TWI286544B - Deacetylase inhibitors - Google Patents

Deacetylase inhibitors Download PDF

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Publication number
TWI286544B
TWI286544B TW090121617A TW90121617A TWI286544B TW I286544 B TWI286544 B TW I286544B TW 090121617 A TW090121617 A TW 090121617A TW 90121617 A TW90121617 A TW 90121617A TW I286544 B TWI286544 B TW I286544B
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TW
Taiwan
Prior art keywords
group
alkyl
aromatic
aryl
compound
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TW090121617A
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English (en)
Chinese (zh)
Inventor
Kenneth Walter Bair
Micha El A Green
Lawrence B Perez
Stacy W Remiszewski
Lidia Sambucetti
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Novartis Ag
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Publication of TWI286544B publication Critical patent/TWI286544B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16Tryptamines
    • 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
    • C07D233/64Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Structural Engineering (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Materials Engineering (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW090121617A 2000-09-01 2001-08-31 Deacetylase inhibitors TWI286544B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22994300P 2000-09-01 2000-09-01
US29223201P 2001-05-18 2001-05-18

Publications (1)

Publication Number Publication Date
TWI286544B true TWI286544B (en) 2007-09-11

Family

ID=26923760

Family Applications (1)

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TW090121617A TWI286544B (en) 2000-09-01 2001-08-31 Deacetylase inhibitors

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US (5) US6552065B2 (OSRAM)
EP (2) EP1870399A1 (OSRAM)
JP (1) JP4012819B2 (OSRAM)
KR (1) KR100585484B1 (OSRAM)
CN (1) CN1300110C (OSRAM)
AR (1) AR035057A1 (OSRAM)
AT (1) ATE376999T1 (OSRAM)
AU (2) AU2001282129B2 (OSRAM)
BE (1) BE2015C062I2 (OSRAM)
BR (1) BRPI0113669B8 (OSRAM)
CA (1) CA2420899C (OSRAM)
CY (2) CY1107839T1 (OSRAM)
CZ (1) CZ302707B6 (OSRAM)
DE (1) DE60131179T2 (OSRAM)
DK (1) DK1318980T3 (OSRAM)
EC (1) ECSP034492A (OSRAM)
ES (1) ES2292610T3 (OSRAM)
FR (1) FR15C0086I2 (OSRAM)
HU (2) HU229796B1 (OSRAM)
IL (2) IL154574A0 (OSRAM)
LU (1) LU92890I2 (OSRAM)
MX (1) MXPA03001832A (OSRAM)
MY (1) MY136892A (OSRAM)
NL (1) NL300778I2 (OSRAM)
NO (2) NO324942B1 (OSRAM)
NZ (1) NZ524365A (OSRAM)
PE (1) PE20020354A1 (OSRAM)
PL (1) PL221738B1 (OSRAM)
PT (1) PT1318980E (OSRAM)
RU (1) RU2302408C3 (OSRAM)
SI (1) SI1318980T1 (OSRAM)
SK (1) SK287609B6 (OSRAM)
TW (1) TWI286544B (OSRAM)
WO (1) WO2002022577A2 (OSRAM)
ZA (1) ZA200301423B (OSRAM)

Families Citing this family (456)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US6822267B1 (en) * 1997-08-20 2004-11-23 Advantest Corporation Signal transmission circuit, CMOS semiconductor device, and circuit board
KR101026205B1 (ko) 1999-11-23 2011-03-31 메틸진 인코포레이티드 히스톤 디아세틸라제의 억제제
US20030129724A1 (en) 2000-03-03 2003-07-10 Grozinger Christina M. Class II human histone deacetylases, and uses related thereto
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
ATE430567T1 (de) 2000-09-29 2009-05-15 Topotarget Uk Ltd Carbaminsäurederivate enthaltend eine amidgruppe zur behandlung von malaria
US7312247B2 (en) * 2001-03-27 2007-12-25 Errant Gene Therapeutics, Llc Histone deacetylase inhibitors
CA2463552C (en) 2001-10-16 2011-05-17 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases and cancer of the brain
DE60217895T2 (de) * 2001-11-06 2007-07-05 Novartis Ag Kombination cyclooxygenase-2 inhibitor/ histone deacetylase inhibitor
US7148257B2 (en) 2002-03-04 2006-12-12 Merck Hdac Research, Llc Methods of treating mesothelioma with suberoylanilide hydroxamic acid
RU2394022C2 (ru) 2002-03-04 2010-07-10 МЕРК ЭйчДиЭйСи Рисерч, ЛЛС Способы индукции конечной дифференцировки
US7456219B2 (en) 2002-03-04 2008-11-25 Merck Hdac Research, Llc Polymorphs of suberoylanilide hydroxamic acid
DE60321775D1 (de) 2002-04-03 2008-08-07 Topotarget Uk Ltd Carbaminsäurederivate enthaltend eine piperazin verknüpfung als hdac-inhibitoren
WO2003087066A1 (en) * 2002-04-11 2003-10-23 Sk Chemicals, Co., Ltd. α,β-UNSATURATED HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS
BR0309280A (pt) * 2002-04-15 2005-02-22 Sloan Kettering Inst Cancer Terapia de combinação para o tratamento de câncer
JP2005535608A (ja) * 2002-06-10 2005-11-24 ノバルティス アクチエンゲゼルシャフト エポシロンを含む組み合わせおよびその薬学的使用
AU2003254951A1 (en) * 2002-08-20 2004-03-11 Yamanouchi Pharmaceutical Co., Ltd. Arthrodial cartilage extracellular matrix degradation inhibitor
ATE521354T1 (de) * 2002-09-13 2011-09-15 Univ Virginia Commonwealth Kombination aus imatinib und einem histondeacetylase-hemmer zur behandlung von leukämie
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7250514B1 (en) 2002-10-21 2007-07-31 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1562898A1 (en) * 2002-11-19 2005-08-17 Takeda Pharmaceutical Company Limited Indole derivatives as somatostatin agonists or antagonists
AU2003296310A1 (en) 2002-12-06 2004-06-30 University Of South Florida Histone deacetylase inhibitor enhancement of trail-induced apoptosis
US7135493B2 (en) * 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
EP1583736A1 (en) 2003-01-17 2005-10-12 TopoTarget UK Limited Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors
AU2003900587A0 (en) * 2003-02-11 2003-02-27 Fujisawa Pharmaceutical Co., Ltd. Hdac inhibitor
AU2003900608A0 (en) * 2003-02-11 2003-02-27 Fujisawa Pharmaceutical Co., Ltd. Hdac inhibitor
JP4790594B2 (ja) 2003-02-25 2011-10-12 トポターゲット ユーケー リミテッド Hdacインヒビターとしての、二環式ヘテロアリール基を含むヒドロキサム酸化合物
US7375228B2 (en) 2003-03-17 2008-05-20 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2006528952A (ja) * 2003-05-21 2006-12-28 ノバルティス アクチエンゲゼルシャフト ヒストンデアセチラーゼ阻害剤と化学療法剤の組み合わせ
WO2005011598A2 (en) 2003-07-31 2005-02-10 University Of South Florida Leukemia treatment method and composition
WO2005013958A1 (en) * 2003-08-07 2005-02-17 Novartis Ag Histone deacetylase inhibitors as immunosuppressants
WO2005014004A1 (en) * 2003-08-08 2005-02-17 Novartis Ag Combinations comprising staurosporines
DE602004026321D1 (de) 2003-08-26 2010-05-12 Merck Hdac Res Llc Verwendung von SAHA zur Behandlung von Mesotheliom
US20070190022A1 (en) 2003-08-29 2007-08-16 Bacopoulos Nicholas G Combination methods of treating cancer
CN100455564C (zh) * 2003-09-12 2009-01-28 深圳微芯生物科技有限责任公司 组蛋白去乙酰化酶抑制剂及其药用制剂的制备和应用
EP1667720A1 (en) * 2003-09-18 2006-06-14 Novartis AG Combination of a histone deacetylase inhibitor with a death receptor ligand
EP1673349B1 (en) * 2003-09-22 2010-06-30 S*Bio Pte Ltd Benzimidazole derivatives: preparation and pharmaceutical applications
TWI349664B (en) 2003-09-22 2011-10-01 S Bio Pte Ltd Benzimidazole derivatives: preparation and pharmaceutical applications
EA200600495A1 (ru) * 2003-09-23 2006-10-27 Новартис Аг Комбинация ингибитора vegf рецептора с химиотерапевтическим агентом
US20070167499A1 (en) * 2003-10-27 2007-07-19 A*Bio Pte Ltd. Biaryl linked hydroxamates: preparation and pharmaceutical applications
WO2005055928A2 (en) 2003-12-02 2005-06-23 The Ohio State University Research Foundation Zn2+ -chelating motif-tethered short -chain fatty acids as a novel class of histone deacetylase inhibitors
EP1541549A1 (en) * 2003-12-12 2005-06-15 Exonhit Therapeutics S.A. Tricyclic hydroxamate and benzaminde derivatives, compositions and methods
US20050137234A1 (en) * 2003-12-19 2005-06-23 Syrrx, Inc. Histone deacetylase inhibitors
WO2005065681A1 (en) * 2003-12-19 2005-07-21 Takeda San Diego, Inc. N- hydroxy-3-(3-(1h-imidazol-2-yl)-phenyl)-acrylamide derivatives and related compounds as histone deacetylase (hdac) inhibitors for the treatment of cancer
US20050197336A1 (en) * 2004-03-08 2005-09-08 Miikana Therapeutics Corporation Inhibitors of histone deacetylase
US7345043B2 (en) * 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
SI2253614T1 (sl) 2004-04-07 2013-01-31 Novartis Ag Inhibitorji za IAP
CN101018547A (zh) * 2004-07-19 2007-08-15 默克公司 组蛋白脱乙酰基酶抑制剂
JP4946861B2 (ja) * 2004-08-09 2012-06-06 アステラス製薬株式会社 ヒストンデアセチラーゼ(hdac)の阻害活性を有するヒドロキシアミド化合物
ITMI20041869A1 (it) * 2004-10-01 2005-01-01 Dac Srl Nuovi inibitori delle istone deacetilasi
US8242175B2 (en) 2004-10-01 2012-08-14 Dac S.R.L. Class of histone deacetylase inhibitors
US20070021612A1 (en) * 2004-11-04 2007-01-25 University Of Notre Dame Du Lac Processes and compounds for preparing histone deacetylase inhibitors and intermediates thereof
US7235688B1 (en) 2004-11-04 2007-06-26 University Of Notre Dame Du Lac Process for preparing histone deacetylase inhibitors and intermediates thereof
WO2006066133A2 (en) 2004-12-16 2006-06-22 Takeda San Diego, Inc. Histone deacetylase inhibitors
WO2006088949A1 (en) 2005-02-14 2006-08-24 Miikana Therapeutics, Inc. Fused heterocyclic compounds useful as inhibitors of histone deacetylase
US7666880B2 (en) 2005-03-21 2010-02-23 S*Bio Pte Ltd. Imidazo[1,2-A]pyridine derivatives: preparation and pharmaceutical applications
WO2006102557A2 (en) 2005-03-22 2006-09-28 The President And Fellows Of Harvard College Treatment of protein degradation disorders
GB0509223D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
GB0509225D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
EP1896436A2 (en) 2005-05-11 2008-03-12 Takeda San Diego, Inc. Histone deacetylase inhibitors
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
TWI415603B (zh) 2005-05-20 2013-11-21 Merck Sharp & Dohme 1,8-辛二醯基苯胺羥胺酸(suberoylanilide hydroxamic acid)之調配物及其製配方法
EP1904452A2 (en) 2005-07-14 2008-04-02 Takeda San Diego, Inc. Histone deacetylase inhibitors
WO2007016532A2 (en) * 2005-08-02 2007-02-08 Novartis Ag Mutations and polymorphisms of hdac4
CA2617274C (en) 2005-08-03 2017-10-10 Novartis Ag Use of hdac inhibitors for the treatment of myeloma
WO2007021682A1 (en) * 2005-08-10 2007-02-22 Novartis Ag Method of use of deacetylase inhibitors
CA2617979A1 (en) * 2005-08-11 2007-02-22 Novartis Ag Combination of a pyrimydlaminobenzamide tyrosine kinase inhibitor and a histone deacetylase inhibitor
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
KR20080052611A (ko) * 2005-08-26 2008-06-11 메틸진 인크. 히스톤 탈아세틸 효소의 벤조디아제핀 및 벤조피페라진유도체 억제제
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
WO2007030454A2 (en) * 2005-09-07 2007-03-15 Novartis Ag Mutations and polymorphisms of hdac9
WO2007030455A2 (en) * 2005-09-07 2007-03-15 Novartis Ag Mutations and polymorphisms of hdac10
WO2007038073A2 (en) * 2005-09-22 2007-04-05 Novartis Ag Mutations and polymorphisms of hdac11
AR058065A1 (es) 2005-09-27 2008-01-23 Novartis Ag Compuestos de carboxiamina y uso de los mismos.composiciones farmaceuticas.
