BR0212896A - Derivados de 2-piridinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4- ona e 7-piridinil-2,3dihidroimidazo[1,2-a] pirimidin-5(1h)ona substituìdos - Google Patents
Derivados de 2-piridinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4- ona e 7-piridinil-2,3dihidroimidazo[1,2-a] pirimidin-5(1h)ona substituìdosInfo
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- 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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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- 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
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Abstract
"DERIVADOS DE 2-PIRIDINIL-6,7,8,9-TETRAHIDROPIRIMIDO[1,2-a]PIRIMIDIN-4- ONA E 7-PIRIDINIL-2,3-DIHIDROIMIDAZO[1,2-a] PIRIMIDIN-5(1H)ONA SUBSTITUìDOS". A invenção refere-se a um derivado de pirimidona representado pela fórmula (I), ou um sal deste, onde X representa dois átomos de hidrogênio, um átomo de enxofre, um átomo de oxigênio ou um grupo C~ 1-2~ alquila e um átomo de hidrogênio; Y representa uma ligação, um grupo etenileno, um grupo etinileno, um átomo de oxigênio, um átomo de enxofre, um grupo sulfonila, um grupo sulfóxido, um grupo carbonila, um grupo hidroxilminometileno, um grupo dioxolano, um átomo de nitrogênio sendo opcionalmente substituído; ou um grupo metileno opcionalmente substituído; ou um grupo metileno opcionalmente substituído; R1 representa um anel de 2, 3 ou 4 piridinas opcionalmente substituído; R2 pode representar um grupo C~ 1-6~ alquila opcionalmente; um grupo C~ 3-6~ cicloalquila, um grupo C~ 1-4~ alquiltio, um grupo C~ 1-4~ alcóxi, um grupo C~ 1-2~ alquila perhalogenada, um grupo C~ 1-3~ alquila halogenada, um grupo feniltio, um grupo benzila, um anel de benzeno, um anel de indano, um anel de 5,6,7,8-tetrahidronaftaleno, um anel de naftaleno, um anel piridina, um anel de pirrol, um anel de tiofeno, um anel de furano, ou um anel de imidazol; R3 e R4 representam, cada independentemente, um átomo de hidrogênio, um grupo C~ 1-6~ alquila, um grupo de hidróxi, um grupo C~ 1-4~ alcóxi ou um átomo de halogênio; R5 representa um átomo de hidrogênio, um grupo C~ 1-6~ alquila ou um átomo de halogênio; com a condição de que quando R3 e R4 representarem, cada, um átomo de hidrogênio, então R5 não seja um átomo de hidrogênio. A invenção refere-se também a um medicamento compreendendo o referido derivado ou um sal deste como um ingrediente ativo que é usado para o tratamento preventivo e/ou terapêutico de uma doença neurodegenerativa causada por atividade anormal de GSK3<225>, ou GSK3<225> e cdk5 / p25, tal como doença de Alzheimer.
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 (1)
| Publication Number | Publication Date |
|---|---|
| BR0212896A true BR0212896A (pt) | 2004-10-13 |
Family
ID=26077256
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0212896-9A BR0212896A (pt) | 2001-09-21 | 2002-09-19 | Derivados de 2-piridinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4- ona e 7-piridinil-2,3dihidroimidazo[1,2-a] pirimidin-5(1h)ona substituìdos |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7214682B2 (pt) |
| EP (2) | EP1430057B1 (pt) |
| JP (3) | JP4570362B2 (pt) |
| KR (1) | KR100868841B1 (pt) |
| CN (2) | CN100398541C (pt) |
| AR (1) | AR036600A1 (pt) |
| AT (2) | ATE401309T1 (pt) |
| AU (1) | AU2002350487C1 (pt) |
| BR (1) | BR0212896A (pt) |
| CA (1) | CA2457965C (pt) |
| CY (1) | CY1108341T1 (pt) |
| DE (2) | DE60227718D1 (pt) |
| DK (2) | DK1430057T3 (pt) |
| EA (1) | EA006859B1 (pt) |
| ES (2) | ES2247398T3 (pt) |
| HK (1) | HK1091208A1 (pt) |
| HU (1) | HUP0500328A3 (pt) |
| IL (2) | IL160402A0 (pt) |
| MX (1) | MXPA04002629A (pt) |
| NO (1) | NO329565B1 (pt) |
| NZ (2) | NZ547205A (pt) |
| PL (1) | PL370349A1 (pt) |
| PT (1) | PT1674456E (pt) |
| SI (1) | SI1430057T1 (pt) |
| WO (1) | WO2003027116A2 (pt) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1430057T3 (da) * | 2001-09-21 | 2006-01-16 | Sanofi Aventis | Substituerede 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)onderivater |
| 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 derivatives -one 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 |
| EP2275095A3 (en) | 2005-08-26 | 2011-08-17 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2377530A3 (en) | 2005-10-21 | 2012-06-20 | Braincells, Inc. | Modulation of neurogenesis by PDE inhibition |
| EP2314289A1 (en) | 2005-10-31 | 2011-04-27 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| CA2651813A1 (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 |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| EP2448939B1 (fr) * | 2009-07-02 | 2017-03-01 | Sanofi | Derives de 2,3-dihydro-1h-imidazo {1,2-a} pyrimidin-5-one, leur preparation et leur utilisation pharmaceutique |
| RU2561130C2 (ru) * | 2009-07-02 | 2015-08-20 | Санофи | НОВЫЕ ПРОИЗВОДНЫЕ 1,2,3,4-ТЕТРАГИДРОПИРИМИДО{1,2-a}ПИРИМИДИН-6-ОНА, ИХ ПОЛУЧЕНИЕ И ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ |
| 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) |
| 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) |
| EP2655375B1 (fr) * | 2010-12-23 | 2014-12-03 | Sanofi | Derives de pyrimidinone, leur preparation et leur utilisation pharmaceutique |
| 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 |
| WO2015155738A2 (en) | 2014-04-09 | 2015-10-15 | 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4920397A (en) * | 1996-10-11 | 1998-05-11 | Chiron Corporation | Purine inhibitors of glycogen synthase kinase 3 (gsk3) |
| WO1998024780A2 (en) | 1996-12-05 | 1998-06-11 | Amgen Inc. | Substituted pyrimidinone and pyridinone compounds and their use |
| EP1087963B1 (en) | 1998-06-19 | 2004-08-25 | 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 |
| YU74601A (sh) * | 1999-03-22 | 2004-05-12 | Ortho-Mcneil Pharmaceutical Inc., U.S. | POSTUPAK ZA DOBIJANJE (S-(R*,S*)]-p-[[[1-OkSO-3-(4-PIPERIDINIL)PROPIL]-3-PIPERIDINIL]KARBONIL]AMINO]-3-PIPERIDINPROPIONSKE KISELINE I NJENIH DERIVATA |
| 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 |
| 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 |
| DK1430057T3 (da) * | 2001-09-21 | 2006-01-16 | Sanofi Aventis | Substituerede 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)onderivater |
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2002
- 2002-09-19 DK DK02785157T patent/DK1430057T3/da active
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