[go: up one dir, main page]

PE20020544A1 - Derivados de indolilmaleimida - Google Patents

Derivados de indolilmaleimida

Info

Publication number
PE20020544A1
PE20020544A1 PE2001001093A PE2001001093A PE20020544A1 PE 20020544 A1 PE20020544 A1 PE 20020544A1 PE 2001001093 A PE2001001093 A PE 2001001093A PE 2001001093 A PE2001001093 A PE 2001001093A PE 20020544 A1 PE20020544 A1 PE 20020544A1
Authority
PE
Peru
Prior art keywords
alkyl
refers
residue
pirrol
diona
Prior art date
Application number
PE2001001093A
Other languages
English (en)
Inventor
Rainer Albert
Nigel Graham Cooke
Sylvain Cottens
Claus Ehrhardt
Gerhard Zenke
Richard Sedrani
Matt Peter Von
Jurgen Wagner
Jean-Pierre Evenou
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 PE20020544A1 publication Critical patent/PE20020544A1/es

Links

Classifications

    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • 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
    • C07D403/02Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

SE REFIERE A DERIVADOS DE INDOLILMALEIMIDA DE FORMULA I; Ra ES H, ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO CON OH, NH2, NH-ALQUILO C1-C4, N-(ALQUILO C1-C4)2; Rb ES H, ALQUILO C1-C4; R ES UN GRUPO a, b, c, d, e, f; UNO DE R1, R4, R7, R8, R11, R14 ES OH, SH, UN RESIDUO HETEROCICLO, NR161R7; R16 Y R17 ES H, ALQUILO C1-C4 O JUNTO A N FORMAN UN RESIDUO HETEROCICLICO, X-Rc-Y; X ES UN ENLACE, O, S, NR18; R18 ES H, ALQUILO C1-C4; Rc ES ALQUILENO C1-C4 OPCIONALMENTE UN CH2 ES REEEMPLAZADO POR CRxRy; UNO DE Rx Y Ry ES H Y EL OTRO ES CH3 O FORMAN JUNTOS CH2-CH2; Y ES OH, UN RESIDUO HETEROCICLICO, NR19R20; R19 Y R20 SON H, CICLOALQUILO C3-C6, ARILALQUILO C1-C4, ENTRE OTROS; R2, R3, R4, R5, R6, R9, R10, R12, R13, R15, R15' ES H, HALOGENO, ALQUILO C1-C4, CF3, OH, SH, NH2, ALCOXILO C1-C4 TIOALQUILO C1-C4, NH-ALQUILO C1-C4; E ES N=, G ES CH=; E ES CH=, G ES N=. SON COMPUESTOS PREFERIDOS 3-(1H-INDOL-3-IL)-4-[2-(4-METIL-PIPERAZIN-1-IL)QUINAZOLIN-4-IL]PIRROL-2,5-DIONA; 3-(1H-1-METIL-INDOL-3-IL)-4-[2-(4,7-DIAZA-ESPIRO[2,5-OCT-7-IL)-QUINAZOLIN-4-IL]-PIRROL-2,5-DIONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. TAMBIEN SE REFIERE A UNA COMBINACION QUE COMPRENDE UN INHIBIDOR DE PKC, ACTIVAVION O PROLIFERACION DE CELULAS T; AGENTE INMUNOSUPRESOR, INMUNOMODULADOR, ANTIINFLAMATORIO, ANTIPROLIFERATIVO, ANTIDIABETICO
PE2001001093A 2000-11-07 2001-11-05 Derivados de indolilmaleimida PE20020544A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24640000P 2000-11-07 2000-11-07
US28370501P 2001-04-13 2001-04-13

Publications (1)

Publication Number Publication Date
PE20020544A1 true PE20020544A1 (es) 2002-07-30

Family

ID=26937956

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001001093A PE20020544A1 (es) 2000-11-07 2001-11-05 Derivados de indolilmaleimida

Country Status (30)

Country Link
EP (2) EP2070921A1 (es)
JP (1) JP4234426B2 (es)
KR (3) KR20080014934A (es)
CN (1) CN1253449C (es)
AR (1) AR035211A1 (es)
AT (1) ATE445613T1 (es)
AU (3) AU2002221810B2 (es)
BR (1) BRPI0115193B1 (es)
CA (1) CA2428133C (es)
CY (1) CY1110564T1 (es)
CZ (1) CZ307144B6 (es)
DE (1) DE60140201D1 (es)
DK (1) DK1337527T3 (es)
EC (1) ECSP104578A (es)
ES (1) ES2332770T3 (es)
HU (1) HU228999B1 (es)
IL (3) IL155618A0 (es)
MX (1) MXPA03004037A (es)
MY (2) MY139979A (es)
NO (1) NO327427B1 (es)
NZ (2) NZ535616A (es)
PE (1) PE20020544A1 (es)
PL (1) PL208794B1 (es)
PT (1) PT1337527E (es)
RU (2) RU2329263C2 (es)
SG (1) SG159378A1 (es)
SI (1) SI1337527T1 (es)
SK (1) SK287919B6 (es)
TW (2) TW200738687A (es)
WO (1) WO2002038561A1 (es)

Families Citing this family (84)

* 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
ES2312785T3 (es) 2002-06-05 2009-03-01 Janssen Pharmaceutica Nv Pirrolinas sustituidas utiles como inhibidores de quinasa.
RU2004135382A (ru) 2002-06-05 2005-06-27 Янссен Фармацевтика Н.В. (Be) Замещенные пирролины в качестве ингибиторов киназы
GB0303319D0 (en) 2003-02-13 2003-03-19 Novartis Ag Organic compounds
WO2005025602A1 (en) * 2003-09-16 2005-03-24 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
WO2005046698A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
WO2005068455A1 (en) 2004-01-19 2005-07-28 Novartis Ag Indolylmaleimde derivatives as pkc inhibitors
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
EP1819697B1 (en) 2004-12-08 2012-08-01 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
MX2008000463A (es) 2005-07-11 2008-03-11 Novartis Ag Derivados de indolil-maleimida.
DK2848258T3 (en) 2005-10-26 2018-03-19 Novartis Ag Treatment of familial Mediterranean fever with anti-IL-1beta antibodies
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
US20100179175A1 (en) * 2006-08-23 2010-07-15 Sivak Jeremy M Use of pkc inhibitors in ocular diseases
CN101522664B (zh) * 2006-10-20 2013-06-12 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
JP2010512335A (ja) * 2006-12-07 2010-04-22 ノバルティス アーゲー 移植におけるpkc阻害剤の使用
ES2410955T3 (es) * 2006-12-19 2013-07-04 Novartis Ag Derivados de indolilmaleimida como inhibidores de la quinasa
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
US8282922B2 (en) 2007-05-29 2012-10-09 Novartis Ag Method of treating an auto-inflammatory syndrome with a human IL-1β binding antibody
US8076160B2 (en) 2007-09-27 2011-12-13 Novartis Ag Drug monitoring assay
EP2209916B1 (en) 2007-11-08 2011-12-21 Novartis AG Gene expression signatures for chronic/sclerosing allograft nephropathy
CA2707554C (en) 2007-12-05 2015-06-30 Gerd Dannhardt 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
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
KR101461767B1 (ko) * 2010-03-30 2014-11-13 노파르티스 아게 만성 활성 b-세포-수용체 신호전달이 있는 b-세포 림프종의 치료를 위한 pkc 억제제
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
SG195067A1 (en) 2011-06-27 2013-12-30 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives
GB201111427D0 (en) * 2011-07-05 2011-08-17 Amakem Nv Novel bisindolylmaleimides, pan-pkc inhibitors
KR20140058543A (ko) 2011-07-08 2014-05-14 노파르티스 아게 신규 피롤로 피리미딘 유도체
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
US8846712B2 (en) 2011-09-12 2014-09-30 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP2014530851A (ja) 2011-10-21 2014-11-20 ノバルティスアーゲー Pi3kモジュレータとしてのキナゾリン誘導体
