AR093519A1 - 1,6-naftiridinas sustituidas - Google Patents

1,6-naftiridinas sustituidas

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Publication number
AR093519A1
AR093519A1 ARP130104234A ARP130104234A AR093519A1 AR 093519 A1 AR093519 A1 AR 093519A1 AR P130104234 A ARP130104234 A AR P130104234A AR P130104234 A ARP130104234 A AR P130104234A AR 093519 A1 AR093519 A1 AR 093519A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
optionally substituted
substituted
halogen
alkoxy
Prior art date
Application number
ARP130104234A
Other languages
English (en)
Inventor
M Ceccarelli Simona
Jagasia Ravi
E Martin Rainer
Peters Jens
Uwe - Wichmann Juergen
Jakob-Roetne Roland
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 AR093519A1 publication Critical patent/AR093519A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic 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
    • A61P25/18Antipsychotics, 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
    • A61P25/22Anxiolytics
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente se refiere al uso de compuestos de la fórmula general (1) en la que: R es hidrógeno o alquilo inferior; R¹ es halógeno, alquilo inferior, cicloalquilo o ciano; o es fenilo, opcionalmente sustituido de una a tres veces por sustituyentes elegidos entre alquilo inferior, alquilo inferior sustituido por halógeno, alcoxi inferior, alcoxi inferior sustituido por halógeno, halógeno, ciano, hidroxi, C(O)-NH-alquilo inferior, CH₂-C(O)-NH-alquilo inferior, CH₂-NH-C(O)-alquilo inferior, CH₂NH₂, S(O)₂CH₃, S(O)₂N(CH₃)₂, o por grupos heterocicloalquilo; o es pirazol-1-, -4- ó -5-ilo, opcionalmente sustituido por alquilo inferior; o es tiazol-5-ilo, opcionalmente sustituido por uno o dos grupos alquilo inferior; o es piridin-2-, -3- ó -4-ilo, opcionalmente sustituido por alquilo inferior, alcoxi inferior, halógeno o N(CH₃)₂; o es 3,6-dihidro-2H-pirano; o es benzo[d][1,3]dioxol-5-ilo; o es 2,3-dihidrobenzo[b][1,4]dioxin-6-ilo; R² es hidrógeno, alquilo inferior o alquilo inferior sustituido por alcoxi; R³ es hidrógeno, alquilo inferior, alquilo inferior Sustituido por halógeno, alquilo inferior sustituido por hidroxi, NH-S(O)₂CH₃, -(CH₂)ₘ-O-alquilo inferior o -(CH₂)ₙ-S(O)₂-CH₃; o es -(CR²)ₙ-fenilo, opcionalmente sustituido por -S(O)₂CH₃ o alcoxi inferior; o es -(CH₂)ₙ-heterocicloalquilo opcionalmente sustituido por alquilo inferior y =O; o es -(CH₂)ₙ-heteroarilo opcionalmente sustituido por uno o dos grupos alquilo inferior; o es -(CH₂)ₙ-cicloalquilo opcionalmente sustituido por ciano; o R² y R³ junto con el átomo de N, al que están unidos, forman un anillo heterocíclico elegido entre morfolina, piperidina, 1,1-dioxo-tiomorfolina y piperazina, que puede estar sustituido por alquilo inferior o C(O)O-alquilo inferior, o pueden formar un anillo pirrolidina, opcionalmente sustituido por hidroxi; R es con independencia hidrógeno o alquilo inferior; n es el número 0, 1, 2, 3; m es el número 2; o una sal de adición de ácido farmacéuticamente aceptable, una mezcla racémica o sus enantiómeros correspondientes y/o isómeros ópticos de los mismos, para el tratamiento de la esquizofrenia, el trastorno de personalidad obsesivo-compulsivo, la depresión, los trastornos bipolares, los trastornos de ansiedad, el envejecimiento normal, la epilepsia la degeneración retinal, la lesión cerebral traumática, 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 el desequilibrio cognitivo moderado, la disfunción cognitiva inducida por la quimioterapia (quimiocerebro), el síndrome de Down, los trastornos del espectro autista, la pérdida de audición, el tintineo (tinnitus, acufenos) la ataxia espinocerebelar, la esclerosis lateral amiotrófica la esclerosis múltiple, la enfermedad de Huntington, la apoplejía, los trastornos debidos a la terapia de radiación el estrés crónico, la neuropatía óptica o degeneración macular, o el abuso de drogas neuroactivas elegidas entre alcohol, opiáceos, metanfetamina, fenciclidina y cocaína.
ARP130104234A 2012-11-20 2013-11-18 1,6-naftiridinas sustituidas AR093519A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12193311 2012-11-20

