RU96124399A - Водорастворимые сложные эфиры рапамицина, фармацевтическая композиция и способы лечения - Google Patents
Водорастворимые сложные эфиры рапамицина, фармацевтическая композиция и способы леченияInfo
- Publication number
- RU96124399A RU96124399A RU96124399/04A RU96124399A RU96124399A RU 96124399 A RU96124399 A RU 96124399A RU 96124399/04 A RU96124399/04 A RU 96124399/04A RU 96124399 A RU96124399 A RU 96124399A RU 96124399 A RU96124399 A RU 96124399A
- Authority
- RU
- Russia
- Prior art keywords
- och
- mammal
- hydrogen
- compound
- coch
- Prior art date
Links
- QFJCIRLUMZQUOT-HPLJOQBZSA-N Sirolimus Chemical compound 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 title claims 2
- 150000002148 esters Chemical class 0.000 title claims 2
- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- 229960002930 sirolimus Drugs 0.000 title claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 241000124008 Mammalia Species 0.000 claims 12
- -1 methoxypolyethylene glycol thiol Chemical class 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 230000000843 anti-fungal Effects 0.000 claims 1
- 230000003110 anti-inflammatory Effects 0.000 claims 1
- 230000001028 anti-proliferant Effects 0.000 claims 1
- 230000003409 anti-rejection Effects 0.000 claims 1
- 230000000259 anti-tumor Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000009030 carcinoma Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 0 CC(C[C@](C)C=CC=CC=C(C)[C@](CC(CCC1=C)OC1(*)C(C(C(CCCC1)[C@@]1C(O[C@](*CC(CC1)C[C@@](*)C1O)CC([C@](*)C=C(C)[C@@]([C@]1O)O)O)=O)=O)=O)O)C1=O Chemical compound CC(C[C@](C)C=CC=CC=C(C)[C@](CC(CCC1=C)OC1(*)C(C(C(CCCC1)[C@@]1C(O[C@](*CC(CC1)C[C@@](*)C1O)CC([C@](*)C=C(C)[C@@]([C@]1O)O)O)=O)=O)=O)O)C1=O 0.000 description 1
Claims (16)
2. Соединение по п.1, в котором n = 8-200.
3. Соединение по п.1, в котором n = 8-135.
4. Соединение по п.1, в котором n = 8-20.
5. Соединение по п.1, в котором n = 90-120.
6. Соединение по п.16, представляющее собой 31,42- диэфир с метоксиполиэтиленгликольтиолом 5000.
7. Соединение по п. 1, представляющее собой 42-эфир с метоксиполиэтиленгликольтиолом 5000.
8. Соединение по п. 1, представляющее собой 4-эфир с метоксиполиэтиленгликольтиолом 750.
9. Способ лечения отторжения трансплантата или реакции несовместимости у млекопитающего, отличающийся тем, что включает введение млекопитающему эффективного против отторжения количества соединения формулы
где R1 и R2 каждый независимо представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что оба R1 и R2 не являются водородом.
где R1 и R2 каждый независимо представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что оба R1 и R2 не являются водородом.
10. Способ лечения грибковой инфекции у млекопитающего, отличающийся тем, что включает введение этому млекопитающему противогрибкового эффективного количества соединения формулы
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что оба R1 и R2 не являются водородом.
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что оба R1 и R2 не являются водородом.
11. Способ лечения ревматоидного артрита млекопитающего, отличающийся тем, что включает введение этому млекопитающему эффективного против артрита количества соединения формулы
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-250,
при условии, что оба R1 и R2 не являются водородом.
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-250,
при условии, что оба R1 и R2 не являются водородом.
12. Способ лечения растеноза в млекопитающем, отличающийся тем, что включает введение этому млекопитающему антипролиферативного эффективного количества соединения формулы
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CHр2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CHр2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
13. Способ лечения воспаления легких в млекопитающем, отличающийся тем, что включает введение этому млекопитающему противовоспалительного эффективного количества соединения формулы
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2) -CH2-О-СН2 СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2) -CH2-О-СН2 СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
14. Способ лечения твердых опухолей в млекопитающем, отличающийся тем, что включает введение этому млекопитающему противоопухолевого эффективного количества соединения формулы
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
где R1 и R2, каждый независимо, представляют собой водород или -COCH2-S-CH2СН2-О-СН2-(СН2ОСН2)n -CH2-О-СН2СН2-ОСН3,
n = 8-450,
при условии, что R1 и R2 оба не являются водородом.
