JP6256771B2 - ヒストンデメチラーゼ阻害剤 - Google Patents

ヒストンデメチラーゼ阻害剤 Download PDF

Info

Publication number
JP6256771B2
JP6256771B2 JP2015545854A JP2015545854A JP6256771B2 JP 6256771 B2 JP6256771 B2 JP 6256771B2 JP 2015545854 A JP2015545854 A JP 2015545854A JP 2015545854 A JP2015545854 A JP 2015545854A JP 6256771 B2 JP6256771 B2 JP 6256771B2
Authority
JP
Japan
Prior art keywords
compound
pyrazol
formula
hydrogen
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2015545854A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016501882A (ja
JP2016501882A5 (OSRAM
Inventor
ニエ,チェ
スタッフォード,ジェフリー,アラン
ヴィール,ジェイムス,マービン
ウォレス,マイケル,ブレナン
Original Assignee
セルジーン クオンティセル リサーチ,インク.
セルジーン クオンティセル リサーチ,インク.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by セルジーン クオンティセル リサーチ,インク., セルジーン クオンティセル リサーチ,インク. filed Critical セルジーン クオンティセル リサーチ,インク.
Publication of JP2016501882A publication Critical patent/JP2016501882A/ja
Publication of JP2016501882A5 publication Critical patent/JP2016501882A5/ja
Application granted granted Critical
Publication of JP6256771B2 publication Critical patent/JP6256771B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D401/04Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2015545854A 2012-12-06 2013-12-05 ヒストンデメチラーゼ阻害剤 Expired - Fee Related JP6256771B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261734330P 2012-12-06 2012-12-06
US61/734,330 2012-12-06
US201361784414P 2013-03-14 2013-03-14
US61/784,414 2013-03-14
PCT/US2013/073424 WO2014089364A1 (en) 2012-12-06 2013-12-05 Histone demethylase inhibitors

Publications (3)

Publication Number Publication Date
JP2016501882A JP2016501882A (ja) 2016-01-21
JP2016501882A5 JP2016501882A5 (OSRAM) 2016-12-01
JP6256771B2 true JP6256771B2 (ja) 2018-01-10

Family

ID=50884011

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015545854A Expired - Fee Related JP6256771B2 (ja) 2012-12-06 2013-12-05 ヒストンデメチラーゼ阻害剤

Country Status (7)

