ATE204852T1 - Alkylcarboxy-aminosäure modulatoren für den kainat-rezeptor - Google Patents
Alkylcarboxy-aminosäure modulatoren für den kainat-rezeptorInfo
- Publication number
- ATE204852T1 ATE204852T1 AT96908476T AT96908476T ATE204852T1 AT E204852 T1 ATE204852 T1 AT E204852T1 AT 96908476 T AT96908476 T AT 96908476T AT 96908476 T AT96908476 T AT 96908476T AT E204852 T1 ATE204852 T1 AT E204852T1
- Authority
- AT
- Austria
- Prior art keywords
- activation
- kainic acid
- amino acid
- receptor
- compounds
- Prior art date
Links
- 102000000079 Kainic Acid Receptors Human genes 0.000 title abstract 2
- 108010069902 Kainic Acid Receptors Proteins 0.000 title abstract 2
- 230000004913 activation Effects 0.000 abstract 2
- VLSMHEGGTFMBBZ-UHFFFAOYSA-N alpha-Kainic acid Natural products CC(=C)C1CNC(C(O)=O)C1CC(O)=O VLSMHEGGTFMBBZ-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- VLSMHEGGTFMBBZ-OOZYFLPDSA-N kainic acid Chemical compound CC(=C)[C@H]1CN[C@H](C(O)=O)[C@H]1CC(O)=O VLSMHEGGTFMBBZ-OOZYFLPDSA-N 0.000 abstract 2
- 229950006874 kainic acid Drugs 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
- 239000000774 AMPA receptor agonist Substances 0.000 abstract 1
- 108091005462 Cation channels Proteins 0.000 abstract 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- -1 class of alkyl carboxy amino acid Chemical class 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000009849 deactivation Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 235000013922 glutamic acid Nutrition 0.000 abstract 1
- 239000004220 glutamic acid Substances 0.000 abstract 1
- 230000001057 ionotropic effect Effects 0.000 abstract 1
- 239000002909 kainic acid receptor agonist Substances 0.000 abstract 1
- 230000003924 mental process Effects 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 230000003557 neuropsychological effect Effects 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/24—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one carboxyl group bound to the carbon skeleton, e.g. aspartic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
- C07C275/06—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton
- C07C275/16—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
- C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38991695A | 1995-02-15 | 1995-02-15 | |
| PCT/US1996/002227 WO1996025387A1 (en) | 1995-02-15 | 1996-02-13 | Alkylcarboxy amino acids-modulators of the kainate receptor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE204852T1 true ATE204852T1 (de) | 2001-09-15 |
Family
ID=23540296
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT96908476T ATE204852T1 (de) | 1995-02-15 | 1996-02-13 | Alkylcarboxy-aminosäure modulatoren für den kainat-rezeptor |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US5731348A (de) |
| EP (1) | EP0809624B1 (de) |
| JP (1) | JPH11501619A (de) |
| AT (1) | ATE204852T1 (de) |
| CA (1) | CA2216648A1 (de) |
| DE (1) | DE69614835T2 (de) |
| WO (1) | WO1996025387A1 (de) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996025387A1 (en) * | 1995-02-15 | 1996-08-22 | Symphony Pharmaceuticals, Inc. | Alkylcarboxy amino acids-modulators of the kainate receptor |
| GB2346883B (en) * | 1996-09-02 | 2001-02-14 | Lilly Industries Ltd | GluR5 receptor binding assay |
| CA2282357A1 (en) * | 1997-02-28 | 1998-09-03 | Bearsden Bio, Inc. | Method of determining protein-ligand interactions via computer modeling |
| NZ337827A (en) * | 1997-04-07 | 2000-12-22 | Lilly Co Eli | Use of GluR5 receptor antagonists in the manufacture of medicaments for treating pain |
| US6245521B1 (en) | 1999-03-03 | 2001-06-12 | Eli Lilly And Company | Assay for evaluating the affinity of compounds to the glutamate GluR5 receptor |
| NZ514813A (en) | 1999-04-08 | 2004-12-24 | Ortho Mcneil Pharm Inc | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
| EP1314041A2 (de) * | 2000-09-01 | 2003-05-28 | Annovis, Inc. | Screening von inhibitoren, stimulatoren und modulatoren der glutamatwiederaufnahme |
| US20020115721A1 (en) * | 2000-10-30 | 2002-08-22 | Annovis, Inc. | Esters of alkycarboxy amino acids as prodrugs of modulators of the kainate receptor |
| AU2002237717A1 (en) * | 2000-10-30 | 2002-05-27 | Annovis, Inc. | Method for modulation, stimulation, and inhibition of glutamate reuptake |
| TW200612905A (en) * | 2004-06-16 | 2006-05-01 | Janssen Pharmaceutica Nv | Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders |
| MY147767A (en) * | 2004-06-16 | 2013-01-31 | Janssen Pharmaceutica Nv | Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders |
| KR20070057848A (ko) * | 2004-08-24 | 2007-06-07 | 얀센 파마슈티카 엔.브이. | 항경련제로 유용한 신규 벤조-융합된 헤테로아릴 설파미드유도체 |
| EP1881959A1 (de) * | 2005-05-20 | 2008-01-30 | Janssen Pharmaceutica N.V. | Verfahren zur herstellung von sulfamidderivaten |
| US20070155823A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives as neuroprotective agents |
| US20070155827A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of depression |
| US20070155824A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives for disease modification / epileptogenesis |
| US8937096B2 (en) * | 2005-12-19 | 2015-01-20 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of mania and bipolar disorder |
| AR058389A1 (es) * | 2005-12-19 | 2008-01-30 | Janssen Pharmaceutica Nv | Uso de derivados heterociclicos benzo-fusionados de sulfamida para el tratamiento de la obesidad |
| US8691867B2 (en) * | 2005-12-19 | 2014-04-08 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of substance abuse and addiction |
| US8497298B2 (en) * | 2005-12-19 | 2013-07-30 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for lowering lipids and lowering blood glucose levels |
| US8716231B2 (en) * | 2005-12-19 | 2014-05-06 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of pain |
| US20070191460A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of Benzo-Heteroaryl Sulfamide Derivatives for the Treatment of Disease Modification / Epileptogenesis |
| US20070191474A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of migraine |
| US20070191451A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of benzo-heteroaryl sulfamide derivatives as neuroprotective agents |
| EP2026790A2 (de) * | 2006-05-19 | 2009-02-25 | Janssen Pharmaceutica, N.V. | Kombinationstherapie zur behandlung von epilepsie und assoziierten erkrankungen |
| US20090247617A1 (en) * | 2008-03-26 | 2009-10-01 | Abdel-Magid Ahmed F | Process for the preparation of benzo-fused heteroaryl sulfamates |
| US20090247616A1 (en) * | 2008-03-26 | 2009-10-01 | Smith-Swintosky Virginia L | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of anxiety |
| BRPI0915890A2 (pt) | 2008-06-23 | 2015-11-03 | Janssen Pharmaceutica Nv | forma cristalina de (2s)-(-)-n-(6-cloro-2,3-di-hidro-benzo[1,4]dioxin-2-ilmetil)-sulfamida |
| US8815939B2 (en) * | 2008-07-22 | 2014-08-26 | Janssen Pharmaceutica Nv | Substituted sulfamide derivatives |
| WO2012090201A2 (en) | 2010-12-26 | 2012-07-05 | Carmel-Haifa University Economic Corp. | Methods of improving cognitive function |
| CN115650881B (zh) | 2022-09-06 | 2025-01-17 | 浙江医药股份有限公司新昌制药厂 | 一种利用微反应器合成喹诺酮类化合物中间体的工艺方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1057652A (en) * | 1963-01-16 | 1967-02-08 | Merck & Co Inc | Amino derivatives of amino acids |
| DK146787A (da) * | 1987-03-23 | 1988-09-24 | Ferrosan | Heterocykliske forbindelser, deres fremstilling og anvendelse |
| US4904681A (en) * | 1987-12-01 | 1990-02-27 | G. D. Searle & Co. | D-cycloserine and its prodrugs as cognitive enhancers |
| US5061721A (en) * | 1989-03-15 | 1991-10-29 | G. D. Searle & Co. | Composition containing d-cycloserine and d-alanine for memory and learning enhancement or treatment of a cognitive or psychotic disorder |
| US5086702A (en) * | 1990-04-12 | 1992-02-11 | Atlas Powder Company | Modular blasting system |
| US5364876A (en) * | 1992-12-02 | 1994-11-15 | Guilford Pharmaceuticals Inc. | Omega-[2-(alkyl)phenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors |
| AU6836394A (en) * | 1993-06-01 | 1994-12-20 | Cortex Pharmaceuticals, Inc. | Use of metabotropic receptor agonists in progressive neurodegenerative deseases |
| WO1996025387A1 (en) * | 1995-02-15 | 1996-08-22 | Symphony Pharmaceuticals, Inc. | Alkylcarboxy amino acids-modulators of the kainate receptor |
-
1996
- 1996-02-13 WO PCT/US1996/002227 patent/WO1996025387A1/en not_active Ceased
- 1996-02-13 EP EP96908476A patent/EP0809624B1/de not_active Expired - Lifetime
- 1996-02-13 CA CA002216648A patent/CA2216648A1/en not_active Abandoned
- 1996-02-13 JP JP8525195A patent/JPH11501619A/ja active Pending
- 1996-02-13 US US08/600,330 patent/US5731348A/en not_active Expired - Fee Related
- 1996-02-13 AT AT96908476T patent/ATE204852T1/de not_active IP Right Cessation
- 1996-02-13 DE DE69614835T patent/DE69614835T2/de not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US5731348A (en) | 1998-03-24 |
| JPH11501619A (ja) | 1999-02-09 |
| EP0809624A1 (de) | 1997-12-03 |
| DE69614835D1 (de) | 2001-10-04 |
| EP0809624B1 (de) | 2001-08-29 |
| DE69614835T2 (de) | 2002-04-25 |
| WO1996025387A1 (en) | 1996-08-22 |
| CA2216648A1 (en) | 1996-08-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| UEP | Publication of translation of european patent specification | ||
| REN | Ceased due to non-payment of the annual fee |