyl, lower alkoxy, halogen, O (CH₂) ₂-lower alkoxy, O (CH₂) ₂N (CH₃) ₂ or O (CH₂) -morpholinyl; Het is a heteroaryl group of 5 or 6 elements, in which the heteroatoms are selected from N, O or S; X is -CRR-, -CRR-NR-, -C (O) -, -CH₂-S-, -CH₂-S (O) ₂-, CH₂-O- or -CH₂-CRR-; R / R are, independently, hydrogen, lower alkyl, hydroxy or phenyl, or R and R may form together with the carbon atom to which a cyclopropyl ring is attached; R² is lower alkyl, -C (O) O-lower alkyl, C₃₋₆ cycloalkyl optionally substituted with lower alkyl or = O, bridged cyclohexyl or C₃₋₆ cycloalkenyl, or is a 5-element heteroaryl group, in which the heteroatom it is selected from N, O or S and is optionally substituted with one or more lower alkyls, or is pyridinyl, optionally substituted with halogen or lower alkoxy, or is phenyl, optionally substituted with one or more R², selected from among halogen, cyano, S (O) ₂-lower alkyl, lower alkyl, lower alkyl with halogen, lower alkoxy, lower alkoxy substituted with halogen or amino, or is benzo [1,3] dioxolyl, naphthyl, indolyl, benzo-isoxazolyl, 2 , 3-dihydro-1H-indenyl, optionally substituted with lower alkoxy or with an oxo group, or is 3,4-dihydro-2H- [1,4] oxazinyl, optionally substituted with an oxo group, or is a heterocycloalkyl group of five or six elements; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and / or optical isomers thereof.

ARP130104296A 2012-11-23 2013-11-21 SUBSTITUTED HETEROCICLIC DERIVATIVES AR093576A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12193945 2012-11-23

Publications (1)

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AR093576A1 true AR093576A1 (en) 2015-06-10

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AR (1) AR093576A1 (en)
TW (1) TW201425296A (en)
WO (1) WO2014079850A1 (en)

Families Citing this family (9)

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US10752593B2 (en) 2018-12-28 2020-08-25 Endogena Therapeutics, Inc. Compounds for use as therapeutically active substances in the treatment of retinal diseases
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
AR094929A1 (en) * 2013-02-28 2015-09-09 Bristol Myers Squibb Co DERIVATIVES OF PHENYLPIRAZOL AS POWERFUL INHIBITORS OF ROCK1 AND ROCK2
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
UY36390A (en) 2014-11-05 2016-06-01 Flexus Biosciences Inc MODULATING COMPOUNDS OF INDOLAMINE ENZYME 2,3-DIOXYGENASE (IDO), ITS SYNTHESIS METHODS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
CN107205970A (en) 2014-11-05 2017-09-26 弗莱塞斯生物科学公司 Immunomodulator
CA3031423A1 (en) * 2015-10-30 2017-05-04 Trillium Therapeutics Inc. Fluorinated amide derivatives and their uses as therapeutic agents
EP3366683A1 (en) * 2017-02-28 2018-08-29 Acousia Therapeutics GmbH Cyclic amides, acteamides and ureas useful as potassium channel openers
US10807973B2 (en) 2018-12-28 2020-10-20 Endogena Therapeutics, Inc. Compounds for use as therapeutically active substances in the treatment of retinal diseases

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US7078423B2 (en) * 2002-07-18 2006-07-18 Inotek Pharmaceuticals Corporation 5-Aryltetrazole compounds, compositions thereof, and uses therefor
JP2007519754A (en) * 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション Compound
CA2602583A1 (en) * 2005-03-24 2006-09-28 Janssen Pharmaceutica N.V. Biaryl derived amide modulators of vanilloid vr1 receptor
WO2007026920A2 (en) * 2005-09-02 2007-03-08 Astellas Pharma Inc. Amide derivatives as rock inhibitors
WO2008046072A2 (en) 2006-10-13 2008-04-17 The Board Of Regents Of The University Of Texas System Chemical inducers of neurogenesis
WO2010036316A1 (en) * 2008-09-24 2010-04-01 Yangbo Feng Urea and carbamate compounds and analogs as kinase inhibitors
JP6126528B2 (en) 2010-07-07 2017-05-10 ザ・ボード・オブ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・テキサス・システムＴｈｅ Ｂｏａｒｄ Ｏｆ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｔｅｘａｓ Ｓｙｓｔｅｍ Neurogenesis-promoting compound

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TW201425296A (en) 2014-07-01

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