JP2007532134A - ラパマイシン42−エステル誘導体の位置特異的合成 - Google Patents
ラパマイシン42−エステル誘導体の位置特異的合成 Download PDFInfo
- Publication number
- JP2007532134A JP2007532134A JP2007508442A JP2007508442A JP2007532134A JP 2007532134 A JP2007532134 A JP 2007532134A JP 2007508442 A JP2007508442 A JP 2007508442A JP 2007508442 A JP2007508442 A JP 2007508442A JP 2007532134 A JP2007532134 A JP 2007532134A
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- rapamycin
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- lipase
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- 0 C*C(C(C)C[C@](CCC1C)O[C@]1(C(C(N(CCCC1)[C@@]1C(*[C@@](CC([C@](C)C=C1C)=O)[C@](C)C[C@](CC[C@]2O)C[C@]2OC)=O)=O)=*)O)[C@]1O Chemical compound C*C(C(C)C[C@](CCC1C)O[C@]1(C(C(N(CCCC1)[C@@]1C(*[C@@](CC([C@](C)C=C1C)=O)[C@](C)C[C@](CC[C@]2O)C[C@]2OC)=O)=O)=*)O)[C@]1O 0.000 description 2
Classifications
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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
-
- 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
-
- 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)
- Oncology (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (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)
Abstract
Description
Claims (18)
- 使用されるリパーゼが、微生物、例えば、アスペルギルス・ニガー(Aspergillus niger)、カンジダ・アンタルクチカ(Candida antarctica)、カンジダ・ルゴサ(Candida rugosa)、ムコール・ミーヘイ(Mucor miehei)、シュードモナス・セパシア(Pseudomonas cepacia)、シュードモナス・フルオレッセンス(Pseudomonas fluorescens)、リゾープス・デレマ(Rhizopus delemar)からの細菌リパーゼである、請求項1に記載の方法。
- 使用されるリパーゼが、B型カンジダ・アンタルクチカ(Candida antarctica type B)からのもの(NOVOZYME 435リパーゼ)またはシュードモナス・セパシア(Pseudomonas cepacia)からのもの(リパーゼPS−C「Aamano」II)である、請求項2に記載の方法。
- 前記アシル供与体が、ビニルエステル、イソプロペニルエステルまたは無水物である、請求項1から3のいずれか一項に記載の方法。
- 前記ビニルエステルが、式CH2=CH−O−COR1(式中、R1は、ヒドロキシル、ハロゲンおよびSHから独立して選択される基で場合によっては置換されている、C1〜C6アルキル、C2〜C6アルケニル、C6〜C14アリール、ベンジルから成る群より選択される)を有する、請求項4に記載の方法。
- 前記ビニルエステルが、ビニルアセテート、ビニルプロピオネート、ビニルクロロアセテート、ビニルクロトネート、ビニルベンゾエートおよびビニルデカノエートから成る群より選択される、請求項5に記載の方法。
- 前記ビニルエステルが、イソプロピリデン保護ビニル3−ヒドロキシ−2−(ヒドロキシメチル)−2−メチルプロピオネートである、請求項4に記載の方法。
- 前記イソプロペニルエステルが、式CH2=C(CH3)−OCOR2(式中、R2は、ヒドロキシル、ハロゲンおよびSHから独立して選択される基で場合によっては置換されている、C1〜C6アルキル、C2〜C6アルケニル、C6〜C14アリール、ベンジルから成る群より選択される)を有する、請求項4に記載の方法。
- 前記イソプロペニルエステルが、イソプロペニルアセテートである、請求項8に記載の方法。
- 前記無水物が、ハロゲンおよびヒドロキシルから独立して選択される基で場合によっては置換されている、C1〜C8直鎖または分枝鎖アルカン酸無水物である、請求項4に記載の方法。
- 前記反応が、トルエン、t−ブチルメチルエーテル(TBME)、エチルエーテル、THF、MeCN、CH2Cl2、CHCl3、ヘキサン、ジオキサンまたはこれらの混合物から成る群より選択される有機溶媒中で行われる、請求項1から10のいずれか一項に記載の方法。
- 前記反応が、20℃から75℃の範囲内で行われる、請求項1から11のいずれか一項に記載の方法。
- CCI−779の前駆体である、イソプロピリデンケタール保護3−ヒドロキシ−2−(ヒドロキシメチル)−2−メチルプロピオン酸とのラパマイシン42−エステルの位置特異的製剤。
- 請求項1から12のいずれか一項に記載の方法に従って製造された位置特異的ラパマイシン42−誘導体を含む組成物。
- 請求項13に記載の位置特異的ラパマイシン42−誘導体製剤を含む組成物。
- 生理適合性担体をさらに含む、請求項14または15に記載の組成物。
- 請求項14から16のいずれか一項に記載の組成物および前記組成物のための容器を含む製品。
- 請求項1から12のいずれか一項に従って製造された位置特異的ラパマイシン42−誘導体の複数の単位を単位剤形で含む薬学的キット。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US56192604P | 2004-04-14 | 2004-04-14 | |
