AR039209A1 - Derivados de indolilmaleimida - Google Patents

Derivados de indolilmaleimida

Info

Publication number
AR039209A1
AR039209A1 ARP030101128A ARP030101128A AR039209A1 AR 039209 A1 AR039209 A1 AR 039209A1 AR P030101128 A ARP030101128 A AR P030101128A AR P030101128 A ARP030101128 A AR P030101128A AR 039209 A1 AR039209 A1 AR 039209A1
Authority
AR
Argentina
Prior art keywords
piperazin
methyl
formula
radical
diaza
Prior art date
Application number
ARP030101128A
Other languages
English (en)
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=28676503&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR039209(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0207729A external-priority patent/GB0207729D0/en
Priority claimed from GB0303323A external-priority patent/GB0303323D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR039209A1 publication Critical patent/AR039209A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • 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
    • 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
    • A61P27/14Decongestants or antiallergics
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/06Immunosuppressants, 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • 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

Landscapes

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

Abstract

Se proporcionan compuestos de indolilmaleimida, proceso para prepararlos, composición farmacéutica. etil como fármaco inmunosupresor, inmunomodulador, antiinflamatorio, antiproliferativo o antidiabético, enfermedades mediadas por linfocitos T y/o PKC o GSK-3b. Reivindicación 1: Un compuesto de la fórmula (1) en donde Ra es H, CH3, CH2-CH3, o isopropilo, Rb es H, halógeno, alcoxilo C1-6, o alquilo C1-6, y cualquiera de I) R es un radical de la fórmula (2) en donde: R1 es piperazín-1-ilo opcionalmente sustituido por CH3 en la posición 3 o 4; o 4,7-diaza-espiro[2.5]oct-7-ilo; R2 es Cl, Br, CF3, o CH3; y R3 es H, CH3, o CF3, siendo R2 diferente de CH3 o de Cl cuando R3 es H, Ra es H o CH3, Rb es H, y R1 es 4-metil-1-piperazinilo; o (II) R es un radical de la fórmula (3) en donde R4 es piperazín-1-ilo sustituido en las posiciones 3 y/o 4 por CH3; o 4,7-diaza-espiro[2.5]oct-7-ilo; siendo Ra diferente de H o CH3 cuando R4 es 4-metil-1-piperazinilo; o (III) R es un radical de la fórmula (4) en donde: R14 es piperazín -1-ilo opcionalmente sustituido por CH3 en la posición 3 y/o 4, o en la posición 3 por etilo, fenilalquilo C1-4, alcoxilo (C1-4)-alquilo (C1-4), o haloalquilo C1-4; o 4,7-diaza-espiro[2.5]oct-7-ilo; R15 es halógeno; CF3, o CH3, siendo R15 diferente de CH3 cuando R16 es CH3, Ra es H o CH3, Rb es H , R14 es 4-metil-1-piperazinilo; y R16 es H, CH3; o CF3; siendo R16 diferente de H cuando R15 es Cl, Ra es H o CH3, Rb es H y R14 es 4-metil-1-piperazinilo; o (IV) R es un radical de la fórmula (5) en donde R8 es piperazin-1-ilo, 3-metil-piperazin-1-ilo, o 4-bencil-piperazin-1-ilo; o (V) R es un radical de la fórmula (6) en donde R9 es 4,7-diaza-espiro[2.5]oct-7-ilo; o piperazin-1-ilo sustituido en la posición 3 por metilo o etilo, y opcionalmente en la posición 4 por metilo, o una sal del mismo.
ARP030101128A 2002-04-03 2003-04-01 Derivados de indolilmaleimida AR039209A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0207729A GB0207729D0 (en) 2002-04-03 2002-04-03 Organic compounds
GB0303323A GB0303323D0 (en) 2003-02-13 2003-02-13 Organic compounds

Publications (1)

Publication Number Publication Date
AR039209A1 true AR039209A1 (es) 2005-02-09

Family

ID=28676503

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101128A AR039209A1 (es) 2002-04-03 2003-04-01 Derivados de indolilmaleimida

Country Status (26)

