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MX2010009341A - Modulacion de enzima y receptor intracelulares. - Google Patents

Modulacion de enzima y receptor intracelulares.

Info

Publication number
MX2010009341A
MX2010009341A MX2010009341A MX2010009341A MX2010009341A MX 2010009341 A MX2010009341 A MX 2010009341A MX 2010009341 A MX2010009341 A MX 2010009341A MX 2010009341 A MX2010009341 A MX 2010009341A MX 2010009341 A MX2010009341 A MX 2010009341A
Authority
MX
Mexico
Prior art keywords
receptor
intracellular enzyme
modulator
cells
enzyme
Prior art date
Application number
MX2010009341A
Other languages
English (en)
Inventor
Stephen John Davies
Alan Hornsby Davidson
Alan Hastings Drummond
David Festus Charles Moffat
Alistair David Graham Donald
Original Assignee
Chroma Therapeutics Ltd
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 Chroma Therapeutics Ltd filed Critical Chroma Therapeutics Ltd
Publication of MX2010009341A publication Critical patent/MX2010009341A/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Analytical Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Los conjugados covalentes de un éster de glicina a,a-disubstituida y un modulador de la actividad de una enzima intracelular o receptor objetivo, en donde el grupo éster del conjugado es hidrolizable por una o más enzimas carboxilesterasas intracelulares al ácido correspondiente, y el éster de glicina a,a-disubstituida es conjugado al modulador en una posición remota de la interfase de enlace entre el inhibidor y la enzima o receptor objetivo pasan a las células y el producto de hidrólisis ácida activo se acumula dentro de las células.
MX2010009341A 2008-02-29 2009-02-27 Modulacion de enzima y receptor intracelulares. MX2010009341A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0803747.5A GB0803747D0 (en) 2008-02-29 2008-02-29 Enzyme and receptor modulation
PCT/GB2009/000561 WO2009106848A2 (en) 2008-02-29 2009-02-27 Enzyme and receptor modulation

Publications (1)

Publication Number Publication Date
MX2010009341A true MX2010009341A (es) 2010-09-24

Family

ID=39315698

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2010009341A MX2010009341A (es) 2008-02-29 2009-02-27 Modulacion de enzima y receptor intracelulares.

Country Status (15)

Country Link
US (3) US20100317865A1 (es)
EP (1) EP2252328A2 (es)
JP (1) JP2011513289A (es)
KR (2) KR20100126762A (es)
CN (1) CN101959534B (es)
AU (1) AU2009219926B2 (es)
BR (1) BRPI0908893A2 (es)
CA (2) CA2934402C (es)
EA (1) EA019838B1 (es)
GB (1) GB0803747D0 (es)
IL (1) IL207537A (es)
MX (1) MX2010009341A (es)
NZ (1) NZ587341A (es)
WO (1) WO2009106848A2 (es)
ZA (1) ZA201006071B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007017228A (ja) * 2005-07-06 2007-01-25 Cti Science System Co Ltd 河床高測定装置および河床高測定方法
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
GB201009853D0 (en) 2010-06-11 2010-07-21 Chroma Therapeutics Ltd HSP90 inhibitors
WO2012025701A1 (en) * 2010-08-25 2012-03-01 Chroma Therapeutics Ltd. Alpha, alpha - di substituted glycine ester derivatives and their use as hdac inhibitors
GB201211310D0 (en) 2012-06-26 2012-08-08 Chroma Therapeutics Ltd CSF-1R kinase inhibitors
DK3222616T3 (da) 2012-10-17 2019-08-19 Macrophage Pharma Ltd N-[2-{4-[6-amino-5-(2,4-difluorbenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorphenyl}ethyl]-L-alanin og terbutylester deraf
WO2017216297A1 (en) 2016-06-16 2017-12-21 Glaxosmithkline Intellectual Property Development Limited Dosage regimen
GB201713975D0 (en) 2017-08-31 2017-10-18 Macrophage Pharma Ltd Medical use
CN115896065B (zh) * 2022-09-06 2023-08-11 江南大学 一种立体选择性羧酯酶、编码基因、载体及其应用

