NO20084390L - Substituerte naftylindol-derivater som inhibitorer av plasminogen-aktivatorinhibitor type-1 (PAI-1) - Google Patents
Substituerte naftylindol-derivater som inhibitorer av plasminogen-aktivatorinhibitor type-1 (PAI-1)Info
- Publication number
- NO20084390L NO20084390L NO20084390A NO20084390A NO20084390L NO 20084390 L NO20084390 L NO 20084390L NO 20084390 A NO20084390 A NO 20084390A NO 20084390 A NO20084390 A NO 20084390A NO 20084390 L NO20084390 L NO 20084390L
- Authority
- NO
- Norway
- Prior art keywords
- optionally substituted
- alkyl
- alkanoyl
- pai
- inhibitors
- Prior art date
Links
- XEQHAEZWPZICKJ-UHFFFAOYSA-N 2-naphthalen-1-yl-1h-indole Chemical class C1=CC=C2C(C3=CC4=CC=CC=C4N3)=CC=CC2=C1 XEQHAEZWPZICKJ-UHFFFAOYSA-N 0.000 title 1
- 102000010752 Plasminogen Inactivators Human genes 0.000 title 1
- 108010077971 Plasminogen Inactivators Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000002797 plasminogen activator inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000001589 carboacyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 3
- 229920001774 Perfluoroether Polymers 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 125000003435 aroyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 229910018828 PO3H2 Inorganic materials 0.000 abstract 1
- 102000012335 Plasminogen Activator Inhibitor 1 Human genes 0.000 abstract 1
- 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 abstract 1
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- PGRHXDWITVMQBC-UHFFFAOYSA-N dehydroacetic acid Natural products CC(=O)C1C(=O)OC(C)=CC1=O PGRHXDWITVMQBC-UHFFFAOYSA-N 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000003278 mimic effect Effects 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- PEQJBOMPGWYIRO-UHFFFAOYSA-N n-ethyl-3,4-dimethoxyaniline Chemical compound CCNC1=CC=C(OC)C(OC)=C1 PEQJBOMPGWYIRO-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
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- 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
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- 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
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Emergency Medicine (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
Abstract
Foreliggende oppfinnelse tilveiebringer PAI-1-hemmende forbindelser med formel I: hvor: R1, R2, R3 og R4 hver er H, alkyl, alkanoyl, halogen, OH, aryl eventuelt substituert med R8, perfluoralkyl, alkoksy, amino, alkylamino, dialkylamino, perfluoralkoksy; R5 er H, alkyl, perfluoralkyl, aryl eventuelt substituert med R8, alkanoyl, aroyl eventuelt substituert med R8; R6 er H, alkyl, alkylaryl, benzyl eventuelt substituert med R8, alkanoyl, aroyl eventuelt substituert med R8; R7 er H, alkyl, alkylaryl, aryl eventuelt substituert med R8; n er 0-6; A er COOH eller en syre-etterligner så som tetraazol, SO3H, PO3H2, tetronsyre, etc.; R8 er H, alkyl, cykloalkyl, alkanoyl, halogen, OH, perfluoralkyl, alkoksy, amino, alkylamino, dialkylamino, perfluoralkoksy;, eller et farmasøytisk akseptabelt salt derav; så vel som farmasøytiske preparater og fremgangsmåter for behandling ved anvendelse av disse forbindelser.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29965101P | 2001-06-20 | 2001-06-20 | |
