KR930007961A - 벤즈이미다졸 포스포노-아미노산 - Google Patents
벤즈이미다졸 포스포노-아미노산 Download PDFInfo
- Publication number
- KR930007961A KR930007961A KR1019920018638A KR920018638A KR930007961A KR 930007961 A KR930007961 A KR 930007961A KR 1019920018638 A KR1019920018638 A KR 1019920018638A KR 920018638 A KR920018638 A KR 920018638A KR 930007961 A KR930007961 A KR 930007961A
- Authority
- KR
- South Korea
- Prior art keywords
- benzimidazole
- compound
- amino
- lower alkyl
- phosphonomethyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims abstract 9
- -1 pivaloyloxymethyl Chemical group 0.000 claims abstract 9
- 125000000217 alkyl group Chemical group 0.000 claims abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 6
- 239000001257 hydrogen Substances 0.000 claims abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 6
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 3
- 125000001475 halogen functional group Chemical group 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 3
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- UGEGLXMMUVGKKC-SSDOTTSWSA-N (2r)-2-amino-3-[1-(phosphonomethyl)benzimidazol-2-yl]propanoic acid Chemical compound C1=CC=C2N(CP(O)(O)=O)C(C[C@@H](N)C(O)=O)=NC2=C1 UGEGLXMMUVGKKC-SSDOTTSWSA-N 0.000 claims 1
- PYAFCWDVRQHNFL-SSDOTTSWSA-N (2r)-2-amino-3-[5,6-dichloro-1-(phosphonomethyl)benzimidazol-2-yl]propanoic acid Chemical compound ClC1=C(Cl)C=C2N(CP(O)(O)=O)C(C[C@@H](N)C(O)=O)=NC2=C1 PYAFCWDVRQHNFL-SSDOTTSWSA-N 0.000 claims 1
- YVRNGHASPMHOMK-SECBINFHSA-N (2r)-2-amino-3-[5,6-dimethyl-1-(phosphonomethyl)benzimidazol-2-yl]propanoic acid Chemical compound C1=C(C)C(C)=CC2=C1N(CP(O)(O)=O)C(C[C@@H](N)C(O)=O)=N2 YVRNGHASPMHOMK-SECBINFHSA-N 0.000 claims 1
- IJESEVVUJRTURR-SSDOTTSWSA-N (2r)-2-amino-3-[5-chloro-1-(phosphonomethyl)benzimidazol-2-yl]propanoic acid Chemical compound ClC1=CC=C2N(CP(O)(O)=O)C(C[C@@H](N)C(O)=O)=NC2=C1 IJESEVVUJRTURR-SSDOTTSWSA-N 0.000 claims 1
- UMEDZDZHWRVHJN-SSDOTTSWSA-N (2r)-2-amino-3-[6-chloro-1-(phosphonomethyl)benzimidazol-2-yl]propanoic acid Chemical compound C1=C(Cl)C=C2N(CP(O)(O)=O)C(C[C@@H](N)C(O)=O)=NC2=C1 UMEDZDZHWRVHJN-SSDOTTSWSA-N 0.000 claims 1
- 206010001497 Agitation Diseases 0.000 claims 1
- 102000018899 Glutamate Receptors Human genes 0.000 claims 1
- 108010027915 Glutamate Receptors Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 1
- 230000000324 neuroprotective effect Effects 0.000 claims 1
- 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 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 239000003257 excitatory amino acid Substances 0.000 abstract 1
- 230000002461 excitatory amino acid Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 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
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
-
- 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
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
- C07F9/65068—Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring 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
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Insulating Materials (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
하기 일반식의 화합물 또는 약리학적으로 허용되는 이의 염은 흥분성 아미노산 수용체의 과도흥분으로 인한 중추신경계 관련 장애를 치료하고 예방하는데 유용한 NMDA 길항제이다.
