EA201591889A1 - 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd - Google Patents

6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd

Info

Publication number
EA201591889A1
EA201591889A1 EA201591889A EA201591889A EA201591889A1 EA 201591889 A1 EA201591889 A1 EA 201591889A1 EA 201591889 A EA201591889 A EA 201591889A EA 201591889 A EA201591889 A EA 201591889A EA 201591889 A1 EA201591889 A1 EA 201591889A1
Authority
EA
Eurasian Patent Office
Prior art keywords
nicotinamide
pyrazol
hydroxy
phd inhibitors
phd
Prior art date
Application number
EA201591889A
Other languages
English (en)
Other versions
EA031647B1 (ru
Inventor
Джейсон В. Браун
Мелинда Дэвис
Энтони Ивтак
Бенджамин Джоунс
Андре А. Кирянов
Джон Кюхлер
Мэрион Ланье
Джоанн Миура
Шон Мерфи
Сяолунь Ван
Original Assignee
Такеда Фармасьютикал Компани Лимитед
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 Такеда Фармасьютикал Компани Лимитед filed Critical Такеда Фармасьютикал Компани Лимитед
Publication of EA201591889A1 publication Critical patent/EA201591889A1/ru
Publication of EA031647B1 publication Critical patent/EA031647B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/445—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
    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/535—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
    • 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
    • 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

Настоящее изобретение обеспечивает соединения формулы (I)которые применяют в качестве ингибиторов PHD, их фармацевтические композиции, способы лечение состояний, связанных с HIF, способы получения соединений и их промежуточных соединений.
EA201591889A 2013-03-29 2014-03-26 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd EA031647B1 (ru)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
EA201591889A1 true EA201591889A1 (ru) 2016-01-29
EA031647B1 EA031647B1 (ru) 2019-02-28

Family

ID=50792544

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591889A EA031647B1 (ru) 2013-03-29 2014-03-26 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd

Country Status (40)

Country Link
US (5) US9040522B2 (ru)
EP (2) EP3336084B1 (ru)
JP (4) JP6282724B2 (ru)
KR (1) KR102376354B1 (ru)
CN (1) CN105492433B (ru)
AP (1) AP2015008783A0 (ru)
AU (1) AU2014241183B2 (ru)
BR (1) BR112015020350B1 (ru)
CA (1) CA2903875C (ru)
CL (1) CL2015002473A1 (ru)
CR (1) CR20150517A (ru)
CY (1) CY1120029T1 (ru)
DK (1) DK2978752T3 (ru)
EA (1) EA031647B1 (ru)
EC (1) ECSP15045801A (ru)
ES (1) ES2660914T3 (ru)
GE (1) GEP201706761B (ru)
HK (1) HK1217701A1 (ru)
HR (1) HRP20180341T1 (ru)
HU (1) HUE038220T2 (ru)
IL (1) IL240803B (ru)
JO (1) JO3722B1 (ru)
LT (1) LT2978752T (ru)
ME (1) ME03024B (ru)
MX (1) MX370388B (ru)
MY (1) MY184218A (ru)
PE (1) PE20151860A1 (ru)
PH (1) PH12015502248A1 (ru)
PL (1) PL2978752T3 (ru)
PT (1) PT2978752T (ru)
RS (1) RS56974B1 (ru)
SG (1) SG11201506749XA (ru)
SI (1) SI2978752T1 (ru)
TN (1) TN2015000397A1 (ru)
TR (1) TR201802632T4 (ru)
TW (1) TWI635084B (ru)
UA (1) UA118965C2 (ru)
UY (1) UY35513A (ru)
WO (1) WO2014160810A1 (ru)
ZA (1) ZA201506484B (ru)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105492433B (zh) 2013-03-29 2018-11-23 武田药品工业株式会社 6-(5-羟基-1h-吡唑-1-基)烟碱酰胺衍生物和其作为phd抑制剂的用途
CN112279808B (zh) 2014-10-06 2024-03-08 弗特克斯药品有限公司 囊性纤维化跨膜转导调节因子调节剂
PE20191147A1 (es) 2016-09-30 2019-09-02 Vertex Pharma Modulador de regulador de conductancia de transmembrana de fibrosis quistica, composiciones farmaceuticas, metodos de tratamiento y proceso para producir el modulador
UY37513A (es) 2016-12-09 2018-07-31 Vertex Pharma Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador
BR112019025801A2 (pt) 2017-06-08 2020-07-07 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
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
EP3654969A1 (en) 2017-07-17 2020-05-27 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AU2018309043B2 (en) 2017-08-02 2022-03-31 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
KR20200097293A (ko) 2017-12-08 2020-08-18 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
US20210139514A1 (en) * 2018-04-05 2021-05-13 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP3774825A1 (en) * 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated 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
JP2023518543A (ja) * 2020-03-20 2023-05-02 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、及びそれらの使用
CA3176140A1 (en) * 2020-03-20 2021-09-23 Akebia Therapeutics, Inc. Phd inhibitor compounds, compositions, and use
EP4121426A1 (en) * 2020-03-20 2023-01-25 Akebia Therapeutics Inc. Phd inhibitor compounds, compositions, and use
EP4138825A1 (en) 2020-04-20 2023-03-01 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
WO2022251563A1 (en) 2021-05-27 2022-12-01 Keryx Biopharmaceuticals, Inc. Pediatric formulations of ferric citrate

