JP5967827B2 - Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 - Google Patents

Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 Download PDF

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JP5967827B2
JP5967827B2 JP2012543295A JP2012543295A JP5967827B2 JP 5967827 B2 JP5967827 B2 JP 5967827B2 JP 2012543295 A JP2012543295 A JP 2012543295A JP 2012543295 A JP2012543295 A JP 2012543295A JP 5967827 B2 JP5967827 B2 JP 5967827B2
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JP2013513613A (ja
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フランセスコ ジー． サリトゥロ，
フランセスコ ジー． サリトゥロ，
ジェフリー オー． サウンダーズ，
ジェフリー オー． サウンダーズ，
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アジオス ファーマシューティカルズ， インコーポレイテッド
アジオス ファーマシューティカルズ， インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/16—Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
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    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
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    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • General Health & Medical Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Indole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
JP2012543295A 2009-12-09 2010-12-09 Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物 Expired - Fee Related JP5967827B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US28512209P 2009-12-09 2009-12-09
US61/285,122 2009-12-09
US31353210P 2010-03-12 2010-03-12
US61/313,532 2010-03-12
PCT/US2010/059778 WO2011072174A1 (en) 2009-12-09 2010-12-09 Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation

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JP2015113075A Division JP2015193633A (ja) 2009-12-09 2015-06-03 Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物

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JP2013513613A JP2013513613A (ja) 2013-04-22
JP2013513613A5 JP2013513613A5 (enExample) 2014-01-30
JP5967827B2 true JP5967827B2 (ja) 2016-08-10

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JP2015113075A Withdrawn JP2015193633A (ja) 2009-12-09 2015-06-03 Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物