WO2007047998A2 (en) * 2005-10-21 2007-04-26 Novartis Ag Mutations and polymorphisms of hdac2
EP2377530A3 (en) 2005-10-21 2012-06-20 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
CN101291664A (zh) 2005-10-24 2008-10-22 诺瓦提斯公司 组蛋白脱乙酰基酶抑制剂与放射的组合
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
WO2007053502A2 (en) * 2005-11-01 2007-05-10 Novartis Ag Mutations and polymorphisms of hdac5
WO2007058992A2 (en) * 2005-11-14 2007-05-24 Novartis Ag Mutations and polymorphisms of hdac6
CA2629245C (en) 2005-11-21 2016-07-12 Novartis Ag Neuroendocrine tumor treatment
US20070207950A1 (en) * 2005-12-21 2007-09-06 Duke University Methods and compositions for regulating HDAC6 activity
JP2009525955A (ja) * 2006-01-13 2009-07-16 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
PL1981877T3 (pl) * 2006-02-07 2012-12-31 Astellas Pharma Inc Związki N-hydroksyakryloamidowe
JP5441416B2 (ja) * 2006-02-14 2014-03-12 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二官能性ヒストンデアセチラーゼインヒビター
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
GB0605120D0 (en) 2006-03-14 2006-04-26 Novartis Ag Organic Compounds
CN102861338A (zh) 2006-04-05 2013-01-09 诺瓦提斯公司 用于治疗癌症、包含bcr-abl/c-kit/pdgf-r tk抑制剂的组合
KR20080108517A (ko) 2006-04-05 2008-12-15 노파르티스 아게 암을 치료하기 위한 치료제의 조합물
US8168383B2 (en) 2006-04-14 2012-05-01 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
US7700339B2 (en) 2006-04-14 2010-04-20 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
CA2650520A1 (en) 2006-04-24 2008-01-31 Gloucester Pharmaceuticals Treatment of ras-expressing tumors
US20090018142A9 (en) * 2006-05-02 2009-01-15 Zhengping Zhuang Use of phosphatases to treat tumors overexpressing N-CoR
AU2007249435A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 HT receptor mediated neurogenesis
BRPI0711385A2 (pt) 2006-05-09 2011-11-08 Novartis Ag combinação compreendendo um quelante de ferro e um agente anti-neoplástico e seu uso
JP2009536669A (ja) 2006-05-09 2009-10-15 ブレインセルス,インコーポレイティド アンジオテンシン調節による神経新生
US8957027B2 (en) 2006-06-08 2015-02-17 Celgene Corporation Deacetylase inhibitor therapy
EP2394991B1 (en) * 2006-06-12 2015-09-23 Novartis AG Process for making starting materials for N-hydroxy-3-[4-[2-(2-methyl-1 H-indol-3-yl)-ethylaminomethyl]-phenyl]-2E-2-propenamide
US7989639B2 (en) 2006-06-12 2011-08-02 Novartis Ag Process for making salts of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide
MX2008015900A (es) 2006-06-12 2009-03-06 Novartis Ag Polimorfos de n-hidroxi-3-[4-[[[2-(2-metil-1h-indol-3-il)etil]amin o]metil]fenil]-2e-2-propenamida.
PL2032531T3 (pl) * 2006-06-12 2016-07-29 Novartis Ag Sole N-hydroksy-3-[4-[[[2-(2-metylo-1H-indol-3-ilo)etylo]amino]metylo]fenylo]-2E-2-propenoamidu
UA95289C2 (en) * 2006-06-12 2011-07-25 Новартис Аг Salts of n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2e-2-propenamide
KR20090023631A (ko) * 2006-06-26 2009-03-05 노파르티스 아게 유기 화합물
AU2007292848A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2008036046A1 (en) 2006-09-20 2008-03-27 S*Bio Pte Ltd IMIDAZO[l,2-a]PYRIDINE HYDROXYMATE COMPOUNDS THAT ARE INHIBITORS OF HISTONE DEACETYLASE
CA2663614A1 (en) * 2006-09-28 2008-04-10 Merck And Co., Inc. Amine base salts of saha and polymorphs thereof
MX2009003185A (es) 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
GB0619753D0 (en) * 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
EA017198B1 (ru) 2006-10-30 2012-10-30 Хрома Терапьютикс Лтд. Гидроксаматы в качестве ингибиторов гистон-деацетилазы
CA2669675A1 (en) * 2006-11-10 2008-05-15 Syndax Pharmaceuticals, Inc. Combination of er.alpha.+ ligands and histone deacetylase inhibitors for the treatment of cancer
BRPI0719746A2 (pt) * 2006-12-04 2013-12-10 Novartis Ag Combinação
CN101583599A (zh) * 2006-12-15 2009-11-18 安斯泰来制药有限公司 N-羟基丙烯酰胺化合物
BRPI0806341A2 (pt) * 2007-01-10 2011-09-06 Novartis Ag formulações de inibidores de desacetilase
BRPI0806365B8 (pt) 2007-02-06 2021-05-25 Lixte Biotechnology Holdings Inc composto, uso do composto, composição farmacêutica e uso da composição farmacêutica
WO2008100985A2 (en) 2007-02-15 2008-08-21 Novartis Ag Combination of lbh589 with other therapeutic agents for treating cancer
CA2680838A1 (en) 2007-03-28 2008-10-16 Santen Pharmaceutical Co., Ltd. Intraocular pressure-lowering agent comprising compound having histone deacetylase inhibitory effect as active ingredient
AU2008235212B2 (en) 2007-04-09 2014-01-16 Methylgene Inc. Inhibitors of histone deacetylase
MX2009011692A (es) * 2007-05-04 2009-11-10 Novartis Ag Uso de inhibidores de desacetilasa de histona (hdac) para el tratamiento de canceres gastrointestinales.
TW200911231A (en) * 2007-05-11 2009-03-16 Novartis Ag Use of HDAC inhibitors for the treatment of melanoma
US20100179208A1 (en) * 2007-05-30 2010-07-15 Novartis Ag Use of HDAC Inhibitors for the Treatment of Bone Destruction
US7737175B2 (en) 2007-06-01 2010-06-15 Duke University Methods and compositions for regulating HDAC4 activity
WO2009020565A1 (en) * 2007-08-03 2009-02-12 Lixte Biotechnology, Inc. Use of phosphates to treat neuroblastomas and medullogastomas
CL2008002786A1 (es) * 2007-09-20 2009-05-15 Novartis Ag Torta farmceuticamente aceptable, formada por liofilizacion, que comprende: n-hidroxi-3-[4-[[[2-(2-metil-1h-indol-3-il]-etil]-amino]-metil]-fenil]-2e-2-propenamida o una sal, un regulador de ph seleciondo de lactato o acidop lactico, fodfato o acido fosforico o una combinacion y un agente de volumen; proceso de elaboracion.