WO2013082282A1 (en) 2011-12-02 2013-06-06 lNOVARTIS AG Anti-il-1beta (interleukin-1beta) antibody-based prophylactic therapy to prevent complications leading to vaso-occlusion in sickle cell disease.
ES2661510T3 (es) 2011-12-15 2018-04-02 Novartis Ag Uso de inhibidores de la actividad o función de PI3K
LT2794600T (lt) 2011-12-22 2018-02-26 Novartis Ag 2,3-dihidro-benzo[1,4]oksazino dariniai ir giminingi junginiai kaip fosfoinozitido-3 kinazės (pi3k) inhibitoriai, skirti gydymui, pavyzdžiui, reumatoidinio artrito
WO2013093850A1 (en) 2011-12-22 2013-06-27 Novartis Ag Quinoline derivatives
WO2013167403A1 (en) 2012-05-09 2013-11-14 Sanofi Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
EP2917205A1 (en) 2012-11-07 2015-09-16 Novartis AG Substituted indole derivatives
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫-吡啶并-□衍生物之固體形式
ES2669248T3 (es) 2012-11-29 2018-05-24 Novartis Ag Combinaciones farmacéuticas
ES2851208T3 (es) * 2012-12-10 2021-09-03 Centogene Gmbh Uso de derivados de maleimida para prevenir y tratar el cáncer
CA2892927A1 (en) 2012-12-10 2014-06-19 Centogene Ag Use of maleimide derivatives for preventing and treating leukemia
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
AU2014321419B2 (en) 2013-09-22 2017-06-15 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
EP3122729A4 (en) 2014-03-28 2017-11-15 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
ES2667424T3 (es) 2014-04-24 2018-05-10 Novartis Ag Derivados de pirazina como inhibidores de fosfatidil-inositol-3-quinasa
CN106458980A (zh) 2014-04-24 2017-02-22 诺华股份有限公司 作为磷脂酰肌醇3‑激酶抑制剂的氨基吡啶衍生物
MX2016013812A (es) 2014-04-24 2017-03-09 Novartis Ag Derivados de amino-pirazina como inhibidores de fosfatidil-inositol-3-cinasa.
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
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
EP3187495A1 (en) 2015-12-30 2017-07-05 Johannes Gutenberg-Universität Mainz 3-(5-fluoroindolyl)-4-arylmaleimide compounds and their use in tumor treatment
CN109414384A (zh) 2016-02-03 2019-03-01 高德美研究及发展公司 新的双芳香基丙炔基化合物,包含该化合物的药物和化妆品组合物及其用途
WO2018175302A1 (en) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Polymer conjugates targeting c-src with reduced exposure
EP3600440A1 (en) 2017-03-20 2020-02-05 Sienna Biopharmaceuticals, Inc. Reduced exposure conjugates modulating therapeutic targets
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
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
KR20220012280A (ko) 2019-05-23 2022-02-03 노파르티스 아게 Btk 저해제의 결정질 형태
US12006366B2 (en) 2020-06-11 2024-06-11 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4066674A (en) 1975-11-12 1978-01-03 Schering Aktiengesellschaft Process for the preparation of 1,3-oxygenated 8α-estratrienes and novel intermediates obtained therefrom
NZ227850A (en) * 1988-02-10 1991-11-26 Hoffmann La Roche Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders
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
ATE284387T1 (de) * 1998-10-08 2004-12-15 Smithkline Beecham Plc 3-(3-chloro-4-hydroxyphenylamino)-4-(2- nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3)
GB9828640D0 (en) * 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
CZ2003555A3 (en) * 2000-07-27 2004-03-17 F. Hoffmann-La Roche Ag 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3beta

Also Published As

Publication number Publication date
HK1058789A1 (en) 2004-06-04
BRPI0115193B1 (pt) 2016-08-09
WO2002038561A1 (en) 2002-05-16
JP4234426B2 (ja) 2009-03-04
DK1337527T3 (da) 2010-01-04
SK287919B6 (sk) 2012-03-02
NO20032034D0 (no) 2003-05-06
TWI290553B (en) 2007-12-01
JP2004513168A (ja) 2004-04-30
HUP0301651A2 (en) 2008-10-28
IL182428A0 (en) 2007-07-24
CN1253449C (zh) 2006-04-26
CN1478087A (zh) 2004-02-25
IL155618A0 (en) 2003-11-23
CY1110564T1 (el) 2015-04-29
CA2428133C (en) 2009-12-29
SG159378A1 (en) 2010-03-30
DE60140201D1 (en) 2009-11-26
KR20060099542A (ko) 2006-09-19
TW200738687A (en) 2007-10-16
MY127157A (en) 2006-11-30
CZ307144B6 (cs) 2018-02-07
BR0115193A (pt) 2004-02-03
AU2005202387A1 (en) 2005-06-23
EP2070921A1 (en) 2009-06-17
IL155618A (en) 2007-07-04
HUP0301651A3 (en) 2009-08-28
HU228999B1 (en) 2013-07-29
AR035211A1 (es) 2004-05-05
RU2008105345A (ru) 2009-08-20
RU2329263C2 (ru) 2008-07-20
NZ525656A (en) 2004-12-24
WO2002038561A8 (en) 2003-12-18
AU2002221810B2 (en) 2005-06-23
AU2005202387B2 (en) 2009-03-26
ATE445613T1 (de) 2009-10-15
MXPA03004037A (es) 2003-08-19
PL361409A1 (en) 2004-10-04
PT1337527E (pt) 2009-12-10
EP1337527B1 (en) 2009-10-14
SI1337527T1 (sl) 2010-02-26
KR100748386B1 (ko) 2007-08-10
SK5462003A3 (en) 2003-11-04
EP1337527A1 (en) 2003-08-27
NO327427B1 (no) 2009-06-29
NO20032034L (no) 2003-07-04
AU2181002A (en) 2002-05-21
CA2428133A1 (en) 2002-05-16
PL208794B1 (pl) 2011-06-30
KR20030042036A (ko) 2003-05-27
NZ535616A (en) 2006-03-31
KR100916613B1 (ko) 2009-09-14
KR20080014934A (ko) 2008-02-14
ECSP104578A (es) 2010-04-30
CZ20031266A3 (es) 2003-07-16
MY139979A (en) 2009-11-30
ES2332770T3 (es) 2010-02-12

Similar Documents

Publication Publication Date Title
PE20020544A1 (es) Derivados de indolilmaleimida
PE20020131A1 (es) Derivados de pirazol
PE20010543A1 (es) Derivados de purina como inhibidores de tirosincinasa syk
PE20030137A1 (es) Derivados antimicrobianos de quinolona
PE20021056A1 (es) Derivados de pirazol
PE20010741A1 (es) Derivados de piperazina como antagonistas de taquicininas
HRP20070430T3 (en) (3-oxo-3,4-dihydro-quinoxalin-2-yl-amino)-benzamide derivatives and related compounds as glycogen phosphorylase inhibitors for the treatment of diabetes and obesity
PE20050874A1 (es) Compuestos de bencimidazolona que tienen actividad agonista del receptor 5-ht4
PE20020589A1 (es) 5-espiropirimidin-2,4,6-triona como inhibidores de metaloproteinasas
PE20001093A1 (es) 3-amino-4-aril-maleimidas como inhibidores de gsk-3
PE20011089A1 (es) Tioamidas de oxazolidinona con sustituyentes de piperazin-amida
PE20050132A1 (es) Piperazinas heterociclicas sustituidas
AR057107A2 (es) Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentos
AR032466A1 (es) Ciclilamina sulfonamidas, utilizacion de las mismas para la manufactura de un medicamento y composiciones farmaceuticas utiles como agonistas de los receptores beta-3 adrenergicos
FR2673427B1 (fr) Derives heterocycliques diazotes n-substitues par un groupement biphenylmethyle, leur preparation, les compositions pharmaceutiques en contenant.
AR018915A1 (es) Inhibidores de proteasas diacilhidrazinicos, composicion farmaceutica que la comprenden, usos de los mismos para la manufactura de un medicamento, unprocedimiento de fabricacion de dichos compuestos
AR041246A1 (es) Derivados de piridina; un procedimiento de preparacion de los mismos y composicion farmaceutica que los contiene
PE20050587A1 (es) Derivados de diazindol-dicarbonilo-piperazinilo como agentes antivirales
PE20040757A1 (es) Derivados de benzoxazina
PE20021018A1 (es) DERIVADOS DE ß - CARBOLINA
PE20080311A1 (es) Derivados de oxadiazol como agentes afines a receptores nicotinicos
MX9306310A (es) Compuestos antagonistas del receptor de 5-ht4, procedimiento para su preparacion y composiciones farmaceuticas que los contienen
PE20020444A1 (es) Antagonistas de receptores de taquiquinina zwitterionica
PE51499A1 (es) Derivados de 5-aroilnaftaleno
NO961797L (no) Anvendelse av benzopyranderivater for fremstilling av farmasöytiske sammensetninger beregnet for behandling av patologier forbundet med den Na+-uavhengige C1-HCO3-utbytter

Legal Events

Date Code Title Description
FC Refusal