EA200501311A1 - ПРОИЗВОДНЫЕ ЗАМЕЩЁННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА - Google Patents
ПРОИЗВОДНЫЕ ЗАМЕЩЁННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНАInfo
- Publication number
- EA200501311A1 EA200501311A1 EA200501311A EA200501311A EA200501311A1 EA 200501311 A1 EA200501311 A1 EA 200501311A1 EA 200501311 A EA200501311 A EA 200501311A EA 200501311 A EA200501311 A EA 200501311A EA 200501311 A1 EA200501311 A1 EA 200501311A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl group
- group
- atom
- hydrogen atom
- substituted
- Prior art date
Links
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000019058 Glycogen Synthase Kinase 3 beta Human genes 0.000 abstract 1
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 150000008318 pyrimidones Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Настоящее изобретение относится к производному замещенного пиримидона, представленному формулой (I), или его соли, где X представляет собой два атома водорода, атом серы, атом кислорода или Cалкильную группу и атом водорода; Y представляет собой связь, карбонильную группу, возможно замещенную метиленовую группу; R1 представляет собой 2-, 3- или 4-пиридиновое кольцо либо 2-, 4- или 5-пиримидиновое кольцо, причем эти кольца возможно замещены; R2 представляет собой фенильную группу или нафталиновое кольцо, причем фенильная группа и нафталиновое кольцо возможно замещены; R3 представляет собой атом водорода или Cалкильную группу; R4 представляет собой Cпергалогенированную алкильную группу или Cгалогенированную алкильную группу; R5 представляет собой атом водорода, Cалкильную группу или атом галогена; n равно 0-3; и p+q равно от 0 до 3. Настоящее изобретение относится также к лекарственному средству, содержащему в качестве активного ингредиента указанное производное или его соль, которое используют для профилактического и/или терапевтического лечения нейродегенеративных заболеваний, вызванных аномальной активностью GSK3β, например, таких как болезнь Альцгеймера.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03290728A EP1460076A1 (en) | 2003-03-21 | 2003-03-21 | Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives |
| PCT/EP2004/004013 WO2004083210A1 (en) | 2003-03-21 | 2004-03-19 | SUBSTITUTED 8-PERFLUOROALKYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200501311A1 true EA200501311A1 (ru) | 2006-04-28 |
| EA009198B1 EA009198B1 (ru) | 2007-12-28 |
Family
ID=32799141
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200501311A EA009198B1 (ru) | 2003-03-21 | 2004-03-19 | ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7217715B2 (ru) |
| EP (2) | EP1460076A1 (ru) |
| JP (1) | JP4572194B2 (ru) |
| KR (1) | KR101070075B1 (ru) |
| CN (1) | CN100368412C (ru) |
| AR (1) | AR053082A1 (ru) |
| AT (1) | ATE433977T1 (ru) |
| AU (1) | AU2004222105B2 (ru) |
| BR (1) | BRPI0408605A (ru) |
| CA (1) | CA2517774C (ru) |
| CY (1) | CY1109345T1 (ru) |
| DE (1) | DE602004021572D1 (ru) |
| DK (1) | DK1608653T3 (ru) |
| EA (1) | EA009198B1 (ru) |
| ES (1) | ES2328812T3 (ru) |
| HK (1) | HK1088893A1 (ru) |
| IL (1) | IL170634A (ru) |
| MX (1) | MXPA05010112A (ru) |
| NO (1) | NO20054331L (ru) |
| NZ (1) | NZ542224A (ru) |
| PL (1) | PL1608653T3 (ru) |
| PT (1) | PT1608653E (ru) |
| SI (1) | SI1608653T1 (ru) |
| TW (1) | TWI322809B (ru) |
| WO (1) | WO2004083210A1 (ru) |
| ZA (1) | ZA200507192B (ru) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1460076A1 (en) * | 2003-03-21 | 2004-09-22 | Sanofi-Synthelabo | Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives |
| US9708735B2 (en) | 2005-06-23 | 2017-07-18 | Sumitomo Electric Industries, Ltd. | Group III nitride crystal substrate, epilayer-containing group III nitride crystal substrate, semiconductor device and method of manufacturing the same |
| US8771552B2 (en) * | 2005-06-23 | 2014-07-08 | Sumitomo Electric Industries, Ltd. | Group III nitride crystal substrate, epilayer-containing group III nitride crystal substrate, semiconductor device and method of manufacturing the same |
| JP4277826B2 (ja) | 2005-06-23 | 2009-06-10 | 住友電気工業株式会社 | 窒化物結晶、窒化物結晶基板、エピ層付窒化物結晶基板、ならびに半導体デバイスおよびその製造方法 |
| EP1928437A2 (en) | 2005-08-26 | 2008-06-11 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| JP2009512711A (ja) | 2005-10-21 | 2009-03-26 | ブレインセルス，インコーポレイティド | Ｐｄｅ阻害による神経新生の調節 |
| AU2006308889A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | GABA receptor mediated modulation of neurogenesis |
