CN105492433B - 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 - Google Patents

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 Download PDF

Info

Publication number
CN105492433B
CN105492433B CN201480018116.6A CN201480018116A CN105492433B CN 105492433 B CN105492433 B CN 105492433B CN 201480018116 A CN201480018116 A CN 201480018116A CN 105492433 B CN105492433 B CN 105492433B
Authority
CN
China
Prior art keywords
base
hydroxyl
methyl
carbonyl
pyridine
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.)
Active
Application number
CN201480018116.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN105492433A (zh
Inventor
J·W·布朗
M·戴维斯
A·艾弗塔克
B·琼斯
A·A·科亚诺夫
J·库勒
M·兰尼尔
J·缪拉
S·墨菲
X·王
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Takeda Pharmaceutical Co Ltd
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 Takeda Pharmaceutical Co Ltd filed Critical Takeda Pharmaceutical Co Ltd
Publication of CN105492433A publication Critical patent/CN105492433A/zh
Application granted granted Critical
Publication of CN105492433B publication Critical patent/CN105492433B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
CN201480018116.6A 2013-03-29 2014-03-26 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 Active CN105492433B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361806806P 2013-03-29 2013-03-29
US61/806,806 2013-03-29
US201361916715P 2013-12-16 2013-12-16
US61/916,715 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
CN105492433A CN105492433A (zh) 2016-04-13
CN105492433B true CN105492433B (zh) 2018-11-23

Family

ID=50792544

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480018116.6A Active CN105492433B (zh) 2013-03-29 2014-03-26 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

Country Status (40)

Country Link
US (5) US9040522B2 (https=)
EP (2) EP2978752B1 (https=)
JP (4) JP6282724B2 (https=)
KR (1) KR102376354B1 (https=)
CN (1) CN105492433B (https=)
AP (1) AP2015008783A0 (https=)
AU (1) AU2014241183B2 (https=)
BR (1) BR112015020350B1 (https=)
CA (1) CA2903875C (https=)
CL (1) CL2015002473A1 (https=)
CR (1) CR20150517A (https=)
CY (1) CY1120029T1 (https=)
DK (1) DK2978752T3 (https=)
EA (1) EA031647B1 (https=)
EC (1) ECSP15045801A (https=)
ES (1) ES2660914T3 (https=)
GE (1) GEP201706761B (https=)
HR (1) HRP20180341T1 (https=)
HU (1) HUE038220T2 (https=)
IL (1) IL240803B (https=)
JO (1) JO3722B1 (https=)
LT (1) LT2978752T (https=)
ME (1) ME03024B (https=)
MX (1) MX370388B (https=)
MY (1) MY184218A (https=)
PE (1) PE20151860A1 (https=)
PH (1) PH12015502248B1 (https=)
PL (1) PL2978752T3 (https=)
PT (1) PT2978752T (https=)
RS (1) RS56974B1 (https=)
SG (1) SG11201506749XA (https=)
SI (1) SI2978752T1 (https=)
SM (1) SMT201800112T1 (https=)
TN (1) TN2015000397A1 (https=)
TR (1) TR201802632T4 (https=)
TW (1) TWI635084B (https=)
UA (1) UA118965C2 (https=)
UY (1) UY35513A (https=)
WO (1) WO2014160810A1 (https=)
ZA (1) ZA201506484B (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2978752T (pt) 2013-03-29 2018-03-09 Takeda Pharmaceuticals Co Derivados de 6-(5-hidroxi-1h-pirazol-1-il)nicotinamida e o seu uso como inibidores de phd
MA41051B1 (fr) 2014-10-06 2020-11-30 Vertex Pharma Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose
CN109803962B (zh) 2016-09-30 2022-04-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物
MD3551622T2 (ro) 2016-12-09 2021-03-31 Vertex Pharma Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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
MA49631A (fr) 2017-07-17 2020-05-27 Vertex Pharma Méthodes de traitement de la fibrose kystique
JP7121794B2 (ja) 2017-08-02 2022-08-18 バーテックス ファーマシューティカルズ インコーポレイテッド ピロリジン化合物を調製するためのプロセス
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
EP3720849A2 (en) 2017-12-08 2020-10-14 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
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
EP3778583B1 (en) 2018-03-30 2025-06-18 Sumitomo Chemical Company, Limited Heterocyclic compound and arthropod pest control composition containing same
WO2019195739A1 (en) * 2018-04-05 2019-10-10 Alexander Russell Abela 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
TW202140443A (zh) * 2020-03-20 2021-11-01 美商阿克比治療有限公司 Ｐｈｄ抑制劑化合物、組成物及使用方法
WO2021188944A1 (en) * 2020-03-20 2021-09-23 Akebia Therapeutics, Inc. Phd inhibitor compounds, compositions, and their use
AR121621A1 (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
CN117999069A (zh) 2021-05-27 2024-05-07 凯克斯生物制药公司 柠檬酸铁的儿科调配物
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101600710A (zh) * 2006-10-26 2009-12-09 拜耳先灵制药股份公司 取代的二吡啶基二氢吡唑啉酮和它们的应用
CN102333769A (zh) * 2008-12-29 2012-01-25 赛诺菲 2-吡啶-2-基-吡唑-3(2h)-酮的衍生物、其制备和作为hif激活剂的治疗用途
CN102333776A (zh) * 2008-12-29 2012-01-25 赛诺菲 2-吡啶-2-基-吡唑-3(2h)-酮的衍生物、其制备和治疗用途

