AU1757188A - N-substituted derivatives of staurosporine - Google Patents

N-substituted derivatives of staurosporine

Info

Publication number
AU1757188A
AU1757188A AU17571/88A AU1757188A AU1757188A AU 1757188 A AU1757188 A AU 1757188A AU 17571/88 A AU17571/88 A AU 17571/88A AU 1757188 A AU1757188 A AU 1757188A AU 1757188 A AU1757188 A AU 1757188A
Authority
AU
Australia
Prior art keywords
substituted derivatives
formula
staurosporine
stau
staurosporin
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
AU17571/88A
Other versions
AU617324B2 (en
Inventor
Giorgio Caravatti
Andreas Fredenhagen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU1757188A publication Critical patent/AU1757188A/en
Application granted granted Critical
Publication of AU617324B2 publication Critical patent/AU617324B2/en
Assigned to NOVARTIS AG reassignment NOVARTIS AG Request to Amend Deed and Register Assignors: CIBA-GEIGY AG
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

Links

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 System
    • 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

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.
AU17571/88A 1987-06-15 1988-06-10 N-substituted derivatives of staurosporine Expired AU617324B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CH224487 1987-06-15
CH2244/87 1987-06-15
CH1440/88 1988-04-19
CH144088 1988-04-19

Publications (2)

Publication Number Publication Date
AU1757188A true AU1757188A (en) 1988-12-15
AU617324B2 AU617324B2 (en) 1991-11-28

Family

ID=25687663

Family Applications (1)

Application Number Title Priority Date Filing Date
AU17571/88A Expired AU617324B2 (en) 1987-06-15 1988-06-10 N-substituted derivatives of staurosporine

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)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5461146A (en) * 1992-07-24 1995-10-24 Cephalon, Inc. Selected protein kinase inhibitors for the treatment of neurological disorders
US5621101A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
US5621100A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5741808A (en) * 1992-07-24 1998-04-21 Cephalon, Inc. Protein kinase inhibitors for treatmen of neurological disorders
US6184217B1 (en) 1996-06-25 2001-02-06 Cephalon, Inc. Use of K-252a derivative
US6306849B1 (en) 1996-06-03 2001-10-23 Cephalon, Inc. Selected derivatives of K-252a
US6875865B1 (en) 1996-06-03 2005-04-05 Cephalon, Inc. Selected derivatives of K-252a

Families Citing this family (48)

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JPS62220196A (en) * 1986-03-20 1987-09-28 Kyowa Hakko Kogyo Co Ltd Ucn-01 and production thereof
JP2766360B2 (en) * 1988-02-04 1998-06-18 協和醗酵工業株式会社 Staurosporine derivative
CZ280738B6 (en) * 1988-02-10 1996-04-17 F. Hoffmann - La Roche And Co., Aktiengesellschaft Substituted pyrroles, their use for preparing medicaments and medicaments based thereon
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
DE69331228D1 (en) * 1992-09-21 2002-01-10 Kyowa Hakko Kogyo Kk Heilmittel für thrombozytopenia
US5981568A (en) 1993-01-28 1999-11-09 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
ATE485825T1 (en) 1993-01-28 2010-11-15 Boston Scient Ltd THERAPEUTIC INHIBITORS OF VASCULAR SMOOTH CELLS
PH30300A (en) * 1993-05-07 1997-01-20 Ciba Geigy Ag Polycyclic compounds and processes for the preparation thereof
AU7080994A (en) * 1993-07-09 1995-02-06 Institute Of Cancer Research, The 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
ES2226120T3 (en) 1997-03-31 2005-03-16 Boston Scientific Limited THERAPEUTIC CELL INHIBITOR OF THE VASCULAR SMOOTH MUSCLE.
ES2211197T3 (en) * 1998-11-23 2004-07-01 Novartis Ag USE OF ESTAUROSPORINE DERIVATIVES TO TREAT OCULAR NEOVASCULAR DISEASES.
PL414997A1 (en) 2001-02-19 2016-02-29 Novartis Ag Application of 40-O-(2-hydroxyethyl)-rapamycin for treatment of solid kidney tumors
DE60219617T2 (en) 2001-05-16 2008-01-03 Novartis Ag COMBINATION OF N-5- 4- (4-METHYL-PIPERAZINO-METHYL) -BENZOYLAMIDO -2-METHYLPHENYL -4- (3-PYRIDIL) -2-PYRIMIDINE AMINE WITH A BIPHOSPHONATE
PT1441737E (en) 2001-10-30 2006-12-29 Dana Farber Cancer Inst Inc 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
KR20120125398A (en) 2002-05-16 2012-11-14 노파르티스 아게 Use of edg receptor binding agents in cancer
EP2319493A3 (en) * 2002-07-23 2011-07-27 Novartis AG Ophthalmic ointment composition comprising a drug, an ointment base and a solubilizing/dispersing agent
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
CA2524048C (en) 2003-05-19 2013-06-25 Irm Llc Immunosuppressant compounds and compositions
US20040246627A1 (en) * 2003-06-06 2004-12-09 Durrum Thomas M. Disc drive pivot bearing assembly
BRPI0413439A (en) 2003-08-08 2006-10-17 Novartis Ag combinations comprising staurosporines
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
BRPI0514765A (en) * 2004-08-31 2008-06-24 Novartis Ag organic compounds
JO2897B1 (en) * 2004-11-05 2015-09-15 نوفارتيس ايه جي Organic compounds
ES2481671T3 (en) 2005-11-21 2014-07-31 Novartis Ag MTOR inhibitors in the treatment of endocrine tumors
MX2011006610A (en) 2008-12-18 2011-06-30 Novartis Ag New polymorphic form of 1-(4-{l-[(e)-4-cyclohexyl--3-triflu oromethyl-benzyloxyimino]-ethyl)-2-ethyl-benzy l)-azetidine -3-carboxylic.
KR20170062554A (en) 2008-12-18 2017-06-07 노파르티스 아게 Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid
WO2010080455A1 (en) 2008-12-18 2010-07-15 Novartis Ag New salts
EP2327706A1 (en) 2009-11-30 2011-06-01 Novartis AG Polymorphous forms III and IV of N-benzoyl-staurosporine
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
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
EP2760862B1 (en) 2011-09-27 2015-10-21 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
WO2021097256A1 (en) 2019-11-14 2021-05-20 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2766360B2 (en) * 1988-02-04 1998-06-18 協和醗酵工業株式会社 Staurosporine derivative

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5461146A (en) * 1992-07-24 1995-10-24 Cephalon, Inc. Selected protein kinase inhibitors for the treatment of neurological disorders
US5621101A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
US5621100A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5741808A (en) * 1992-07-24 1998-04-21 Cephalon, Inc. Protein kinase inhibitors for treatmen of neurological disorders
US5756494A (en) * 1992-07-24 1998-05-26 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
US6306849B1 (en) 1996-06-03 2001-10-23 Cephalon, Inc. Selected derivatives of K-252a
US6875865B1 (en) 1996-06-03 2005-04-05 Cephalon, Inc. Selected derivatives of K-252a
US6184217B1 (en) 1996-06-25 2001-02-06 Cephalon, Inc. Use of K-252a derivative

Also Published As

Publication number Publication date
DE3855015D1 (en) 1996-03-28
PT87719B (en) 1992-10-30
ATE134375T1 (en) 1996-03-15
GR3019064T3 (en) 1996-05-31
MY104316A (en) 1994-03-31
HK1003788A1 (en) 1998-11-06
PT87719A (en) 1988-07-01
IE881787L (en) 1988-12-15
EP0296110B1 (en) 1996-02-21
JPS6434989A (en) 1989-02-06
KR890000494A (en) 1989-03-15
NO170634C (en) 1992-11-11
NO882613L (en) 1988-12-16
EP0296110A3 (en) 1991-02-27
DK175507B1 (en) 2004-11-15
KR970001529B1 (en) 1997-02-11
EP0296110A2 (en) 1988-12-21
DK324888A (en) 1988-12-16
FI89362B (en) 1993-06-15
IL86632A0 (en) 1988-11-30
AU617324B2 (en) 1991-11-28
IE70523B1 (en) 1996-12-11
YU115488A (en) 1989-12-31
DK324888D0 (en) 1988-06-14
CA1337763C (en) 1995-12-19
FI882808A0 (en) 1988-06-13
FI89362C (en) 1993-09-27
NO882613D0 (en) 1988-06-14
NZ225018A (en) 1990-09-26
FI882808A (en) 1988-12-16
NO170634B (en) 1992-08-03
ES2083956T3 (en) 1996-05-01
JP2708047B2 (en) 1998-02-04
HU201329B (en) 1990-10-28
HUT47587A (en) 1989-03-28

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