| PCT/US2002/021113 WO2003000684A1 (en) | 2001-06-20 | 2002-06-18 | Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (pai-1) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NO20084390L true NO20084390L (no) | 2003-12-17 |
Family
ID=23155676
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20035635A NO326316B1 (no) | 2001-06-20 | 2003-12-17 | Substituerte naftylindol-derivater, fremgangsmate for fremstilling av disse, farmasoytiske preparater inneholdende slike forbindelser samt anvendelse av slike forbindelser for fremstilling av medikament for behandling av sykdom. |
| NO20084390A NO20084390L (no) | 2001-06-20 | 2008-10-20 | Substituerte naftylindol-derivater som inhibitorer av plasminogen-aktivatorinhibitor type-1 (PAI-1) |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20035635A NO326316B1 (no) | 2001-06-20 | 2003-12-17 | Substituerte naftylindol-derivater, fremgangsmate for fremstilling av disse, farmasoytiske preparater inneholdende slike forbindelser samt anvendelse av slike forbindelser for fremstilling av medikament for behandling av sykdom. |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US6800654B2 (no) |
| EP (1) | EP1397356B1 (no) |
| JP (1) | JP4520144B2 (no) |
| KR (1) | KR20040007744A (no) |
| CN (1) | CN1280288C (no) |
| AR (1) | AR036101A1 (no) |
| AT (1) | ATE431346T1 (no) |
| AU (1) | AU2002316533B2 (no) |
| BR (1) | BR0210504A (no) |
| CA (1) | CA2448798C (no) |
| CO (1) | CO5540286A2 (no) |
| DE (1) | DE60232328D1 (no) |
| EA (1) | EA009696B1 (no) |
| EC (1) | ECSP034904A (no) |
| ES (1) | ES2325733T3 (no) |
| HU (1) | HUP0400233A3 (no) |
| IL (1) | IL159449A0 (no) |
| MX (1) | MXPA03011522A (no) |
| NO (2) | NO326316B1 (no) |
| NZ (1) | NZ530312A (no) |
| PL (1) | PL367525A1 (no) |
| TW (1) | TWI224101B (no) |
| UA (1) | UA78708C2 (no) |
| WO (1) | WO2003000684A1 (no) |
| ZA (1) | ZA200400380B (no) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI224101B (en) * | 2001-06-20 | 2004-11-21 | Wyeth Corp | Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) |
| DE60221391T2 (de) * | 2001-06-20 | 2008-04-17 | Wyeth | Substituierte indolsäurederivate als inhibitoren von plasminogen-aktivator-inhibitor-1 (pai-1) |
| US7291639B2 (en) * | 2001-06-20 | 2007-11-06 | Wyeth | Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) |
| CN1726191A (zh) * | 2002-12-10 | 2006-01-25 | 惠氏公司 | 用作纤溶酶原激活物抑制剂－1(pai－1)的抑制剂的取代的吲哚氧代－乙酰氨基乙酸衍生物 |
| UA80453C2 (en) * | 2002-12-10 | 2007-09-25 | Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1) | |
| ES2266907T3 (es) * | 2002-12-10 | 2007-03-01 | Wyeth | Derivados sustituidos del acido 3-carbonil-indol-1-il-acetico como inhibidor del activador del plasminogeno-1 (pal-1). |
| ATE331708T1 (de) * | 2002-12-10 | 2006-07-15 | Wyeth Corp | Substituierte 3-alkyl- und 3-arylalkyl-1h-indol-1-yl-essigsäure-derivate als plasminogen aktivator inhibitor-1 (pai-1) inhibitoren |
| WO2004052854A2 (en) * | 2002-12-10 | 2004-06-24 | Wyeth | Aryl, aryloxy, and alkyloxy substituted 1h-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1) |
| JP4390460B2 (ja) * | 2003-02-21 | 2009-12-24 | 株式会社静岡カフェイン工業所 | オキサゾール誘導体 |
| US7268159B2 (en) * | 2003-09-25 | 2007-09-11 | Wyeth | Substituted indoles |
| US7342039B2 (en) * | 2003-09-25 | 2008-03-11 | Wyeth | Substituted indole oximes |
| US7163954B2 (en) * | 2003-09-25 | 2007-01-16 | Wyeth | Substituted naphthyl benzothiophene acids |
| US7446201B2 (en) * | 2003-09-25 | 2008-11-04 | Wyeth | Substituted heteroaryl benzofuran acids |
