SK286688B6 - Spôsob stabilizácie rapamycínu alebo rapamycínového derivátu - Google Patents
Spôsob stabilizácie rapamycínu alebo rapamycínového derivátu Download PDFInfo
- Publication number
- SK286688B6 SK286688B6 SK766-2001A SK7662001A SK286688B6 SK 286688 B6 SK286688 B6 SK 286688B6 SK 7662001 A SK7662001 A SK 7662001A SK 286688 B6 SK286688 B6 SK 286688B6
- Authority
- SK
- Slovakia
- Prior art keywords
- rapamycin
- derivative
- antioxidant
- rapamycin derivative
- hydroxy
- 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 abstract description 48
- 229960002930 sirolimus Drugs 0.000 title claims abstract description 28
- 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 title claims abstract description 27
- 238000000034 method Methods 0.000 title claims abstract description 15
- 230000000087 stabilizing effect Effects 0.000 title claims abstract description 4
- 239000000203 mixture Substances 0.000 claims abstract description 24
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 15
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 14
- 239000012442 inert solvent Substances 0.000 claims abstract description 3
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical group CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims description 9
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 230000001506 immunosuppresive effect Effects 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 2
- 239000002244 precipitate Substances 0.000 claims 1
- 239000008247 solid mixture Substances 0.000 claims 1
- 238000001556 precipitation Methods 0.000 abstract description 3
- 230000001861 immunosuppressant effect Effects 0.000 abstract 1
- 239000003120 macrolide antibiotic agent Substances 0.000 description 18
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 12
- 235000006708 antioxidants Nutrition 0.000 description 8
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 6
- 239000007787 solid Substances 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 4
- 239000013543 active substance Substances 0.000 description 4
- 229940041033 macrolides Drugs 0.000 description 4
- 230000003647 oxidation Effects 0.000 description 4
- 238000007254 oxidation reaction Methods 0.000 description 4
- 238000003860 storage Methods 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- ZDQSOHOQTUFQEM-PKUCKEGBSA-N ascomycin Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C\C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](O)[C@H](OC)C1 ZDQSOHOQTUFQEM-PKUCKEGBSA-N 0.000 description 3
- ZDQSOHOQTUFQEM-XCXYXIJFSA-N ascomycin Natural products CC[C@H]1C=C(C)C[C@@H](C)C[C@@H](OC)[C@H]2O[C@@](O)([C@@H](C)C[C@H]2OC)C(=O)C(=O)N3CCCC[C@@H]3C(=O)O[C@H]([C@H](C)[C@@H](O)CC1=O)C(=C[C@@H]4CC[C@@H](O)[C@H](C4)OC)C ZDQSOHOQTUFQEM-XCXYXIJFSA-N 0.000 description 3
- 239000013078 crystal Substances 0.000 description 3
- 238000002425 crystallisation Methods 0.000 description 3
- 230000008025 crystallization Effects 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 238000002955 isolation Methods 0.000 description 3
- 150000003951 lactams Chemical class 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 239000003381 stabilizer Substances 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- -1 hydroxyalkoxyalkyl Chemical group 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 239000007962 solid dispersion Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 241000187747 Streptomyces Species 0.000 description 1
- 241001647839 Streptomyces tsukubensis Species 0.000 description 1
- 206010052779 Transplant rejections Diseases 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 125000004945 acylaminoalkyl group Chemical group 0.000 description 1
- 125000004103 aminoalkyl group Chemical group 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 229910052786 argon Inorganic materials 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000007857 degradation product Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 230000003463 hyperproliferative effect Effects 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 150000002596 lactones Chemical group 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000006748 scratching Methods 0.000 description 1
- 230000002393 scratching effect Effects 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 150000003527 tetrahydropyrans Chemical class 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
-
- 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
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9826882.4A GB9826882D0 (en) | 1998-12-07 | 1998-12-07 | Organic compounds |
| GBGB9904934.8A GB9904934D0 (en) | 1998-12-07 | 1999-03-04 | Organic compounds |
| PCT/EP1999/009521 WO2000033878A2 (en) | 1998-12-07 | 1999-12-06 | Stabilization of macrolides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SK7662001A3 SK7662001A3 (en) | 2001-12-03 |
| SK286688B6 true SK286688B6 (sk) | 2009-03-05 |
Family
ID=26314797
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK766-2001A SK286688B6 (sk) | 1998-12-07 | 1999-12-06 | Spôsob stabilizácie rapamycínu alebo rapamycínového derivátu |
| SK5032-2008A SK287325B6 (sk) | 1998-12-07 | 1999-12-06 | Zmes obsahujúca 40-O-(2-hydroxy)etylrapamycín a antioxidant a farmaceutická kompozícia s obsahom tejto zmesi |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK5032-2008A SK287325B6 (sk) | 1998-12-07 | 1999-12-06 | Zmes obsahujúca 40-O-(2-hydroxy)etylrapamycín a antioxidant a farmaceutická kompozícia s obsahom tejto zmesi |
Country Status (38)
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070032853A1 (en) | 2002-03-27 | 2007-02-08 | Hossainy Syed F | 40-O-(2-hydroxy)ethyl-rapamycin coated stent |
| US7452692B2 (en) | 2002-02-13 | 2008-11-18 | Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság | Method for extracting a macrolide from biomatter |
| CA2475383C (en) | 2002-02-13 | 2009-12-22 | Biogal Gyogyszergyar Rt. | Method for extracting a macrolide from biomatter |
| KR101131794B1 (ko) | 2002-07-30 | 2012-03-30 | 와이어쓰 엘엘씨 | Ｃｃｉ-779 공용매 농축액, 비경구 ｃｃｉ-779 제형 및 비경구 ｃｃｉ-779 제형의 제조방법 |
| KR20050114262A (ko) * | 2003-03-31 | 2005-12-05 | 테바 기오기스제르갸르 레스즈베니타르사사그 | 마크로라이드의 결정화 및 정제 |
| US20050118344A1 (en) | 2003-12-01 | 2005-06-02 | Pacetti Stephen D. | Temperature controlled crimping |
| WO2005010015A1 (en) | 2003-07-24 | 2005-02-03 | Teva Gyogyszergyar Reszvenytarsasag | Method of purifying macrolides |
| CA2539324A1 (en) | 2003-09-18 | 2005-03-31 | Macusight, Inc. | Transscleral delivery |
| US9114198B2 (en) * | 2003-11-19 | 2015-08-25 | Advanced Cardiovascular Systems, Inc. | Biologically beneficial coatings for implantable devices containing fluorinated polymers and methods for fabricating the same |
| JP2007520262A (ja) * | 2003-12-10 | 2007-07-26 | アクルックス・ディ・ディ・エス・プロプライエタリー・リミテッド | 経皮または局所薬物輸送に伴う副作用の処置方法 |
| US8551512B2 (en) * | 2004-03-22 | 2013-10-08 | Advanced Cardiovascular Systems, Inc. | Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS |
| WO2006039237A1 (en) * | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| BRPI0607606B1 (pt) | 2005-02-09 | 2021-06-22 | Santen Pharmaceutical, Co., Ltd. | Formulação líquida |
| AR058283A1 (es) * | 2005-12-07 | 2008-01-30 | Wyeth Corp | Metodos para la preparacion de rapamicina cristalina y para la medicion de la cristalinidad de los compuestos de rapamicina utilizando calorimetria diferencial de barrido |
| US7700614B2 (en) * | 2005-12-14 | 2010-04-20 | Abbott Laboratories | One pot synthesis of tetrazole derivatives of rapamycin |
| JP2009520818A (ja) * | 2005-12-20 | 2009-05-28 | ワイス | 薬物物質不純物の制御によるｃｃｉ−７７９製剤安定性の制御 |
| CN101605529B (zh) * | 2006-02-09 | 2013-03-13 | 参天制药株式会社 | 稳定制剂及它们的制备和使用方法 |
| BRPI0709016A2 (pt) | 2006-03-23 | 2011-06-21 | Macusight Inc | formulações e métodos para doenças ou condições relacionadas com a permeabilidade vascular |
| AU2011260016B2 (en) | 2010-06-02 | 2013-08-22 | Fresenius Kabi Oncology Ltd. | Stable pharmaceutical compositions of Rapamycin esters |
| WO2011156025A1 (en) * | 2010-06-07 | 2011-12-15 | Telik, Inc. | Crystalline Ezatiostat Hydrochloride Ansolvate |
| US9321782B2 (en) * | 2010-08-04 | 2016-04-26 | Meril Life Sciences Pvt. Ltd. | Process for preparation of novel 42-O-(heteroalkoxyalkyl) rapamicin compounds with anti-proliferative properties |
| WO2012066502A1 (en) | 2010-11-19 | 2012-05-24 | Biocon Limited | Processes for preparation of everolimus and intermediates thereof |
| WO2012170384A1 (en) | 2011-06-06 | 2012-12-13 | Chevron Phillips Chemical Company Lp | Use of metallocene compounds for cancer treatment |
| WO2013022201A1 (en) * | 2011-08-11 | 2013-02-14 | Dong-A Pharm. Co., Ltd. | Process of preparing a stabilized and solubilized formulation of sirolimus derivatives |
| US9610385B2 (en) | 2013-03-07 | 2017-04-04 | Abbott Cardiovascular Systems Inc. | Method of fabricating an implantable medical device comprising a rapamycin derivative |
| IN2013MU02532A (enExample) | 2013-07-31 | 2015-06-26 | Sahajanand Medical Technologies Pvt Ltd | |
| CN104721158B (zh) * | 2013-12-24 | 2018-01-30 | 正大天晴药业集团股份有限公司 | 一种稳定的依维莫司片剂 |
| CN104892632B (zh) * | 2015-06-03 | 2017-12-26 | 道中道（菏泽）制药有限公司 | 一种晶体形式的依维莫司及其制备方法 |
| EP3329916A4 (en) | 2015-07-28 | 2019-03-20 | Nippon Kayaku Kabushiki Kaisha | PHARMACEUTICAL COMPOSITION COMPRISING RAPAMYCIN OR A DERIVATIVE THEREOF, AND PROCESS FOR PRODUCING THE SAME |
| US20190015513A1 (en) * | 2015-08-28 | 2019-01-17 | Nippon Kayaku Kabushiki Kaisha | Pharmaceutical composition comprising rapamycin or derivative thereof |
| WO2017047618A1 (ja) * | 2015-09-18 | 2017-03-23 | 日本化薬株式会社 | ラパマイシン又はその誘導体を含有する医薬組成物 |
| WO2017129772A1 (en) | 2016-01-29 | 2017-08-03 | Xellia Phamaceuticals Aps | Stable pharmaceutical compositions of temsirolimus |
| JP6855470B2 (ja) | 2016-05-27 | 2021-04-07 | 日本化薬株式会社 | ラパマイシン又はその誘導体を含有する医薬組成物 |
| KR102051806B1 (ko) * | 2018-01-12 | 2019-12-04 | 주식회사 종근당 | 에베로리무스를 포함하는 안정화된 약제학적 제제 |
| EP4126882A1 (en) * | 2020-03-27 | 2023-02-08 | Boston Scientific Scimed Inc. | Methods for crystallization of drugs |
| JP2023028473A (ja) * | 2021-08-19 | 2023-03-03 | 日本マイクロバイオファーマ株式会社 | エベロリムスの製造方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) * | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US3996355A (en) | 1975-01-02 | 1976-12-07 | American Home Products Corporation | Permanent suspension pharmaceutical dosage form |
| US4049128A (en) | 1976-11-18 | 1977-09-20 | Westinghouse Air Brake Company | Control system for automatic railway car coupler |
| AU543727B2 (en) * | 1980-06-02 | 1985-05-02 | Ayerst Mckenna & Harrison Inc. | Injectable composition of rapamycin |
| GB8803836D0 (en) | 1988-02-18 | 1988-03-16 | Glaxo Group Ltd | Compositions |
| CA1338150C (en) † | 1988-02-18 | 1996-03-12 | Edward George Howard, Jr. | Ceramic/distillable binder compositions |
| KR0159766B1 (ko) * | 1989-10-16 | 1998-12-01 | 후지사와 토모키치로 | 양모제 조성물 |
| JPH04230389A (ja) * | 1990-07-16 | 1992-08-19 | American Home Prod Corp | ラパマイシン誘導体 |
| FI97472C (fi) * | 1991-05-07 | 1996-12-27 | American Home Prod | Menetelmä terapeuttisesti käyttökelpoisten rapamysiinijohdannaisten valmistamiseksi anti-inflammatorisina ja antifungaalisina aineina |
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| EP1266900A1 (en) | 1992-10-13 | 2002-12-18 | Wyeth | Carbamates of rapamycin |
| RU2181054C2 (ru) * | 1994-11-02 | 2002-04-10 | Новартис Аг | Микроэмульсионный предконцентрат |
| ATE228135T1 (de) * | 1995-06-09 | 2002-12-15 | Novartis Erfind Verwalt Gmbh | Rapamycinderivate |
| FR2736550B1 (fr) * | 1995-07-14 | 1998-07-24 | Sandoz Sa | Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule |
| EP1208847B8 (en) * | 1996-07-30 | 2007-02-14 | Novartis AG | Pharmaceutical compositions for the treatment of transplant rejection, as well as autoimmune or inflammatory conditions |
| US6362264B1 (en) * | 1996-12-20 | 2002-03-26 | Ck Witco Corporation | Stabilizer for food contact and medical grade PVC |
| JP2001511780A (ja) | 1997-02-04 | 2001-08-14 | アボツト・ラボラトリーズ | 鎮痛性非経口リポソーム配合物 |
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1998
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1999
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| PC4A | Assignment and transfer of rights |
Owner name: NOVARTIS PHARMA AG, BASEL, CH Free format text: FORMER OWNER: NOVARTIS AG, BASEL, CH Effective date: 20190619 Owner name: NOVARTIS INTERNATIONAL PHARMACEUTICAL AG, BASE, CH Free format text: FORMER OWNER: NOVARTIS AG, BASEL, CH Effective date: 20190619 |
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Free format text: NON-EXCLUSIVE LICENCE Name of requester: NOVARTIS SLOVAKIA S.R.O., BRATISLAVA, SK Effective date: 20190513 |
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| MK4A | Patent expired |
Expiry date: 20191206 |