15. Способ по п. 14, отличающийся тем, что твердая опухоль является карциномой или саркомой.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US933895P | 1995-12-27 | 1995-12-27 | |
US60/009,338 | 1995-12-27 |
Publications (2)
Publication Number | Publication Date |
---|---|
RU96124399A true RU96124399A (ru) | 1999-02-20 |
RU2160739C2 RU2160739C2 (ru) | 2000-12-20 |
Family
ID=21737027
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU96124399/04A RU2160739C2 (ru) | 1995-12-27 | 1996-12-25 | Сложные эфиры рапамицина |
Country Status (27)
Country | Link |
---|---|
US (2) | US5780462A (ru) |
EP (1) | EP0781776B1 (ru) |
JP (1) | JP4080560B2 (ru) |
KR (1) | KR100444003B1 (ru) |
CN (1) | CN1088710C (ru) |
AR (1) | AR005421A1 (ru) |
AT (1) | ATE233769T1 (ru) |
AU (1) | AU702750B2 (ru) |
BR (1) | BR9606173A (ru) |
CA (1) | CA2193329C (ru) |
CY (1) | CY2377B1 (ru) |
CZ (1) | CZ293711B6 (ru) |
DE (1) | DE69626481T2 (ru) |
DK (1) | DK0781776T3 (ru) |
ES (1) | ES2189858T3 (ru) |
HK (1) | HK1002864A1 (ru) |
HU (1) | HUP9603582A3 (ru) |
IL (1) | IL119921A (ru) |
MX (1) | MX9606716A (ru) |
NO (1) | NO308303B1 (ru) |
NZ (1) | NZ299974A (ru) |
PT (1) | PT781776E (ru) |
RU (1) | RU2160739C2 (ru) |
SI (1) | SI0781776T1 (ru) |
SK (1) | SK283912B6 (ru) |
TW (1) | TW403753B (ru) |
ZA (1) | ZA9610892B (ru) |
Families Citing this family (133)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT1293795B1 (it) * | 1997-07-28 | 1999-03-10 | Angelini Ricerche Spa | Farmaco attivo nel ridurre la produzione di proteina mcp-1 |
US6015809A (en) * | 1998-08-17 | 2000-01-18 | American Home Products Corporation | Photocyclized rapamycin |
US7276506B2 (en) * | 1998-12-28 | 2007-10-02 | 4 Aza Bioscience Nv | Immunosuppressive effects of pteridine derivatives |
US6946465B2 (en) * | 1999-02-02 | 2005-09-20 | 4 Aza Bioscience Nv | Immunosuppressive effects of pteridine derivatives |
US6365385B1 (en) | 1999-03-22 | 2002-04-02 | Duke University | Methods of culturing and encapsulating pancreatic islet cells |
US6303355B1 (en) * | 1999-03-22 | 2001-10-16 | Duke University | Method of culturing, cryopreserving and encapsulating pancreatic islet cells |
US6331547B1 (en) | 1999-08-18 | 2001-12-18 | American Home Products Corporation | Water soluble SDZ RAD esters |
WO2001012633A1 (en) * | 1999-08-18 | 2001-02-22 | American Home Products Corporation | Water soluble sdz-rad esters |
WO2001068134A2 (en) * | 2000-03-14 | 2001-09-20 | Genetics Institute, Inc. | Therapies that improve graft survival, using antibodies against a b7 antigen |
WO2001068133A1 (en) * | 2000-03-14 | 2001-09-20 | Genetics Institute, Inc. | Use of rapamycin and agents that inhibit b7 activity in immunomodulation |
US7300662B2 (en) * | 2000-05-12 | 2007-11-27 | Cordis Corporation | Drug/drug delivery systems for the prevention and treatment of vascular disease |
US8236048B2 (en) | 2000-05-12 | 2012-08-07 | Cordis Corporation | Drug/drug delivery systems for the prevention and treatment of vascular disease |
US6670355B2 (en) | 2000-06-16 | 2003-12-30 | Wyeth | Method of treating cardiovascular disease |
ATE278421T1 (de) | 2000-08-11 | 2004-10-15 | Wyeth Corp | Verfahren zur behandlung eines östrogenrezeptor positives karzinoms |
EP1319008B1 (en) * | 2000-09-19 | 2008-10-15 | Wyeth | Water soluble rapamycin esters |
US6399625B1 (en) | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
US8303609B2 (en) | 2000-09-29 | 2012-11-06 | Cordis Corporation | Coated medical devices |
US6399626B1 (en) | 2000-10-02 | 2002-06-04 | Wyeth | Hydroxyesters of 7-desmethylrapamycin |
US6440991B1 (en) | 2000-10-02 | 2002-08-27 | Wyeth | Ethers of 7-desmethlrapamycin |
US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
EP1521828B1 (en) | 2002-07-16 | 2015-07-01 | Buck Institute for Research on Aging | Production of polyketides |