EP2200439B1 (en) 2007-10-01 2017-03-22 Lixte Biotechnology, Inc. Hdac inhibitors
EP2209765A4 (en) * 2007-10-22 2010-12-01 Orchid Res Lab Ltd HISTONE DEACETYLASE INHIBITORS
CN101417967A (zh) * 2007-10-26 2009-04-29 浙江海正药业股份有限公司 组蛋白去乙酰酶抑制剂、其组合物及其应用
US20090131367A1 (en) * 2007-11-19 2009-05-21 The Regents Of The University Of Colorado Combinations of HDAC Inhibitors and Proteasome Inhibitors
US20110044952A1 (en) * 2007-11-27 2011-02-24 Ottawa Health Research Institute Amplification of cancer-specific oncolytic viral infection by histone deacetylase inhibitors
CA2708281A1 (en) 2007-12-11 2009-08-27 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties
ITFI20070288A1 (it) 2007-12-21 2009-06-22 A I L Firenze Sezione Autonoma Inibitori delle deacetilasi istoniche
EP2100879A1 (en) * 2008-03-13 2009-09-16 4Sc Ag Novel N-substituted tetrahydroisoquinoline/isoindoline hydroxamic acid compounds
PL2268612T3 (pl) 2008-03-24 2015-02-27 Novartis Ag Arylosulfonamidowe inhibitory metaloproteinaz macierzy
EP2628726A1 (en) * 2008-03-26 2013-08-21 Novartis AG Hydroxamate-based inhibitors of deacetylases b
KR20110031980A (ko) * 2008-07-18 2011-03-29 노파르티스 아게 호지킨병의 치료를 위한 hdac 억제제의 용도
RU2515611C2 (ru) 2008-07-23 2014-05-20 Президент Энд Феллоуз Оф Гарвард Колледж Ингибиторы деацетилазы и их применение
WO2010147612A1 (en) 2009-06-18 2010-12-23 Lixte Biotechnology, Inc. Methods of modulating cell regulation by inhibiting p53
US8227473B2 (en) * 2008-08-01 2012-07-24 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes, their preparation and use
AU2009277179A1 (en) * 2008-08-01 2010-02-04 Lixte Biotechnology, Inc. Methods for regulating cell mitosis by inhibiting serine/threonine phosphatase
US8058268B2 (en) * 2008-08-01 2011-11-15 Lixte Biotechnology, Inc. Neuroprotective agents for the prevention and treatment of neurodegenerative diseases
WO2010083617A1 (en) 2009-01-21 2010-07-29 Oncalis Ag Pyrazolopyrimidines as protein kinase inhibitors
PT2391366E (pt) 2009-01-29 2013-02-05 Novartis Ag Benzimidazoles substituídos para o tratamento de astrocitomas
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
GB0903480D0 (en) * 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
KR101168801B1 (ko) 2009-03-27 2012-07-25 주식회사종근당 신규한 하이드록사메이트 유도체, 이의 제조방법, 및 이를 함유하는 약제학적 조성물
US7994357B2 (en) 2009-04-03 2011-08-09 Naturewise Biotech & Medicals Corporation Cinamic compounds and derivatives therefrom for the inhibition of histone deacetylase
ES2473792T3 (es) 2009-04-03 2014-07-07 Naturewise Biotech & Medicals Corporation Compuestos cin�micos y derivados de los mismos para la inhibición de la histona desacetilasa
WO2011006908A2 (en) 2009-07-16 2011-01-20 Royal College Of Surgeons In Ireland Metal complexes having dual histone deacetylase inhibitory and dna-binding activity
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
WO2011019393A2 (en) 2009-08-11 2011-02-17 President And Fellows Of Harvard College Class- and isoform-specific hdac inhibitors and uses thereof
EP2464649A1 (en) 2009-08-12 2012-06-20 Novartis AG Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
JP5819831B2 (ja) 2009-08-17 2015-11-24 インテリカイン, エルエルシー 複素環式化合物およびそれらの使用
JP5775871B2 (ja) 2009-08-20 2015-09-09 ノバルティス アーゲー ヘテロ環式オキシム化合物
EP2470502A1 (en) 2009-08-26 2012-07-04 Novartis AG Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
US20110053925A1 (en) * 2009-08-28 2011-03-03 Novartis Ag Hydroxamate-Based Inhibitors of Deacetylases
JP5466767B2 (ja) 2009-11-04 2014-04-09 ノバルティス アーゲー Mek阻害剤として有用なヘテロ環式スルホンアミド誘導体
CN102781237A (zh) 2009-11-23 2012-11-14 天蓝制药公司 用于传递治疗剂的基于环糊精的聚合物
CA2781218A1 (en) 2009-12-08 2011-06-16 Novartis Ag Heterocyclic sulfonamide derivatives
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CU24130B1 (es) 2009-12-22 2015-09-29 Novartis Ag Isoquinolinonas y quinazolinonas sustituidas
US20130040998A1 (en) * 2010-01-08 2013-02-14 Dana-Farber Cancer Institute, Inc. Fluorinated hdac inhibitors and uses thereof
WO2011088181A1 (en) 2010-01-13 2011-07-21 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2011088192A1 (en) 2010-01-13 2011-07-21 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2011090940A1 (en) 2010-01-19 2011-07-28 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
UY33236A (es) 2010-02-25 2011-09-30 Novartis Ag Inhibidores dimericos de las iap
US8217079B2 (en) 2010-03-26 2012-07-10 Italfarmaco Spa Method for treating Philadelphia-negative myeloproliferative syndromes
US20110237686A1 (en) 2010-03-26 2011-09-29 Cerulean Pharma Inc Formulations and methods of use
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
EP2407164A1 (en) 2010-07-14 2012-01-18 Dublin Institute of Technology Intellectual Property Ltd Copper II complexes of phenanthroline and their use in cancer treatment
WO2012025701A1 (en) * 2010-08-25 2012-03-01 Chroma Therapeutics Ltd. Alpha, alpha - di substituted glycine ester derivatives and their use as hdac inhibitors
WO2012025155A1 (en) * 2010-08-26 2012-03-01 Novartis Ag Hydroxamate-based inhibitors of deacetylases
EA201390292A1 (ru) * 2010-08-27 2013-08-30 Новартис Аг Ингибиторы деацетилазы на основе гидроксамата
WO2012080260A1 (en) 2010-12-13 2012-06-21 Novartis Ag Dimeric iap inhibitors
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
EP3239154A1 (en) 2011-01-10 2017-11-01 Nimbus Iris, Inc. Irak inhibitors and uses thereof
TW201245115A (en) 2011-01-24 2012-11-16 Chdi Foundation Inc Histone deacetylase inhibitors and compositions and methods of use thereof
EP2673277A1 (en) 2011-02-10 2013-12-18 Novartis AG [1, 2, 4]triazolo [4, 3 -b]pyridazine compounds as inhibitors of the c-met tyrosine kinase
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
US20140051716A1 (en) 2011-03-09 2014-02-20 Cereno Scientific Ab Compounds and methods for improving impaired endogenous fibrinolysis using histone deacetylase inhibitors
EP2718276A1 (en) 2011-06-09 2014-04-16 Novartis AG Heterocyclic sulfonamide derivatives
JP6200884B2 (ja) 2011-06-14 2017-09-20 ノバルティス アーゲー 骨髄増殖性腫瘍などの癌の治療におけるパノビノスタットおよびルキソリチニブの組合せ
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
US8859586B2 (en) 2011-06-20 2014-10-14 Novartis Ag Cyclohexyl isoquinolinone compounds
SG195067A1 (en) 2011-06-27 2013-12-30 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives
WO2014081405A2 (en) 2011-08-17 2014-05-30 Dennis Brown Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted hexitols such as dibromodulcitol
ES2691650T3 (es) 2011-09-15 2018-11-28 Novartis Ag 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como inhibidores de tirosina quinasa c-Met
WO2013070996A1 (en) 2011-11-11 2013-05-16 Novartis Ag Method of treating a proliferative disease
AU2012340759C1 (en) 2011-11-23 2019-11-28 Array Biopharma Inc. Pharmaceutical formulations
CN103130673B (zh) * 2011-11-28 2017-05-03 重庆医药工业研究院有限责任公司 一种阿戈美拉晶型i的制备方法
JP5992054B2 (ja) 2011-11-29 2016-09-14 ノバルティス アーゲー ピラゾロピロリジン化合物
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
PL2794600T3 (pl) 2011-12-22 2018-06-29 Novartis Ag Pochodne 2,3-dihydro-benzo[1,4]oksazyny i powiązane związki jako inhibitory kinazy fosfoinozytydu-3 (PI3K) do leczenia np. reumatoidalnego zapalenia stawów
WO2013093850A1 (en) 2011-12-22 2013-06-27 Novartis Ag Quinoline derivatives
CN104125953A (zh) 2011-12-23 2014-10-29 诺华股份有限公司 用于抑制bcl2与结合配偶体相互作用的化合物
KR20140107578A (ko) 2011-12-23 2014-09-04 노파르티스 아게 Bcl2와 결합 파트너의 상호작용을 억제하기 위한 화합물
MX2014007729A (es) 2011-12-23 2015-01-12 Novartis Ag Compuestos para inhibir la interaccion de bcl2 con los componentes de enlace.
