UA83245C2 - Regioselective synthesis of cci-779 - Google Patents
Regioselective synthesis of cci-779Info
- Publication number
- UA83245C2 UA83245C2 UAA200602447A UAA200602447A UA83245C2 UA 83245 C2 UA83245 C2 UA 83245C2 UA A200602447 A UAA200602447 A UA A200602447A UA A200602447 A UAA200602447 A UA A200602447A UA 83245 C2 UA83245 C2 UA 83245C2
- Authority
- UA
- Ukraine
- Prior art keywords
- cci
- regioselective synthesis
- regioselective
- synthesis
- boronate
- Prior art date
Links
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[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 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 229960000235 temsirolimus Drugs 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 abstract 1
- 239000000543 intermediate Substances 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
- C07D498/02—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 two hetero rings
- C07D498/08—Bridged systems
-
- 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
-
- 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
-
- 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
- C07D498/22—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 four or more hetero rings
-
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Catalysts (AREA)
Abstract
Предлагается способ региоселективного синтеза ССІ-779, основанный на химии боронатов. Также предложены новые промежуточные продукты, которые применяются в данном способе.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49324903P | 2003-08-07 | 2003-08-07 | |
| PCT/US2004/022860 WO2005016935A2 (en) | 2003-08-07 | 2004-07-15 | Regioselective synthesis of cci-779 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA83245C2 true UA83245C2 (en) | 2008-06-25 |
Family
ID=34193170
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA200602447A UA83245C2 (en) | 2003-08-07 | 2004-07-15 | Regioselective synthesis of cci-779 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US7153957B2 (ru) |
| EP (1) | EP1658295B1 (ru) |
| JP (1) | JP4227649B2 (ru) |
| KR (1) | KR20060057605A (ru) |
| CN (1) | CN1829722B (ru) |
| AR (1) | AR045217A1 (ru) |
| AT (1) | ATE365169T1 (ru) |
| AU (1) | AU2004265267A1 (ru) |
| BR (1) | BRPI0412667A (ru) |
| CA (1) | CA2532988A1 (ru) |
| CO (1) | CO5650251A2 (ru) |
| CR (1) | CR8189A (ru) |
| DE (1) | DE602004007145T2 (ru) |
| DK (1) | DK1658295T3 (ru) |
| EC (1) | ECSP066413A (ru) |
| ES (1) | ES2287772T3 (ru) |
| IL (1) | IL173134A0 (ru) |
| MX (1) | MXPA06000951A (ru) |
| NO (1) | NO20060494L (ru) |
| PL (1) | PL1658295T3 (ru) |
| PT (1) | PT1658295E (ru) |
| RU (1) | RU2339639C2 (ru) |
| TW (1) | TW200508241A (ru) |
| UA (1) | UA83245C2 (ru) |
| WO (1) | WO2005016935A2 (ru) |
| ZA (1) | ZA200601055B (ru) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1389209B1 (en) * | 2001-04-24 | 2009-04-08 | Purdue Research Foundation | Folate mimetics and folate-receptor binding conjugates thereof |
| WO2003097647A1 (en) * | 2002-05-15 | 2003-11-27 | Endocyte, Inc. | Vitamin-mitomycin conjugates |
| NZ537829A (en) | 2002-07-30 | 2006-09-29 | Wyeth Corp | Parenteral formulations containing a rapamycin hydroxyester |
| DK1592457T3 (da) | 2003-01-27 | 2012-10-22 | Endocyte Inc | Folat-vinblastin-konjugat som lægemiddel |
| RU2345999C2 (ru) * | 2003-09-03 | 2009-02-10 | Уайт | Аморфный 42-эфир рапамицина и 3-гидрокси-2(гидроксиметил)-2-метилпропионовой кислоты и содержащие его фармацевтические композиции |
| JP2007517879A (ja) * | 2004-01-08 | 2007-07-05 | ワイス | Cci−779経口投与用の直接圧縮可能な医薬組成物 |
| JP4224115B2 (ja) | 2004-04-14 | 2009-02-12 | ワイス | ラパマイシン42−エステル誘導体の位置特異的合成 |
| AU2005238432A1 (en) | 2004-04-14 | 2005-11-10 | Wyeth | Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies |
| AU2005233612A1 (en) | 2004-04-14 | 2005-10-27 | Wyeth | Proline CCI-779 (proline-rapamycin 42-ester with 2,2-bis (hydroxymethyl) propionic acid) and two-step enzymatic synthesis of proline CCI-779 and CCI-779 using microbial lipase |