RU2344821C2 (ru) | 2002-07-30 | 2009-01-27 | Уайт | Парентеральные композиции, содержащие гидроксиэфиры рапамицина |
JP2006524289A (ja) * | 2003-04-23 | 2006-10-26 | ワイス・ホールディングズ・コーポレイション | Peg−ワートマニンコンジュゲート |
EP1663244B1 (en) * | 2003-09-12 | 2007-08-15 | 4 Aza Ip Nv | Pteridine derivatives for the treatment of tnf-alpha-related diseases. |
US20070032477A1 (en) * | 2003-10-17 | 2007-02-08 | Waer Mark J A | Pteridine derivatives useful for making pharmaceutical compositions |
MXPA06011881A (es) | 2004-04-14 | 2006-12-14 | Wyeth Corp | Sintesis regioespecifica de derivados de ester-42 de rapamicina. |
DE602005010228D1 (de) * | 2004-04-14 | 2008-11-20 | Wyeth Corp | Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörper |
AU2005238493A1 (en) * | 2004-04-27 | 2005-11-10 | Wyeth | Labeling of rapamycin using rapamycin-specific methylases |
GB0417852D0 (en) | 2004-08-11 | 2004-09-15 | Biotica Tech Ltd | Production of polyketides and other natural products |
KR20070083941A (ko) * | 2004-10-04 | 2007-08-24 | 큐엘티 유에스에이, 인코포레이티드 | 중합체 전달 조성을 갖는 눈 전달 |
US8313763B2 (en) * | 2004-10-04 | 2012-11-20 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of rapamycin compounds |
MX2007005153A (es) * | 2004-10-28 | 2007-06-26 | Wyeth Corp | Uso de un inhibidor del mtor en el tratamiento de leiomioma del utero. |
GB0428475D0 (en) * | 2004-12-30 | 2005-02-02 | 4 Aza Bioscience Nv | Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders |
GB0503936D0 (en) | 2005-02-25 | 2005-04-06 | San Raffaele Centro Fond | Method |
CA2602010A1 (en) | 2005-03-07 | 2006-09-14 | Wyeth | Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin |
US20100061994A1 (en) * | 2005-03-11 | 2010-03-11 | Rose Mary Sheridan | Medical uses of 39-desmethoxyrapamycin and analogues thereof |
GB0504994D0 (en) | 2005-03-11 | 2005-04-20 | Biotica Tech Ltd | Novel compounds |
CA2599547A1 (en) | 2005-03-11 | 2006-09-14 | Biotica Technology Limited | Medical uses of 39-desmethoxyrapamycin and analogues thereof |
US8232278B2 (en) * | 2005-06-24 | 2012-07-31 | Gilead Sciences, Inc. | Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C |
SI1912675T1 (sl) | 2005-07-25 | 2014-07-31 | Emergent Product Development Seattle, Llc | zmanjšanje števila celic B z uporabo molekul, ki se specifično vežejo na CD37 in CD20 |
KR101354828B1 (ko) | 2005-11-04 | 2014-02-18 | 와이어쓰 엘엘씨 | mTOR 저해자, 헤르셉틴, 및/또는 HKI-272의항신생물성 조합 |
EP1962819A1 (en) * | 2005-12-20 | 2008-09-03 | Wyeth | Control of cci-779 dosage form stability through control of drug substance impurities |
EP1993610A2 (en) * | 2006-03-07 | 2008-11-26 | Wyeth | Process for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants |
GB0609962D0 (en) * | 2006-05-19 | 2006-06-28 | Biotica Tech Ltd | Novel compounds |
GB0609963D0 (en) * | 2006-05-19 | 2006-06-28 | Biotica Tech Ltd | Novel compounds |
WO2008009079A2 (en) * | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | Substituted pteridines useful for the treatment and prevention of viral infections |
US8338435B2 (en) * | 2006-07-20 | 2012-12-25 | Gilead Sciences, Inc. | Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections |
US20080051691A1 (en) * | 2006-08-28 | 2008-02-28 | Wyeth | Implantable shunt or catheter enabling gradual delivery of therapeutic agents |
TW200824713A (en) * | 2006-10-18 | 2008-06-16 | Wyeth Corp | Processes for the synthesis of individual isomers of mono-PEG CCI-779 |
US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
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 |
US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
US8414525B2 (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 |
US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
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 |
US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
