UY35471A - INHIBITORS OF THE CELLULAR AND CONJUGATED PROLIFERATION OF THE SAME - Google Patents

INHIBITORS OF THE CELLULAR AND CONJUGATED PROLIFERATION OF THE SAME

Info

Publication number
UY35471A
UY35471A UY0001035471A UY35471A UY35471A UY 35471 A UY35471 A UY 35471A UY 0001035471 A UY0001035471 A UY 0001035471A UY 35471 A UY35471 A UY 35471A UY 35471 A UY35471 A UY 35471A
Authority
UY
Uruguay
Prior art keywords
inhibitors
proliferation
conjugated
cellular
same
Prior art date
Application number
UY0001035471A
Other languages
Spanish (es)
Inventor
Paul A Barsanti
Chamoin Sylvie
Bernhard Hubert Geierstanger
Robert Martin Grotzfeld
Darryl Brynley Jones
Lionel Doumampouom-Metoul
Stephanie Guerro-Lagasse
Karpov Alexei
Lafrance Marc
Cristina Nieto Oberhuber
Ou Weijia
Piizzi Grazia
Original Assignee
Novartis Ag
Irm Llc
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, Irm Llc filed Critical Novartis Ag
Publication of UY35471A publication Critical patent/UY35471A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Se describen en el presente documento inmunoconjugados que comprenden un inhibidor de Eg5 unido a u na fracción de unión a antígeno tal como un anticuerpo, útil para el tratamiento de trastornos prol iferativos de células. También se describen nuevos inhibidores de Eg5 que pueden ser utilizados ya sea solos o como parte de un inmunoconjugado para el tratamiento de trastornos de proliferación celular. Los inhibidores de Eg5 incluyen compuestos de esta fórmula como se describe en el presente d ocumento:Immunoconjugates comprising an inhibitor of Eg5 bound to an antigen-binding fraction such as an antibody, useful for the treatment of prolific cell disorders are described herein. New Eg5 inhibitors are also described that can be used either alone or as part of an immunoconjugate for the treatment of cell proliferation disorders. Eg5 inhibitors include compounds of this formula as described herein:

UY0001035471A 2013-03-15 2014-03-14 INHIBITORS OF THE CELLULAR AND CONJUGATED PROLIFERATION OF THE SAME UY35471A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361799384P 2013-03-15 2013-03-15
US201361869496P 2013-08-23 2013-08-23

Publications (1)

Publication Number Publication Date
UY35471A true UY35471A (en) 2014-10-31

Family

ID=50721875

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001035471A UY35471A (en) 2013-03-15 2014-03-14 INHIBITORS OF THE CELLULAR AND CONJUGATED PROLIFERATION OF THE SAME

Country Status (6)

Country Link
EP (1) EP2968591A1 (en)
JP (1) JP2016516035A (en)
CN (1) CN105451773A (en)
TW (1) TW201512174A (en)
UY (1) UY35471A (en)
WO (1) WO2014151030A1 (en)

