JPH01500513A - 特異的興奮性アミノ酸神経伝達物質受容体の拮抗物質 - Google Patents
特異的興奮性アミノ酸神経伝達物質受容体の拮抗物質Info
- Publication number
- JPH01500513A JPH01500513A JP62501875A JP50187587A JPH01500513A JP H01500513 A JPH01500513 A JP H01500513A JP 62501875 A JP62501875 A JP 62501875A JP 50187587 A JP50187587 A JP 50187587A JP H01500513 A JPH01500513 A JP H01500513A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- substance
- compound
- amino
- phenyl
- 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.)
- Pending
Links
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- JNGZXGGOCLZBFB-IVCQMTBJSA-N compound E Chemical compound N([C@@H](C)C(=O)N[C@@H]1C(N(C)C2=CC=CC=C2C(C=2C=CC=CC=2)=N1)=O)C(=O)CC1=CC(F)=CC(F)=C1 JNGZXGGOCLZBFB-IVCQMTBJSA-N 0.000 description 1
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- XRIXXWKUETUCIS-UHFFFAOYSA-N diethyl 2-acetamido-2-methylpropanedioate Chemical compound CCOC(=O)C(C)(NC(C)=O)C(=O)OCC XRIXXWKUETUCIS-UHFFFAOYSA-N 0.000 description 1
- ISOLMABRZPQKOV-UHFFFAOYSA-N diethyl 2-acetamidopropanedioate Chemical compound CCOC(=O)C(NC(C)=O)C(=O)OCC ISOLMABRZPQKOV-UHFFFAOYSA-N 0.000 description 1
- CVEQLWWOYIJJSD-UHFFFAOYSA-N diethyl 2-acetamidopropanedioate;sodium Chemical compound [Na].CCOC(=O)C(NC(C)=O)C(=O)OCC CVEQLWWOYIJJSD-UHFFFAOYSA-N 0.000 description 1
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- 239000007788 liquid Substances 0.000 description 1
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- 239000010452 phosphate Chemical class 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
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- 239000000843 powder Substances 0.000 description 1
- 238000011533 pre-incubation Methods 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 210000004129 prosencephalon Anatomy 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
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- MFBOGIVSZKQAPD-UHFFFAOYSA-M sodium butyrate Chemical compound [Na+].CCCC([O-])=O MFBOGIVSZKQAPD-UHFFFAOYSA-M 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
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- RXJKFRMDXUJTEX-UHFFFAOYSA-N triethylphosphine Chemical compound CCP(CC)CC RXJKFRMDXUJTEX-UHFFFAOYSA-N 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
- C07F9/3882—Arylalkanephosphonic acids
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
- C07F9/3834—Aromatic acids (P-C aromatic linkage)
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US06/849,696 US4657899A (en) | 1986-04-09 | 1986-04-09 | Antagonists of specific excitatory amino acid neurotransmitter receptors |
| US849,696 | 1986-04-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH01500513A true JPH01500513A (ja) | 1989-02-23 |
Family
ID=25306304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP62501875A Pending JPH01500513A (ja) | 1986-04-09 | 1987-02-25 | 特異的興奮性アミノ酸神経伝達物質受容体の拮抗物質 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US4657899A (fr) |
| EP (1) | EP0242709A3 (fr) |
| JP (1) | JPH01500513A (fr) |
| AU (1) | AU7166787A (fr) |
| CA (1) | CA1297492C (fr) |
| WO (1) | WO1987006131A1 (fr) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5243062A (en) * | 1984-10-12 | 1993-09-07 | Ciba-Geigy Corporation | Substituted propane-phosphonous acid compounds |
| US5457095A (en) * | 1984-10-12 | 1995-10-10 | Ciba-Geigy Corporation | Substituted propane-phosponous acid compounds |
| GB8600783D0 (en) * | 1986-01-14 | 1986-02-19 | Merck Sharp & Dohme | N-methyl-d-aspartate receptor antagonists |
| US5051413A (en) * | 1986-02-13 | 1991-09-24 | Ciba-Geigy Corporation | Unsaturated amino acids |
| US5175344A (en) * | 1986-02-13 | 1992-12-29 | Ciba-Geigy Corporation | Unsaturated amino acids |
| US5395827A (en) * | 1986-04-09 | 1995-03-07 | Guilford Pharmaceuticals Inc. | ω-[2-(phosphonoalkyl)phenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors |
| US4812458A (en) * | 1986-09-16 | 1989-03-14 | A/S Ferrosan | 6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics |
| US5321016A (en) * | 1986-10-30 | 1994-06-14 | Sandoz Pharmaceuticals Corp. | Use of certain substituted α-amino acids in treating stress-related psychiatric disorders |
| GB8625941D0 (en) * | 1986-10-30 | 1986-12-03 | Sandoz Ltd | Substituted alpha-amino acids |
| US4761405A (en) * | 1987-03-04 | 1988-08-02 | Nova Pharmaceutical Corporation | Antagonists of specific excitatory amino acid neurotransmitter receptors having increased potency |
| US4970297A (en) * | 1987-03-13 | 1990-11-13 | Syntex (U.S.A.) Inc. | Transglutaminase inhibitors |
| US4918064A (en) * | 1987-10-21 | 1990-04-17 | G. D. Searle & Co. | Phenyl glycines for use in reducing neurotoxic injury |
| US5175153A (en) * | 1987-11-30 | 1992-12-29 | Warner-Lambert Company | Substituted alpha-amino acids having pharmaceutical activity |
| US5190933A (en) * | 1987-12-04 | 1993-03-02 | Ciba-Geigy Corporation | Substituted propane-phosphinic acid compounds |
| US5300679A (en) * | 1987-12-04 | 1994-04-05 | Ciba-Geigy Corporation | Substituted propane-phosphinic acid compounds |
| FR2634763B1 (fr) * | 1988-08-01 | 1991-07-12 | Inst Nat Sante Rech Med | Amino-acides et peptides presentant un residu tyrosine modifiee, leur preparation et leur application comme medicaments |
| US4997821A (en) * | 1988-10-21 | 1991-03-05 | Cordi Alexis A | Phosphono-hydroisoquinoline compounds useful in reducing neurotoxic injury |
| US5177240A (en) * | 1988-10-21 | 1993-01-05 | G. D. Searle & Co. | O-phosphono(alkyl)-n-sulfonyl-phenyl-alanine derivatives useful as intermediates for preparation of phosphono-hydroisoquinolines |
| US5049555A (en) * | 1988-12-19 | 1991-09-17 | Nova Pharmaceutical Corporation | Antagonists of specific excitatory amino acid receptors as neuroprotectants and anxiolytics |
| US5100654A (en) * | 1989-04-07 | 1992-03-31 | Yale University | Phosphorylated derivatives of l-dopa and compositions and methods for increasing the melanin content in mammalian skin and hair |
| ATE112282T1 (de) * | 1989-04-07 | 1994-10-15 | Ciba Geigy Ag | Ungesättigte aminodicarbonsäurederivate. |
| US5567840A (en) * | 1989-05-13 | 1996-10-22 | Ciba-Geigy Corporation | Substituted aminoalkylphosphinic acids |
| US5281747A (en) * | 1989-05-13 | 1994-01-25 | Ciba-Geigy Corporation | Substituted aminoalkylphosphinic acids |
| US5488140A (en) * | 1989-09-26 | 1996-01-30 | Ciba-Geigy Corporation | 4-substituted 2-aminoalk-3-enoic |
| US5294734A (en) * | 1989-09-26 | 1994-03-15 | Ciba-Geigy Corp. | 4-substituted 2-aminoalk-3-enoic acids |
| US5716964A (en) * | 1989-12-04 | 1998-02-10 | G.D. Searle & Co. | Tetrazolyl substituted imidazo 1,2-a!pyridinylalkyl compounds for treatment of neurotoxic injury |
| KR910011852A (ko) * | 1989-12-04 | 1991-08-07 | 폴 디. 매튜카이티스 | 신경독 장해 치료용 이미다조[1,2-a]피리디닐알킬 화합물 |
| US5238958A (en) * | 1990-02-26 | 1993-08-24 | Warner-Lambert Company | Substituted α-amino acids having selected acidic moieties for use as excitatory amino acid antagonists in pharmaceuticals |
| US5194430A (en) * | 1990-05-17 | 1993-03-16 | Merrell Dow Pharmaceuticals Inc. | Heterocyclic-nmda antagonists |
| IL114631A (en) * | 1990-06-22 | 1998-12-06 | Novartis Ag | Anti-epileptic compositions containing gabab- antagonistic compounds |
| DE69118700D1 (de) * | 1990-08-13 | 1996-05-15 | Searle & Co | Verwendung von heterozyklischen aminoalkoholverbindungen zur herstellung eines medikaments für die behandlung von erkrankungen des zns |
| US5118675A (en) * | 1991-02-15 | 1992-06-02 | American Home Products Corporation | Quinoxaline phosphono-amino acids |
| WO1993005772A1 (fr) * | 1991-09-26 | 1993-04-01 | Nova Pharmaceutical Corporation | ACIDES φ-[2-(PHOSPHONOALKYL)PHENYL]-2-AMINO-ALCANOIQUES UTILISES COMME ANTAGONISTES DE RECEPTEURS D'ACIDES AMINES EXCITATEURS |
| US5200546A (en) * | 1991-09-30 | 1993-04-06 | The United States Of America As Represented By The Department Of Health And Human Services | Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis |
| US5264607A (en) * | 1991-09-30 | 1993-11-23 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Process of making benzylic α,α-diflurophosphonates from benzylic α-ketophosphorates |
