BR112016030730A8 - composto - Google Patents

composto

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Publication number
BR112016030730A8
BR112016030730A8 BR112016030730A BR112016030730A BR112016030730A8 BR 112016030730 A8 BR112016030730 A8 BR 112016030730A8 BR 112016030730 A BR112016030730 A BR 112016030730A BR 112016030730 A BR112016030730 A BR 112016030730A BR 112016030730 A8 BR112016030730 A8 BR 112016030730A8
Authority
BR
Brazil
Prior art keywords
methods
gls1
inhibiting
activity
treatment
Prior art date
Application number
BR112016030730A
Other languages
English (en)
Other versions
BR112016030730A2 (pt
BR112016030730B1 (pt
Inventor
Yau Anne
Czako Barbara
Lawrence Carroll Christopher
Liu Gang
P Burke Jason
Theroff Jay
Le Kang
Emilia Di Francesco Maria
Hamilton Matthew
P Soth Michael
Jones Philip
Lewis Richard
Heffernan Timothy
Mcafoos Timothy
Palmer Wylie
Herrera Zachary
Kang Zhijun
Original Assignee
Univ Texas
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 Univ Texas filed Critical Univ Texas
Publication of BR112016030730A2 publication Critical patent/BR112016030730A2/pt
Publication of BR112016030730A8 publication Critical patent/BR112016030730A8/pt
Publication of BR112016030730B1 publication Critical patent/BR112016030730B1/pt

Links

Classifications

    • 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
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal 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)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

composto, composição, método para inibição da atividade de gls1 em uma amostra biológica, métodos para tratamento de um distúrbio mediado por gls1 em um sujeito com necessidade do mesmo, e uso de um composto . a presente invenção descreve compostos e composições utéis no tratamento de doenças mediadas por gls1, tais como câncer, tendo a estrutura da fórmula i. também são providos métodos de inibição da atividade de gls1 em um ser humano ou animal. consequentemente, os presentes inventores divulgam novas composições e métodos para a inibição da atividade de glutaminase. a presente divulgação se refere a novos compostos e composições heterocíclicas e à sua utilização como fármacos para o tratamento de doenças. também são providos métodos de inibição da atividade de gls1 em um ser humano ou animal para o tratamento de doenças, tais como câncer.
BR112016030730-5A 2014-07-03 2015-07-02 Composto BR112016030730B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462020539P 2014-07-03 2014-07-03
US62/020,539 2014-07-03
PCT/US2015/039134 WO2016004404A2 (en) 2014-07-03 2015-07-02 Gls1 inhibitors for treating disease

Publications (3)

Publication Number Publication Date
BR112016030730A2 BR112016030730A2 (pt) 2017-08-22
BR112016030730A8 true BR112016030730A8 (pt) 2021-07-20
BR112016030730B1 BR112016030730B1 (pt) 2023-05-02

Family

ID=55020106

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016030730-5A BR112016030730B1 (pt) 2014-07-03 2015-07-02 Composto

Country Status (17)

Country Link
US (5) US9809588B2 (pt)
EP (2) EP3164394B1 (pt)
JP (2) JP6619758B2 (pt)
CN (1) CN107074805B (pt)
AU (1) AU2015283850B2 (pt)
BR (1) BR112016030730B1 (pt)
CA (1) CA2953989C (pt)
CY (1) CY1123216T1 (pt)
DK (1) DK3164394T3 (pt)
ES (1) ES2788449T3 (pt)
HU (1) HUE049600T2 (pt)
LT (1) LT3164394T (pt)
NZ (1) NZ726695A (pt)
PL (1) PL3164394T3 (pt)
PT (1) PT3164394T (pt)
SI (1) SI3164394T1 (pt)
WO (1) WO2016004404A2 (pt)

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BR112016030730B1 (pt) * 2014-07-03 2023-05-02 Board Of Regents, The University Of Texas System Composto
WO2016004417A1 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
US10125128B2 (en) 2015-06-30 2018-11-13 Board Of Regents, The University Of Texas System GLS1 inhibitors for treating disease
AU2016378746B2 (en) 2015-12-22 2021-05-20 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
JP7120549B2 (ja) * 2016-12-15 2022-08-17 小野薬品工業株式会社 Ｔｒｅｋ（ｔｗｉｋ関連ｋチャネル）チャネルのアクチベータ
EP3697764A4 (en) * 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY
CN109988124B (zh) * 2017-12-29 2024-01-09 杭州健昵福生物科技有限公司 一种含氧族元素二唑或四氮唑结构的肾型谷氨酰胺酶变构位点的抑制剂
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BR112016030730B1 (pt) 2014-07-03 2023-05-02 Board Of Regents, The University Of Texas System Composto
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AU2016378746B2 (en) 2015-12-22 2021-05-20 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
EP3697764A4 (en) 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY

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US11370786B2 (en) 2022-06-28
CA2953989C (en) 2023-10-10
CA2953989A1 (en) 2016-01-07
EP3677579A1 (en) 2020-07-08
SI3164394T1 (sl) 2020-08-31
JP2020059715A (ja) 2020-04-16
NZ726695A (en) 2024-02-23
EP3164394B1 (en) 2020-04-01
US20200407353A1 (en) 2020-12-31
PT3164394T (pt) 2020-05-08
HUE049600T2 (hu) 2020-10-28
US20230124815A1 (en) 2023-04-20
LT3164394T (lt) 2020-05-25
EP3164394A2 (en) 2017-05-10
US20160009704A1 (en) 2016-01-14
CY1123216T1 (el) 2021-10-29
JP6619758B2 (ja) 2019-12-11
CN107074805A (zh) 2017-08-18
US20170291895A1 (en) 2017-10-12
BR112016030730A2 (pt) 2017-08-22
EP3164394A4 (en) 2018-02-28
US10344025B2 (en) 2019-07-09
PL3164394T3 (pl) 2020-09-07
WO2016004404A2 (en) 2016-01-07
CN107074805B (zh) 2021-02-26
AU2015283850A1 (en) 2016-12-15
US11958849B2 (en) 2024-04-16
DK3164394T3 (da) 2020-05-04
US10766892B2 (en) 2020-09-08
US9809588B2 (en) 2017-11-07
AU2015283850B2 (en) 2020-06-04
BR112016030730B1 (pt) 2023-05-02
WO2016004404A3 (en) 2016-03-24
ES2788449T3 (es) 2020-10-21
US20190270736A1 (en) 2019-09-05
JP2017522294A (ja) 2017-08-10

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