Country Link
US (7) US9604961B2 (OSRAM)
EP (2) EP2928471B1 (OSRAM)
JP (1) JP6256771B2 (OSRAM)
CA (1) CA2894399A1 (OSRAM)
ES (1) ES2834959T3 (OSRAM)
MX (1) MX2015007205A (OSRAM)
WO (1) WO2014089364A1 (OSRAM)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102160320B1 (ko) 2012-10-02 2020-09-28 에피테라퓨틱스 에이피에스 히스톤 탈메틸효소의 저해제
ES2834959T3 (es) 2012-12-06 2021-06-21 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa
SI2961736T1 (en) 2013-02-27 2018-06-29 Gilead Sciences, Inc. Histone demethylase inhibitors
JP2017066030A (ja) * 2014-02-04 2017-04-06 アグロカネショウ株式会社 新規なピラゾール誘導体およびこれを有効成分とする農園芸用薬剤
CA2946538A1 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
JP6521535B2 (ja) 2014-06-25 2019-05-29 セルジーン クオンティセル リサーチ,インク. ヒストンデメチラーゼ阻害剤
CA2954212C (en) 2014-07-31 2023-09-19 Basf Se Process for preparing pyrazoles
WO2016023954A2 (en) 2014-08-12 2016-02-18 Syngenta Participations Ag Pesticidally active heterocyclic derivatives with sulphur containing substituents
MX2017002451A (es) 2014-08-27 2017-05-23 Gilead Sciences Inc Compuestos y metodos para inhibir histona desmetilasas.
EA201790502A1 (ru) 2014-09-16 2017-10-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы гистоновых диметилаз
US9896436B2 (en) 2014-09-16 2018-02-20 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
JP6833718B2 (ja) 2015-05-11 2021-02-24 ビーエイエスエフ・ソシエタス・エウロパエアBasf Se 4−アミノ−ピリダジンを製造するための方法
WO2017133942A1 (en) 2016-02-02 2017-08-10 Basf Se Catalytic hydrogenation process for preparing pyrazoles
US20190055212A1 (en) * 2016-02-16 2019-02-21 Stephen Gwaltney Histone demethylase inhibitors
JP6970680B2 (ja) * 2016-03-15 2021-11-24 セルジーン クオンティセル リサーチ,インク. ヒストンデメチラーゼ阻害剤
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
WO2017198785A1 (en) * 2016-05-18 2017-11-23 Ieo - Istituto Europeo Di Oncologia S.R.L. Oxime derivatives useful as inhibitors of histone demethylase kdm4c
WO2017205078A1 (en) 2016-05-27 2017-11-30 Gilead Sciences, Inc. Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
WO2017207813A1 (en) 2016-06-03 2017-12-07 Oryzon Genomics, S.A. Heteroaryl-carboxylic acids as histone demethylase inhibitors
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
ES2906581T3 (es) 2016-09-02 2022-04-19 Gilead Sciences Inc Compuestos moduladores de los receptores tipo Toll
US10640499B2 (en) 2016-09-02 2020-05-05 Gilead Sciences, Inc. Toll like receptor modulator compounds
BR112019007450A2 (pt) 2016-10-14 2020-07-07 Precision Biosciences, Inc. meganucleases modificadas específicas para sequências de reconhecimento no genoma do vírus da hepatite b
TWI714820B (zh) 2017-01-31 2021-01-01 美商基利科學股份有限公司 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
WO2018219478A1 (en) 2017-06-02 2018-12-06 Oryzon Genomics, S.A. Heteroaryl-carboxamides as histone demethylase inhibitors
CN111566120B (zh) 2017-12-20 2023-09-29 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的3’3’环状二核苷酸
EP3728282B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CN111712494A (zh) 2018-02-13 2020-09-25 吉利德科学公司 Pd-1/pd-l1抑制剂
CA3091142C (en) 2018-02-26 2023-04-11 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
WO2019195181A1 (en) 2018-04-05 2019-10-10 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 2,2,─環二核苷酸
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
EP4600247A3 (en) 2018-04-19 2025-11-19 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
WO2019211799A1 (en) 2018-05-03 2019-11-07 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide
KR20230159715A (ko) 2018-07-13 2023-11-21 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