US20140357666A1 (en) 2011-12-23 2014-12-04 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
US20130178520A1 (en) 2011-12-23 2013-07-11 Duke University Methods of treatment using arylcyclopropylamine compounds
CN104125954A (zh) 2011-12-23 2014-10-29 诺华股份有限公司 用于抑制bcl2与结合配偶体相互作用的化合物
HK1200809A1 (en) * 2011-12-29 2015-08-14 药品循环有限责任公司 Cinnamic acid hydroxyamides as inhibitors of histone deacetylase 8
EP3608317A1 (en) 2012-01-12 2020-02-12 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
AR092790A1 (es) * 2012-02-01 2015-05-06 Euro Celtique Sa Derivados bencimidazolicos del acido hidroxamico
JP2015512425A (ja) 2012-04-03 2015-04-27 ノバルティス アーゲー チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用
ES2646777T3 (es) 2012-05-15 2017-12-15 Novartis Ag Derivados de pirimidina, piridina y pirazina amida sustituidos con tiazol o imidazol y compuestos relacionados como inhibidores de ABL1, ABL2 y BCR-ABL1 para el tratamiento del cáncer, infecciones víricas específicas y trastornos específicos del CNS
KR20150020169A (ko) 2012-05-15 2015-02-25 노파르티스 아게 Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체
BR112014027244A2 (pt) 2012-05-15 2017-06-27 Novartis Ag derivados de benzamida para inibição da atividade de abl1, abl2 e bcr-abl1
MA37519B1 (fr) 2012-05-15 2017-03-31 Novartis Ag Composés et compositions pour inhiber l'activité d'abl1, abl2 et bcr-abl1
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
AU2013274101B2 (en) 2012-06-15 2017-09-07 The Brigham And Women's Hospital, Inc. Compositions for treating cancer and methods for making the same
TW201408628A (zh) 2012-07-16 2014-03-01 Chdi Foundation Inc 組蛋白去乙醯酶抑制劑及組成物,暨其使用之方法
US9738643B2 (en) 2012-08-06 2017-08-22 Duke University Substituted indazoles for targeting Hsp90
ES2654143T3 (es) 2012-10-02 2018-02-12 Gilead Sciences, Inc. Inhibidores de desmetilasas de histonas
JP6343285B2 (ja) 2012-10-30 2018-06-13 メイ ファーマ, インク.Mei Pharma, Inc. 併用療法
WO2014071402A1 (en) 2012-11-05 2014-05-08 Dana-Farber Cancer Institute, Inc. Xbp1, cd138, and cs1, pharmaceutical compositions that include the peptides, and methods of using such petides and compositions
JP2015536964A (ja) 2012-11-08 2015-12-24 ノバルティス アーゲー B−raf阻害剤とヒストン脱アセチル化酵素阻害剤を含む医薬組合せおよび増殖性疾患の治療におけるそれらの使用
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫-吡啶并-□衍生物之固體形式
US9556180B2 (en) 2013-01-22 2017-01-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction
US9403827B2 (en) 2013-01-22 2016-08-02 Novartis Ag Substituted purinone compounds
WO2014128612A1 (en) 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
AP2015008676A0 (en) 2013-02-27 2015-08-31 Epitherapeutics Aps Inhibitors of histone demethylases
EP2968340A4 (en) 2013-03-15 2016-08-10 Intellikine Llc COMBINING KINASE INHIBITORS AND USES THEREOF
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
AU2014251038A1 (en) 2013-04-08 2015-11-26 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
MX2015014249A (es) 2013-04-09 2016-06-02 Lixte Biotechnology Inc Formulaciones de oxabicicloheptanos y oxabicicloheptenos.
MX372861B (es) * 2013-04-29 2020-07-07 Chong Kun Dang Pharmaceutical Corp Compuestos novedosos para inhibidores selectivos de histona deacetilasa, y composición farmacéutica que comprende los mismos.
US20150018376A1 (en) 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
EP3024456A4 (en) 2013-07-26 2017-04-12 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
WO2015022663A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
WO2015022664A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
RU2675105C9 (ru) 2013-09-22 2019-01-09 Саншайн Лейк Фарма Ко., Лтд. Замещенные аминопиримидиновые соединения и способы их использования
EP3049442A4 (en) 2013-09-26 2017-06-28 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
CN103467359B (zh) * 2013-09-27 2015-04-22 山东大学 一种含有吲哚的肉桂酰胺类组蛋白去乙酰化酶抑制剂及其制备方法和应用
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
CN103664734B (zh) * 2013-12-10 2015-09-23 广州康缔安生物科技有限公司 杂环羟肟酸类化合物及其药用组合物和应用
PT3080125T (pt) 2013-12-12 2018-12-14 Chong Kun Dang Pharmaceutical Corp Novos derivados de azaindole como inibidores seletivos da histona-desacetilase (hdac) e composições farmacêuticas que compreendem os mesmos
KR101685639B1 (ko) 2014-01-03 2016-12-12 주식회사 종근당 신규한 인돌 유도체 화합물 및 이를 포함하는 약제학적 조성물
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
EP3110820B1 (en) 2014-02-28 2022-04-06 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
DK3116909T3 (da) 2014-03-14 2020-01-20 Novartis Ag Antistofmolekyler til lag-3 og anvendelser deraf
US10000469B2 (en) 2014-03-25 2018-06-19 Duke University Heat shock protein 70 (hsp-70) receptor ligands
EP3122730B1 (en) 2014-03-28 2020-03-25 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
US20170369444A1 (en) 2014-03-31 2017-12-28 Marc Labelle Inhibitors of histone demethylases
MX2016012893A (es) 2014-04-03 2017-05-12 Invictus Oncology Pvt Ltd Sustancias terapéuticas combinadas supramoleculares.
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
GB201409485D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
GB201409488D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
GB201409471D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
BR112017001695A2 (pt) 2014-07-31 2017-11-21 Novartis Ag terapia de combinação
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
EP4578865A3 (en) 2014-08-12 2025-07-30 Monash University Lymph directing prodrugs
SG11201701182VA (en) 2014-08-27 2017-03-30 Gilead Sciences Inc Compounds and methods for inhibiting histone demethylases
EP2995630A1 (en) 2014-09-09 2016-03-16 Dublin Institute of Technology Hybrid compounds formed from ionic liquids and uses thereof in ion selective electrodes
US11344620B2 (en) 2014-09-13 2022-05-31 Novartis Ag Combination therapies
EP3200775B1 (en) 2014-10-03 2019-11-20 Novartis AG Combination therapies
SI3215518T1 (sl) 2014-10-29 2021-08-31 Bicyclerd Limited Biciklični peptidni ligandi, značilni za MT1-MMP
TWI744225B (zh) 2015-02-27 2021-11-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途
MX2017011597A (es) 2015-03-10 2018-05-11 Aduro Biotech Inc Composiciones y metodos para activar la señalizacion dependiente del "estimulador del gen de interferon".
