KR940004072B1 - 라파마이신 전구체의 제조방법 - Google Patents
라파마이신 전구체의 제조방법 Download PDFInfo
- Publication number
- KR940004072B1 KR940004072B1 KR1019860010339A KR860010339A KR940004072B1 KR 940004072 B1 KR940004072 B1 KR 940004072B1 KR 1019860010339 A KR1019860010339 A KR 1019860010339A KR 860010339 A KR860010339 A KR 860010339A KR 940004072 B1 KR940004072 B1 KR 940004072B1
- Authority
- KR
- South Korea
- Prior art keywords
- rapamycin
- acid
- precursor
- carbon atoms
- acylating agent
- 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 - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US806152 | 1985-12-06 | ||
| US06/806,152 US4650803A (en) | 1985-12-06 | 1985-12-06 | Prodrugs of rapamycin |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019910022103A Division KR940004073B1 (ko) | 1985-12-06 | 1991-12-04 | 라파마이신 전구체의 제조방법 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR870006072A KR870006072A (ko) | 1987-07-09 |
| KR940004072B1 true KR940004072B1 (ko) | 1994-05-11 |
Family
ID=25193443
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019860010339A Expired - Fee Related KR940004072B1 (ko) | 1985-12-06 | 1986-12-04 | 라파마이신 전구체의 제조방법 |
| KR1019910022103A Expired - Fee Related KR940004073B1 (ko) | 1985-12-06 | 1991-12-04 | 라파마이신 전구체의 제조방법 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019910022103A Expired - Fee Related KR940004073B1 (ko) | 1985-12-06 | 1991-12-04 | 라파마이신 전구체의 제조방법 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US4650803A (enExample) |
| EP (1) | EP0227355B1 (enExample) |
| JP (2) | JPH0670066B2 (enExample) |
| KR (2) | KR940004072B1 (enExample) |
| AT (1) | ATE74134T1 (enExample) |
| AU (1) | AU583439B2 (enExample) |
| CA (2) | CA1273920A (enExample) |
| DE (1) | DE3684574D1 (enExample) |
| DK (2) | DK169409B1 (enExample) |
| ES (1) | ES2032750T3 (enExample) |
| GB (1) | GB2183647A (enExample) |
| GR (1) | GR3004530T3 (enExample) |
| HU (1) | HU198054B (enExample) |
| IE (1) | IE64506B1 (enExample) |
| PT (1) | PT83843B (enExample) |
| ZA (1) | ZA869181B (enExample) |
Families Citing this family (222)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2420367A (en) * | 1943-11-09 | 1947-05-13 | Celanese Corp | Fluffing up artificial staple fibers |
| US5206018A (en) * | 1978-11-03 | 1993-04-27 | Ayerst, Mckenna & Harrison, Inc. | Use of rapamycin in treatment of tumors |
| DK520482A (da) * | 1982-11-23 | 1984-05-24 | Jacobsen P E B | Sundhedsmadras |
| DK406686D0 (da) * | 1986-08-26 | 1986-08-26 | Hans Bundgaard | Carboxylsyrederivater |
| GB8728820D0 (en) * | 1987-12-09 | 1988-01-27 | Fisons Plc | Compounds |
| ES2071681T3 (es) * | 1987-12-09 | 1995-07-01 | Fisons Plc | Compuestos macrociclicos. |
| EP0378318A1 (en) * | 1989-01-11 | 1990-07-18 | Merck & Co. Inc. | Process for synthesis of FK-506 and tricarbonyl intermediates |
| US4960790A (en) * | 1989-03-09 | 1990-10-02 | University Of Kansas | Derivatives of taxol, pharmaceutical compositions thereof and methods for the preparation thereof |
| US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
| DE69021833T2 (de) * | 1989-11-09 | 1996-03-21 | Sandoz Ag | Heteroatome enthaltende tricyclische Verbindungen. |
| US5352671A (en) * | 1989-11-09 | 1994-10-04 | Sandoz Ltd. | Heteroatoms-containing tricyclic compounds |
| US5208228A (en) * | 1989-11-13 | 1993-05-04 | Merck & Co., Inc. | Aminomacrolides and derivatives having immunosuppressive activity |
| US5120726A (en) * | 1991-03-08 | 1992-06-09 | American Home Products Corporation | Rapamycin hydrazones |
| US5023264A (en) * | 1990-07-16 | 1991-06-11 | American Home Products Corporation | Rapamycin oximes |
| JPH04230389A (ja) * | 1990-07-16 | 1992-08-19 | American Home Prod Corp | ラパマイシン誘導体 |
| US5023263A (en) * | 1990-08-09 | 1991-06-11 | American Home Products Corporation | 42-oxorapamycin |
| US5023262A (en) * | 1990-08-14 | 1991-06-11 | American Home Products Corporation | Hydrogenated rapamycin derivatives |
| PT98990A (pt) * | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5358944A (en) * | 1990-09-19 | 1994-10-25 | American Home Products Corporation | Rapamycin esters for treating transplantation rejection |
| US5378696A (en) * | 1990-09-19 | 1995-01-03 | American Home Products Corporation | Rapamycin esters |
| US5221670A (en) * | 1990-09-19 | 1993-06-22 | American Home Products Corporation | Rapamycin esters |
| US5130307A (en) * | 1990-09-28 | 1992-07-14 | American Home Products Corporation | Aminoesters of rapamycin |
| US5143918A (en) * | 1990-10-11 | 1992-09-01 | Merck & Co., Inc. | Halomacrolides and derivatives having immunosuppressive activity |
| US5233036A (en) * | 1990-10-16 | 1993-08-03 | American Home Products Corporation | Rapamycin alkoxyesters |
| US5120842A (en) * | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) * | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5194447A (en) * | 1992-02-18 | 1993-03-16 | American Home Products Corporation | Sulfonylcarbamates of rapamycin |
| NO921449L (no) * | 1991-04-17 | 1992-10-19 | American Home Prod | Karbamater av rapamycin |
| US5118678A (en) * | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5147877A (en) * | 1991-04-18 | 1992-09-15 | Merck & Co. Inc. | Semi-synthetic immunosuppressive macrolides |
| 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 |
| US5162334A (en) * | 1991-05-13 | 1992-11-10 | Merck & Co., Inc. | Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosuppressive activity |
| US5565560A (en) * | 1991-05-13 | 1996-10-15 | Merck & Co., Inc. | O-Aryl,O-alkyl,O-alkenyl and O-alkynylmacrolides having immunosuppressive activity |
| US5776943A (en) * | 1991-05-14 | 1998-07-07 | American Home Products Corporation | Rapamycin metabolites |
| US5118677A (en) * | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| EP0516347A1 (en) * | 1991-05-29 | 1992-12-02 | American Home Products Corporation | Rapamycin derivatives |
| US5432183A (en) * | 1991-05-31 | 1995-07-11 | Pfizer Inc. | Use of rapamycin prodrugs as immunosuppressant agents |
| ZA924953B (en) * | 1991-07-25 | 1993-04-28 | Univ Louisville Res Found | Method of treating ocular inflammation |
| US5189042A (en) * | 1991-08-22 | 1993-02-23 | Merck & Co. Inc. | Fluoromacrolides having immunosuppressive activity |
| US5208241A (en) * | 1991-09-09 | 1993-05-04 | Merck & Co., Inc. | N-heteroaryl, n-alkylheteroaryl, n-alkenylheteroaryl and n-alkynylheteroarylmacrolides having immunosuppressive activity |
| US5162333A (en) * | 1991-09-11 | 1992-11-10 | American Home Products Corporation | Aminodiesters of rapamycin |
| US5151413A (en) * | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| US5164399A (en) * | 1991-11-18 | 1992-11-17 | American Home Products Corporation | Rapamycin pyrazoles |
| US5262424A (en) * | 1992-02-18 | 1993-11-16 | American Home Products Corporation | Composition of sulfonylcarbamates of rapamycin and method of treating diseases requiring immunosuppression therewith |
| WO1993018043A1 (en) * | 1992-03-05 | 1993-09-16 | American Home Products Corporation | Novel rapamycin 42-sulfonates and 42-(n-carboalkoxy)sulfamates useful as immunosuppressive agents |
| JP2741285B2 (ja) * | 1992-05-22 | 1998-04-15 | 千寿製薬株式会社 | 緑内障治療剤 |
| ZA935111B (en) * | 1992-07-17 | 1994-02-04 | Smithkline Beecham Corp | Rapamycin derivatives |
| US5256790A (en) * | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
| CA2106034A1 (en) * | 1992-09-24 | 1994-03-25 | Ralph J. Russo | 21-norrapamycin |
| US5302584A (en) * | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| US5480989A (en) * | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
