NZ225018A - Staurosporine derivatives of the formula (stau)-n(ch 3 )-r, pharmaceutical compositions and processes for preparation - Google Patents
Staurosporine derivatives of the formula (stau)-n(ch 3 )-r, pharmaceutical compositions and processes for preparationInfo
- Publication number
- NZ225018A NZ225018A NZ225018A NZ22501888A NZ225018A NZ 225018 A NZ225018 A NZ 225018A NZ 225018 A NZ225018 A NZ 225018A NZ 22501888 A NZ22501888 A NZ 22501888A NZ 225018 A NZ225018 A NZ 225018A
- Authority
- NZ
- New Zealand
- Prior art keywords
- formula
- stau
- processes
- preparation
- pharmaceutical compositions
- Prior art date
Links
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical class C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 102000003923 Protein Kinase C Human genes 0.000 abstract 1
- 108090000315 Protein Kinase C Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 230000010933 acylation Effects 0.000 abstract 1
- 238000005917 acylation reaction Methods 0.000 abstract 1
- 230000029936 alkylation Effects 0.000 abstract 1
- 238000005804 alkylation reaction Methods 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- HKSZLNNOFSGOKW-UHFFFAOYSA-N ent-staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(C)O1 HKSZLNNOFSGOKW-UHFFFAOYSA-N 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D498/22—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 four or more hetero rings
-
- 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
- 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
- A61P37/04—Immunostimulants
-
- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (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)
- Steroid Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
N-Substituted derivatives of staurosporin of the formula [Stau]-N(CH3)-R (I> in which [Stau] represents the radical of the sub-formula <IMAGE> in which R represents a hydrocarbyl R<0> or an acyl Ac, which preferably have at most 30 C atoms, and salts of compounds of the formula I having salt-forming properties, are distinguished as selective inhibitors of protein kinase C. They are prepared by conventional alkylation or acylation of staurosporin.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH224487 | 1987-06-15 | ||
| CH144088 | 1988-04-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ225018A true NZ225018A (en) | 1990-09-26 |
Family
ID=25687663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ225018A NZ225018A (en) | 1987-06-15 | 1988-06-14 | Staurosporine derivatives of the formula (stau)-n(ch 3 )-r, pharmaceutical compositions and processes for preparation |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP0296110B1 (en) |
| JP (1) | JP2708047B2 (en) |
| KR (1) | KR970001529B1 (en) |
| AT (1) | ATE134375T1 (en) |
| AU (1) | AU617324B2 (en) |
| CA (1) | CA1337763C (en) |
| DE (1) | DE3855015D1 (en) |
| DK (1) | DK175507B1 (en) |
| ES (1) | ES2083956T3 (en) |
| FI (1) | FI89362C (en) |
| GR (1) | GR3019064T3 (en) |
| HK (1) | HK1003788A1 (en) |
| HU (1) | HU201329B (en) |
| IE (1) | IE70523B1 (en) |
| IL (1) | IL86632A0 (en) |
| MY (1) | MY104316A (en) |
| NO (1) | NO170634C (en) |
| NZ (1) | NZ225018A (en) |
| PT (1) | PT87719B (en) |
| YU (1) | YU115488A (en) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62220196A (en) * | 1986-03-20 | 1987-09-28 | Kyowa Hakko Kogyo Co Ltd | Ucn-01 and production thereof |
| WO1989007105A1 (en) * | 1988-02-04 | 1989-08-10 | Kyowa Hakko Kogyo Co., Ltd. | Staurosporin derivatives |
| SK278989B6 (en) * | 1988-02-10 | 1998-05-06 | F. Hoffmann-La Roche Ag | Substituted pyrroles, their use for producing a drug, and the drug on their base |
| USRE36736E (en) * | 1989-02-06 | 2000-06-13 | Hoffman-La Roche Inc. | Substituted pyrroles |
| DE3924538A1 (en) * | 1989-07-25 | 1991-01-31 | Goedecke Ag | INDOLOCARBAZOL AND THEIR USE |
| US5618809A (en) * | 1989-12-14 | 1997-04-08 | Schering Corporation | Indolocarbazoles from saccharothrix aerocolonigenes copiosa subsp. nov SCC 1951 ATCC 53856 |
| US5292747A (en) * | 1990-08-07 | 1994-03-08 | Hoffman-La Roche Inc. | Substituted pyrroles |
| EP0540185A1 (en) * | 1991-10-10 | 1993-05-05 | Schering Corporation | 4'-(N-substituted-N-oxide)staurosporine derivatives |
| EP0541486A1 (en) * | 1991-11-07 | 1993-05-12 | Ciba-Geigy Ag | Polycyclic conjugates |
| WO1993018771A1 (en) * | 1992-03-24 | 1993-09-30 | Asahi Kasei Kogyo Kabushiki Kaisha | PLATELET AGGLUTINATION INHIBITOR CONTAINING STAUROSPORINE η-LACTAM DERIVATIVE |
| US5621101A (en) * | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
| US5461146A (en) * | 1992-07-24 | 1995-10-24 | Cephalon, Inc. | Selected protein kinase inhibitors for the treatment of neurological disorders |
| US5621100A (en) * | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | K-252a derivatives for treatment of neurological disorders |
| US5756494A (en) * | 1992-07-24 | 1998-05-26 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
| DE69331228D1 (en) * | 1992-09-21 | 2002-01-10 | Kyowa Hakko Kogyo Kk | Heilmittel für thrombozytopenia |
| DE69435318D1 (en) | 1993-01-28 | 2010-12-09 | Boston Scient Ltd | THERAPEUTIC INHIBITORS OF THE CELLS OF THE SMOOTH VASCULAR MUSCULAR |
| US5981568A (en) | 1993-01-28 | 1999-11-09 | Neorx Corporation | Therapeutic inhibitor of vascular smooth muscle cells |
| PH30300A (en) * | 1993-05-07 | 1997-01-20 | Ciba Geigy Ag | Polycyclic compounds and processes for the preparation thereof |
| WO1995002057A1 (en) * | 1993-07-09 | 1995-01-19 | The Institute Of Cancer Research | Protein tyrosine kinase and ligands thereof |
| GB9325395D0 (en) * | 1993-12-11 | 1994-02-16 | Ciba Geigy Ag | Compositions |
| EP0711557A1 (en) * | 1994-11-09 | 1996-05-15 | Ciba-Geigy Ag | Base for formulating pharmaceutical agents |
| US6875865B1 (en) | 1996-06-03 | 2005-04-05 | Cephalon, Inc. | Selected derivatives of K-252a |
| UA67725C2 (en) | 1996-06-03 | 2004-07-15 | Cephalon Inc | K-252a derivatives and a method for improvement of functioning and cell survival enhancement |
| JP2000514420A (en) | 1996-06-25 | 2000-10-31 | セファロン・インコーポレイテッド | Use of K-252A Derivatives for the Treatment of Peripheral or Central Nervous Disorders and Cytokine Overproduction |
