EA023238B1 - Замещенные производные индола для лечения иммунологических расстройств - Google Patents

Замещенные производные индола для лечения иммунологических расстройств Download PDF

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Publication number
EA023238B1
EA023238B1 EA201391710A EA201391710A EA023238B1 EA 023238 B1 EA023238 B1 EA 023238B1 EA 201391710 A EA201391710 A EA 201391710A EA 201391710 A EA201391710 A EA 201391710A EA 023238 B1 EA023238 B1 EA 023238B1
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EA
Eurasian Patent Office
Prior art keywords
formula
alkyl
compound
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
EA201391710A
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English (en)
Russian (ru)
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EA201391710A1 (ru
Inventor
Найджел Грэхэм Кук
Рита Рамос
Карен Каммертэн
Морис Ван Эйс
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201391710A1 publication Critical patent/EA201391710A1/ru
Publication of EA023238B1 publication Critical patent/EA023238B1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/499—Spiro-condensed pyrazines or piperazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • AIDS & HIV (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
EA201391710A 2011-05-17 2012-05-16 Замещенные производные индола для лечения иммунологических расстройств EA023238B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161486808P 2011-05-17 2011-05-17
PCT/IB2012/052473 WO2012156936A1 (en) 2011-05-17 2012-05-16 Substituted indole derivatives for the treatment of immunological disorders

Publications (2)

Publication Number Publication Date
EA201391710A1 EA201391710A1 (ru) 2014-03-31
EA023238B1 true EA023238B1 (ru) 2016-05-31

Family

ID=46210333

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391710A EA023238B1 (ru) 2011-05-17 2012-05-16 Замещенные производные индола для лечения иммунологических расстройств

Country Status (15)

Country Link
US (2) US8703782B2 (enExample)
EP (1) EP2709998B1 (enExample)
JP (1) JP6043344B2 (enExample)
KR (1) KR20140023354A (enExample)
CN (1) CN103534250B (enExample)
AR (1) AR088414A1 (enExample)
AU (1) AU2012257345B2 (enExample)
BR (1) BR112013029416A2 (enExample)
CA (1) CA2835169C (enExample)
EA (1) EA023238B1 (enExample)
ES (1) ES2565200T3 (enExample)
MX (1) MX2013013436A (enExample)
TW (1) TW201249858A (enExample)
UY (1) UY34072A (enExample)
WO (1) WO2012156936A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY34072A (es) 2011-05-17 2013-01-03 Novartis Ag Derivados sustituidos de indol
MX2015005737A (es) * 2012-11-07 2015-09-16 Novartis Ag Derivados de indol sustituido.
MX378263B (es) * 2013-08-14 2025-03-10 Novartis Ag Terapia de combinación para el tratamiento del cáncer.
JP6998657B2 (ja) 2013-09-18 2022-02-04 エピアクシス セラピューティクス プロプライエタリー リミテッド 幹細胞調節ｉｉ
EP3185858A4 (en) 2014-08-25 2017-12-27 University of Canberra Compositions for modulating cancer stem cells and uses therefor
WO2025091442A1 (zh) * 2023-11-03 2025-05-08 北京凯因科技股份有限公司 一种神经氨酸酶抑制剂及在流感病毒中的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001027106A1 (en) * 1999-10-12 2001-04-19 F. Hoffmann-La Roche Ag Substituted pyrroles as antiproliferative agents for the treatment of cancer
WO2003082859A1 (en) * 2002-04-03 2003-10-09 Novartis Ag Indolylmaleimide derivatives

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4925860A (en) 1987-08-05 1990-05-15 E. I. Du Pont De Nemours And Company Stable pharmaceutical composition of 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester
DE4005970A1 (de) 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh Neue trisubstituierte maleinimide, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6204257B1 (en) 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
PE20020544A1 (es) * 2000-11-07 2002-07-30 Novartis Ag Derivados de indolilmaleimida
CA2470423C (en) 2001-12-21 2011-03-15 Guilford Pharmaceuticals, Inc. Process for preparing water-soluble phosphonooxymethyl derivatives of alcohol and phenol
CA2470500C (en) 2001-12-28 2012-05-15 Guilford Pharmaceuticals, Inc. Aqueous based pharmaceutical formulations of water-soluble prodrugs of propofol
EP1492544A4 (en) 2002-04-08 2005-10-12 Guilford Pharm Inc PHARMACEUTICAL COMPOSITIONS CONTAINING PROPOFOL-BASED WATER-SOLUBLE PRODRUGS AND METHODS OF ADMINISTRATION THEREOF
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AU2003223104A1 (en) 2003-03-19 2004-10-11 Suven Life Sciences Limited A process for the preparation of indolymaleimides
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2007008514A2 (en) 2005-07-07 2007-01-18 Georgetown University Inhibitors of glycogen synthase kinase 3
US20070203236A1 (en) 2006-01-11 2007-08-30 Smith Jeffrey W Novel antagonists of the human fatty acid synthase thioesterase
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
US8163902B2 (en) 2006-11-21 2012-04-24 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2011057204A2 (en) 2009-11-06 2011-05-12 The Johns Hopkins University Lrrk2-mediated neuronal toxicity
CN101812097B (zh) 2010-04-17 2012-04-25 中国海洋大学 吲哚咔唑和双吲哚马来酰亚胺生物碱及其制备方法和应用
UY34072A (es) 2011-05-17 2013-01-03 Novartis Ag Derivados sustituidos de indol

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001027106A1 (en) * 1999-10-12 2001-04-19 F. Hoffmann-La Roche Ag Substituted pyrroles as antiproliferative agents for the treatment of cancer
WO2003082859A1 (en) * 2002-04-03 2003-10-09 Novartis Ag Indolylmaleimide derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KUMPULAINEN H. ET AL.: "Synthesis, in vitro and in vivo characterization of novel ethyl dioxy phosphate prodrug of propofol", EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, ELSEVIER, AMSTERDAM, NL, vol. 34, no. 2-3, 3 July 2008 (2008-07-03), pages 110-117, XP022696122, ISSN: 0928-0987, DOI: 10.1016/J.EJPS.2008.02.121 [retrieved on 2008-03-02], page 110, left-hand column, last paragraph *

Also Published As

Publication number Publication date
EA201391710A1 (ru) 2014-03-31
US9029396B2 (en) 2015-05-12
BR112013029416A2 (pt) 2017-01-31
CA2835169A1 (en) 2012-11-22
US8703782B2 (en) 2014-04-22
ES2565200T3 (es) 2016-04-01
CA2835169C (en) 2019-05-14
UY34072A (es) 2013-01-03
TW201249858A (en) 2012-12-16
CN103534250B (zh) 2016-05-11
EP2709998B1 (en) 2016-01-06
CN103534250A (zh) 2014-01-22
US20130157980A1 (en) 2013-06-20
AU2012257345B2 (en) 2016-03-24
EP2709998A1 (en) 2014-03-26
JP2014518870A (ja) 2014-08-07
AR088414A1 (es) 2014-06-11
JP6043344B2 (ja) 2016-12-14
KR20140023354A (ko) 2014-02-26
MX2013013436A (es) 2013-12-06
US20140179634A1 (en) 2014-06-26
WO2012156936A1 (en) 2012-11-22

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