| CA2562164A1 (en) * | 2004-04-27 | 2005-11-10 | Wyeth | Labeling of rapamycin using rapamycin-specific methylases |
| JP5149620B2 (ja) | 2004-07-23 | 2013-02-20 | エンドサイト,インコーポレイテッド | 2価リンカーおよびその結合体 |
| MX2007001676A (es) * | 2004-08-10 | 2007-04-12 | Wyeth Corp | Derivados de 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionico y metodos para hacer los mismos. |
| KR20070070184A (ko) | 2004-10-28 | 2007-07-03 | 와이어쓰 | 자궁근종의 치료에 있어서 mTOR 억제제의 용도 |
| CA2595766A1 (en) * | 2005-02-09 | 2006-08-17 | Wyeth | Cci-779 polymorph and use thereof |
| CA2599580A1 (en) | 2005-03-02 | 2006-09-08 | Wyeth | Recovery of cci-779 from mother liquors |
| JP2008531686A (ja) | 2005-03-02 | 2008-08-14 | ワイス | ラパマイシンの精製 |
| EP1863816B1 (en) | 2005-03-16 | 2014-06-25 | Endocyte, Inc. | Synthesis and purification of pteroic acid and conjugates thereof |
| AU2006279304A1 (en) | 2005-08-19 | 2007-02-22 | Endocyte, Inc. | Multi-drug ligand conjugates |
| EP2382995A3 (en) * | 2005-08-19 | 2013-09-25 | Endocyte, Inc. | Ligand conjugates of Vinca alkaloids, analogs and derivatives |
| WO2007056175A2 (en) * | 2005-11-04 | 2007-05-18 | Wyeth | 41-methoxy isotope labeled rapamycin 42-ester |
| JP2009514870A (ja) | 2005-11-04 | 2009-04-09 | ワイス | mTORインヒビター、ハーセプチン、および/またはHKI−272の抗悪性腫瘍性組み合わせ |
| AR058282A1 (es) * | 2005-12-07 | 2008-01-30 | Wyeth Corp | Forma cristalina purificada de cci-779, un proceso para la preparacion del mismo, un metodo para monitorear la cristalizacion del cci-779, un kit y una composicion farmaceutica que lo comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer. |
| BRPI0619592A2 (pt) * | 2005-12-07 | 2016-09-06 | Wyeth Corp | métodos para medir a qualidade da partícula de um composto de rapamicina, para determinar o tamanho de partícula médio de uma amostra e a cristalinidade de um composto de rapamicina, e para a purificação de rapamicina |
| US7622578B2 (en) * | 2005-12-07 | 2009-11-24 | Wyeth | Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate |
| RU2008121713A (ru) * | 2005-12-20 | 2010-01-27 | Вайет (Us) | Контроль стабильности лекарственной формы cci-779 посредством контроля примесей лекарственныхого вещества |
| US20070203169A1 (en) * | 2006-02-28 | 2007-08-30 | Zhao Jonathon Z | Isomers and 42-epimers of rapamycin ester analogs, methods of making and using the same |
| TW200824713A (en) * | 2006-10-18 | 2008-06-16 | Wyeth Corp | Processes for the synthesis of individual isomers of mono-PEG CCI-779 |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8430055B2 (en) | 2008-08-29 | 2013-04-30 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| US8414526B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
| US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| 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 |
| WO2008101231A2 (en) | 2007-02-16 | 2008-08-21 | Endocyte, Inc. | Methods and compositions for treating and diagnosing kidney disease |
| CN104127878A (zh) * | 2007-03-14 | 2014-11-05 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
| TW200901989A (en) | 2007-04-10 | 2009-01-16 | Wyeth Corp | Anti-tumor activity of CCI-779 in papillary renal cell cancer |
| BRPI0812970A2 (pt) * | 2007-06-25 | 2019-09-24 | Endocyte Inc | conjugados contendo espaçadores hidrofílicos |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| US9187521B2 (en) | 2007-10-25 | 2015-11-17 | Endocyte, Inc. | Tubulysins and processes for preparing |
| WO2011051960A2 (en) | 2009-09-25 | 2011-05-05 | Cadila Healthcare Limited | Process for the preparation of rapamycin derivatives |
| AU2011210227A1 (en) * | 2010-01-28 | 2012-08-30 | Fresenius Kabi Oncology Ltd. | Process for the preparation of Temsirolimus and its intermediates |
| CN102020662B (zh) * | 2011-01-07 | 2013-02-13 | 天津市炜杰科技有限公司 | 一种驮瑞塞尔制备方法 |
| CN102020661B (zh) * | 2011-01-07 | 2013-02-13 | 天津市炜杰科技有限公司 | 一种驮瑞塞尔合成方法 |
