ES2116290T3 - 2(5h)-furanonas sustituidas en posicion 3, como antagonistas del canal del ca2+ y agentes anti-inflamatorios. - Google Patents
2(5h)-furanonas sustituidas en posicion 3, como antagonistas del canal del ca2+ y agentes anti-inflamatorios.Info
- Publication number
- ES2116290T3 ES2116290T3 ES91907515T ES91907515T ES2116290T3 ES 2116290 T3 ES2116290 T3 ES 2116290T3 ES 91907515 T ES91907515 T ES 91907515T ES 91907515 T ES91907515 T ES 91907515T ES 2116290 T3 ES2116290 T3 ES 2116290T3
- Authority
- ES
- Spain
- Prior art keywords
- substituted
- arylalkyl
- alkyl
- inflammatory agents
- aryl
- 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
- 239000005557 antagonist Substances 0.000 title abstract 2
- 229940121363 anti-inflammatory agent Drugs 0.000 title abstract 2
- 239000002260 anti-inflammatory agent Substances 0.000 title abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 102100037611 Lysophospholipase Human genes 0.000 abstract 1
- 108010058864 Phospholipases A2 Proteins 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D307/58—One oxygen atom, e.g. butenolide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
SE PRESENTAN COMPUESTOS DE LA FORMULA (I) EN LA QUE R ES ALQUIL, ARALQUIL O ARILALQUIL SUBSTITUIDO, O ALQUENIL QUE CONTIENE UNO O MAS ENLACES OLEFINICOS; X ES O, NH O NR1, DONDE R1 ES ALQUIL DE ENTRE 1 Y 20 ATOMOS DE CARBONO O ARALQUIL; E Y ES H, ALQUIL DE ENTRE 1 Y 20 ATOMOS DE CARBONO, ARALQUIL, ARIL, ARIL SUBSTITUIDO, ARILALQUIL SUBSTITUIDO, ALQUENIL CONTENIENDO UNO O MAS ENLACES OLEFINICOS, PO(0H)2, PO(OH)OR2, PO(OH)R2, PO(OR2)2, DONDE R2 ES INDEPENDIENTEMENTE ALQUIL DE ENTRE 1 Y 20N ATOMOS DE CARBONO, FENIL O FENIL SUBSTITUIDO, ADEMAS Y ES CO-R3, CO-OR3, CONHR3, SO2R3, SO2NHR3, (CH2)-O-R3, O (CH2)N-O-(CH2)M-OR3, DONDE N, Y M, SON ENTEROS Y VALEN INDEPENDIENTEMENTE ENTRE 1 Y 20 Y R3 ES H, ALQUIL, ALQUENIL CONTENIENDO UNO O MAS ENLACES OLEFINICOS, ARIL, ARIL SUBSTITUIDO, ARILALQUIL O ARILALQUIL SUBSTITUIDO, CON LA CONDICION DE QUE CUANDO Y SEA CO-R3, CO-OR3 Y CONHR3, ENTONCES R3 NO SERA HIDROGENO. LOS COMPUESTOS SON ANTAGONISTAS DEL CANAL CA2+, TIENEN POCA O NINGUNA ACTIVIDAD COMO INHIBIDORES DE LA FOSFOLIPASA A2, Y SON AGENTES ANTIINFLAMATORIOS.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/510,367 US5043457A (en) | 1990-04-17 | 1990-04-17 | 2(5H)-furanones substituted in the 3 position, as Ca2+ channel antagonists and anti-inflammatory agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2116290T3 true ES2116290T3 (es) | 1998-07-16 |
Family
ID=24030459
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES91907515T Expired - Lifetime ES2116290T3 (es) | 1990-04-17 | 1991-03-25 | 2(5h)-furanonas sustituidas en posicion 3, como antagonistas del canal del ca2+ y agentes anti-inflamatorios. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US5043457A (es) |
| EP (1) | EP0525002B1 (es) |
| JP (1) | JPH05506024A (es) |
| AT (1) | ATE165972T1 (es) |
| CA (1) | CA2078770A1 (es) |
| DE (1) | DE69129408T2 (es) |
| ES (1) | ES2116290T3 (es) |
| IE (1) | IE911266A1 (es) |