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4663327A (en) 1984-05-23 1987-05-05 Bayer Aktiengesellschaft 1-heteroaryl-4-aryl-pyrazolin-5-ones
DE3443308A1 (de) * 1984-11-28 1986-05-28 Bayer Ag, 5090 Leverkusen 1-heteroaryl-4-aryl-pyrazolin-5-one zur verwendung als arzneimittel
US20040014744A1 (en) * 2002-04-05 2004-01-22 Fortuna Haviv Substituted pyridines having antiangiogenic activity
US20040067955A1 (en) * 2002-09-06 2004-04-08 Fujisawa Pharmaceutical Co. Ltd. Pyridazinone compound and pharmaceutical use thereof
DE102005019712A1 (de) 2005-04-28 2006-11-09 Bayer Healthcare Ag Dipyridyl-dihydropyrazolone und ihre Verwendung
CN101291923A (zh) 2005-08-19 2008-10-22 阿斯利康(瑞典)有限公司 治疗结核的吡唑啉酮衍生物
KR101130592B1 (ko) * 2006-06-26 2012-04-02 워너 칠콧 컴퍼니 엘엘씨 프롤릴 히드록실라제 저해제 및 사용 방법
PT2090570E (pt) * 2006-09-05 2011-12-29 Kyowa Hakko Kirin Co Ltd Derivado de imidazole
DE102006050516A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dihydropyrazolone und ihre Verwendung
DE102006050515A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dipyridiyl-dihydropyrazolone und ihre Verwendung
MY147780A (en) 2006-12-29 2013-01-31 Abbvie Deutschland Carboxamide compounds and their use as calpain inhibitors
DE102007044032A1 (de) 2007-09-14 2009-03-19 Bayer Healthcare Ag Substituierte heterocyclische Verbindungen und ihre Verwendung
AU2009225869B2 (en) * 2008-03-18 2014-01-23 Merck Sharp & Dohme Llc Substituted 4-hydroxypyrimidine-5-carboxamides
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
MY179093A (en) * 2008-12-29 2020-10-27 Sanofi Sa Derivatives of 2-pyridin-2-yl-pyrazol-3(2h)-one, preparation and therapeutic use thereof as hif activators
CA2748413A1 (fr) * 2008-12-29 2010-07-08 Sanofi Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one, leur preparation et leur application en therapeutique
CN105492433B (zh) * 2013-03-29 2018-11-23 武田药品工业株式会社 6-(5-羟基-1h-吡唑-1-基)烟碱酰胺衍生物和其作为phd抑制剂的用途

