NO20041141L - Substituerte 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-A]pyrimidin-4-on og 7-pyridinyl-2,3-dihydroimidazo[1,2-A]pyrimidin-5(1H)on-derivater - Google Patents
Substituerte 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-A]pyrimidin-4-on og 7-pyridinyl-2,3-dihydroimidazo[1,2-A]pyrimidin-5(1H)on-derivaterInfo
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- NO20041141L NO20041141L NO20041141A NO20041141A NO20041141L NO 20041141 L NO20041141 L NO 20041141L NO 20041141 A NO20041141 A NO 20041141A NO 20041141 A NO20041141 A NO 20041141A NO 20041141 L NO20041141 L NO 20041141L
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- atom
- optionally substituted
- alkyl group
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- YHPVIBUEXBEHPV-UHFFFAOYSA-N 2,6-dihydro-1h-pyrimidin-5-one Chemical class O=C1CNCN=C1 YHPVIBUEXBEHPV-UHFFFAOYSA-N 0.000 title 1
- KTZSHRGZRORXJO-UHFFFAOYSA-N 2-pyridin-2-yl-1,6,7,8-tetrahydropyrimido[1,2-a]pyrimidin-4-one Chemical class N1=C2NCCCN2C(=O)C=C1C1=CC=CC=N1 KTZSHRGZRORXJO-UHFFFAOYSA-N 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical group C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 101150053721 Cdk5 gene Proteins 0.000 abstract 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical group C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 abstract 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 abstract 1
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- SZTLZVPTFVVGML-UHFFFAOYSA-N n-ethenylidenehydroxylamine Chemical group ON=C=C SZTLZVPTFVVGML-UHFFFAOYSA-N 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 150000008318 pyrimidones Chemical class 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 125000003375 sulfoxide group Chemical group 0.000 abstract 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical group C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
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Abstract
Oppfinnelsen vedrører et pyrimidonderivat representert ved formel {I) eller et salt derav hvori X representerer to hydrogenatomer, et svovelatom, et oksygenatom eller en-alkylgruppe og et hydrogenatom; Y representerer en binding, en etenylengruppe, en etynylengruppe, et oJcsygenatom, et svovelatom, en sulfonylgruppe, en sulfoksydgruppe, en karbo-nylgruppe, en hydroksyiminoetylengruppe, en dioksolangruppe, et nitrogenatom som eventuelt er substituert; eller en metylengruppe som eventuelt er substituert; eller en metylengruppe som eventuelt er substituert; RI representerer en 2-,- eller 4-pyridinring som eventuelt er substituert;kan representere en C-g-alkylgruppe som eventuelt er substituert; en C_-cykloalkylgruppe, en C-alkyltiogruppe, en Cj__4-alkoksygruppe, en Cpérhalogenert alkylgruppe, en Chalogenert alkylgruppe, en fenyltiogruppe, en benzylgruppe, en benzenring, en indanring, en 5,6,7,8-tetrahydronaftalen-ring, en naftalenring, en pyridinring, en pyrrolring, en tio-fenring, en furanring eller en imidazolring; R3 og R4 representerer hver uavhengig et hydrogenatom, en C^.g-alkylgruppe, en hydroksygruppe, en Calkoksygruppe eller et halogenatom; R5 representerer et hydrogenatom, en Cx_ 6- alkylgruppe eller et halogenatom; med den betingelse at når R3 og R4 hver representerer et hydrogenatom da er R5 ikke et hydrogenatom. Oppfinnelsen vedrører også et legemiddel som omfatter derivatet eller et salt derav som en aktiv bestanddel som anvendes for forebyggende og/eller terapeutisk behandling av en nevrodegenerativ sykdom forårsaket av abnorm aktivitet avellerog cdk5/p25, slik somlzheimers sykdom.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01402432A EP1295885A1 (en) | 2001-09-21 | 2001-09-21 | Substituted 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 |
| EP02290489A EP1340761A1 (en) | 2002-02-28 | 2002-02-28 | Substituted 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 |
| PCT/EP2002/011128 WO2003027116A2 (en) | 2001-09-21 | 2002-09-19 | Substituted 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20041141L true NO20041141L (no) | 2004-06-21 |
| NO329565B1 NO329565B1 (no) | 2010-11-15 |
Family
ID=26077256
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20041141A NO329565B1 (no) | 2001-09-21 | 2004-03-18 | Substituerte 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-on og 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)on-derivater, anvendelser av slike derivater, og legemidler og inhibitorer omfattende slike derivater |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US7214682B2 (no) |
| EP (2) | EP1674456B1 (no) |
| JP (3) | JP4570362B2 (no) |
| KR (1) | KR100868841B1 (no) |
| CN (2) | CN1247585C (no) |
| AR (1) | AR036600A1 (no) |
| AT (2) | ATE401309T1 (no) |
| AU (1) | AU2002350487C1 (no) |
| BR (1) | BR0212896A (no) |
| CA (1) | CA2457965C (no) |
| CY (1) | CY1108341T1 (no) |
| DE (2) | DE60227718D1 (no) |
| DK (2) | DK1430057T3 (no) |
| EA (1) | EA006859B1 (no) |
| ES (2) | ES2310787T3 (no) |
| HU (1) | HUP0500328A3 (no) |
| IL (2) | IL160402A0 (no) |
| MX (1) | MXPA04002629A (no) |
| NO (1) | NO329565B1 (no) |
| NZ (2) | NZ547205A (no) |
| PL (1) | PL370349A1 (no) |
| PT (1) | PT1674456E (no) |
| SI (1) | SI1430057T1 (no) |
| WO (1) | WO2003027116A2 (no) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ547205A (en) * | 2001-09-21 | 2007-11-30 | Sanofi Aventis | Intermediates of substituted 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 |
| TWI335221B (en) | 2001-09-27 | 2011-01-01 | Alcon Inc | Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma |
| EP1454909B1 (en) * | 2003-03-07 | 2008-08-20 | Sanofi Aventis | 8'-pyridinyl-dihydrospiro- (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one derivatives and their use against neurodegenerative diseases |
| EP1454900A1 (en) | 2003-03-07 | 2004-09-08 | Sanofi-Synthelabo | Process for the preparation of pyridinyl and pyrimidinyl mono-fluorinated beta keto-esters |
| EP1557417B1 (en) * | 2003-12-19 | 2007-03-07 | Sanofi-Aventis | Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives |
| US7504403B2 (en) | 2004-01-22 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| JP2009506069A (ja) | 2005-08-26 | 2009-02-12 | ブレインセルス，インコーポレイティド | ムスカリン性受容体調節による神経発生 |
| US7985756B2 (en) | 2005-10-21 | 2011-07-26 | Braincells Inc. | Modulation of neurogenesis by PDE inhibition |
| WO2007053596A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| WO2007134136A2 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| CN101735211B (zh) * | 2008-11-04 | 2012-11-14 | 复旦大学 | 2,3-二氢[1,5]苯并噻氮杂*类化合物或其盐在制备GSK-3β抑制剂中的用途 |
| WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| MX2012000103A (es) * | 2009-07-02 | 2012-05-22 | Sanofi Sa | Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica. |
| FR2947550B1 (fr) * | 2009-07-02 | 2012-05-18 | Sanofi Aventis | Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb) |
| ES2627428T3 (es) * | 2009-07-02 | 2017-07-28 | Sanofi | Nuevos derivados de 2,3-dihidro-1H-imidazo{1,2-a}pirimidin-5-ona, su preparación y su utilización farmacéutica |
| FR2947551B1 (fr) * | 2009-07-02 | 2012-05-18 | Sanofi Aventis | Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a)pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb) |
| US8815853B2 (en) | 2010-12-23 | 2014-08-26 | Sanofi | Pyrimidinone derivatives, preparation thereof and pharmaceutical use thereof |
| 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 |
| US20170165230A1 (en) | 2014-04-09 | 2017-06-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
| CN109836427B (zh) * | 2017-11-29 | 2022-04-15 | 暨南大学 | 嘧啶并嘧啶酮类化合物及其应用 |
| CN114957246B (zh) * | 2021-02-19 | 2025-11-11 | 苏州恩华生物医药科技有限公司 | 5,6,7,8-四氢吡啶并[4,3-d]嘧啶-4（3H）-酮衍生物及其应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998016528A1 (en) * | 1996-10-11 | 1998-04-23 | Chiron Corporation | Purine inhibitors of glycogen synthase kinase 3 (gsk3) |
| HUP0001140A3 (en) * | 1996-12-05 | 2002-05-28 | Amgen Inc Thousand Oaks | Substituted pyrimidinone and pyridone compounds and methods of use |
| US6417185B1 (en) * | 1998-06-19 | 2002-07-09 | Chiron Corporation | Inhibitors of glycogen synthase kinase 3 |
| TWI241298B (en) * | 1998-09-25 | 2005-10-11 | Mitsubishi Chem Corp | Pyrimidone derivatives |
| JP2000264888A (ja) * | 1999-01-11 | 2000-09-26 | Sagami Chem Res Center | 双環性ピリミジン誘導体、それらの製造中間体及びそれらの製造方法、並びにそれらを有効成分とする除草剤 |
| MXPA01009615A (es) * | 1999-03-22 | 2003-07-21 | Johnson & Johnson | Procedimiento para la preparacion de acido [s -(r*s*)] -°-[[[1[1- oxo-3 -(4-piperidinil) propil]3 -piperidini] carbonil] amino] -3-piridinil] carbonil] amino] -3-piridinpropanoico, y derivados del mismo. |
| WO2001042224A1 (en) * | 1999-12-09 | 2001-06-14 | Mitsubishi Pharma Corporation | Carboxyamido derivatives |
| CN100335479C (zh) * | 1999-12-17 | 2007-09-05 | 希龙公司 | 糖元合成酶激酶3的双环抑制剂 |
| AU1224902A (en) * | 2000-09-01 | 2002-03-13 | 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 |
| NZ547205A (en) * | 2001-09-21 | 2007-11-30 | Sanofi Aventis | Intermediates of substituted 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 |
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