SG11201707418WA (en) 2015-03-13 2017-10-30 Forma Therapeutics Inc Alpha-cinnamide compounds and compositions as hdac8 inhibitors
KR20230175343A (ko) 2015-03-18 2023-12-29 아비나스 오퍼레이션스, 인코포레이티드 타겟화된 단백질들의 향상된 분해를 위한 화합물들 및 방법들
DK3297992T3 (da) 2015-05-22 2020-04-20 Chong Kun Dang Pharmaceutical Corp Heterocykliske alkylderivatforbindelser som selektive histondeacetylase-inhibitorer og farmaceutiske sammensætninger omfattende samme
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2017004133A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2017024318A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
WO2017032281A1 (zh) * 2015-08-21 2017-03-02 苏州晶云药物科技有限公司 帕比司他乳酸盐的新晶型
EP3344624B8 (en) 2015-09-02 2023-11-29 Takeda Pharmaceutical Company Limited Tyk2 inhibitors and uses thereof
CN114031658A (zh) 2015-09-08 2022-02-11 莫纳什大学 定向淋巴的前药
WO2017044434A1 (en) 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
DK3364958T3 (da) 2015-10-23 2023-04-11 Navitor Pharm Inc Modulatorer af sestrin-gator2-interaktion og anvendelser deraf
RU2018120330A (ru) 2015-11-02 2019-12-04 Йейл Юниверсити Химерные соединения, осуществляющие нацеливание для протеолиза, и способы их получения и применения
ITUB20155193A1 (it) 2015-11-03 2017-05-03 Italfarmaco Spa Sospensioni orali di Givinostat fisicamente e chimicamente stabili
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
CA3008279A1 (en) 2015-12-14 2017-06-22 X4 Pharmaceuticals, Inc. Methods for treating cancer
ES2907489T3 (es) 2015-12-14 2022-04-25 X4 Pharmaceuticals Inc Métodos para el tratamiento del cáncer
WO2017112894A1 (en) 2015-12-22 2017-06-29 X4 Pharmaceuticals, Inc. Methods for treating immunodeficiency disease
CN105732467A (zh) * 2016-01-13 2016-07-06 深圳市康立生生物科技有限公司 一种panobinostat(帕比司他)的制备方法
HRP20211220T1 (hr) 2016-03-09 2021-10-29 Raze Therapeutics Inc. Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba
WO2017156179A1 (en) 2016-03-09 2017-09-14 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
IL261721B (en) 2016-03-15 2022-07-01 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
CN114377137A (zh) 2016-03-15 2022-04-22 奥莱松基因组股份有限公司 用于治疗血液恶性肿瘤的lsd1抑制剂的组合
EP3440112A4 (en) 2016-04-08 2019-10-09 X4 Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90
AR108257A1 (es) 2016-05-02 2018-08-01 Mei Pharma Inc Formas polimórficas de 3-[2-butil-1-(2-dietilamino-etil)-1h-bencimidazol-5-il]-n-hidroxi-acrilamida y usos de las mismas
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
CN109640988A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
EP3471727B1 (en) 2016-06-21 2020-12-09 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
EP3484858A4 (en) * 2016-06-21 2020-02-26 The University of Melbourne HIV LATENCY ACTIVATORS
JP6994767B2 (ja) 2016-06-21 2022-01-14 エックス4 ファーマシューティカルズ, インコーポレイテッド Cxcr4阻害剤およびその使用
WO2018015493A1 (en) 2016-07-20 2018-01-25 Royal College Of Surgeons In Ireland Metal complexes having therapeutic applications
WO2018039203A1 (en) 2016-08-23 2018-03-01 Oncopep, Inc. Peptide vaccines and durvalumab for treating multiple myeloma
CA3034666A1 (en) 2016-08-23 2018-03-01 Oncopep, Inc. Peptide vaccines and durvalumab for treating breast cancer
WO2018054960A1 (en) 2016-09-21 2018-03-29 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for predicting and treating resistance to chemotherapy in npm-alk(+) alcl
US10207998B2 (en) 2016-09-29 2019-02-19 Duke University Substituted benzimidazole and substituted benzothiazole inhibitors of transforming growth factor-β kinase and methods of use thereof
US10927083B2 (en) 2016-09-29 2021-02-23 Duke University Substituted benzimidazoles as inhibitors of transforming growth factor-β kinase
WO2018068832A1 (en) 2016-10-11 2018-04-19 Euro-Celtique S.A. Hodgkin lymphoma therapy
IL315777A (en) 2016-10-14 2024-11-01 Takeda Pharmaceuticals Co Tyk2 inhibitors and uses thereof
CA3040286A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2018089499A1 (en) 2016-11-08 2018-05-17 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
WO2018102397A1 (en) 2016-11-29 2018-06-07 PureTech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
CN110234647B (zh) 2016-12-08 2023-05-23 利克斯特生物技术公司 用于调节免疫应答的氧杂双环庚烷
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
TW202515876A (zh) 2017-03-08 2025-04-16 日商武田藥品工業股份有限公司 Tyk2抑制劑及其用途
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
US11339144B2 (en) 2017-04-10 2022-05-24 Navitor Pharmaceuticals, Inc. Heteroaryl Rheb inhibitors and uses thereof
JOP20180036A1 (ar) 2017-04-18 2019-01-30 Vifor Int Ag أملاح لمثبطات فروبورتين جديدة
US10857196B2 (en) 2017-04-27 2020-12-08 Bicycletx Limited Bicyclic peptide ligands and uses thereof
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
CN107141244B (zh) * 2017-05-08 2019-11-19 潍坊医学院 吲哚丁酸类组蛋白去乙酰酶抑制剂及其制备方法和应用
GB201709405D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating ovarian cancer
GB201709406D0 (en) 2017-06-13 2017-07-26 Euro-Cletique S A Compounds for treating TNBC
GB201709402D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating t-pll
GB201709403D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating sarcoma
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019002842A1 (en) 2017-06-26 2019-01-03 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF
KR20240153614A (ko) 2017-07-28 2024-10-23 다케다 야쿠힌 고교 가부시키가이샤 Tyk2 억제제 및 이의 용도
WO2019025811A1 (en) 2017-08-04 2019-02-07 Bicycletx Limited SPECIFIC BICYCLIC PEPTIDE LIGANDS OF CD137
KR101977970B1 (ko) 2017-08-04 2019-05-14 중원대학교 산학협력단 신규한 벤즈아미드계 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암 예방 또는 치료용 약학 조성물
EP3668550A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
US20200291096A1 (en) 2017-08-14 2020-09-17 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2019046491A1 (en) 2017-08-29 2019-03-07 Ariya Therapeutics, Inc. LIPIDIC PRODRUGS DIRECTING TO THE LYMPHATIC SYSTEM
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
EP3461488A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dbait molecule and a hdac inhibitor for treating cancer
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
WO2019083960A1 (en) 2017-10-24 2019-05-02 Oncopep, Inc. PEPTIDE VACCINES AND HDAC INHIBITORS FOR THE TREATMENT OF MULTIPLE MYELOMA
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
CN111465411A (zh) 2017-10-24 2020-07-28 恩科佩普股份有限公司 用于治疗乳腺癌的肽疫苗和派姆单抗
JP7254076B2 (ja) 2017-11-19 2023-04-07 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ヘテロアリール化合物及び使用方法
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
