CA2428133C - Indolylmaleimide derivatives as protein kinase c inhibitors - Google Patents

Indolylmaleimide derivatives as protein kinase c inhibitors Download PDF

Info

Publication number
CA2428133C
CA2428133C CA002428133A CA2428133A CA2428133C CA 2428133 C CA2428133 C CA 2428133C CA 002428133 A CA002428133 A CA 002428133A CA 2428133 A CA2428133 A CA 2428133A CA 2428133 C CA2428133 C CA 2428133C
Authority
CA
Canada
Prior art keywords
4alkyl
compound
methyl
formula
inflammatory
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.)
Expired - Fee Related
Application number
CA002428133A
Other languages
English (en)
French (fr)
Other versions
CA2428133A1 (en
Inventor
Rainer Albert
Nigel Graham Cooke
Sylvain Cottens
Claus Ehrhardt
Jean-Pierre Evenou
Richard Sedrani
Peter Von Matt
Jurgen Wagner
Gerhard Zenke
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 CA2428133A1 publication Critical patent/CA2428133A1/en
Application granted granted Critical
Publication of CA2428133C publication Critical patent/CA2428133C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • 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
    • 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
    • A61P37/06—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
CA002428133A 2000-11-07 2001-11-05 Indolylmaleimide derivatives as protein kinase c inhibitors Expired - Fee Related CA2428133C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24640000P 2000-11-07 2000-11-07
US60/246,400 2000-11-07
US28370501P 2001-04-13 2001-04-13
US60/283,705 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
CA2428133A1 CA2428133A1 (en) 2002-05-16
CA2428133C true CA2428133C (en) 2009-12-29

Family

ID=26937956

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002428133A Expired - Fee Related CA2428133C (en) 2000-11-07 2001-11-05 Indolylmaleimide derivatives as protein kinase c inhibitors

Country Status (30)

Country Link
EP (2) EP1337527B1 (enExample)
JP (1) JP4234426B2 (enExample)
KR (3) KR100748386B1 (enExample)
CN (1) CN1253449C (enExample)
AR (1) AR035211A1 (enExample)
AT (1) ATE445613T1 (enExample)
AU (3) AU2181002A (enExample)
BR (1) BRPI0115193B1 (enExample)
CA (1) CA2428133C (enExample)
CY (1) CY1110564T1 (enExample)
CZ (1) CZ307144B6 (enExample)
DE (1) DE60140201D1 (enExample)
DK (1) DK1337527T3 (enExample)
EC (1) ECSP104578A (enExample)
ES (1) ES2332770T3 (enExample)
HU (1) HU228999B1 (enExample)
IL (3) IL155618A0 (enExample)
MX (1) MXPA03004037A (enExample)
MY (2) MY127157A (enExample)
NO (1) NO327427B1 (enExample)
NZ (2) NZ525656A (enExample)
PE (1) PE20020544A1 (enExample)
PL (1) PL208794B1 (enExample)
PT (1) PT1337527E (enExample)
RU (2) RU2329263C2 (enExample)
SG (1) SG159378A1 (enExample)
SI (1) SI1337527T1 (enExample)
SK (1) SK287919B6 (enExample)
TW (2) TWI290553B (enExample)
WO (1) WO2002038561A1 (enExample)

Families Citing this family (84)

