ES2164323T3 - Derivados de 5h,10h-imidazol(1,2-a)indeno(1,2-e)pirizina-4-ona antagonistas de los receptores ampa y nmda, su preparacion, sus productos intermedios y los medicamentos que los contienen. - Google Patents
Derivados de 5h,10h-imidazol(1,2-a)indeno(1,2-e)pirizina-4-ona antagonistas de los receptores ampa y nmda, su preparacion, sus productos intermedios y los medicamentos que los contienen.Info
- Publication number
- ES2164323T3 ES2164323T3 ES97900236T ES97900236T ES2164323T3 ES 2164323 T3 ES2164323 T3 ES 2164323T3 ES 97900236 T ES97900236 T ES 97900236T ES 97900236 T ES97900236 T ES 97900236T ES 2164323 T3 ES2164323 T3 ES 2164323T3
- Authority
- ES
- Spain
- Prior art keywords
- alq
- cooh
- radical
- antagonists
- ampa
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 title abstract 4
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 title abstract 4
- 239000005557 antagonist Substances 0.000 title abstract 3
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- 102000003678 AMPA Receptors Human genes 0.000 title 1
- 108090000078 AMPA Receptors Proteins 0.000 title 1
- 239000013067 intermediate product Substances 0.000 title 1
- 150000003254 radicals Chemical group 0.000 abstract 5
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- YZCKVEUIGOORGS-UHFFFAOYSA-N Hydrogen atom Chemical group [H] YZCKVEUIGOORGS-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000036963 noncompetitive effect Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nutrition Science (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I), EN LA CUAL: R REPRESENTA UN ATOMO DE HIDROGENO O UN RADICAL - COOH, ALQ - COOH, - PO 3 H 2 , - CH 2 PO 3 H 2 , CH - CH - COOH O FENILO SUSTITUIDO POR UN RADICAL CARBOXI; Y R1 REPRESENTA UN RADICAL - ALQ - CN, - ALQ - COOH, ALK HE T, - ALQ - PO 3 H 2 O - ALQ - CO - NH SO 2 R 2 , DONDE R 2 REPRESENTA UN RADICAL ALQUILO O FENILO, ALQ REPRESENTA UN RADICAL ALQUILO Y HET REPRESENTA UN HETEROCICLO MONO O POLICICLICO SATURADO O INSATURADO CON DE 1 A 9 ATOMOS DE CARBONO Y UNO O VARIOS HETEROATOMOS ELEGIDO ENTRE O, S, N, PUDIENDO ESTAR EL HETEROCICLO SUSTITUIDO POR UNO O VARIOS RADICALES ALQUILO, FENILO O FENILALQUILO, Y TENIENDO EN CUENTA QUE, CUANDO R REPRESENTE UN ATOMO DE HIDROGENO O UN RADICAL COOH O - PO 3 H 2 , R 1 NO PUEDE REPRESENTAR - ALQ COOH. LA INVENCION SE REFIERE ASIMISMO A SUS ISOMEROS, RACEMICOS, ENANTIOMEROS Y DIASTEREOISOMEROS, SUS SALES, SU PREPARACION, LOS INTERMEDIARIOS Y LOS MEDICAMENTOS QUE LOS CONTIENEN. LOS COMPUESTOS DEFORMULA (I) PRESENTAN PROPIEDADES FARMACOLOGICAS INTERESANTES. SON ANTAGONISTAS DEL RECEPTOR DEL ACIDO AL - AMINO - 3 - HIDROXI - 5 - METIL - 4 ISOXAZOLPROPIONICO (AMPA), CONOCIDO TAMBIEN COMO RECEPTOR DEL QUISCUALATO. POR OTRA PARTE, SON ANTAGONISTAS NO COMPETITIVOS DEL RECEPTOR N - METIL - D - ASPARTATO (NMDA) Y, MAS CONCRETAMENTE, LIGANDOS PARA LOS SITIOS MODULADORES DE LA GLICINA DEL RECEPTOR NMDA.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9600192A FR2743366B1 (fr) | 1996-01-10 | 1996-01-10 | Derives de 5h,10h-imidazo(1,2-a)indeno(1,2-e)pyrazine-4-one, leur preparation, leurs intermediaires et les medicaments les contenant |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2164323T3 true ES2164323T3 (es) | 2002-02-16 |
Family
ID=9487995
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES97900236T Expired - Lifetime ES2164323T3 (es) | 1996-01-10 | 1997-01-06 | Derivados de 5h,10h-imidazol(1,2-a)indeno(1,2-e)pirizina-4-ona antagonistas de los receptores ampa y nmda, su preparacion, sus productos intermedios y los medicamentos que los contienen. |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US5990108A (es) |
| EP (1) | EP0880522B1 (es) |
| JP (1) | JP2000505073A (es) |
| KR (1) | KR19990077135A (es) |
| AR (1) | AR005424A1 (es) |
| AT (1) | ATE205847T1 (es) |
| AU (1) | AU1383097A (es) |
| BG (1) | BG102618A (es) |
| CA (1) | CA2239254A1 (es) |
| CZ (1) | CZ216698A3 (es) |
| DE (1) | DE69706830T2 (es) |
| DK (1) | DK0880522T3 (es) |
| ES (1) | ES2164323T3 (es) |
| FR (1) | FR2743366B1 (es) |
| MX (1) | MX9805167A (es) |