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US9504756B2 (en) 2012-05-15 2016-11-29 Seattle Genetics, Inc. Self-stabilizing linker conjugates
KR102144069B1 (en) * 2012-05-15 2020-08-13 시애틀 지네틱스, 인크. Self-stabilizing linker conjugates
CN105143271A (en) 2013-02-08 2015-12-09 Irm责任有限公司 Specific sites for modifying antibodies to make immunoconjugates
BR112016014830A2 (en) * 2013-12-23 2017-09-19 Bayer Pharma AG ANTIBODY DRUG CONJUGATES (ADCS) WITH KSP INHIBITORS
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
JP6743015B2 (en) * 2014-12-15 2020-08-19 バイエル ファーマ アクチエンゲゼルシャフト Antibody drug conjugates (ADCs) with deglycosylated anti-TWEAKR antibody of KSP inhibitor
CN104478957A (en) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 Derivative containing nitrile-based benzene and bis-O-glucoside, preparation method thereof and application
CN113456829A (en) * 2015-03-19 2021-10-01 杭州多禧生物科技有限公司 Novel hydrophilic linkers and their use in ligand-drug conjugate conjugates
CA2990076A1 (en) * 2015-06-22 2016-12-29 Bayer Pharma Aktiengesellschaft Antibody drug conjugates (adcs) and antibody prodrug conjugates (apdcs) with enzymatically cleavable groups
CN108025085A (en) * 2015-06-23 2018-05-11 拜耳制药股份公司 The antibody drug conjugate (ADC) of KSP inhibitor and anti-B7H3 antibody
US20180318438A1 (en) 2015-06-23 2018-11-08 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-tweakr-antibodies
US11071788B2 (en) 2015-06-23 2021-07-27 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with antiB7H3-antibodies
US10744205B2 (en) 2015-06-23 2020-08-18 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with anti-CD123-antibodies
US10973923B2 (en) * 2015-06-23 2021-04-13 Bayer Pharma Aktiengesellschaft Site specific homogeneous with KSP inhibitors
MA44334A (en) 2015-10-29 2018-09-05 Novartis Ag ANTIBODY CONJUGATES INCLUDING A TOLL-TYPE RECEPTOR AGONIST
SG11201808167VA (en) * 2016-03-24 2018-10-30 Bayer Pharma AG Prodrugs of cytotoxic active agents having enzymatically cleavable groups
US10464969B2 (en) 2016-05-05 2019-11-05 Novartis Ag Amatoxin derivatives and conjugates thereof as inhibitors of RNA polymerase
US11001636B2 (en) 2016-06-15 2021-05-11 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (ADCs) with KSP inhibitors and anti-CD123-antibodies
KR20230066647A (en) * 2016-06-17 2023-05-16 마젠타 테라퓨틱스 인코포레이티드 Compositions and methods for the depletion of cd117+cells
WO2017219025A1 (en) * 2016-06-17 2017-12-21 Magenta Therapeutics, Inc. Compositions and methods for the depletion of cells
KR20190038579A (en) 2016-08-09 2019-04-08 시애틀 지네틱스, 인크. A drug conjugate with a self-stabilizing linker having improved physicochemical properties
IL310558A (en) 2016-12-21 2024-03-01 Bayer Pharma AG Antibody drug conjugates (adcs) having enzymatically cleavable groups
WO2018114804A1 (en) 2016-12-21 2018-06-28 Bayer Pharma Aktiengesellschaft Specific antibody drug conjugates (adcs) having ksp inhibitors
WO2018233571A1 (en) * 2017-06-19 2018-12-27 四川百利药业有限责任公司 Antibody-drug conjugate having acidic self-stabilization junction
US10646585B2 (en) 2017-09-15 2020-05-12 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and ligand-drug conjugates thereof
AU2019289506A1 (en) 2018-06-18 2021-02-04 Bayer Aktiengesellschaft Binder-drug conjugates directed against CXCR5, having enzymatically cleavable linkers and improved activity profile
CN115417802A (en) * 2021-05-16 2022-12-02 上海鼎雅药物化学科技有限公司 Preparation method of sepiatinib and intermediate thereof

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US7662581B1 (en) * 2003-12-18 2010-02-16 Novartis Vaccines And Diagnostics, Inc. Eg5 co-crystals
BRPI0510929A (en) * 2004-06-18 2007-07-17 Chiron Corp n- (1- (1-benzyl-4-phenyl-1h-imidazol-2-yl) -2,2-dimethylpropyl) benzamide derivatives and related compounds as kinesin axis protein (ksp) inhibitors for the treatment of cancer
MY147188A (en) * 2005-08-09 2012-11-14 Novartis Ag Substituted imidazole compounds as ksp inhibitors
US8129358B2 (en) * 2006-11-13 2012-03-06 Novartis Ag Substituted pyrazole and triazole compounds as KSP inhibitors
US7820646B2 (en) * 2007-01-05 2010-10-26 Novartis Vaccines And Diagnostics, Inc. Cyclized derivatives as Eg-5 inhibitors
US8252832B2 (en) * 2007-12-14 2012-08-28 Novartis Ag Kinesin inhibitors as cancer therapeutics
HUE025507T2 (en) * 2008-03-18 2016-02-29 Genentech Inc Combinations of an anti-her2 antibody-drug conjugate and chemotherapeutic agents, and methods of use
JP2012515749A (en) * 2009-01-26 2012-07-12 ノバルティス アーゲー Salts and polymorphs of kinesin inhibiting compounds
US8748626B2 (en) * 2010-04-15 2014-06-10 Novartis Ag Oxazole and thiazole compounds as KSP inhibitors
MX2012011910A (en) * 2010-04-15 2012-11-29 Novartis Ag Triazole compounds as ksp inhibitors.
KR102356286B1 (en) * 2011-05-27 2022-02-08 암브룩스, 인코포레이티드 Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
BR112013031819B1 (en) * 2011-06-10 2022-05-03 Mersana Therapeutics, Inc Polymeric support, pharmaceutical composition, compound and support use

Also Published As

Publication number Publication date
EP2968591A1 (en) 2016-01-20
TW201512174A (en) 2015-04-01
CN105451773A (en) 2016-03-30
JP2016516035A (en) 2016-06-02
WO2014151030A1 (en) 2014-09-25

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Legal Events

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Effective date: 20211206