WO2008083169A2 (en) * | 2006-12-26 | 2008-07-10 | The Johns Hopkins University | Compositions and methods for the treatment of immunologic disorders |
TW200840584A (en) * | 2006-12-26 | 2008-10-16 | Gilead Sciences Inc | Pyrido(3,2-d)pyrimidines useful for treating viral infections |
CA2673659A1 (en) * | 2006-12-27 | 2008-07-10 | The Johns Hopkins University | Methods of detecting and diagnosing inflamatory responses and disorders by determining the level of soluble b7-h4 |
US7989173B2 (en) * | 2006-12-27 | 2011-08-02 | The Johns Hopkins University | Detection and diagnosis of inflammatory disorders |
US20090142342A1 (en) * | 2006-12-27 | 2009-06-04 | Johns Hopkins University | B7-h4 receptor agonist compositions and methods for treating inflammation and auto-immune diseases |
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 |
US20100048913A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
JP5647098B2 (ja) | 2008-03-21 | 2014-12-24 | ザ ユニヴァーシティー オヴ シカゴ | オピオイド拮抗薬とmTOR阻害薬を用いた治療 |
EP2132228B1 (en) | 2008-04-11 | 2011-06-22 | Emergent Product Development Seattle, LLC | Cd37 immunotherapeutic and combination with bifunctional chemotherapeutic thereof |
US20110098241A1 (en) * | 2008-04-14 | 2011-04-28 | Poniard Pharmaceuticals, Inc. | Rapamycin analogs as anti-cancer agents |
WO2010024898A2 (en) | 2008-08-29 | 2010-03-04 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
CA2937492C (en) | 2008-11-11 | 2019-08-13 | The Board Of Regents Of The University Of Texas System | Inhibition of mammalian target of rapamycin |
AU2010210422A1 (en) | 2009-02-05 | 2011-08-18 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal CYP17 inhibitors/antiandrogens |
CA2754890C (en) | 2009-03-13 | 2018-01-16 | Piet Herdewijn | Bicyclic heterocycles |
US20120010144A1 (en) * | 2009-04-03 | 2012-01-12 | Ragheb Assaly | Peg-albumin composition having at least one protected thiol region as a platform for medications |
CN102666581A (zh) | 2009-08-31 | 2012-09-12 | 艾普利穆恩公司 | 用于抑制移植物排斥的方法和组合物 |
KR20120115237A (ko) | 2009-10-30 | 2012-10-17 | 어리어드 파마슈티칼스, 인코포레이티드 | 암 치료 방법 및 조성물 |
US9283211B1 (en) | 2009-11-11 | 2016-03-15 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
US20130195919A1 (en) | 2010-03-05 | 2013-08-01 | President And Fellows Of Harvard College | Induced dendritic cell compositions and uses thereof |
EP2563391B1 (en) | 2010-04-27 | 2020-08-26 | Roche Glycart AG | Combination therapy of an afucosylated cd20 antibody with a mtor inhibitor |
GB201012889D0 (en) | 2010-08-02 | 2010-09-15 | Univ Leuven Kath | Antiviral activity of novel bicyclic heterocycles |
GB201015411D0 (en) | 2010-09-15 | 2010-10-27 | Univ Leuven Kath | Anti-cancer activity of novel bicyclic heterocycles |
WO2012149014A1 (en) | 2011-04-25 | 2012-11-01 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
EP2532740A1 (en) | 2011-06-11 | 2012-12-12 | Michael Schmück | Antigen-specific CD4+ and CD8+ central-memory T cell preparations for adoptive T cell therapy |
WO2013013708A1 (en) | 2011-07-26 | 2013-01-31 | Fundació Institut D'investigació Biomèdica De Bellvitge | Treatment of acute rejection in renal transplant |
GB201115665D0 (en) | 2011-09-09 | 2011-10-26 | Univ Leuven Kath | Autoimmune and inflammatory disorder therapy |
GB201122305D0 (en) | 2011-12-23 | 2012-02-01 | Biotica Tech Ltd | Novel compound |
WO2013155487A1 (en) | 2012-04-12 | 2013-10-17 | Yale University | Vehicles for controlled delivery of different pharmaceutical agents |
US9750728B2 (en) | 2012-09-29 | 2017-09-05 | Targeted Therapeutics, Llc | Method and pharmaceutical composition for inhibiting PI3K/AKT/mTOR signaling pathway |
CN103705925B (zh) | 2012-09-29 | 2018-03-30 | 段磊 | 抑制PI3K/AKT/mTOR信号通路的药物组合 |
EP2906214A1 (en) | 2012-10-12 | 2015-08-19 | The Board of Regents of The University of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
US20150258127A1 (en) | 2012-10-31 | 2015-09-17 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for preventing antiphospholipid syndrome (aps) |
WO2014100483A1 (en) | 2012-12-19 | 2014-06-26 | Amplimmune, Inc. | Anti-human b7-h4 antibodies and their uses |
WO2014160328A1 (en) | 2013-03-13 | 2014-10-02 | The Board Of Regents Of The University Of Texas System | Mtor inhibitors for prevention of intestinal polyp growth |
BR112015023098A2 (pt) | 2013-03-14 | 2017-07-18 | Univ Jefferson | agentes de infrarregulação do receptor de andrógeno e usos dos mesmos |
EP2997373A1 (en) | 2013-05-17 | 2016-03-23 | MedImmune, LLC | Receptors for b7-h4 |
CN105636594A (zh) | 2013-08-12 | 2016-06-01 | 托凯药业股份有限公司 | 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物 |
US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
ES2900426T3 (es) | 2013-12-31 | 2022-03-16 | Rapamycin Holdings Llc | Preparaciones orales y uso de nanopartículas de rapamicina |
WO2015149001A1 (en) | 2014-03-27 | 2015-10-01 | The Brigham And Women's Hospital, Inc. | Metabolically-activated drug conjugates to overcome resistance in cancer therapy |
CA2968049A1 (en) | 2014-04-16 | 2015-10-22 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
EP3148564B1 (en) | 2014-06-02 | 2020-01-08 | Children's Medical Center Corporation | Methods and compositions for immunomodulation |
JP6692798B2 (ja) | 2014-09-11 | 2020-05-13 | ザ・リージエンツ・オブ・ザ・ユニバーシテイ・オブ・カリフオルニア | mTORC1阻害剤 |
KR101756050B1 (ko) | 2015-03-04 | 2017-07-07 | 길리애드 사이언시즈, 인코포레이티드 | 톨 유사 수용체 조정제 화합물 |
WO2017029391A1 (en) | 2015-08-20 | 2017-02-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | New method for treating cancer |
CN108351687B (zh) | 2015-09-04 | 2022-01-07 | 耶鲁大学 | 靶向胰腺和结肠的聚合胆汁酸纳米组合物 |
WO2017173453A1 (en) | 2016-04-01 | 2017-10-05 | The Brigham And Women's Hospital, Inc. | Stimuli-responsive nanoparticles for biomedical applications |
SI3507276T1 (sl) | 2016-09-02 | 2022-01-31 | Gilead Sciences, Inc. | Spojine modulatorja toličnih receptorjev |
US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
BR112019005292A2 (pt) | 2016-09-21 | 2019-09-03 | Nextcure Inc | anticorpos para siglec-15 e métodos de uso dos mesmos. |
EP4360714A2 (en) | 2016-09-21 | 2024-05-01 | Nextcure, Inc. | Antibodies for siglec-15 and methods of use thereof |
GB201701087D0 (en) | 2017-01-23 | 2017-03-08 | Univ Leuven Kath | Novel prodrugs of mizoribine |
CN110603038A (zh) | 2017-02-10 | 2019-12-20 | 塔姆山治疗公司 | 雷帕霉素类似物 |
EP3848065B1 (en) | 2017-05-15 | 2023-07-26 | C. R. Bard, Inc. | Medical device with drug-eluting coating and intermediate layer |
US20200129486A1 (en) | 2017-06-26 | 2020-04-30 | Inserm (Institut National De La Santé Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of olmsted syndrome |
EP3652306A1 (en) | 2017-07-13 | 2020-05-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for increasing expansion and immunosuppressive capacity of a population of cd8+cd45rclow/-tregs |
PE20212112A1 (es) | 2018-05-01 | 2021-11-04 | Revolution Medicines Inc | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor |
CA3098698A1 (en) | 2018-05-01 | 2019-11-07 | Revolution Medicines, Inc. | C26-linked rapamycin analogs as mtor inhibitors |
US20210115378A1 (en) | 2018-05-09 | 2021-04-22 | Yale University | Compositions and systems for ex vivo cell modulation and methods of use thereof |
EP3790592A1 (en) | 2018-05-09 | 2021-03-17 | Yale University | Particles for spatiotemporal release of agents |
EP3826650A4 (en) | 2018-07-23 | 2022-07-27 | Enclear Therapies, Inc. | METHODS OF TREATMENT OF NEUROLOGICAL DISEASES |
CN113164563A (zh) | 2018-07-23 | 2021-07-23 | 因柯利尔疗法公司 | 神经性病症的治疗方法 |
WO2020053125A1 (en) | 2018-09-10 | 2020-03-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of neurofibromatosis |
