JP4399265B2 - 3,4−ジアリールピラゾール、および癌の治療におけるそれらの使用 - Google Patents

3,4−ジアリールピラゾール、および癌の治療におけるそれらの使用 Download PDF

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JP4399265B2
JP4399265B2 JP2003556391A JP2003556391A JP4399265B2 JP 4399265 B2 JP4399265 B2 JP 4399265B2 JP 2003556391 A JP2003556391 A JP 2003556391A JP 2003556391 A JP2003556391 A JP 2003556391A JP 4399265 B2 JP4399265 B2 JP 4399265B2
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phenyl
arh
compound
group
mmol
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JP2003556391A
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Japanese (ja)
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JP2005517675A (ja
JP2005517675A5 (enExample
Inventor
ドライスデール,マーティン,ジェームス
ディモック,ブライアン,ウィリアム
バリル−アロンソ,グザヴィエ
ワークマン,ポール
パール,ローレンス,ハリス
プロドロモウ,クリソストモス
マクドナルド,エドワード
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Institute of Cancer Research Royal Cancer Hospital
Vernalis Cambridge Ltd
Cancer Research Technology Ltd
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Institute of Cancer Research Royal Cancer Hospital
Vernalis Cambridge Ltd
Cancer Research Technology Ltd
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Priority claimed from GB0130733A external-priority patent/GB0130733D0/en
Priority claimed from GB0225688A external-priority patent/GB0225688D0/en
Application filed by Institute of Cancer Research Royal Cancer Hospital, Vernalis Cambridge Ltd, Cancer Research Technology Ltd filed Critical Institute of Cancer Research Royal Cancer Hospital
Publication of JP2005517675A publication Critical patent/JP2005517675A/ja
Publication of JP2005517675A5 publication Critical patent/JP2005517675A5/ja
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • 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
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    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
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    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/16Halogen atoms or nitro radicals
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    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
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    • 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
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    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
JP2003556391A 2001-12-21 2002-12-19 3,4−ジアリールピラゾール、および癌の治療におけるそれらの使用 Expired - Fee Related JP4399265B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0130733A GB0130733D0 (en) 2001-12-21 2001-12-21 Therapeutic compounds and their use in therapy
GB0225688A GB0225688D0 (en) 2002-11-04 2002-11-04 Therapeutic compounds and their use in therapy
PCT/GB2002/005778 WO2003055860A1 (en) 2001-12-21 2002-12-19 3,4-diarylpyrazoles and their use in the therapy of cancer

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JP2005517675A JP2005517675A (ja) 2005-06-16
JP2005517675A5 JP2005517675A5 (enExample) 2006-02-09
JP4399265B2 true JP4399265B2 (ja) 2010-01-13

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JP2003556391A Expired - Fee Related JP4399265B2 (ja) 2001-12-21 2002-12-19 3,4−ジアリールピラゾール、および癌の治療におけるそれらの使用

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US (1) US7247734B2 (enExample)
EP (1) EP1456180B1 (enExample)
JP (1) JP4399265B2 (enExample)
AT (1) ATE374753T1 (enExample)
AU (1) AU2002356301A1 (enExample)
DE (1) DE60222804T2 (enExample)
WO (1) WO2003055860A1 (enExample)

Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7875728B2 (en) 2001-11-30 2011-01-25 Valocor Therapeutics, Inc. Hydrazonopyrazole derivatives and their use as therapeutics
US6770597B2 (en) * 2002-07-17 2004-08-03 Ishihara Sangyo Kaisha, Ltd. Benzohydrazide derivatives as herbicides and desiccant compositions containing them
EP1542997B1 (en) 2002-07-24 2012-02-29 Dermira (Canada), Inc. Pyrazolylbenzothiazole derivatives and their use as therapeutic agents
DE60304718T2 (de) 2002-08-06 2007-04-26 Astrazeneca Ab Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität
WO2004014886A1 (en) * 2002-08-07 2004-02-19 University Of Mississippi Antigiardial agents and use thereof
GB0228417D0 (en) 2002-12-05 2003-01-08 Cancer Rec Tech Ltd Pyrazole compounds
GB0229618D0 (en) 2002-12-19 2003-01-22 Cancer Rec Tech Ltd Pyrazole compounds
SI1611112T1 (sl) * 2003-02-11 2012-12-31 Vernalis (R&D) Limited Izoksazolne spojine kot inhibitorji vroäśinskih ĺ ok proteinov
CA2520804A1 (en) 2003-04-03 2004-10-28 Merck & Co., Inc. Biaryl substituted pyrazoles as sodium channel blockers
GB0309637D0 (en) * 2003-04-28 2003-06-04 Cancer Rec Tech Ltd Pyrazole compounds
GB0313915D0 (en) * 2003-06-16 2003-07-23 Smithkline Beecham Corp Compounds
US7538241B2 (en) 2003-12-26 2009-05-26 Kyowa Hakko Kogyo Co., Ltd. Hsp90 family protein inhibitors
EP1706400A1 (en) * 2004-01-09 2006-10-04 Novartis AG Phenyl- 4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl -amine derivatives as igf-ir inhibitors
GB0402518D0 (en) 2004-02-05 2004-03-10 Astrazeneca Ab Therapeutic agents
WO2005110963A1 (en) * 2004-05-19 2005-11-24 Cellzome Ag (biphenyl-3-yl)-carboxylic acids and derivatives thereof and their use in therapy
EP1604970A1 (en) * 2004-05-19 2005-12-14 Cellzome Ag 2-(Biphenyl-3-yl)-carboxylic acids of gamma-secretase-modulating activity
DE102004039280A1 (de) * 2004-08-13 2006-02-23 Merck Patent Gmbh 1,5-Diphenyl-pyrazole
BRPI0515573A (pt) 2004-09-22 2008-07-29 Nippon Kayaku Kk copolìmero por blocos, preparação de micela e agente anticáncer contendo a mesma como o ingrediente ativo
DE102004049078A1 (de) * 2004-10-08 2006-04-13 Merck Patent Gmbh Phenylpyrazole
EP2298748B1 (en) 2004-11-18 2016-07-20 Synta Pharmaceuticals Corp. Triazole compounds that modulate HSP90 activity
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
DE102005007304A1 (de) 2005-02-17 2006-08-24 Merck Patent Gmbh Triazolderivate
EA011617B1 (ru) * 2005-02-21 2009-04-28 Киова Хакко Кирин Ко., Лтд. Противоопухолевое средство
DE102005009440A1 (de) 2005-03-02 2006-09-07 Merck Patent Gmbh Thienopyridinderivate
JP5044730B2 (ja) 2005-03-09 2012-10-10 日本化薬株式会社 新規なhsp90阻害剤
US20080306054A1 (en) 2005-04-13 2008-12-11 Astex Therapeutics Limited Pharmaceutical Compounds
JP2008540586A (ja) * 2005-05-18 2008-11-20 フォルシュングスフェアブント ベルリン エー ファウ Akap−pka相互作用の非ペプチド阻害剤
FR2885904B1 (fr) * 2005-05-19 2007-07-06 Aventis Pharma Sa Nouveaux derives du fluorene, compositions les contenant et utilisation
US7473784B2 (en) * 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
US7608635B2 (en) 2005-08-12 2009-10-27 Synta Pharmaceuticals Corp. Pyrazole compounds that modulate HSP90 activity
EP1928846B1 (en) 2005-08-18 2014-06-04 Synta Pharmaceuticals Corp. Triazole compounds that modulate hsp90 activity
NL2000351C2 (nl) 2005-12-22 2007-09-11 Pfizer Prod Inc Estrogeen-modulatoren.
US20070253896A1 (en) * 2006-02-07 2007-11-01 Conforma Therapeutics Corporation 7,9-Dihydro-Purin-8-One and Related Analogs as HSP90-Inhibitors
US7754725B2 (en) 2006-03-01 2010-07-13 Astex Therapeutics Ltd. Dihydroxyphenyl isoindolymethanones
CA2643066A1 (en) * 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
JP5249016B2 (ja) 2006-03-28 2013-07-31 日本化薬株式会社 タキサン類の高分子結合体
DE102006023336A1 (de) * 2006-05-18 2007-11-22 Merck Patent Gmbh 1,5-Diphenyl-pyrazole II
CA2652656A1 (en) 2006-05-18 2007-11-29 Nippon Kayaku Kabushiki Kaisha High-molecular weight conjugate of podophyllotoxins