| ATE278397T1 (en) | 1997-03-31 | 2004-10-15 | Boston Scient Ltd | USE OF CYTOSKELETON INHIBITORS TO PREVENT RESTENOSIS |
| ATE252387T1 (en) * | 1998-11-23 | 2003-11-15 | Novartis Pharma Gmbh | USE OF STAUROSPORINE DERIVATIVES FOR THE TREATMENT OF OCCULAR NEOVASCULAR DISEASES |
| PT2269603E (en) | 2001-02-19 | 2015-09-09 | Novartis Ag | Treatment of breast tumors with a rapamycin derivative in combination with exemestane |
| JP4477303B2 (en) | 2001-05-16 | 2010-06-09 | ノバルティス アーゲー | N- {5- [4- (4-Methyl-piperazino-methyl) -benzoylamide] -2-methylphenyl} -4- (3-pyridyl) -2-pyrimidin-amine and a combination comprising a chemotherapeutic agent Agent |
| KR20090087139A (en) * | 2001-10-30 | 2009-08-14 | 노파르티스 아게 | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
| US6887864B2 (en) | 2002-03-12 | 2005-05-03 | Hoffmann-La Roche Inc. | Azepane derivatives |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| CN1652757B (en) | 2002-05-16 | 2012-02-08 | 诺瓦提斯公司 | Use of EDG receptor binding agents in cancer |
| WO2004009056A1 (en) * | 2002-07-23 | 2004-01-29 | Novartis Ag | Ophtalmic ointment composition comprising a drug, an ointment base and a solubiling/dispersing agent |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| PE20050158A1 (en) | 2003-05-19 | 2005-05-12 | Irm Llc | IMMUNOSUPPRESSOR COMPOUNDS AND COMPOSITIONS |
| US20040246627A1 (en) * | 2003-06-06 | 2004-12-09 | Durrum Thomas M. | Disc drive pivot bearing assembly |
| JP2007501774A (en) | 2003-08-08 | 2007-02-01 | ノバルティス アクチエンゲゼルシャフト | Combinations containing staurosporine |
| TW200538433A (en) | 2004-02-24 | 2005-12-01 | Irm Llc | Immunosuppressant compounds and compositiions |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| WO2006024494A1 (en) * | 2004-08-31 | 2006-03-09 | Novartis Ag | Use of midostaurin for treating gastrointestinal stromal tumors |
| JO2897B1 (en) * | 2004-11-05 | 2015-09-15 | نوفارتيس ايه جي | Organic compounds |
| SI2275103T1 (en) | 2005-11-21 | 2014-07-31 | Novartis Ag | mTOR inhibitors in the treatment of endocrine tumors |
| PE20120336A1 (en) | 2008-12-18 | 2012-04-30 | Novartis Ag | 1- [4- [1- (4-CYCLOHEXIL-3-TRIFLOURO-METHYL-BENZYLOXY-IMINO) -ETHYL) -2-ETHYL-BENZYL] -AZETHYL-3-CARBOXYL ACID SALT OF HEMI-FUMARATE |
| AU2009335887A1 (en) | 2008-12-18 | 2011-06-30 | Novartis Ag | New salts |
| BRPI0922457A2 (en) | 2008-12-18 | 2015-12-15 | Novartis Ag | polymorphic form of 1- (4- {1 - [(e) -4-cyclohexyl-3-trifluoromethyl-benzyloxy-imino] -ethyl) -2-ethyl-benzyl) -azetidine-3-carboxylic acid " |
| EP2327706A1 (en) | 2009-11-30 | 2011-06-01 | Novartis AG | Polymorphous forms III and IV of N-benzoyl-staurosporine |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US8846712B2 (en) | 2011-09-12 | 2014-09-30 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013167403A1 (en) | 2012-05-09 | 2013-11-14 | Sanofi | Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors |
| WO2019215759A1 (en) * | 2018-05-09 | 2019-11-14 | Alaparthi Lakshmi Prasad | An improved process for preparation of midostaurin |
| US20220395553A1 (en) | 2019-11-14 | 2022-12-15 | Cohbar, Inc. | Cxcr4 antagonist peptides |
| IT202000004291A1 (en) * | 2020-03-02 | 2021-09-02 | Indena Spa | PROCESS FOR THE PURIFICATION OF CARBAZOLIC INDOLE ALKALOIDS |
| CN112812129A (en) * | 2020-12-31 | 2021-05-18 | 浙江海正药业股份有限公司 | Novel crystalline form of midostaurin, process for its preparation and its use |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1989007105A1 (en) * | 1988-02-04 | 1989-08-10 | Kyowa Hakko Kogyo Co., Ltd. | Staurosporin derivatives |
-
1988
- 1988-06-06 IL IL86632A patent/IL86632A0/en not_active IP Right Cessation
- 1988-06-09 EP EP88810383A patent/EP0296110B1/en not_active Expired - Lifetime
- 1988-06-09 ES ES88810383T patent/ES2083956T3/en not_active Expired - Lifetime
- 1988-06-09 MY MYPI88000629A patent/MY104316A/en unknown
- 1988-06-09 DE DE3855015T patent/DE3855015D1/en not_active Expired - Lifetime
- 1988-06-09 AT AT88810383T patent/ATE134375T1/en not_active IP Right Cessation
- 1988-06-10 AU AU17571/88A patent/AU617324B2/en not_active Expired
- 1988-06-13 FI FI882808A patent/FI89362C/en active IP Right Grant
- 1988-06-13 CA CA000569303A patent/CA1337763C/en not_active Expired - Lifetime
- 1988-06-14 YU YU01154/88A patent/YU115488A/en unknown
- 1988-06-14 PT PT87719A patent/PT87719B/en not_active IP Right Cessation
- 1988-06-14 DK DK198803248A patent/DK175507B1/en not_active IP Right Cessation
- 1988-06-14 HU HU883048A patent/HU201329B/en unknown
- 1988-06-14 KR KR1019880007102A patent/KR970001529B1/en not_active IP Right Cessation
- 1988-06-14 NO NO882613A patent/NO170634C/en not_active IP Right Cessation
- 1988-06-14 NZ NZ225018A patent/NZ225018A/en unknown
- 1988-06-14 IE IE178788A patent/IE70523B1/en not_active IP Right Cessation
- 1988-06-15 JP JP63145937A patent/JP2708047B2/en not_active Expired - Lifetime
-
1996
- 1996-02-22 GR GR960400221T patent/GR3019064T3/en unknown
-
1998
- 1998-04-04 HK HK98102862A patent/HK1003788A1/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| DK175507B1 (en) | 2004-11-15 |
| FI89362C (en) | 1993-09-27 |
| HUT47587A (en) | 1989-03-28 |
| ATE134375T1 (en) | 1996-03-15 |
| EP0296110B1 (en) | 1996-02-21 |
| KR970001529B1 (en) | 1997-02-11 |
| KR890000494A (en) | 1989-03-15 |
| YU115488A (en) | 1989-12-31 |
| NO882613D0 (en) | 1988-06-14 |
| PT87719A (en) | 1988-07-01 |
| NO170634C (en) | 1992-11-11 |
| IE70523B1 (en) | 1996-12-11 |
| IE881787L (en) | 1988-12-15 |
| GR3019064T3 (en) | 1996-05-31 |
| JPS6434989A (en) | 1989-02-06 |
| AU1757188A (en) | 1988-12-15 |
| ES2083956T3 (en) | 1996-05-01 |
| DK324888A (en) | 1988-12-16 |
| EP0296110A3 (en) | 1991-02-27 |
| PT87719B (en) | 1992-10-30 |
| IL86632A0 (en) | 1988-11-30 |
| HU201329B (en) | 1990-10-28 |
| AU617324B2 (en) | 1991-11-28 |
| FI882808A0 (en) | 1988-06-13 |
| DE3855015D1 (en) | 1996-03-28 |
| EP0296110A2 (en) | 1988-12-21 |
| HK1003788A1 (en) | 1998-11-06 |
| MY104316A (en) | 1994-03-31 |
| CA1337763C (en) | 1995-12-19 |
| FI882808A (en) | 1988-12-16 |
| NO170634B (en) | 1992-08-03 |
| NO882613L (en) | 1988-12-16 |
| JP2708047B2 (en) | 1998-02-04 |
| DK324888D0 (en) | 1988-06-14 |
| FI89362B (en) | 1993-06-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RENW | Renewal (renewal fees accepted) |