AU2019366355B2 (en) 2018-10-24 2022-10-13 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
CN113227089B (zh) 2018-10-31 2024-07-05 吉利德科学公司 作为hpk1抑制剂的取代的6-氮杂苯并咪唑化合物
CN117105933A (zh) 2018-10-31 2023-11-24 吉利德科学公司 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
US20220143061A1 (en) 2019-03-07 2022-05-12 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
EP3934757B1 (en) 2019-03-07 2023-02-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
JP7237311B2 (ja) * 2019-06-06 2023-03-13 京都府公立大学法人 化合物、医薬組成物、kdm5c阻害剤及び抗うつ剤
CN110128347A (zh) * 2019-06-17 2019-08-16 韶远科技(上海)有限公司 一种1-甲基-1h-吲唑-6-甲酸的合成方法
JP7295283B2 (ja) 2019-06-25 2023-06-20 ギリアード サイエンシーズ, インコーポレイテッド Flt3l-fc融合タンパク質及び使用方法
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
EP4017476A1 (en) 2019-08-19 2022-06-29 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
HRP20241379T1 (hr) 2019-09-30 2024-12-20 Gilead Sciences, Inc. Cjepiva za hbv i postupci za liječenje hbv
ES3022990T3 (en) 2019-12-06 2025-05-29 Prec Biosciences Inc Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
USD1000624S1 (en) 2019-12-27 2023-10-03 Thomas Nichols Personal care device with camera
CN121085892A (zh) * 2020-03-20 2025-12-09 阿克比治疗有限公司 Phd抑制剂化合物、组合物和用途
TWI845826B (zh) 2020-03-20 2024-06-21 美商基利科學股份有限公司 4'-c-經取代-2-鹵基-2'-去氧腺苷核苷之前藥及其製造與使用方法
JP7768890B2 (ja) * 2020-03-20 2025-11-12 アケビア セラピューティクス インコーポレイテッド Phd阻害剤化合物、組成物、および使用
US20230212138A1 (en) * 2020-03-20 2023-07-06 Akebia Therapeutics, Inc. Phd inhibitor compounds, compositions, and their use
MX2023001507A (es) 2020-08-07 2023-03-06 Gilead Sciences Inc Profarmacos de analogos de nucleotidos de fosfonamida y su uso farmaceutico.
CN116249692B (zh) * 2020-09-28 2024-08-23 四川科伦博泰生物医药股份有限公司 吡唑类化合物及其制备方法和用途
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
TW202348237A (zh) 2021-05-13 2023-12-16 美商基利科學股份有限公司 TLR8調節化合物及抗HBV siRNA療法之組合
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
CN117480155A (zh) 2021-06-23 2024-01-30 吉利德科学公司 二酰基甘油激酶调节化合物
CN117377671A (zh) 2021-06-23 2024-01-09 吉利德科学公司 二酰基甘油激酶调节化合物
EP4359415A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
EP4617260A1 (en) * 2022-11-09 2025-09-17 Mitsubishi Gas Chemical Next Company, Inc. Production method for 1-alkyl-5-hydroxypyrazole
US20250345389A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
US20250345390A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI68369C (fi) 1983-03-01 1985-09-10 Waertsilae Oy Ab Bestrykningsanordning
US4824859A (en) 1983-05-21 1989-04-25 Fisons Plc. Pyrazoline compounds compositions and use
FI855180A7 (fi) 1985-01-18 1986-07-19 Nissan Chemical Ind Ltd Pyratsolisulfonamidijohdannainen, menetelmä sen valmistamiseksi ja sitä sisältävä rikkaruohomyrkky.
US4699647A (en) 1985-05-30 1987-10-13 E. I. Du Pont De Nemours And Company Herbicidal sulfonamides
DE3528477A1 (de) 1985-08-08 1987-02-19 Bayer Ag 1-aryl-pyrazole
DE3538731A1 (de) 1985-10-31 1987-05-07 Bayer Ag 1-aryl-4-nitro-pyrazole
DE3539844A1 (de) 1985-11-09 1987-05-14 Bayer Ag Substituierte 5-amino-1-aryl-pyrazole
DE3543034A1 (de) 1985-12-05 1987-06-11 Bayer Ag 5-perfluoracylamino-4-nitro-1-aryl-pyrazol-salze
DE3543035A1 (de) 1985-12-05 1987-06-11 Bayer Ag 5-fluoracylamino-4-nitro-1-aryl-pyrazole
DE3600950A1 (de) 1986-01-15 1987-07-16 Bayer Ag 5-acylamido-1-aryl-pyrazole
DE3609542A1 (de) 1986-03-21 1987-10-01 Bayer Ag 5-acylamino-pyrazol-derivate
DE3625686A1 (de) 1986-07-30 1988-02-04 Bayer Ag 4-cyano(nitro)-5-oxy(thio)-pyrazol-derivate
DE3628892A1 (de) 1986-08-26 1988-03-10 Bayer Ag Substituierte 1-aryl-3-tert.-butyl-pyrazole
