AR036599A1 - Un derivado de 2-pirimidinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-pirimidinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)ona sustituidos, uso del mismo, un medicamento que lo comprende y un inhibidor de gsk3beta o gsk3beta y cdk5/p25 seleccionado entre el grupo de dicho derivado - Google Patents
Un derivado de 2-pirimidinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-pirimidinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)ona sustituidos, uso del mismo, un medicamento que lo comprende y un inhibidor de gsk3beta o gsk3beta y cdk5/p25 seleccionado entre el grupo de dicho derivadoInfo
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- AR036599A1 AR036599A1 ARP020103540A ARP020103540A AR036599A1 AR 036599 A1 AR036599 A1 AR 036599A1 AR P020103540 A ARP020103540 A AR P020103540A AR P020103540 A ARP020103540 A AR P020103540A AR 036599 A1 AR036599 A1 AR 036599A1
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- Prior art keywords
- group
- ring
- alkyl
- alkyl group
- optionally substituted
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- 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
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- 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
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Abstract
Un derivado de pirimidona representado por la fórmula (1) o una sal del mismo, o un solvato del mismo o un hidrato del mismo, donde: X representa dos átomos de hidrógeno, un átomo de azufre, un átomo de oxígeno o un grupo alquilo C1-2 y un átomo de hidrógeno; Y representa una unión, un grupo etenileno, un grupo etinileno, un átomo de oxígeno, un átomo de azufre, un grupo sulfonilo, un grupo sulfóxido, un grupo carbonilo, un átomo de nitrógeno opcionalmente sustituido por un grupo alquilo C1-6, un fenilo o un grupo bencilo; o un grupo metileno opcionalmente sustituido por uno o dos grupos seleccionados entre un grupo alquilo C1-6, un grupo bencilo, un grupo hidroxilo, un grupo alcoxi C1-4, un grupo cicloalquil-metiloxi C3-6, un grupo alquilo perhalogenado C1-2, un grupo amino, un grupo acetil-amino o un grupo fenilo; R1 representa un anillo de pirimidina opcionalmente sustituido por un grupo cicloalquilo C3-6 o un grupo alquilo C1-4, un grupo alcoxi C1-4, un grupo bencilo o un átomo de halógeno; cuando Y representa una unión, un grupo metileno opcionalmente sustituido o un grupo carbonilo, entonces R2 representa un grupo alquilo C1-6 opcionalmente sustituido por un ariloxi C6-10 o un grupo arilamino C6-10; un grupo cicloalquilo C3-6, un grupo alquiltio C1-4, un grupo alcoxi C1-4, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo feniltio, un grupo bencilo, un anillo de fenilo, un anillo de indanilo, un anillo de 5,6,7,8-tetrahidro-naftilo, un anillo de naftilo, un anillo de piridina, un anillo de pirrol, un anillo de tiofeno, un anillo de furano o un anillo de imidazol; donde el grupo bencilo o los anillos son opcionalmente sustituidos por 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un grupo metilendioxi, un átomo de halógeno, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo hidroxilo, un grupo alcoxi C1-4, un nitro, un ciano, un amino, un grupo monoalquilamino C1-5, un grupo dialquilamino C2-10, un grupo alquilcarbonil-amino C1-6, un grupo aril-carbonil-amino C6-10, un grupo alquil-sulfonilo C1-4, un grupo alquil-sulfoniloxi C1-4 o un fenilo; cuando Y representa un grupo etenileno, un grupo etinileno, un átomo de oxígeno, un átomo de azufre, un grupo sulfonilo, un grupo sulfóxido o un átomo de nitrógeno opcionalmente sustituido, entonces R2 representa un grupo alquilo C1-6 (opcionalmente sustituido por un grupo ariloxi C1-6 o un grupo arilamino C6-10), un grupo cicloalquilo C3-6, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo bencilo, un anillo de fenilo, un anillo de indanilo, un anillo de 5,6,7,8-tetrahidro-naftilo, un anillo de naftilo, un anillo de piridina, un anillo de pirrol, un anillo de tiofeno, un anillo de furano o un anillo de imidazol; donde el grupo bencilo o los anillos son opcionalmente sustituidos por 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un grupo metilendioxi, un átomo de halógeno, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo hidroxilo, un grupo alcoxi C1-4, un nitro, un ciano, un amino , un grupo monoalquilamino C1-5, un grupo dialquilamino C2-10, un grupo alquil-carbonil-amino C1-6, un grupo aril-carbonil-amino C6-10, un grupo alquil-sulfonilo C1-4, grupo alquil-sulfoniloxi C1-4 o un grupo fenilo; R3 y R4 representan cada uno, independientemente, un átomo de hidrógeno, un grupo alquilo C1-6, un grupo hidroxi, un grupo alcoxi C1-4 o un átomo de halógeno; R5 representa un átomo de hidrógeno, un grupo alquilo C1-6 o un átomo de halógeno; cuando m es igual a 0, p es igual a 1, 2 ó 3; cuando m es igual a 1, p es igual a 0, 1 ó 2; cuando m es igual a 2, p es igual a 0 o 1; y n representa entre 0 y 3. También se divulga un medicamento que comprende el derivado o una sal del mismo como ingrediente activo que es utilizado para el tratamiento preventivo y/o terapéutico de una enfermedad neurodegenerativa producida por la actividad anormal de GSK3beta ó GSK3beta y cdk5/p25, como ser, mal de Alzheimer; un inhibidor de GSK3beta ó GSK3beta y cdk5/p25 seleccionado entre el grupo del derivado de pirimidona representado por la fórmula (1) o sales del mismo, o un solvato del mismo, o un hidrato del mismo; y el uso del derivado de pirimidona.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01402431A EP1295884A1 (en) | 2001-09-21 | 2001-09-21 | 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 7-Pyrimidinyl-2,3-Dihydroimidazo[1,2-a]Pyrimidin-5(1H)one derivatives |
