[go: up one dir, main page]

EA201691135A1 - Новые ингибиторы глутаминазы - Google Patents

Новые ингибиторы глутаминазы

Info

Publication number
EA201691135A1
EA201691135A1 EA201691135A EA201691135A EA201691135A1 EA 201691135 A1 EA201691135 A1 EA 201691135A1 EA 201691135 A EA201691135 A EA 201691135A EA 201691135 A EA201691135 A EA 201691135A EA 201691135 A1 EA201691135 A1 EA 201691135A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new
glutaminase inhibitors
methods
glutaminase
inhibitors
Prior art date
Application number
EA201691135A
Other languages
English (en)
Other versions
EA033163B1 (ru
Inventor
Прашант Кашинат Бхавар
Сваруп Кумар Венката Сатья Ваккаланка
Срикант Висванадха
Мерикапуди Гаятри Сваруп
Говиндараджулу Бабу
Original Assignee
Ризен Фармасьютикалз Са
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52478027&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201691135(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ризен Фармасьютикалз Са filed Critical Ризен Фармасьютикалз Са
Publication of EA201691135A1 publication Critical patent/EA201691135A1/ru
Publication of EA033163B1 publication Critical patent/EA033163B1/ru

Links

Classifications

    • 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
    • C07D417/06Heterocyclic 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
    • 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
    • A61K31/433Thidiazoles
    • 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
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4545Non 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines 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
    • A61K31/50Pyridazines; 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
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/08Antibacterial agents for leprosy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen 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
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • C07D417/08Heterocyclic 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 alicyclic rings
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)

Abstract

В настоящем изобретении предложены соединения формулы (I)-(III) в качестве ингибиторов глутаминазы, способы их получения, содержащие их фармацевтические композиции, а также способы лечения, предотвращения и/или ослабления заболеваний или нарушений, в которых задействован глутамин.
EA201691135A 2014-01-06 2015-01-05 Ингибиторы глутаминазы EA033163B1 (ru)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
IN39CH2014 2014-01-06
IN36CH2014 2014-01-06
IN2647CH2014 2014-05-29
IN2639CH2014 2014-05-29
IN2783CH2014 2014-06-06
IN3525CH2014 2014-07-18
IN3612CH2014 2014-07-24
IN3613CH2014 2014-07-24
IN5438CH2014 2014-10-31
PCT/IB2015/050076 WO2015101958A2 (en) 2014-01-06 2015-01-05 Novel inhibitors of glutaminase

Publications (2)

Publication Number Publication Date
EA201691135A1 true EA201691135A1 (ru) 2016-12-30
EA033163B1 EA033163B1 (ru) 2019-09-30

Family

ID=52478027

Family Applications (3)

Application Number Title Priority Date Filing Date
EA201991183A EA201991183A1 (ru) 2014-01-06 2015-01-05 Новые ингибиторы глутаминазы
EA201691135A EA033163B1 (ru) 2014-01-06 2015-01-05 Ингибиторы глутаминазы
EA201691134A EA035499B1 (ru) 2014-01-06 2015-01-05 Новые ингибиторы глутаминазы

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201991183A EA201991183A1 (ru) 2014-01-06 2015-01-05 Новые ингибиторы глутаминазы

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201691134A EA035499B1 (ru) 2014-01-06 2015-01-05 Новые ингибиторы глутаминазы

Country Status (16)

Country Link
US (4) US20160297761A1 (ru)
EP (2) EP3092235A2 (ru)
JP (3) JP6783663B2 (ru)
KR (3) KR20160100407A (ru)
CN (5) CN112920180A (ru)
AU (1) AU2015204210B2 (ru)
BR (1) BR112016015706A8 (ru)
CA (2) CA2934700A1 (ru)
CL (1) CL2016001715A1 (ru)
DK (1) DK3092236T3 (ru)
EA (3) EA201991183A1 (ru)
ES (1) ES2833576T3 (ru)
IL (1) IL246362B (ru)
SG (1) SG11201605478XA (ru)
WO (2) WO2015101957A2 (ru)
ZA (1) ZA201604272B (ru)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2922832B1 (en) 2012-11-21 2019-10-09 Agios Pharmaceuticals, Inc. Glutaminase inhibitors and methods of use
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
CN112920180A (zh) * 2014-01-06 2021-06-08 理森制药股份公司 谷氨酰胺酶抑制剂
CN106231900B (zh) * 2014-03-21 2019-05-28 阿吉奥斯制药公司 化合物及其使用方法
HRP20192056T1 (hr) * 2014-04-30 2020-02-21 Pfizer Inc. Derivati diheterocikla vezani na cikloalkil
HUE049600T2 (hu) 2014-07-03 2020-10-28 Univ Texas GLS1 inhibitorok betegségek kezelésére
US10660861B2 (en) 2014-07-09 2020-05-26 The Johns Hopkins University Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy
EP3316887B1 (en) 2015-06-30 2020-04-08 Board of Regents, The University of Texas System Gls1 inhibitors for treating disease
CN112920092B (zh) 2015-07-31 2024-04-26 约翰霍普金斯大学 谷氨酰胺类似物的前药
US10842763B2 (en) 2015-07-31 2020-11-24 The Johns Hopkins University Methods for cancer and immunotherapy using prodrugs of glutamine analogs
EP3328376A4 (en) * 2015-07-31 2019-03-13 The Johns Hopkins University Methods and compositions for treating metabolic reprogramming disorders
WO2017021177A1 (en) * 2015-08-04 2017-02-09 Universitat De Barcelona Pharmaceutical combinations for use in the treatment of cancer
GB201520959D0 (en) * 2015-11-27 2016-01-13 Astrazeneca Ab And Cancer Res Technology Ltd Bis-pyridazine compounds and their use in treating cancer
US10040789B2 (en) 2015-11-30 2018-08-07 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
TW201730188A (zh) * 2015-11-30 2017-09-01 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
US10323028B2 (en) * 2015-11-30 2019-06-18 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
WO2017109793A1 (en) * 2015-12-21 2017-06-29 Council Of Scientific & Industrial Research Novel 1,2,3 triazole-thiazole compounds, process for preparation and use thereof
KR102777513B1 (ko) 2015-12-22 2025-03-06 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 (r)-1-(4-(6-(2-(4-(3,3-디플루오로시클로부톡시)-6-메틸피리딘-2-일)아세트아미도)피리다진-3-일)-2-플루오로부틸)-n-메틸-1h-1,2,3-트리아졸-4-카르복사미드의 염 형태 및 다형체
CN107474024B (zh) * 2016-06-08 2022-12-13 北京赛林泰医药技术有限公司 一种谷氨酰酶抑制剂及其组合物和用途
WO2018102715A1 (en) * 2016-12-02 2018-06-07 Indiana University Research And Technology Corporation Compositions and methods for treating and/or reducing corneal dystrophy
CN110381956B (zh) * 2017-01-27 2024-02-02 康奈尔大学 两性离子修饰的聚合物和水凝胶
EP3640250B1 (en) * 2017-06-13 2021-12-15 Medshine Discovery Inc. Compound as gls1 inhibitor
JP7361687B2 (ja) 2017-10-18 2023-10-16 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム グルタミナーゼ阻害薬療法
HRP20230502T1 (hr) 2017-10-27 2023-09-15 Boehringer Ingelheim International Gmbh Inhibitori trpc6
US20190269705A1 (en) * 2017-11-27 2019-09-05 Regents Of The University Of Minnesota Methods and materials for treating graft versus host disease
WO2020028115A1 (en) * 2018-07-31 2020-02-06 Eli Lilly And Company 5-methyl-4-fluoro-thiazol-2-yl compounds
JP7606960B2 (ja) 2018-09-19 2024-12-26 バイオジェン・エムエイ・インコーポレイテッド O-糖タンパク質-2-アセトアミド-2-デオキシ-3-d-グルコピラノシダーゼ阻害剤
US20220119768A1 (en) * 2018-11-08 2022-04-21 The University Of Tokyo Method for removing senescent cell, and method for preparing senescent cell
CN109223778B (zh) * 2018-11-16 2021-07-27 上海市肺科医院 C24h24n6o2s3在制备抗结核菌药物中的用途
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
EP3962903A1 (en) 2019-05-01 2022-03-09 Boehringer Ingelheim International GmbH (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate
CN110746416A (zh) * 2019-09-05 2020-02-04 中国药科大学 含有三氮唑结构的谷氨酰胺酶gls1抑制剂或其可药用的盐、其制备方法及用途
JP2023509452A (ja) 2020-01-03 2023-03-08 バーグ エルエルシー がんを処置するためのube2kモジュレータとしての多環式アミド
CN111643669A (zh) * 2020-06-30 2020-09-11 广东省中医院(广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院) 谷氨酰胺酶抑制剂在制备治疗银屑病的药物中的应用
MX2023001818A (es) 2020-08-13 2023-03-13 Boehringer Ingelheim Int Compuestos para usarse en tratamiento de deterioro cognitivo asociado con la esquizofrenia.
KR20230088761A (ko) 2020-10-13 2023-06-20 베링거 인겔하임 인터내셔날 게엠베하 재가공하는 방법
CA3217423A1 (en) 2021-06-16 2022-12-22 Jeffrey M. Schkeryantz Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases
CN114805346A (zh) * 2021-07-08 2022-07-29 成都硕德药业有限公司 杂环类衍生物、其制备方法及用途
CN116023375A (zh) * 2021-10-25 2023-04-28 成都苑东生物制药股份有限公司 一种杂环类衍生物、其制备方法及用途
CA3236890A1 (en) 2021-12-14 2023-06-22 Boehringer Ingelheim International Gmbh Aldosterone synthase inhibitors for treating chronic kidney disease
WO2023212718A2 (en) * 2022-04-29 2023-11-02 Cornell University Methods of treating a virus infection and methods of inhibiting viral replication
CN114874186B (zh) * 2022-05-16 2023-07-11 深圳大学 一种谷氨酰胺酰基环化酶同工酶抑制剂及其制备方法与应用
WO2024233839A1 (en) * 2023-05-10 2024-11-14 Leal Therapeutics, Inc. Small molecule inhibitors of glutaminase
CN119192178A (zh) * 2024-09-23 2024-12-27 浙江师范大学行知学院 一种氨基脲衍生物及其制备方法与应用

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2104783A1 (en) * 1970-07-14 1972-04-21 Berlin Chemie Veb 2,5-disubstd 2-amino-1,3,4-thiadiazoles-from 4-substd 1-acylthiosemic - virustatics
JPH0358980A (ja) * 1989-07-28 1991-03-14 Canon Inc 液晶性化合物、これを含む液晶組成物、およびこれを使用した液晶素子
EP0656210A1 (en) 1993-11-19 1995-06-07 Takeda Chemical Industries, Ltd. Imidazole derivatives as glutaminose inhibitors
WO1999009825A1 (en) 1997-08-29 1999-03-04 Elan Pharmaceuticals, Inc. Method of preventing neuronal death
AU4030200A (en) 1999-04-02 2000-10-23 Children's Hospital Of Los Angeles Use of asparaginase and glutaminase to treat autoimmune disease and graft versushost disease
US6451828B1 (en) 2000-08-10 2002-09-17 Elan Pharmaceuticals, Inc. Selective inhibition of glutaminase by bis-thiadiazoles
NO315152B1 (no) 2001-06-28 2003-07-21 Tomm Slater Anordning for rensing av luft
EP1434576A4 (en) 2001-09-13 2006-03-29 Kenneth E Miller METHOD FOR RELIEVING PAIN
SE0300456D0 (sv) * 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
EP1597256A1 (en) * 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
DE10326821A1 (de) 2003-06-11 2005-01-05 Medical Enzymes Ag Pharmazeutische Kombinationspräparate zur Krebstherapie
WO2007001395A2 (en) 2004-10-04 2007-01-04 University Of South Carolina Prevention and treatment of influenza with glutamine antagonist agents
JP4871289B2 (ja) 2005-10-06 2012-02-08 日本曹達株式会社 環状アミン化合物および有害生物防除剤
AU2007247321B2 (en) 2006-05-10 2013-06-20 New Medical Enzymes Ag GlutaDON
TW200819437A (en) * 2006-08-17 2008-05-01 Astrazeneca Ab Chemical compounds
ZA200904281B (en) * 2006-12-28 2010-08-25 Metabolex Inc Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
KR20100033419A (ko) 2007-07-19 2010-03-29 메타볼렉스, 인코포레이티드 당뇨병 및 대사 장애의 치료를 위한 rup3 또는 gpr119 수용체의 작용제로서 n-아자시클릭 치환된 피롤, 피라졸, 이미다졸, 트리아졸 및 테트라졸 유도체
WO2009126535A1 (en) * 2008-04-07 2009-10-15 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2009131127A1 (ja) * 2008-04-22 2009-10-29 第一三共株式会社 5-ヒドロキシピリミジン-4-カルボキサミド化合物
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
EP2311822A4 (en) 2008-08-01 2011-08-31 Nippon Chemiphar Co GPR119 AGONIST
WO2010033871A2 (en) 2008-09-18 2010-03-25 The Johns Hopkins University Compositions and methods targeting glutaminase
US20110224187A1 (en) * 2008-10-16 2011-09-15 Anandan Palani Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof
WO2010048149A2 (en) * 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
JP2010138082A (ja) * 2008-12-09 2010-06-24 Nippon Soda Co Ltd 環状アミン化合物またはその塩、並びに有害生物防除剤
US10532034B2 (en) 2009-03-25 2020-01-14 Cornell University Inhibition of glutaminase C
WO2011025006A1 (ja) * 2009-08-31 2011-03-03 日本ケミファ株式会社 Gpr119作動薬
PL2496567T3 (pl) * 2009-11-05 2018-01-31 Rhizen Pharmaceuticals S A Nowe benzopiranowe modulatory kinazy
ES2362770B1 (es) 2009-12-24 2012-05-22 Universidad De Sevilla Uso de compuesto n-fenil-n'-(3-metil-2-butenil)tiourea para la elaboración de medicamentos destinados al tratamiento de la encefalopatía hepática.
WO2011093501A1 (ja) * 2010-02-01 2011-08-04 日本ケミファ株式会社 Gpr119作動薬
US20130109643A1 (en) 2010-05-10 2013-05-02 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
AU2011254242B2 (en) * 2010-05-17 2015-10-29 Incozen Therapeutics Pvt. Ltd. Novel 3,5-disubstitued-3H-imidazo[4,5-b]pyridine and 3,5- disubstitued -3H-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases
WO2012006506A1 (en) 2010-07-09 2012-01-12 Massachusetts Institute Of Technology Metabolic gene, enzyme, and flux targets for cancer therapy
US20130252983A1 (en) 2010-09-10 2013-09-26 Cornell University Activating phosphorylation site on glutaminase c
JP2014094886A (ja) * 2011-02-28 2014-05-22 Nippon Chemiphar Co Ltd Gpr119作動薬
CN103030597B (zh) 2011-09-30 2014-10-01 南昌滨西科技有限公司 肾脏型谷氨酰胺酶抑制剂及其制备方法和用途
AR088256A1 (es) 2011-10-08 2014-05-21 Novartis Ag Derivados de carbamato / urea como antagonistas del receptor h3
US8604016B2 (en) 2011-11-21 2013-12-10 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
KR20190127971A (ko) * 2011-11-21 2019-11-13 칼리테라 바이오사이언시즈, 인코포레이티드 글루타미나제의 헤테로사이클릭 억제제
EP2895623B1 (en) 2012-09-17 2018-08-22 Agios Pharmaceuticals, Inc. Use of e-cadherin and vimentin for selection of treatment responsive patients
CN105051041B (zh) 2012-11-16 2018-03-30 卡利泰拉生物科技公司 杂环谷氨酰胺酶抑制剂
EP2922832B1 (en) 2012-11-21 2019-10-09 Agios Pharmaceuticals, Inc. Glutaminase inhibitors and methods of use
US9029531B2 (en) * 2012-11-22 2015-05-12 Agios Pharmaceuticals, Inc. Compounds and their methods of use
WO2014079011A1 (en) * 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
EP2925318A4 (en) 2012-12-03 2016-07-13 Calithera Biosciences Inc TREATMENT OF CANCER WITH HETEROCYCLIC GLUTAMINASE INHIBITORS
CN112920180A (zh) * 2014-01-06 2021-06-08 理森制药股份公司 谷氨酰胺酶抑制剂
HRP20192056T1 (hr) * 2014-04-30 2020-02-21 Pfizer Inc. Derivati diheterocikla vezani na cikloalkil

Also Published As

Publication number Publication date
JP2019163290A (ja) 2019-09-26
CL2016001715A1 (es) 2017-02-03
EA201991183A1 (ru) 2020-02-28
CN105960405B (zh) 2021-02-19
KR20220013017A (ko) 2022-02-04
BR112016015706A2 (pt) 2017-08-08
IL246362B (en) 2022-02-01
EA201691134A1 (ru) 2016-12-30
US20160318921A1 (en) 2016-11-03
ES2833576T3 (es) 2021-06-15
JP6666263B2 (ja) 2020-03-13
SG11201605478XA (en) 2016-08-30
AU2015204210A1 (en) 2016-07-07
EA035499B1 (ru) 2020-06-25
WO2015101957A3 (en) 2015-11-19
US20210032236A1 (en) 2021-02-04
EA033163B1 (ru) 2019-09-30
JP2017501234A (ja) 2017-01-12
JP2017505808A (ja) 2017-02-23
WO2015101958A2 (en) 2015-07-09
CN106029659A (zh) 2016-10-12
WO2015101958A3 (en) 2015-10-29
CN111393431A (zh) 2020-07-10
EP3092235A2 (en) 2016-11-16
CN112920180A (zh) 2021-06-08
BR112016015706A8 (pt) 2020-06-09
AU2015204210B2 (en) 2019-07-18
EP3092236A2 (en) 2016-11-16
JP6783663B2 (ja) 2020-11-11
CN111892589A (zh) 2020-11-06
WO2015101957A2 (en) 2015-07-09
DK3092236T3 (en) 2020-11-30
CA2934702A1 (en) 2015-07-09
US20160297761A1 (en) 2016-10-13
IL246362A0 (en) 2016-08-31
CN105960405A (zh) 2016-09-21
US20180057487A1 (en) 2018-03-01
KR20160100408A (ko) 2016-08-23
US10611759B2 (en) 2020-04-07
KR20160100407A (ko) 2016-08-23
CN106029659B (zh) 2020-08-11
US9783533B2 (en) 2017-10-10
ZA201604272B (en) 2019-04-24
CA2934700A1 (en) 2015-07-09
EP3092236B1 (en) 2020-08-26

Similar Documents

Publication Publication Date Title
EA201691135A1 (ru) Новые ингибиторы глутаминазы
PH12019550050A1 (en) Isoxazole analogs as fxr agonists and methods of use thereof
EA201792231A1 (ru) Ингибиторы индоламин-2,3-диоксигеназы и способы их применения
EA201990495A1 (ru) Биарильные соединения, применимые в качестве иммуномодуляторов
EA201890307A1 (ru) Индазольные и азаиндазольные соединения как ингибиторы irak-4
EA201990221A1 (ru) 1,3-дигидроксифенильные производные, применимые в качестве иммуномодуляторов
EA201890308A1 (ru) Замещенные азасоединения как ингибиторы irak-4
EA201692079A1 (ru) Ингибиторы лизин-специфической деметилазы-1
EA201891910A1 (ru) Гетероарильные ингибиторы pad4
EA201791018A1 (ru) Производные 6-амино-7-бицикло-7-деазапурина в качестве ингибиторов протеинкиназы
EA201691857A1 (ru) Соединения, применимые в качестве иммуномодуляторов
EA201690306A1 (ru) Ингибиторы ido
EA201591823A1 (ru) Ингибиторы ido
EA201591599A1 (ru) Ингибиторы ido
EA201690027A1 (ru) Ингибиторы ido
EA201791874A1 (ru) Фторированные ингибиторы лизилоксидазоподобного фермента-2 и их применение
EA201690152A1 (ru) Ингибиторы ido
EA201790078A1 (ru) Ингибиторы mnk и связанные с ними способы
EA201792028A1 (ru) Альфа-цинамидные соединения и композиции как ингибиторы hdac8
EA201692268A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
EA201891347A1 (ru) Аза-бензимидазольные ингибиторы pad4
EA202091731A1 (ru) Ингибиторы аутотаксина и их применения
EA201891379A1 (ru) Ингибиторы тирозинкиназы брутона и способы их применения
EA202091865A1 (ru) Композиции и способы для снижения экспрессии tau
EA201990678A1 (ru) Гетероарилкарбоксамидные соединения в качестве ингибиторов ripk2