Publications (1)

Publication Number Publication Date
AR093519A1 true AR093519A1 (es) 2015-06-10

Family

ID=47189816

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130104234A AR093519A1 (es) 2012-11-20 2013-11-18 1,6-naftiridinas sustituidas

Country Status (13)

Country Link
US (1) US9657014B2 (es)
EP (1) EP2922540A1 (es)
JP (1) JP2016505534A (es)
KR (1) KR20150085538A (es)
CN (1) CN104812387A (es)
AR (1) AR093519A1 (es)
BR (1) BR112015011094A2 (es)
CA (1) CA2890685A1 (es)
HK (1) HK1207317A1 (es)
MX (1) MX2015006364A (es)
RU (1) RU2015120217A (es)
TW (1) TW201425312A (es)
WO (1) WO2014079787A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI529171B (zh) * 2013-07-29 2016-04-11 赫孚孟拉羅股份公司 1,7-萘啶衍生物
EP3169678A1 (en) * 2014-07-17 2017-05-24 Merck Patent GmbH Novel naphthryidines and isoquinolines and their use as cdk8/19 inhibitors
KR20170117479A (ko) * 2015-02-11 2017-10-23 바실리어 파마슈티카 인터내셔널 리미티드 치환된 모노- 및 폴리아자나프탈렌 유도체 및 이의 용도
CN108516958B (zh) 2015-03-24 2020-07-17 上海璎黎药业有限公司 稠环衍生物、其制备方法、中间体、药物组合物及应用
PE20181010A1 (es) * 2015-11-06 2018-06-26 Neurocrine Biosciences Inc Derivados de n-[2-(1-benzilpiperidin-4-il)etil]-4-(pirazin-2-il)-piperazina-1-carboxamida y compuestos relacionados como antagonistas del receptor muscarinico 4 (m4) para tratar trastornos neurologicos
EA039638B1 (ru) * 2016-01-06 2022-02-21 Нейрокрин Байосайенсиз, Инк. Антагонисты мускаринового рецептора 4 и способы их применения
EP3591040A4 (en) 2017-03-03 2020-11-11 Kyoto University METHOD FOR PRODUCING PANCREATIC ANALYZER CELLS

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GB9605437D0 (en) 1996-03-15 1996-05-15 Iaf Biochem Int Cytomegalovirus inhibiting compounds
JP2001525365A (ja) * 1997-12-11 2001-12-11 バイオケム・フアーマ・インコーポレーテツド 抗ウイルス化合物
WO2002051413A2 (en) 2000-12-27 2002-07-04 Shire Biochem Inc. Macrocyclic anti-viral compounds
MX2007001267A (es) * 2004-08-03 2007-07-11 Serenex Inc Derivados de naftiridinas 2,8-disustituidas.
FR2904317A1 (fr) 2006-07-27 2008-02-01 Inst Nat Sante Rech Med Analogues d'halogenobenzamides marques a titre de radiopharmaceutiques
US20080242694A1 (en) 2006-09-18 2008-10-02 D Sidocky Neil R Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
WO2008046072A2 (en) 2006-10-13 2008-04-17 The Board Of Regents Of The University Of Texas System Chemical inducers of neurogenesis
NZ593996A (en) * 2009-01-19 2012-10-26 Daiichi Sankyo Co Ltd Naphthyridine-carboxamide and isoquinoline-carboxamide derivatives for treating osteoporosis
WO2010101949A1 (en) * 2009-03-02 2010-09-10 Sirtris Pharmaceuticals, Inc. 8-substituted quinolines and related analogs as sirtuin modulators
KR20120006016A (ko) 2009-04-06 2012-01-17 다이이찌 산쿄 가부시키가이샤 치환 페닐기를 갖는 고리형 화합물
JP6126528B2 (ja) 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 神経新生促進化合物
JP2012036168A (ja) 2010-07-15 2012-02-23 Daiichi Sankyo Co Ltd ヘテロ原子を有する環状化合物を含有する医薬組成物

Also Published As

Publication number Publication date
BR112015011094A2 (pt) 2017-07-11
CN104812387A (zh) 2015-07-29
TW201425312A (zh) 2014-07-01
US9657014B2 (en) 2017-05-23
WO2014079787A1 (en) 2014-05-30
MX2015006364A (es) 2015-10-05
US20150252044A1 (en) 2015-09-10
KR20150085538A (ko) 2015-07-23
JP2016505534A (ja) 2016-02-25
HK1207317A1 (en) 2016-01-29
EP2922540A1 (en) 2015-09-30
RU2015120217A (ru) 2017-01-10
CA2890685A1 (en) 2014-05-30

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