| EP1790649A1 (en) * | 2005-11-21 | 2007-05-30 | Sanofi-Aventis | Substituted bicyclic pyrimidone derivatives |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| EP2021000A2 (en) | 2006-05-09 | 2009-02-11 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| EP1939187A1 (en) * | 2006-12-20 | 2008-07-02 | Sanofi-Aventis | Substituted heteroaryl pyridopyrimidone derivatives |
| EP2138493A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidone derivatives |
| EP2138498A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted tricyclic derivatives against neurodegenerative diseases |
| EP2138485A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted N-Oxide pyrazine derivatives |
| EP2138495A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives |
| EP2138494A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted alkyl pyrimidin-4-one derivatives |
| EP2138492A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidin-4-one derivatives |
| EP2138488A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases |
| ES2487623T3 (es) | 2009-07-02 | 2014-08-22 | Sanofi | Derivados de 6,7,8,9-tetrahidro-pirimido{1,2-a}pirimidin-4-ona, su preparación y su aplicación farmacéutica |
| SI2655375T1 (sl) | 2010-12-23 | 2015-03-31 | Sanofi | Derivati pirimidinona, njihova priprava in njihova farmacevtska uporaba |
| FR2992314B1 (fr) | 2012-06-22 | 2015-10-16 | Sanofi Sa | Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique |
| FR2992316A1 (fr) | 2012-06-22 | 2013-12-27 | Sanofi Sa | Derives de pyrimidinones, leur preparation et leur application en therapeutique |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1136482A1 (en) * | 2000-03-23 | 2001-09-26 | Sanofi-Synthelabo | 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors |
| JP2001270884A (ja) * | 2000-03-23 | 2001-10-02 | Mitsubishi-Tokyo Pharmaceuticals Inc | ピリミドン誘導体 |
| EP1184383A1 (en) * | 2000-09-01 | 2002-03-06 | Sanofi-Synthelabo | 9-[Alkyl], 9-[(heteroaryl)alkyl] and 9-[(aryl)alkyl]-2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives |
| EP1315731B1 (en) * | 2000-09-01 | 2004-06-16 | Sanofi-Synthelabo | 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1h)one derivatives |
| EP1460076A1 (en) * | 2003-03-21 | 2004-09-22 | Sanofi-Synthelabo | Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives |
-
2003
- 2003-03-21 EP EP03290728A patent/EP1460076A1/en not_active Withdrawn
-
2004
- 2004-03-17 TW TW093107078A patent/TWI322809B/zh not_active IP Right Cessation
- 2004-03-19 SI SI200431223T patent/SI1608653T1/sl unknown
- 2004-03-19 AR ARP040100918A patent/AR053082A1/es unknown
- 2004-03-19 KR KR1020057017571A patent/KR101070075B1/ko not_active IP Right Cessation
- 2004-03-19 NZ NZ542224A patent/NZ542224A/en not_active IP Right Cessation
- 2004-03-19 EP EP04721905A patent/EP1608653B1/en not_active Expired - Lifetime
- 2004-03-19 EA EA200501311A patent/EA009198B1/ru not_active IP Right Cessation
- 2004-03-19 CA CA2517774A patent/CA2517774C/en not_active Expired - Fee Related
- 2004-03-19 CN CNB2004800120101A patent/CN100368412C/zh not_active Expired - Fee Related
- 2004-03-19 DE DE602004021572T patent/DE602004021572D1/de not_active Expired - Lifetime
- 2004-03-19 WO PCT/EP2004/004013 patent/WO2004083210A1/en active Application Filing
- 2004-03-19 PL PL04721905T patent/PL1608653T3/pl unknown
- 2004-03-19 JP JP2006505151A patent/JP4572194B2/ja not_active Expired - Fee Related
- 2004-03-19 PT PT04721905T patent/PT1608653E/pt unknown
- 2004-03-19 AT AT04721905T patent/ATE433977T1/de active
- 2004-03-19 BR BRPI0408605-8A patent/BRPI0408605A/pt not_active IP Right Cessation
- 2004-03-19 ES ES04721905T patent/ES2328812T3/es not_active Expired - Lifetime
- 2004-03-19 ZA ZA200507192A patent/ZA200507192B/xx unknown
- 2004-03-19 MX MXPA05010112A patent/MXPA05010112A/es active IP Right Grant
- 2004-03-19 AU AU2004222105A patent/AU2004222105B2/en not_active Ceased
- 2004-03-19 DK DK04721905T patent/DK1608653T3/da active
-
2005
- 2005-09-01 IL IL170634A patent/IL170634A/en not_active IP Right Cessation
- 2005-09-13 US US11/224,873 patent/US7217715B2/en not_active Expired - Fee Related
- 2005-09-20 NO NO20054331A patent/NO20054331L/no not_active Application Discontinuation
-
2006
- 2006-07-25 HK HK06108282A patent/HK1088893A1/xx not_active IP Right Cessation
-
2007
- 2007-04-04 US US11/696,256 patent/US7393853B2/en not_active Expired - Fee Related
-
2009
- 2009-09-02 CY CY20091100926T patent/CY1109345T1/el unknown
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