ES2177627T3 - Esteres aminoalcanoicos de rapamicina. - Google Patents
Esteres aminoalcanoicos de rapamicina.Info
- Publication number
- ES2177627T3 ES2177627T3 ES95906728T ES95906728T ES2177627T3 ES 2177627 T3 ES2177627 T3 ES 2177627T3 ES 95906728 T ES95906728 T ES 95906728T ES 95906728 T ES95906728 T ES 95906728T ES 2177627 T3 ES2177627 T3 ES 2177627T3
- Authority
- ES
- Spain
- Prior art keywords
- hydrogen
- arylalkyl
- alkyl
- image
- aminoalcanoic
- 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
- 150000002148 esters Chemical class 0.000 title 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 title 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 title 1
- 229960002930 sirolimus Drugs 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- -1 fluorenylmethyl Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 230000000843 anti-fungal effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 229940121375 antifungal agent Drugs 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Transplantation (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
LA INVENCION SUMINISTRA UN COMPUESTO DE LA ESTRUCTURA (I) EN LA QUE R1 Y R2 SON CADA UNA, INDEPENDIENTEMENTE, HIDROGENO O (1); R3 ES - CH{SUB, 2}{SUB, Q}CO{SUB, 2}R6; R4 ES HIDROGENO, ALQUILO, O ARILALQUILO; R5 ES HIDROGENO O COOR7; R6 ES HIDROGENO, ALQUILO, ALQUENILO, ARILALQUILO, FLUORENILMETILO, O FENILO QUE ESTA OPCIONALMENTE SUSTITUIDO; R7 ES ALQUILO, ALQUENILO, ARILALQUILO, FLUORENILMETILO, O FENILO QUE ESTA OPCIONALMENTE SUSTITUIDO; M Y N SON INDEPENDIENTES EN CADA UNA DE LAS SUBUNIDADES (2) CUANDO P = 2; CON LA CONDICION DE QUE R1 Y R2 NO SEAN AMBAS HIDROGENO; Y CON LA CONDICION ADICIONAL DE QUE SI R5 ES CO{SUB, 2}R7, ENTONCES R6 ES HIDROGENO; Y TENIENDO EN CUENTA ADEMAS QUE SI R6 NO ES HIDROGENO, ENTONCES R5 ES HIDROGENO; TAMBIEN SE PRESENTAN LAS SALES FARMACOLOGICAMENTE ACEPTABLES DEL COMPUESTO QUE SON UTILES COMO AGENTES INMUNOSUPRESORES, ANTIIFLAMATORIOS, ANTIFUNGALES, ANTIPROLIFERATIVOS Y ANTITUMORALES.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/174,120 US5389639A (en) | 1993-12-29 | 1993-12-29 | Amino alkanoic esters of rapamycin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2177627T3 true ES2177627T3 (es) | 2002-12-16 |
Family
ID=22634919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES95906728T Expired - Lifetime ES2177627T3 (es) | 1993-12-29 | 1994-12-28 | Esteres aminoalcanoicos de rapamicina. |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US5389639A (es) |
| EP (1) | EP0737197B1 (es) |
| JP (1) | JPH09507236A (es) |
| KR (1) | KR100338582B1 (es) |
| AT (1) | ATE217312T1 (es) |
| AU (1) | AU1519895A (es) |
| CA (1) | CA2179307A1 (es) |
| DE (1) | DE69430586T2 (es) |
| DK (1) | DK0737197T3 (es) |
| ES (1) | ES2177627T3 (es) |
| PT (1) | PT737197E (es) |
| SG (1) | SG47843A1 (es) |
| WO (1) | WO1995018133A1 (es) |
Families Citing this family (92)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US5780462A (en) * | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| US5922730A (en) * | 1996-09-09 | 1999-07-13 | American Home Products Corporation | Alkylated rapamycin derivatives |
| US6015809A (en) * | 1998-08-17 | 2000-01-18 | American Home Products Corporation | Photocyclized rapamycin |
| US6331547B1 (en) | 1999-08-18 | 2001-12-18 | American Home Products Corporation | Water soluble SDZ RAD esters |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| US8236048B2 (en) | 2000-05-12 | 2012-08-07 | Cordis Corporation | Drug/drug delivery systems for the prevention and treatment of vascular disease |