Family Cites Families (14)

* 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
CA2619262A1 (en) 2005-08-19 2007-02-22 Astrazeneca Ab Pyrazolone derivatives for the treatment of tuberculosis
BRPI0713350B1 (pt) * 2006-06-26 2022-04-12 Akebia Therapeutics Inc Composto, e, composição
AU2007292155B2 (en) * 2006-09-05 2012-11-01 Kyowa Kirin Co., Ltd. Imidazole derivative
DE102006050516A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dihydropyrazolone und ihre Verwendung
KR101578674B1 (ko) 2006-12-29 2015-12-18 아비에 도이치란트 게엠베하 운트 콤파니 카게 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도
DE102007044032A1 (de) 2007-09-14 2009-03-19 Bayer Healthcare Ag Substituierte heterocyclische Verbindungen und ihre Verwendung
JP5557832B2 (ja) * 2008-03-18 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 置換４−ヒドロキシピリジン−５−カルボキサミド
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
PT2978752T (pt) * 2013-03-29 2018-03-09 Takeda Pharmaceuticals Co Derivados de 6-(5-hidroxi-1h-pirazol-1-il)nicotinamida e o seu uso como inibidores de phd

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101600710A (zh) * 2006-10-26 2009-12-09 拜耳先灵制药股份公司 取代的二吡啶基二氢吡唑啉酮和它们的应用
CN102333769A (zh) * 2008-12-29 2012-01-25 赛诺菲 2-吡啶-2-基-吡唑-3(2h)-酮的衍生物、其制备和作为hif激活剂的治疗用途
CN102333776A (zh) * 2008-12-29 2012-01-25 赛诺菲 2-吡啶-2-基-吡唑-3(2h)-酮的衍生物、其制备和治疗用途

