CA2266039A1 - Derives de rapamycine alkyles - Google Patents
Derives de rapamycine alkyles Download PDFInfo
- Publication number
- CA2266039A1 CA2266039A1 CA002266039A CA2266039A CA2266039A1 CA 2266039 A1 CA2266039 A1 CA 2266039A1 CA 002266039 A CA002266039 A CA 002266039A CA 2266039 A CA2266039 A CA 2266039A CA 2266039 A1 CA2266039 A1 CA 2266039A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- ch2ch2o
- independently
- ch2ch2ch2o
- phenyl
- 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.)
- Abandoned
Links
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- 210000001519 tissue Anatomy 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- 150000005671 trienes Chemical class 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La présente invention concerne des composés présentant une activité immunodépressive et/ou anti-tumorale et/ou anti-inflammatoire in vivo et inhibant la prolifération de thymocytes in vitro. Ces composés sont donc utiles dans le traitement du rejet d'une transplantation, des affections auto-immunes telles que le lupus érythémateux, la polyarthrite rhumatoïde, le diabète sucré, la sclérose en plaques, et dans le traitement des infections dues au Candida albicans, ainsi que dans le traitement de maladies inflammatoires. Ces composés sont représentés par la formule (I), dans laquelle W et Y désignent OR?1¿ et X et Z forment une liaison ou W et X désignent OR?2¿ et Y et Z forment une liaison, formule dans laquelle: R?1¿ est sélectionné parmi -(CH¿2?)¿n?-Ar où Ar ne désigne pas un phényle, -(CH¿2?CH¿2?O)¿n?CH¿3? où n ne désigne pas 1, -CH¿2?CH¿2?CH¿2?O(CH¿2?CH¿2?O)¿m?-CH¿3?, -(CH¿2?)¿n?-CH¿2?CH(OR?3¿)CH¿2?OR?4¿ où R?3¿ et R?4¿ désignent H, alkyle C¿1?-C¿10?, ou R?3¿ et R?4¿ désignent ensemble un éthylène, un méthylène ou un diméthyméthylène; -CH¿2?(CH¿2?)¿n?-OR?3¿ où R?3¿ ne désigne pas H, alkyle C¿1?-C¿10?, ou C(O)alkyleC¿1?-C¿10?; et -CH¿2?(CH¿2?)¿n?-X où X désigne F, Cl, Br ou I; R?2¿ est sélectionné parmi H, alkyle C¿1?-C¿10?, Ar(CH¿2?)¿n?-, alcényle C¿3?-C¿10?, -(CH¿2?CH¿2?O)¿n?CH¿3?, -CH¿2?CH¿2?CH¿2?O(CH¿2?CH¿2?O)¿m?-CH¿3?, -CH¿2?(CH¿2?)¿n?-OR?3¿, -CH¿2?(CH¿2?)¿n?-X où X désigne F, Cl, Br ou I; et -(CH¿2?)¿n?-CH¿2?CH(OR?5¿)CH¿2?OR?6¿ où R?5¿ et R?6¿ sont sélectionnés de façon autonome parmi H, alkyle C¿1?-C¿10?, -(CH¿2?)¿n?-Ar, -CONH(CH¿2?)¿n?-Ar ou COC(CH¿3?)¿2?-(CH¿2?)¿n?-Ar, -COR?7¿ et -CO¿2?R?7¿, où R?7¿ désigne alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, ou Ar; n = 1-10 de façon autonome m = 1-5 de façon autonome; et Ar est sélectionné de façon autonome parmi phényle, pyridinyle, quinolinyle, indolyle, furanyle; 1,2,3-triazolyle et tetrazolyle, et un sel d'addition d'acide acceptable au niveau pharmaceutique là où on peut en former un.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70959196A | 1996-09-09 | 1996-09-09 | |
| US08/709,591 | 1996-09-09 | ||
| PCT/US1997/015439 WO1998009970A2 (fr) | 1996-09-09 | 1997-09-03 | Derives de rapamycine alkyles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2266039A1 true CA2266039A1 (fr) | 1998-03-12 |
Family
ID=24850507
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002266039A Abandoned CA2266039A1 (fr) | 1996-09-09 | 1997-09-03 | Derives de rapamycine alkyles |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP0927182A2 (fr) |