| DK0593227T3 (da) * | 1992-10-13 | 2006-05-01 | Wyeth Corp | Carbamater af rapamycin |
| US5480988A (en) * | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5489680A (en) * | 1992-10-13 | 1996-02-06 | American Home Products Corporation | Carbamates of rapamycin |
| US5434260A (en) * | 1992-10-13 | 1995-07-18 | American Home Products Corporation | Carbamates of rapamycin |
| US5262423A (en) * | 1992-10-29 | 1993-11-16 | American Home Products Corporation | Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents |
| US5258389A (en) * | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| US5260300A (en) * | 1992-11-19 | 1993-11-09 | American Home Products Corporation | Rapamycin carbonate esters as immuno-suppressant agents |
| US5349060A (en) * | 1993-01-07 | 1994-09-20 | American Home Products Corporation | Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents |
| US5252579A (en) * | 1993-02-16 | 1993-10-12 | American Home Products Corporation | Macrocyclic immunomodulators |
| US5310901A (en) * | 1993-03-05 | 1994-05-10 | Merck & Co., Inc. | O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynlheteroarylrapamycin derivatives |
| US5310903A (en) * | 1993-03-05 | 1994-05-10 | Merck & Co., Inc. | Imidazolidyl rapamycin derivatives |
| USRE40596E1 (en) * | 1993-04-08 | 2008-12-02 | Novartis Ag | Rapamycin assay |
| GB9307491D0 (en) | 1993-04-08 | 1993-06-02 | Sandoz Ltd | Organic compounds |
| US5504091A (en) * | 1993-04-23 | 1996-04-02 | American Home Products Corporation | Biotin esters of rapamycin |
| US7279561B1 (en) | 1993-04-23 | 2007-10-09 | Wyeth | Anti-rapamycin monoclonal antibodies |
| EP1181938B1 (en) | 1993-04-23 | 2007-11-14 | Wyeth | Rapamycin conjugates and antibodies |
| USRE37421E1 (en) | 1993-07-16 | 2001-10-23 | Smithkline Beecham Corporation | Rapamycin derivatives |
| US5387680A (en) * | 1993-08-10 | 1995-02-07 | American Home Products Corporation | C-22 ring stabilized rapamycin derivatives |
| US5373014A (en) * | 1993-10-08 | 1994-12-13 | American Home Products Corporation | Rapamycin oximes |
| US5391730A (en) * | 1993-10-08 | 1995-02-21 | American Home Products Corporation | Phosphorylcarbamates of rapamycin and oxime derivatives thereof |
| US5378836A (en) * | 1993-10-08 | 1995-01-03 | American Home Products Corporation | Rapamycin oximes and hydrazones |
| US5527907A (en) * | 1993-11-19 | 1996-06-18 | Abbott Laboratories | Macrolide immunomodulators |
| US5385908A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered esters of rapamycin |
| US5385909A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5385910A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Gem-distributed esters of rapamycin |
| US5389639A (en) * | 1993-12-29 | 1995-02-14 | American Home Products Company | Amino alkanoic esters of rapamycin |
| US5362735A (en) * | 1994-02-23 | 1994-11-08 | Smithkline Beecham Corporation | Rapamycin derivatives |
| US5525610A (en) * | 1994-03-31 | 1996-06-11 | American Home Products Corporation | 42-Epi-rapamycin and pharmaceutical compositions thereof |
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US5463048A (en) * | 1994-06-14 | 1995-10-31 | American Home Products Corporation | Rapamycin amidino carbamates |
| US5693648A (en) * | 1994-09-30 | 1997-12-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides having immunosuppressive activity |
| US5491231A (en) * | 1994-11-28 | 1996-02-13 | American Home Products Corporation | Hindered N-oxide esters of rapamycin |
| US5563145A (en) * | 1994-12-07 | 1996-10-08 | American Home Products Corporation | Rapamycin 42-oximes and hydroxylamines |
| 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 |
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| US8394398B2 (en) * | 1997-09-26 | 2013-03-12 | Abbott Laboratories | Methods of administering rapamycin analogs with anti-inflammatories using medical devices |