Also Published As

Publication number Publication date
HRP20180341T1 (hr) 2018-04-20
HK1217701A1 (en) 2017-01-20
JP6462911B2 (ja) 2019-01-30
NZ711522A (en) 2021-02-26
US20170275271A1 (en) 2017-09-28
DK2978752T3 (en) 2018-03-12
TW201446752A (zh) 2014-12-16
KR20150135794A (ko) 2015-12-03
AP2015008783A0 (en) 2015-10-31
UA118965C2 (uk) 2019-04-10
SMT201800112T1 (it) 2018-05-02
PL2978752T3 (pl) 2018-06-29
LT2978752T (lt) 2018-03-26
PH12015502248A1 (en) 2016-02-01
WO2014160810A1 (en) 2014-10-02
BR112015020350B1 (pt) 2023-04-25
IL240803B (en) 2019-02-28
CR20150517A (es) 2016-01-12
CN105492433A (zh) 2016-04-13
EA201591889A1 (ru) 2016-01-29
SI2978752T1 (en) 2018-04-30
JP2016515582A (ja) 2016-05-30
TR201802632T4 (tr) 2018-03-21
AU2014241183B2 (en) 2018-08-09
TN2015000397A1 (en) 2017-01-03
JP2019069997A (ja) 2019-05-09
US9708296B2 (en) 2017-07-18
US20150224113A1 (en) 2015-08-13
JO3722B1 (ar) 2021-01-31
US20180186772A1 (en) 2018-07-05
US10407409B2 (en) 2019-09-10
CL2015002473A1 (es) 2016-08-26
ECSP15045801A (es) 2017-02-24
IL240803A0 (en) 2015-10-29
CA2903875A1 (en) 2014-10-02
AU2014241183A1 (en) 2015-09-24
JP6282724B2 (ja) 2018-02-21
SG11201506749XA (en) 2015-09-29
ZA201506484B (en) 2017-11-29
UY35513A (es) 2014-10-31
CY1120029T1 (el) 2018-12-12
US20160251337A1 (en) 2016-09-01
GEP201706761B (en) 2017-10-25
EP2978752B1 (en) 2017-11-29
HUE038220T2 (hu) 2018-10-29
PH12015502248B1 (en) 2016-02-01
JP2018083838A (ja) 2018-05-31
EP3336084A1 (en) 2018-06-20
PE20151860A1 (es) 2015-12-16
EA031647B1 (ru) 2019-02-28
EP2978752A1 (en) 2016-02-03
BR112015020350A2 (pt) 2017-07-18
US20140296200A1 (en) 2014-10-02
KR102376354B1 (ko) 2022-04-04
JP6874114B2 (ja) 2021-05-19
MX2015013687A (es) 2016-02-25
PT2978752T (pt) 2018-03-09
MY184218A (en) 2021-03-26
US9944626B2 (en) 2018-04-17
EP3336084B1 (en) 2021-03-17
JP2020073538A (ja) 2020-05-14
US9040522B2 (en) 2015-05-26
TWI635084B (zh) 2018-09-11
US9345713B2 (en) 2016-05-24
RS56974B1 (sr) 2018-05-31
ES2660914T3 (es) 2018-03-26
JP6640978B2 (ja) 2020-02-05
MX370388B (es) 2019-12-11
ME03024B (me) 2018-10-20
CA2903875C (en) 2021-07-20

Similar Documents

Publication Publication Date Title
CN105492433B (zh) 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
CN109195965B (zh) Wdr5蛋白质-蛋白质结合的抑制剂
CN116531380B (zh) 用于治疗癌症的2-杂芳基-3-氧代-2,3-二氢哒嗪-4-甲酰胺
CN114423753A (zh) 作为cd38抑制剂的杂双环酰胺
CN106795147B (zh) 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
CN110312719A (zh) 作为jak家族激酶抑制剂的咪唑并吡咯并吡啶
CN106029076A (zh) 作为bet溴域抑制剂的苯并哌嗪组合物
TW201734020A (zh) 布魯頓氏酪胺酸激酶抑制劑及其使用方法
CN112566910A (zh) 用于治疗由IgE引起的疾病的噻吩衍生物
HK40098354A (zh) 用於治疗癌症的2-杂芳基-3-氧代-2，3-二氢哒嗪-4-甲酰胺
HK40097687B (zh) 用於治疗癌症的2-杂芳基-3-氧代-2 ,3-二氢哒嗪-4-甲酰胺
HK40097687A (zh) 用於治疗癌症的2-杂芳基-3-氧代-2 ,3-二氢哒嗪-4-甲酰胺
HK40110578A (zh) 用作单酰基甘油脂肪酶抑制剂的双环杂环化合物
HK40111682A (zh) 新颖杂环化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant