NO329805B1 - Pyrimidonderivat, anvendeser derav, legemiddel og GSK3beta eller GSK3beta og cdk5/p25 inhibitor - Google Patents
Pyrimidonderivat, anvendeser derav, legemiddel og GSK3beta eller GSK3beta og cdk5/p25 inhibitor Download PDFInfo
- Publication number
- NO329805B1 NO329805B1 NO20043565A NO20043565A NO329805B1 NO 329805 B1 NO329805 B1 NO 329805B1 NO 20043565 A NO20043565 A NO 20043565A NO 20043565 A NO20043565 A NO 20043565A NO 329805 B1 NO329805 B1 NO 329805B1
- Authority
- NO
- Norway
- Prior art keywords
- pyrimidin
- ylmethyl
- tetrahydropyrimido
- dimethyl
- pyridin
- Prior art date
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- 101150053721 Cdk5 gene Proteins 0.000 title claims description 34
- 239000003814 drug Substances 0.000 title claims description 29
- 229940079593 drug Drugs 0.000 title claims description 26
- 150000008318 pyrimidones Chemical class 0.000 title claims description 20
- 239000003112 inhibitor Substances 0.000 title claims description 12
- 102000019058 Glycogen Synthase Kinase 3 beta Human genes 0.000 title description 4
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims description 119
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- 150000003839 salts Chemical class 0.000 claims description 36
- 125000004432 carbon atom Chemical group C* 0.000 claims description 23
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 20
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
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- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- HXITXNWTGFUOAU-UHFFFAOYSA-N phenylboronic acid Chemical compound OB(O)C1=CC=CC=C1 HXITXNWTGFUOAU-UHFFFAOYSA-N 0.000 description 1
- 230000000865 phosphorylative effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
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- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 230000026938 proteasomal ubiquitin-dependent protein catabolic process Effects 0.000 description 1
- 230000009822 protein phosphorylation Effects 0.000 description 1
- SHNUBALDGXWUJI-UHFFFAOYSA-N pyridin-2-ylmethanol Chemical compound OCC1=CC=CC=N1 SHNUBALDGXWUJI-UHFFFAOYSA-N 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- ZFCHNZDUMIOWFV-UHFFFAOYSA-N pyrimidine-2-carboxylic acid Chemical compound OC(=O)C1=NC=CC=N1 ZFCHNZDUMIOWFV-UHFFFAOYSA-N 0.000 description 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 1
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- 238000007920 subcutaneous administration Methods 0.000 description 1
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- 239000003765 sweetening agent Substances 0.000 description 1
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- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000005424 tosyloxy group Chemical group S(=O)(=O)(C1=CC=C(C)C=C1)O* 0.000 description 1
- GGUBFICZYGKNTD-UHFFFAOYSA-N triethyl phosphonoacetate Chemical compound CCOC(=O)CP(=O)(OCC)OCC GGUBFICZYGKNTD-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000010798 ubiquitination Methods 0.000 description 1
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Classifications
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- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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- 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
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
-
- 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)
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- Engineering & Computer Science (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
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- Psychiatry (AREA)
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- Addiction (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
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- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02290486A EP1348708A1 (fr) | 2002-02-28 | 2002-02-28 | Dérivés substitués par hétéroaryle de la 2-pyrimidinyl-6,7,8,9-tétrahydropyrimido[1,2-a]pyrimidin-4-one et de la 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one |
| EP02290485A EP1340758A1 (fr) | 2002-02-28 | 2002-02-28 | Dérivés substitués par hétéroaryle de la 2-pyridinyl-6,7,8,9-tétrahydro[1,2-a]pyridin-4-one et de la 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidinone |
| PCT/EP2003/002651 WO2003072579A1 (fr) | 2002-02-28 | 2003-02-26 | Derives de 2-pyridinyl- et 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one subtituee par heteroaryle |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20043565L NO20043565L (no) | 2004-11-25 |
| NO329805B1 true NO329805B1 (no) | 2010-12-20 |
Family
ID=27767034
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20043565A NO329805B1 (no) | 2002-02-28 | 2004-08-26 | Pyrimidonderivat, anvendeser derav, legemiddel og GSK3beta eller GSK3beta og cdk5/p25 inhibitor |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7232827B2 (fr) |
| EP (1) | EP1480983B1 (fr) |
| JP (1) | JP4458851B2 (fr) |
| KR (1) | KR101030629B1 (fr) |
| CN (1) | CN1315832C (fr) |
| AR (1) | AR038619A1 (fr) |
| AT (1) | ATE309247T1 (fr) |
| AU (1) | AU2003221500B9 (fr) |
| BR (1) | BR0308109A (fr) |
| CA (1) | CA2474823C (fr) |
| DE (1) | DE60302221T2 (fr) |
| DK (1) | DK1480983T3 (fr) |
| EA (1) | EA007737B1 (fr) |
| ES (1) | ES2250883T3 (fr) |
| IL (1) | IL163287A (fr) |
| MX (1) | MXPA04008364A (fr) |
| NO (1) | NO329805B1 (fr) |
| NZ (1) | NZ534466A (fr) |
| PL (1) | PL372465A1 (fr) |
| SI (1) | SI1480983T1 (fr) |
| TW (1) | TWI303637B (fr) |
| WO (1) | WO2003072579A1 (fr) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1454910A1 (fr) | 2003-03-07 | 2004-09-08 | Sanofi-Synthelabo | Dérivés de pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidones substitues |
| AR043486A1 (es) * | 2003-03-07 | 2005-08-03 | Sanofi Aventis | Derivados de 2-(diaza-biciclo-alquil)-pirimidona |
| EP1557417B1 (fr) * | 2003-12-19 | 2007-03-07 | Sanofi-Aventis | Dérivés de 8'-pyri(mi)dinyl-dihydrospiro-[cycloaklyamine]-pyrimido[1,2-a]pyrimidin-6-one substitués |
| EP1723427A2 (fr) * | 2004-02-26 | 2006-11-22 | Bayer HealthCare AG | Diagnostic et traitement de maladies associees a la glycogene synthase kinase 3 beta (gsk3b) |
| DE102004010207A1 (de) | 2004-03-02 | 2005-09-15 | Aventis Pharma S.A. | Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate |
| DE102004010194A1 (de) * | 2004-03-02 | 2005-10-13 | Aventis Pharma Deutschland Gmbh | 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate, ihre Herstellung und Verwendung in Arzneimitteln |
| WO2007025177A2 (fr) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenese par modulation du recepteur muscarinique |
| EP2258358A3 (fr) | 2005-08-26 | 2011-09-07 | Braincells, Inc. | Neurogenèse avec un inhibiteur de l'acetylcholinestérase |
| EP2377530A3 (fr) | 2005-10-21 | 2012-06-20 | Braincells, Inc. | Modulation de neurogénèse par inhibition PDE |
| US20070112017A1 (en) | 2005-10-31 | 2007-05-17 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| EP2377531A2 (fr) | 2006-05-09 | 2011-10-19 | Braincells, Inc. | Neurogénèse par modulation de l'angiotensine |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| WO2010099217A1 (fr) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation de neurogenèse à l'aide de combinaisons de d-cyclosérine |
| CN102482286B (zh) * | 2009-07-02 | 2015-07-15 | 赛诺菲 | 新型1,2,3,4-四氢嘧啶并{1,2-a}嘧啶-6-酮衍生物、其制备以及其医药用途 |
| 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) |
| DK2448939T3 (en) * | 2009-07-02 | 2017-06-19 | Sanofi Sa | DERIVATIVES OF 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ON, PREPARATION AND PHARMACEUTICAL USE thereof |
| 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) |
| CN102715186A (zh) * | 2012-06-15 | 2012-10-10 | 王学权 | 一种增效除草组合物 |
| 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 |
| AU2015242330B2 (en) * | 2014-04-01 | 2017-08-17 | Pfizer Inc. | Chromene and 1,1 a,2,7b-tetrahydrocyclopropa[c]chromene pyridopyrazinediones as gamma-secretase modulators |
| WO2015155738A2 (fr) | 2014-04-09 | 2015-10-15 | Christopher Rudd | Utilisation d'inhibiteurs ou d'activateurs de gsk -3 qui modulent l'expression de pd -1 ou de t-bet pour moduler l'immunité due aux lymphocytes t |
| WO2018214866A1 (fr) * | 2017-05-24 | 2018-11-29 | 上海和誉生物医药科技有限公司 | Dérivé d'azaaryle, son procédé de préparation et son application pour une utilisation en pharmacie |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002514195A (ja) * | 1996-12-05 | 2002-05-14 | アムジエン・インコーポレーテツド | 置換ピリミジン化合物およびそれの使用 |
| TWI241298B (en) | 1998-09-25 | 2005-10-11 | Mitsubishi Chem Corp | Pyrimidone derivatives |
| DE60103909T2 (de) * | 2000-09-01 | 2005-09-22 | Sanofi-Aventis | 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-on- und 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5 1honderivate |
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