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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NO20032034L (no
NO20032034D0 (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
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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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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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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    • A61P21/04Drugs 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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    • 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
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    • 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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    • 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
    • A61P37/04Immunostimulants
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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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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
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    • 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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    • 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
    • C07D403/02Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (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) EP2070921A1 (pt)
JP (1) JP4234426B2 (pt)
KR (3) KR100916613B1 (pt)
CN (1) CN1253449C (pt)
AR (1) AR035211A1 (pt)
AT (1) ATE445613T1 (pt)
AU (3) AU2002221810B2 (pt)
BR (1) BRPI0115193B1 (pt)
CA (1) CA2428133C (pt)
CY (1) CY1110564T1 (pt)
CZ (1) CZ307144B6 (pt)
DE (1) DE60140201D1 (pt)
DK (1) DK1337527T3 (pt)
EC (1) ECSP104578A (pt)
ES (1) ES2332770T3 (pt)
HK (1) HK1058789A1 (pt)
HU (1) HU228999B1 (pt)
IL (3) IL155618A0 (pt)
MX (1) MXPA03004037A (pt)
MY (2) MY127157A (pt)
NO (1) NO327427B1 (pt)
NZ (2) NZ535616A (pt)
PE (1) PE20020544A1 (pt)
PL (1) PL208794B1 (pt)
PT (1) PT1337527E (pt)
RU (2) RU2329263C2 (pt)
SG (1) SG159378A1 (pt)
SI (1) SI1337527T1 (pt)
SK (1) SK287919B6 (pt)
TW (2) TW200738687A (pt)
WO (1) WO2002038561A1 (pt)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20040079A1 (es) 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
JP2005531609A (ja) 2002-06-05 2005-10-20 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ キナーゼ阻害剤としてのシスインドリル−マレイミド誘導体
US7232906B2 (en) 2002-06-05 2007-06-19 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
GB0303319D0 (en) 2003-02-13 2003-03-19 Novartis Ag Organic compounds
EP1670497A4 (en) * 2003-09-16 2009-07-15 Garvan Inst Med Res METHODS OF IDENTIFYING C-EPSILON PROTEIN KINASE (PKC ™) MODULATORS AND METHOD FOR TREATING ABERRANT GLUCOSE METABOLISM THEREOF
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
ES2303218T3 (es) 2004-01-19 2008-08-01 Novartis Ag Derivados de indolilmaleimida.
GB0401089D0 (en) * 2004-01-19 2004-02-18 Novartis Ag Organic compounds
AU2005230399B2 (en) * 2004-04-08 2009-07-09 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
KR20080023732A (ko) * 2005-07-11 2008-03-14 노파르티스 아게 인돌릴말레이미드 유도체
US8105587B2 (en) 2005-10-26 2012-01-31 Novartis Ag Methods of treating arthritis using IL-1β binding molecules
JP2009516671A (ja) 2005-11-21 2009-04-23 ノバルティス アクチエンゲゼルシャフト mTOR阻害剤を使用する神経内分泌腫瘍処置
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
JP2010501586A (ja) * 2006-08-23 2010-01-21 ノバルティス アクチエンゲゼルシャフト 眼疾患におけるpkc阻害剤、特にインドリルマレイミド誘導体の使用
CN103265533A (zh) * 2006-10-20 2013-08-28 诺瓦提斯公司 3-(1h-吲哚-3-基)-4-[2-(4-甲基-哌嗪-1-基)-喹唑啉-4-基]-吡咯-2,5-二酮的晶型
US20100075997A1 (en) * 2006-12-07 2010-03-25 Alexander Korn Use of pkc inhibitors in transplantation
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
JP2010528086A (ja) 2007-05-29 2010-08-19 ノバルティス アーゲー 抗il−1治療に関する新しい適応症
RU2010116351A (ru) * 2007-09-27 2012-05-20 Новартис АГ (CH) Мониторинг лекарственных средств
US20100233716A1 (en) 2007-11-08 2010-09-16 Pierre Saint-Mezard Transplant rejection markers
EP2217231B1 (en) * 2007-12-05 2011-11-30 Johannes Gutenberg-Universität Mainz Use of 3-(indolyl)- or 3-(azaindolyl)-4-arylmaleimide derivatives in leukemia management
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
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
MX2012011341A (es) 2010-03-30 2012-11-12 Novartis Ag Inhibidores de pkc para el tratamiento de linfoma de celulas-b que tenga señalizacion activa cronica de receptores de celulas-b.
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