| EP02290488A EP1340760A1 (en) | 2002-02-28 | 2002-02-28 | Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036599A1 true AR036599A1 (es) | 2004-09-22 |
Family
ID=26077255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103540A AR036599A1 (es) | 2001-09-21 | 2002-09-20 | Un derivado de 2-pirimidinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-pirimidinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)ona sustituidos, uso del mismo, un medicamento que lo comprende y un inhibidor de gsk3beta o gsk3beta y cdk5/p25 seleccionado entre el grupo de dicho derivado |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7388005B2 (es) |
| EP (1) | EP1430056B1 (es) |
| JP (2) | JP4570361B2 (es) |
| KR (1) | KR100868840B1 (es) |
| CN (1) | CN1247586C (es) |
| AR (1) | AR036599A1 (es) |
| AT (1) | ATE307815T1 (es) |
| AU (1) | AU2002342798C1 (es) |
| BR (1) | BR0212904A (es) |
| CA (1) | CA2457952C (es) |
| CY (1) | CY1105553T1 (es) |
| DE (1) | DE60206946T2 (es) |
| DK (1) | DK1430056T3 (es) |
| EA (2) | EA009456B1 (es) |
| ES (1) | ES2250721T3 (es) |
| HU (1) | HUP0500332A3 (es) |
| IL (2) | IL160397A0 (es) |
| MX (1) | MXPA04002632A (es) |
| NO (1) | NO329566B1 (es) |
| NZ (1) | NZ531244A (es) |
| PL (1) | PL370535A1 (es) |
| SI (1) | SI1430056T1 (es) |
| WO (1) | WO2003027115A1 (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| DE602005006240T2 (de) | 2004-01-22 | 2009-06-25 | Amgen Inc., Thousand Oaks | Substituierte heterocyclische verbindungen und anwendungsverfahren |
| WO2006138192A1 (en) * | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| CA2620333A1 (en) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| AU2006304787A1 (en) | 2005-10-21 | 2007-04-26 | 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 |
| 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 |
| EP1992624A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide pyrimidone compounds |
| EP1992620A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP1992621A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP1992625A1 (en) | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone compounds |
| EP2090578A1 (en) * | 2008-01-29 | 2009-08-19 | Sanofi-Aventis | Substituted arylamide diazepinopyrimidone derivatives for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3-beta |
| EP2090579A1 (en) * | 2008-01-29 | 2009-08-19 | Sanofi-Aventis | Substituted heteroarylamide diazepinopyrimidone derivatives |
| EP2085399A1 (en) * | 2008-01-29 | 2009-08-05 | Sanofi-Aventis | substituted arylamide oxazepinopyrimidone derivatives |
| EP2085400A1 (en) * | 2008-01-29 | 2009-08-05 | Sanofi-Aventis | Substituted heteroarylamide oxazepinopyrimidone derivatives |
| EP2138485A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted N-Oxide pyrazine 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 |
| EP2138498A1 (en) * | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted tricyclic derivatives against neurodegenerative diseases |
| EP2138492A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidin-4-one derivatives |
| EP2138494A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted alkyl pyrimidin-4-one derivatives |
| EP2138495A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives |
| EP2138493A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidone derivatives |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| US8421890B2 (en) | 2010-01-15 | 2013-04-16 | Picofield Technologies, Inc. | Electronic imager using an impedance sensor grid array and method of making |
| 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 |
| JP7403351B2 (ja) | 2020-02-27 | 2023-12-22 | 三菱重工業株式会社 | 通信ポイント決定装置、通信ポイント決定方法およびプログラム、並びに点検システム |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3865836A (en) * | 1972-12-08 | 1975-02-11 | Janssen Pharmaceutica Nv | Bicyclic imidazoles |
| SU600143A1 (ru) * | 1976-12-06 | 1978-03-30 | Ордена Трудового Красного Знамени Институт Органического Синтеза Ан Латвийской Сср | Способ получени гетероциклических систем, содержащих бормзамещенный имидазол |
| JPS63216886A (ja) * | 1987-03-05 | 1988-09-09 | Sumitomo Chem Co Ltd | ピリミドピリミジン誘導体およびその製造法 |
| JP2862958B2 (ja) * | 1990-06-09 | 1999-03-03 | 三協化学株式会社 | 感熱転写記録用色素 |
| US6153618A (en) * | 1996-10-11 | 2000-11-28 | Chiron Corporation | Inhibitors of glycogen synthase 3 kinase |
| NZ335992A (en) * | 1996-12-05 | 2001-09-28 | Amgen Inc | Substituted pyrimidinone and pyridone compounds and methods of use |
| KR20010041015A (ko) * | 1998-02-17 | 2001-05-15 | 윌리엄 제이. 리플린 | 항바이러스성 피리미딘 유도체 |
| WO2001044246A1 (en) | 1999-12-17 | 2001-06-21 | Chiron Corporation | Bicyclic inhibitors of glycogen synthase kinase 3 |
| FR2804959B1 (fr) | 2000-02-15 | 2006-04-28 | Centre Nat Rech Scient | Utilisation de derives de paullones pour la fabrication de medicaments |
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