| US20050002986A1 (en) * | 2000-05-12 | 2005-01-06 | Robert Falotico | Drug/drug delivery systems for the prevention and treatment of vascular disease |
| US6670355B2 (en) | 2000-06-16 | 2003-12-30 | Wyeth | Method of treating cardiovascular disease |
| JP2004507465A (ja) | 2000-08-11 | 2004-03-11 | ワイス | エストロゲン受容体陽性癌腫の治療方法 |
| ATE411321T1 (de) | 2000-09-19 | 2008-10-15 | Wyeth Corp | Wasserlösliche rapamycin-ester |
| US6399625B1 (en) | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
| CA2424029C (en) * | 2000-09-29 | 2008-01-29 | Cordis Corporation | Coated medical devices |
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| US6440991B1 (en) | 2000-10-02 | 2002-08-27 | Wyeth | Ethers of 7-desmethlrapamycin |
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| US5194447A (en) * | 1992-02-18 | 1993-03-16 | American Home Products Corporation | Sulfonylcarbamates of rapamycin |
| US5091389A (en) * | 1991-04-23 | 1992-02-25 | Merck & Co., Inc. | Lipophilic macrolide useful as an immunosuppressant |
| US5138051A (en) * | 1991-08-07 | 1992-08-11 | American Home Products Corporation | Rapamycin analogs as immunosuppressants and antifungals |
| US5102876A (en) * | 1991-05-07 | 1992-04-07 | American Home Products Corporation | Reduction products of rapamycin |
| US5118677A (en) * | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| US5169851A (en) * | 1991-08-07 | 1992-12-08 | American Home Products Corporation | Rapamycin analog as immunosuppressants and antifungals |
| US5286731A (en) * | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory bowel disease |
| US5286730A (en) * | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory disease |
| US5151413A (en) * | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| US5177203A (en) * | 1992-03-05 | 1993-01-05 | American Home Products Corporation | Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents |
-
1993
- 1993-12-29 US US08/174,120 patent/US5389639A/en not_active Expired - Lifetime
-
1994
- 1994-12-28 KR KR1019960703482A patent/KR100338582B1/ko not_active Expired - Fee Related
- 1994-12-28 CA CA002179307A patent/CA2179307A1/en not_active Abandoned
- 1994-12-28 WO PCT/US1994/014960 patent/WO1995018133A1/en not_active Ceased
- 1994-12-28 JP JP7518187A patent/JPH09507236A/ja not_active Withdrawn
- 1994-12-28 ES ES95906728T patent/ES2177627T3/es not_active Expired - Lifetime
- 1994-12-28 PT PT95906728T patent/PT737197E/pt unknown
- 1994-12-28 AT AT95906728T patent/ATE217312T1/de not_active IP Right Cessation
- 1994-12-28 AU AU15198/95A patent/AU1519895A/en not_active Abandoned
- 1994-12-28 DE DE69430586T patent/DE69430586T2/de not_active Expired - Fee Related
- 1994-12-28 SG SG1996004668A patent/SG47843A1/en unknown
- 1994-12-28 DK DK95906728T patent/DK0737197T3/da active
- 1994-12-28 EP EP95906728A patent/EP0737197B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| US5389639A (en) | 1995-02-14 |
| DE69430586T2 (de) | 2002-11-21 |
| WO1995018133A1 (en) | 1995-07-06 |
| SG47843A1 (en) | 1998-04-17 |
| AU1519895A (en) | 1995-07-17 |
| DK0737197T3 (da) | 2002-08-26 |
| PT737197E (pt) | 2002-09-30 |
| DE69430586D1 (de) | 2002-06-13 |
| KR100338582B1 (ko) | 2002-10-12 |
| ATE217312T1 (de) | 2002-05-15 |
| CA2179307A1 (en) | 1995-07-06 |
| EP0737197B1 (en) | 2002-05-08 |
| JPH09507236A (ja) | 1997-07-22 |
| EP0737197A1 (en) | 1996-10-16 |
| HK1011355A1 (en) | 1999-07-09 |
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