US11541152B2 (en) | 2018-11-14 | 2023-01-03 | Lutonix, Inc. | Medical device with drug-eluting coating on modified device surface |
CA3123886A1 (en) | 2019-01-17 | 2020-07-23 | James DAHLMAN | Drug delivery systems containing oxidized cholesterols |
US20220176084A1 (en) | 2019-04-08 | 2022-06-09 | Bard Peripheral Vascular, Inc. | Medical device with drug-eluting coating on modified device surface |
JP2022526671A (ja) | 2019-04-11 | 2022-05-25 | エンクリアー セラピーズ, インク. | 脳脊髄液の改善の方法ならびにそのためのデバイスおよびシステム |
TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
TW202115056A (zh) | 2019-06-28 | 2021-04-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑化合物的製備方法 |
WO2021258042A1 (en) | 2020-06-19 | 2021-12-23 | Yale University | Polymeric bile acid ester nanoparticles comprising an immunomodulator agent to induce antigen-specific tolerance |
CA3223081A1 (en) | 2021-07-15 | 2023-01-19 | Samir Mitragotri | Compositions and methods relating to cells with adhered particles |
WO2024008799A1 (en) | 2022-07-06 | 2024-01-11 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of proliferative glomerulonephritis |
WO2024028433A1 (en) | 2022-08-04 | 2024-02-08 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of lymphoproliferative disorders |
Family Cites Families (56)
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 |
US4885171A (en) * | 1978-11-03 | 1989-12-05 | American Home Products Corporation | Use of rapamycin in treatment of certain tumors |
US4684728A (en) * | 1979-01-12 | 1987-08-04 | Bayer Aktiengesellschaft | Solubilizing biologically active compounds with reactive hydrogen atoms |
US4316885A (en) * | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
US4401653A (en) * | 1981-03-09 | 1983-08-30 | Ayerst, Mckenna & Harrison Inc. | Combination of rapamycin and picibanil for the treatment of tumors |
US4375464A (en) * | 1981-11-19 | 1983-03-01 | Ayerst, Mckenna & Harrison Inc. | Antibiotic AY24,668 and process of preparation |
EP0429436A3 (en) * | 1985-12-06 | 1991-12-27 | The University Of Kansas | Prodrugs of rapamycin |
US4650803A (en) * | 1985-12-06 | 1987-03-17 | University Of Kansas | Prodrugs of rapamycin |
JP2631710B2 (ja) | 1988-08-16 | 1997-07-16 | 日本ヘキスト・マリオン・ルセル株式会社 | ピラノ〔f〕キノリノン誘導体及び該化合物を有効成分とする医薬組成物 |
US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
US5023264A (en) * | 1990-07-16 | 1991-06-11 | American Home Products Corporation | Rapamycin oximes |
US5023263A (en) * | 1990-08-09 | 1991-06-11 | American Home Products Corporation | 42-oxorapamycin |
US5023262A (en) * | 1990-08-14 | 1991-06-11 | American Home Products Corporation | Hydrogenated rapamycin derivatives |
PT98990A (pt) * | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
US5378696A (en) * | 1990-09-19 | 1995-01-03 | American Home Products Corporation | Rapamycin esters |
US5130307A (en) * | 1990-09-28 | 1992-07-14 | American Home Products Corporation | Aminoesters of rapamycin |
US5221670A (en) * | 1990-09-19 | 1993-06-22 | American Home Products Corporation | Rapamycin esters |
US5233036A (en) * | 1990-10-16 | 1993-08-03 | American Home Products Corporation | Rapamycin alkoxyesters |
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 |
US5120842A (en) * | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
IL101353A0 (en) * | 1991-04-03 | 1992-11-15 | American Home Prod | Pharmaceutical compositions for treating diabetes |
US5321009A (en) * | 1991-04-03 | 1994-06-14 | American Home Products Corporation | Method of treating diabetes |
US5100883A (en) * | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
US5194447A (en) * | 1992-02-18 | 1993-03-16 | American Home Products Corporation | Sulfonylcarbamates of rapamycin |
US5118678A (en) * | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
US5093338A (en) | 1991-04-23 | 1992-03-03 | Merck & Co., Inc. | Lipophilic macrolide useful as an immunosuppressant |
US5091389A (en) * | 1991-04-23 | 1992-02-25 | Merck & Co., Inc. | Lipophilic macrolide useful as an immunosuppressant |
US5138051A (en) * | 1991-08-07 | 1992-08-11 | American Home Products Corporation | Rapamycin analogs as immunosuppressants and antifungals |
US5102876A (en) * | 1991-05-07 | 1992-04-07 | American Home Products Corporation | Reduction products of rapamycin |
US5118677A (en) * | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
JPH06502659A (ja) * | 1991-05-31 | 1994-03-24 | ファイザー インク | 免疫抑制剤としてのラパマイシンプロドラッグの使用 |
SG43072A1 (en) * | 1991-06-18 | 1997-10-17 | American Home Prod | Method of treating adult t-cell leukemia/lymphoma |
ZA924953B (en) * | 1991-07-25 | 1993-04-28 | Univ Louisville Res Found | Method of treating ocular inflammation |
US5169851A (en) * | 1991-08-07 | 1992-12-08 | American Home Products Corporation | Rapamycin analog as immunosuppressants and antifungals |
US5151413A (en) * | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
US5516781A (en) * | 1992-01-09 | 1996-05-14 | American Home Products Corporation | Method of treating restenosis with rapamycin |
US5177203A (en) * | 1992-03-05 | 1993-01-05 | American Home Products Corporation | Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents |
CA2132636C (en) * | 1992-03-30 | 2002-12-17 | Robert P. Waranis | Rapamycin formulation for iv injection |
US5256790A (en) | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
GB9221220D0 (en) * | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
US5302584A (en) * | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
US5258389A (en) * | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
US5260300A (en) * | 1992-11-19 | 1993-11-09 | American Home Products Corporation | Rapamycin carbonate esters as immuno-suppressant agents |
US5516770A (en) * | 1993-09-30 | 1996-05-14 | American Home Products Corporation | Rapamycin formulation for IV injection |
US5391730A (en) * | 1993-10-08 | 1995-02-21 | American Home Products Corporation | Phosphorylcarbamates of rapamycin and oxime derivatives thereof |
US5385908A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered esters of rapamycin |
US5385909A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
US5385910A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Gem-distributed esters of rapamycin |
US5389639A (en) * | 1993-12-29 | 1995-02-14 | American Home Products Company | Amino alkanoic esters of rapamycin |
US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
US5463048A (en) * | 1994-06-14 | 1995-10-31 | American Home Products Corporation | Rapamycin amidino carbamates |
US5491231A (en) * | 1994-11-28 | 1996-02-13 | American Home Products Corporation | Hindered N-oxide esters of rapamycin |
US5563145A (en) * | 1994-12-07 | 1996-10-08 | American Home Products Corporation | Rapamycin 42-oximes and hydroxylamines |
US5496832A (en) * | 1995-03-09 | 1996-03-05 | American Home Products Corporation | Method of treating cardiac inflammatory disease |
-
1996
- 1996-12-11 US US08/763,768 patent/US5780462A/en not_active Expired - Lifetime
- 1996-12-18 CZ CZ19963734A patent/CZ293711B6/cs not_active IP Right Cessation
- 1996-12-18 CA CA002193329A patent/CA2193329C/en not_active Expired - Fee Related
- 1996-12-19 NZ NZ299974A patent/NZ299974A/en unknown
- 1996-12-19 SK SK1638-96A patent/SK283912B6/sk unknown
- 1996-12-19 MX MX9606716A patent/MX9606716A/es not_active IP Right Cessation
- 1996-12-20 DE DE69626481T patent/DE69626481T2/de not_active Expired - Fee Related
- 1996-12-20 SI SI9630585T patent/SI0781776T1/xx unknown
- 1996-12-20 EP EP96309369A patent/EP0781776B1/en not_active Expired - Lifetime
- 1996-12-20 PT PT96309369T patent/PT781776E/pt unknown
- 1996-12-20 AT AT96309369T patent/ATE233769T1/de not_active IP Right Cessation