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US5331006A (en) * 1990-08-31 1994-07-19 Warner-Lambert Company Amino acid analogs as CCK antagonists
JPH08151364A (ja) * 1994-02-18 1996-06-11 Nissan Chem Ind Ltd 含窒素環状化合物および除草剤
MX9704683A (es) * 1994-12-23 1997-09-30 Pfizer Inhibidores de la escualeno sintetasa.
JP2000198735A (ja) * 1998-10-28 2000-07-18 Takeda Chem Ind Ltd 縮合ピリダジン誘導体を含有してなる医薬
JP2003171381A (ja) * 2001-09-25 2003-06-20 Takeda Chem Ind Ltd エントリー阻害剤
MXPA04008822A (es) 2002-03-14 2004-11-26 Bayer Healthcare Ag Aroilpiridinonas monociclicas.
US20060235012A1 (en) * 2003-06-16 2006-10-19 Chroma Therapeutics Limited Carboline and betacarboline derivatives for use as hdac enzyme inhibitors
WO2005012324A2 (en) * 2003-07-30 2005-02-10 Gilead Sciences, Inc. Nucleobase phosphonate analogs for antiviral treatment
CN101014603B (zh) * 2004-05-14 2014-08-20 千禧药品公司 通过抑制极光激酶抑制有丝分裂的化合物和方法
EP2261226B1 (en) * 2004-05-14 2015-04-01 Millennium Pharmaceuticals, Inc. Methods for preparing aurora kinase inhibitors
GB0509223D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
GB0509227D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Intracellular enzyme inhibitors
GB0509225D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
EP1964577B1 (en) 2005-05-05 2016-04-13 GlaxoSmithKline Intellectual Property Development Limited Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase
GB0510204D0 (en) 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
AU2007246869B2 (en) 2006-05-04 2012-10-18 Macrophage Pharma Limited p38 MAP kinase inhibitors
GB0608837D0 (en) 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of MAP kinase
GB0608823D0 (en) 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of P13 kinase
GB0608821D0 (en) 2006-05-04 2006-06-14 Chroma Therapeutics Ltd DHFR enzyme inhibitors
WO2008018447A1 (en) * 2006-08-08 2008-02-14 Kyorin Pharmaceutical Co., Ltd. Aminoalcohol derivative and immunosuppressant containing the same as active ingredient
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
AU2007310604B2 (en) 2006-10-25 2012-02-02 Chroma Therapeutics Ltd. Pteridine derivatives as polo-like kinase inhibitors useful in the treatment of cancer
JP2010507648A (ja) * 2006-10-25 2010-03-11 ラモット アット テル−アビブ ユニバーシティー リミテッド グルタミン酸ｎｍｄａ活性を有する新規向精神薬
GB0621203D0 (en) 2006-10-25 2006-12-06 Chroma Therapeutics Ltd PLK inhibitors
JP5043120B2 (ja) 2006-10-30 2012-10-10 クロマ セラピューティクス リミテッド ヒストンデアセチラーゼの阻害剤としてのヒドロキサメート
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GB0622084D0 (en) 2006-11-06 2006-12-13 Chroma Therapeutics Ltd Inhibitors of HSP90
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JP2011503042A (ja) 2007-11-07 2011-01-27 クロマ セラピューティクス リミテッド ｐ３８ＭＡＰキナーゼ阻害剤
WO2009106844A1 (en) * 2008-02-29 2009-09-03 Chroma Therapeutics Ltd. Inhibitors of p38 map kinase
GB0807451D0 (en) * 2008-04-24 2008-05-28 Chroma Therapeutics Ltd Inhibitors of PLK
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors

Also Published As

Publication number Publication date
EP2252328A2 (en) 2010-11-24
CA2717020C (en) 2016-06-28
IL207537A0 (en) 2010-12-30
CA2934402C (en) 2020-04-21
JP2011513289A (ja) 2011-04-28
US9636409B2 (en) 2017-05-02
WO2009106848A2 (en) 2009-09-03
US20140088159A1 (en) 2014-03-27
US20160151509A1 (en) 2016-06-02
CA2934402A1 (en) 2009-09-03
CN101959534A (zh) 2011-01-26
KR20160074017A (ko) 2016-06-27
CN101959534B (zh) 2013-11-27
BRPI0908893A2 (pt) 2015-08-25
CA2717020A1 (en) 2009-09-03
AU2009219926A1 (en) 2009-09-03
US20100317865A1 (en) 2010-12-16
AU2009219926B2 (en) 2014-04-17
NZ587341A (en) 2012-07-27
GB0803747D0 (en) 2008-04-09
IL207537A (en) 2016-10-31
ZA201006071B (en) 2011-05-25
WO2009106848A3 (en) 2010-05-14
EA019838B1 (ru) 2014-06-30
KR20100126762A (ko) 2010-12-02
EA201001390A1 (ru) 2011-06-30

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Owner name: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT