NO332698B1 - Fremgangsmate for stabilisering av rapamycinderivat - Google Patents

Fremgangsmate for stabilisering av rapamycinderivat Download PDF

Info

Publication number: NO332698B1
Authority: NO; Norway
Prior art keywords: rapamycin; antioxidant; rapamycin derivative; hydroxy; ethyl
Prior art date: 1998-12-07

Application number

NO20012424A

Other languages

English (en)

Norwegian (no)

Other versions

NO20012424D0 (no

NO20012424L (no

Inventor

Francois Navarro

Samuel Petit

Guy Stone

Original Assignee

Novartis Ag

Priority date (The priority date 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 date listed.)

1998-12-07

Filing date

2001-05-16

Publication date

2012-12-10

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26314797&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO332698(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2001-05-16 Application filed by Novartis Ag filed Critical Novartis Ag

2001-05-16 Publication of NO20012424D0 publication Critical patent/NO20012424D0/no

2001-05-16 Publication of NO20012424L publication Critical patent/NO20012424L/no

2012-12-10 Publication of NO332698B1 publication Critical patent/NO332698B1/no

Links

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 title claims description 26
238000000034 method Methods 0.000 title claims description 14
230000000087 stabilizing effect Effects 0.000 title claims description 3
239000000203 mixture Substances 0.000 claims description 28
229960002930 sirolimus Drugs 0.000 claims description 20
239000003963 antioxidant agent Substances 0.000 claims description 14
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 description 14
230000003078 antioxidant effect Effects 0.000 claims description 13
-1 ethyl rapamycin Chemical compound 0.000 claims description 9
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 7
235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 7
230000001506 immunosuppresive effect Effects 0.000 claims description 5
239000008194 pharmaceutical composition Substances 0.000 claims description 5
238000001556 precipitation Methods 0.000 claims description 4
239000012442 inert solvent Substances 0.000 claims description 3
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
239000008247 solid mixture Substances 0.000 claims 1
239000003120 macrolide antibiotic agent Substances 0.000 abstract description 16
230000006641 stabilisation Effects 0.000 abstract description 2
238000011105 stabilization Methods 0.000 abstract description 2
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 12
235000006708 antioxidants Nutrition 0.000 description 9
239000004480 active ingredient Substances 0.000 description 6
VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 6
239000007787 solid Substances 0.000 description 6
IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 4
239000013078 crystal Substances 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
238000002425 crystallisation Methods 0.000 description 3
230000008025 crystallization Effects 0.000 description 3
239000003085 diluting agent Substances 0.000 description 3
238000009472 formulation Methods 0.000 description 3
239000004615 ingredient Substances 0.000 description 3
238000002955 isolation Methods 0.000 description 3
150000003951 lactams Chemical class 0.000 description 3
229940041033 macrolides Drugs 0.000 description 3
238000002360 preparation method Methods 0.000 description 3
239000000047 product Substances 0.000 description 3
239000003381 stabilizer Substances 0.000 description 3
238000003756 stirring Methods 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
206010052779 Transplant rejections Diseases 0.000 description 2
239000000969 carrier Substances 0.000 description 2
230000003197 catalytic effect Effects 0.000 description 2
239000007788 liquid Substances 0.000 description 2
230000002265 prevention Effects 0.000 description 2
239000007962 solid dispersion Substances 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
IFKPLJWIEQBPGG-QGZVFWFLSA-N (5s)-6-(dimethylamino)-5-methyl-4,4-diphenylhexan-3-one Chemical compound C=1C=CC=CC=1C([C@H](C)CN(C)C)(C(=O)CC)C1=CC=CC=C1 IFKPLJWIEQBPGG-QGZVFWFLSA-N 0.000 description 1
208000023275 Autoimmune disease Diseases 0.000 description 1
239000004322 Butylated hydroxytoluene Substances 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
229930003268 Vitamin C Natural products 0.000 description 1
229930003427 Vitamin E Natural products 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
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 1
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 1
208000006673 asthma Diseases 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
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
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000002552 dosage form Substances 0.000 description 1
239000008298 dragée Substances 0.000 description 1
238000001035 drying Methods 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
235000019264 food flavour enhancer Nutrition 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
239000007789 gas Substances 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
239000001866 hydroxypropyl methyl cellulose Substances 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
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
235000010979 hydroxypropyl methyl cellulose Nutrition 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
238000004519 manufacturing process Methods 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
239000004530 micro-emulsion Substances 0.000 description 1
238000002156 mixing Methods 0.000 description 1
210000000056 organ Anatomy 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
230000003389 potentiating effect Effects 0.000 description 1
239000000843 powder Substances 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
150000003839 salts Chemical class 0.000 description 1
238000007790 scraping Methods 0.000 description 1
239000000243 solution Substances 0.000 description 1
239000002904 solvent Substances 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)