EP3730483B1 (en) 2017-12-21 2023-08-30 Hefei Institutes of Physical Science, Chinese Academy of Sciences Class of pyrimidine derivative kinase inhibitors
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
US10988477B2 (en) 2018-01-29 2021-04-27 Merck Patent Gmbh GCN2 inhibitors and uses thereof
AU2019212969B2 (en) 2018-01-29 2025-01-23 Merck Patent Gmbh GCN2 inhibitors and uses thereof
EP4410802A3 (en) 2018-02-12 2024-10-30 Inimmune Corporation Toll-like receptor ligands
AU2019224659A1 (en) 2018-02-23 2020-10-15 Bicycletx Limited Multimeric bicyclic peptide ligands
SG11202008067QA (en) 2018-02-27 2020-09-29 Artax Biopharma Inc Chromene derivatives as inhibitors of tcr-nck interaction
WO2019183523A1 (en) 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
EP3774772A1 (en) 2018-04-13 2021-02-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
PT4043460T (pt) 2018-04-24 2024-09-10 Merck Patent Gmbh Compostos antiproliferação e utilizações dos mesmos
AU2019257651B2 (en) 2018-04-24 2023-05-25 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
WO2019238886A1 (en) 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting usp14
CA3103205A1 (en) 2018-06-13 2019-12-19 Amphista Therapeutics Ltd Bifunctional molecules for targeting uchl5
US11925690B2 (en) 2018-06-13 2024-03-12 Amphista Therapeutics Limited Bifunctional molecules for targeting Rpn11
DK3813946T3 (da) 2018-06-15 2024-08-19 Janssen Pharmaceutica Nv Rapamycin-analoger og anvendelser deraf
IL279489B1 (en) 2018-06-22 2025-06-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate comprising the peptide ligand and a pharmaceutical composition comprising the drug conjugate
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
CN108752255A (zh) * 2018-07-19 2018-11-06 重庆医科大学 一种帕比司他及其关键中间体的制备方法
US12220423B2 (en) 2018-07-24 2025-02-11 Hygia Pharmaceuticals, Llc Compounds, derivatives, and analogs for cancer
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
CA3115088A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN112955459A (zh) 2018-10-23 2021-06-11 拜斯科技术开发有限公司 双环肽配体和其用途
CN109574936B (zh) * 2018-11-23 2022-02-22 沈阳药科大学 一种具有hdac6抑制活性的异羟肟酸类化合物及其应用
BR112021010484A2 (pt) 2018-11-30 2021-08-24 Kymera Therapeutics, Inc. Degradadores de irak e usos dos mesmos
CA3120866A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
EP3897626B1 (en) 2018-12-18 2025-09-10 Mundipharma International Corporation Limited Tinostamustine for treating multiple myeloma
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN DEGRADATION
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
JP7699052B2 (ja) 2019-01-23 2025-06-26 武田薬品工業株式会社 Tyk2阻害剤およびその使用
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
CA3135569A1 (en) 2019-04-02 2020-10-08 Bicycletx Limited Bicycle toxin conjugates and uses thereof
MX2021012216A (es) 2019-04-05 2022-01-24 Kymera Therapeutics Inc Degradadores de transductores de señal y activadores de transcripción (stat) y usos de los mismos.
SG11202113154YA (en) 2019-05-31 2021-12-30 Ikena Oncology Inc Tead inhibitors and uses thereof
GB201913122D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913124D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913123D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
AU2020345962A1 (en) 2019-09-11 2022-03-31 Vincere Biosciences, Inc. USP30 inhibitors and uses thereof
GB201913121D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
PH12022550605A1 (en) 2019-09-13 2023-09-25 Nimbus Saturn Inc Hpk1 antagonists and uses thereof
EP3798250A1 (en) 2019-09-25 2021-03-31 University College Dublin Hyperbranched cationic polymers useful as nucleic acid delivery vectors for transfecting
WO2021058492A1 (en) 2019-09-25 2021-04-01 University College Dublin Nanoparticle compositions for gene therapy
WO2021092174A1 (en) * 2019-11-06 2021-05-14 Dana-Farber Cancer Institute, Inc. Selective histone deacetylase (hdac) degraders and methods of use thereof
TW202134234A (zh) 2019-12-05 2021-09-16 美商奈維特製藥公司 雷帕黴素類似物及其用途
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADATION AGENTS AND THEIR USES
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR20220151160A (ko) 2019-12-23 2022-11-14 카이메라 쎄라퓨틱스 인코포레이티드 Smarca 분해제 및 이의 용도
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3166908A1 (en) 2020-02-05 2021-08-12 Daniel Kenneth BONNER Lipid prodrugs of neurosteroids
IT202000004075A1 (it) 2020-02-27 2021-08-27 Flamma Spa Processo per la preparazione di panobinostat
CA3170411A1 (en) 2020-03-03 2021-09-10 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
CN115515585A (zh) 2020-03-10 2022-12-23 X4 制药有限公司 用于治疗中性粒细胞减少症的方法
WO2021185844A1 (en) 2020-03-16 2021-09-23 Pvac Medical Technologies Ltd Use of substance and pharmaceutical composition thereof, and medical treatments or uses thereof
WO2021233534A1 (en) 2020-05-20 2021-11-25 Pvac Medical Technologies Ltd Use of substance and pharmaceutical composition thereof, and medical treatments or uses thereof
CN115776887A (zh) 2020-03-19 2023-03-10 凯麦拉医疗公司 Mdm2降解剂和其用途
US12359208B2 (en) 2020-04-15 2025-07-15 California Institute Of Technology Thermal control of T-cell immunotherapy through molecular and physical actuation
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
WO2022029220A1 (en) 2020-08-05 2022-02-10 Ellipses Pharma Ltd Treatment of cancer using a cyclodextrin-containing polymer-topoisomerase inhibitor conjugate and a parp inhibitor
AU2021327130A1 (en) 2020-08-17 2023-03-02 Bicycletx Limited Bicycle conjugates specific for Nectin-4 and uses thereof
WO2022047259A1 (en) 2020-08-28 2022-03-03 California Institute Of Technology Synthetic mammalian signaling circuits for robust cell population control
TW202233612A (zh) 2020-10-23 2022-09-01 美商林伯士科羅索公司 Ctps1抑制劑及其用途
KR20230131189A (ko) 2020-12-02 2023-09-12 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
AU2021400059A1 (en) 2020-12-18 2023-07-06 Amphista Therapeutics Limited Novel bifunctional molecules for targeted protein degradation
GB202020359D0 (en) 2020-12-22 2021-02-03 Midatech Pharma Wales Ltd Pharmaceutical compositions and use thereof in combination therapy for brain cancer
CA3202360A1 (en) 2020-12-30 2022-07-07 Nello Mainolfi Irak degraders and uses thereof
EP4288427A1 (en) 2021-02-02 2023-12-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
MX2023009059A (es) 2021-02-02 2023-09-15 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
CA3207049A1 (en) 2021-02-15 2022-08-18 Jared Gollob Irak4 degraders and uses thereof
MX2023011933A (es) 2021-04-09 2024-01-05 Nimbus Clio Inc Moduladores del linfoma de linaje b de casitas de ligasa e3 b (cbl-b) y usos de estos.
