ES2130669T3 - Espiro(heterociclo-imidazo(1,2-a)indeno(1,2-e)-pirazina)-4'-345 onas, su preparacion y los medicamentos que les contienen. - Google Patents
Espiro(heterociclo-imidazo(1,2-a)indeno(1,2-e)-pirazina)-4'-345 onas, su preparacion y los medicamentos que les contienen.Info
- Publication number
- ES2130669T3 ES2130669T3 ES95936624T ES95936624T ES2130669T3 ES 2130669 T3 ES2130669 T3 ES 2130669T3 ES 95936624 T ES95936624 T ES 95936624T ES 95936624 T ES95936624 T ES 95936624T ES 2130669 T3 ES2130669 T3 ES 2130669T3
- Authority
- ES
- Spain
- Prior art keywords
- alk
- cycle
- receptor
- het
- compounds
- 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
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102000005962 receptors Human genes 0.000 abstract 3
- 108020003175 receptors Proteins 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 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
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 abstract 1
- FUFZNHHSSMCXCZ-UHFFFAOYSA-N 5-piperidin-4-yl-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole Chemical compound FC(F)(F)C1=CC=CC(C=2N=C(ON=2)C2CCNCC2)=C1 FUFZNHHSSMCXCZ-UHFFFAOYSA-N 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
- -1 RADICAL CARBOXY Chemical class 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 230000036963 noncompetitive effect Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/20—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (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)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
COMPUESTO DE FORMULA (I) EN LA QUE R 1 Y R 4 FORMN JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN UNIDOS (A) UN CICLO 2- O 3-PIRROLIDINA, UN CICLO 2- O 4-PIPERIDINA O UN CICLO 2-AZACICLOHEPTANO, ESTANDO ESTOS CICLOS EVENTUALMENTE SUSTITUIDOS SOBRE NITROGENO POR UN RADICAL ALQUILO, -CHO, -CHOOR11, CO-AL-COOR6, -CO-ALK-NR6R12, -CO-ALKCONR6R8, -CO-COOR6, -CO-CH2-O-CH2COOR6, -CO-NH-HET, -CO-NH-ALK-HET, -CO-NH-ALK. -CON(ALK)AL'', -CS-NH2, CS-NH-AL, -CS-NH-AR", -CS-NH-HET. -ALKHET, -ALK-NR6R8, ALK-CO-NR6R8, -ALK-AR", SO2-ALK, -SO2-AR O -CO-CICLOALQUILO, ESTANDO EL CICLOALQUILO EVENTUALMENTE SUSTITUIDO EN -2 POR UN RADICAL CARBOXI O (B) UN CICLO 2-PIOOLIDINA-5-ONA. LOS COMPUESTOS DE FORMULA (I) PRESENTAN PROPIEDADES FARMACOLOGICAS INTERESANTES. ESTOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DEL ACIDO {ALAMINO-3-HIDROXI-5-METIL-4-ISOXAZOLEPROPIONICO (AMPA), TAMBIEN CONOCIDO BAJO EL NOMBRE DE RECEPTOR DE QUISCALATO. POR OTRA PARTE, LOS COMPUESTOS DE FORMULA (I) SON ANTAGONISTAS NO COMPETITIVOS DEL RECEPTOR N-METIL-D-ASPARTATO (NMDA), Y MAS PARTICULARMENTE, SON LIGANDOS PARA LOS SITIOS MODULADORES DE LA GLICINA DEL RECEPTOR NMDA.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9413060A FR2726275B1 (fr) | 1994-11-02 | 1994-11-02 | Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2130669T3 true ES2130669T3 (es) | 1999-07-01 |
Family
ID=9468413
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES95936624T Expired - Lifetime ES2130669T3 (es) | 1994-11-02 | 1995-10-30 | Espiro(heterociclo-imidazo(1,2-a)indeno(1,2-e)-pirazina)-4'-345 onas, su preparacion y los medicamentos que les contienen. |
Country Status (12)
Country | Link |
---|---|
US (1) | US5777114A (es) |
EP (1) | EP0789699B1 (es) |
JP (1) | JPH10508311A (es) |
AT (1) | ATE177747T1 (es) |
AU (1) | AU3848595A (es) |
DE (1) | DE69508421T2 (es) |
DK (1) | DK0789699T3 (es) |
ES (1) | ES2130669T3 (es) |
FR (1) | FR2726275B1 (es) |
GR (1) | GR3029714T3 (es) |
WO (1) | WO1996014318A1 (es) |
ZA (1) | ZA959044B (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2005506292A (ja) * | 2001-03-08 | 2005-03-03 | エモリー ユニバーシティ | pHに依存するNMDAレセプターアンタゴニスト |
US7045527B2 (en) | 2002-09-24 | 2006-05-16 | Amgen Inc. | Piperidine derivatives |
US7732162B2 (en) | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
CA2667839C (en) * | 2006-10-30 | 2016-01-12 | Hybrigenics Sa | Novel tetracyclic inhibitors of cysteine proteases, the pharmaceutical compositions thereof and their therapeutic applications |
WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
EP2117540A1 (en) | 2007-03-01 | 2009-11-18 | Probiodrug AG | New use of glutaminyl cyclase inhibitors |
JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | 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チオ尿素誘導体 |
CN103058957A (zh) | 2007-06-29 | 2013-04-24 | 埃莫里大学 | 用于神经保护的nmda受体拮抗剂 |
SG178953A1 (en) | 2009-09-11 | 2012-04-27 | Probiodrug Ag | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
EP2338492A1 (en) | 2009-12-24 | 2011-06-29 | Universidad del Pais Vasco | Methods and compositions for the treatment of alzheimer |
US9181233B2 (en) | 2010-03-03 | 2015-11-10 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
AU2011226074B2 (en) | 2010-03-10 | 2015-01-22 | Vivoryon Therapeutics N.V. | Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) |
US8541596B2 (en) | 2010-04-21 | 2013-09-24 | Probiodrug Ag | Inhibitors |
ES2570167T3 (es) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Derivados de benzimidazol como inhibidores de glutaminil ciclasa |
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 |
---|---|---|---|---|
US4354027A (en) * | 1980-05-19 | 1982-10-12 | Usv Pharmaceutical Corporation | Triazoloquinoxalin-4-ones |
DK101290D0 (da) * | 1990-04-24 | 1990-04-24 | Novo Nordisk As | Heterocykliske forbindelser, deres fremstilling og anvendelse |
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. |
FR2707643B1 (fr) * | 1993-07-16 | 1995-08-11 | Rhone Poulenc Rorer Sa | Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant. |
-
1994
- 1994-11-02 FR FR9413060A patent/FR2726275B1/fr not_active Expired - Fee Related
-
1995
- 1995-10-25 ZA ZA959044A patent/ZA959044B/xx unknown
- 1995-10-30 EP EP95936624A patent/EP0789699B1/fr not_active Expired - Lifetime
- 1995-10-30 ES ES95936624T patent/ES2130669T3/es not_active Expired - Lifetime
- 1995-10-30 DE DE69508421T patent/DE69508421T2/de not_active Expired - Fee Related
- 1995-10-30 US US08/836,410 patent/US5777114A/en not_active Expired - Fee Related
- 1995-10-30 AT AT95936624T patent/ATE177747T1/de not_active IP Right Cessation
- 1995-10-30 AU AU38485/95A patent/AU3848595A/en not_active Abandoned
- 1995-10-30 JP JP8515088A patent/JPH10508311A/ja not_active Ceased
- 1995-10-30 WO PCT/FR1995/001430 patent/WO1996014318A1/fr active IP Right Grant
- 1995-10-30 DK DK95936624T patent/DK0789699T3/da active
-
1999
- 1999-03-18 GR GR990400113T patent/GR3029714T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
FR2726275B1 (fr) | 1996-12-06 |
AU3848595A (en) | 1996-05-31 |
FR2726275A1 (fr) | 1996-05-03 |
US5777114A (en) | 1998-07-07 |
ATE177747T1 (de) | 1999-04-15 |
DE69508421T2 (de) | 1999-07-15 |
JPH10508311A (ja) | 1998-08-18 |
DE69508421D1 (de) | 1999-04-22 |
GR3029714T3 (en) | 1999-06-30 |
WO1996014318A1 (fr) | 1996-05-17 |
EP0789699B1 (fr) | 1999-03-17 |
DK0789699T3 (da) | 1999-10-11 |
EP0789699A1 (fr) | 1997-08-20 |
ZA959044B (en) | 1996-05-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG2A | Definitive protection |
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