ES2130438T3 - Derivados de imidazo(1,2-a)pirazin-4-ona, su preparacion y los medicamentos que les contienen. - Google Patents
Derivados de imidazo(1,2-a)pirazin-4-ona, su preparacion y los medicamentos que les contienen.Info
- Publication number
- ES2130438T3 ES2130438T3 ES94922904T ES94922904T ES2130438T3 ES 2130438 T3 ES2130438 T3 ES 2130438T3 ES 94922904 T ES94922904 T ES 94922904T ES 94922904 T ES94922904 T ES 94922904T ES 2130438 T3 ES2130438 T3 ES 2130438T3
- Authority
- ES
- Spain
- Prior art keywords
- alk
- alkyl
- represent
- hydrogen
- het
- 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
- 239000003814 drug Substances 0.000 title 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 ALKYL ALCOXI Chemical class 0.000 abstract 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 2
- 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
- 239000005557 antagonist Substances 0.000 abstract 2
- 150000003254 radicals Chemical group 0.000 abstract 2
- 102000005962 receptors Human genes 0.000 abstract 2
- 108020003175 receptors Proteins 0.000 abstract 2
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 abstract 1
- 101100439663 Arabidopsis thaliana CHR7 gene Proteins 0.000 abstract 1
- 239000004471 Glycine Substances 0.000 abstract 1
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 abstract 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical group [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 230000036963 noncompetitive effect Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
COMPUESTOS DE FORMULA (I) EN LA QUE BIEN R REPRESENTA C=R3, C(R4 R5 O CH-R6, R1 Y R2 REPRESENTAN HIDROGENO, HALOGENO,ALQUILO ALCOXI, AMINO ACILAMINO NH_CONH_ AR. C=CH-N(ALK)ALK'', NITRO CIANO, FENILO IMIDAZOLILO O SO3H,R3 REPRESENTA OXIGENO, NOH, NO-ALK,COOX O CHR7, R4 REPRESENTA ALQUILO ALK-HRT O ALK-AR, R5 REPRESENTA ALQUILO, ALK-HET O ALK-AR O BIEN C(R4)R5 REPRESENTA CICLOALQUILO, R6 REPRESENTA HIDROXI,ALQUILO, NR8R9, ALK-OH, ALK-NR8R9, ALK-HET O ALKHET, R7 REPRESENTA HIROXI, ALQUILO, FENILO. ALK-AR, -ALKHET, -NR10R11 O UN HETEROCICLO, R8 Y R9 REPRESENTAN ALQUILO, O BIEN R 8 REPRESENTA HIDROGENO, Y R9 REPRESENTA HIDROGENO OP ALQUILO, -COR1, CSR30 O SO2 R13, R10 Y R11 REPRESENTAN ALQUILO OCICLOALQUILO, R12 REPRESENTA ALQUILO CICLOALQUILO FENILO, -COO-ALK, -NH-HET, BIEN R REPRESENTA UN RADICAL 2-IMIDAZOLILMETILO Y R1 Y R2 REPRESENTAN CADA UNO UN ATOMO DE HIDROGENO -NH-ALK, -NH-AR, NH2 O -NH-HET, BIEN R REPRESENTA UN RADICAL 2-IMIDALILMETILO Y R1 Y R2 REPRESENTAN CADA UNO UN ATOMO DE HIDROGENO. LOS COMPUESTOS DE FORMULAS (I) SON ANTAGONISTAS DEL RECEPTOR DEL ACIDO {AL-AMINO-3-HIDROXI-5-METIL-4-ISOXAZOLOPROPIONICO (AMPA), CONOCIDO TAMBIEN BAJO EL NOMBRE DE RECEPTOR DE QUISCALATO. POR OTRA PARTE, LOS COMPUESTOS DE FORMULA (I) SON ANTAGONISTAS NO COMPETITIVOS DEL RECEPTOR N-METIL-D-ASPARATO (NMDA), Y MAS EN PARTICULAR, SON LIGANDOS PARA LOS LUGARES MODULADORES DE LA GLICINA DEL RECEPTOR NMDA:
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9308754A FR2707643B1 (fr) | 1993-07-16 | 1993-07-16 | Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2130438T3 true ES2130438T3 (es) | 1999-07-01 |
Family
ID=9449312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES94922904T Expired - Lifetime ES2130438T3 (es) | 1993-07-16 | 1994-07-11 | Derivados de imidazo(1,2-a)pirazin-4-ona, su preparacion y los medicamentos que les contienen. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US5753657A (es) |
| EP (1) | EP0708774B1 (es) |
| JP (1) | JPH09500873A (es) |
| AT (1) | ATE177746T1 (es) |
| AU (1) | AU681688B2 (es) |
| CA (1) | CA2167169A1 (es) |
| DE (1) | DE69417235T2 (es) |
| DK (1) | DK0708774T3 (es) |
| ES (1) | ES2130438T3 (es) |
| FI (1) | FI960160A7 (es) |
| FR (1) | FR2707643B1 (es) |
| GR (1) | GR3029713T3 (es) |
| HU (1) | HUT74678A (es) |
| IL (1) | IL110329A0 (es) |
| NO (1) | NO955192D0 (es) |
| PL (1) | PL312571A1 (es) |
| WO (1) | WO1995002601A1 (es) |
| ZA (1) | ZA945045B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2717813B1 (fr) * | 1994-03-28 | 1996-05-10 | Rhone Poulenc Rorer Sa | Dérivés d'imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant . |
| FR2717805B1 (fr) * | 1994-03-28 | 1996-05-10 | Rhone Poulenc Rorer Sa | Dérivés de 5H-indeno[1,2-b]pyrazine-2,3-dione, leur préparation et les médicaments les contenant . |
| 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. |
| FR2726275B1 (fr) * | 1994-11-02 | 1996-12-06 | Rhone Poulenc Rorer Sa | Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants |
| FR2738821B1 (fr) * | 1995-09-15 | 1997-11-21 | Rhone Poulenc Rorer Sa | Indeno[1,2-e]pyrazin-4-ones, leur preparation et les medicaments les contenant |
| US7375136B2 (en) * | 2001-03-08 | 2008-05-20 | Emory University | pH-dependent NMDA receptor antagonists |
| US7732162B2 (en) | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| JP5543209B2 (ja) * | 2006-10-30 | 2014-07-09 | ヒブリジェニクス・エスアー | 新規のシステインプロテアーゼのテトラサイクリン阻害剤、その薬剤組成物および治療のためのその使用 |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| JP5930573B2 (ja) | 2007-03-01 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤の新規使用 |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| EA201070077A1 (ru) * | 2007-06-29 | 2010-08-30 | Эмори Юниверсити | Антагонисты nmda-рецепторов с нейропротективным действием |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| NZ602312A (en) | 2010-03-10 | 2014-02-28 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU9049391A (en) * | 1990-12-20 | 1992-07-22 | Warner-Lambert Company | 2-acylamido derivatives of 3,4-dihydro-3-oxo-quinoxaline having pharmaceutical activity |
| US5153196A (en) * | 1991-06-05 | 1992-10-06 | Eli Lilly And Company | Excitatory amino acid receptor antagonists and methods for the use thereof |
| US5196421A (en) | 1991-06-05 | 1993-03-23 | Eli Lilly And Company | Excitatory amino acid receptor antagonists in methods for the use thereof |
| FR2696466B1 (fr) * | 1992-10-02 | 1994-11-25 | Rhone Poulenc Rorer Sa | Dérivés de 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant. |
-
1993
- 1993-07-16 FR FR9308754A patent/FR2707643B1/fr not_active Expired - Fee Related
-
1994
- 1994-07-11 EP EP94922904A patent/EP0708774B1/fr not_active Expired - Lifetime
- 1994-07-11 JP JP7504376A patent/JPH09500873A/ja active Pending
- 1994-07-11 US US08/583,126 patent/US5753657A/en not_active Expired - Fee Related
- 1994-07-11 ES ES94922904T patent/ES2130438T3/es not_active Expired - Lifetime
- 1994-07-11 AT AT94922904T patent/ATE177746T1/de not_active IP Right Cessation
- 1994-07-11 DK DK94922904T patent/DK0708774T3/da active
- 1994-07-11 WO PCT/FR1994/000866 patent/WO1995002601A1/fr not_active Ceased
- 1994-07-11 PL PL94312571A patent/PL312571A1/xx unknown
- 1994-07-11 HU HU9503955A patent/HUT74678A/hu unknown
- 1994-07-11 CA CA002167169A patent/CA2167169A1/fr not_active Abandoned
- 1994-07-11 AU AU72652/94A patent/AU681688B2/en not_active Withdrawn - After Issue
- 1994-07-11 DE DE69417235T patent/DE69417235T2/de not_active Expired - Fee Related
- 1994-07-12 ZA ZA945045A patent/ZA945045B/xx unknown
- 1994-07-14 IL IL11032994A patent/IL110329A0/xx unknown
-
1995
- 1995-12-20 NO NO955192A patent/NO955192D0/no unknown
-
1996
- 1996-01-12 FI FI960160A patent/FI960160A7/fi not_active Application Discontinuation
-
1999
- 1999-03-18 GR GR980402654T patent/GR3029713T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JPH09500873A (ja) | 1997-01-28 |
| AU7265294A (en) | 1995-02-13 |
| FI960160A0 (fi) | 1996-01-12 |
| NO955192L (no) | 1995-12-20 |
| HU9503955D0 (en) | 1996-03-28 |
| PL312571A1 (en) | 1996-04-29 |
| ATE177746T1 (de) | 1999-04-15 |
| US5753657A (en) | 1998-05-19 |
| AU681688B2 (en) | 1997-09-04 |
| FR2707643B1 (fr) | 1995-08-11 |
| FI960160A7 (fi) | 1996-01-12 |
| DE69417235D1 (de) | 1999-04-22 |
| NO955192D0 (no) | 1995-12-20 |
| HUT74678A (en) | 1997-01-28 |
| CA2167169A1 (fr) | 1995-01-26 |
| IL110329A0 (en) | 1994-10-21 |
| DK0708774T3 (da) | 1999-10-11 |
| EP0708774A1 (fr) | 1996-05-01 |
| ZA945045B (en) | 1995-02-22 |
| FR2707643A1 (fr) | 1995-01-20 |
| GR3029713T3 (en) | 1999-06-30 |
| WO1995002601A1 (fr) | 1995-01-26 |
| EP0708774B1 (fr) | 1999-03-17 |
| DE69417235T2 (de) | 1999-07-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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