Also Published As

Publication number Publication date
DK2978752T3 (en) 2018-03-12
ES2660914T3 (es) 2018-03-26
IL240803B (en) 2019-02-28
KR20150135794A (ko) 2015-12-03
AP2015008783A0 (en) 2015-10-31
ZA201506484B (en) 2017-11-29
CY1120029T1 (el) 2018-12-12
MX370388B (es) 2019-12-11
NZ711522A (en) 2021-02-26
US20170275271A1 (en) 2017-09-28
JP2016515582A (ja) 2016-05-30
EA031647B1 (ru) 2019-02-28
EP2978752A1 (en) 2016-02-03
IL240803A0 (en) 2015-10-29
US20140296200A1 (en) 2014-10-02
RS56974B1 (sr) 2018-05-31
JP2020073538A (ja) 2020-05-14
UA118965C2 (uk) 2019-04-10
JP6282724B2 (ja) 2018-02-21
US20180186772A1 (en) 2018-07-05
WO2014160810A1 (en) 2014-10-02
AU2014241183B2 (en) 2018-08-09
SI2978752T1 (en) 2018-04-30
PH12015502248B1 (en) 2016-02-01
EP3336084B1 (en) 2021-03-17
AU2014241183A1 (en) 2015-09-24
BR112015020350B1 (pt) 2023-04-25
PE20151860A1 (es) 2015-12-16
US10407409B2 (en) 2019-09-10
ME03024B (me) 2018-10-20
KR102376354B1 (ko) 2022-04-04
ECSP15045801A (es) 2017-02-24
TW201446752A (zh) 2014-12-16
CA2903875A1 (en) 2014-10-02
JP6874114B2 (ja) 2021-05-19
US20150224113A1 (en) 2015-08-13
US9708296B2 (en) 2017-07-18
HK1217701A1 (zh) 2017-01-20
JP2019069997A (ja) 2019-05-09
JP2018083838A (ja) 2018-05-31
CL2015002473A1 (es) 2016-08-26
US20160251337A1 (en) 2016-09-01
HRP20180341T1 (hr) 2018-04-20
US9944626B2 (en) 2018-04-17
EP2978752B1 (en) 2017-11-29
CN105492433A (zh) 2016-04-13
UY35513A (es) 2014-10-31
JP6640978B2 (ja) 2020-02-05
MX2015013687A (es) 2016-02-25
PT2978752T (pt) 2018-03-09
JP6462911B2 (ja) 2019-01-30
CN105492433B (zh) 2018-11-23
PL2978752T3 (pl) 2018-06-29
PH12015502248A1 (en) 2016-02-01
CA2903875C (en) 2021-07-20
SG11201506749XA (en) 2015-09-29
HUE038220T2 (hu) 2018-10-29
EP3336084A1 (en) 2018-06-20
TWI635084B (zh) 2018-09-11
US9345713B2 (en) 2016-05-24
TR201802632T4 (tr) 2018-03-21
MY184218A (en) 2021-03-26
BR112015020350A2 (pt) 2017-07-18
LT2978752T (lt) 2018-03-26
CR20150517A (es) 2016-01-12
TN2015000397A1 (en) 2017-01-03
US9040522B2 (en) 2015-05-26
GEP201706761B (en) 2017-10-25
JO3722B1 (ar) 2021-01-31

Similar Documents

Publication Publication Date Title
EA201591889A1 (ru) 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd
CY1120969T1 (el) Παραγωγα κινοξαλινης χρησιμα ως τροποποιητες fgfr κινασης
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201792535A1 (ru) Гетероциклические амиды в качестве ингибиторов киназ
EA201991198A1 (ru) АМИНОТИАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit
EA201891910A1 (ru) Гетероарильные ингибиторы pad4
PH12018500408A1 (en) Bicyclic compounds as atx inhibitors
EA201790595A1 (ru) Пиримидиноны в качестве ингибиторов фактора xia
EA201691272A1 (ru) Тетрагидропиридопиразины в качестве модуляторов gpr6
MX2018001430A (es) Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
PH12018500409A1 (en) New bicyclic compounds as dual atx/ca inhibitors
MX2018001890A (es) Compuestos biciclicos como inhibidores de autotaxina (atx).
TR201906366T4 (tr) Polisiklik-karbamoilpiridon bileşiklerinin sentezi.
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
EA201891251A1 (ru) Бициклические ингибиторы pad4
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA201692143A1 (ru) Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы
EA201891347A1 (ru) Аза-бензимидазольные ингибиторы pad4
EA201690844A1 (ru) Ингибиторы gsk-3
NZ711192A (en) Process for making benzoxazepin compounds
MX2018007219A (es) Metodos para preparacion de compuestos heterociclicos de 1,3-benzodioxol.
TW201613934A (en) Methods for the preparation of 1,3-benzodioxole heterocyclic compounds
EA201690227A1 (ru) Азаиндольные соединения, их получение и способы их применения
EA201792288A1 (ru) Способы лечения рака
EA201691632A1 (ru) Пиразины в качестве модуляторов gpr6