| US5475129A (en) * | 1991-09-30 | 1995-12-12 | The United States Of America As Represented By The Department Of Health And Human Services | Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis |
| US5302586A (en) * | 1991-12-19 | 1994-04-12 | G. D. Searle & Co. | Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury |
| US5252563A (en) * | 1991-12-19 | 1993-10-12 | G. D. Searle & Company | 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine compounds for treatment of neurotoxic injury |
| US5216003A (en) * | 1992-01-02 | 1993-06-01 | G. D. Searle & Co. | Diacid-containing benzimidazole compounds for treatment of neurotoxic injury |
| 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 |
| US5331001A (en) * | 1992-12-02 | 1994-07-19 | Guilford Pharmaceuticals Inc. | ω-[2-(tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors |
| US5342946A (en) * | 1992-12-02 | 1994-08-30 | Guilford Pharmaceuticals Inc. | Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic excitatory amino acid receptors |
| GB9325360D0 (en) * | 1993-12-10 | 1994-02-16 | Univ Bristol | Organic compounds |
| US5489717A (en) * | 1994-07-08 | 1996-02-06 | Warner-Lambert Company | Glutamate (NMDA) receptor antagonists |
| US7354955B2 (en) * | 2004-01-07 | 2008-04-08 | Abbott Laboratories | (2S)-amino(phenyl)acetic acid and derivatives as α2δ voltage-gated calcium channel ligands |
| US20050148671A1 (en) * | 2004-01-07 | 2005-07-07 | Chih-Hung Lee | (2S)-amino(phenyl)acetic acid and derivatives as alpha2delta voltage-gated calcium channel ligands |
| EP3427729A1 (fr) | 2017-07-13 | 2019-01-16 | Paris Sciences et Lettres - Quartier Latin | Probénécide destiné à être utilisé dans le traitement de maladies, troubles ou états épileptiques |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE550634A (fr) * | 1955-08-30 | |||
| US2966074A (en) * | 1958-10-29 | 1960-12-27 | Houdaille Industries Inc | Viscous torsional vibration damper |
| US3754085A (en) * | 1971-07-19 | 1973-08-21 | Merck & Co Inc | Phosphonic acid anti-fibrinolytic agents |
| SU431171A1 (ru) * | 1972-09-27 | 1974-06-05 | С. Н. Еременко, Н. С. Фрумина, А. М. Лукин, Г. Б. Заварихина | СПОСОБ ПОЛУЧЕНИЯ n-ФOCФOHOФEHИЛAHTPAHJИЛOBOЙ1Изобретение относитс к способу получени производного фенил антраниловой кислоты, содержащего фосфоногруппу ^в га-положении по отношению к аминному азоту, которое может найти применение в аналитической хи'мии. 5Известен способ получени различных замещенных фенилантраниловой кислоты, например днфениламино-3-сульфо-2'-карбоновой кислоты, нагреванием солей о-хлорбензойной кислоты и сульфаниловой кислоты с поташом ю в присутствии порощ.ка меди в за1па нной трубке.Предлагаемый способ получени п-фосфо- нофенилантраниловой кислоты заключаетс в конденсации п-аминафенилфосфоновой кислоты с о-хлорбензойной кислотой в ще.лочной среде в присутствии порошха .меди или ее солей в качестве катализатора при нагревании, например до 120—130°С, с последующим выделением целевого продукта известными приемами.Реакци протекает по схеме:Ct, .^а.,СОзCUS04 t",СООМа•NaCl |
| DE2459491A1 (de) * | 1974-12-17 | 1976-06-24 | Bayer Ag | Gegenueber isocyanaten reaktive phosphorhaltige flammschutzmittel |
-
1986
- 1986-04-09 US US06/849,696 patent/US4657899A/en not_active Expired - Fee Related
-
1987
- 1987-02-25 JP JP62501875A patent/JPH01500513A/ja active Pending
- 1987-02-25 WO PCT/US1987/000444 patent/WO1987006131A1/fr not_active Ceased
- 1987-02-25 AU AU71667/87A patent/AU7166787A/en not_active Abandoned
- 1987-03-20 CA CA000532659A patent/CA1297492C/fr not_active Expired - Lifetime
- 1987-04-08 EP EP87105189A patent/EP0242709A3/fr not_active Ceased
Non-Patent Citations (1)
| Title |
|---|
| CHEM PHARM BULL=1984 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO1987006131A1 (fr) | 1987-10-22 |
| EP0242709A2 (fr) | 1987-10-28 |
| EP0242709A3 (fr) | 1989-07-26 |
| US4657899A (en) | 1987-04-14 |
| CA1297492C (fr) | 1992-03-17 |
| AU7166787A (en) | 1987-11-09 |
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