JP2003519655A5 - - Google Patents
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- Publication number
- JP2003519655A5 JP2003519655A5 JP2001551473A JP2001551473A JP2003519655A5 JP 2003519655 A5 JP2003519655 A5 JP 2003519655A5 JP 2001551473 A JP2001551473 A JP 2001551473A JP 2001551473 A JP2001551473 A JP 2001551473A JP 2003519655 A5 JP2003519655 A5 JP 2003519655A5
- Authority
- JP
- Japan
- Prior art keywords
- rapamycin
- ethyl
- pharmaceutical composition
- group
- methyl
- 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.)
- Withdrawn
Links
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 23
- 229960002930 sirolimus Drugs 0.000 claims 23
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class C1C[C@@H](O)[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 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 17
- -1 arylsulfonamidoalkyl Chemical group 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 201000001268 lymphoproliferative syndrome Diseases 0.000 claims 10
- 125000004103 aminoalkyl group Chemical group 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 230000002401 inhibitory effect Effects 0.000 claims 5
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 4
- 125000004945 acylaminoalkyl group Chemical group 0.000 claims 4
- 125000005041 acyloxyalkyl group Chemical group 0.000 claims 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 125000004001 thioalkyl group Chemical group 0.000 claims 4
- 241000699666 Mus <mouse, genus> Species 0.000 claims 3
- 210000003719 b-lymphocyte Anatomy 0.000 claims 3
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 2
- 241000699670 Mus sp. Species 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 239000002831 pharmacologic agent Substances 0.000 claims 2
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 208000020674 atypical lymphoproliferative disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- WIAGFHVCTJFWDT-ASDRUYPJSA-N chembl140442 Chemical compound O=C([C@@H]1CCCCN1C(=O)C1=O)O[C@H]([C@H](C)C[C@@H](CCO)CCC(=O)OC)CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(/C)[C@@H](OC)C[C@@H]2CC[C@@H](C)[C@@]1(O)O2 WIAGFHVCTJFWDT-ASDRUYPJSA-N 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000008029 eradication Effects 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 210000002751 lymph Anatomy 0.000 claims 1
- 230000001926 lymphatic effect Effects 0.000 claims 1
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000000116 mitigating effect Effects 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 208000002491 severe combined immunodeficiency Diseases 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17608600P | 2000-01-14 | 2000-01-14 | |
| US60/176,086 | 2000-01-14 | ||
| PCT/US2001/001537 WO2001051049A1 (en) | 2000-01-14 | 2001-01-12 | O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008000081A Division JP5184894B2 (ja) | 2000-01-14 | 2008-01-04 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
| JP2009269988A Division JP5180177B2 (ja) | 2000-01-14 | 2009-11-27 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003519655A JP2003519655A (ja) | 2003-06-24 |
| JP2003519655A5 true JP2003519655A5 (https=) | 2005-09-22 |
Family
ID=22642913
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001551473A Withdrawn JP2003519655A (ja) | 2000-01-14 | 2001-01-12 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
| JP2008000081A Expired - Lifetime JP5184894B2 (ja) | 2000-01-14 | 2008-01-04 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
| JP2009269988A Expired - Lifetime JP5180177B2 (ja) | 2000-01-14 | 2009-11-27 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008000081A Expired - Lifetime JP5184894B2 (ja) | 2000-01-14 | 2008-01-04 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