WO2022221866A1 (en) 2021-04-16 2022-10-20 Ikena Oncology, Inc. Mek inhibitors and uses thereof
JP2024519215A (ja) 2021-05-07 2024-05-09 カイメラ セラピューティクス, インコーポレイテッド Cdk2分解剤およびそれらの使用
US12234231B2 (en) 2021-08-25 2025-02-25 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
JP2024532276A (ja) 2021-08-25 2024-09-05 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
WO2023041805A1 (en) 2021-09-20 2023-03-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for improving the efficacy of hdac inhibitor therapy and predicting the response to treatment with hdac inhibitor
GB2611043A (en) 2021-09-22 2023-03-29 Univ Dublin City A cis-platinum(II)-oligomer hybrid
CA3236265A1 (en) 2021-10-29 2023-05-04 William Leong Irak4 degraders and synthesis thereof
CN118632688A (zh) 2021-11-19 2024-09-10 布朗卡布努斯有限公司 一种包含包装在药物递送载体中的治疗活性剂的组合物
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
IL314437A (en) 2022-01-31 2024-09-01 Kymera Therapeutics Inc IRAK joints and their uses
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023194441A1 (en) 2022-04-05 2023-10-12 Istituto Nazionale Tumori Irccs - Fondazione G. Pascale Combination of hdac inhibitors and statins for use in the treatment of pancreatic cancer
GB2617409B (en) 2022-04-27 2024-06-26 Cancertain Ltd Method for predicting responsiveness to therapy
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
JP2025519119A (ja) 2022-05-25 2025-06-24 イケナ オンコロジー, インコーポレイテッド Mek阻害剤及びその使用
CN119384408A (zh) 2022-06-16 2025-01-28 安菲斯塔治疗有限责任公司 用于靶向蛋白降解的双功能分子
IL318710A (en) 2022-08-02 2025-03-01 Univ Hokkaido Nat Univ Corp Methods for improving cellular therapy with organelle complexes
EP4565569A1 (en) 2022-08-02 2025-06-11 Liminal Biosciences Limited Aryl-triazolyl and related gpr84 antagonists and uses thereof
CN120019047A (zh) 2022-08-02 2025-05-16 里米诺生物科学有限公司 杂芳基甲酰胺和相关gpr84拮抗剂及其用途
AU2023317742A1 (en) 2022-08-02 2025-03-20 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
EP4577210A1 (en) 2022-08-26 2025-07-02 Biodexa Ltd. Combination therapy for brain cancer
AR131141A1 (es) 2022-11-22 2025-02-19 Pic Therapeutics Inc Inhibidores de eif4e y usos de los mismos
WO2024184266A1 (en) 2023-03-03 2024-09-12 Ionctura Sa Combination of roginolisib and hdac inhibitor in the treatment of haematological malignancy
AU2024312190A1 (en) 2023-06-23 2025-07-03 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2025026925A1 (en) 2023-07-28 2025-02-06 Ospedale San Raffaele S.R.L. Gtf2i inhibitors and uses thereof
CN119490449A (zh) * 2023-08-16 2025-02-21 沈阳药科大学 含n-苄基-2-(5-苯基吡啶-2-基)乙酰胺的异羟肟酸类化合物及制备方法和应用
WO2025062372A1 (en) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
WO2025078542A1 (en) 2023-10-11 2025-04-17 Technological University Dublin Coumarin-metal complexes and uses thereof
CN118027033A (zh) * 2024-01-26 2024-05-14 四川大学 一种hdac6抑制剂及其制备方法和在抗炎和溃疡性结肠炎中的用途

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5700811A (en) * 1991-10-04 1997-12-23 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and method of use thereof
EP0570594B1 (en) 1991-12-10 1997-07-30 Shionogi & Co., Ltd. Hydroxamic acid derivative based on aromatic sulfonamide
GB9215665D0 (en) * 1992-07-23 1992-09-09 British Bio Technology Compounds
US5569668A (en) * 1995-03-29 1996-10-29 Webster; John M. Indole derivatives with antibacterial and antimycotic properties
US5722242A (en) * 1995-12-15 1998-03-03 Borealis Technical Limited Method and apparatus for improved vacuum diode heat pump
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
JPH10182583A (ja) 1996-12-25 1998-07-07 Mitsui Chem Inc 新規ヒドロキサム酸誘導体
AUPO721997A0 (en) * 1997-06-06 1997-07-03 Queensland Institute Of Medical Research, The Anticancer compounds
US6127392A (en) 1997-08-05 2000-10-03 American Home Products Corporation Anthranilic acid analogs
EP1003712A1 (en) 1997-08-05 2000-05-31 American Home Products Corporation Anthranilic acid analogs
DE69920247T2 (de) 1998-10-19 2005-09-29 Methylgene, Inc., Saint-Laurent Veränderung der dns methyltransferase durch kombinationstherapie
US6110922A (en) 1998-12-29 2000-08-29 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
UA74781C2 (en) 1999-04-02 2006-02-15 Abbott Lab Antiinflammatory and immumosuppressive compounds inhibiting cell adhesion
CA2383999A1 (en) 1999-09-08 2001-03-15 Sloan-Kettering Institute For Cancer Research Novel class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
GB9922173D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
KR101026205B1 (ko) * 1999-11-23 2011-03-31 메틸진 인코포레이티드 히스톤 디아세틸라제의 억제제
JP2003516144A (ja) 1999-12-08 2003-05-13 アクシス・ファーマシューティカルズ・インコーポレイテッド ヒストン脱アセチル化酵素−8のタンパク質、核酸およびその使用方法
TW427572U (en) * 1999-12-17 2001-03-21 Hon Hai Prec Ind Co Ltd Electrical connector
WO2001070675A2 (en) 2000-03-24 2001-09-27 Methylgene, Inc. Inhibitors of histone deacetylase
EP1438404A2 (en) 2000-03-24 2004-07-21 Methylgene, Inc. Inhibition of specific histone deacetylase isoforms
EP1314721A1 (en) 2000-08-31 2003-05-28 Wakunaga Pharmaceutical Co., Ltd. Novel propenohydroxamic acid derivatives
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
KR20030067675A (ko) 2000-10-05 2003-08-14 후지사와 야꾸힝 고교 가부시키가이샤 벤자미드 화합물
SE0101386D0 (sv) 2001-04-20 2001-04-20 Astrazeneca Ab New compounds
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
HUP0500573A2 (hu) 2001-08-11 2005-11-28 Bristol-Myers Squibb Pharma Company Trifenil-etilén származékok, mint szelektív ösztrogén receptor modulátorok és ezeket tartalmazó gyógyszerkészítmények
US6706686B2 (en) * 2001-09-27 2004-03-16 The Regents Of The University Of Colorado Inhibition of histone deacetylase as a treatment for cardiac hypertrophy
DE10152764A1 (de) * 2001-10-29 2003-05-08 Linde Ag Ventil für kryogene Medien

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