상기식에서, R은 수소, 저급 알킬, 벤질 또는 피발로일옥시메틸이고, R1및 R2는 독립적으로 수소, 저급 알킬, 저급 알콕시, 트리플루오로메틸, 트리플루오로메톡시, 메탄설포닐아미노, 아세틸아미노 또는 할로이거나, R1및 R2는 함께 메틸렌디옥시 그룹을 나타낸다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (7)
- 하기 일반식의 화합물 및 약리학적으로 허용되는 이의 염.상기식에서, R은 수소, 저급 알킬, 벤질 또는 피발로일옥시메틸이고, R1및 R2는 독립적으로 수소, 저급 알킬, 저급 알콕시, 트리플루오로메틸, 트리플루오로메톡시, 메탄설포닐아미노, 아세틸아미노 또는 할로이거나, R1및 R2는 함께 메틸렌디옥시 그룹을 나타낸다.
- 제1항에 있어서, R-α-아미노-1-(포스포노메틸)-1H-벤즈이미다졸-2-프로파노산인 화합물.
- 제1항에 있어서, R-α-아미노-5,6-디클로로-1-(포스포노메틸)-1H-벤즈이미다졸-2-프로파노산인 화합물.
- 제1항에 있어서, R-α-아미노-5,6-디메틸-1-(포스포노메틸)-1H-벤즈이미다졸-2-프로파노산인 화합물.
- 제1항에 있어서, R-α-아미노-6-클로로-1-(포스포노메틸)-1H-벤즈이미다졸-2-프로파노산인 화합물.
- 제1항에 있어서, R-α-아미노-5-클로로-1-(포스포노메틸)-1H-벤즈이미다졸-2-프로파노산인 화합물.
- 흥분성 아미노산 수용체의 과도흥분으로 인한 신경장애가 있는 포유동물에게 NMDA 길항제만 하기 일반식의 화합물 또는 약리학적으로 허용되는 이의 염을 신경보호량으로 투여함을 특징으로 하여, 흥분성 아미노산 수용체의 과도흥분으로 인한 신경장애를 치료하고 예방하는 방법.상기식에서, R은 수소, 저급 알킬, 벤질 또는 피발로일옥시메틸이고, R1및 R2는 독립적으로 수소, 저급 알킬, 저급 알콕시, 트리플루오로메틸, 트리플루오로메톡시, 메탄설포닐아미노, 아세틸아미노 또는 할로이거나, R1및 R2는 함께 메틸렌디옥시 그룹을 나타낸다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US07/776,528 US5124319A (en) | 1991-10-11 | 1991-10-11 | Benzimidazole phosphono-amino acids |
US07/776,528 | 1991-10-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR930007961A true KR930007961A (ko) | 1993-05-20 |
Family
ID=25107643
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019920018638A KR930007961A (ko) | 1991-10-11 | 1992-10-10 | 벤즈이미다졸 포스포노-아미노산 |
Country Status (22)
Country | Link |
---|---|
US (1) | US5124319A (ko) |
EP (1) | EP0539057B1 (ko) |
JP (1) | JPH05222077A (ko) |
KR (1) | KR930007961A (ko) |
AT (1) | ATE155473T1 (ko) |
AU (1) | AU656811B2 (ko) |
CA (1) | CA2080253A1 (ko) |
CZ (1) | CZ308392A3 (ko) |
DE (1) | DE69220879T2 (ko) |
DK (1) | DK0539057T3 (ko) |
ES (1) | ES2104841T3 (ko) |
FI (1) | FI924570A (ko) |
GR (1) | GR3024767T3 (ko) |
HU (2) | HUT62196A (ko) |
IL (1) | IL103330A (ko) |
MX (1) | MX9205816A (ko) |
NO (1) | NO300690B1 (ko) |
NZ (1) | NZ244587A (ko) |
RU (1) | RU2073004C1 (ko) |
SG (1) | SG47768A1 (ko) |
SK (1) | SK279381B6 (ko) |
ZA (1) | ZA927535B (ko) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5334618A (en) * | 1991-04-04 | 1994-08-02 | The Children's Medical Center Corporation | Method of preventing NMDA receptor-mediated neuronal damage |
US5124319A (en) * | 1991-10-11 | 1992-06-23 | American Home Products Corporation | Benzimidazole phosphono-amino acids |
US5321012A (en) * | 1993-01-28 | 1994-06-14 | Virginia Commonwealth University Medical College | Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance |
USRE39300E1 (en) | 1993-01-28 | 2006-09-19 | Virginia Commonwealth University Medical College Of Virginia | Inhibiting the development of tolerance to and/or dependence on an addictive substance |
IS4233A (is) * | 1993-12-22 | 1995-06-23 | Astra Aktiebolag | Misleit hringtengd efnasambönd |
US5864040A (en) * | 1996-01-11 | 1999-01-26 | American Home Products Corporation | Benzimidazole phosphono-amino acids |
DK0970095T3 (da) * | 1997-03-07 | 2004-03-08 | Metabasis Therapeutics Inc | Hidtil ukendte benzimidazolinhibitorer for fructose-1,6-bisphosphase |
AU6452098A (en) * | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel purine inhibitors of fructose-1,6-bisphosphatase |
GB9917822D0 (en) * | 1999-07-29 | 1999-09-29 | Imperial College | Nmda antagonist |
US6316474B1 (en) * | 1999-10-29 | 2001-11-13 | Merck & Co., Inc. | 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists |
US7375136B2 (en) * | 2001-03-08 | 2008-05-20 | Emory University | pH-dependent NMDA receptor antagonists |
UA78529C2 (en) * | 2001-10-10 | 2007-04-10 | Wyeth Corp | Derivatives of [[2-(amino-3,4-dioxo-1-cyclobutene-1-yl)amino]alkyl] acid for treating pain |
US20040082543A1 (en) * | 2002-10-29 | 2004-04-29 | Pharmacia Corporation | Compositions of cyclooxygenase-2 selective inhibitors and NMDA receptor antagonists for the treatment or prevention of neuropathic pain |
PL1611144T3 (pl) * | 2003-04-09 | 2011-03-31 | Wyeth Llc | Pochodne kwasu 2-(8,9-diokso-2,6-diazabicyklo(5.2.0)non-1(7)-en-2-ylo)alkilofosfonowego i ich zastosowanie jako antagonistów receptora N-metylo-D-asparaginianu (NMDA) |
BRPI0409088A (pt) * | 2003-04-09 | 2006-04-11 | Wyeth Corp | composições farmacêuticas para administração intranasal de ácido [2-(8,9-dioxo-2,6-diazabiciclo [5.2.0]non-1(7)-en-2-il)alquil]-fosfÈnico e derivados e métodos de uso dos mesmos |
US20050142192A1 (en) * | 2003-10-15 | 2005-06-30 | Wyeth | Oral administration of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and derivatives |
TW200514775A (en) * | 2003-10-22 | 2005-05-01 | Wyeth Corp | Methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl} phosphonic acid and esters thereof |
AU2008272964A1 (en) * | 2007-06-29 | 2009-01-08 | Emory University | NMDA receptor antagonists for neuroprotection |
JP2010537999A (ja) * | 2007-08-27 | 2010-12-09 | ワイス・エルエルシー | 麻酔薬節約効果を得るためのnmda拮抗薬を用いる組成物および方法 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SU959724A1 (ru) * | 1981-05-06 | 1982-09-23 | Ленинградский Ордена Трудового Красного Знамени Сельскохозяйственный Институт | Способ регулировани роста растений огурца |
PH23848A (en) * | 1985-05-24 | 1989-11-23 | Ciba Geigy Ag | Certain phosphonic acids and derivatives |
US4746653A (en) * | 1986-02-28 | 1988-05-24 | Ciba-Geigy Corporation | Certain hetero phosphonic acid derivatives of 2-piperidine or 2-tetrahydropyridinecarboxylates and esters thereof which are useful for the treatment of disorders responsive to blockade of the NMDA receptor in mammals |
EP0400835A1 (en) * | 1989-05-15 | 1990-12-05 | Merck & Co. Inc. | Substituted benzimidazoles as angiotensin II antagonists |