PCT/US2005/012266 WO2005105811A1 (en) | 2004-04-14 | 2005-04-12 | Regiospecific synthesis of rapamycin 42-ester derivatives |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2007532134A true JP2007532134A (ja) | 2007-11-15 |
JP2007532134A5 JP2007532134A5 (ja) | 2008-03-13 |
JP4224115B2 JP4224115B2 (ja) | 2009-02-12 |
Family
ID=34965235
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007508442A Expired - Fee Related JP4224115B2 (ja) | 2004-04-14 | 2005-04-12 | ラパマイシン42−エステル誘導体の位置特異的合成 |
Country Status (23)
Country | Link |
---|---|
US (1) | US7268144B2 (ja) |
EP (1) | EP1737869A1 (ja) |
JP (1) | JP4224115B2 (ja) |
KR (1) | KR20070015544A (ja) |
CN (1) | CN1942476A (ja) |
AR (1) | AR049019A1 (ja) |
AU (1) | AU2005238431A1 (ja) |
BR (1) | BRPI0509852A (ja) |
CA (1) | CA2562952A1 (ja) |
CL (1) | CL2008000507A1 (ja) |
CR (1) | CR8646A (ja) |
EC (1) | ECSP066927A (ja) |
GT (1) | GT200500085A (ja) |
IL (1) | IL178315A0 (ja) |
MX (1) | MXPA06011881A (ja) |
NO (1) | NO20065090L (ja) |
PA (1) | PA8629901A1 (ja) |
PE (1) | PE20060253A1 (ja) |
RU (1) | RU2387657C2 (ja) |
SG (1) | SG152234A1 (ja) |
TW (1) | TW200536542A (ja) |
UA (1) | UA87492C2 (ja) |
WO (1) | WO2005105811A1 (ja) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2015518869A (ja) * | 2012-06-08 | 2015-07-06 | バイオトロニック アクチェンゲゼルシャフト | ラパマイシン−40−o−環状炭化水素エステル、組成物及び方法 |
JP2016519086A (ja) * | 2013-03-15 | 2016-06-30 | バイオセンサーズ インターナショナル グループ、リミテッド | ラパマイシン誘導体の精製 |
JP2021503500A (ja) * | 2017-11-20 | 2021-02-12 | アイカーン スクール オブ メディスン アット マウント サイナイ | 治療用ナノバイオロジー組成物での訓練された免疫の阻害 |
US11859021B2 (en) | 2021-03-19 | 2024-01-02 | Icahn School Of Medicine At Mount Sinai | Compounds for regulating trained immunity, and their methods of use |
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AU2005238493A1 (en) * | 2004-04-27 | 2005-11-10 | Wyeth | Labeling of rapamycin using rapamycin-specific methylases |
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AU2006213061A1 (en) | 2005-02-09 | 2006-08-17 | Wyeth | CCI-779 polymorph and use thereof |
US7538119B2 (en) * | 2005-11-04 | 2009-05-26 | Wyeth | 41-Methoxy isotope labeled rapamycin 42-ester |
CA2630786A1 (en) * | 2005-12-07 | 2007-06-14 | Wyeth | Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry |
BRPI0619578A2 (pt) * | 2005-12-07 | 2011-10-04 | Wyeth Corp | processo para preparar um 42-éster de rapamicina, composto, método para isolar o boronato do 42-éster de rapamicina bruto a partir do licor mãe, método para purificação de um boronato do 42-éster de rapamicina, e, boronato de cci-779 |
BRPI0619493A2 (pt) * | 2005-12-07 | 2016-09-06 | Wyeth Corp | forma cristalina purificada de cci-779, processo para a purificação de cc-779, produto, método para monitorar a cristalização de cci-779, kit, composição farmacêutica, método para o tratamento de câncer, e, uso de um cci-779 purificado |
CN101394867A (zh) * | 2006-03-07 | 2009-03-25 | 惠氏公司 | 大环内酯类免疫抑制剂的水溶性聚乙二醇结合物的制备方法 |
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US20080276935A1 (en) | 2006-11-20 | 2008-11-13 | Lixiao Wang | Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs |
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RU2603261C2 (ru) * | 2011-04-01 | 2016-11-27 | Сандоз Аг | Региоселективное ацилирование рапамицина в положении с-42 |
US10751450B2 (en) | 2012-06-08 | 2020-08-25 | Biotronik Ag | Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods |
US20160030401A1 (en) | 2013-03-13 | 2016-02-04 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors for prevention of intestinal polyp growth and cancer |
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-
2005
- 2005-04-12 CA CA002562952A patent/CA2562952A1/en not_active Abandoned
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Cited By (10)
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JP2015518869A (ja) * | 2012-06-08 | 2015-07-06 | バイオトロニック アクチェンゲゼルシャフト | ラパマイシン−40−o−環状炭化水素エステル、組成物及び方法 |
JP2016519086A (ja) * | 2013-03-15 | 2016-06-30 | バイオセンサーズ インターナショナル グループ、リミテッド | ラパマイシン誘導体の精製 |
US10202402B2 (en) | 2013-03-15 | 2019-02-12 | Biosensors International Group, Ltd. | Purification of rapamycin derivatives using temperature induced phase separation |
US10597406B2 (en) | 2013-03-15 | 2020-03-24 | Biosensors International Group, Ltd. | Purification of rapamycin derivatives using temperature induced phase separation |
US11046711B2 (en) | 2013-03-15 | 2021-06-29 | Biosensors International Group, Ltd. | Purification of rapamycin derivatives using temperature induced phase separation |
JP2021121601A (ja) * | 2013-03-15 | 2021-08-26 | バイオセンサーズ インターナショナル グループ、リミテッド | ラパマイシン誘導体の精製 |
US11780850B2 (en) | 2013-03-15 | 2023-10-10 | Biosensors International Group, Ltd. | Purification of rapamycin derivatives using temperature induced phase separation |
JP2021503500A (ja) * | 2017-11-20 | 2021-02-12 | アイカーン スクール オブ メディスン アット マウント サイナイ | 治療用ナノバイオロジー組成物での訓練された免疫の阻害 |
JP7357629B2 (ja) | 2017-11-20 | 2023-10-06 | アイカーン スクール オブ メディスン アット マウント サイナイ | 治療用ナノバイオロジー組成物での訓練された免疫の阻害 |
US11859021B2 (en) | 2021-03-19 | 2024-01-02 | Icahn School Of Medicine At Mount Sinai | Compounds for regulating trained immunity, and their methods of use |
Also Published As
Publication number | Publication date |
---|---|
IL178315A0 (en) | 2007-02-11 |
SG152234A1 (en) | 2009-05-29 |
CR8646A (es) | 2007-08-28 |
KR20070015544A (ko) | 2007-02-05 |
US7268144B2 (en) | 2007-09-11 |
JP4224115B2 (ja) | 2009-02-12 |
RU2006134014A (ru) | 2008-05-20 |
US20050234234A1 (en) | 2005-10-20 |
RU2387657C2 (ru) | 2010-04-27 |
CA2562952A1 (en) | 2005-11-10 |
NO20065090L (no) | 2006-11-13 |
EP1737869A1 (en) | 2007-01-03 |
GT200500085A (es) | 2005-11-03 |
CL2008000507A1 (es) | 2008-07-04 |
AU2005238431A1 (en) | 2005-11-10 |
WO2005105811A1 (en) | 2005-11-10 |
TW200536542A (en) | 2005-11-16 |
ECSP066927A (es) | 2006-12-20 |
PA8629901A1 (es) | 2006-06-02 |
BRPI0509852A (pt) | 2007-10-23 |
MXPA06011881A (es) | 2006-12-14 |
CN1942476A (zh) | 2007-04-04 |
PE20060253A1 (es) | 2006-03-30 |
AR049019A1 (es) | 2006-06-21 |
UA87492C2 (en) | 2009-07-27 |
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