DK2433637T3 - Anvendelse af quinazolin derivater til neurodegenerative sygedomme - Google Patents

Anvendelse af quinazolin derivater til neurodegenerative sygedomme Download PDF

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Publication number
DK2433637T3
DK2433637T3 DK10732398.2T DK10732398T DK2433637T3 DK 2433637 T3 DK2433637 T3 DK 2433637T3 DK 10732398 T DK10732398 T DK 10732398T DK 2433637 T3 DK2433637 T3 DK 2433637T3
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Denmark
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aryl
alkyl
use according
compound
formula
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DK10732398.2T
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DK2433637T5 (da
Inventor
Castillo Ana Pérez
Gil Ana Martínez
Ayuso-Gontan Carmen Gil
Martín Concepción Pérez
García José Morales
Sancho Miriam Redondo
San Cristóbal Marina Sanz
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Consejo Superior Investigacion
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    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/28Drugs 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
    • A61P9/00Drugs for disorders of the cardiovascular system

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

Claims (14)

1. Anvendelse af en forbindelse ifølge formel (I):
hvor: A, er en splejset carbocyklus eller heterocyklus eventuelt substitueret med 5, 6 eller 7 mættede eller umættede medlemmer, — kan være en dobbeltbinding; X og Y, er uafhængigt af hinanden valgt mellem gruppen bestående af hydrogen, alkyl, =0, =S, aryl, O-alkyl, O-aryl, S-alkyl eller -S-aryl; og R, R1, R2 og R3 er uafhængigt af hinanden valgt mellem gruppen bestående af hydrogen, halogen, alkyl, haloalkyl, aryl, cycloalkyl, (CH2)n-aryl, -OR3; - C(0)0R3, (CH2)n-C(0)0R3 eller -S(0)t-, hvor n er større end eller lig med O, og hvor t er 1 eller 2, eller et farmaceutisk acceptabelt salt, prodrug, solvat eller stereoisomer deraf, hvor prodruget er en ester af carboxylsyre, en aminosyreester, en phosphatester, en sulfona-testermetalsalt, en carbamat eller et amid afledt af forbindelsen ifølge formel (I), hvilken når administreret til et individ er i stand til direkte eller indirekte at tilvejebringe forbindelsen ifølge formel (I), til fremstilling af et lægemiddel til behandling af neurodegenerative og/eller neurologiske sygdomme, kendetegnet ved, at den neurodegenerative og/eller neurologiske sygdom er valgt blandt den følgende gruppe: Alzheimers sygdom, Parkinsons sygdom, amyotrofisk lateral sklerose, hjerneiskæmi, post-encephalitisk parkinson syndrom, dystoni, Tourettes syndrom, periodiske lemme-bevægelseslidelser, restless legs syndrome, forstyrrelse af aktivitet og opmærksomhed .
2. Anvendelse ifølge krav 1, hvor A er en carbocyklus med 6 medlemmer, fortrinsvis phenyl.
3. Anvendelse ifølge krav 1, kendetegnet ved, at forbindelsen ifølge formel (I) er en forbindelse ifølge formel (II):
hvor X og Y er uafhængigt af hinanden valgt mellem O eller S; og R og R1 er uafhængigt af hinanden valgt mellem gruppen bestående af hydrogen, ha-Awa#158371 logen, alkyl, haloalkyl, aryl, cycloalkyl, (CH2)n-aryl, heteroaryl,-OR3; -C(0)0R3, (CH2)n-C(0)0R3 eller -S(0)t-, hvor R3 er valgt mellem hydrogen, alkyl, aryl eller cycloalkyl, n er større end eller lig med 0 og t er 1 eller 2;
4. Anvendelse ifølge krav 3, hvor X er O og Y er S.
5. Anvendelse ifølge krav 3, hvor X er S og Y er S.
6. Anvendelse ifølge et hvilket som helst af krav 3 to 5, hvor R er valgt mellem H eller alkyl Ci-C5, fortrinsvis methyl.
7. Anvendelse ifølge krav 1, kendetegnet ved, at forbindelsen ifølge formel (I) er en forbindelse ifølge formel (III):
hvor: X er valgt mellem O eller S og Y er valgt mellem O-aryl eller S-alkyl; og R og R1 er uafhængigt af hinanden valgt mellem gruppen bestående af hydrogen, ha logen, alkyl, haloalkyl, aryl, cycloalkyl, (CH2)n-aryl, -0R3;-C(0)0R3, (CH2)n-C(0)0R3 eller -S(0)t-, hvor R3 er valgt mellem hydrogen, alkyl, aryl eller cycloalkyl, n er større end eller lig med 0 og t er 1 eller 2
8. Anvendelse ifølge krav 7, hvor X er O.
9. Anvendelse ifølge krav 7, hvor X er S.
10. Anvendelse ifølge et hvilket som helst af kravene 7 til 9, hvor Y er S-alkyl Ci-C6, fortrinsvis S-CH3.
11. Anvendelse ifølge et hvilket som helst af de foregående krav, hvor R er valgt mellem H eller alkyl C1-C6, fortrinsvis methyl.
12. Anvendelse ifølge ethvert af de foregående krav, hvor R1 er phenyl substitueret eller ikke-substitueret.
13. Anvendelse ifølge de foregående krav, hvor R1 er phenyl substitueret med mindst én halogen valgt mellem Br eller F.
14. Anvendelse ifølge krav 1, kendetegnet ved, at forbindelsen ifølge formel (I) er en forbindelse valgt blandt den følgende gruppe: - 3-phenyl-4-oxo-2-thioxo-l,2,3,4-tetrahydroquinazolin, - 3-(2,6-difluorphenyl)-4-oxo-2-thioxo-l,2,3,4-tetrahydroquinazolin, - 3-(2-bromphenyl)-8-methyl-4-oxo-2-thioxo-l,2,3,4-tetrahydroquinazolin, - 3-(2,6-Difluorphenyl)-8-methyl-2-methylthio-4-oxo-3,4-dihydroquinazolin, - 3-(2-bromphenyl)-8-methyl-2-methylthio-4-oxo-3,4-dihydroquinazolin, - 3-Phenyl-2,4-dithioxo-l,2,3,4-tetrahydroquinazolin, og - 3-Phenyl-2-methylthio-4-thioxo-3,4-dihydroquinazolin - 3-(2,6-Difluorphenyl)-2,4-dithioxo-l,2,3,4-tetrahydroquinazolin. Awa#158371
DK10732398.2T 2009-05-20 2010-05-20 Anvendelse af quinazolin derivater til neurodegenerative sygdomme DK2433637T5 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES200930189A ES2353093B1 (es) 2009-05-20 2009-05-20 Uso de derivados de quinazolinas y sus composiciones farmacéuticas en enfermedades neurodegenerativas.
PCT/ES2010/070338 WO2010133742A1 (es) 2009-05-20 2010-05-20 Uso de derivados de quinazolinas en enfermedades neurodegenerativas

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DK2433637T3 true DK2433637T3 (da) 2014-08-18
DK2433637T5 DK2433637T5 (da) 2015-08-31

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US (1) US9192610B2 (da)
EP (1) EP2433637B9 (da)
JP (1) JP5563068B2 (da)
AU (1) AU2010251044B2 (da)
DK (1) DK2433637T5 (da)
ES (2) ES2353093B1 (da)
PL (1) PL2433637T3 (da)
PT (1) PT2433637E (da)
SI (1) SI2433637T1 (da)
WO (1) WO2010133742A1 (da)

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SI2118074T1 (sl) 2007-02-01 2014-05-30 Resverlogix Corp. Spojine za preprečevanje in zdravljenje kardiovaskularnih bolezni
CN105859639A (zh) 2009-03-18 2016-08-17 雷斯韦洛吉克斯公司 新的抗炎剂
JO3789B1 (ar) 2015-03-13 2021-01-31 Resverlogix Corp التراكيب والوسائل العلاجية المعتمدة لمعالجة الامراض المتعلقة بالمتممة
ES2544519B1 (es) 2015-05-22 2016-03-04 Consejo Superior De Investigaciones Científicas (Csic) Quinazolinas S-sustituidas y sus aplicaciones terapéuticas para el tratamiento de enfermedades mediadas por PDE7
JP6745824B2 (ja) 2015-06-26 2020-08-26 武田薬品工業株式会社 複素環化合物
JP6740354B2 (ja) * 2015-10-05 2020-08-12 ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法
WO2017069173A1 (ja) * 2015-10-20 2017-04-27 武田薬品工業株式会社 複素環化合物
CA3150878A1 (en) * 2019-09-12 2021-03-18 Jonathan Bentley Inhibitors of sarm1
WO2024038090A1 (en) 2022-08-18 2024-02-22 Mitodicure Gmbh Use of substituted benzoxazole and benzofuran compounds for the treatment and prevention of diseases associated with chronic fatigue, exhaustion and/or exertional intolerance

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JPH07107056B2 (ja) * 1987-01-30 1995-11-15 日清製粉株式会社 4(3h)−キナゾリノン誘導体、その製造方法およびそれを有効成分とする抗潰瘍剤
FR2828693B1 (fr) * 2001-08-14 2004-06-18 Exonhit Therapeutics Sa Nouvelle cible moleculaire de la neurotoxicite
WO2005051974A2 (en) * 2003-06-09 2005-06-09 The Regents Of The University Of California Novel molecules for regulating cell death
ES2308916B1 (es) * 2007-03-22 2009-10-29 Consejo Superior De Investigaciones Cientificas Compuesto inhibidor dual de las enzimas pde7 y/o pde4, composiciones farmaceuticas y sus aplicaciones.
CN104758291B (zh) 2007-03-27 2020-03-03 奥默罗斯公司 用于治疗运动障碍的pde7抑制剂的用途
WO2008130619A2 (en) * 2007-04-20 2008-10-30 Trustees Of Boston College A composition comprising an inhibitor of pde4 and/or pde7

Also Published As

Publication number Publication date
JP5563068B2 (ja) 2014-07-30
EP2433637B1 (en) 2014-06-11
US20120129877A1 (en) 2012-05-24
EP2433637B9 (en) 2015-06-10
ES2353093B1 (es) 2012-01-03
ES2498828T3 (es) 2014-09-25
SI2433637T1 (sl) 2014-09-30
PL2433637T3 (pl) 2014-12-31
EP2433637A1 (en) 2012-03-28
ES2353093A1 (es) 2011-02-25
AU2010251044B2 (en) 2014-08-28
AU2010251044A1 (en) 2012-03-01
US9192610B2 (en) 2015-11-24
PT2433637E (pt) 2014-09-09
DK2433637T5 (da) 2015-08-31
JP2012527434A (ja) 2012-11-08
WO2010133742A1 (es) 2010-11-25

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