* 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
JP2005531607A (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置換ピロリン
EP1513830A1 (en) 2002-06-05 2005-03-16 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
WO2005039549A1 (en) * 2003-10-27 2005-05-06 Novartis Ag Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation
CA2545340A1 (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
ATE391127T1 (de) 2004-01-19 2008-04-15 Novartis Pharma Gmbh Indolylmaleimidderivate
BRPI0509754A (pt) * 2004-04-08 2007-10-16 Novartis Ag inibidores de proteìna quinase c para o tratamento de doenças auto-imunes e de rejeição a transplante
GB0410713D0 (en) * 2004-05-13 2004-06-16 Novartis Ag Organic compounds
WO2006061212A1 (en) 2004-12-08 2006-06-15 Johannes Gutenberg-Universität Mainz 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
DE602006019732D1 (de) 2005-07-11 2011-03-03 Novartis Ag Indolylmaleimidderivate
BRPI0617830B8 (pt) 2005-10-26 2021-05-25 Novartis Ag uso de um anticorpo de ligação il-1beta e composições farmacêuticas compreendendo o mesmo
NZ568182A (en) 2005-11-21 2010-08-27 Novartis Ag Neuroendocrine tumor treatment using MTOR inhibitors
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
RU2009110257A (ru) * 2006-08-23 2010-09-27 Новартис АГ (CH) Применение ингибиторов ркс, прежде всего производных индолилмалеимида для лечения глазных заболеваний
KR20090073231A (ko) * 2006-10-20 2009-07-02 노파르티스 아게 ３-(１ｈ-인돌-３-일)-４-[２-(４-메틸-피페라진-１-일)-퀴나졸린-４-일]-피롤-２,５-디온의 결정 변체
RU2494738C2 (ru) * 2006-12-07 2013-10-10 Новартис Аг Применение ингибиторов пкс при трансплантации
EP2094689B1 (en) * 2006-12-19 2013-04-03 Novartis AG Indolylmaleimide derivatives as kinase inhibitors
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
BRPI0812040A2 (pt) 2007-05-29 2014-10-21 Novartis Ag Indicações para terapia de anti-il-i-beta
AU2008303540B2 (en) * 2007-09-27 2012-04-26 Novartis Ag Drug monitoring assay
JP2011515068A (ja) 2007-11-08 2011-05-19 ノバルティス アーゲー 慢性／硬化性同種移植腎症に対する遺伝子発現シグネチャー
WO2009071620A1 (en) * 2007-12-05 2009-06-11 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
CA2767616A1 (en) 2009-07-09 2011-01-13 The Scripps Research Institute Gene expression profiles associated with chronic allograft nephropathy
RU2441000C2 (ru) * 2009-11-27 2012-01-27 Общество с ограниченной ответственностью "Молекулярные Технологии" 4-(1-(4-(4-метоксифенилтио)-2,5-диоксо-2,5-дигидро-1н-пирро-3-ил)-1н-индол-3-ил)бутилкарбамимидотиоат и способ его применения
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
WO2011120911A1 (en) 2010-03-30 2011-10-06 Novartis Ag Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
EP2474541A1 (en) 2010-12-23 2012-07-11 Johannes- Gutenberg-Universität Mainz Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
CN102153605B (zh) * 2011-03-02 2014-02-19 福建省微生物研究所 一种咪唑立宾的提纯方法
UY34072A (es) 2011-05-17 2013-01-03 Novartis Ag Derivados sustituidos de indol
JP2014518256A (ja) 2011-06-27 2014-07-28 ノバルティス アーゲー テトラヒドロ−ピリド−ピリミジン誘導体の固体形態および塩類
GB201111427D0 (en) * 2011-07-05 2011-08-17 Amakem Nv Novel bisindolylmaleimides, pan-pkc inhibitors
CA2841111A1 (en) 2011-07-08 2013-01-17 Novartis Ag Novel pyrrolo pyrimidine derivatives
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
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
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
WO2013057711A1 (en) 2011-10-21 2013-04-25 Novartis Ag Quinazoline derivatives as pi3k modulators
US20140348848A1 (en) 2011-12-02 2014-11-27 Dhananjay Kaul Anti-il-1beta (interleukin-1beta) antibody-based prophylactic therapy to prevent complications leading to vaso-occlusion in sickle cell disease
PL2790705T3 (pl) 2011-12-15 2018-06-29 Novartis Ag Zastosowanie inhibitorów czynności lub funkcji PI3K
US20150148377A1 (en) 2011-12-22 2015-05-28 Novartis Ag Quinoline Derivatives
EA025322B1 (ru) 2011-12-22 2016-12-30 Новартис Аг Производные дигидробензооксазина и дигидропиридооксазина
EP2847191B1 (en) 2012-05-09 2016-06-15 Sanofi Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
JP2016500057A (ja) 2012-11-07 2016-01-07 ノバルティス アーゲー 置換インドール誘導体
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫－吡啶并－□衍生物之固體形式
EP2925366B1 (en) 2012-11-29 2018-02-21 Novartis AG Pharmaceutical combinations
CA2892927A1 (en) * 2012-12-10 2014-06-19 Centogene Ag Use of maleimide derivatives for preventing and treating leukemia
CA2892921A1 (en) 2012-12-10 2014-06-19 Centogene Ag Use of maleimide derivatives for preventing and treating cancer
WO2014128612A1 (en) 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
WO2014174478A1 (en) 2013-04-26 2014-10-30 Novartis Ag Pharmaceutical combinations of a pkc inhibitor and a c-met receptor tyrosine kinase inhibitor
US9657007B2 (en) 2013-09-22 2017-05-23 Calitor Sciences, Llc Substituted aminopyrimidine compounds and methods of use
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
EP3312164B1 (en) 2014-03-28 2020-12-09 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
BR112016024533A8 (pt) 2014-04-24 2021-03-30 Novartis Ag derivados de amino pirazina como inibidores de fosfatidilinositol 3-cinase ou sal, seu uso, e composição e combinação farmacêuticas
KR20160145780A (ko) 2014-04-24 2016-12-20 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피리딘 유도체
WO2015162461A1 (en) 2014-04-24 2015-10-29 Novartis Ag Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
US11104951B2 (en) 2014-05-22 2021-08-31 The Scripps Research Institute Molecular signatures for distinguishing liver transplant rejections or injuries
EP3146077A4 (en) 2014-05-22 2018-05-02 The Scripps Research Institute Tissue molecular signatures of kidney transplant rejections
US10443100B2 (en) 2014-05-22 2019-10-15 The Scripps Research Institute Gene expression profiles associated with sub-clinical kidney transplant rejection
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
RU2018108804A (ru) 2015-08-14 2019-09-16 Новартис Аг Фармацевтические комбинации и их применение
WO2017044434A1 (en) 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
EP3187495A1 (en) 2015-12-30 2017-07-05 Johannes Gutenberg-Universität Mainz 3-(5-fluoroindolyl)-4-arylmaleimide compounds and their use in tumor treatment
CA3013411A1 (en) 2016-02-03 2017-08-10 Galderma Research & Development Novel biaromatic propynyl compounds, pharmaceutical and cosmetic compositions containing same, and uses thereof
EP3600440A1 (en) 2017-03-20 2020-02-05 Sienna Biopharmaceuticals, Inc. Reduced exposure conjugates modulating therapeutic targets
WO2018175302A1 (en) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Polymer conjugates targeting c-src with reduced exposure
JP7254076B2 (ja) 2017-11-19 2023-04-07 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ヘテロアリール化合物及び使用方法
KR102737185B1 (ko) 2018-01-20 2024-12-05 선샤인 레이크 파르마 컴퍼니 리미티드 치환된 아미노피리미딘 화합물 및 이의 사용 방법
CN110551103B (zh) * 2018-05-30 2022-08-23 北京大学深圳研究生院 一种jak3选择性抑制剂
BR112021022682A2 (pt) 2019-05-14 2022-02-22 Provention Bio Inc Métodos e composições para prevenir diabetes do tipo 1
CA3137790A1 (en) 2019-05-23 2020-11-26 Novartis Ag Crystalline forms of a btk inhibitor
JP2023530109A (ja) 2020-06-11 2023-07-13 プロヴェンション・バイオ・インコーポレイテッド １型糖尿病を予防するための方法および組成物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7612609A (nl) 1975-11-12 1977-05-16 Schering Ag Werkwijze voor het bereiden van 1,3-geoxyge- neerde 8(alpha)-ostratienen.
IL89167A (en) * 1988-02-10 1994-02-27 Hoffmann La Roche Substituted pyrroles, their manufacture and pharmaceutical compositions containing them
FR2637591B1 (fr) 1988-10-11 1992-10-23 Synthelabo Derives de quinoleinone, leur preparation et leur application en therapeutique
DE4217964A1 (de) * 1992-05-30 1993-12-02 Goedecke Ag Indolocarbazol-Imide und deren Verwendung
EP1119548B1 (en) * 1998-10-08 2004-12-08 SmithKline Beecham plc 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1h-pyrrole-2,5-dione as glycogen synthase kinase-3 inhibitor (gsk-3)
GB9828640D0 (en) * 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
ATE284885T1 (de) * 2000-07-27 2005-01-15 Hoffmann La Roche 3-indolyl-4-phenyl-1h-pyrrol-2,5-dion derivate als glycogen synthase kinase 3beta inhibitoren

