[go: up one dir, main page]

HUE055662T2 - Laktát-dehidrogenáz kismolekulás inhibitorai és alkalmazási eljárásai - Google Patents

Laktát-dehidrogenáz kismolekulás inhibitorai és alkalmazási eljárásai

Info

Publication number
HUE055662T2
HUE055662T2 HUE15839113A HUE15839113A HUE055662T2 HU E055662 T2 HUE055662 T2 HU E055662T2 HU E15839113 A HUE15839113 A HU E15839113A HU E15839113 A HUE15839113 A HU E15839113A HU E055662 T2 HUE055662 T2 HU E055662T2
Authority
HU
Hungary
Prior art keywords
methods
small molecule
lactate dehydrogenase
molecule inhibitors
inhibitors
Prior art date
Application number
HUE15839113A
Other languages
English (en)
Inventor
David J Maloney
Ajit Jadhav
Ganesha Rai Bantukallu
Kyle Ryan Brimacombe
Bryan T Mott
Shyh Ming Yang
Daniel Jason Urban
Xin Hu
Anton Simeonov
Jennifer L Kouznetsova
Alex Gregory Waterson
Gary Allen Sulikowski
Kwangho Kim
Plamen Christov
Somnath Jana
Victor M Darley-Usmar
Leonard M Neckers
William J Moore
Chi V Dang
Original Assignee
Us Health
Univ Vanderbilt
Univ Pennsylvania
Uab Res Found
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 Us Health, Univ Vanderbilt, Univ Pennsylvania, Uab Res Found filed Critical Us Health
Publication of HUE055662T2 publication Critical patent/HUE055662T2/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
HUE15839113A 2014-12-29 2015-12-29 Laktát-dehidrogenáz kismolekulás inhibitorai és alkalmazási eljárásai HUE055662T2 (hu)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462097226P 2014-12-29 2014-12-29

Publications (1)

Publication Number Publication Date
HUE055662T2 true HUE055662T2 (hu) 2021-12-28

Family

ID=55451544

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE15839113A HUE055662T2 (hu) 2014-12-29 2015-12-29 Laktát-dehidrogenáz kismolekulás inhibitorai és alkalmazási eljárásai

Country Status (12)

Country Link
US (5) US10351532B2 (hu)
EP (2) EP3954685A1 (hu)
JP (3) JP6903580B2 (hu)
CN (1) CN107624112B (hu)
AU (2) AU2015374118B2 (hu)
CA (2) CA3210002A1 (hu)
DK (1) DK3240785T3 (hu)
ES (1) ES2883938T3 (hu)
HU (1) HUE055662T2 (hu)
PL (1) PL3240785T3 (hu)
SI (1) SI3240785T1 (hu)
WO (1) WO2016109559A2 (hu)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3954685A1 (en) * 2014-12-29 2022-02-16 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
EA201891626A1 (ru) * 2016-01-21 2019-04-30 Зибо Биополар Чангшенг Фармасьютикал Ко. Лтд. Ингибиторы тирозинкиназы брутона
WO2018005807A1 (en) * 2016-06-29 2018-01-04 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services 1 h-pyrazol-1 -yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
BR112019014270B1 (pt) 2017-01-10 2023-12-26 Bayer Cropscience Aktiengesellschaft Derivados de heterociclo, seus usos, formulação agroquímica, e método para controlar pragas animais
BR112020003725A2 (pt) 2017-10-06 2020-11-03 Forma Therapeutics, Inc. inibição da peptidase 30 específica de ubiquitina
CA3098628A1 (en) 2018-05-17 2019-11-21 Forma Therapeutics, Inc. Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
EP3833345B1 (en) 2018-08-07 2024-07-17 Kemijski Institut Small molecule-inhibitors of 6-phosphofructo-1-kinase for reducing lactate generation by cancer cells
EP3632908A1 (en) 2018-10-02 2020-04-08 Inventiva Inhibitors of the yap/taz-tead interaction and their use in the treatment of cancer
SI3860989T1 (sl) 2018-10-05 2023-06-30 Forma Therapeutics, Inc. Kondenzirani pirolini,ki delujejo kot zaviralci ubikvitin-specifične proteaze (usp30)
TWI820231B (zh) 2018-10-11 2023-11-01 德商拜耳廠股份有限公司 用於製備經取代咪唑衍生物之方法
PE20211871A1 (es) 2018-11-22 2021-09-21 Qilu Regor Therapeutics Inc Agonistas de glp-1r y usos de los mismos
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
WO2020221899A1 (en) * 2019-05-02 2020-11-05 Université Catholique de Louvain Lactate dehydrogenase inhibitor polypeptides for use in the treatment of cancer
US11725026B2 (en) * 2019-06-28 2023-08-15 The Research Foundation For The State University Of New York Compositions and methods for inhibiting lactate dehydrogenase a activity
WO2021026290A1 (en) 2019-08-07 2021-02-11 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services T cells having enhanced anti-tumor activity
WO2021234543A1 (en) * 2020-05-18 2021-11-25 Chinook Therapeutics Canada, Inc. Substituted pyrazolyl compounds and methods of use thereof
US11752138B2 (en) 2020-05-18 2023-09-12 Vanderbilt University Treating primary or idiopathic hyperoxaluria with small molecule inhibitors of lactate dehydrogenase
CN115996924B (zh) * 2020-05-18 2025-03-07 诺华医药股份公司 取代的吡唑基化合物及其使用方法
WO2021251842A1 (en) * 2020-06-08 2021-12-16 Qatar Foundation For Education, Science And Community Development Targeting of lactate dehydrogenase c, methods of preparing same, and methods of using same in combination with anti-cancer treatments
CN116033828A (zh) 2020-07-02 2023-04-28 拜耳公司 作为害虫防治剂的杂环衍生物
US20240066027A1 (en) * 2020-12-03 2024-02-29 Domain Therapeutics Novel par-2 inhibitors
WO2024212024A1 (en) * 2023-04-09 2024-10-17 Meta Pharmaceuticals (Hk) Limited Novel substituted pyrrole compounds, compositions comprising the substituted pyrrole compound, and methods of use thereof
WO2025011479A1 (en) * 2023-07-13 2025-01-16 Meta Pharmaceuticals (Hk) Limited Pyrazole based inhibitors of LDH and their use in immune and inflammatory diseases
WO2025026738A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft 6-[5-(ethylsulfonyl)-1-methyl-1h-imidazol-4-yl]-7-methyl-3-(pentafluoroethyl)-7h-imidazo[4,5-c]pyridazine derivatives as pesticides