| US8257726B2 (en) * | 1997-09-26 | 2012-09-04 | Abbott Laboratories | Compositions, systems, kits, and methods of administering rapamycin analogs with paclitaxel using medical devices |
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| US20070032853A1 (en) * | 2002-03-27 | 2007-02-08 | Hossainy Syed F | 40-O-(2-hydroxy)ethyl-rapamycin coated stent |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE877700A (fr) * | 1978-11-03 | 1980-01-14 | Ayerst Mckenna & Harrison | Compositions pharmaceutiques a base de rapamycine pour le traitement de tumeurs carcinogenes |
| AU543727B2 (en) * | 1980-06-02 | 1985-05-02 | Ayerst Mckenna & Harrison Inc. | Injectable composition of rapamycin |
| US4316885A (en) * | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
-
1985
- 1985-12-06 US US06/806,152 patent/US4650803A/en not_active Expired - Lifetime
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1986
- 1986-12-02 PT PT83843A patent/PT83843B/pt not_active IP Right Cessation
- 1986-12-03 CA CA000524469A patent/CA1273920A/en not_active Expired - Lifetime
- 1986-12-04 AU AU66080/86A patent/AU583439B2/en not_active Ceased
- 1986-12-04 AT AT86309449T patent/ATE74134T1/de not_active IP Right Cessation
- 1986-12-04 EP EP86309449A patent/EP0227355B1/en not_active Expired - Lifetime
- 1986-12-04 DE DE8686309449T patent/DE3684574D1/de not_active Expired - Lifetime
- 1986-12-04 ES ES198686309449T patent/ES2032750T3/es not_active Expired - Lifetime
- 1986-12-04 ZA ZA869181A patent/ZA869181B/xx unknown
- 1986-12-04 KR KR1019860010339A patent/KR940004072B1/ko not_active Expired - Fee Related
- 1986-12-04 JP JP61289750A patent/JPH0670066B2/ja not_active Expired - Lifetime
- 1986-12-04 GB GB08628994A patent/GB2183647A/en active Granted
- 1986-12-05 DK DK584886A patent/DK169409B1/da not_active IP Right Cessation
- 1986-12-05 IE IE319886A patent/IE64506B1/en not_active IP Right Cessation
- 1986-12-05 HU HU865042Q patent/HU198054B/hu unknown
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1990
- 1990-08-24 CA CA000615850A patent/CA1312076C/en not_active Expired - Lifetime
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1991
- 1991-12-04 KR KR1019910022103A patent/KR940004073B1/ko not_active Expired - Fee Related
-
1992
- 1992-05-07 GR GR920400868T patent/GR3004530T3/el unknown
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1993
- 1993-03-25 DK DK034793A patent/DK170750B1/da not_active IP Right Cessation
- 1993-12-03 JP JP5303867A patent/JPH0747593B2/ja not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU6608086A (en) | 1987-06-11 |
| JPS62215592A (ja) | 1987-09-22 |
| JPH0670066B2 (ja) | 1994-09-07 |
| EP0227355A2 (en) | 1987-07-01 |
| GR3004530T3 (enExample) | 1993-04-28 |
| AU583439B2 (en) | 1989-04-27 |
| PT83843B (pt) | 1989-01-17 |
| ATE74134T1 (de) | 1992-04-15 |
| ES2032750T3 (es) | 1993-03-01 |
| EP0227355B1 (en) | 1992-03-25 |
| DK584886A (da) | 1987-06-07 |
| ZA869181B (en) | 1988-07-27 |
| DE3684574D1 (de) | 1992-04-30 |
| CA1273920A (en) | 1990-09-11 |
| HU198054B (en) | 1989-07-28 |
| DK584886D0 (da) | 1986-12-05 |
| GB2183647B (enExample) | 1989-10-18 |
| DK34793A (da) | 1993-03-25 |
| EP0227355A3 (en) | 1988-10-12 |
| DK170750B1 (da) | 1996-01-08 |
| CA1312076C (en) | 1992-12-29 |
| DK34793D0 (da) | 1993-03-25 |
| IE863198L (en) | 1987-06-06 |
| GB8628994D0 (en) | 1987-01-14 |
| DK169409B1 (da) | 1994-10-24 |
| IE64506B1 (en) | 1995-08-09 |
| KR940004073B1 (ko) | 1994-05-11 |
| KR870006072A (ko) | 1987-07-09 |
| GB2183647A (en) | 1987-06-10 |
| JPH0747593B2 (ja) | 1995-05-24 |
| JPH06263765A (ja) | 1994-09-20 |
| PT83843A (en) | 1987-01-01 |
| US4650803A (en) | 1987-03-17 |
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