DE3631003A1 (de) 1986-09-12 1988-03-24 Bayer Ag Verfahren zur herstellung von 4-substituierten 1-aryl-5-amino-pyrazolen
DE3637710A1 (de) 1986-11-05 1988-05-11 Bayer Ag 5-acylamino-pyrazol-derivate
DE3707551A1 (de) 1987-03-10 1988-09-22 Bayer Ag Substituierte 1-arylpyrazole
DE3721868A1 (de) 1987-07-02 1989-01-12 Bayer Ag 1-arylpyrazole
DE3911556A1 (de) 1989-04-08 1990-10-11 Bayer Ag Substituierte 1-arylpyrazole
DE4023488A1 (de) * 1990-07-24 1992-01-30 Bayer Ag 1-(pyri(mi)dyl-(2)) -5-hydroxy-pyrazol-mikrobizide
US5298368A (en) 1991-04-23 1994-03-29 Eastman Kodak Company Photographic coupler compositions and methods for reducing continued coupling
US5292844A (en) 1991-05-22 1994-03-08 Minnesota Mining And Manufacturing Company Vinyl acetate modified suspension polymer beads, adhesives made therefrom and a method of making
US5262284A (en) 1991-07-15 1993-11-16 Eastman Kodak Company Arylidene pyrazolone coupler
DE4126244A1 (de) 1991-08-08 1993-02-11 Bayer Ag Massefaerben von kunststoffen
US5200309A (en) 1991-08-29 1993-04-06 Eastman Kodak Company Color photographic materials including magenta coupler, carbonamide compound and aniline or amine compound, and methods
US5250405A (en) 1991-08-29 1993-10-05 Eastman Kodak Company Color photographic materials including magenta coupler, inhibitor-releasing coupler and carbonamide compound, and methods
US5376519A (en) 1992-04-23 1994-12-27 Eastman Kodak Company Photographic material containing a coupler composition comprising magenta coupler, phenolic solvent, and at least one aniline or amine
US5340707A (en) 1992-09-16 1994-08-23 Konica Corporation Silver halide photographic light-sensitive material
ZA942125B (en) 1993-03-26 1994-11-10 Shell Res Ltd Herbicidal heterocyclic compounds.
US5389504A (en) 1993-06-24 1995-02-14 Eastman Kodak Company Color photographic elements containing a combination of pyrazolone and pyrazoloazole couplers
EP0690345B1 (en) 1994-06-23 2001-09-05 Eastman Kodak Company Two-equivalent magenta photographic couplers with activity-modifying ballasting groups
WO1997011941A1 (fr) 1995-09-28 1997-04-03 Suntory Limited Derives de la quinazoline et leurs emplois
JP2001508767A (ja) 1996-12-02 2001-07-03 藤沢薬品工業株式会社 5―ht拮抗作用を有するインドール―ウレア誘導体
US5821043A (en) 1996-12-30 1998-10-13 Eastman Kodak Company 1,2,4-triazole-releasing pyrazolone DIR couplers
CO5060426A1 (es) 1997-03-10 2001-07-30 Rhone Poulenc Agrochimie 1-aril-3-imidiopirazoles plaguicidas
US5958662A (en) 1997-03-25 1999-09-28 Eastman Kodak Company Photographic element containing a DIR coupler
US5942381A (en) 1997-06-12 1999-08-24 Eastman Kodak Company Photographic element and process employing active, stable benzotriazole-releasing DIR couplers
US5998424A (en) 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group
BR9812041B1 (pt) 1997-09-05 2009-08-11 processo para a preparação de derivados n-acilados (hetero) aromáticos da hidroxilamina.
DE19804486A1 (de) 1998-02-05 1999-08-12 Basf Ag 2-(Pyrazolyloxy)-pyridin-3-ylessigsäure- Derivate, sie enthaltende Mittel und ihr
US6121271A (en) 1998-05-12 2000-09-19 American Home Products Corporation Naphtho[2,3-B]heteroar-4-yl derivatives
US6010839A (en) 1998-06-26 2000-01-04 Eastman Kodak Company Color photographic elements containing yellow-colored magenta dye-forming masking couplers
US20030191279A1 (en) 1999-08-27 2003-10-09 Goldstein Steven Wayne Urea derivatives useful as anticancer agents
US6132943A (en) 1999-10-14 2000-10-17 Eastman Kodak Company Color photographic elements containing yellow-colored magenta dye-forming masking couplers
