TWI666208B - 治療活性化合物及其使用方法(三) - Google Patents

治療活性化合物及其使用方法(三) Download PDF

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Publication number
TWI666208B
TWI666208B TW103126335A TW103126335A TWI666208B TW I666208 B TWI666208 B TW I666208B TW 103126335 A TW103126335 A TW 103126335A TW 103126335 A TW103126335 A TW 103126335A TW I666208 B TWI666208 B TW I666208B
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TW
Taiwan
Prior art keywords
compound
dose
crystal form
trifluoromethyl
pyridin
Prior art date
Application number
TW103126335A
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English (en)
Chinese (zh)
Other versions
TW201524971A (zh
Inventor
塞繆爾 阿格雷斯塔
崇輝 顧
大衛 辛凱因
樺 楊
郭立挺
唐甄
王建明
張延鋒
周嚴
Original Assignee
美商阿吉斯藥品有限公司
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
Priority claimed from PCT/CN2013/081170 external-priority patent/WO2015018060A1/en
Application filed by 美商阿吉斯藥品有限公司 filed Critical 美商阿吉斯藥品有限公司
Publication of TW201524971A publication Critical patent/TW201524971A/zh
Application granted granted Critical
Publication of TWI666208B publication Critical patent/TWI666208B/zh

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    • 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
    • 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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
TW103126335A 2013-08-02 2014-08-01 治療活性化合物及其使用方法(三) TWI666208B (zh)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US201361861884P 2013-08-02 2013-08-02
US61/861,884 2013-08-02
??PCT/CN2013/081170 2013-08-09
PCT/CN2013/081170 WO2015018060A1 (en) 2013-08-09 2013-08-09 Crystalline forms of therapeutically active compounds and use thereof
US201461939098P 2014-02-12 2014-02-12
US61/939,098 2014-02-12
US201461975448P 2014-04-04 2014-04-04
US61/975,448 2014-04-04
US201462011948P 2014-06-13 2014-06-13
US62/011948 2014-06-13

Publications (2)

Publication Number Publication Date
TW201524971A TW201524971A (zh) 2015-07-01
TWI666208B true TWI666208B (zh) 2019-07-21

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
TW103126335A TWI666208B (zh) 2013-08-02 2014-08-01 治療活性化合物及其使用方法(三)
TW108110624A TWI701242B (zh) 2013-08-02 2014-08-01 治療活性化合物及其使用方法(三)

Family Applications After (1)

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TW108110624A TWI701242B (zh) 2013-08-02 2014-08-01 治療活性化合物及其使用方法(三)

Country Status (21)

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US (6) US9738625B2 (enExample)
EP (3) EP3027193A4 (enExample)
JP (3) JP6742905B2 (enExample)
CN (3) CN110372670B (enExample)
AU (2) AU2014295938B2 (enExample)
BR (1) BR112016002287A2 (enExample)
CA (1) CA2919382A1 (enExample)
CL (2) CL2016000263A1 (enExample)
EA (1) EA030428B1 (enExample)
ES (1) ES2886211T3 (enExample)
IL (2) IL243833A0 (enExample)
MX (2) MX389250B (enExample)
MY (1) MY177994A (enExample)
NI (1) NI201600022A (enExample)
PE (1) PE20160840A1 (enExample)
PH (1) PH12016500164B1 (enExample)
SA (1) SA516370523B1 (enExample)
SG (2) SG11201600479WA (enExample)
TW (2) TWI666208B (enExample)
UA (1) UA121021C2 (enExample)
WO (1) WO2015017821A2 (enExample)