Country Link
US (5) US20050119274A1 (es)
EP (1) EP1490355B1 (es)
JP (1) JP4247125B2 (es)
KR (2) KR100942329B1 (es)
CN (1) CN100351251C (es)
AR (1) AR039209A1 (es)
AT (1) ATE517888T1 (es)
AU (1) AU2003224031B2 (es)
BR (1) BR0308979A (es)
CA (1) CA2477774C (es)
CO (1) CO5611127A2 (es)
CY (1) CY1111982T1 (es)
DK (1) DK1490355T3 (es)
EC (2) ECSP045254A (es)
IL (1) IL163892A0 (es)
MX (1) MXPA04009632A (es)
MY (1) MY137566A (es)
NO (1) NO329166B1 (es)
NZ (1) NZ535613A (es)
PE (1) PE20040079A1 (es)
PL (1) PL213480B1 (es)
PT (1) PT1490355E (es)
RU (1) RU2340610C2 (es)
SI (1) SI1490355T1 (es)
TW (2) TWI324064B (es)
WO (1) WO2003082859A1 (es)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6645970B2 (en) * 2000-11-07 2003-11-11 Novartis Ag Indolylmaleimide derivatives
TWI324064B (en) * 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
GB0303319D0 (en) * 2003-02-13 2003-03-19 Novartis Ag Organic compounds
EP1682103A1 (en) * 2003-10-27 2006-07-26 Novartis AG Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation
US7582631B2 (en) 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
CA2552738A1 (en) * 2004-01-19 2005-07-28 Novartis Ag Indolylmaleimide derivatives
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
GB0504203D0 (en) * 2005-03-01 2005-04-06 Novartis Ag Organic compounds
JP4747364B2 (ja) * 2005-04-04 2011-08-17 独立行政法人産業技術総合研究所 紫外線皮膚炎抑止剤およびアトピー性皮膚炎抑止剤
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
CA2611607A1 (en) * 2005-07-11 2007-01-18 Novartis Ag Indolylmaleimide derivatives
EP1749523A1 (en) * 2005-07-29 2007-02-07 Neuropharma, S.A. GSK-3 inhibitors
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス,インコーポレイティド ムスカリン性受容体調節による神経発生
RS52110B2 (sr) 2005-09-14 2018-05-31 Takeda Pharmaceuticals Co Inhibitori dipeptidil peptidaze za lečenje dijabetesa
CN101360723A (zh) 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス,インコーポレイティド Pde阻害による神経新生の調節
TR201802449T4 (tr) 2005-10-26 2018-03-21 Novartis Ag Ailesel akdeniz hummasının anti ıl-1beta antikorları ile tedavisi.
EP1942879A1 (en) 2005-10-31 2008-07-16 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
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
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
GB0605691D0 (en) * 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
GB0613162D0 (en) * 2006-06-30 2006-08-09 Novartis Ag Organic compounds
BRPI0716615A2 (pt) * 2006-08-23 2013-10-08 Novartis Ag Uso de inibidores de pkc em doenças oculares
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008073770A1 (en) * 2006-12-07 2008-06-19 Novartis Ag Use of pkc inhibitors in transplantation
ES2410955T3 (es) 2006-12-19 2013-07-04 Novartis Ag Derivados de indolilmaleimida como inhibidores de la quinasa
JP5291093B2 (ja) * 2007-05-16 2013-09-18 ザ ブリガム アンド ウィメンズ ホスピタル インコーポレイテッド シヌクレイノパチーの治療
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
US7943163B2 (en) 2007-08-22 2011-05-17 Response Scientific, Inc. Medical food or nutritional supplement, method of manufacturing same, and method of managing diabetes
US20090054513A1 (en) * 2007-08-22 2009-02-26 Response Scientific, Inc. Method of managing blood glucose levels, insulin levels and/or insulin receptor functionality in individuals with diabetes, polycystic ovarian syndrome and/or alzheimer's disease
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
AR069799A1 (es) * 2007-12-21 2010-02-17 Novartis Ag Composicion farmaceutica
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
ES2331451B1 (es) * 2008-06-30 2010-10-21 Consejo Superior De Investigaciones Cientificas (Csic) Inmunosupresor basado en la interrupcion de la interaccion tcr-nck.
US8475790B2 (en) 2008-10-06 2013-07-02 Bristol-Myers Squibb Company Combination of CD137 antibody and CTLA-4 antibody for the treatment of proliferative diseases
DE202008014557U1 (de) 2008-10-27 2009-03-12 Eberhard-Karls-Universität Tübingen Universitätsklinikum Therapeutische Verwendung
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN101671329B (zh) * 2009-06-17 2012-11-07 东华大学 3-氨基醇取代的吲哚马来酰亚胺化合物、其制备和应用
US9752191B2 (en) 2009-07-09 2017-09-05 The Scripps Research Institute Gene expression profiles associated with chronic allograft nephropathy
TW201119651A (en) * 2009-10-26 2011-06-16 Lg Life Sciences Ltd Pharmaceutical composition comprising indole compound
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
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
BR112013004266A8 (pt) 2010-08-23 2018-01-02 Univ Texas anticorpos anti-ox40 e métodos de uso dos mesmos.
CZ305457B6 (cs) * 2011-02-28 2015-09-30 Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití
UY34072A (es) * 2011-05-17 2013-01-03 Novartis Ag Derivados sustituidos de indol
CN103608349A (zh) 2011-06-27 2014-02-26 诺瓦提斯公司 四氢-吡啶并-嘧啶衍生物的固体形式和盐
MX2014000338A (es) 2011-07-08 2014-05-01 Novartis Ag Derivados de pirrolo-pirimidina novedoso.
WO2013057711A1 (en) 2011-10-21 2013-04-25 Novartis Ag Quinazoline derivatives as pi3k modulators
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.
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
WO2013093850A1 (en) 2011-12-22 2013-06-27 Novartis Ag Quinoline derivatives
JO3398B1 (ar) 2011-12-22 2019-10-20 Novartis Ag مشتقات 2،3- ثانى هيدرو- بنزو[1,4] أوكسازين والمركبات المتعلقة بها كمثبطات كيناز فسفواينوسيتيد-3 (pi3k) لمعالجة على سبيل المثال التهاب المفاصل الروماتيدي
EA201590886A1 (ru) 2012-11-07 2015-08-31 Новартис Аг Замещенные производные индола
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫-吡啶并-□衍生物之固體形式
US9446043B2 (en) 2012-11-29 2016-09-20 Novartis Ag Pharmaceutical combinations
CA2899206C (en) 2013-01-24 2019-07-09 Transderm, Inc. Compositions for transdermal delivery of mtor inhibitors
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
WO2015179773A1 (en) 2014-05-22 2015-11-26 The Scripps Research Institute Tissue molecular signatures of kidney transplant rejections
SG11201600028YA (en) 2013-09-22 2016-02-26 Calitor Sciences Llc Substituted aminopyrimidine compounds and methods of use
KR101630806B1 (ko) 2013-11-14 2016-06-16 대한민국 돼지의 초위성체 마커를 이용한 개체식별 방법
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
EP3327006B1 (en) 2014-03-28 2020-05-20 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
EA032075B1 (ru) 2014-04-24 2019-04-30 Новартис Аг Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы
BR112016024484A2 (pt) 2014-04-24 2017-08-15 Novartis Ag derivados de aminopiridina como inibidores de fosfatidilinositol 3-quinase
EP3134395B1 (en) 2014-04-24 2018-01-31 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
US10443100B2 (en) 2014-05-22 2019-10-15 The Scripps Research Institute Gene expression profiles associated with sub-clinical kidney transplant rejection
WO2016003450A1 (en) 2014-07-01 2016-01-07 The Regents Of The University Of California Pkc-epsilon inhibitors
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
TWI820377B (zh) 2015-05-07 2023-11-01 美商艾吉納斯公司 抗ox40抗體及其使用方法
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
MX2018006477A (es) 2015-12-02 2018-09-03 Agenus Inc Anticuerpos y metodos de uso de estos.
CA3041340A1 (en) 2016-11-09 2018-05-17 Agenus Inc. Anti-ox40 antibodies, anti-gitr antibodies, and methods of use thereof
WO2018129364A1 (en) 2017-01-06 2018-07-12 Palvella Therapeutics Llc Anhydrous compositions of mtor inhibitors and methods of use
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
JP2021530463A (ja) 2018-07-02 2021-11-11 パルヴェラ セラピューティクス、インク. mTOR阻害剤の無水組成物および使用方法
WO2020234779A1 (en) 2019-05-23 2020-11-26 Novartis Ag Crystalline forms of a btk inhibitor