Also Published As

Publication number Publication date
JP4234426B2 (ja) 2009-03-04
KR20080014934A (ko) 2008-02-14
PT1337527E (pt) 2009-12-10
BR0115193A (pt) 2004-02-03
PL208794B1 (pl) 2011-06-30
SI1337527T1 (sl) 2010-02-26
ECSP104578A (es) 2010-04-30
NO20032034D0 (no) 2003-05-06
WO2002038561A8 (en) 2003-12-18
CN1253449C (zh) 2006-04-26
NZ535616A (en) 2006-03-31
NZ525656A (en) 2004-12-24
AU2005202387A1 (en) 2005-06-23
MXPA03004037A (es) 2003-08-19
CY1110564T1 (el) 2015-04-29
ATE445613T1 (de) 2009-10-15
IL155618A (en) 2007-07-04
SK287919B6 (sk) 2012-03-02
BRPI0115193B1 (pt) 2016-08-09
AU2002221810B2 (en) 2005-06-23
KR100748386B1 (ko) 2007-08-10
HU228999B1 (en) 2013-07-29
PL361409A1 (en) 2004-10-04
HUP0301651A3 (en) 2009-08-28
RU2329263C2 (ru) 2008-07-20
SK5462003A3 (en) 2003-11-04
NO327427B1 (no) 2009-06-29
HK1058789A1 (en) 2004-06-04
AU2005202387B2 (en) 2009-03-26
NO20032034L (no) 2003-07-04
DE60140201D1 (en) 2009-11-26
MY139979A (en) 2009-11-30
EP2070921A1 (en) 2009-06-17
HUP0301651A2 (en) 2008-10-28
IL182428A0 (en) 2007-07-24
MY127157A (en) 2006-11-30
EP1337527B1 (en) 2009-10-14
TWI290553B (en) 2007-12-01
CA2428133A1 (en) 2002-05-16
DK1337527T3 (da) 2010-01-04
AU2181002A (en) 2002-05-21
PE20020544A1 (es) 2002-07-30
CN1478087A (zh) 2004-02-25
CZ20031266A3 (enExample) 2003-07-16
EP1337527A1 (en) 2003-08-27
CZ307144B6 (cs) 2018-02-07
KR20060099542A (ko) 2006-09-19
IL155618A0 (en) 2003-11-23
KR20030042036A (ko) 2003-05-27
TW200738687A (en) 2007-10-16
JP2004513168A (ja) 2004-04-30
WO2002038561A1 (en) 2002-05-16
ES2332770T3 (es) 2010-02-12
KR100916613B1 (ko) 2009-09-14
SG159378A1 (en) 2010-03-30
AR035211A1 (es) 2004-05-05
RU2008105345A (ru) 2009-08-20

Similar Documents

Publication Publication Date Title
CA2428133C (en) Indolylmaleimide derivatives as protein kinase c inhibitors
US7825124B2 (en) Indolylmaleimide derivatives
AU2002221810A1 (en) Indolylmaleimide derivatives as protein kinase C inhibitors
US8426440B2 (en) Indolymaleimide derivatives
CA2513613A1 (en) Indolylmaleimide derivatives
HK1131620A (en) Indolylmaleimide derivatives as protein kinase c inhibitors
HK1058789B (en) Indolylmaleimide derivatives as protein kinase c inhibitors

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20181105