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US (2) US20130035329A1 (enExample)
EP (1) EP2509600B1 (enExample)
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ES (1) ES2642109T3 (enExample)
WO (1) WO2011072174A1 (enExample)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6067226B2 (ja) 2009-03-13 2017-01-25 アジオス ファーマシューティカルズ， インコーポレイテッド 細胞増殖関連疾患のための方法および組成物
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
CA2766873C (en) 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
AR077292A1 (es) 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas
WO2011050211A2 (en) 2009-10-21 2011-04-28 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
ES2594402T3 (es) 2009-10-21 2016-12-20 Agios Pharmaceuticals, Inc. Métodos y composiciones para trastornos relacionados con la proliferación celular
EP2651898B1 (en) 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
US9328077B2 (en) 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
HUE065700T2 (hu) 2011-05-03 2024-06-28 Agios Pharmaceuticals Inc Piruvát-kináz aktivátorok terápiában történõ alkalmazásra
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827073A (zh) * 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
JP6026544B2 (ja) 2011-09-27 2016-11-16 ノバルティス アーゲー 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類
CA2860623A1 (en) 2012-01-06 2013-07-11 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9474779B2 (en) * 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
JP6385352B2 (ja) 2012-10-15 2018-09-05 アジオス ファーマシューティカルズ， インコーポレイテッド 治療化合物および組成物
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
GEP201706699B (en) 2013-03-14 2017-07-10 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
EP3004396B1 (en) 2013-06-06 2019-10-16 The General Hospital Corporation Compositions for the treatment of cancer
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
SG11201600058XA (en) 2013-07-11 2016-02-26 Agios Pharmaceuticals Inc N,6-bis(aryl or heteroaryl)-1,3,5-triazine-2,4-diamine compounds as idh2 mutants inhibitors for the treatment of cancer
WO2015003360A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
AU2014287121B2 (en) 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
MA39092B1 (fr) 2013-12-05 2018-09-28 Pfizer Pyrrolo[2,3-d]pyrimidinyle, pyrrolo[2,3-b]pyrazinyle et pyrollo[2,3-d]pyridinyle acrylamides
WO2015121210A1 (en) 2014-02-11 2015-08-20 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
US9951027B2 (en) 2014-02-11 2018-04-24 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as MIDH1 inhibitors
CA2942072C (en) 2014-03-14 2022-07-26 Agios Pharmaceuticals, Inc. Pharmaceutical compositions and use of (s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-( 4-cyanopyridin-2-yl)-n-( 5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
US9926286B2 (en) * 2014-05-09 2018-03-27 Shanghai Syncores Technologies Inc. Ltd. Vortioxetine intermediate and synthesis process thereof
HUE062424T2 (hu) 2014-09-19 2023-11-28 Forma Therapeutics Inc Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok
US10005734B2 (en) 2014-09-19 2018-06-26 Forma Therapeutics, Inc. Pyridin-2(1H)-one quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
JP6751081B2 (ja) * 2014-09-19 2020-09-02 フォーマ セラピューティクス，インコーポレイテッド 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのピリジニルキノリノン誘導体
EP3194383B1 (en) 2014-09-19 2019-11-06 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
EP3237385B1 (en) 2014-12-22 2021-11-24 The United States of America, as represented by The Secretary, Department of Health and Human Services Mutant idh1 inhibitors useful for treating cancer
WO2016171756A1 (en) * 2015-04-21 2016-10-27 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
US10294206B2 (en) 2015-04-21 2019-05-21 Forma Tm2, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
PL3307271T3 (pl) 2015-06-11 2024-02-05 Agios Pharmaceuticals, Inc. Sposoby stosowania aktywatorów kinazy pirogronianowej
US10765675B2 (en) 2015-08-24 2020-09-08 The Methodist Hospital Compositions and methods for treating Ewing family tumors
RS62829B1 (sr) 2015-10-15 2022-02-28 Servier Lab Kombinovana terapija za lečenje maligniteta
IL258684B2 (en) 2015-10-15 2023-04-01 Agios Pharmaceuticals Inc Combination therapy including an isocitrate dehydrogenase (1idh) inhibitor for use in the treatment of acute myelogenous leukemia (aml) characterized by the presence of a mutant allele of 1idh
MX2018008169A (es) * 2015-12-30 2019-02-20 Agios Pharmaceuticals Inc Tratamiento de tumores que incorpora isocitrato deshidrogenasa mutante.
WO2017153952A1 (en) * 2016-03-10 2017-09-14 Glaxosmithkline Intellectual Property Development Limited 5-sulfamoyl-2-hydroxybenzamide derivatives
WO2017162156A1 (zh) * 2016-03-22 2017-09-28 正大天晴药业集团股份有限公司 丙啶磺酰胺类化合物及其使用方法
MX2019012640A (es) 2017-04-24 2020-12-11 Aurigene Discovery Tech Ltd Metodos de uso de derivados de benzotriazoles trisustituidos como inhibidores de dihidroorotato-oxigenasa.
US20180369206A1 (en) 2017-04-24 2018-12-27 Aurigene Discovery Technologies Limited Methods of Use for Trisubstituted Benzotriazole Derivatives as Dihydroorotate Oxygenase Inhibitors
CN109897044A (zh) * 2017-12-07 2019-06-18 北京大学 抗神经病理性疼痛化合物及其制备方法
CN111757731B (zh) 2018-02-20 2024-06-25 法国施维雅药厂 三取代苯并三唑衍生物的使用方法
US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)
WO2019222553A1 (en) 2018-05-16 2019-11-21 Forma Therapeutics, Inc. Inhibiting mutant idh-1
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US10532047B2 (en) 2018-05-16 2020-01-14 Forma Therapeutics, Inc. Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
CN108822082B (zh) * 2018-06-06 2020-11-03 青岛科技大学 一种含氟吡啶哌嗪酰胺类化合物及其应用
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
CN114685399A (zh) * 2022-04-26 2022-07-01 河北广祥制药有限公司 一种乌拉地尔中间体1-(2-甲氧基苯基)哌嗪及其盐的制备方法
CN116425653A (zh) * 2023-03-22 2023-07-14 烟台盛凯伦化学科技有限公司 一种n,n’-二(对乙氧基苯基)-1,4-苯二甲亚胺的制备方法
AU2024271540A1 (en) * 2023-05-18 2025-11-27 Concarlo Therapeutics, Inc. Small molecule inhibitors of p27

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2735127B1 (fr) * 1995-06-09 1997-08-22 Pf Medicament Nouvelles piperazines heteroaromatiques utiles comme medicaments.
GB9602166D0 (en) * 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
WO2004074438A2 (en) * 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
WO2004073619A2 (en) * 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
JP2008526723A (ja) * 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するピラゾール誘導体
SG183049A1 (en) * 2007-07-20 2012-08-30 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
GB0722779D0 (en) 2007-11-20 2008-01-02 Sterix Ltd Compound
JP6067226B2 (ja) * 2009-03-13 2017-01-25 アジオス ファーマシューティカルズ， インコーポレイテッド 細胞増殖関連疾患のための方法および組成物
AR077292A1 (es) * 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas

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