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL89167A (en) * 1988-02-10 1994-02-27 Hoffmann La Roche Substituted pyrroles, their manufacture and pharmaceutical compositions containing them
ID27510A (id) * 1998-07-30 2001-04-12 Japan Tobacco Inc Senyawa malimida tersubstitusi dan penggunaan farmasinya
US6281356B1 (en) * 1999-12-22 2001-08-28 Hoffmann-La Roche Inc. Substituted pyrroles
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
MXPA03004037A (es) * 2000-11-07 2003-08-19 Novartis Ag Derivados de indolilmaleimida como inhibidores de proteina de cinasa c.
US6645970B2 (en) * 2000-11-07 2003-11-11 Novartis Ag Indolylmaleimide derivatives
TWI324064B (en) * 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
EP1682103A1 (en) * 2003-10-27 2006-07-26 Novartis AG Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation

Also Published As

Publication number Publication date
AU2003224031B2 (en) 2007-06-28
US7534808B2 (en) 2009-05-19
ATE517888T1 (de) 2011-08-15
US20080108628A1 (en) 2008-05-08
CA2477774C (en) 2011-03-15
PL213480B1 (pl) 2013-03-29
WO2003082859A1 (en) 2003-10-09
ECSP085254A (es) 2009-01-30
MY137566A (en) 2009-02-27
US7235555B2 (en) 2007-06-26
CN1639153A (zh) 2005-07-13
PE20040079A1 (es) 2004-04-19
EP1490355B1 (en) 2011-07-27
NO329166B1 (no) 2010-09-06
JP4247125B2 (ja) 2009-04-02
ECSP045254A (es) 2004-09-28
TWI324064B (en) 2010-05-01
KR100886521B1 (ko) 2009-03-02
KR100942329B1 (ko) 2010-02-12
NZ535613A (en) 2007-07-27
US20050119274A1 (en) 2005-06-02
CN100351251C (zh) 2007-11-28
JP2005527563A (ja) 2005-09-15
IL163892A0 (en) 2005-12-18
US20070037826A1 (en) 2007-02-15
KR20040094901A (ko) 2004-11-10
TW200918046A (en) 2009-05-01
BR0308979A (pt) 2005-01-04
US7358253B2 (en) 2008-04-15
CY1111982T1 (el) 2015-11-04
PT1490355E (pt) 2011-11-03
RU2340610C2 (ru) 2008-12-10
KR20070043900A (ko) 2007-04-25
EP1490355A1 (en) 2004-12-29
TW200306818A (en) 2003-12-01
MXPA04009632A (es) 2005-01-11
PL371322A1 (en) 2005-06-13
DK1490355T3 (da) 2011-11-21
US20070032507A1 (en) 2007-02-08
CO5611127A2 (es) 2006-02-28
US20080146578A1 (en) 2008-06-19
RU2004132203A (ru) 2005-07-10
NO20044613L (no) 2004-10-26
SI1490355T1 (sl) 2011-11-30
AU2003224031A1 (en) 2003-10-13
CA2477774A1 (en) 2003-10-09

Similar Documents

Publication Publication Date Title
AR039209A1 (es) Derivados de indolilmaleimida
RU2336275C2 (ru) Пиримидопроизводные, характеризующиеся антипролиферативной активностью, и фармацевтическая композиция
Piętka-Ottlik et al. New organoselenium compounds active against pathogenic bacteria, fungi and viruses
PE20070839A1 (es) Derivados de indolobenzazepina como inhibidores de ns5b de vhc
DE602005013248D1 (de) Amidderivate von 3-phenyldihydropyrimidoä4,5-düpyrimidinonen, deren herstellung und verwendung als pharmazeutische mittel
KR20050113198A (ko) 디하이드로프테리디논, 이의 제조 방법 및 약제로서의 이의용도
JP2006501181A5 (es)
ATE288443T1 (de) Neue pyrazin-derivate oder salze davon, pharmazeutische zusammensetzungen, die die derivate oder deren salze enthalten und intermediate zu beider herstellung
RU2009138471A (ru) Новое адениновое соединение
AR068413A2 (es) Derivados 8-amino, metodos de preparacion, composiciones farmaceuticas y su uso en terapia
NO20052683L (no) Nye pyridopyrimidinonforbindelser, fremgangsmate for deres fremstilling og farmasoytiske sammensetninger inneholdende dem
JP2006521359A5 (es)
AR047339A1 (es) Derivados de difenilazetidona.proceso de obtencion.
AU2006343832A1 (en) New benzothiazinone derivatives and their use as antibacterial agents
DE602004012758D1 (de) Chinoxalinderivate als inhibitoren der neutrophilelastase und deren verwendung
CA2382129A1 (en) Novel derivatives of flavones, xanthones and coumarins
AU2005266493A1 (en) Inhibitors of Hsp90
KR920019746A (ko) 신규한 시클로헥실벤즈아미드 유도체, 그의 제조방법 및 약제로서의 용도
KR960034205A (ko) 피페리딘 유도체와 그것의 제조방법 및 치료적 이용
ATE276257T1 (de) Pyrazinonderivate
FI82687C (fi) Foerfarande foer framstaellning av nya terapeutiskt anvaendbara pyridinkarboxylsyraestrar och deras anvaendning som laekemedel.
ES2129483T3 (es) Derivados de indol-7-carboxamida como analgesicos.
WO1993016698A1 (en) SUBSTITUTED FURO[3',4':6,7]INDOLIZINO[1,2-b]QUINOLINONES
Cutrı̀ et al. Synthesis of new 3, 4, 5-trisubstituted isothiazoles as effective inhibitory agents of enteroviruses
KR940019705A (ko) 2- [4 -(4 - 아졸릴 부틸)-1- 피페라지닐]-5- 히드록시- 피라미딘 유도체, 이들의 제조 및 의약제품으로서 이들의 이용

Legal Events

Date Code Title Description
FG Grant, registration