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SK287919B6 - Indolylmaleimide derivatives, method for the preparation thereof and pharmaceutical composition comprising same - Google Patents

Indolylmaleimide derivatives, method for the preparation thereof and pharmaceutical composition comprising same Download PDF

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Publication number
SK287919B6
SK287919B6 SK546-2003A SK5462003A SK287919B6 SK 287919 B6 SK287919 B6 SK 287919B6 SK 5462003 A SK5462003 A SK 5462003A SK 287919 B6 SK287919 B6 SK 287919B6
Authority
SK
Slovakia
Prior art keywords
piperazinyl
compound
methylpiperazin
methyl
formula
Prior art date
Application number
SK546-2003A
Other languages
English (en)
Slovak (sk)
Other versions
SK5462003A3 (en
Inventor
Rainer Albert
Nigel Graham Cooke
Sylvain Cottens
Claus Ehrhardt
Jean-Pierre Evenou
Richard Sedrani
Matt Peter Von
Jurgen Wagner
Gerhard Zenke
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 SK5462003A3 publication Critical patent/SK5462003A3/sk
Publication of SK287919B6 publication Critical patent/SK287919B6/sk

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
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    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
SK546-2003A 2000-11-07 2001-11-05 Indolylmaleimide derivatives, method for the preparation thereof and pharmaceutical composition comprising same SK287919B6 (sk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24640000P 2000-11-07 2000-11-07
US28370501P 2001-04-13 2001-04-13
PCT/EP2001/012785 WO2002038561A1 (en) 2000-11-07 2001-11-05 Indolylmaleimide derivatives as protein kinase c inhibitors

Publications (2)

Publication Number Publication Date
SK5462003A3 SK5462003A3 (en) 2003-11-04
SK287919B6 true SK287919B6 (sk) 2012-03-02

Family

ID=26937956

Family Applications (1)

Application Number Title Priority Date Filing Date
SK546-2003A SK287919B6 (sk) 2000-11-07 2001-11-05 Indolylmaleimide derivatives, method for the preparation thereof and pharmaceutical composition comprising same

Country Status (31)

Country Link
EP (2) EP1337527B1 (no)
JP (1) JP4234426B2 (no)
KR (3) KR100916613B1 (no)
CN (1) CN1253449C (no)
AR (1) AR035211A1 (no)
AT (1) ATE445613T1 (no)
AU (3) AU2002221810B2 (no)
BR (1) BRPI0115193B1 (no)
CA (1) CA2428133C (no)
CY (1) CY1110564T1 (no)
CZ (1) CZ307144B6 (no)
DE (1) DE60140201D1 (no)
DK (1) DK1337527T3 (no)
EC (1) ECSP104578A (no)
ES (1) ES2332770T3 (no)
HK (1) HK1058789A1 (no)
HU (1) HU228999B1 (no)
IL (3) IL155618A0 (no)
MX (1) MXPA03004037A (no)
MY (2) MY127157A (no)
NO (1) NO327427B1 (no)
NZ (2) NZ535616A (no)
PE (1) PE20020544A1 (no)
PL (1) PL208794B1 (no)
PT (1) PT1337527E (no)
RU (2) RU2329263C2 (no)
SG (1) SG159378A1 (no)
SI (1) SI1337527T1 (no)
SK (1) SK287919B6 (no)
TW (2) TWI290553B (no)
WO (1) WO2002038561A1 (no)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI324064B (en) * 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
CA2488798A1 (en) 2002-06-05 2003-12-18 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
WO2003104222A1 (en) 2002-06-05 2003-12-18 Janssen Pharmaceutica N.V. Bisindolyl-maleimid derivatives as kinase inhibitors
GB0303319D0 (en) * 2003-02-13 2003-03-19 Novartis Ag Organic compounds
US8598146B2 (en) 2003-09-16 2013-12-03 Garvan Institute Of Medical Research Methods for identifying modulators of protein kinase C-epsilon (PKCε) and method of treatment of aberrant glucose metabolism associated therewith
US20070142401A1 (en) * 2003-10-27 2007-06-21 Novartis Ag Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation
AU2004289303A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
GB0401089D0 (en) * 2004-01-19 2004-02-18 Novartis Ag Organic compounds
RU2373201C2 (ru) 2004-01-19 2009-11-20 Новартис Аг Индолилмалеимидные производные
CA2560311A1 (en) * 2004-04-08 2005-10-20 Novartis Ag Protein kinase c inhibitors for the treatment of autoimmune diseases and of transplant rejection
GB0410713D0 (en) * 2004-05-13 2004-06-16 Novartis Ag Organic compounds
US8008320B2 (en) 2004-12-08 2011-08-30 Johannes Gutenberg-Universitatis 3-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors
GB0504203D0 (en) * 2005-03-01 2005-04-06 Novartis Ag Organic compounds
GB0507918D0 (en) 2005-04-19 2005-05-25 Novartis Ag Organic compounds
WO2006117212A2 (en) 2005-05-04 2006-11-09 Develogen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
GB0511060D0 (en) 2005-05-31 2005-07-06 Novartis Ag Organic compounds
ES2396671T3 (es) 2005-07-11 2013-02-25 Novartis Ag Derivados de la indolilmaleimida como inhibidores de la proteína quinasa
KR20170038131A (ko) 2005-10-26 2017-04-05 노파르티스 아게 Ｉｌ-1베타 화합물의 신규 용도
ES2481671T3 (es) 2005-11-21 2014-07-31 Novartis Ag Inhibidores de mTOR en el tratamiento de tumores endocrinos
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
GB0605691D0 (en) * 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
GB0613162D0 (en) * 2006-06-30 2006-08-09 Novartis Ag Organic compounds
MX2009001936A (es) * 2006-08-23 2009-03-06 Novartis Ag Uso de inhibidores de pkc en particular derivados de indolilmaleimida en enfermedades ocualres.
WO2008051440A1 (en) * 2006-10-20 2008-05-02 Novartis Ag Crystal modifications -3- (1h-ind0l-3-yl) -4- [2- (4-methyl-piperazin-1-yl) -quinazolin-4-yl] -pyrrole-2, 5-d ione
MX2009005945A (es) * 2006-12-07 2009-06-17 Novartis Ag Uso de inhibidores de pkc en transplantes.
US8193236B2 (en) 2006-12-19 2012-06-05 Novartis Ag Indolylmaleimide derivatives processes for their production and pharmaceutical compositions
BRPI0808354A2 (pt) * 2007-03-09 2014-07-29 Novartis Ag Sais de 3-(1h-indol-3-il)-4-[2-(4-metil-piperazin-1-il)-quinazolin-4 -il]-pirrola-2,5-diona
EP4177268A3 (en) 2007-05-29 2023-05-24 Novartis AG New indications for anti-il-1beta therapy
RU2010116351A (ru) * 2007-09-27 2012-05-20 Новартис АГ (CH) Мониторинг лекарственных средств
EP2209916B1 (en) 2007-11-08 2011-12-21 Novartis AG Gene expression signatures for chronic/sclerosing allograft nephropathy
JP5576290B2 (ja) * 2007-12-05 2014-08-20 ヨハネス、グーテンベルク−ウニフェルジテート、マインツ 白血病の管理における３−（インドリル）−または３−（アザインドリル）−４−アリールマレイミド誘導体の用途
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
WO2011006119A2 (en) 2009-07-09 2011-01-13 The Scripps Research Institute Gene expression profiles associated with chronic allograft nephropathy
EP2343291A1 (en) 2009-12-18 2011-07-13 Johannes Gutenberg-Universität Mainz 3-(Indolyl)- or 3-(Azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
EP2338486A1 (en) 2009-12-18 2011-06-29 Johannes Gutenberg-Universität Mainz 3-(indolyl)- or 3-(azaindolyl)-4-arylmaleimide derivatives for use in the treatment of colon and gastric adenocarcinoma
US8791100B2 (en) 2010-02-02 2014-07-29 Novartis Ag Aryl benzylamine compounds
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