| WO (1) | WO1991016048A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5134128A (en) * | 1987-06-08 | 1992-07-28 | Allergan, Inc. | Anti-inflammatory furanones |
| US5089485A (en) * | 1988-11-18 | 1992-02-18 | Allergan, Inc. | Anti-inflammatory furanones |
| US5171863A (en) * | 1987-06-08 | 1992-12-15 | Allergan, Inc. | Intermediates for preparing 4-substituted 2-5(H)-furanones as anti-inflammatory agents |
| US5045564A (en) * | 1988-12-07 | 1991-09-03 | Allergan, Inc. | Anti-inflammatory 2-furanones |
| US5258400A (en) * | 1989-11-20 | 1993-11-02 | Allergan, Inc. | Anti-inflammatory furanone compounds |
| US5112853A (en) * | 1989-11-20 | 1992-05-12 | Allergan, Inc. | Anti-inflammatory furanone compounds |
| US5225571A (en) * | 1991-04-30 | 1993-07-06 | Allergan, Inc. | Substituted dihydroxy-bis-[5-hydroxy-2(5H)-furanone-4-yl]-alkanes as anti-inflammatory agents |
| US5183906A (en) * | 1991-04-30 | 1993-02-02 | Allergan, Inc. | 2- and 5-alkyl and phenyl substituted 4-(1-hydroxy, 1-acyloxy or 1-carbamoyloxy)-5-hydroxy-2 (5h)-furanones as anti-inflammatory agents |
| US5169963A (en) * | 1991-08-30 | 1992-12-08 | Allergan, Inc. | Di-(5-hydroxy-2(5H)2-oxo-4-furyl)alkylmethyl-alpha,omega alkanedioates and N,N-bis-(5-hydroxy-2(5H)2-oxo-4-furyl)alkylmethyl-alpha,omega-dialkanoic acid amides as anti-inflammatory agents |
| US5171864A (en) * | 1991-08-30 | 1992-12-15 | Allergan, Inc. | Di-(5-hydroxy-2(5H)-2-oxo-4-furyl)methyl-alpha,omega alkane-dioates and N,N-bis-(5-hydroxy-2(5H)-2-oxo-4-furyl)methyl-alpha,omega-dialkanoic acid amides as anti-inflammatory agents |
| US5268387A (en) * | 1992-04-24 | 1993-12-07 | Allergan, Inc. | Pharmaceutical compositions and method for administering 3 and 4-substituted 2(5H)-furanones to a mammal for inhibiting bone loss |
| US5451686A (en) * | 1994-04-15 | 1995-09-19 | Allergan, Inc. | 3 and 5 alkyl and phenyl 4-(hydroxy or acyloxy)-alkyl substituted 2(5H)-furanones as anti-inflammatory agents |
| JP4202250B2 (ja) | 2001-07-25 | 2008-12-24 | バイオマリン ファーマシューティカル インコーポレイテッド | 血液脳関門輸送を調節するための組成物および方法 |
| DE60326482D1 (de) * | 2002-10-10 | 2009-04-16 | Merck & Co Inc | Testverfahren für zustandsabhängige calciumkanal-agonisten/-antagonisten |
| EP3827747A1 (en) | 2005-04-28 | 2021-06-02 | Otsuka Pharmaceutical Co., Ltd. | Pharma-informatics system |
| CN101594878A (zh) | 2006-09-18 | 2009-12-02 | 雷普特药品公司 | 通过给予受体相关蛋白(rap)-缀合物对肝病症的治疗 |
| DK3395372T3 (da) | 2009-02-20 | 2022-04-19 | Enhanx Biopharm Inc | System til afgivelse af glutathion-baseret medikament |
| CN110075069A (zh) | 2009-05-06 | 2019-08-02 | 实验室护肤股份有限公司 | 包含活性剂-磷酸钙颗粒复合物的皮肤递送组合物及其应用 |
| US20120077778A1 (en) | 2010-09-29 | 2012-03-29 | Andrea Bourdelais | Ladder-Frame Polyether Conjugates |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2359208A (en) * | 1941-03-21 | 1944-09-26 | Lilly Co Eli | beta-substituted-delta alpha,beta-gamma-butyrolactones and beta-substituted-beta-hydroxy-gamma-butyrolactones and the methods of preparing them |
| US2359096A (en) * | 1941-03-21 | 1944-09-26 | Lilly Co Eli | beta-substituted-delta alpha, beta-gamma-butyrolactones and beta-substituted - beta - hydroxy-gamma-butyrolactones and methods of preparing them |
| US4447455A (en) * | 1980-12-01 | 1984-05-08 | Madaus And Company | Oral urolithiasis remedy |
| US4616089A (en) * | 1983-08-03 | 1986-10-07 | University Of California | Synthetic anti-inflammatory derivatives of manoalide |
| DE3472958D1 (en) * | 1983-08-03 | 1988-09-01 | Univ California | Synthetic analgesic and/or anti-inflammatory derivatives of manoalide |
| JPS6058973A (ja) * | 1983-09-13 | 1985-04-05 | Mitsubishi Yuka Yakuhin Kk | γ−プチロラクトン誘導体及びそれを有効成分とする免疫調節剤 |
| US4789749A (en) * | 1984-06-18 | 1988-12-06 | The Regents Of The University Of California | Manoalide analogs |
| ZA864674B (en) * | 1985-07-01 | 1988-02-24 | Lilly Co Eli | Furanone derivatives |
| US4786651A (en) * | 1986-02-03 | 1988-11-22 | Allergan, Inc. | Treatment of cutaneous hyperproliferative dermatoses with manoalide |
| DE3615157A1 (de) * | 1986-05-05 | 1987-11-12 | Schwabe Willmar Gmbh & Co | 5-arylalkyl-4-alkoxy-2(5h)-furanone, zwischenprodukte und verfahren zu ihrer herstellung sowie ihre anwendung als therapeutische wirkstoffe |
| CA1329390C (en) * | 1987-06-08 | 1994-05-10 | John N. Bonfiglio | Anti-inflammatory furanones |
| US4916241A (en) * | 1988-06-06 | 1990-04-10 | American Home Products Corporation | Inhibition of bone loss by 4-substituted-5-hydroxy-2(5H)-furanones |
| US4935530A (en) * | 1988-10-18 | 1990-06-19 | Allergan, Inc. | Process for preparing 5-substituted-3-furaldehydes |
| US4957917A (en) * | 1989-10-25 | 1990-09-18 | Allergan, Inc. | Anti-inflammatory furanones |
| US5013850A (en) * | 1990-03-30 | 1991-05-07 | Allergan, Inc. | 4-ethyl and 4-ethenyl-5-hydroxy-2(5H)-furanones substituted on alpha carbon of the ethyl or ethenyl side chain with a long chain alkyl group and on the beta carbon with a polar group, as anti-inflammatory agents |
-
1990
- 1990-04-17 US US07/510,367 patent/US5043457A/en not_active Expired - Fee Related
-
1991
- 1991-03-25 CA CA002078770A patent/CA2078770A1/en not_active Abandoned
- 1991-03-25 DE DE69129408T patent/DE69129408T2/de not_active Expired - Fee Related
- 1991-03-25 JP JP91507355A patent/JPH05506024A/ja active Pending
- 1991-03-25 WO PCT/US1991/002006 patent/WO1991016048A1/en not_active Ceased
- 1991-03-25 EP EP91907515A patent/EP0525002B1/en not_active Expired - Lifetime
- 1991-03-25 ES ES91907515T patent/ES2116290T3/es not_active Expired - Lifetime
- 1991-03-25 AT AT91907515T patent/ATE165972T1/de active
- 1991-04-16 IE IE126691A patent/IE911266A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0525002A4 (en) | 1993-03-10 |
| EP0525002B1 (en) | 1998-05-13 |
| DE69129408D1 (de) | 1998-06-18 |
| JPH05506024A (ja) | 1993-09-02 |
| CA2078770A1 (en) | 1991-10-18 |
| DE69129408T2 (de) | 1998-09-03 |
| EP0525002A1 (en) | 1993-02-03 |
| WO1991016048A1 (en) | 1991-10-31 |
| IE911266A1 (en) | 1991-10-23 |
| ATE165972T1 (de) | 1998-05-15 |
| US5043457A (en) | 1991-08-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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