NO20012424A 1998-12-07 2001-05-16 Fremgangsmate for stabilisering av rapamycinderivat NO332698B1 (no)

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 (fr)	1998-12-07	1999-12-06	Macrolides

Publications (3)

Publication Number	Publication Date
NO20012424D0 NO20012424D0 (no)	2001-05-16
NO20012424L NO20012424L (no)	2001-05-16
NO332698B1 true NO332698B1 (no)	2012-12-10

Family

ID=26314797

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
NO20012424A NO332698B1 (no)	1998-12-07	2001-05-16	Fremgangsmate for stabilisering av rapamycinderivat
NO20121113A NO334612B1 (no)	1998-12-07	2012-10-01	Stabilisering av makrolider

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
NO20121113A NO334612B1 (no)	1998-12-07	2012-10-01	Stabilisering av makrolider

Country Status (38)

Country	Link
US (5)	US6605613B2 (fr)
EP (4)	EP2279751A3 (fr)
JP (3)	JP3805625B2 (fr)
KR (2)	KR100695834B1 (fr)
CN (2)	CN1261163C (fr)
AR (3)	AR026102A1 (fr)
AT (1)	ATE365051T1 (fr)
AU (1)	AU759219B2 (fr)
BE (1)	BE1012869A3 (fr)
BR (1)	BR9915986A (fr)
CA (3)	CA2351580C (fr)
CO (1)	CO4980847A1 (fr)
CY (1)	CY1106870T1 (fr)
CZ (2)	CZ303006B6 (fr)
DE (1)	DE69936352T3 (fr)
DK (1)	DK1137439T4 (fr)
ES (1)	ES2288033T5 (fr)
FR (1)	FR2786771B1 (fr)
GB (2)	GB9826882D0 (fr)
HK (1)	HK1038889B (fr)
HU (2)	HU228939B1 (fr)
ID (1)	ID29250A (fr)
IL (1)	IL143092A0 (fr)
IT (1)	IT1319701B1 (fr)
MY (2)	MY127579A (fr)
NO (2)	NO332698B1 (fr)
NZ (2)	NZ511936A (fr)
PE (1)	PE20001333A1 (fr)
PL (2)	PL208854B1 (fr)
PT (1)	PT1137439E (fr)
RU (1)	RU2243769C2 (fr)
SG (1)	SG151072A1 (fr)
SI (1)	SI1137439T2 (fr)
SK (2)	SK286688B6 (fr)
TR (2)	TR200101416T2 (fr)
TW (2)	TWI270550B (fr)
WO (1)	WO2000033878A2 (fr)
ZA (1)	ZA200104360B (fr)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
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
MXPA04007847A (es)	2002-02-13	2005-02-24	Biogal Gyogyszergyar	Metodo para extraer un macrolido de biomateria.
NZ537829A (en)	2002-07-30	2006-09-29	Wyeth Corp	Parenteral formulations containing a rapamycin hydroxyester
TR200500302T3 (tr) *	2003-03-31	2005-04-21	Biogal Gyogyszergyar Rt.	Makrolidlerin kristalizasyonu ve saflaştırılması.
US20050118344A1 (en)	2003-12-01	2005-06-02	Pacetti Stephen D.	Temperature controlled crimping
TW200523266A (en)	2003-07-24	2005-07-16	Biogal Gyogyszergyar	Method of purifying macrolides
CA2539324A1 (fr)	2003-09-18	2005-03-31	Macusight, Inc.	Administration transsclerale d'agents therapeutiques
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
CN1889994A (zh) *	2003-12-10	2007-01-03	艾克若克斯Dds有限公司	伴随透皮或局部药物输送的不希望的效果的治疗方法
US8551512B2 (en)	2004-03-22	2013-10-08	Advanced Cardiovascular Systems, Inc.	Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
US20060094744A1 (en) *	2004-09-29	2006-05-04	Maryanoff Cynthia A	Pharmaceutical dosage forms of stable amorphous rapamycin like compounds
JP4974903B2 (ja)	2005-02-09	2012-07-11	参天製薬株式会社	疾患または状態を処置するための液体処方物
BRPI0619592A2 (pt) *	2005-12-07	2016-09-06	Wyeth Corp	métodos para medir a qualidade da partícula de um composto de rapamicina, para determinar o tamanho de partícula médio de uma amostra e a cristalinidade de um composto de rapamicina, e para a purificação de rapamicina
US7700614B2 (en) *	2005-12-14	2010-04-20	Abbott Laboratories	One pot synthesis of tetrazole derivatives of rapamycin
RU2008121713A (ru) *	2005-12-20	2010-01-27	Вайет (Us)	Контроль стабильности лекарственной формы cci-779 посредством контроля примесей лекарственныхого вещества
WO2007092620A2 (fr) *	2006-02-09	2007-08-16	Macusight, Inc.	Formulations stables et leurs procedes de preparation et d'utilisation
PL2001466T3 (pl)	2006-03-23	2016-06-30	Santen Pharmaceutical Co Ltd	Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń
WO2011151704A2 (fr)	2010-06-02	2011-12-08	Fresenius Kabi Oncology Ltd.	Compositions pharmaceutiques stables d'esters de rapamycine
WO2011156025A1 (fr) *	2010-06-07	2011-12-15	Telik, Inc.	Chlorhydrate d'ézatiostat non solvaté cristallisé
EP2601201B1 (fr) *	2010-08-04	2014-09-24	Meril Life Sciences Pvt. Ltd.	Procédé pour la préparation des composés nouveaux du 42-o-(hétéroalkyloxy) rapamycin avec les propriétaires antiprolifiques.
WO2012066502A1 (fr)	2010-11-19	2012-05-24	Biocon Limited	Procédés de préparation d'évérolimus et d'intermédiaires de celui-ci
JP2014516075A (ja)	2011-06-06	2014-07-07	シェブロンフィリップスケミカルカンパニーエルピー	癌治療のためのメタロセン化合物の使用
WO2013022201A1 (fr) *	2011-08-11	2013-02-14	Dong-A Pharm. Co., Ltd.	Procédé de préparation d'une formulation stabilisée et solubilisée de dérivés de sirolimus
US9610385B2 (en)	2013-03-07	2017-04-04	Abbott Cardiovascular Systems Inc.	Method of fabricating an implantable medical device comprising a rapamycin derivative
IN2013MU02532A (fr)	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
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CN119431400A (zh) *	2020-03-27	2025-02-14	波士顿科学国际有限公司	用于使药物结晶的方法
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1998
- 1998-12-07 GB GBGB9826882.4A patent/GB9826882D0/en not_active Ceased
1999
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- 1999-12-06 RU RU2001118266/15A patent/RU2243769C2/ru active
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Publication number	Publication date
ITMI992520A1 (it)	2001-06-02
BE1012869A3 (fr)	2001-04-03
ES2288033T3 (es)	2007-12-16
US7572804B2 (en)	2009-08-11
SI1137439T2 (sl)	2012-05-31
GB9904934D0 (en)	1999-04-28
ITMI992520A0 (it)	1999-12-02
AU1657300A (en)	2000-06-26
JP2006111637A (ja)	2006-04-27
HUP0104489A3 (en)	2004-05-28
FR2786771A1 (fr)	2000-06-09
PE20001333A1 (es)	2000-12-12
PT1137439E (pt)	2007-09-25
CZ303006B6 (cs)	2012-02-22
NO20012424D0 (no)	2001-05-16
WO2000033878A3 (fr)	2000-11-02
WO2000033878A2 (fr)	2000-06-15
CA2732620A1 (fr)	2000-06-15
IL143092A0 (en)	2002-04-21
US7741338B2 (en)	2010-06-22
FR2786771B1 (fr)	2002-12-27
AR048073A2 (es)	2006-03-29
EP2269651A2 (fr)	2011-01-05
RU2243769C2 (ru)	2005-01-10
TR200101416T2 (tr)	2002-01-21
JP2002531527A (ja)	2002-09-24
NO20012424L (no)	2001-05-16
CZ20012001A3 (cs)	2001-09-12
ID29250A (id)	2001-08-16
NO20121113L (no)	2001-05-16
US20050107418A1 (en)	2005-05-19
CY1106870T1 (el)	2012-09-26
DK1137439T3 (da)	2007-09-10
US20030191148A1 (en)	2003-10-09
PL348333A1 (en)	2002-05-20
CN1876657B (zh)	2013-01-09
EP2279751A3 (fr)	2011-02-16
US6605613B2 (en)	2003-08-12
CA2351580C (fr)	2012-03-20
TWI270550B (en)	2007-01-11
US20090270441A1 (en)	2009-10-29
EP1743657A3 (fr)	2007-03-28
US6852729B2 (en)	2005-02-08
GB9826882D0 (en)	1999-01-27
TW200540179A (en)	2005-12-16
JP3805625B2 (ja)	2006-08-02
SI1137439T1 (sl)	2008-06-30
US20080161334A1 (en)	2008-07-03
EP2279751A2 (fr)	2011-02-02
BR9915986A (pt)	2001-09-04
EP1137439A2 (fr)	2001-10-04
MY120594A (en)	2005-11-30
DE69936352T2 (de)	2008-02-14
ES2288033T5 (es)	2012-04-10
CO4980847A1 (es)	2000-11-27
PL196627B1 (pl)	2008-01-31
HK1038889A1 (en)	2002-04-04
US7297703B2 (en)	2007-11-20
ZA200104360B (en)	2002-01-16
CZ302210B6 (cs)	2010-12-22
EP1743657A2 (fr)	2007-01-17
TWI248938B (en)	2006-02-11
HU228939B1 (en)	2013-07-29
EP1137439B1 (fr)	2007-06-20
ATE365051T1 (de)	2007-07-15
TR200201428T2 (tr)	2002-12-23
AR026102A1 (es)	2003-01-29
NO334612B1 (no)	2014-04-22
HU230174B1 (hu)	2015-09-28
NZ527781A (en)	2004-11-26
KR20010101128A (ko)	2001-11-14
CA2351580A1 (fr)	2000-06-15
JP5043308B2 (ja)	2012-10-10
HUP0104489A2 (hu)	2002-03-28
CN1876657A (zh)	2006-12-13
JP2005200429A (ja)	2005-07-28
CN1374872A (zh)	2002-10-16
SK286688B6 (sk)	2009-03-05
JP5165199B2 (ja)	2013-03-21
EP1137439B2 (fr)	2011-11-23
CA2651609A1 (fr)	2000-06-15
AR054444A2 (es)	2007-06-27
SK287325B6 (sk)	2010-07-07
DK1137439T4 (da)	2012-03-19
SK7662001A3 (en)	2001-12-03
PL208854B1 (pl)	2011-06-30
MY127579A (en)	2006-12-29
KR100695834B1 (ko)	2007-03-19
DE69936352D1 (de)	2007-08-02
AU759219B2 (en)	2003-04-10
CN1261163C (zh)	2006-06-28
US20020032213A1 (en)	2002-03-14
NZ511936A (en)	2003-10-31
KR20060096477A (ko)	2006-09-11
SG151072A1 (en)	2009-06-29
CA2732620C (fr)	2013-08-06
EP2269651A3 (fr)	2011-03-09
DE69936352T3 (de)	2012-05-03
IT1319701B1 (it)	2003-10-27
HK1038889B (en)	2008-01-25

Legal Events

Date	Code	Title	Description
2020-01-13	MK1K	Patent expired

Publication	Publication Date	Title
NO332698B1 (no)	2012-12-10	Fremgangsmate for stabilisering av rapamycinderivat
MXPA01005720A (en)	2002-02-26	Macrolides
AU2003200370B2 (en)	2005-10-27	Stabilization of macrolides
RU2264405C2 (ru)	2005-11-20	40-o-(2-гидрокси)этилрапамицин в кристаллической несольватированной форме, фармацевтическая композиция, содержащая такой макролид в качестве действующего вещества, и способ его получения
HK1146246A (en)	2011-05-27	Stabilisation of macrolides
HK1102910A (en)	2007-12-07	Stabilisation of macrolides
HK1151741A (en)	2012-02-10	Stabilisation of macrolides