CA2653329C (en) 2006-05-25 2018-01-16 Synta Pharmaceuticals Corp. Triazole compounds that modulate hsp90 activity
AU2007267803B2 (en) * 2006-05-25 2011-08-25 Synta Pharmaceuticals Corp. Method for treating non-Hodgkin's lymphoma
EP2034995A2 (en) * 2006-05-25 2009-03-18 Synta Pharmaceuticals Corporation Method for treating proliferative disorders associated with protooncogene products
AR061185A1 (es) 2006-05-26 2008-08-13 Chugai Pharmaceutical Co Ltd Compuestos heterociclicos como inhibidores de hsp90. composiciones farmaceuticas.
WO2008041610A1 (fr) 2006-10-03 2008-04-10 Nippon Kayaku Kabushiki Kaisha Mélange d'un dérivé de résorcinol avec un polymère
JP5721949B2 (ja) 2006-10-12 2015-05-20 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited 複合薬剤
JP5518478B2 (ja) 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
WO2008044027A2 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical compounds having hsp90 inhibitory or modulating activity
WO2008044045A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
EP2080779B1 (en) 2006-11-06 2016-05-18 Nippon Kayaku Kabushiki Kaisha Polymeric derivative of nucleic acid metabolic antagonist
EP2090607B1 (en) 2006-11-08 2015-05-20 Nippon Kayaku Kabushiki Kaisha Polymeric derivative of nucleic acid metabolic antagonist
DE102007002715A1 (de) 2007-01-18 2008-07-24 Merck Patent Gmbh Triazolderivat
CL2008000629A1 (es) 2007-03-01 2008-08-29 Chugai Pharmaceutical Co Ltd Compuestos macrociclicos derivados de 6-aril-4-mercapto-[1.3.5]triazina/[1.3]pirimidin-2-amina; composicion farmaceutica, utiles en el tratamiento del cancer.
CA2680161A1 (en) 2007-03-05 2008-09-12 Kyowa Hakko Kirin Co., Ltd. Pharmaceutical composition
US8993608B2 (en) 2007-03-12 2015-03-31 Synta Pharmaceuticals Corp. Method for inhibiting topoisomerase II
KR20100038119A (ko) * 2007-08-01 2010-04-12 화이자 인코포레이티드 피라졸 화합물 및 raf 억제제로서 이의 용도
WO2009026658A1 (en) * 2007-08-29 2009-03-05 The University Of Sydney Ppar agonists
CN101854955B (zh) * 2007-09-10 2012-07-18 马萨诸塞大学 靶向线粒体的抗肿瘤剂
USRE46190E1 (en) 2007-09-28 2016-11-01 Nippon Kayaku Kabushiki Kaisha High-molecular weight conjugate of steroids
JP5687899B2 (ja) 2008-03-18 2015-03-25 日本化薬株式会社 生理活性物質の高分子結合体
GB0806527D0 (en) 2008-04-11 2008-05-14 Astex Therapeutics Ltd Pharmaceutical compounds
WO2009136572A1 (ja) 2008-05-08 2009-11-12 日本化薬株式会社 葉酸若しくは葉酸誘導体の高分子結合体
WO2010001989A1 (ja) * 2008-07-03 2010-01-07 協和発酵キリン株式会社 癌幹細胞及び/または癌前駆細胞の減少剤並びに癌の再発及び/または転移の予防剤
PL2324008T3 (pl) 2008-07-24 2012-09-28 Nerviano Medical Sciences Srl 3,4-diarylopirazole jako inhibitory kinazy białkowej
EP2151434A1 (en) 2008-08-05 2010-02-10 Institut Pasteur Alkoxypyrazoles and the process for their preparation
EP2151433A1 (en) 2008-08-05 2010-02-10 Institut Pasteur Alkoxypyrazoles and the process for their preparation
BRPI1008949B1 (pt) * 2009-03-11 2018-07-10 Bayer Intellectual Property Gmbh Cetoenóis haloalquilmetilenóxi-fenil-substituídos e seu uso, composição, seu uso e seu método de produção, métodos para combate de pestes animais e/ou crescimento de plantas indesejadas
WO2010121963A1 (en) 2009-04-21 2010-10-28 Nerviano Medical Sciences S.R.L. Resorcinol derivatives as hsp90 inhibitors
EP2431403B1 (en) 2009-05-15 2016-09-28 Nipponkayaku Kabushikikaisha Polymer conjugate of bioactive substance having hydroxy group
NZ598262A (en) * 2009-08-17 2014-05-30 Sloan Kettering Inst Cancer Heat shock protein binding compounds, compositions, and methods for making and using same
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
WO2011040421A1 (ja) 2009-09-29 2011-04-07 武田薬品工業株式会社 スクリーニング方法
AR078538A1 (es) * 2009-10-07 2011-11-16 Karobio Ab Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos
CN104958294A (zh) * 2010-01-27 2015-10-07 内尔维安诺医学科学有限公司 作为蛋白激酶抑制剂的3,4-二芳基吡唑的亚磺酰氨基衍生物
WO2011102660A2 (en) * 2010-02-17 2011-08-25 Ildong Pharm Co., Ltd. A novel 5-membered heterocycle derivatives and manufacturing process thereof
EP2560640A1 (en) 2010-04-19 2013-02-27 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor
JP5938038B2 (ja) 2010-08-03 2016-06-22 ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用
WO2012067138A1 (ja) 2010-11-17 2012-05-24 日本化薬株式会社 新規なシチジン系代謝拮抗剤の高分子誘導体
GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
ES2635117T3 (es) 2011-09-11 2017-10-02 Nippon Kayaku Kabushiki Kaisha Método para la fabricación de un copolímero de bloques
JP2014534228A (ja) 2011-11-02 2014-12-18 シンタ ファーマシューティカルズ コーポレーション 白金含有剤とhsp90阻害剤の組合せ療法
WO2013067162A1 (en) 2011-11-02 2013-05-10 Synta Pharmaceuticals Corp. Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors
US11007194B2 (en) 2011-11-11 2021-05-18 Array Biopharma Inc. Method of treating a proliferative disease
EP2780010A1 (en) 2011-11-14 2014-09-24 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with braf inhibitors
WO2013078264A1 (en) 2011-11-23 2013-05-30 Novartis Ag Pharmaceutical formulations
CN103183640B (zh) * 2011-12-30 2016-04-27 沈阳药科大学 二芳基吡唑类化合物及其制备方法与用途
US20140079636A1 (en) * 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
DE102013012685A1 (de) * 2013-07-31 2015-02-05 Johann-Wolfgang-Goethe Universität Frankfurt am Main Arylierte Pyrazolderivate und deren Verwendung als Fluoreszenzfarbstoffe
CN104974091B (zh) * 2014-04-10 2018-01-02 沈阳药科大学 3‑甲基‑1,5‑二芳基吡唑类化合物及其制备方法和用途
EA201692155A1 (ru) 2014-05-13 2017-04-28 Мемориал Слоун-Кеттеринг Кэнсэ Сентр МОДУЛЯТОРЫ Hsp70 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
FR3022244B1 (fr) * 2014-06-17 2016-07-01 Centre Nat De La Rech Scient (Cnrs) Utilisation d'un nouveau compose 3-aryl-4-catechol-pyrrole-n-propanol et ses derives pour le traitement du cancer et des pathologies associees a une angiogenese excessive
CN107108591B (zh) * 2015-01-22 2020-05-05 正大天晴药业集团股份有限公司 作为hsp90抑制剂的间苯二酚类衍生物
GB201706806D0 (en) 2017-04-28 2017-06-14 Sentinel Oncology Ltd Pharmaceutical compounds
JP2020524154A (ja) 2017-06-20 2020-08-13 マドリガル ファーマシューティカルズ インコーポレイテッドMadrigal Pharmaceuticals,Inc. 標的治療薬
JP2020524156A (ja) 2017-06-20 2020-08-13 マドリガル ファーマシューティカルズ インコーポレイテッドMadrigal Pharmaceuticals,Inc. 標的治療薬を含む併用療法
WO2019236765A1 (en) * 2018-06-05 2019-12-12 Flagship Pioneering Innovations V, Inc. Acylated catechin polyphenols and methods of their use for the treatment of cancer
CN109134204B (zh) * 2018-11-16 2022-03-08 棓诺(苏州)新材料有限公司 中间体2-溴-4-氟-5-氯苯酚的合成法
CN110283080A (zh) * 2019-07-05 2019-09-27 山西大学 一种含氟的二苯甲酮衍生物及其制备方法和应用
EP3827825A1 (en) * 2019-11-26 2021-06-02 Wageningen Universiteit Use of 3, 4-diarylpyrazoles as antibacterial agents
KR20260058912A (ko) * 2020-09-14 2026-04-30 젠자임 코포레이션 겸상 적혈구 질환 치료를 위한 비스-포스포글리세레이트 뮤타제 조절제로서의 화합물
CA3215697A1 (en) * 2021-04-28 2022-11-03 Cornell University Soluble adenylyl cyclase (sac) inhibitors and uses thereof
WO2023004280A1 (en) * 2021-07-19 2023-01-26 The Board Of Trustees Of The Leland Stanford Junior University Selective pyrazole lrrk2 inhibitors and methods for use thereof
CN120623147B (zh) * 2025-08-01 2025-12-16 广东省科学院动物研究所 吡唑喹啉醚类化合物及其在制备神经保护药物中的应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559137A (en) 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5486534A (en) * 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
AR037061A1 (es) 1997-05-22 2004-10-20 Searle & Co Compuesto derivado de pirazol sustituido, procesos para preparar dicho compuesto, composicion farmaceutica que lo contiene y su uso en la preparacion de medicamentos
ATE355279T1 (de) * 1998-08-07 2006-03-15 Novartis Vaccines & Diagnostic Pyrazole als modulatoren des östrogenrezeptors
WO2000019994A1 (en) 1998-10-02 2000-04-13 Board Of Trustees Of The University Of Illinois Estrogen receptor ligands
GB0102687D0 (en) 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
US20040087623A1 (en) * 2001-02-02 2004-05-06 Gellibert Francoise Jeanne Pyrazole derivatives against tgf overexpression
JP2005022972A (ja) 2001-05-16 2005-01-27 Teikoku Hormone Mfg Co Ltd 4−(4−ピリダジニル)ピラゾール誘導体

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