NO317058B1 - Rapamycinderivater, fremgangsmate for fremstilling derav, farmasoytisk preparat omfattende et slikt derivat, kit omfattende et preparat samt anvendelse av derivatene - Google Patents
Rapamycinderivater, fremgangsmate for fremstilling derav, farmasoytisk preparat omfattende et slikt derivat, kit omfattende et preparat samt anvendelse av derivatene Download PDFInfo
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- NO317058B1 NO317058B1 NO19975432A NO975432A NO317058B1 NO 317058 B1 NO317058 B1 NO 317058B1 NO 19975432 A NO19975432 A NO 19975432A NO 975432 A NO975432 A NO 975432A NO 317058 B1 NO317058 B1 NO 317058B1
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- Norway
- Prior art keywords
- formula
- compound
- rapamycin
- alkyl
- preparation
- Prior art date
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- 238000002360 preparation method Methods 0.000 title claims description 8
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- HPNSFSBZBAHARI-RUDMXATFSA-N mycophenolic acid Chemical compound OC1=C(C\C=C(/C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-RUDMXATFSA-N 0.000 description 1
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- 230000000414 obstructive effect Effects 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052763 palladium Inorganic materials 0.000 description 1
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- 210000000496 pancreas Anatomy 0.000 description 1
- 230000003071 parasitic effect Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 description 1
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- LJCNRYVRMXRIQR-OLXYHTOASA-L potassium sodium L-tartrate Chemical compound [Na+].[K+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O LJCNRYVRMXRIQR-OLXYHTOASA-L 0.000 description 1
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- GRJJQCWNZGRKAU-UHFFFAOYSA-N pyridin-1-ium;fluoride Chemical compound F.C1=CC=NC=C1 GRJJQCWNZGRKAU-UHFFFAOYSA-N 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
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- 208000016691 refractory malignant neoplasm Diseases 0.000 description 1
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- 229910052703 rhodium Inorganic materials 0.000 description 1
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- MHOVAHRLVXNVSD-UHFFFAOYSA-N rhodium atom Chemical compound [Rh] MHOVAHRLVXNVSD-UHFFFAOYSA-N 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 201000000306 sarcoidosis Diseases 0.000 description 1
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- 239000012679 serum free medium Substances 0.000 description 1
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- 210000003491 skin Anatomy 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- JHJLBTNAGRQEKS-UHFFFAOYSA-M sodium bromide Inorganic materials [Na+].[Br-] JHJLBTNAGRQEKS-UHFFFAOYSA-M 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000011006 sodium potassium tartrate Nutrition 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
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- 210000000278 spinal cord Anatomy 0.000 description 1
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- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
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- 239000011593 sulfur Substances 0.000 description 1
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- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 description 1
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical group C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- HFRXJVQOXRXOPP-UHFFFAOYSA-N thionyl bromide Chemical compound BrS(Br)=O HFRXJVQOXRXOPP-UHFFFAOYSA-N 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 238000005809 transesterification reaction Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 125000004665 trialkylsilyl group Chemical group 0.000 description 1
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- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- SCHZCUMIENIQMY-UHFFFAOYSA-N tris(trimethylsilyl)silicon Chemical compound C[Si](C)(C)[Si]([Si](C)(C)C)[Si](C)(C)C SCHZCUMIENIQMY-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
-
- 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
-
- 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
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- 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
- A61P37/02—Immunomodulators
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9511704.0A GB9511704D0 (en) | 1995-06-09 | 1995-06-09 | Organic compounds |
GBGB9513754.3A GB9513754D0 (en) | 1995-07-06 | 1995-07-06 | Organic compounds |
PCT/EP1996/002441 WO1996041807A1 (en) | 1995-06-09 | 1996-06-05 | Rapamycin derivatives |
Publications (3)
Publication Number | Publication Date |
---|---|
NO975432D0 NO975432D0 (no) | 1997-11-26 |
NO975432L NO975432L (no) | 1997-11-26 |
NO317058B1 true NO317058B1 (no) | 2004-08-02 |
Family
ID=26307190
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO19975432A NO317058B1 (no) | 1995-06-09 | 1997-11-26 | Rapamycinderivater, fremgangsmate for fremstilling derav, farmasoytisk preparat omfattende et slikt derivat, kit omfattende et preparat samt anvendelse av derivatene |
Country Status (30)
Country | Link |
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US (2) | US5985890A (da) |
EP (1) | EP0833828B1 (da) |
JP (1) | JP3226545B2 (da) |
KR (1) | KR100400620B1 (da) |
CN (1) | CN1124276C (da) |
AR (1) | AR003426A1 (da) |
AT (1) | ATE228135T1 (da) |
AU (1) | AU712193B2 (da) |
BR (1) | BR9609260A (da) |
CA (1) | CA2219659C (da) |
CO (1) | CO4440629A1 (da) |
CZ (1) | CZ292233B6 (da) |
DE (1) | DE69624921T2 (da) |
DK (1) | DK0833828T3 (da) |
ES (1) | ES2187660T3 (da) |
FI (1) | FI113051B (da) |
HK (1) | HK1014949A1 (da) |
HU (1) | HU228234B1 (da) |
IL (1) | IL122212A (da) |
MY (1) | MY145291A (da) |
NO (1) | NO317058B1 (da) |
NZ (1) | NZ311647A (da) |
PE (1) | PE4598A1 (da) |
PL (1) | PL184731B1 (da) |
PT (1) | PT833828E (da) |
RU (1) | RU2158267C2 (da) |
SK (1) | SK284529B6 (da) |
TR (1) | TR199701567T1 (da) |
TW (1) | TW410226B (da) |
WO (1) | WO1996041807A1 (da) |
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GB9606452D0 (en) * | 1996-03-27 | 1996-06-05 | Sandoz Ltd | Organic compounds |
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1996
- 1996-06-05 PT PT96921931T patent/PT833828E/pt unknown
- 1996-06-05 CA CA002219659A patent/CA2219659C/en not_active Expired - Lifetime
- 1996-06-05 WO PCT/EP1996/002441 patent/WO1996041807A1/en active IP Right Grant
- 1996-06-05 EP EP96921931A patent/EP0833828B1/en not_active Expired - Lifetime
- 1996-06-05 HU HU9802200A patent/HU228234B1/hu unknown
- 1996-06-05 AU AU63006/96A patent/AU712193B2/en not_active Expired
- 1996-06-05 BR BR9609260A patent/BR9609260A/pt not_active Application Discontinuation
- 1996-06-05 DE DE69624921T patent/DE69624921T2/de not_active Expired - Lifetime
- 1996-06-05 CN CN96194681A patent/CN1124276C/zh not_active Expired - Lifetime
- 1996-06-05 TR TR97/01567T patent/TR199701567T1/xx unknown
- 1996-06-05 ES ES96921931T patent/ES2187660T3/es not_active Expired - Lifetime
- 1996-06-05 IL IL12221296A patent/IL122212A/xx not_active IP Right Cessation
- 1996-06-05 KR KR1019970709247A patent/KR100400620B1/ko not_active IP Right Cessation
- 1996-06-05 JP JP50258797A patent/JP3226545B2/ja not_active Expired - Fee Related
- 1996-06-05 RU RU98100481/04A patent/RU2158267C2/ru active
- 1996-06-05 AT AT96921931T patent/ATE228135T1/de active
- 1996-06-05 PL PL96323310A patent/PL184731B1/pl unknown
- 1996-06-05 SK SK1682-97A patent/SK284529B6/sk not_active IP Right Cessation
- 1996-06-05 CZ CZ19973922A patent/CZ292233B6/cs not_active IP Right Cessation
- 1996-06-05 DK DK96921931T patent/DK0833828T3/da active
- 1996-06-05 US US08/973,604 patent/US5985890A/en not_active Expired - Lifetime
- 1996-06-05 NZ NZ311647A patent/NZ311647A/xx not_active IP Right Cessation
- 1996-06-06 AR ARP960102978A patent/AR003426A1/es active IP Right Grant
- 1996-06-06 MY MYPI96002232A patent/MY145291A/en unknown
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- 1996-06-07 CO CO96029756A patent/CO4440629A1/es unknown
- 1996-06-07 TW TW085106847A patent/TW410226B/zh not_active IP Right Cessation
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1997
- 1997-10-17 FI FI973991A patent/FI113051B/fi not_active IP Right Cessation
- 1997-11-26 NO NO19975432A patent/NO317058B1/no not_active IP Right Cessation
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1999
- 1999-01-11 HK HK99100122A patent/HK1014949A1/xx not_active IP Right Cessation
- 1999-07-19 US US09/356,587 patent/US6200985B1/en not_active Expired - Lifetime
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