| PL (1) | PL327942A1 (es) |
| PT (1) | PT880522E (es) |
| SK (1) | SK93498A3 (es) |
| WO (1) | WO1997025328A1 (es) |
| ZA (1) | ZA9786B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6242493B1 (en) | 1998-03-13 | 2001-06-05 | Merck Frosst Canada & Co. | Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment |
| WO1999047497A2 (en) * | 1998-03-13 | 1999-09-23 | Merck Frosst Canada & Co. | Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment |
| DE60226756D1 (de) * | 2001-10-04 | 2008-07-03 | Merck & Co Inc | Heteroarylsubstituierte tetrazolmodulatoren des metabotropischen glutamatrezeptors-5 |
| JPWO2003070722A1 (ja) * | 2002-02-21 | 2005-06-09 | アルフレッサファーマ株式会社 | イミダゾール誘導体の改良製法およびその新規中間体 |
| GB0415320D0 (en) * | 2004-07-08 | 2004-08-11 | Astrazeneca Ab | Novel compounds |
| US7649098B2 (en) * | 2006-02-24 | 2010-01-19 | Lexicon Pharmaceuticals, Inc. | Imidazole-based compounds, compositions comprising them and methods of their use |
| TW200920355A (en) * | 2007-09-06 | 2009-05-16 | Lexicon Pharmaceuticals Inc | Compositions and methods for treating immunological and inflammatory diseases and disorders |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| AU2018284335A1 (en) | 2017-06-12 | 2020-01-30 | Glytech Llc. | Treatment of depression with NMDA antagonists and D2/5HT2A or selective 5HT2A antagonists |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2717812B1 (fr) * | 1994-03-28 | 1996-05-10 | Rhone Poulenc Rorer Sa | Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant. |
| FR2732681B1 (fr) * | 1995-04-05 | 1997-07-04 | Rhone Poulenc Rorer Sa | Derives de 10h-imidazo(1,2-a)indeno(1,2-e)pyrazin-4-one, leur preparation et les medicaments les contenant |
-
1996
- 1996-01-10 FR FR9600192A patent/FR2743366B1/fr not_active Expired - Fee Related
-
1997
- 1997-01-06 JP JP9524911A patent/JP2000505073A/ja not_active Ceased
- 1997-01-06 ES ES97900236T patent/ES2164323T3/es not_active Expired - Lifetime
- 1997-01-06 ZA ZA9786A patent/ZA9786B/xx unknown
- 1997-01-06 SK SK934-98A patent/SK93498A3/sk unknown
- 1997-01-06 PT PT97900236T patent/PT880522E/pt unknown
- 1997-01-06 KR KR1019980705272A patent/KR19990077135A/ko not_active Application Discontinuation
- 1997-01-06 US US09/101,428 patent/US5990108A/en not_active Expired - Fee Related
- 1997-01-06 CZ CZ982166A patent/CZ216698A3/cs unknown
- 1997-01-06 WO PCT/FR1997/000019 patent/WO1997025328A1/fr not_active Application Discontinuation
- 1997-01-06 DK DK97900236T patent/DK0880522T3/da active
- 1997-01-06 PL PL97327942A patent/PL327942A1/xx unknown
- 1997-01-06 DE DE69706830T patent/DE69706830T2/de not_active Expired - Fee Related
- 1997-01-06 EP EP97900236A patent/EP0880522B1/fr not_active Expired - Lifetime
- 1997-01-06 CA CA002239254A patent/CA2239254A1/fr not_active Abandoned
- 1997-01-06 AU AU13830/97A patent/AU1383097A/en not_active Abandoned
- 1997-01-06 AT AT97900236T patent/ATE205847T1/de not_active IP Right Cessation
- 1997-01-09 AR ARP970100091A patent/AR005424A1/es unknown
-
1998
- 1998-06-25 MX MX9805167A patent/MX9805167A/es unknown
- 1998-07-10 BG BG102618A patent/BG102618A/xx unknown
-
1999
- 1999-07-13 US US09/352,216 patent/US6100264A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP0880522B1 (fr) | 2001-09-19 |
| PL327942A1 (en) | 1999-01-04 |
| WO1997025328A1 (fr) | 1997-07-17 |
| AR005424A1 (es) | 1999-06-23 |
| FR2743366A1 (fr) | 1997-07-11 |
| US5990108A (en) | 1999-11-23 |
| SK93498A3 (en) | 1998-12-02 |
| CA2239254A1 (fr) | 1997-07-17 |
| MX9805167A (es) | 1998-10-31 |
| CZ216698A3 (cs) | 1998-10-14 |
| PT880522E (pt) | 2002-05-31 |
| AU1383097A (en) | 1997-08-01 |
| DE69706830T2 (de) | 2002-04-25 |
| KR19990077135A (ko) | 1999-10-25 |
| DK0880522T3 (da) | 2002-01-21 |
| DE69706830D1 (de) | 2001-10-25 |
| EP0880522A1 (fr) | 1998-12-02 |
| ZA9786B (en) | 1997-07-17 |
| BG102618A (en) | 1999-09-30 |
| JP2000505073A (ja) | 2000-04-25 |
| US6100264A (en) | 2000-08-08 |
| ATE205847T1 (de) | 2001-10-15 |
| FR2743366B1 (fr) | 1998-02-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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