| JP2009269988A Expired - Lifetime JP5180177B2 (ja) | 2000-01-14 | 2009-11-27 | リンパ増殖症候群の緩和および阻害のためのｏ−メチル化ラパマイシン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (5) | US7754734B2 (https=) |
| EP (2) | EP2298299A3 (https=) |
| JP (3) | JP2003519655A (https=) |
| AT (1) | ATE475418T1 (https=) |
| AU (2) | AU2001230956B2 (https=) |
| CA (1) | CA2397354C (https=) |
| DE (1) | DE60142677D1 (https=) |
| ES (1) | ES2349458T3 (https=) |
| WO (1) | WO2001051049A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6890546B2 (en) | 1998-09-24 | 2005-05-10 | Abbott Laboratories | Medical devices containing rapamycin analogs |
| EP2298299A3 (en) * | 2000-01-14 | 2012-02-29 | The Trustees Of The University Of Pennsylvania | O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders |
| PL409579A1 (pl) * | 2001-02-19 | 2015-03-02 | Novartis Ag | Leczenie raka |
| AU2011226833B9 (en) * | 2001-02-19 | 2014-07-03 | Novartis Ag | Cancer treatment |
| US7682387B2 (en) | 2002-04-24 | 2010-03-23 | Biosensors International Group, Ltd. | Drug-delivery endovascular stent and method for treating restenosis |
| US6939376B2 (en) * | 2001-11-05 | 2005-09-06 | Sun Biomedical, Ltd. | Drug-delivery endovascular stent and method for treating restenosis |
| US20040024450A1 (en) * | 2002-04-24 | 2004-02-05 | Sun Biomedical, Ltd. | Drug-delivery endovascular stent and method for treating restenosis |
| US7169404B2 (en) * | 2003-07-30 | 2007-01-30 | Advanced Cardiovasular Systems, Inc. | Biologically absorbable coatings for implantable devices and methods for fabricating the same |
| US7901451B2 (en) | 2004-09-24 | 2011-03-08 | Biosensors International Group, Ltd. | Drug-delivery endovascular stent and method for treating restenosis |
| US20080097591A1 (en) | 2006-10-20 | 2008-04-24 | Biosensors International Group | Drug-delivery endovascular stent and method of use |
| US8067055B2 (en) * | 2006-10-20 | 2011-11-29 | Biosensors International Group, Ltd. | Drug-delivery endovascular stent and method of use |
| US20080103584A1 (en) * | 2006-10-25 | 2008-05-01 | Biosensors International Group | Temporal Intraluminal Stent, Methods of Making and Using |
| KR100930167B1 (ko) * | 2007-09-19 | 2009-12-07 | 삼성전기주식회사 | 초광각 광학계 |
| US20110098241A1 (en) * | 2008-04-14 | 2011-04-28 | Poniard Pharmaceuticals, Inc. | Rapamycin analogs as anti-cancer agents |
| EP2365802B1 (en) | 2008-11-11 | 2017-08-02 | The Board of Regents,The University of Texas System | Microcapsules of rapamycin and use for treating cancer |
| US9283211B1 (en) | 2009-11-11 | 2016-03-15 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
| US20170079962A1 (en) | 2009-11-11 | 2017-03-23 | Rapamycin Holdings, Llc | Oral Rapamycin Preparation and Use for Stomatitus |
| CN102268015B (zh) * | 2011-08-30 | 2013-08-28 | 成都摩尔生物医药有限公司 | 一种依维莫司的合成方法 |
| US20150290176A1 (en) | 2012-10-12 | 2015-10-15 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
| EP2968281B1 (en) | 2013-03-13 | 2020-08-05 | The Board of Regents of The University of Texas System | Mtor inhibitors for prevention of intestinal polyp growth |
| US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
| AU2014373683B2 (en) | 2013-12-31 | 2020-05-07 | Rapamycin Holdings, Llc | Oral rapamycin nanoparticle preparations and use |
| CN105254646A (zh) * | 2014-05-28 | 2016-01-20 | 上海博邦医药科技有限公司 | 一种制备依维莫司的方法 |
| JP6716139B2 (ja) | 2015-01-19 | 2020-07-01 | 学校法人慶應義塾 | 内耳性難聴治療薬 |
| JP2020507632A (ja) * | 2017-02-10 | 2020-03-12 | マウント タム セラピューティクス, インコーポレイテッドMount Tam Therapeutics, Inc. | ラパマイシン類似体 |
| EP3848065B1 (en) | 2017-05-15 | 2023-07-26 | C. R. Bard, Inc. | Medical device with drug-eluting coating and intermediate layer |
| EP3880266B1 (en) | 2018-11-14 | 2025-05-07 | Lutonix, Inc. | Medical device with drug-eluting coating on modified device surface |
| CN109776571B (zh) * | 2019-01-31 | 2021-06-11 | 哈药慈航制药股份有限公司 | 一种雷帕霉素类似物及其制备方法和应用 |
| WO2020209828A1 (en) | 2019-04-08 | 2020-10-15 | Bard Peripheral Vascular, Inc. | Medical device with drug-eluting coating on modified device surface |
| CN110917194A (zh) * | 2019-11-07 | 2020-03-27 | 福建省微生物研究所 | 雷帕霉素噻唑类衍生物在制备抗阿尔茨海默症药物中的应用 |
| CN113653305B (zh) * | 2021-09-07 | 2024-11-05 | 中国五冶集团有限公司 | 一种电动顶升操作平台 |
| CN115323915B (zh) * | 2022-10-17 | 2023-01-06 | 广州市市政工程试验检测有限公司 | 一种桥梁索杆检测与修复机器人 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5206018A (en) * | 1978-11-03 | 1993-04-27 | Ayerst, Mckenna & Harrison, Inc. | Use of rapamycin in treatment of tumors |
| US4401653A (en) * | 1981-03-09 | 1983-08-30 | Ayerst, Mckenna & Harrison Inc. | Combination of rapamycin and picibanil for the treatment of tumors |
| US4699783A (en) * | 1983-03-11 | 1987-10-13 | Terman David S | Products and methods for treatment of cancer |
| ATE135583T1 (de) * | 1991-06-18 | 1996-04-15 | American Home Prod | Verwendung von rapamycin zur behandlung von t- zellen lymphom/leukämie bei erwachsenen |
| 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 |
| US5527907A (en) * | 1993-11-19 | 1996-06-18 | Abbott Laboratories | Macrolide immunomodulators |
| US5525610A (en) * | 1994-03-31 | 1996-06-11 | American Home Products Corporation | 42-Epi-rapamycin and pharmaceutical compositions thereof |
| ATE233098T1 (de) * | 1996-06-11 | 2003-03-15 | Novartis Ag | Kombination eines somatostatin analogs und eines rapamycins |
| JP3352411B2 (ja) * | 1998-03-05 | 2002-12-03 | 株式会社東芝 | 制御システム、電力系統保護制御システムおよびプログラムを記憶した記憶媒体 |
| JP2002544167A (ja) | 1999-05-10 | 2002-12-24 | ノバルティス アクチエンゲゼルシャフト | 有機化合物 |
| EP2298299A3 (en) * | 2000-01-14 | 2012-02-29 | The Trustees Of The University Of Pennsylvania | O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders |
| EP1319008B1 (en) * | 2000-09-19 | 2008-10-15 | Wyeth | Water soluble rapamycin esters |
| US6399625B1 (en) * | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
| US6440991B1 (en) * | 2000-10-02 | 2002-08-27 | Wyeth | Ethers of 7-desmethlrapamycin |
| US6399626B1 (en) * | 2000-10-02 | 2002-06-04 | Wyeth | Hydroxyesters of 7-desmethylrapamycin |
-
2001
- 2001-01-12 EP EP10007811A patent/EP2298299A3/en not_active Withdrawn
- 2001-01-12 WO PCT/US2001/001537 patent/WO2001051049A1/en not_active Ceased
- 2001-01-12 ES ES01903095T patent/ES2349458T3/es not_active Expired - Lifetime
- 2001-01-12 AU AU2001230956A patent/AU2001230956B2/en not_active Expired
- 2001-01-12 AU AU3095601A patent/AU3095601A/xx active Pending
- 2001-01-12 AT AT01903095T patent/ATE475418T1/de not_active IP Right Cessation
- 2001-01-12 JP JP2001551473A patent/JP2003519655A/ja not_active Withdrawn
- 2001-01-12 EP EP01903095A patent/EP1250135B1/en not_active Expired - Lifetime
- 2001-01-12 CA CA2397354A patent/CA2397354C/en not_active Expired - Lifetime
- 2001-01-12 DE DE60142677T patent/DE60142677D1/de not_active Expired - Lifetime
-
2002
- 2002-07-09 US US10/192,193 patent/US7754734B2/en not_active Expired - Lifetime
-
2007
- 2007-09-07 US US11/899,673 patent/US7781447B2/en not_active Expired - Fee Related
-
2008
- 2008-01-04 JP JP2008000081A patent/JP5184894B2/ja not_active Expired - Lifetime
-
2009
- 2009-11-27 JP JP2009269988A patent/JP5180177B2/ja not_active Expired - Lifetime
-
2010
- 2010-06-07 US US12/795,335 patent/US8569332B2/en not_active Expired - Fee Related
- 2010-06-09 US US12/797,085 patent/US8759370B2/en not_active Expired - Fee Related
- 2010-07-06 US US12/830,883 patent/US8778961B2/en not_active Expired - Fee Related
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