PE20010854A1 - USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS - Google Patents
USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORSInfo
- Publication number
- PE20010854A1 PE20010854A1 PE2000001131A PE0011312000A PE20010854A1 PE 20010854 A1 PE20010854 A1 PE 20010854A1 PE 2000001131 A PE2000001131 A PE 2000001131A PE 0011312000 A PE0011312000 A PE 0011312000A PE 20010854 A1 PE20010854 A1 PE 20010854A1
- Authority
- PE
- Peru
- Prior art keywords
- derivatives
- antagonists
- substituted pyrimidine
- carbocyclic
- alkyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 108010014719 metabotropic glutamate receptor type 1 Proteins 0.000 title abstract 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 title 1
- 102100036834 Metabotropic glutamate receptor 1 Human genes 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 229930195712 glutamate Natural products 0.000 title 1
- -1 4-SUBSTITUTED PYRIMIDINE Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Psychiatry (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE AL USO DE DERIVADOS DE PIRIMIDINA 4-SUSTITUIDAS DE FORMULA I, DONDE X1 ES O, NH; L ES UN ENLACE, ALQUILENO C1-C6 OPCIONALMENTE SUSTITUIDO CON F, OH, ALCOXI C1-C4, OXO; R1 ES CARBOCICLICO, HETEROCICLICO; R2 ES H, HALOGENO, CARBOXILO, CIANO, SCH2N, X2-R5; X2 ES UN ENLACE, O, S, SO, SO2, NH; R5 ES ALQUILO C1-C8, CICLOALQUILO C3-C10, HALOALQUILO C1-C6, HIDROXIALQUILO C1-C6, ENTRE OTROS; R3 Y R4 SON ALQUILO C1-C4 O JUNTO A C FORMAN UN ANILLO CARBOCICLICO, HETEROCICLICO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION, A COMPUESTOS INTERMEDIOS. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE GLUTAMATO mGluR1 Y PUEDE SER UTIL PARA EL TRATAMIENTO DE DOLOR, MIGRANAREFERS TO THE USE OF 4-SUBSTITUTED PYRIMIDINE DERIVATIVES OF FORMULA I, WHERE X1 IS O, NH; L IS A BOND, C1-C6 ALKYLENE OPTIONALLY SUBSTITUTED WITH F, OH, C1-C4 ALCOXY, OXO; R1 IS CARBOCYCLIC, HETEROCYCLIC; R2 IS H, HALOGEN, CARBOXYL, CYANE, SCH2N, X2-R5; X2 IS A LINK, O, S, SO, SO2, NH; R5 IS C1-C8 ALKYL, C3-C10 CYCLOALKYL, C1-C6 HALOALKYL, C1-C6 HYDROXYALKYL, AMONG OTHERS; R3 AND R4 ARE C1-C4 ALKYL OR TOGETHER WITH C, THEY FORM A CARBOCYCLIC, HETEROCICLIC RING. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION, TO INTERMEDIATE COMPOUNDS. COMPOUND I IS AN ANTAGONIST OF THE GLUTAMATE RECEPTOR mGluR1 AND MAY BE USEFUL FOR THE TREATMENT OF PAIN, MIGRAN
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16290099P | 1999-11-01 | 1999-11-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20010854A1 true PE20010854A1 (en) | 2001-08-28 |
Family
ID=22587589
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2000001131A PE20010854A1 (en) | 1999-11-01 | 2000-10-20 | USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1230225A2 (en) |
| AR (1) | AR026275A1 (en) |
| AU (1) | AU1071301A (en) |
| CO (1) | CO5261605A1 (en) |
| PE (1) | PE20010854A1 (en) |
| SV (1) | SV2002000205A (en) |
| WO (1) | WO2001032632A2 (en) |
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| KR20200036063A (en) | 2014-01-21 | 2020-04-06 | 얀센 파마슈티카 엔.브이. | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
| EP3134405B1 (en) | 2014-04-25 | 2019-08-28 | Pfizer Inc | Heteroaromatic compounds and their use as dopamine d1 ligands |
