CO2017011506A2 - Derivados de pirazol útiles como inhibidores de proteína activadora de 5-lipoxigenasa (flap) - Google Patents

Derivados de pirazol útiles como inhibidores de proteína activadora de 5-lipoxigenasa (flap)

Info

Publication number
CO2017011506A2
CO2017011506A2 CONC2017/0011506A CO2017011506A CO2017011506A2 CO 2017011506 A2 CO2017011506 A2 CO 2017011506A2 CO 2017011506 A CO2017011506 A CO 2017011506A CO 2017011506 A2 CO2017011506 A2 CO 2017011506A2
Authority
CO
Colombia
Prior art keywords
flap
inhibitors
pyrazole derivatives
derivatives useful
activator protein
Prior art date
Application number
CONC2017/0011506A
Other languages
English (en)
Inventor
Johan Olof Broddefalk
Hans Fredrik Emtenäs
Kenneth Lars Granberg
Malin Anita Lemurell
Daniel Tor Pettersen
Alleyn Thomas Plowright
Lars Johan Andreas Ulander
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CO2017011506A2 publication Critical patent/CO2017011506A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/46—Oxygen atom in position 3 or 5 and nitrogen atom in position 4
    • C07D231/50—Acylated on said nitrogen atom
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

R E S U M E N La presente solicitud se refiere a compuestos de fórmula (I) a su utilidad para tratar y/o prevenir afecciones clínicas incluyendo enfermedades cardiovasculares (ECV), a métodos para su uso terapéutico, a composiciones farmacéuticas que los contienen y a procesos para preparar dichos compuestos.
CONC2017/0011506A 2015-05-04 2017-11-09 Derivados de pirazol útiles como inhibidores de proteína activadora de 5-lipoxigenasa (flap) CO2017011506A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562156424P 2015-05-04 2015-05-04
PCT/EP2016/059848 WO2016177703A1 (en) 2015-05-04 2016-05-03 Pyrazole derivatives useful as 5-lipoxygenase activating protein (flap) inhibitors

Publications (1)

Publication Number Publication Date
CO2017011506A2 true CO2017011506A2 (es) 2018-01-31

Family

ID=55910253

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0011506A CO2017011506A2 (es) 2015-05-04 2017-11-09 Derivados de pirazol útiles como inhibidores de proteína activadora de 5-lipoxigenasa (flap)

Country Status (38)

Country Link
US (5) US10183947B2 (es)
EP (2) EP3292105B1 (es)
JP (1) JP6564062B2 (es)
KR (1) KR102623474B1 (es)
CN (1) CN107646036B (es)
AR (1) AR104512A1 (es)
AU (1) AU2016258874B2 (es)
BR (1) BR112017022757B1 (es)
CA (1) CA2983668C (es)
CL (1) CL2017002660A1 (es)
CO (1) CO2017011506A2 (es)
CR (1) CR20170513A (es)
CY (2) CY1122689T1 (es)
DK (2) DK3292105T3 (es)
DO (1) DOP2017000244A (es)
EA (1) EA032221B1 (es)
ES (2) ES2902139T3 (es)
GT (1) GT201700220A (es)
HK (1) HK1245255A1 (es)
HR (2) HRP20211993T1 (es)
HU (2) HUE047445T2 (es)
IL (1) IL255069B (es)
LT (1) LT3670499T (es)
ME (1) ME03663B (es)
MX (1) MX2017013571A (es)
MY (1) MY186647A (es)
PE (1) PE20180247A1 (es)
PH (1) PH12017502112B1 (es)
PL (2) PL3670499T3 (es)
PT (2) PT3670499T (es)
RS (2) RS59671B1 (es)
SG (1) SG11201708558RA (es)
SI (2) SI3292105T1 (es)
SV (1) SV2017005549A (es)
TN (1) TN2017000458A1 (es)
TW (1) TWI718146B (es)
WO (1) WO2016177703A1 (es)
ZA (1) ZA201708189B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3292105T1 (sl) * 2015-05-04 2020-01-31 Astrazeneca Ab Derivati pirazola uporabni kot inhibitorji proteina, ki aktivira 5-lipoksigenazo (FLAP)
CA3040341C (en) 2016-10-28 2024-03-05 Astrazeneca Ab Crystalline form of (1r,2r)-2-[4-(3-methy1-1h-pyrazol-5-yl)benzoyl]-n-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide
CN110169969B (zh) * 2019-06-28 2022-05-27 南京医科大学 Mk571在制备预防和治疗心脏病药物中应用
CN111084775A (zh) * 2020-02-17 2020-05-01 牡丹江医学院 一种用于治疗癫痫的药物组合物
CN111419800B (zh) * 2020-04-23 2021-03-19 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 用于治疗红斑狼疮的药物制剂及其制备方法
CN111643498B (zh) * 2020-07-20 2021-05-07 黑龙江中医药大学 一种治疗肾结石的药物组合物及其用途
CN111714499B (zh) * 2020-07-27 2021-05-11 黑龙江中医药大学 一种用于治疗多囊卵巢综合征的药物组合物

Family Cites Families (11)

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AP9400632A0 (en) 1993-04-29 1995-10-07 Zeneca Ltd Ether derivatives.
US5773422A (en) 1996-01-29 1998-06-30 Komer; Gene Avermectin formulation
CA2572750A1 (en) * 2003-09-10 2005-03-17 Anil Koul Heterobicyclic compounds as pharmaceutically active agents
GB2431927B (en) 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
TW200815351A (en) * 2006-05-02 2008-04-01 Astrazeneca Ab Novel compounds
US20100204282A1 (en) 2007-02-05 2010-08-12 Hutchinson John H Reverse indoles as 5-lipoxygenase-activating protein (FLAP) inhibitors
GB0702456D0 (en) * 2007-02-08 2007-03-21 Astrazeneca Ab New combination
MX2009011357A (es) * 2007-04-20 2009-11-05 Schering Corp Derivados de tetrahidropirido[4,3-d] pirimidinona y metodos de uso de los mismos.
NZ580801A (en) * 2007-05-10 2012-09-28 Bristol Myers Squibb Co Aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
EP2207547A4 (en) 2007-10-05 2010-11-17 Amira Pharmaceuticals Inc PROTEIN INHIBITORS THAT ACTIVATE 5-LIPOXYGENASE
SI3292105T1 (sl) * 2015-05-04 2020-01-31 Astrazeneca Ab Derivati pirazola uporabni kot inhibitorji proteina, ki aktivira 5-lipoksigenazo (FLAP)

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DK3292105T3 (da) 2019-12-09
CN107646036A (zh) 2018-01-30
TN2017000458A1 (en) 2019-04-12
EP3292105B1 (en) 2019-10-02
WO2016177703A1 (en) 2016-11-10
ES2760466T3 (es) 2020-05-14
EA032221B1 (ru) 2019-04-30
US10183947B2 (en) 2019-01-22
US10508119B2 (en) 2019-12-17
PT3670499T (pt) 2021-12-24
RS62729B1 (sr) 2022-01-31
TW201713625A (zh) 2017-04-16
KR20180002784A (ko) 2018-01-08
US20190084991A1 (en) 2019-03-21
US20180237439A1 (en) 2018-08-23
MY186647A (en) 2021-08-03
CL2017002660A1 (es) 2018-04-13
PT3292105T (pt) 2019-12-13
US20230219967A1 (en) 2023-07-13
HRP20211993T1 (hr) 2022-04-01
SI3292105T1 (sl) 2020-01-31
SG11201708558RA (en) 2017-11-29
CY1125179T1 (el) 2023-03-24
KR102623474B1 (ko) 2024-01-09
JP2018514535A (ja) 2018-06-07
AR104512A1 (es) 2017-07-26
PH12017502112A1 (en) 2018-05-07
SI3670499T1 (sl) 2022-02-28
US11691978B2 (en) 2023-07-04
CA2983668C (en) 2023-06-27
EP3670499B1 (en) 2021-09-29
HRP20192172T1 (hr) 2020-02-21
CA2983668A1 (en) 2016-11-10
HUE047445T2 (hu) 2020-04-28
EP3670499A1 (en) 2020-06-24
IL255069A0 (en) 2017-12-31
TWI718146B (zh) 2021-02-11
DK3670499T3 (da) 2022-01-03
ME03663B (me) 2020-07-20
US11001589B2 (en) 2021-05-11
RS59671B1 (sr) 2020-01-31
GT201700220A (es) 2018-12-19
PH12017502112B1 (en) 2018-05-07
MX2017013571A (es) 2018-02-26
HK1245255A1 (zh) 2018-08-24
PL3670499T3 (pl) 2022-02-14
EA201792341A1 (ru) 2018-05-31
ES2902139T3 (es) 2022-03-25
PL3292105T3 (pl) 2020-04-30
PE20180247A1 (es) 2018-02-02
CY1122689T1 (el) 2021-03-12
NZ737672A (en) 2020-11-27
CN107646036B (zh) 2020-05-19
CR20170513A (es) 2018-02-13
AU2016258874A1 (en) 2017-12-14
SV2017005549A (es) 2018-03-12
ZA201708189B (en) 2018-11-28
IL255069B (en) 2019-12-31
US20200157113A1 (en) 2020-05-21
US20210355127A1 (en) 2021-11-18
EP3292105A1 (en) 2018-03-14
BR112017022757B1 (pt) 2023-02-23
JP6564062B2 (ja) 2019-08-21
AU2016258874B2 (en) 2020-04-30
LT3670499T (lt) 2021-12-27
BR112017022757A2 (pt) 2018-07-17
HUE056875T2 (hu) 2022-03-28
DOP2017000244A (es) 2017-11-15

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