| US7141592B2 (en) * | 2003-09-25 | 2006-11-28 | Wyeth | Substituted oxadiazolidinediones |
| US7582773B2 (en) * | 2003-09-25 | 2009-09-01 | Wyeth | Substituted phenyl indoles |
| US7351726B2 (en) * | 2003-09-25 | 2008-04-01 | Wyeth | Substituted oxadiazolidinediones |
| US7411083B2 (en) * | 2003-09-25 | 2008-08-12 | Wyeth | Substituted acetic acid derivatives |
| US7534894B2 (en) * | 2003-09-25 | 2009-05-19 | Wyeth | Biphenyloxy-acids |
| US7265148B2 (en) * | 2003-09-25 | 2007-09-04 | Wyeth | Substituted pyrrole-indoles |
| US7332521B2 (en) * | 2003-09-25 | 2008-02-19 | Wyeth | Substituted indoles |
| US7442805B2 (en) * | 2003-09-25 | 2008-10-28 | Wyeth | Substituted sulfonamide-indoles |
| US7420083B2 (en) * | 2003-09-25 | 2008-09-02 | Wyeth | Substituted aryloximes |
| US7115815B2 (en) * | 2003-10-31 | 2006-10-03 | Adc Telecommunications, Inc. | Cable utilizing varying lay length mechanisms to minimize alien crosstalk |
| CA2577782A1 (en) * | 2004-08-23 | 2006-03-02 | Wyeth | Pyrrolo-naphthyl acids as pai-1 inhibitors |
| BRPI0514572A (pt) * | 2004-08-23 | 2008-06-17 | Wyeth Corp | ácidos de tiazolo-naftila |
| KR20070055563A (ko) * | 2004-08-23 | 2007-05-30 | 와이어쓰 | 혈전증 및 심혈관 질병의 치료에 유용한 플라스미노겐활성화제 억제제 타입-1(ｐａｉ-1)의 조절제로서의옥사졸로-나프틸 산 |
| RU2007121255A (ru) * | 2005-01-27 | 2009-03-10 | Вайет (Us) | Способы и соединения для получения замещенных производных нафтилиндола |
| JP2009504762A (ja) * | 2005-08-17 | 2009-02-05 | ワイス | 置換インドール類およびそれらの使用方法 |
| JP2009528290A (ja) * | 2006-02-27 | 2009-08-06 | ワイス | 筋肉病の処置のためのｐａｉ−１阻害剤 |
| AU2007307599A1 (en) | 2006-10-12 | 2008-04-17 | Institute Of Medicinal Molecular Design. Inc. | N-phenyloxamic acid derivatives |
| WO2008044729A1 (fr) | 2006-10-12 | 2008-04-17 | Institute Of Medicinal Molecular Design. Inc. | Dérivé d'acide carboxylique |
| US8759327B2 (en) | 2007-04-16 | 2014-06-24 | The Regents Of The University Of Michigan | Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism |
| US9120744B2 (en) | 2007-04-16 | 2015-09-01 | The Regents Of The University Of Michigan | Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism |
| JP5213855B2 (ja) | 2007-06-27 | 2013-06-19 | 興和株式会社 | ピラゾロン誘導体 |
| BRPI0816560A2 (pt) | 2007-10-23 | 2015-09-01 | Inst Med Molecular Design Inc | Método de inibição de produção de pai-1 método para prevenção ou melhora de uma doença causada por uma super-produção de pai-1" |
| CA2720096A1 (en) | 2008-04-11 | 2009-10-15 | Institute Of Medicinal Molecular Design, Inc. | Pai-1 inhibitor |
| US8633245B2 (en) * | 2008-04-11 | 2014-01-21 | Institute Of Medicinal Molecular Design, Inc. | PAI-1 inhibitor |
| US9718760B2 (en) | 2012-10-31 | 2017-08-01 | The Regents Of The University Of Michigan | Plasminogen activator inhibitor-1 inhibitors and methods of use thereof |
| CN106890324A (zh) * | 2015-12-18 | 2017-06-27 | 深圳瑞健生命科学研究院有限公司 | 一种预防和治疗糖尿病肾病的方法 |
| CN108778307A (zh) | 2015-12-18 | 2018-11-09 | 泰伦基国际有限公司 | 一种预防和治疗糖尿病肾病的方法 |
| JP7171572B2 (ja) | 2016-12-15 | 2022-11-15 | タレンゲン インターナショナル リミテッド | 糖尿病を治療するための新しい方法 |
| CA3070303A1 (en) | 2017-07-27 | 2019-01-31 | The Regents Of The University Of Michigan | Plasminogen activator inhibitor-1 (pai-1) inhibitor and method of use |
| CN114057623B (zh) * | 2021-12-07 | 2023-07-21 | 湖南第一师范学院 | 一种n-萘基吲哚衍生物及其合成方法 |
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