RU2355399C2 - Противоопухолевые композиции, содержащие производное рапамицина и ингибитор ароматазы - Google Patents
Противоопухолевые композиции, содержащие производное рапамицина и ингибитор ароматазы Download PDFInfo
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- RU2355399C2 RU2355399C2 RU2005130767/14A RU2005130767A RU2355399C2 RU 2355399 C2 RU2355399 C2 RU 2355399C2 RU 2005130767/14 A RU2005130767/14 A RU 2005130767/14A RU 2005130767 A RU2005130767 A RU 2005130767A RU 2355399 C2 RU2355399 C2 RU 2355399C2
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- cci
- letrozole
- combination
- aromatase inhibitor
- treatment
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- 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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- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
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- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US45228903P | 2003-03-05 | 2003-03-05 | |
| US60/452,289 | 2003-03-05 |
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| RU2005130767A RU2005130767A (ru) | 2006-02-10 |
| RU2355399C2 true RU2355399C2 (ru) | 2009-05-20 |
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| RU2005130767/14A RU2355399C2 (ru) | 2003-03-05 | 2004-03-01 | Противоопухолевые композиции, содержащие производное рапамицина и ингибитор ароматазы |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2707285C2 (ru) * | 2013-10-08 | 2019-11-26 | ЭйАй ТЕРАПЬЮТИКС, ИНК. | Рапамицин для лечения лимфангиолейомиоматоза |
| US11103449B2 (en) | 2014-04-04 | 2021-08-31 | AI Therapeutics, Inc. | Inhalable rapamycin formulation for treating age-related conditions |
| US11491143B2 (en) | 2014-10-07 | 2022-11-08 | AI Therapeutics, Inc. | Inhalable rapamycin formulation for the treatment of pulmonary hypertension |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI233359B (en) * | 2001-04-06 | 2005-06-01 | Wyeth Corp | Pharmaceutical composition for treating neoplasm |
| ZA200603888B (en) * | 2001-06-01 | 2007-05-30 | Wyeth Corp | Antineoplastic combinations |
| CN1829514A (zh) * | 2003-07-25 | 2006-09-06 | 惠氏公司 | Cci－779冻干制剂 |
| RU2006122517A (ru) * | 2004-01-08 | 2008-02-20 | Вайет (Us) | Фармацевтический состав для прямого прессования, предназначенный для перорального введения cci-779 |
| AR047988A1 (es) * | 2004-03-11 | 2006-03-15 | Wyeth Corp | Combinaciones antineoplásicas de cci-779 y rituximab |
| MX2007005153A (es) * | 2004-10-28 | 2007-06-26 | Wyeth Corp | Uso de un inhibidor del mtor en el tratamiento de leiomioma del utero. |
| DE602006021142D1 (de) | 2005-02-03 | 2011-05-19 | Gen Hospital Corp | Verfahren zur behandlung von gefitinib-resistentem krebs |
| PE20070763A1 (es) * | 2005-11-04 | 2007-08-08 | Wyeth Corp | COMBINACIONES ANTINEOPLASICAS DE UN INHIBIDOR DE mTOR, TRASTUZUMAB Y/O HKI-272 |
| CA2629245C (en) * | 2005-11-21 | 2016-07-12 | Novartis Ag | Neuroendocrine tumor treatment |
| DE102006008074B4 (de) * | 2006-02-22 | 2013-08-14 | RUHR-UNIVERSITäT BOCHUM | Behandlung von Krebs mit Geruchsrezeptor-Liganden |
| DE102006011507A1 (de) * | 2006-03-14 | 2007-09-20 | Lts Lohmann Therapie-Systeme Ag | Wirkstoffbeladene Nanopartikel auf Basis hydrophiler Proteine |
| US20100081681A1 (en) * | 2006-08-16 | 2010-04-01 | Blagosklonny Mikhail V | Methods and compositions for preventing or treating age-related diseases |
| US8414526B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
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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 |
| US8414525B2 (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 |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| TW200901989A (en) * | 2007-04-10 | 2009-01-16 | Wyeth Corp | Anti-tumor activity of CCI-779 in papillary renal cell cancer |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| ES2692769T3 (es) | 2008-06-17 | 2018-12-05 | Wyeth Llc | Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina |
| CN109464445A (zh) | 2008-08-04 | 2019-03-15 | 惠氏有限责任公司 | 4-苯胺基-3-氰基喹啉和卡培他滨的抗肿瘤组合 |
| WO2010024898A2 (en) | 2008-08-29 | 2010-03-04 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| US20110212977A1 (en) * | 2008-11-11 | 2011-09-01 | Eli Lilly And Company | P70 s6 kinase inhibitor and mtor inhibitor combination therapy |
| LT3000467T (lt) | 2009-04-06 | 2023-04-11 | Wyeth Llc | Krūties vėžio gydymo schema naudojant neratinibą |
| WO2010118419A2 (en) * | 2009-04-10 | 2010-10-14 | Haiyan Qi | Novel anti-aging agents and methods to identify them |
| JP6091431B2 (ja) * | 2011-01-31 | 2017-03-15 | ルコラス−エム．ディー．リミテッド | 医薬的使用 |
| US9682066B2 (en) * | 2012-12-04 | 2017-06-20 | University Of Cincinnati | Methods of treating primary brain tumors by administering letrozole |
| WO2015014284A1 (zh) * | 2013-07-31 | 2015-02-05 | 北京盛诺基医药科技有限公司 | 一种乳腺癌的治疗方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5A (en) * | 1836-08-10 | Thomas Blanchard | Machine for mortising solid wooden shells of ships' tackle-blocks | |
| US6A (en) * | 1836-08-10 | Thomas Blanchard | Machine for forming end pieces of plank blocks for ships | |
| RU2126409C1 (ru) * | 1992-10-13 | 1999-02-20 | Американ Хоум Продактс Корпорейшн | Производные рапамицина, фармацевтическая композиция и способ стимулирования иммунодепрессии |
| RU2134267C1 (ru) * | 1994-04-18 | 1999-08-10 | Американ Хоум Продактс Корпорейшн | Гидроксиэфиры рапамицина, способ их получения и способы лечения |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) * | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US3993749A (en) * | 1974-04-12 | 1976-11-23 | Ayerst Mckenna And Harrison Ltd. | Rapamycin and process of preparation |
| US5066493A (en) * | 1978-11-03 | 1991-11-19 | American Home Products Corporation | Rapamycin in treatment of tumors |
| US4885171A (en) * | 1978-11-03 | 1989-12-05 | American Home Products Corporation | Use of rapamycin in treatment of certain tumors |
| 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 |
| US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
| US5078999A (en) * | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
| US5080899A (en) * | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
| US5321009A (en) * | 1991-04-03 | 1994-06-14 | American Home Products Corporation | Method of treating diabetes |
| IL102414A (en) * | 1991-07-25 | 1996-08-04 | Univ Louisville Res Found | Medicinal preparations for the treatment of ocular inflammation, containing rapamycin |
| US5286731A (en) * | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory bowel disease |
| US5286730A (en) * | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory disease |
| US5516781A (en) * | 1992-01-09 | 1996-05-14 | American Home Products Corporation | Method of treating restenosis with rapamycin |
| US5288711A (en) * | 1992-04-28 | 1994-02-22 | American Home Products Corporation | Method of treating hyperproliferative vascular disease |
| US5561138A (en) * | 1994-12-13 | 1996-10-01 | American Home Products Corporation | Method of treating anemia |
| US5496832A (en) * | 1995-03-09 | 1996-03-05 | American Home Products Corporation | Method of treating cardiac inflammatory disease |
| US6002008A (en) * | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6277983B1 (en) * | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| PT1318837E (pt) * | 2000-08-11 | 2004-12-31 | Wyeth Corp | Metodo de tratamenton de carcinoma positivo a receptor de estrogenio |
| TWI286074B (en) * | 2000-11-15 | 2007-09-01 | Wyeth Corp | Pharmaceutical composition containing CCI-779 as an antineoplastic agent |
| CZ309178B6 (cs) * | 2001-02-19 | 2022-04-20 | Novartis Pharma Ag | 40-O-(2-hydroxyethyl)rapamycin pro použití při léčení |
| TWI233359B (en) * | 2001-04-06 | 2005-06-01 | Wyeth Corp | Pharmaceutical composition for treating neoplasm |
| DE60228699D1 (de) * | 2001-04-06 | 2008-10-16 | Wyeth Corp | Antineoplastische kombinationspräparate enthaltend cci-779 (rapamycin derivat) zusammen mit gemcitabin oder fluoro-uracil |
| TWI296196B (en) * | 2001-04-06 | 2008-05-01 | Wyeth Corp | Antineoplastic combinations |
| PL367267A1 (en) * | 2001-06-01 | 2005-02-21 | Wyeth | Antineoplastic combinations |
| US20030008923A1 (en) * | 2001-06-01 | 2003-01-09 | Wyeth | Antineoplastic combinations |
| UA77200C2 (en) * | 2001-08-07 | 2006-11-15 | Wyeth Corp | Antineoplastic combination of cci-779 and bkb-569 |
-
2004
- 2004-01-03 UA UAA200509283A patent/UA83484C2/uk unknown
- 2004-02-26 AR ARP040100603A patent/AR043403A1/es unknown
- 2004-03-01 MX MXPA05009246A patent/MXPA05009246A/es not_active Application Discontinuation
- 2004-03-01 KR KR1020057016528A patent/KR20050109965A/ko not_active Ceased
- 2004-03-01 EP EP04716169A patent/EP1603561A2/en not_active Withdrawn
- 2004-03-01 RU RU2005130767/14A patent/RU2355399C2/ru not_active IP Right Cessation
- 2004-03-01 WO PCT/US2004/006354 patent/WO2004078133A2/en not_active Ceased
- 2004-03-01 NZ NZ542738A patent/NZ542738A/xx unknown
- 2004-03-01 CA CA002516353A patent/CA2516353A1/en not_active Abandoned
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- 2004-03-01 JP JP2006509002A patent/JP2006519862A/ja active Pending
- 2004-03-01 BR BRPI0408024-6A patent/BRPI0408024A/pt not_active IP Right Cessation
- 2004-03-01 US US10/790,488 patent/US20040176339A1/en not_active Abandoned
- 2004-03-01 AU AU2004218439A patent/AU2004218439A1/en not_active Withdrawn
- 2004-03-02 TW TW093105371A patent/TW200529829A/zh unknown
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- 2005-09-01 NI NI200500148A patent/NI200500148A/es unknown
- 2005-09-05 EC EC2005006001A patent/ECSP056001A/es unknown
- 2005-09-06 NO NO20054133A patent/NO20054133L/no not_active Application Discontinuation
- 2005-10-04 ZA ZA200508029A patent/ZA200508029B/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5A (en) * | 1836-08-10 | Thomas Blanchard | Machine for mortising solid wooden shells of ships' tackle-blocks | |
| US6A (en) * | 1836-08-10 | Thomas Blanchard | Machine for forming end pieces of plank blocks for ships | |
| RU2126409C1 (ru) * | 1992-10-13 | 1999-02-20 | Американ Хоум Продактс Корпорейшн | Производные рапамицина, фармацевтическая композиция и способ стимулирования иммунодепрессии |
| RU2134267C1 (ru) * | 1994-04-18 | 1999-08-10 | Американ Хоум Продактс Корпорейшн | Гидроксиэфиры рапамицина, способ их получения и способы лечения |
Non-Patent Citations (3)
| Title |
|---|
| реферат. * |
| формула, реферат. * |
| формула. * |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2707285C2 (ru) * | 2013-10-08 | 2019-11-26 | ЭйАй ТЕРАПЬЮТИКС, ИНК. | Рапамицин для лечения лимфангиолейомиоматоза |
| US11123289B2 (en) | 2013-10-08 | 2021-09-21 | AI Therapeutics, Inc. | Rapamycin for the treatment of lymphangioleiomyomatosis |
| US11744797B2 (en) | 2013-10-08 | 2023-09-05 | AI Therapeutics, Inc. | Rapamycin for the treatment of lymphangioleiomyomatosis |
| US12171874B2 (en) | 2013-10-08 | 2024-12-24 | Orphai Therapeutics Inc. | Rapamycin for the treatment of lymphangioleiomyomatosis |
| US11103449B2 (en) | 2014-04-04 | 2021-08-31 | AI Therapeutics, Inc. | Inhalable rapamycin formulation for treating age-related conditions |
| US11648199B2 (en) | 2014-04-04 | 2023-05-16 | Al Therapeutics, Inc. | Inhalable rapamycin formulation for treating age-related conditions |
| US11491143B2 (en) | 2014-10-07 | 2022-11-08 | AI Therapeutics, Inc. | Inhalable rapamycin formulation for the treatment of pulmonary hypertension |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004078133A3 (en) | 2004-11-11 |
| UA83484C2 (uk) | 2008-07-25 |
| EP1603561A2 (en) | 2005-12-14 |
| AR043403A1 (es) | 2005-07-27 |
| NZ542738A (en) | 2009-02-28 |
| CA2516353A1 (en) | 2004-09-16 |
| NI200500148A (es) | 2006-03-30 |
| TW200529829A (en) | 2005-09-16 |
| ZA200508029B (en) | 2007-04-25 |
| US20040176339A1 (en) | 2004-09-09 |
| RU2005130767A (ru) | 2006-02-10 |
| JP2006519862A (ja) | 2006-08-31 |
| ECSP056001A (es) | 2006-01-27 |
| KR20050109965A (ko) | 2005-11-22 |
| AU2004218439A1 (en) | 2004-09-16 |
| MXPA05009246A (es) | 2005-10-19 |
| BRPI0408024A (pt) | 2006-02-14 |
| CR7942A (es) | 2006-02-07 |
| NO20054133D0 (no) | 2005-09-06 |
| WO2004078133A2 (en) | 2004-09-16 |
| NO20054133L (no) | 2005-10-03 |
| WO2004078133A8 (en) | 2005-09-01 |
| CN1756549A (zh) | 2006-04-05 |
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