RU2006134014A - Региоспецифический синтез производных 42-эфира рапамицина - Google Patents
Региоспецифический синтез производных 42-эфира рапамицина Download PDFInfo
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- RU2006134014A RU2006134014A RU2006134014/04A RU2006134014A RU2006134014A RU 2006134014 A RU2006134014 A RU 2006134014A RU 2006134014/04 A RU2006134014/04 A RU 2006134014/04A RU 2006134014 A RU2006134014 A RU 2006134014A RU 2006134014 A RU2006134014 A RU 2006134014A
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- Prior art keywords
- vinyl
- rapamycin
- lipase
- ether
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
-
- 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
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
- C12N9/18—Carboxylic ester hydrolases (3.1.1)
- C12N9/20—Triglyceride splitting, e.g. by means of lipase
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
- C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Oncology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Enzymes And Modification Thereof (AREA)
Claims (18)
1. Способ региоспецифического получения производных 42-эфира рапамицина с формулой (I)
где R является линейным или циклическим, алифатическим или ароматическим, насыщенным или ненасыщенным углеводородом, который по выбору содержит гидроксил, галоген и/или серу, вышеуказанный способ, включающий ацилирование 42-гидроксирапамицина с ацильным донором в присутствии липазы.
2. Способ, по п.1, используемая липаза представляет собой микробную липазу, полученную из таких микроорганизмов, как Aspergillus niger, Candida antarctica, Candida rugosa, Mucor miehei, Pseudomonas cepacia, Pseudomonas fluorescens, Rhizopus delemar.
3. Способ, по п.2, в котором используют липазу типа В, полученную из Candida antarctica (липаза NOVOZYM 435) или Pseudemonas cepacia (липаза PS-C "Amano" II).
4. Способ, по любому из пп.1-3, в котором ацильным донором является виниловый эфир, изопропениловый эфир или ангидрид.
5. Способ по п.4, в котором виниловый эфир имеет формулу СН2=СН-O-COR1, где R1 выбирается из группы, состоящей из алкила C1-C6, алкенила С2-С6, арила C6-C14, бензила, замещенных по выбору группой, независимо выбранной из гидроксила, галогена и SH.
6. Способ по п.5, в котором виниловый эфир выбирается из группы, состоящей из винилацетата, винилпропионата, винилхлорацетата, винилкротоната, винилбензоата и винилдеканоата.
7. Способ по п.4, в котором виниловым эфиром является изопропилиден защищенный винил 3-гидрокси-2-(гидроксиметил)-2-метилпропионат.
8. Способ по п.4, в котором изопропениловый эфир имеет формулу СН2=С(СН3)-OCOR2, где R2 выбирается из группы, состоящей из алкила C1-C6, алкенила С2-С6, арила С6-С14, бензила, замещенных по выбору группой, независимо выбранной из гидроксила, галогена и SH.
9. Способ по п.8, где изопропениловым эфиром является изопропенилацетат.
10. Способ по п.4, в котором ангидридом является алкановый ангидрид С1-С8 с прямой или разветвленной цепью, замещенный по выбору группой независимо выбранной из галогена или гидроксила.
11. Способ по любому из пп.1-3 или 5-10, в которых реакция происходит в органическом растворителе, выбранном из группы растворителей, состоящей из толуола, трет-бутилметилового эфира (ТБМЭ), этилового эфира, тетрагидрофурана (ТГФ), MeCN, CH2Cl2, CHCl3, гексана, диоксана или их смеси.
12. Способ по п.11, в котором реакцию проводят в диапазоне температур 20-75°С.
13. Региоспецифическое приготовление 42-эфира рапамицина с изопропилиденкеталь защищенной 3-гидрокси-2-(гидроксиметил)-2-метилпропионовой кислотой, предшественником CCI-779.
14. Состав, включающий региоспецифические 42-производные рапамицина, полученные в соответствии со способом любого из пп.1-12.
15. Состав, включающий получение региоспецифических 42-производных рапамицина в соответствии с п.13.
16. Состав, в соответствии с п.14 или 15, кроме того, включающий физиологически совместимый носитель.
17. Продукт, включающий состав в соответствии с любым из пп.14-16 и упаковку для вышеуказанной композиции.