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WO2017016513A1 (zh) 2015-07-30 2017-02-02 正大天晴药业集团股份有限公司 1,3,5-三嗪衍生物及其使用方法
EP3331866B1 (en) 2015-08-05 2023-07-26 Les Laboratoires Servier Methods of preparing a 6-heteroaryl-1,3,5-triazine-2,4-diol and a 6-heteroaryl-1,3,5-triazine-2,4-diamine
CA3001599A1 (en) 2015-10-15 2017-04-20 Agios Pharmaceuticals, Inc. Combination therapy for treating malignancies
MX381582B (es) * 2015-10-15 2025-03-12 Celgene Corp Terapia de combinacion para el tratamiento de neoplasias malignas.
JP6588647B2 (ja) * 2015-10-21 2019-10-09 ノイフォルム・ファーマシューティカルズ・インコーポレイテッドNeuform Pharmaceuticals, Inc. 血液悪性腫瘍を治療するための重水素化合物及びその組成物並びに方法
IL298663A (en) 2015-12-04 2023-01-01 Agios Pharmaceuticals Inc Methods for treating acute myeloid leukemia characterized by the presence of a mutant allele of idh2 and the absence of a mutant allele of nras
WO2017140758A1 (en) 2016-02-19 2017-08-24 Debiopharm International S.A. Derivatives of 2-amino-4-(2-oxazolidinon-3-yl)-pyrimidine fused with a five-membered heteroaromatic ring in 5,6-position which are useful for the treatment of various cancers
WO2017146795A1 (en) * 2016-02-26 2017-08-31 Agios Pharmaceuticals, Inc. Idh1 inhibitors for the treatment of haematological malignancies and solid tumours
US20180042930A1 (en) 2016-08-03 2018-02-15 Celgene Corporation Methods of treatment of malignancies
JP7093764B2 (ja) * 2016-08-03 2022-06-30 セルジーン コーポレイション 骨髄異形成症候群の治療方法
JP2019529534A (ja) 2016-09-07 2019-10-17 セルジーン コーポレイション 錠剤組成物
CN113549056A (zh) 2017-01-22 2021-10-26 正大天晴药业集团股份有限公司 1,3,5-三嗪衍生物的盐及其晶体、它们的制备方法、药物组合物和用途
EP3618828B1 (en) 2017-05-05 2023-11-01 Memorial Sloan Kettering Cancer Center Methods of treatment of myeloproliferative neoplasm
PL3644999T3 (pl) 2017-06-30 2023-05-08 Celgene Corporation Kompozycje i sposoby zastosowania 2-(4-chlorofenylo)-n-((2-(2,6-dioksopiperydyn-3-ylo)-1-oksoizoindolin-5-ylo)metylo)-2,2-difluoroacetamidu
CN109467538A (zh) 2017-09-07 2019-03-15 和记黄埔医药(上海)有限公司 环烯烃取代的杂芳环类化合物及其用途
US20220017489A1 (en) 2018-11-02 2022-01-20 Celgene Corporation Solid dispersions for treatment of cancer
US20220017490A1 (en) 2018-11-02 2022-01-20 Celgene Corporation Co-crystals of 2-methyl-1 -[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl) pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol, compositions and methods of use thereof
US12215094B2 (en) * 2018-11-02 2025-02-04 Celgene Corporation Solid forms of 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl) amino]propan-2-ol
WO2021097160A1 (en) 2019-11-14 2021-05-20 Celgene Corporation Pediatric formulations for treatment of cancer
CN114773320A (zh) * 2022-05-29 2022-07-22 重庆医科大学 1,3,5-三嗪化合物及其制备方法和用途

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PE20160840A1 (es) 2016-09-22
CL2016000263A1 (es) 2016-08-19
IL270347B (en) 2021-08-31
JP6742905B2 (ja) 2020-08-19
CN110372670B (zh) 2023-04-07
US20160194305A1 (en) 2016-07-07
MX394658B (es) 2025-03-24
JP2021176893A (ja) 2021-11-11
EP3027193A2 (en) 2016-06-08
EP3027193A4 (en) 2017-04-26
US20260085059A1 (en) 2026-03-26
US9738625B2 (en) 2017-08-22
AU2014295938B2 (en) 2018-07-19
US20180370951A1 (en) 2018-12-27
TWI701242B (zh) 2020-08-11
SG11201600479WA (en) 2016-02-26
AU2018247242A1 (en) 2018-11-01
EP3566706A1 (en) 2019-11-13
PH12016500164A1 (en) 2016-04-25
WO2015017821A3 (en) 2015-04-09
WO2015017821A2 (en) 2015-02-05
AU2018247242B2 (en) 2020-03-12
JP2019142930A (ja) 2019-08-29
CN110386922A (zh) 2019-10-29
EP3932408A1 (en) 2022-01-05
US10093654B2 (en) 2018-10-09
NI201600022A (es) 2016-03-16
EA030428B1 (ru) 2018-08-31
TW201932455A (zh) 2019-08-16
CN110372670A (zh) 2019-10-25
US20210155603A1 (en) 2021-05-27
BR112016002287A2 (pt) 2017-08-01
TW201524971A (zh) 2015-07-01
UA121021C2 (uk) 2020-03-25
MX389250B (es) 2025-03-20
IL243833A0 (en) 2016-04-21
ES2886211T3 (es) 2021-12-16
JP2016527279A (ja) 2016-09-08
EA201690322A1 (ru) 2016-07-29
PH12016500164B1 (en) 2023-11-08
CA2919382A1 (en) 2015-02-05
MX2020011397A (es) 2022-08-05
US20240132474A1 (en) 2024-04-25
SA516370523B1 (ar) 2019-01-10
SG10201709187TA (en) 2017-12-28
CN105916507A (zh) 2016-08-31
NZ716226A (en) 2021-08-27
EP3566706B1 (en) 2021-07-14
AU2014295938A1 (en) 2016-02-18
MY177994A (en) 2020-09-28
US10730854B2 (en) 2020-08-04
MX2016001361A (es) 2016-06-14
US20170305885A1 (en) 2017-10-26
CL2017002240A1 (es) 2018-04-20

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