| CN108290855A (en) | 2015-07-01 | 2018-07-17 | 西北大学 | Substituted quinazoline compound and its purposes for adjusting glucocerebrosidase activity |
| DK3325490T3 (en) | 2015-07-23 | 2020-02-03 | Takeda Pharmaceuticals Co | 1-SUBSTITUTED 1,2,3,4-TETRAHYDRO-1,7-NAPHTHYRIDINE-8-AMINE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR ANTAGONISTS |
| KR20180067584A (en) | 2015-10-09 | 2018-06-20 | 아세아 테라퓨틱스 인코포레이티드 | PHARMACEUTICALS, PHYSICAL FORM AND COMPOSITIONS OF PYRROLOPYRIMIDINE KINASE INHIBITORS AND METHODS FOR THEIR PREPARATION |
| GB201700814D0 (en) * | 2017-01-17 | 2017-03-01 | Liverpool School Tropical Medicine | Compounds |
| JP2020516682A (en) | 2017-04-07 | 2020-06-11 | エイシア セラピューティクス, インコーポレイテッド | Pharmaceutical salts, physical forms and compositions of pyrrolopyrimidine kinase, and methods of making the same |
| CN115605457B (en) * | 2021-04-26 | 2025-03-18 | 三菱瓦斯化学株式会社 | Compound and method for producing the same |
| WO2025188952A1 (en) * | 2024-03-06 | 2025-09-12 | Ovid Therapeutics Inc. | Fused amino pyrimidine compounds for treatment of synucleinopathies and tdp-43 proteinopathies |
| WO2025188973A1 (en) * | 2024-03-06 | 2025-09-12 | Ovid Therapeutics Inc. | Fused amino pyrimidine compounds for treatment of 22q11.2 deletion/duplication syndromes |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1582407A (en) * | 1977-06-07 | 1981-01-07 | Worcester Controls Uk Ltd | Annular seals |
| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
| PT100905A (en) * | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | BICYCLE HYGIENEOUS HETEROCYCLIC COMPOUNDS CONTAINING BENZENE, CYCLOHEXAN OR PYRIDINE AND PYRIMIDINE, PYRIDINE OR IMIDAZOLE SUBSTITUTES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| AU661533B2 (en) * | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| GB9613021D0 (en) * | 1996-06-21 | 1996-08-28 | Pharmacia Spa | Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors |
| GB9823845D0 (en) * | 1998-11-02 | 1998-12-23 | Lilly Co Eli | Pharmaceutical compounds |
| DE19904710A1 (en) * | 1999-02-05 | 2000-08-10 | Aventis Pharma Gmbh | Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical compositions containing them |
| SE9903290D0 (en) * | 1999-09-15 | 1999-09-15 | Astra Pharma Prod | Novel compounds |
-
2000
- 2000-10-19 WO PCT/US2000/026261 patent/WO2001032632A2/en not_active Ceased
- 2000-10-19 EP EP00971987A patent/EP1230225A2/en not_active Withdrawn
- 2000-10-19 SV SV2000000205A patent/SV2002000205A/en unknown
- 2000-10-19 AU AU10713/01A patent/AU1071301A/en not_active Abandoned
- 2000-10-20 PE PE2000001131A patent/PE20010854A1/en not_active Application Discontinuation
- 2000-10-27 CO CO00082018A patent/CO5261605A1/en unknown
- 2000-10-27 AR ARP000105680A patent/AR026275A1/en unknown
Also Published As
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|---|---|
| CO5261605A1 (en) | 2003-03-31 |
| WO2001032632A2 (en) | 2001-05-10 |
| AU1071301A (en) | 2001-05-14 |
| SV2002000205A (en) | 2002-06-07 |
| EP1230225A2 (en) | 2002-08-14 |
| WO2001032632A3 (en) | 2001-11-08 |
| AR026275A1 (en) | 2003-02-05 |
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