18. Фармацевтический комплект, включающий единицу региоспецифического 42-производного рапамицина, полученного в соответствии с любым из пп.1-12 в форме одноразовой дозированной формы.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56192604P | 2004-04-14 | 2004-04-14 | |
| US60/561,926 | 2004-04-14 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2006134014A true RU2006134014A (ru) | 2008-05-20 |
| RU2387657C2 RU2387657C2 (ru) | 2010-04-27 |
Family
ID=34965235
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2006134014/04A RU2387657C2 (ru) | 2004-04-14 | 2005-04-12 | Региоспецифический синтез производных 42-эфира рапамицина |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US7268144B2 (ru) |
| EP (1) | EP1737869A1 (ru) |
| JP (1) | JP4224115B2 (ru) |
| KR (1) | KR20070015544A (ru) |
| CN (1) | CN1942476A (ru) |
| AR (1) | AR049019A1 (ru) |
| AU (1) | AU2005238431A1 (ru) |
| BR (1) | BRPI0509852A (ru) |
| CA (1) | CA2562952A1 (ru) |
| CL (1) | CL2008000507A1 (ru) |
| CR (1) | CR8646A (ru) |
| EC (1) | ECSP066927A (ru) |
| GT (1) | GT200500085A (ru) |
| IL (1) | IL178315A0 (ru) |
| MX (1) | MXPA06011881A (ru) |
| NO (1) | NO20065090L (ru) |
| PA (1) | PA8629901A1 (ru) |
| PE (1) | PE20060253A1 (ru) |
| RU (1) | RU2387657C2 (ru) |
| SG (1) | SG152234A1 (ru) |
| TW (1) | TW200536542A (ru) |
| UA (1) | UA87492C2 (ru) |
| WO (1) | WO2005105811A1 (ru) |
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| BRPI0514206A (pt) * | 2004-08-10 | 2008-06-03 | Wyeth Corp | composto, anticorpo, kit para monitorar a terapia com cci-779, e, métodos para detectar metabólitos de cci-779, e para produzir um metabólito sintético e um derivado de cci-779 |
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-
2005
- 2005-04-12 MX MXPA06011881A patent/MXPA06011881A/es active IP Right Grant
- 2005-04-12 KR KR1020067021378A patent/KR20070015544A/ko not_active Ceased
- 2005-04-12 CA CA002562952A patent/CA2562952A1/en not_active Abandoned
- 2005-04-12 SG SG200902515-6A patent/SG152234A1/en unknown
- 2005-04-12 JP JP2007508442A patent/JP4224115B2/ja not_active Expired - Fee Related
- 2005-04-12 BR BRPI0509852-1A patent/BRPI0509852A/pt not_active IP Right Cessation
- 2005-04-12 CN CNA2005800112769A patent/CN1942476A/zh active Pending
- 2005-04-12 AU AU2005238431A patent/AU2005238431A1/en not_active Abandoned
- 2005-04-12 EP EP05733853A patent/EP1737869A1/en not_active Withdrawn
- 2005-04-12 RU RU2006134014/04A patent/RU2387657C2/ru not_active IP Right Cessation
- 2005-04-12 US US11/103,799 patent/US7268144B2/en not_active Expired - Fee Related
- 2005-04-12 WO PCT/US2005/012266 patent/WO2005105811A1/en active Application Filing
- 2005-04-13 GT GT200500085A patent/GT200500085A/es unknown
- 2005-04-13 AR ARP050101447A patent/AR049019A1/es unknown
- 2005-04-13 PA PA20058629901A patent/PA8629901A1/es unknown
- 2005-04-13 TW TW094111640A patent/TW200536542A/zh unknown
- 2005-04-13 PE PE2005000409A patent/PE20060253A1/es not_active Application Discontinuation
- 2005-12-04 UA UAA200610949A patent/UA87492C2/ru unknown
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2006
- 2006-09-21 CR CR8646A patent/CR8646A/es not_active Application Discontinuation
- 2006-09-26 IL IL178315A patent/IL178315A0/en unknown
- 2006-10-16 EC EC2006006927A patent/ECSP066927A/es unknown
- 2006-11-03 NO NO20065090A patent/NO20065090L/no not_active Application Discontinuation
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2008
- 2008-02-19 CL CL200800507A patent/CL2008000507A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2008000507A1 (es) | 2008-07-04 |
| NO20065090L (no) | 2006-11-13 |
| US20050234234A1 (en) | 2005-10-20 |
| JP4224115B2 (ja) | 2009-02-12 |
| CR8646A (es) | 2007-08-28 |
| CA2562952A1 (en) | 2005-11-10 |
| US7268144B2 (en) | 2007-09-11 |
| AR049019A1 (es) | 2006-06-21 |
| BRPI0509852A (pt) | 2007-10-23 |
| MXPA06011881A (es) | 2006-12-14 |
| RU2387657C2 (ru) | 2010-04-27 |
| WO2005105811A1 (en) | 2005-11-10 |
| PE20060253A1 (es) | 2006-03-30 |
| TW200536542A (en) | 2005-11-16 |
| CN1942476A (zh) | 2007-04-04 |
| JP2007532134A (ja) | 2007-11-15 |
| PA8629901A1 (es) | 2006-06-02 |
| EP1737869A1 (en) | 2007-01-03 |
| GT200500085A (es) | 2005-11-03 |
| AU2005238431A1 (en) | 2005-11-10 |
| ECSP066927A (es) | 2006-12-20 |
| SG152234A1 (en) | 2009-05-29 |
| IL178315A0 (en) | 2007-02-11 |
| UA87492C2 (en) | 2009-07-27 |
| KR20070015544A (ko) | 2007-02-05 |
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