NO327427B1 - Indolylmaleimidderivater, farmasoytiske sammensetninger samt anvendelser av slike. - Google Patents

Indolylmaleimidderivater, farmasoytiske sammensetninger samt anvendelser av slike. Download PDF

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Publication number
NO327427B1
NO327427B1 NO20032034A NO20032034A NO327427B1 NO 327427 B1 NO327427 B1 NO 327427B1 NO 20032034 A NO20032034 A NO 20032034A NO 20032034 A NO20032034 A NO 20032034A NO 327427 B1 NO327427 B1 NO 327427B1
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NO
Norway
Prior art keywords
compound
formula
dione
alkyl
pyrrole
Prior art date
Application number
NO20032034A
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English (en)
Norwegian (no)
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NO20032034D0 (no
NO20032034L (no
Inventor
Rainer Albert
Richard Sedrani
Nigel Graham Cooke
Claus Ehrhardt
Jean-Pierre Evenou
Peter Von Matt
Juergen Wagner
Gerhard Zenke
Sylvain Cottens
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Novartis Ag
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Publication of NO20032034D0 publication Critical patent/NO20032034D0/no
Publication of NO20032034L publication Critical patent/NO20032034L/no
Publication of NO327427B1 publication Critical patent/NO327427B1/no

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/56Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
NO20032034A 2000-11-07 2003-05-06 Indolylmaleimidderivater, farmasoytiske sammensetninger samt anvendelser av slike. NO327427B1 (no)

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 (3)

Publication Number Publication Date
NO20032034D0 NO20032034D0 (no) 2003-05-06
NO20032034L NO20032034L (no) 2003-07-04
NO327427B1 true NO327427B1 (no) 2009-06-29

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ID=26937956

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20032034A NO327427B1 (no) 2000-11-07 2003-05-06 Indolylmaleimidderivater, farmasoytiske sammensetninger samt anvendelser av slike.

Country Status (31)

Country Link
EP (2) EP1337527B1 (zh)
JP (1) JP4234426B2 (zh)
KR (3) KR100748386B1 (zh)
CN (1) CN1253449C (zh)
AR (1) AR035211A1 (zh)
AT (1) ATE445613T1 (zh)
AU (3) AU2002221810B2 (zh)
BR (1) BRPI0115193B1 (zh)
CA (1) CA2428133C (zh)
CY (1) CY1110564T1 (zh)
CZ (1) CZ307144B6 (zh)
DE (1) DE60140201D1 (zh)
DK (1) DK1337527T3 (zh)
EC (1) ECSP104578A (zh)
ES (1) ES2332770T3 (zh)
HK (1) HK1058789A1 (zh)
HU (1) HU228999B1 (zh)
IL (3) IL155618A0 (zh)
MX (1) MXPA03004037A (zh)
MY (2) MY139979A (zh)
NO (1) NO327427B1 (zh)
NZ (2) NZ535616A (zh)
PE (1) PE20020544A1 (zh)
PL (1) PL208794B1 (zh)
PT (1) PT1337527E (zh)
RU (2) RU2329263C2 (zh)
SG (1) SG159378A1 (zh)
SI (1) SI1337527T1 (zh)
SK (1) SK287919B6 (zh)
TW (2) TW200738687A (zh)
WO (1) WO2002038561A1 (zh)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
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TWI324064B (en) * 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
US7232906B2 (en) 2002-06-05 2007-06-19 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
AU2003238874A1 (en) 2002-06-05 2003-12-22 Janssen Pharmaceutica N.V. Bisindolyl-maleimid derivatives as kinase inhibitors
GB0303319D0 (en) 2003-02-13 2003-03-19 Novartis Ag Organic compounds
CA2539132A1 (en) * 2003-09-16 2005-03-24 Garvan Institute Of Medical Research Methods for identifying modulators of protein kinase c-epsilon (pkc.epsilon.) and method of treatment of aberrant glucose metabolism associated therewith
JP2007509185A (ja) * 2003-10-27 2007-04-12 ノバルティス アクチエンゲゼルシャフト βアミロイド産生および/または凝集と関係がある神経障害および血管障害の処置のためのインドリル−ピロールジオン誘導体
EP1687002A4 (en) * 2003-11-10 2008-07-23 Synta Pharmaceuticals Corp CONDENSED HETEROCYCLIC COMPOUNDS
RU2372348C2 (ru) * 2004-01-19 2009-11-10 Новартис Аг Производные индолилмалеимида в качестве ингибиторов ркс
GB0401089D0 (en) * 2004-01-19 2004-02-18 Novartis Ag Organic compounds
JP2007532506A (ja) * 2004-04-08 2007-11-15 ノバルティス アクチエンゲゼルシャフト 自己免疫疾患および拒絶反応の処置のためのタンパク質キナーゼc阻害剤
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
EP1885454A2 (en) 2005-05-04 2008-02-13 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
ES2944067T3 (es) 2005-10-26 2023-06-19 Novartis Ag Uso de anticuerpos anti il-1beta
NO20220050A1 (no) 2005-11-21 2008-08-12 Novartis Ag Neuroendokrin tumorbehandling
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
EP2056831A2 (en) * 2006-08-23 2009-05-13 Novartis AG Use of pkc inhibitors in particular indolylmaleimide derivatives in ocular diseases
MY158026A (en) * 2006-10-20 2016-08-30 Novartis Ag Crystal modifications-3-(1h-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2, 5-dione
MX2009005945A (es) * 2006-12-07 2009-06-17 Novartis Ag Uso de inhibidores de pkc en transplantes.
CN101558062A (zh) 2006-12-19 2009-10-14 诺瓦提斯公司 作为激酶抑制剂的吲哚基马来酰亚胺衍生物
KR20090118110A (ko) * 2007-03-09 2009-11-17 노파르티스 아게 3-(1h-인돌-3-일)-4-[2-(4-메틸-피페라진-1-일)-퀴나졸린-4-일]-피롤-2,5-디온의 염
CA3213888A1 (en) 2007-05-29 2008-12-04 Novartis Ag New indications for anti-il-i-beta therapy
MX2010003259A (es) * 2007-09-27 2010-04-12 Novartis Ag Ensayo de monitoreo de farmacos.
EP2463383A3 (en) 2007-11-08 2012-10-17 Novartis AG Gene expression signatures for chronic/sclerosing allograft nephropathy
ATE535241T1 (de) 2007-12-05 2011-12-15 Univ Mainz Johannes Gutenberg Verwendung von 3-(indolyl)- oder 3-(azaindolyl)-4-arylmaleimid-derivaten bei der behandlung von leukämie
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
CA2767616A1 (en) 2009-07-09 2011-01-13 The Scripps Research Institute Gene expression profiles associated with chronic allograft nephropathy
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
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
US8791100B2 (en) 2010-02-02 2014-07-29 Novartis Ag Aryl benzylamine compounds
EP2552428A1 (en) * 2010-03-30 2013-02-06 Novartis AG Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
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