JP2001335714A (ja) 2000-03-22 2001-12-04 Fuji Photo Film Co Ltd アゾ色素、その製造方法、インクジェット用インク、インクジェット記録方法
WO2001081332A2 (en) 2000-04-25 2001-11-01 Pharmacia Corporation 2-fluorobenzenesulfonyl compounds for the treatment of inflammation
JP4113323B2 (ja) 2000-08-07 2008-07-09 富士フイルム株式会社 アゾ色素及びそれを含むインクジェット記録用インク、並びにインクジェット記録方法
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
JP2002167531A (ja) 2000-11-29 2002-06-11 Fuji Photo Film Co Ltd インクジェット記録用インク組成物及び画像形成方法
US6673818B2 (en) 2001-04-20 2004-01-06 Pharmacia Corporation Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
US6603000B2 (en) 2001-07-11 2003-08-05 Boehringer Ingelheim Pharmaceuticals, Inc. Synthesis for heteroarylamine compounds
TWI356822B (en) 2001-08-13 2012-01-21 Du Pont Novel substituted dihydro 3-halo-1h-pyrazole-5-car
MY142967A (en) 2001-08-13 2011-01-31 Du Pont Method for controlling particular insect pests by applying anthranilamide compounds
DE60236600D1 (de) 2001-08-13 2010-07-15 Du Pont Substituierte 1h-dihydropyrazole, ihre herstellung und verwendung
ATE417829T1 (de) 2001-08-16 2009-01-15 Du Pont Substituierte anthranilamide und ihre verwendung als pesticide
SE0103644D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
DE60325025D1 (de) 2002-02-15 2009-01-15 Glaxo Group Ltd Modulatoren des vanilloidrezeptors
US7560563B2 (en) 2002-07-23 2009-07-14 Kuraray Co., Ltd. Process for producing 2-substituted pyridine derivative
TWI343376B (en) 2002-07-31 2011-06-11 Du Pont Method for preparing 3-halo-4, 5-dihydro-1h-pyrazoles
TWI326283B (en) 2002-07-31 2010-06-21 Du Pont Method for preparing fused oxazinones
PA8578101A1 (es) 2002-08-13 2004-05-07 Warner Lambert Co Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
WO2004037794A1 (en) 2002-10-23 2004-05-06 Banyu Pharmaceutical Co., Ltd Process for making pyrazole compounds
WO2004046129A2 (en) 2002-11-15 2004-06-03 E.I. Du Pont De Nemours And Company Novel anthranilamide insecticides
ATE359782T1 (de) 2003-01-16 2007-05-15 Sb Pharmco Inc Heteroaryl-substituierte pyrrol(2, 3- b)pyridin- derivate als crf-rezeptor-antagonisten
CA2515544A1 (en) 2003-02-11 2004-08-26 Kemia Inc. Compounds for the treatment of viral infection
TWI367882B (en) 2003-03-26 2012-07-11 Du Pont Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates
KR20060008336A (ko) 2003-06-12 2006-01-26 이 아이 듀폰 디 네모아 앤드 캄파니 융합된 옥사지논 제조 방법
WO2005023773A1 (en) 2003-09-04 2005-03-17 Pfizer Limited Process for the preparation of substituted aryl pyrazoles
GB0323585D0 (en) 2003-10-08 2003-11-12 Glaxo Group Ltd Compounds
DE102004006075A1 (de) 2003-11-14 2005-06-16 Bayer Cropscience Ag Wirkstoffkombinationen mit insektiziden Eigenschaften
DE102004021564A1 (de) 2003-11-14 2005-07-07 Bayer Cropscience Ag Wirkstoffkombinationen mit insektiziden Eigenschaften
DE10353281A1 (de) 2003-11-14 2005-06-16 Bayer Cropscience Ag Wirkstoffkombination mit insektiziden und akariziden Eigenschaften
EP1691611A1 (de) 2003-12-04 2006-08-23 Bayer CropScience Aktiengesellschaft Wirkstoffkombinationen mit insektiziden eigenschaften
WO2005053405A1 (de) 2003-12-04 2005-06-16 Bayer Cropscience Aktiengesellschaft Wirkstoffkombinationen mit insektiziden und akariziden eigenschaften
DE10356550A1 (de) 2003-12-04 2005-07-07 Bayer Cropscience Ag Wirkstoffkombinationen mit insektiziden Eigenschaften
DE102004023635A1 (de) 2004-05-10 2006-04-13 Grünenthal GmbH Heteroarylsubstituierte Cyclohexyl-1,4-diamin-Derivate
CA2565437A1 (en) 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
DE102004031100A1 (de) 2004-06-28 2006-01-12 Bayer Cropscience Ag Anthranilamide
DE102004035134A1 (de) 2004-07-20 2006-02-16 Bayer Cropscience Ag Selektive Insektizide auf Basis von Halogenalkylnicotinsäurederivaten, Anthranilsäureamiden oder Phthalsäurediamiden und Safenern
CA2578122A1 (en) 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
WO2006044456A1 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
US20080119505A1 (en) 2005-02-01 2008-05-22 Altana Pharma Ag Novel 6-Pyridylphenanthridines
AU2006219862A1 (en) 2005-03-02 2006-09-08 Nycomed Gmbh 6-Heteroaryl-1,2,3,4,4a, 10b-hexahydro-phenanthridines as PDE-4 inhibitors for the treatment of inflammatory disorders
EP1728790A1 (en) 2005-06-01 2006-12-06 Max-Delbrück-Centrum Für Molekulare Medizin Shp-2 inhibitors, pharmaceutical compositions comprising them and their use for treating phosphatase-mediated diseases
BRPI0613535A2 (pt) 2005-06-02 2011-01-18 Bayer Cropscience Ag derivados de heteroarila substituìda por fenilalquila
ES2337831T3 (es) 2005-06-24 2010-04-29 Bristol-Myers Squibb Company Derivados de fenilglicinamida y piridilclicinamida utiles como agentes anticoagulantes.
PT1904475E (pt) 2005-07-07 2011-10-03 Basf Se Compostos (en)n-tio-antranilamida e seu uso como pesticidas
ES2337005B1 (es) 2005-07-15 2011-01-10 Laboratorios Del Dr. Esteve, S.A. Compuestos de pirazolina azepan o azocansustituidos, su preparacion ysu uso como medicamentos.
WO2007046809A1 (en) 2005-10-21 2007-04-26 Dow Agrosciences Llc Thieno-pyrimidine compounds having fungicidal activity
US7531482B2 (en) 2005-10-21 2009-05-12 Dow Agrosciences Llc Thieno-pyrimidine compounds having fungicidal activity
EP1954276A2 (en) 2005-11-22 2008-08-13 Merck & Co., Inc. Indole orexin receptor antagonists
JPWO2007063868A1 (ja) 2005-11-29 2009-05-07 東レ株式会社 アリールメチレンウレア誘導体及びその用途
AU2006322067A1 (en) 2005-12-06 2007-06-14 Merck Sharp & Dohme Corp. Morpholine carboxamide prokineticin receptor antagonists
DE102005059470A1 (de) 2005-12-13 2007-06-14 Bayer Cropscience Ag Insektizide Zusammensetzungen mit verbesserter Wirkung
SG170819A1 (en) 2006-03-30 2011-05-30 Ptc Therapeutics Inc Methods for the production of functional protein from dna having a nonsense mutation and the treatment of disorders associated therewith
KR101325062B1 (ko) 2006-05-19 2013-11-05 삼성디스플레이 주식회사 발광 이종 핵 구리-이리듐 착체 및 이를 이용한 유기 전계발광 소자
JP2009544626A (ja) 2006-07-21 2009-12-17 アイアールエム・リミテッド・ライアビリティ・カンパニー Itpkb阻害剤としての化合物および組成物
WO2008023235A1 (en) 2006-08-25 2008-02-28 Pfizer Products Inc. Pyrazole derivatives as anti-platelet and anti-thrombotic agents
CA2666603C (en) 2006-10-16 2013-08-06 Pfizer Products Inc. Therapeutic pyrazolyl thienopyridines and uses thereof for treating tgf.beta. mediated conditions
AU2007333194A1 (en) 2006-12-08 2008-06-19 Exelixis, Inc. LXR and FXR modulators
US8278337B2 (en) 2006-12-20 2012-10-02 Merck Sharp & Dohme Substituted pyridines that are JNK inhibitors
EP1958934A1 (en) 2007-02-16 2008-08-20 Bayer Schering Pharma Aktiengesellschaft Tetrahydronaphthalenylamides, a process for their production and their use as anti-inflammatory agents
WO2008106202A1 (en) 2007-02-27 2008-09-04 Housey Gerard M Theramutein modulators
EP2133331A4 (en) 2007-04-11 2011-06-22 Kissei Pharmaceutical FIVE-GLASS HETEROCYCLIC DERIVATIVE AND ITS USE IN MEDICAL PURPOSES
US8071035B2 (en) 2007-04-12 2011-12-06 Siemens Medical Solutions Usa, Inc. Microfluidic radiosynthesis system for positron emission tomography biomarkers
EP2148878A4 (en) 2007-04-20 2011-08-10 Merck Canada Inc NEW HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE
EP2148868A1 (en) 2007-05-15 2010-02-03 NeuroSearch A/S Novel aromatic heterocyclic carboxylic acid amide derivatives useful as potassium channel modulators
US7776877B2 (en) 2007-06-22 2010-08-17 Chemocentryx, Inc. N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides
WO2009022171A1 (en) 2007-08-13 2009-02-19 Astrazeneca Ab Pyridinyiioxy pyridines as alk5 inhibitors
CA2705848C (en) 2007-11-21 2016-02-02 Bio-Rad Laboratories, Inc. Photoluminescent metal complexes for protein staining
WO2009073973A1 (en) 2007-12-11 2009-06-18 Merck Frosst Canada Ltd. Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
CA2707660A1 (en) 2007-12-20 2009-07-02 Astrazeneca Ab Carbamoyl compounds as dgat1 inhibitors 190
US20100292233A1 (en) 2008-01-25 2010-11-18 Arena Pharmaceuticals, Inc. Dihydro-1h-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives which act as s1p1 agonists
WO2009126691A1 (en) 2008-04-09 2009-10-15 Infinity Pharmaceuticals, Inc Inhibitors of fatty acid amide hydrolase
WO2009137657A1 (en) 2008-05-08 2009-11-12 Bristol-Myers Squibb Company 2-aryl glycinamide derivatives
CN102186809A (zh) 2008-08-14 2011-09-14 拜尔农作物科学股份公司 杀虫性的4-苯基-1h-吡唑
GB0818907D0 (en) 2008-10-15 2008-11-19 Isis Innovation Histone lysine demethylase inhibitors
WO2010048207A2 (en) 2008-10-21 2010-04-29 Metabolex, Inc. Aryl gpr120 receptor agonists and uses thereof
AU2009321601B2 (en) 2008-12-04 2012-11-01 F. Hoffmann-La Roche Ag Pyridazinone derivatives
JP5894438B2 (ja) 2009-02-11 2016-03-30 ダウ アグロサイエンシィズ エルエルシー 殺虫性組成物
WO2010124097A2 (en) 2009-04-22 2010-10-28 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
US9149465B2 (en) 2009-05-18 2015-10-06 Infinity Pharmaceuticals, Inc. Isoxazolines as inhibitors of fatty acid amide hydrolase
US8927551B2 (en) 2009-05-18 2015-01-06 Infinity Pharmaceuticals, Inc. Isoxazolines as inhibitors of fatty acid amide hydrolase
KR101280198B1 (ko) * 2009-09-02 2013-06-28 이화여자대학교 산학협력단 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물
WO2011028043A2 (ko) * 2009-09-02 2011-03-10 이화여자대학교 산학협력단 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
WO2011075684A1 (en) 2009-12-18 2011-06-23 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US8598211B2 (en) 2009-12-22 2013-12-03 Abbvie Inc. Carboxamide compounds and their use as calpain inhibitors IV
US9051304B2 (en) 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
EP2552214A4 (en) 2010-03-26 2013-10-16 Glaxo Group Ltd PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
JP5787977B2 (ja) 2010-04-08 2015-09-30 レスピバート・リミテツド P38mapキナーゼ阻害剤
AU2011253057B2 (en) 2010-05-13 2014-11-20 Amgen Inc. Nitrogen heterocyclic compounds useful as PDE10 inhibitors
WO2012004293A2 (de) 2010-07-08 2012-01-12 Bayer Cropscience Ag Insektizide und fungizide wirkstoffkombinationen
JP5789888B2 (ja) 2010-11-01 2015-10-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン生成のベンゾイミダゾールインヒビター
JP5847830B2 (ja) 2010-11-10 2016-01-27 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd オレキシン受容体拮抗薬として有用なラクタム誘導体
EP2457900A1 (en) 2010-11-25 2012-05-30 Almirall, S.A. New pyrazole derivatives having CRTh2 antagonistic behaviour
US20130253011A1 (en) 2010-12-17 2013-09-26 Syngenta Participations Ag Insecticidal compounds
EP2592154A1 (en) 2011-11-09 2013-05-15 Cellzome Ag Immobilization products and methods for the identification of histone demethylase interacting molecules and for the purification of histone demethylase proteins
ES2834959T3 (es) 2012-12-06 2021-06-21 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa

Also Published As

Publication number Publication date
US20160068507A1 (en) 2016-03-10
US9604961B2 (en) 2017-03-28
EP2928471A1 (en) 2015-10-14
EP2928471A4 (en) 2016-06-15
US9458129B2 (en) 2016-10-04
US9107916B2 (en) 2015-08-18
US9714230B2 (en) 2017-07-25
US9908865B2 (en) 2018-03-06
ES2834959T3 (es) 2021-06-21
WO2014089364A1 (en) 2014-06-12
US20160002201A1 (en) 2016-01-07
US10173996B2 (en) 2019-01-08
US20170158664A1 (en) 2017-06-08
CA2894399A1 (en) 2014-06-12
US20160347733A1 (en) 2016-12-01
MX2015007205A (es) 2016-03-31
US20170275266A1 (en) 2017-09-28
US20150164872A1 (en) 2015-06-18
US8987461B2 (en) 2015-03-24
EP2928471B1 (en) 2020-10-14
EP3763367A1 (en) 2021-01-13
JP2016501882A (ja) 2016-01-21
US20140194469A1 (en) 2014-07-10

Similar Documents

Publication Publication Date Title
JP6256771B2 (ja) ヒストンデメチラーゼ阻害剤
JP6276378B2 (ja) ヒストンデメチラーゼ阻害剤
JP6320506B2 (ja) ヒストンデメチラーゼ阻害剤
CN105026372B (zh) 组蛋白脱甲基酶抑制剂
JP6256772B2 (ja) ヒストンデメチラーゼ阻害剤
KR102400920B1 (ko) 리신 특이적 데메틸라제-1의 억제제
JP6663866B2 (ja) リジン特異的なデメチラーゼ−1の阻害剤
RS56561B1 (sr) Inhibitori histon demetilaze
JP6970680B2 (ja) ヒストンデメチラーゼ阻害剤
JP2017529347A (ja) ヒストンデメチラーゼ阻害剤
TW201738225A (zh) 組織蛋白去甲基酶抑制劑

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150721

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161014

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20161017

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170810

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170816

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171020

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20171101

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20171106

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20171106

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20171122

R150 Certificate of patent or registration of utility model

Ref document number: 6256771

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees