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 PDF

Info

Publication number: NO317058B1
Authority: NO; Norway
Prior art keywords: formula; compound; rapamycin; alkyl; preparation
Prior art date: 1995-06-09

Application number

NO19975432A

Other languages

English (en)

Norwegian (no)

Other versions

NO975432D0 (no

NO975432L (no

Inventor

Sylvain Cottens

Richard Sedrani

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.)

1995-06-09

Filing date

1997-11-26

Publication date

2004-08-02

1995-06-09 Priority claimed from GBGB9511704.0A external-priority patent/GB9511704D0/en

1995-07-06 Priority claimed from GBGB9513754.3A external-priority patent/GB9513754D0/en

1997-11-26 Application filed by Novartis Ag filed Critical Novartis Ag

1997-11-26 Publication of NO975432D0 publication Critical patent/NO975432D0/no

1997-11-26 Publication of NO975432L publication Critical patent/NO975432L/no

2004-08-02 Publication of NO317058B1 publication Critical patent/NO317058B1/no

Links

238000000034 method Methods 0.000 title claims description 30
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239000008194 pharmaceutical composition Substances 0.000 title 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
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229910052703 rhodium Inorganic materials 0.000 description 1
239000010948 rhodium Substances 0.000 description 1
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
150000003342 selenium Chemical class 0.000 description 1
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230000019491 signal transduction Effects 0.000 description 1
150000004756 silanes Chemical class 0.000 description 1
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239000011734 sodium Substances 0.000 description 1
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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
239000002904 solvent Substances 0.000 description 1
230000003595 spectral effect Effects 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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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
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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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239000012991 xanthate Substances 0.000 description 1
239000011701 zinc Substances 0.000 description 1
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Classifications

- 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
- 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

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
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Immunology (AREA)
Pulmonology (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Pain & Pain Management (AREA)
Epidemiology (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Transplantation (AREA)
Rheumatology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

NO19975432A 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 NO317058B1 (no)

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 (29)

Country	Link
US (2)	US5985890A (es)
EP (1)	EP0833828B1 (es)
JP (1)	JP3226545B2 (es)
KR (1)	KR100400620B1 (es)
CN (1)	CN1124276C (es)
AR (1)	AR003426A1 (es)
AT (1)	ATE228135T1 (es)
AU (1)	AU712193B2 (es)
BR (1)	BR9609260A (es)
CA (1)	CA2219659C (es)
CO (1)	CO4440629A1 (es)
CZ (1)	CZ292233B6 (es)
DE (1)	DE69624921T2 (es)
DK (1)	DK0833828T3 (es)
ES (1)	ES2187660T3 (es)
FI (1)	FI113051B (es)
HU (1)	HU228234B1 (es)
IL (1)	IL122212A (es)
MY (1)	MY145291A (es)
NO (1)	NO317058B1 (es)
NZ (1)	NZ311647A (es)
PE (1)	PE4598A1 (es)
PL (1)	PL184731B1 (es)
PT (1)	PT833828E (es)
RU (1)	RU2158267C2 (es)
SK (1)	SK284529B6 (es)
TR (1)	TR199701567T1 (es)
TW (1)	TW410226B (es)
WO (1)	WO1996041807A1 (es)

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1996
- 1996-06-05 CA CA002219659A patent/CA2219659C/en not_active Expired - Lifetime
- 1996-06-05 PL PL96323310A patent/PL184731B1/pl unknown
- 1996-06-05 JP JP50258797A patent/JP3226545B2/ja not_active Expired - Fee Related
- 1996-06-05 KR KR1019970709247A patent/KR100400620B1/ko not_active Expired - Fee Related
- 1996-06-05 PT PT96921931T patent/PT833828E/pt unknown
- 1996-06-05 WO PCT/EP1996/002441 patent/WO1996041807A1/en not_active Ceased
- 1996-06-05 HU HU9802200A patent/HU228234B1/hu unknown
- 1996-06-05 NZ NZ311647A patent/NZ311647A/xx not_active IP Right Cessation
- 1996-06-05 AU AU63006/96A patent/AU712193B2/en not_active Expired
- 1996-06-05 SK SK1682-97A patent/SK284529B6/sk not_active IP Right Cessation
- 1996-06-05 CN CN96194681A patent/CN1124276C/zh not_active Expired - Lifetime
- 1996-06-05 RU RU98100481/04A patent/RU2158267C2/ru active
- 1996-06-05 IL IL12221296A patent/IL122212A/xx not_active IP Right Cessation
- 1996-06-05 EP EP96921931A patent/EP0833828B1/en not_active Expired - Lifetime
- 1996-06-05 CZ CZ19973922A patent/CZ292233B6/cs not_active IP Right Cessation
- 1996-06-05 US US08/973,604 patent/US5985890A/en not_active Expired - Lifetime
- 1996-06-05 DK DK96921931T patent/DK0833828T3/da active
- 1996-06-05 BR BR9609260A patent/BR9609260A/pt not_active Application Discontinuation
- 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 AT AT96921931T patent/ATE228135T1/de active
- 1996-06-05 DE DE69624921T patent/DE69624921T2/de not_active Expired - Lifetime
- 1996-06-06 MY MYPI96002232A patent/MY145291A/en unknown
- 1996-06-06 AR ARP960102978A patent/AR003426A1/es active IP Right Grant
- 1996-06-07 PE PE1996000444A patent/PE4598A1/es not_active IP Right Cessation
- 1996-06-07 CO CO96029756A patent/CO4440629A1/es unknown
- 1996-06-07 TW TW085106847A patent/TW410226B/zh not_active IP Right Cessation
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
1999
- 1999-07-19 US US09/356,587 patent/US6200985B1/en not_active Expired - Lifetime

Also Published As

Publication number	Publication date
JP3226545B2 (ja)	2001-11-05
FI973991A0 (fi)	1997-10-17
AU6300696A (en)	1997-01-09
CZ292233B6 (cs)	2003-08-13
DK0833828T3 (da)	2003-03-17
PL323310A1 (en)	1998-03-16
EP0833828A1 (en)	1998-04-08
HUP9802200A3 (en)	2000-05-29
US6200985B1 (en)	2001-03-13
PE4598A1 (es)	1998-02-19
NZ311647A (en)	1999-11-29
FI113051B (fi)	2004-02-27
DE69624921T2 (de)	2003-09-11
TR199701567T1 (xx)	1998-04-21
FI973991L (fi)	1997-12-09
HUP9802200A2 (hu)	1999-02-01
SK284529B6 (sk)	2005-05-05
NO975432D0 (no)	1997-11-26
KR19990022780A (ko)	1999-03-25
KR100400620B1 (ko)	2004-02-18
CA2219659A1 (en)	1996-12-27
DE69624921D1 (de)	2003-01-02
JP2000510815A (ja)	2000-08-22
IL122212A0 (en)	1998-04-05
MY145291A (en)	2012-01-13
MX9709555A (es)	1998-03-31
CA2219659C (en)	2008-03-18
EP0833828B1 (en)	2002-11-20
HK1014949A1 (en)	1999-10-08
CN1187821A (zh)	1998-07-15
CZ392297A3 (cs)	1998-03-18
IL122212A (en)	2001-08-26
WO1996041807A1 (en)	1996-12-27
CN1124276C (zh)	2003-10-15
RU2158267C2 (ru)	2000-10-27
NO975432L (no)	1997-11-26
AU712193B2 (en)	1999-10-28
PT833828E (pt)	2003-02-28
CO4440629A1 (es)	1997-05-07
HU228234B1 (en)	2013-02-28
ES2187660T3 (es)	2003-06-16
PL184731B1 (pl)	2002-12-31
TW410226B (en)	2000-11-01
US5985890A (en)	1999-11-16
AR003426A1 (es)	1998-08-05
BR9609260A (pt)	1999-05-18
SK168297A3 (en)	1998-05-06
ATE228135T1 (de)	2002-12-15

Publication	Publication Date	Title
NO317058B1 (no)	2004-08-02	Rapamycinderivater, fremgangsmate for fremstilling derav, farmasoytisk preparat omfattende et slikt derivat, kit omfattende et preparat samt anvendelse av derivatene
AU676198B2 (en)	1997-03-06	O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
EP0734389B1 (en)	2000-03-29	Rapamycin derivatives useful as immunosuppressants
JPH0578377A (ja)	1993-03-30	ラパマイシンのシリルエーテル類
MXPA97009555A (es)	1998-10-15	Derivados de rapamicina
HK1014949B (en)	2004-07-09	Rapamycin derivatives
CA2174731C (en)	2006-10-31	Rapamycin derivatives useful as immunosuppressants

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