Family Cites Families (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5182289A (en) 1988-06-14 1993-01-26 Schering Corporation Heterobicyclic compounds having antiinflammatory activity
US5128352A (en) * 1989-01-10 1992-07-07 Pfizer Inc. Anti-inflammatory 1-heteroaryl-oxindole-3-carboxamides
US5602113A (en) 1991-02-07 1997-02-11 Boehringer Ingelheim Pharmaceuticals, Inc. Pyridobenzo- and pyridiothieno-diazepines useful for the treatment of HIV infection
MX9205392A (es) 1991-10-29 1993-04-01 Du Pont Triazolcarbozamidas herbicidas y procedimiento para su obtencion.
JPH0680569A (ja) 1992-09-03 1994-03-22 Asahi Chem Ind Co Ltd 血小板凝集阻害剤
US5342851A (en) 1992-10-07 1994-08-30 Mcneil-Ppc, Inc. Substituted thiazole derivatives useful as platelet aggregation inhibitors
DE4405207A1 (de) 1994-02-18 1995-08-24 Bayer Ag N-Pyrazolylaniline und N-Pyrazolylaminopyridine
US20020028936A1 (en) 1999-04-12 2002-03-07 Gerhard Sperl 1,3-disubstituted indolin-2-ones for neoplasia
US6136079A (en) 1999-04-30 2000-10-24 Eastman Kodak Company Dye for ink jet ink
EP1196380A2 (en) 1999-07-15 2002-04-17 NPS Allelix Corp. Indoles and indazoles for the treatment of migraine
US6407238B1 (en) 1999-10-29 2002-06-18 Boehringer Ingelheim Pharmaceuticals, Inc. Process of making substituted pyrazoles
US6436965B1 (en) 2000-03-02 2002-08-20 Merck Frosst Canada & Co. PDE IV inhibiting amides, compositions and methods of treatment
JP2002167531A (ja) 2000-11-29 2002-06-11 Fuji Photo Film Co Ltd インクジェット記録用インク組成物及び画像形成方法
PA8535601A1 (es) 2000-12-21 2002-11-28 Pfizer Derivados benzimidazol y piridilimidazol como ligandos para gabaa
TWI311133B (en) 2001-04-20 2009-06-21 Eisai R&D Man Co Ltd Carboxylic acid derivativeand the salt thereof
AU2002352148A1 (en) 2001-06-29 2003-03-03 Abbott Gmnh & Co. Kg Bis-aryl thiazole derivatives
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US7320995B2 (en) 2002-08-09 2008-01-22 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
EP1534680B1 (en) 2002-08-14 2012-02-22 Pharmaco Investments, Inc. Prenylation inhibitors and methods of their synthesis and use
AU2003294249A1 (en) 2002-11-08 2004-06-03 Trimeris, Inc. Hetero-substituted benzimidazole compounds and antiviral uses thereof
US7589116B2 (en) 2003-04-03 2009-09-15 Merck & Co. Inc. Biaryl substituted pyrazoles as sodium channel blockers
GB0323845D0 (en) 2003-10-10 2003-11-12 Angeletti P Ist Richerche Bio Chemical compounds,compositions and uses
EP1794196A2 (en) 2004-09-22 2007-06-13 Symyx Technologies, Inc. Heterocycle-amine ligands, compositions, complexes, and catalysts, and methods of making and using the same
WO2006052546A2 (en) 2004-11-04 2006-05-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
CA2594773A1 (en) 2005-01-19 2006-07-27 Biolipox Ab Indoles useful in the treatment of inflammation
JP2008527031A (ja) 2005-01-19 2008-07-24 バイオリポックス エービー 炎症の治療に有用なピロロピリジン誘導体
CA2593155A1 (en) 2005-01-19 2006-07-27 Biolipox Ab Indoles useful in the treatment of inflammation
US20100197687A1 (en) 2005-01-19 2010-08-05 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
US20080249091A1 (en) 2005-01-19 2008-10-09 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
WO2006078891A2 (en) 2005-01-21 2006-07-27 Neurogen Corporation Imidazolylmethyl and pyrazolylmethyl heteroaryl derivatives
GB0507198D0 (en) 2005-04-08 2005-05-18 Sb Pharmco Inc Process for preparing bicyclic compounds
US7456292B2 (en) 2005-06-30 2008-11-25 Bexel Pharmaceuticals, Inc. Hydroxamic acid-containing amino acid derivatives
WO2007018508A1 (en) 2005-07-28 2007-02-15 Glaxo Group Limited Novel m3 muscarinic acetycholine receptor antagonists
WO2007018514A1 (en) 2005-07-28 2007-02-15 Glaxo Group Limited Novel m3 muscarinic acetylcholine receptor antagonists
US7615569B2 (en) 2005-08-16 2009-11-10 Icagen, Inc. Inhibitors of ion channels
WO2007038571A2 (en) 2005-09-26 2007-04-05 Smithkline Beecham Corporation Prolyl hydroxylase antagonists
WO2007039773A1 (en) 2005-10-06 2007-04-12 Merck Sharp & Dohme Limited Use of fused pyrrole carboxylic acids for the treatment of neurodegenerative and psychiatric diseases as d-amino acid oxidase inhibitors
WO2007045386A1 (en) 2005-10-17 2007-04-26 Isagro Ricerca S.R.L. Compounds and relative use for the control of phytopathogens
WO2007048732A1 (de) 2005-10-28 2007-05-03 Basf Aktiengesellschaft Verwendung von 5-amino-pyrazolen zur bekämpfung pflanzenpathogener schadpilze, neue 5-amino-pyrazole, verfahren zu ihrer herstellung und sie enthaltende mittel
ITMI20052459A1 (it) 2005-12-22 2007-06-23 Isagro Spa Sali quaternari e relativo uso per il controllo di fitopatogeni
US20080090834A1 (en) 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
GB0614068D0 (en) * 2006-07-14 2006-08-23 Glaxo Group Ltd Compounds
WO2008009924A2 (en) 2006-07-18 2008-01-24 Biolipox Ab Indoles useful in the treatment of inflammation
US7906544B2 (en) 2007-01-26 2011-03-15 North Carolina State University Inhibition of bacterial biofilms with imidazole derivatives
WO2008121861A2 (en) 2007-03-28 2008-10-09 Xenon Pharmaceuticals Inc. Pyrazole and pyrrole compounds useful in treating iron disorders
MX2010001462A (es) 2007-08-27 2010-03-01 Basf Se Compuestos de pirazol para controlar plagas de invertebrados.
US8389567B2 (en) 2007-12-12 2013-03-05 Calcimedica, Inc. Compounds that modulate intracellular calcium
WO2009108551A2 (en) 2008-02-25 2009-09-03 H. Lundbeck A/S Heteroaryl amide analogues
CA2719234A1 (en) 2008-05-08 2009-11-12 Joan M. Fletcher Spiroazaindoles
US9029408B2 (en) 2008-06-16 2015-05-12 Gtx, Inc. Compounds for treatment of cancer
KR20100122513A (ko) * 2008-07-17 2010-11-22 아사히 가세이 파마 가부시키가이샤 질소 함유 복소환 화합물
CN102089302A (zh) * 2008-07-17 2011-06-08 旭化成制药株式会社 含氮二环性杂环化合物
WO2010010186A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
CN102224149B (zh) 2008-09-24 2014-09-10 巴斯夫欧洲公司 防治无脊椎动物害虫的吡唑化合物
AU2009318098B2 (en) 2008-11-20 2015-07-16 Northwestern University Treatment of amyotrophic lateral sclerosis
WO2010065067A1 (en) * 2008-11-20 2010-06-10 Bodymedia, Inc. Method and apparatus for determining critical care parameters
CN101747276B (zh) 2008-11-28 2011-09-07 中国中化股份有限公司 具有含氮五元杂环的醚类化合物及其应用
CN102239162B (zh) 2008-12-04 2014-05-28 弗·哈夫曼-拉罗切有限公司 哒嗪酮衍生物
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
US8569512B2 (en) 2009-03-23 2013-10-29 Merck Sharp & Dohme Corp. P2X3 receptor antagonists for treatment of pain
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
WO2011057942A1 (en) 2009-11-12 2011-05-19 Basf Se Insecticidal methods using pyridine compounds
ES2460915T3 (es) 2009-12-21 2014-05-16 Novartis Ag Piridinas fusionadas con heteroarilo disustituido
WO2011091410A1 (en) 2010-01-25 2011-07-28 Glaxos Smithkline Llc Trpv4 antagonists
JP2013542255A (ja) 2010-11-10 2013-11-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ミネラルコルチコイド受容体アンタゴニストとしてのピリジル尿素
JPWO2012074022A1 (ja) 2010-12-01 2014-05-19 旭硝子株式会社 イリジウムカチオン錯体および発光組成物
WO2012085167A1 (en) 2010-12-22 2012-06-28 Merz Pharma Gmbh & Co. Kgaa Metabotropic glutamate receptor modulators
US20120225061A1 (en) 2011-03-04 2012-09-06 Matthew Burger Tetrasubstituted cyclohexyl compounds as kinase inhibitors
ES2660996T3 (es) 2011-05-03 2018-03-27 PRCL Research Inc. Compuestos para la inflamación y usos relacionados con el sistema inmunitario
US9181231B2 (en) 2011-05-03 2015-11-10 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
WO2012154880A1 (en) 2011-05-09 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases
JP2013040240A (ja) 2011-08-11 2013-02-28 Fujifilm Corp アゾ化合物、アゾ顔料、顔料分散物、着色組成物、カラーフィルター用着色組成物、カラーフィルター、カラーフィルター用着色組成物の調製方法、インクジェット記録用インク、印刷インク、塗料、染料、及び、レジストインク
EP2749562A4 (en) 2011-08-24 2015-01-07 Kissei Pharmaceutical CONDENSED HETEROCYCLIC DERIVATIVE AND ITS PHARMACEUTICAL USE
ITPI20110143A1 (it) 2011-12-20 2013-06-21 Univ Pisa Agenti terapeutici in grado di ridurre la produzione cellulare di acido lattico e composizioni farmaceutiche che comprendono tali composti
US8871778B2 (en) 2012-01-20 2014-10-28 Genosco Substituted pyrimidine compounds and their use as SYK inhibitors
CA2880165C (en) 2012-07-30 2020-02-11 Taisho Pharmaceutical Co., Ltd. Partially saturated nitrogen-containing heterocyclic compound
US10035790B2 (en) 2012-10-19 2018-07-31 Exelixis, Inc. RORγ modulators
US9556145B2 (en) 2012-12-20 2017-01-31 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-ester orexin receptor antagonists
US9643955B2 (en) 2012-12-20 2017-05-09 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-nitrile-4-substituted orexin receptor antagonists
US9765057B2 (en) 2012-12-20 2017-09-19 Merck Sharp & Dohme Corp. 3-ester-4 substituted orexin receptor antagonists
FR3001219A1 (fr) 2013-01-22 2014-07-25 Centre Nat Rech Scient Inhibiteurs de kinases
US10201614B2 (en) 2013-03-15 2019-02-12 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
EP2980094B1 (en) 2013-03-29 2019-05-01 Konica Minolta, Inc. Isomer-mixture metal complex composition, organic electroluminescent element, illuminator, and display device
WO2014173880A1 (en) 2013-04-22 2014-10-30 Syngenta Participations Ag Novel microbiocides
WO2014176475A2 (en) 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof
US9169221B2 (en) 2013-04-29 2015-10-27 Comsats Institute Of Information Technology Dihydro 1,4-benzoxazines and method of synthesizing the same using sulfonium salts
EP3954685A1 (en) 2014-12-29 2022-02-16 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Small molecule inhibitors of lactate dehydrogenase and methods of use thereof

Also Published As

Publication number Publication date
EP3240785B1 (en) 2021-07-07
CN107624112A (zh) 2018-01-23
PL3240785T3 (pl) 2021-12-06
AU2020257163A1 (en) 2020-11-19
EP3240785A2 (en) 2017-11-08
AU2015374118B2 (en) 2020-07-23
US20180273488A1 (en) 2018-09-27
CN107624112B (zh) 2022-03-04
US20210323928A1 (en) 2021-10-21
ES2883938T3 (es) 2021-12-09
AU2020257163B2 (en) 2022-06-30
US11247971B2 (en) 2022-02-15
SI3240785T1 (sl) 2021-11-30
EP3954685A1 (en) 2022-02-16
WO2016109559A3 (en) 2016-08-25
WO2016109559A2 (en) 2016-07-07
JP2021152064A (ja) 2021-09-30
JP6903580B2 (ja) 2021-07-14
US10351532B2 (en) 2019-07-16
CA3210002A1 (en) 2016-07-07
CA2978823A1 (en) 2016-07-07
DK3240785T3 (da) 2021-09-27
US20240368087A1 (en) 2024-11-07
US20220220078A1 (en) 2022-07-14
US10961200B2 (en) 2021-03-30
JP2023153302A (ja) 2023-10-17
US11897845B2 (en) 2024-02-13
AU2015374118A1 (en) 2017-07-20
JP2018503631A (ja) 2018-02-08
JP7337883B2 (ja) 2023-09-04
US20200002285A1 (en) 2020-01-02
CA2978823C (en) 2023-10-10

Similar Documents

Publication Publication Date Title
PL3240785T3 (pl) Inhibitory drobnocząsteczkowe dehydrogenazy mleczanowej i sposoby ich wykorzystania
IL285154A (en) Therapeutic inhibitor of lactate dehydrogenase and their factors
IL250415B (en) Antibodies against pd-l and methods of using them
EP3160498A4 (en) Il-15-based molecules and methods of use thereof
ZA201605639B (en) Hppd variants and methods of use
IL259801A (en) ezh2 inhibitors and methods of using them
GB201418350D0 (en) Dispenser and methods of use thereof
PL3218005T3 (pl) Związki oddziałujące z glikanami i sposoby ich zastosowania
HUE056172T2 (hu) Szelenoorganikus vegyületeket tartalmazó készítmények és eljárások alkalmazásukra
ZA201606243B (en) Hppd variants and methods of use
LT3089971T (lt) Junginiai ir panaudojimo būdai
EP3226955A4 (en) Self-anchoring catheters and methods of use
EP3177327A4 (en) Inhibitors of myh7b and uses thereof
EP3190886A4 (en) Compositions and methods of use thereof
SG11201509738RA (en) Methods of treatment and compositions with xanthine oxidase inhibitors
EP3137873A4 (en) Viscometer and methods of use thereof
SG11201605915WA (en) Furo-3-carboxamide derivatives and methods of use
EP3134108A4 (en) Agents and methods of treatment
ZA201606450B (en) Compounds and their methods of use
HK1243404A1 (zh) 色酰胺組合物和使用方法
IL266344A (en) Inhibitors of mtor-deptor interactions and methods of use thereof
EP3142999A4 (en) Methods and compositions of dasotraline for treatment of adhd
GB201417248D0 (en) Compostion and methods of treatment
EP3236966A4 (en) Combination of raf inhibitors and taxanes
GB201403697D0 (en) Compounds and methods of use