DK2433637T3 - Anvendelse af quinazolin derivater til neurodegenerative sygedomme - Google Patents
Anvendelse af quinazolin derivater til neurodegenerative sygedomme Download PDFInfo
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- 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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- HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 description 1
- 229950005741 rolipram Drugs 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- 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
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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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 |
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DK10732398.2T DK2433637T5 (da) | 2009-05-20 | 2010-05-20 | Anvendelse af quinazolin derivater til neurodegenerative sygdomme |
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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 |
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2009
- 2009-05-20 ES ES200930189A patent/ES2353093B1/es not_active Expired - Fee Related
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2010
- 2010-05-20 AU AU2010251044A patent/AU2010251044B2/en not_active Ceased
- 2010-05-20 PT PT107323982T patent/PT2433637E/pt unknown
- 2010-05-20 SI SI201030690T patent/SI2433637T1/sl unknown
- 2010-05-20 WO PCT/ES2010/070338 patent/WO2010133742A1/es active Application Filing
- 2010-05-20 PL PL10732398T patent/PL2433637T3/pl unknown
- 2010-05-20 US US13/321,046 patent/US9192610B2/en not_active Expired - Fee Related
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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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