- 1996-12-20 HU HU9603582A patent/HUP9603582A3/hu unknown
- 1996-12-20 ES ES96309369T patent/ES2189858T3/es not_active Expired - Lifetime
- 1996-12-20 DK DK96309369T patent/DK0781776T3/da active
- 1996-12-23 AU AU76517/96A patent/AU702750B2/en not_active Ceased
- 1996-12-23 ZA ZA9610892A patent/ZA9610892B/xx unknown
- 1996-12-23 NO NO965552A patent/NO308303B1/no unknown
- 1996-12-24 CN CN96123983A patent/CN1088710C/zh not_active Expired - Fee Related
- 1996-12-24 KR KR1019960071130A patent/KR100444003B1/ko not_active IP Right Cessation
- 1996-12-24 TW TW085115988A patent/TW403753B/zh not_active IP Right Cessation
- 1996-12-25 RU RU96124399/04A patent/RU2160739C2/ru not_active IP Right Cessation
- 1996-12-26 BR BR9606173A patent/BR9606173A/pt not_active IP Right Cessation
- 1996-12-26 AR ARP960105902A patent/AR005421A1/es active IP Right Grant
- 1996-12-26 JP JP34739396A patent/JP4080560B2/ja not_active Expired - Fee Related
- 1996-12-26 IL IL11992196A patent/IL119921A/xx not_active IP Right Cessation
-
1998
- 1998-03-10 HK HK98101959A patent/HK1002864A1/xx not_active IP Right Cessation
- 1998-03-23 US US09/046,043 patent/US5955457A/en not_active Expired - Fee Related
-
2003
- 2003-09-10 CY CY0300062A patent/CY2377B1/xx unknown
Similar Documents
Publication | Publication Date | Title |
---|---|---|
RU96124399A (ru) | Водорастворимые сложные эфиры рапамицина, фармацевтическая композиция и способы лечения | |
KR970042557A (ko) | 수용성 라파마이신 에스테르(Water soluble rapamycin esters) | |
ES2574640T3 (es) | Métodos para la preparación de conjugados citotóxicos de maitansinoides y agentes que se fijan a las células | |
EP0181110A3 (en) | Histidine derivatives as renin inhibitors | |
RU2000128648A (ru) | Комплексные соединения платины, способы их получения и фармацевтическая композиция | |
DK307787A (da) | Hydrofobe cis-platinkomplekser samt liposomer omfattende saadanne komplekser og fremgangsmaade til fremstilling af saadanne komplekser og liposomer | |
KR920700205A (ko) | 트리-아자 마크로싸이클 화합물과 이들의 금속착화합물 | |
RU2000128058A (ru) | Эктеинасцидины, фармацевтическая композиция, содержащая их и способ лечения опухолей | |
FR2433537A1 (fr) | Derives d'hormones steroides antitumoraux et leur procede de preparation | |
IE812027L (en) | Platinum compound. | |
IL97055A0 (en) | Pharmaceutical compositions for sensitizing tumor cells comprising quinazolinedione derivatives | |
DE69735583D1 (de) | Semisynthetisches verfahren zur herstellung von didemninanalogen | |
RU93005029A (ru) | Трициклические соединения, содержащие гетероатомы | |
IT1054828B (it) | Procedimento per la preparazione di 2.5 dicloro p xilene | |
ATE159527T1 (de) | Alkaloide von mappie foetida, deren anwendung und diese enthaltende zusammensetzungen | |
IL79260A0 (en) | Effector cells and compositions containing them for treatment of cancer and nonmalignant tumors | |
DE69724472D1 (de) | Selenophen-antitumormittel | |
DE19627164C2 (de) | Herstellung polyether-aufweisender Chlorine und Bakteriochlorine, solche Verbindungen und ihre Verwendung | |
ATE2423T1 (de) | 1-acyloxyphenyl-1,2-diphenylalken-derivate, verfahren zu deren herstellung und eine diese derivate enthaltende pharmazeutische zusammensetzung. | |
SE8304124L (sv) | Fluoralkylerade karbapenemderivat | |
KR960700986A (ko) | 리간드 및 이들의 금속착체(ligands and metal complexes thereof) | |
PT85271A (en) | 4-nitrogen substituted isoquinolinol compounds having cardiotonic phosphodiesterase fraction iii inhibiting properties and/or renal vasodilating properties | |
RU97113254A (ru) | Кумаринхинолонкарбоновые кислоты и способы их получения | |
RU2000112002A (ru) | Производные 5h-пирано[2,3-d:6,5-d']дипиримидина, обладающие антимикробным, противовирусным и иммуномодулирующим действием | |
FR2442230A1 (fr) | Procede de preparation de dienones du type narwedine et de leurs derives |