| MX2013011412A (es) * | 2011-04-01 | 2014-04-30 | Sandoz Ag | Acilacion regioselectiva de rapamicina en la posicion c-42. |
| US10080805B2 (en) | 2012-02-24 | 2018-09-25 | Purdue Research Foundation | Cholecystokinin B receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| EP2908818A4 (en) | 2012-10-16 | 2016-07-13 | Endocyte Inc | CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE |
| CN104086564B (zh) * | 2014-07-30 | 2019-02-05 | 江苏奥赛康药业股份有限公司 | 一种高纯度坦罗莫司的制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| DE19857765A1 (de) | 1998-12-15 | 2000-06-21 | Clariant Gmbh | Verfahren zur Herstellung von para-Oxadiazolyl-phenyl-boronsäuren |
| US6277983B1 (en) * | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
-
2004
- 2004-07-15 KR KR1020067002610A patent/KR20060057605A/ko not_active Ceased
- 2004-07-15 ES ES04778398T patent/ES2287772T3/es not_active Expired - Lifetime
- 2004-07-15 RU RU2006106910/04A patent/RU2339639C2/ru not_active IP Right Cessation
- 2004-07-15 CN CN2004800217944A patent/CN1829722B/zh not_active Expired - Fee Related
- 2004-07-15 EP EP04778398A patent/EP1658295B1/en not_active Expired - Lifetime
- 2004-07-15 MX MXPA06000951A patent/MXPA06000951A/es active IP Right Grant
- 2004-07-15 DK DK04778398T patent/DK1658295T3/da active
- 2004-07-15 AT AT04778398T patent/ATE365169T1/de not_active IP Right Cessation
- 2004-07-15 AU AU2004265267A patent/AU2004265267A1/en not_active Abandoned
- 2004-07-15 UA UAA200602447A patent/UA83245C2/ru unknown
- 2004-07-15 JP JP2006522574A patent/JP4227649B2/ja not_active Expired - Fee Related
- 2004-07-15 BR BRPI0412667-0A patent/BRPI0412667A/pt not_active IP Right Cessation
- 2004-07-15 DE DE602004007145T patent/DE602004007145T2/de not_active Expired - Fee Related
- 2004-07-15 WO PCT/US2004/022860 patent/WO2005016935A2/en not_active Ceased
- 2004-07-15 CA CA002532988A patent/CA2532988A1/en not_active Abandoned
- 2004-07-15 PT PT04778398T patent/PT1658295E/pt unknown
- 2004-07-15 PL PL04778398T patent/PL1658295T3/pl unknown
- 2004-07-30 US US10/903,062 patent/US7153957B2/en not_active Expired - Fee Related
- 2004-08-04 AR ARP040102778A patent/AR045217A1/es unknown
- 2004-08-05 TW TW093123422A patent/TW200508241A/zh unknown
-
2006
- 2006-01-12 IL IL173134A patent/IL173134A0/en unknown
- 2006-01-13 CR CR8189A patent/CR8189A/es not_active Application Discontinuation
- 2006-01-31 NO NO20060494A patent/NO20060494L/no not_active Application Discontinuation
- 2006-02-06 ZA ZA200601055A patent/ZA200601055B/en unknown
- 2006-02-28 CO CO06019898A patent/CO5650251A2/es unknown
- 2006-03-07 EC EC2006006413A patent/ECSP066413A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US7153957B2 (en) | 2006-12-26 |
| PL1658295T3 (pl) | 2007-11-30 |
| RU2339639C2 (ru) | 2008-11-27 |
| ZA200601055B (en) | 2008-07-30 |
| TW200508241A (en) | 2005-03-01 |
| ECSP066413A (es) | 2006-09-18 |
| CA2532988A1 (en) | 2005-02-24 |
| HK1085482A1 (en) | 2006-08-25 |
| EP1658295A2 (en) | 2006-05-24 |
| JP4227649B2 (ja) | 2009-02-18 |
| ATE365169T1 (de) | 2007-07-15 |
| AR045217A1 (es) | 2005-10-19 |
| CN1829722B (zh) | 2010-10-27 |
| NO20060494L (no) | 2006-03-06 |
| CN1829722A (zh) | 2006-09-06 |
| BRPI0412667A (pt) | 2006-09-26 |
| DK1658295T3 (da) | 2007-09-24 |
| US20050033046A1 (en) | 2005-02-10 |
| EP1658295B1 (en) | 2007-06-20 |
| DE602004007145T2 (de) | 2008-02-28 |
| MXPA06000951A (es) | 2006-03-30 |
| AU2004265267A1 (en) | 2005-02-24 |
| KR20060057605A (ko) | 2006-05-26 |
| PT1658295E (pt) | 2007-09-25 |
| IL173134A0 (en) | 2006-06-11 |
| WO2005016935A3 (en) | 2005-04-07 |
| RU2006106910A (ru) | 2007-09-20 |
| DE602004007145D1 (de) | 2007-08-02 |
| ES2287772T3 (es) | 2007-12-16 |
| WO2005016935A2 (en) | 2005-02-24 |
| JP2007501783A (ja) | 2007-02-01 |
| CR8189A (es) | 2006-10-04 |
| CO5650251A2 (es) | 2006-06-30 |
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