| JP (1) | JP2001500126A (fr) |
| CN (1) | CN1235608A (fr) |
| AU (1) | AU4176897A (fr) |
| CA (1) | CA2266039A1 (fr) |
| WO (1) | WO1998009970A2 (fr) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6890546B2 (en) | 1998-09-24 | 2005-05-10 | Abbott Laboratories | Medical devices containing rapamycin analogs |
| US6015815A (en) | 1997-09-26 | 2000-01-18 | Abbott Laboratories | Tetrazole-containing rapamycin analogs with shortened half-lives |
| TW557297B (en) * | 1997-09-26 | 2003-10-11 | Abbott Lab | Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same |
| US7455853B2 (en) | 1998-09-24 | 2008-11-25 | Abbott Cardiovascular Systems Inc. | Medical devices containing rapamycin analogs |
| SI3351246T1 (sl) | 2001-02-19 | 2019-08-30 | Novartis Pharma Ag | Derivat rapamicina za zdravljenje trdnega tumorja, povezanega z deregulirano angiogenezo |
| JP2005501868A (ja) * | 2001-08-22 | 2005-01-20 | ワイス | ラパマイシン２９−エノール |
| BR0211905A (pt) | 2001-08-22 | 2004-09-21 | Wyeth Corp | Dialdeìdos de rapamicina |
| EP2407473A3 (fr) | 2002-02-01 | 2012-03-21 | ARIAD Pharmaceuticals, Inc | Procédé de préparation de composés contenant du phosphore |
| AU2003293529A1 (en) | 2002-12-16 | 2004-07-29 | Nitromed, Inc. | Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use |
| JP4716280B2 (ja) * | 2004-03-01 | 2011-07-06 | テルモ株式会社 | Ｏ−アルキル化ラパマイシン誘導体の製造法 |
| EP1768662A2 (fr) | 2004-06-24 | 2007-04-04 | Novartis Vaccines and Diagnostics, Inc. | Immuno-potentialisateurs a petites molecules et analyses visant a detecter leur presence |
| CN104854112A (zh) * | 2012-11-30 | 2015-08-19 | 杭州归创生物医药有限公司 | 雷帕霉素类似物及其制备方法 |
| US20160130280A1 (en) * | 2013-06-20 | 2016-05-12 | Novartis Ag | Alkylation with an alkyl fluoroalkyl sulfonate |
| JP7382353B2 (ja) | 2018-06-15 | 2023-11-16 | ヤンセン ファーマシューティカ エヌ．ベー． | ラパマイシン類似体およびその使用 |
| BR112022010754A2 (pt) | 2019-12-05 | 2022-08-23 | Anakuria Therapeutics Inc | Análogos de rapamicina e usos dos mesmos |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5151413A (en) * | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| ZA935112B (en) * | 1992-07-17 | 1994-02-08 | Smithkline Beecham Corp | Rapamycin derivatives |
| ZA935111B (en) * | 1992-07-17 | 1994-02-04 | Smithkline Beecham Corp | Rapamycin derivatives |
| GB9221220D0 (en) * | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5258389A (en) * | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| GB9307491D0 (en) * | 1993-04-08 | 1993-06-02 | Sandoz Ltd | Organic compounds |
-
1997
- 1997-09-03 JP JP10512815A patent/JP2001500126A/ja active Pending
- 1997-09-03 EP EP97939749A patent/EP0927182A2/fr not_active Withdrawn
- 1997-09-03 CN CN97199423A patent/CN1235608A/zh active Pending
- 1997-09-03 CA CA002266039A patent/CA2266039A1/fr not_active Abandoned
- 1997-09-03 AU AU41768/97A patent/AU4176897A/en not_active Abandoned
- 1997-09-03 WO PCT/US1997/015439 patent/WO1998009970A2/fr not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU4176897A (en) | 1998-03-26 |
| WO1998009970A3 (fr) | 1998-04-16 |
| EP0927182A2 (fr) | 1999-07-07 |
| JP2001500126A (ja) | 2001-01-09 |
| CN1235608A (zh) | 1999-11-17 |
| WO1998009970A2 (fr) | 1998-03-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Dead |