US5124319A (en) * | 1991-10-11 | 1992-06-23 | American Home Products Corporation | Benzimidazole phosphono-amino acids |
-
1991
- 1991-10-11 US US07/776,528 patent/US5124319A/en not_active Expired - Lifetime
-
1992
- 1992-09-30 ZA ZA927535A patent/ZA927535B/xx unknown
- 1992-10-01 NZ NZ244587A patent/NZ244587A/xx unknown
- 1992-10-02 IL IL10333092A patent/IL103330A/en not_active IP Right Cessation
- 1992-10-08 DE DE69220879T patent/DE69220879T2/de not_active Expired - Fee Related
- 1992-10-08 SG SG1996004290A patent/SG47768A1/en unknown
- 1992-10-08 AT AT92309160T patent/ATE155473T1/de not_active IP Right Cessation
- 1992-10-08 AU AU26269/92A patent/AU656811B2/en not_active Ceased
- 1992-10-08 DK DK92309160.7T patent/DK0539057T3/da active
- 1992-10-08 EP EP92309160A patent/EP0539057B1/en not_active Expired - Lifetime
- 1992-10-08 ES ES92309160T patent/ES2104841T3/es not_active Expired - Lifetime
- 1992-10-09 CZ CS923083A patent/CZ308392A3/cs unknown
- 1992-10-09 CA CA002080253A patent/CA2080253A1/en not_active Abandoned
- 1992-10-09 SK SK3083-92A patent/SK279381B6/sk unknown
- 1992-10-09 JP JP4271403A patent/JPH05222077A/ja active Pending
- 1992-10-09 FI FI924570A patent/FI924570A/fi unknown
- 1992-10-09 RU SU925053101A patent/RU2073004C1/ru active
- 1992-10-09 HU HU9203203A patent/HUT62196A/hu unknown
- 1992-10-09 MX MX9205816A patent/MX9205816A/es not_active IP Right Cessation
- 1992-10-09 NO NO923940A patent/NO300690B1/no unknown
- 1992-10-10 KR KR1019920018638A patent/KR930007961A/ko not_active Application Discontinuation
-
1995
- 1995-06-21 HU HU95P/P00314P patent/HU211942A9/hu unknown
-
1997
- 1997-09-17 GR GR970402423T patent/GR3024767T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
ATE155473T1 (de) | 1997-08-15 |
ZA927535B (en) | 1994-03-30 |
IL103330A0 (en) | 1993-03-15 |
NO923940L (no) | 1993-04-13 |
SK279381B6 (sk) | 1998-10-07 |
CZ308392A3 (en) | 1993-08-11 |
JPH05222077A (ja) | 1993-08-31 |
AU656811B2 (en) | 1995-02-16 |
CA2080253A1 (en) | 1993-04-12 |
RU2073004C1 (ru) | 1997-02-10 |
GR3024767T3 (en) | 1997-12-31 |
MX9205816A (es) | 1993-07-01 |
AU2626992A (en) | 1993-04-22 |
ES2104841T3 (es) | 1997-10-16 |
HUT62196A (en) | 1993-04-28 |
SK308392A3 (en) | 1995-02-08 |
EP0539057B1 (en) | 1997-07-16 |
NZ244587A (en) | 1994-04-27 |
IL103330A (en) | 1996-10-31 |
NO923940D0 (no) | 1992-10-09 |
NO300690B1 (no) | 1997-07-07 |
FI924570A0 (fi) | 1992-10-09 |
DE69220879D1 (de) | 1997-08-21 |
DK0539057T3 (da) | 1998-02-09 |
HU9203203D0 (en) | 1992-12-28 |
SG47768A1 (en) | 1998-04-17 |
US5124319A (en) | 1992-06-23 |
HU211942A9 (en) | 1996-01-29 |
DE69220879T2 (de) | 1997-11-20 |
EP0539057A1 (en) | 1993-04-28 |
FI924570A (fi) | 1993-04-12 |
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