SI2978752T1 - 6- (5-Hydroxy-1H-pyrazol-1-yl) nicotinamide derivatives and their use as inhibitors of PHD - Google Patents

6- (5-Hydroxy-1H-pyrazol-1-yl) nicotinamide derivatives and their use as inhibitors of PHD Download PDF

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Publication number
SI2978752T1
SI2978752T1 SI201430629T SI201430629T SI2978752T1 SI 2978752 T1 SI2978752 T1 SI 2978752T1 SI 201430629 T SI201430629 T SI 201430629T SI 201430629 T SI201430629 T SI 201430629T SI 2978752 T1 SI2978752 T1 SI 2978752T1
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Slovenia
Prior art keywords
pyrazol
hydroxy
pyridin
carbonyl
methylbenzonitrile
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SI201430629T
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English (en)
Slovenian (sl)
Inventor
Jason W. Brown
Melinda Davis
Anthony Ivetac
Benjamin Jones
Andre A. Kiryanov
Jon Kuehler
Marion Lanier
Joanne Miura
Sean Murphy
Xiaolun Wang
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Takeda Pharmaceutical Company Limited
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Publication of SI2978752T1 publication Critical patent/SI2978752T1/en

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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SI201430629T 2013-03-29 2014-03-26 6- (5-Hydroxy-1H-pyrazol-1-yl) nicotinamide derivatives and their use as inhibitors of PHD SI2978752T1 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361806806P 2013-03-29 2013-03-29
US201361916715P 2013-12-16 2013-12-16
PCT/US2014/031918 WO2014160810A1 (en) 2013-03-29 2014-03-26 6-(5-hydroxy-1h-pyrazol-1-yl)nicotinamide derivatives and their use as phd inhibitors
EP14726246.3A EP2978752B1 (en) 2013-03-29 2014-03-26 6-(5-hydroxy-1h-pyrazol-1-yl)nicotinamide derivatives and their use as phd inhibitors

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SI2978752T1 true SI2978752T1 (en) 2018-04-30

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US (5) US9040522B2 (enExample)
EP (2) EP2978752B1 (enExample)
JP (4) JP6282724B2 (enExample)
KR (1) KR102376354B1 (enExample)
CN (1) CN105492433B (enExample)
AP (1) AP2015008783A0 (enExample)
AU (1) AU2014241183B2 (enExample)
BR (1) BR112015020350B1 (enExample)
CA (1) CA2903875C (enExample)
CL (1) CL2015002473A1 (enExample)
CR (1) CR20150517A (enExample)
CY (1) CY1120029T1 (enExample)
DK (1) DK2978752T3 (enExample)
EA (1) EA031647B1 (enExample)
EC (1) ECSP15045801A (enExample)
ES (1) ES2660914T3 (enExample)
GE (1) GEP201706761B (enExample)
HR (1) HRP20180341T1 (enExample)
HU (1) HUE038220T2 (enExample)
IL (1) IL240803B (enExample)
JO (1) JO3722B1 (enExample)
LT (1) LT2978752T (enExample)
ME (1) ME03024B (enExample)
MX (1) MX370388B (enExample)
MY (1) MY184218A (enExample)
PE (1) PE20151860A1 (enExample)
PH (1) PH12015502248A1 (enExample)
PL (1) PL2978752T3 (enExample)
PT (1) PT2978752T (enExample)
RS (1) RS56974B1 (enExample)
SG (1) SG11201506749XA (enExample)
SI (1) SI2978752T1 (enExample)
SM (1) SMT201800112T1 (enExample)
TN (1) TN2015000397A1 (enExample)
TR (1) TR201802632T4 (enExample)
TW (1) TWI635084B (enExample)
UA (1) UA118965C2 (enExample)
UY (1) UY35513A (enExample)
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AP2015008783A0 (en) 2013-03-29 2015-10-31 Takeda Pharmaceutical 6-(5-hydroxy-1h-pyrazol-1-yl) nicotinamida derivatives and their use as phd inhibitors
TW202140422A (zh) 2014-10-06 2021-11-01 美商維泰克斯製藥公司 囊腫纖維化症跨膜傳導調節蛋白之調節劑
GEP20217329B (en) 2016-09-30 2021-12-10 Vertex Pharma Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
EA202192783A1 (ru) 2016-12-09 2022-02-24 Вертекс Фармасьютикалз Инкорпорейтед Модулятор регулятора трансмембранной проводимости при муковисцидозе, фармацевтические композиции, способы лечения и способ получения указанного модулятора
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
CN107163043A (zh) * 2017-06-16 2017-09-15 上海毕得医药科技有限公司 一种吡唑并[1,5‑a]吡啶‑3‑羧酸酯衍生物的合成方法
IL272032B2 (en) 2017-07-17 2026-04-01 Vertex Pharma Combination therapy for the treatment of cystic fibrosis including N-(1,3-DIMETHYLPYRAZOL-4-YL)SULFONYL-6-[3-(3,3,3-TRIFLUORO-2,2- DIMETHYL-PROPOXY)PYRAZOL-1-YL]-2-[(4S)-2,2,4- TRIMETHYLPYRROLIDIN-1-YL]PYRIDINE-3-CARBOXAMIDE and
MA49752A (fr) 2017-08-02 2021-04-21 Vertex Pharma Procédés de préparation de composés de pyrrolidine
CA3078893A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
KR102716244B1 (ko) 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
WO2019189731A1 (ja) 2018-03-30 2019-10-03 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
WO2019195739A1 (en) * 2018-04-05 2019-10-10 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator
WO2019200246A1 (en) * 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
WO2020156571A1 (zh) * 2019-02-02 2020-08-06 杭州华东医药集团新药研究院有限公司 一种哒嗪衍生物及其制备方法和医药用途
KR20220156890A (ko) * 2020-03-20 2022-11-28 아케비아 테라퓨틱스 인코포레이티드 Phd 억제제 화합물, 조성물, 및 용도
EP4121425A1 (en) * 2020-03-20 2023-01-25 Akebia Therapeutics Inc. Phd inhibitor compounds, compositions, and use
AR121626A1 (es) * 2020-03-20 2022-06-22 Akebia Therapeutics Inc Compuestos inhibidores de phd, composiciones y métodos de uso
WO2021216530A1 (en) 2020-04-20 2021-10-28 Akebia Therapeutics, Inc. Treatment of viral infections, of organ injury, and of related conditions using a hif prolyl hydroxylase inhibitor or a hif-alpha stabilizer
WO2022150623A1 (en) 2021-01-08 2022-07-14 Akebia Therapeutics, Inc. Compounds and composition for the treatment of anemia
EP4347022A1 (en) 2021-05-27 2024-04-10 Keryx Biopharmaceuticals, Inc. Pediatric formulations of ferric citrate
JP7710897B2 (ja) * 2021-06-01 2025-07-22 三菱ガス化学ネクスト株式会社 １－アルキル－５－ヒドロキシピラゾールの製造方法
WO2023072240A1 (en) * 2021-10-28 2023-05-04 Insilico Medicine Ip Limited Prolyl hydroxylase domain-containing protein (phd) inhibitors and uses thereof
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