HRP20200854T1 - Novi biciklički inhibitori bromodomene - Google Patents

Novi biciklički inhibitori bromodomene Download PDF

Info

Publication number
HRP20200854T1
HRP20200854T1 HRP20200854TT HRP20200854T HRP20200854T1 HR P20200854 T1 HRP20200854 T1 HR P20200854T1 HR P20200854T T HRP20200854T T HR P20200854TT HR P20200854 T HRP20200854 T HR P20200854T HR P20200854 T1 HRP20200854 T1 HR P20200854T1
Authority
HR
Croatia
Prior art keywords
pyridin
imidazo
dimethylisoxazol
benzyl
methyl
Prior art date
Application number
HRP20200854TT
Other languages
English (en)
Inventor
Bryan Cordell Duffy
Shuang Liu
John Frederick Quinn
Ruifang WANG
May Xiaowu Jiang
Gregory Scott Martin
Gregory Steven WAGNER
Peter Roland Young
Original Assignee
Zenith Epigenetics Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Zenith Epigenetics Ltd. filed Critical Zenith Epigenetics Ltd.
Publication of HRP20200854T1 publication Critical patent/HRP20200854T1/hr

Links

Classifications

    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)

Claims (41)

1. Spoj naznačen time, da ima Formulu IIb' ili Formulu IId': [image] ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat gdje: prstenovi A i B mogu biti opcionalno supstituirani sa skupinama koje se neovisno biraju iz deuterija, -NH2, amino, heterocikla(C4-C6), karbocikla(C4-C6), halogena, -CN, -OH, -CF3, alkila(C1-C6), tioalkila(C1-C6), alkenila(C1-C6), i alkoksi(C1-C6); X se bira od -NH-, -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH2CH2O-, -CH2CH2NH-, -CH2CH2S-, -C(O)-, -C(O)CH2-, -C(O)CH2CH2-, -CH2C(O)-, -CH2CH2C(O)-, -C(O)NH-, -C(O)O-, -C(O)S-, -C(O)NHCH2-,-C(O)OCH2-, -C(O)SCH2-, -CH(OH)-, i -CH(CH3)- gdje se jedan ili više vodika mogu neovisno zamijeniti s deuterijem, hidroksi, metilom, halogenom, -CF3, ketonom, i gdje se S može oksidirati do sulfoksida ili sulfona; R4 se bira iz karbocikla i heterocikla od 3-7 članova, opcionalno supstituiranih sa skupinama koje se biraju iz deuteriija, alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida,-CF3, CN, -N3, ketona(C1-C4), -S(O)alkila(C1-C4), -SO2alkil(C1-C4), - tioalkila(C1-C4), karboksila, i/ili estera, svaki od kojih može biti opcionalno supstituiran s vodikom, F, Cl, Br, -OH, -NH2, -NHMe,-OMe, -SMe, okso, i/ili tio-okso; i D1 se bira iz slijedećih 5-tero članih monocikličkih heterocikla: [image] koji se opcionalno supstituiraju s deuterijem, alkilom(C1-C4), alkoksi(C1-C4), amino, halogenom, amidom, -CF3, CN, -N3, ketona(C1-C4), -S(O)Alkila(C1-C4), -SO2alkila(C1-C4), -tioalkila(C1-C4), -COOH, i/ili estera, svaki od kojih može biti opcionalno supstituiran s vodikom, F, Cl, Br, -OH, -NH2,-NHMe, -OMe, -SMe, okso, i/ili thio-okso; gdje svaka aminokiselina, kada je prisutna, ima oblik -NRdRe or -N(Rd)Re-, gdje se Rd i Re neovisno biraju iz alkila, alkenila, alkinila, arila, arilalkila, karbamata, cikloalkila, haloalkila, heteroarila, heterocikla, i vodika, i gdje se Rd i Re mogu spojiti da oblikuju 3- do 12-ero člani prsten, i gdje je svaki amino opcionalno supstituiran s najmanje jednom skupinom koja se bira iz alkoksi, ariloksi, alkila, alkenila, alkinila, amida, amino, arila, arilalkila, karbamata, karbonila, karboksi, cijano, cikloalkila, estera, etera, formila, halogena, haloalkila, heteroarila, heterociklila, hidroksila, ketona, fosfata, sulfida, sulfinila, sulfonila, sulfonske kiseline, sulfonamida, tioketona, ureido, i N.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen Formulom IIb'': [image] ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, gdje se Z bira iz vodika, deuterija, -NH2, amino, alkil(C1-C6), tioalkil(C1-C6), alkenil(C1-C6), i alkoksi(C1-C6).
3. Spoj prema bilo kojem od patentnih zahtjeva 1-2, naznačen time, da je R4 3-7 člani heterocikl.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time, da je R4 5-6 člani heterocikl.
5. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time, da se R4 bira iz cikloalkil(C3-C6) i fenilnog prstena opcionalno supstituiranog s jednom ili više skupina neovisno odabranih iz deuterija, alkil(C1-C4), alkoksi(C1-C4), halogena, -CF3, CN, i -tioalkil(C1-C4), gdje svaki alkil, alkoksi, i tioalkil mogu opcionalno biti supstituirani s F, Cl, ili Br.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-4, naznačen time, da je R4 fenilni prsten opcionalno supstituiran sa skupinama koje se neovisno biraju iz deuterija, alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida, -CF3, CN, -N3, keton (C1-C4), -S(O)alkil(C1-C4), -SO2alkil(C1-C4), -tioalkil(C1-C4), karboksil, i/ili ester, svaki od kojih može biti supstituiran s F, Cl, Br, -OH, -NH2, -NHMe, -OMe, -SMe, okso, i/ili tio-okso.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-4, naznačen time, da se R4 bira iz 5- ili 6-ero članog heterocikla koji ima 1-2 dušika, opcionalno supstituiranih sa skupinama koje se neovisno biraju iz deuterija, alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida, -CF3, CN, -N3, keton (C1-C4), -S(O)alkil(C1-C4), -SO2alkil(C1-C4), -tioalkil(C1-C4), karboksil, i/ili ester, svaki od kojih može biti supstituiran s F, Cl, Br, -OH, -NH2, -NHMe, -OMe, -SMe, okso, i/ili tio-okso.
8. Spoj prema bilo kojem od patentnih zahtjeva 1-4, naznačen time, da se R4 bira iz pirimidila, piridila, izoksazola i pirazola, opcionalno supstituiranih sa skupinama koje se neovisno biraju iz deuterija, alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida, -CF3, CN, -N3, keton (C1-C4), -S(O)alkil(C1-C4), -SO2alkil(C1-C4), -tioalkil(C1-C4), karboksil, i/ili ester, svaki od kojih može biti supstituiran s F, Cl, Br, -OH, -NH2, -NHMe, -OMe, -SMe, okso, i/ili tio-okso.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-8, naznačen time, da je D1 izoksazol opcionalno supstituiran s deuterijem, alkil(C1-C4), od kojih svaki može biti supstituiran s -OH, -F, i NH2.
10. Spoj prema patentnom zahtjevu 9, naznačen time, da se D1 bira iz [image] .
11. Spoj prema bilo kojem od patentnih zahtjeva 1-9, naznačen time, da je D1 [image]
12. Spoj prema bilo kojem od patentnih zahtjeva 1-11, naznačen time, da se X bira iz CH2-, -CH(CH3)-, -CH(OH)-, -NH-, CH2CH2-, gdje se jedan ili više vodika mogu neovisno zamijeniti s deuterijem ili halogenom.
13. Spoj prema patentnom zahtjevu 12, naznačen time, da se X bira iz -CH2-, -CH(CH3)-, i -NH- gdje se jedan ili više vodika mogu neovisno zamijeniti s deuterijem ili halogenom.
14. Spoj prema patentnom zahtjevu 13, naznačen time, da se X bira iz -CH2-, i -CH(CH3)-, gdje se jedan ili više vodika mogu neovisno zamijeniti s deuterijem ili halogenom.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-14, naznačen time, da se X-R4 bira iz -CH2aril.
16. Spoj prema patentnom zahtjevu 1, naznačen time, da se bira iz Formule IIb'' [image] ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, gdje se Z bira iz vodika, deuterija, -NH2, amino, alkil(C1-C6), tioalkil(C1-C6), alkenil(C1-C6), i alkoksi(C1-C6), D1 je [image] X se bira iz -CH2-, -CH(CH3)-; i R4 je fenilni prsten opcionalno supstituiran sa skupinama koje se neovisno biraju iz deuterija, alkil(C1-C4), alkoksi(C1-C4), halogena, -CF3, CN, -tioalkil(C1-C4, gdje svaki alkil, alkoksi, i tioalkil mogu biti opcionalno supstituirani s F, Cl, Br.
17. Spoj prema patentnom zahtjevu 16, naznačen time, da je R4 fenilni prsten opcionalno supstituiran s jednom ili više slijedećih skupina: alkil(C1-C4) odabran iz metila, etila, propila, izopropila, i butila; alkoksi(C1-C4) odabran iz metoksi, etoksi, and izopropoksi; halogen odabran iz F i Cl; i tioalkil(C1-C4) odabran iz -SMe, -SEt, -SPr, and -Sbu.
18. Spoj prema bilo kojem od patentnih zahtjeva 16-17, naznačen time, da se Z bira iz vodika i amino.
19. Spoj, naznačen time, da ima Formulu IIb'': [image] ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, gdje se X bira iz NH-, -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH2CH2O-, -CH2CH2NH-, -CH2CH2S-, -C(O)-, -C(O)CH2-, -C(O)CH2CH2-, -CH2C(O)-, -CH2CH2C(O)-, -C(O)NH-, -C(O)O-, -C(O)S-, -C(O)NHCH2-,-C(O)OCH2-, -C(O)SCH2-, -CH(OH)-, i -CH(CH3)- gdje se jedan ili više vodika mogu neovisno zamijeniti s deuterijem, hidroksi, metilom, halogenom, CF3, ketonom, i gdje S može biti oksidiran do sulfoksida ili sulfona; R4 se bira iz 3-7 članih karbocikala i heterocikala, opcionalno supstituiranih sa skupinama neovisno biranim iz deuterija, alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida,-CF3, CN, -N3, keton(C1-C4), -S(O)alkil(C1-C4), -SO2alkil(C1-C4), -tioalkil(C1-C4), karboksil, i/ili ester, svaki od kojih može biti opcionalno supstituiran s vodikom, F, Cl, Br, -OH, -NH2, -NHMe,-OMe, -SMe, okso, i/ili tio-okso; i D1 se bira od slijedećih 5-ero članih monocikličkih heterocikala: [image] koji su opcionalno supstituirani s vodikom, deuterijem , alkil(C1-C4), alkoksi(C1-C4), amino, halogena, amida,-CF3, CN, -N3, keton(C1-C4), -S(O)alkil(C1-C4), -SO2alkil(C1-C4), -tioalkil(C1-C4), -COOH i/ili ester, svaki od kojih može biti opcionalno supstituiran s vodikom, F, Cl, Br, -OH, -NH2, -NHMe,-OMe, -SMe, okso, i/ili tio-okso; i Z se bira iz -Me, -CF3, -Et, CH3CH2O-, CF3CH2-, -SMe, -SOMe, -SO2Me, -CN, [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] gdje svaka aminokiselina, kada je prisutna, ima oblik -NRdRe or -N(Rd)Re-, gdje se Rd i Re neovisno biraju iz alkila, alkenila, alkinila, arila, arilalkila, karbamata, cikloalkila, haloalkila, heteroarila, heterocikla i vodika, i gdje se Rd i Re mogu biti združeni na način da oblikuju 3- do 12-ero člani prsten, i gdje je svaka aminokiselina opcionalno supstituirana s najmanje jednom skupinom biranom iz alkoksi, ariloksi, alkila, alkenila, alkinila, amida, amino, arila, arilalkila, karbamata, karbonila, karboksi, cijano, cikloalkila, estera, etera, formila, halogena, haloalkila, heteroarila, heterociklila, hidroksila, ketona, fosfata, sulfida, sulfinila, sulfonila, sulfonske kiseline, sulfonamida, tioketona, ureido, i N.
20. Spoj prema patentnom zahtjevu 19, naznačen time, da se Z bira iz -Me, -CF3, -Et, CH3CH2O-, [image] [image] [image] [image] [image] [image] i [image]
21. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da je svaki Rd i Re opcionalno supstituiran s hidroksilom, halogenom, alkoksi, esterom ili amino.
22. Spoj prema patentnom zahtjevu 1, naznačen time, da se bira iz: 4-(1-benzil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(1-benzil-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 3,5-dimetil-4-(1-(1-feniletil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 4-((6-(3,5-dimetilizoksazol-4-il)-2-metil-1H-imidazo[4,5-b]piridin-1-il)metil)benzamida; 3,5-dimetil-4-(1-(4-(trifluorometil)benzil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 4-(1-(4-klorobenzil)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(4-fluorobenzil)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 3,5-dimetil-4-(1-(piridin-2-ilmetil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 4-(1-(4-fluorobenzil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-benzil-2-etoksi-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-((6-(3,5-dimetilizoksazol-4-il)-2-metil-1H-imidazo[4,5-b]piridin-1-il)metil)-3,5-dimetilizoksazola; 4-(1-(2,4-dicklorobenzil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(4-metoksibenzil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(ciklopropilmetil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 3,5-dimetil-4-(2-metil-1-(piridin-3-ilmetil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 3,5-dimetil-4-(2-metil-1-(tiofen-2-ilmetil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 4-((6-(3,5-dimetilizoksazol-4-il)-2-metil-1H-imidazo[4,5-b]piridin-1-il)metil)benzonitrila; 3,5-dimetil-4-(2-metil-1-(piridin-4-ilmetil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 3,5-dimetil-4-(2-metil-1-((5-metilti0fen-2-il)metil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 4-(1-((5-klorotiofen-2-il)metil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 5-((6-(3,5-dimetilizoksazol-4-il)-2-metil-1H-imidazo[4,5-b]piridin-1-il)metil)tiofen-2-karbonitrila; 6-(3,5-dimetilizoksazol-4-il)-1-(4-fluorobenzil)-1H-imidazo[4,5-b]piridin 4-oksida; 4-(1-(4-klorobenzil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-((6-(3,5-dimetilisoksazol-4-il)-2-metil-1H-imidazo[4,5-b]piridin-1-il)metil)fenola; 4-(1-(3,4-diklorobenzil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-(3,4-diklorobenzil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 1-(4-klorobenzil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 6-(3,5-dimetilisoksazol-4-il)-1-(tiofen-2-ilmetil)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-etil-1H-imidazo[4,5-b]piridin-2-amina; 3,5-dimetil-4-(2-metil-1-(1-feniletil)-1H-imidazo[4,5-b]piridin-6-il)izoksazola; 6-(3,5-dimetilizoksazol-4-il)-1-(1-feniletil)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 6-(3,5-dimetilizoksazol-4-il)-N-etil-1-(1-feniletil)-1H-imidazo[4,5-b]piridin-2-amina; 4-(1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)morfolina; 1-(ciklopropilmetil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(2-(azetidin-1-il)-1-benzil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-((5-klorotiofen-2-il)metil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(1-benzil-2-etil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-(ciklopropilmetil)-6-(3,5-dimetilizoksazol-4-il)-N-etil-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-metil-1H-imidazo[4,5-b]piridin-2-amina; N,1-dibenzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-2-metil-6-(1-metil-1H-pirazol-5-il)-1H-imidazo[4,5-b]piridina; N-(1-benzil-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazol-4-amina; 4-(1-benzil-2-(4-metilpiperazin-1-il)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(1-metil-1H-pirazol-5-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(1-benzil-6-(1-metil-1H-pirazol-5-il)-1H-imidazo[4,5-b]piridin-2-il)morfolina; 1-benzil-6-(1-metil-1H-pirazol-5-il)-N-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-7-metil-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(1-benzil-2,7-dimetil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(cikloheksilmetil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(ciklopentilmetil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(ciklobutilmetil)-2-metil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-benzil-2-(pirolidin-1-il)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-(ciklopentilmetil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 1-(ciklobutilmetil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(4-metoksibenzil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-2-metil-6-(1-metil-1H-1,2,3-triazol-5-il)-1H-imidazo[4,5-b]piridina; 4-((1-benzil-6-(3,5-dimetilisoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)amino)cikloheksanola; 4-(1-(ciklopentilmetil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)morfolina; 4-(2-(azetidin-1-il)-1-(ciclopentilmetil)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 4-(1-(ciklobutilmetil)-6-(3,5-dimetilisoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)morfolina; 4-(2-(azetidin-1-il)-1-(ciklobutilmetil)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilisoksazola; 4-(1-benzil-2-(piperazin-1-il)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-benzil-N-ciklopentil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 3-(((1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)amino)metil)benzonitrila; (R)-6-(3,5-dimetilizoksazol-4-il)-1-(1-feniletil)-1H-imidazo[4,5-b]piridin-2(3H)-ona; (S)-6-(3,5-dimetilizoksazol-4-il)-1-(1-feniletil)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 4-(1-benzil-2-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-(ciklopentilmetil)-6-(3,5-dimetilizoksazol-4-il)-N-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-(ciklobutilmetil)-6-(3,5-dimetilizoksazol-4-il)-N-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-b]piridin-2-amina; N1-(1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)cikloheksan-1,4-diamina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(oksetan-3-il)-1H-imidazo[4,5-b]piridin-2-amina; 6-(3,5-dimetilizoksazol-4-il)-1-(4-fluorobenzil)-1H-imidazo[4,5-b]piridin-2(3H)-ona; 6-(3,5-dimetilizoksazol-4-il)-1-(4-fluorobenzil)-N-metil-1H-imidazo[4,5-b]piridin-2-amina; 1-(4-klorobenzil)-6-(3,5-dimetilizoksazol-4-il)-N-metil-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-N-cikloheksil-6-(3,5-dimetilisoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilisoksazol-4-il)-N-(1-metilpiperidin-4-il)-1H-imidazo[4,5-b]piridin-2-amina; ili njihovih stereoizomera, tautomera, soli ili hidrata.
23. Spoj prema patentnom zahtjevu 19, naznačen time, da se bira iz: 4-(1-benzil-2-ciklopropil-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(2-metoksietil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(piridin-4-ilmetil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(piridin-3-ilmetil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(piridin-2-ilmetil)-1H-imidazo[4,5-b]piridin-2-amina; 2-((1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)amino)etanola; N1-(1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)-N2,N2-dimetiletan-1,2-diamina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(2-morfolinoetil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-metil-1H-imidazo[4,5-b]piridin-2-karboksamida; 1-benzil-N-(cikloheksilmetil)-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(3-metoksipropil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(pirazin-2-ilmetil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-((tetrahidro-2H-piran-4-il)metil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(2-(4-metilpiperazin-1-il)etil)-1H-imidazo[4,5-b]piridin-2-amina; 4-(1-benzil-2-(piridin-3-iloksi)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; 1-((1-benzil-6-(3,5-dimetilizoksazol-4-il)-1H-imidazo[4,5-b]piridin-2-il)amino)-2-metilpropan-2-ola; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(2-(pirolidin-1-il)etil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(2-(piperidin-1-il)etil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-(tiazol-2-ilmetil)-1H-imidazo[4,5-b]piridin-2-amina; 1-benzil-6-(3,5-dimetilizoksazol-4-il)-N-((1-metilpiperidin-4-il)metil)-1H-imidazo[4,5-b]piridin-2-amina; 4-(1-benzil-2-(piridin-4-iloksi)-1H-imidazo[4,5-b]piridin-6-il)-3,5-dimetilizoksazola; ili njihovih stereoizomera, tautomera, soli ili hidrata.
24. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1-23 ili njegov stereoizomer, tautomer, farmaceutski prihvatljivu sol, ili hidrat i farmaceutski prihvatljivi nosač.
25. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, naznačen time, da je za uporabu u terapiji.
26. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku: a. liječenja autoimunog poremećaja; ili b. liječenja upalnog poremećaja.
27. Spoj ili pripravak za uporabu prema patentnom zahtjevu 26, naznačen time, da je autoimuni ili upalni poremećaj povezan s proteinima BET i biraju se iz akutnog diseminiranog encefalomijelitisa, agamaglobulinemije, alergijske bolesti, ankilozantnog spondilitisa, anti-GBM/anti-TBM nefritisa, antifosfolipidnog sindroma, autoimune aplastične anemije, autoimunog hepatitisa, autoimune bolesti unutrašnjeg uha, autoimunog miokarditisa, autoimunog pankreatitisa, autoimune retinopatije, autoimune trombocitopenične purpure, Behçetove bolesti, buloznog pemfigoida, Castelmanove bolesti, celijakije, Churg-Straussovog sindroma, Crohnove bolesti, Coganovog sindroma, sindroma suhog oka, esencijalne miješane krioglobulinemije, dermatomiozitisa, Devicove bolesti, encefalitisa, eozinofilnog ezofagitisa, eozinofilnog fasciitisa, nodoznog eritema, gigantocelularnog arteritisa, glomerulonefritisa, Goodpastureovog sindroma, granulomatoze s poliangiitisom (Wegenerove bolesti), Gravesove bolesti, Guillain-Barreovog sindroma, Hashimotovog tireoiditisa, hemolitičke anemije, Henoch-Schönleinove purpure, idiopatske pulmonarne fibroze, IgA nefropatije, miozitisa s inkluzijskim tijelima, dijabetesa tipa I, intersticijskog cistitisa, Kawasakijeve bolesti, leukocitoklastičnog vaskulitisa, lichen planusa, lupusa (SLE), mikroskopskog poliangiitisa, multiple skleroze, miastenije gravis, miozitisa, optičkog neuritisa, pemfigusa, sindroma POEMS, nodoznog poliarteritisa, primarne bilijarne ciroze, psorijaze, psorijatičnog artritisa, pyoderme gangrenosum, rekurentnog polikondritisa, reumatoidnog artritisa, sakrodioze, skleroderme, Sjörgenovog sindroma, Takayasuovog arteritisa, transverzalnog mijelitisa, ulcerativnog kolitisa, uveitisa i vitiliga.
28. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku liječenja akutnog ili kroničnog ne-autoimunog poremećaja karakteriziranim deregulacijom IL-6 i/ili IL-17.
29. Spoj ili pripravak za uporabu prema patentnom zahtjevu 28, naznačen time, da se akutni ili kronični ne-autoimuni upalni poremećaj bira iz sinusitisa, pneumonitisa, osteomijelitisa, gastritisa, enteritisa, gingivitisa, apendicitisa, sindroma iritabilnog kolona, odbacivanja presadka, kronične opstrukcijske plućne bolesti (COPD, prema engl. „ chronic obstructive pulmonary disease“), septičkog šoka, osteoartritisa, akutnog gihta, akutne ozljede pluća, akutnog zatajenja bubrega, opeklina, Herxheimerove reakcije, i sindroma sustavnog upalnog odgovora (SIRS, prema engl. „systemic inflammatory response syndrome“) povezanog s virusnim infekcijama.
30. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku liječenja reumatoidnog artritisa (RA) ili multiple skleroze (MS).
31. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku liječenja karcinoma.
32. Spoj ili pripravak za uporabu prema patentnom zahtjevu 31, naznačen time, da se karcinom bira iz kronične limfocitne leukemije, multiplog mijeloma, folikularnog limfoma, difuznog limfoma velikih B stanica s fenotipom germinalnog centra, Burkittovog limfoma, Hodgkinovog limfoma, folikularnog limfoma, limfoma aktivirane anaplastične velike stanice, neuroblastoma, primarnog neuroektodermalnog tumora, rabdomiosarkoma, karcinoma prostate, karcinoma dojke, NUT srednjeg karcinoma - NMC (prema engl. „NUT-midline carcinoma“), akutne mijeloidne leukemije (AML), akutne B limfoblastične leukemije (B-ALL), Burkittovog limfoma, limfoma B stanice, melanoma, mješovite leukemije, multiplog mijeloma, promijelocitne leukemije (PML), non-Hodgkinovog limfoma, neuroblastoma, meduloblastoma, karcinoma pluća (NSCLC, SCLC), i karcinoma kolona.
33. Spoj ili pripravak za uporabu prema patentnom zahtjevu 31, naznačen time, da karcinom (a) je povezan s prekomjernom ekspresijom, translokacijom, amplifikacijom, ili rearanžmanom onkoproteina obitelji myc koji je osjetljiv na inhibiciju BET; (b) je povezan s prekomjernom ekspresijom, translokacijom, amplifikacijom, ili rearanžmanom proteina BET; (c) se oslanja na pTEFb (Cdk9/ciklin T) i proteine BET kako bi regulirali onkogene; (d) je povezan s regulacijom naviše gena, koji su osjetljivi na BET, CDK6, Bcl2, TYRO3, MYB, i hTERT; i/ili (e) je osjetljiv na učinke inhibicije BET.
34. Spoj ili pripravak za uporabu prema patentnom zahtjevu 33, naznačen time, da se (a) karcinom povezan s prekomjernom ekspresijom, translokacijom, amplifikacijom, ili rearanžmanom onkoproteina obitelji myc koji je osjetljiv na inhibiciju BET bira iz B-akutne limfocitne leukemije, Burkittovog limfoma, difuznog limfoma velikih stanica, multiplog mijeloma, primarne leukemije plazma stanica, atipičnog karcionoidnog raka pluća, karcinoma mjehura, karcinoma dojke, karcinoma cerviksa, karcinoma kolona, karcinoma želuca, glioblastoma, hepatocelularnog karcinoma, neuroendokrinog karcinoma velikih stanica, meduloblastoma, melanoma, nodularnog melanoma, površinskog širenja, neuroblastoma, karcinoma skvamoznih stanica jednjaka, osteosarkoma, karcinoma jajnika, karcinoma prostate, karcinoma renalnih čistih stanica, retinoblastoma, rabdomiosarkoma, i karcinoma pluća malih stanica; (b) karcinom povezan s prekomjernom ekspresijom, translokacijom, amplifikacijom, ili rearanžmanom proteina BET bira iz NUT srednjeg karcinoma, limfoma B-stanica, karcinoma pluća ne-malih stanica, karcinoma jednjaka, karcinoma skvamoznih stanica glave i vrata, i karcinoma kolona; (c) karcinom, koji se oslanja na pTEFb (Cdk9/ciklin T) i proteine BET, kako bi regulirali onkogene bira iz kronične limfocitne leukemije i multiplog mijeloma, folikularnog limfoma, difuznog limfoma velikih B stanica s fenotipom germinalnog centra, Burkittovog limfoma, Hodgkinovog limfoma, folikularnog limfoma i aktiviranog limfoma anaplastičnih velikih stanica, neuroblastoma i primarnog neuroektodermalnog tumora, rabdomiosarkoma, karcionoma prostate, i karcinoma dojke; (d) karcinom povezan s regulacijom naviše gena koji su osjetljivi na BET CDK6, Bcl2, TYRO3, MYB, i hTERT bira iz karcinoma pankreasa, karcinoma dojke, karcinoma kolona, glioblastoma, adenoidnog cističnog karcinoma, prolimfocitne leukemije T-stanica, malignog glioma, karcinoma mjehura, meduloblastoma, tiroidnog karcinoma, melanoma, multiplog mijeloma, Barretovog adenokarcinoma, hepatoma, karcinoma prostate, promijelocitne leukemije, kronične limfocitne leukemije, limfoma stanica plašta, difuznog limfoma velikih B-stanica, karcinoma pluća malih stanica, i renalnog karcinoma; i/ili (e) karcinom osjetljiv na učinke inhibicije BET se bira iz NUT srednjeg karcinoma (NMV), akutne mijeloiodne leukemije (AML), akutne B limfoblastične leukemije (B-ALL), Burkittovog limfoma, limfoma B-stanica, melanoma, mještovite leukemije, multiplog mijeloma, promijelocitne leukemije (PML), non-Hodgkinovog limfoma, neuroblastoma, meduloblastoma, karcinoma pluća (NSCLC, SCLC), i karcinoma kolona.
35. Spoj ili pripravak za uporabu prema bilo kojem patentnom zahtjevu 25-34, naznačen time, da postupak obuhvaća primjenu spoja ili farmaceutskog pripravka u kombinaciji s drugim terapijama, kemoterapijskim agensima ili antiproliferativnim agensima.
36. Spoj ili pripravak za uporabu prema patentnom zahtjevu 35, naznačen time, da se drugi terapijski agens bira iz ABT-737, azacitidina (Vidaza), AZD1152 (Barasertib), AZD2281 (Olaparib), AZD6244 (Selumetinib), BEZ235, bleomicin sulfata, bortezomiba (Velcade), busulfana (Myleran), kamptotecina, cisplatina, ciklofosfamida (Clafen), CYT387, citarabina (Ara-C), dakarbazina, DAPT (GSI-IX), decitabina, deksametazona, doksorubicina (Adriamycin), etopozida, everolimusa (RAD001), flavopiridola (Alvocidib), ganetespiba (STA-9090), gefitiniba (Iressa), idarubicina, ifosfamida (Mitoxana), IFNa2a (Roferon A), melfalana (Alkeran), metazolastona (temozolomide), metformina, mitoksantrona (Novantrone), Paklitaksela, Fenformina, PKC412 (Midostaurin), PLX4032 (Vemurafenib), pomalidomida (CC-4047), prednizona (Deltasone), rapamicina, revlimida (Lenalidomide), ruksolitiniba (INCB018424), sorafeniba (Nexavar), SU11248 (Sunitinib), SU11274, vinblastina, vinkristina (Oncovin), vinorelbina (Navelbine), vorinostata (SAHA), i WP1130 (Degrasyn).
37. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu za liječenje benignog ili proliferativnog ili fibrotičkog poremećaja, odabranog iz skupine koja se sastoji od benignih tumora mekih tkiva, tumora kostiju, tumora mozga ili kralježničine moždine, tumora kapka i orbite, granuloma, lipoma, meningeoma, multiplih endokrinih neoplazija, nazalnih polipa, pituitarnih tumora, prolaktinoma, pseudotumora mozga, seboroičnih keratoza, polipa želuca, tiroidnih čvorova, cističnih neoplazmi pankreasa, hemangioma, čvorova, polica i cista glasnica, Castelmanove bolesti, kronične pilonidalne bolesti, dermatofibroma, pilarne ciste, piogenog granuloma, juvenilnog polipoznog sindroma, idiopatske pulmonarne fibroze, renalne fibroze, post-operativnog suženja, nastanka keloida, skleroderme i srčane fibroze.
38. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku liječenja (a) bolesti ili poremećaja odabranog iz kardiovaskularne bolesti, dislipidemije, ateroskleroze, hiperkolesterolemije, metaboličkog sindroma, i Alzheimerove bolesti; (b) metaboličke bolesti ili poremećaja; (c) karcinoma povezanog s virusom; (d) HIV-a; i/ili (e) neurološkog poremećaja.
39. Spoj ili pripravak za uporabu prema patentnom zahtjevu 38, naznačen time, da se (a) metabolička bolest ili poremećaj se bira iz upale povezane s pretilosti, dijabetesa tipa II, i inzulinske rezistencije; (b) virus bira iz Epstein-Barr virusa (EBV), virusa hepatitisa B (HBV), virusa hepatitisa C (HCV), virusa povezanog s Kaposijevim sarkomom (KSHV), virusa humanog papiloma (HPV), poliomavirusa Merkelovih stanica, i humanog citomegalovirusa (CMV); i/ili (c) neurološke bolesti ili poremećaja odabranih iz Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove bolesti, bipolarnog poremećaja, shizofrenije, Rubistein-Taybijevog sindroma, i epilepsije.
40. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u liječenju infekcije HIV-om, gdje se navedeni spoj ili pripravak primjenjuju u kombinaciji s anti-retroviralnim lijekom.
41. Spoj prema bilo kojem od patentnih zahtjeva 1-23, ili njegov stereoizomer, tautomer, farmaceutski prihvatljiva sol, ili hidrat, ili farmaceutski pripravak prema patentnom zahtjevu 24, naznačen time, da je za uporabu u postupku kontracepcije muškaraca.
HRP20200854TT 2013-06-21 2020-05-27 Novi biciklički inhibitori bromodomene HRP20200854T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361837841P 2013-06-21 2013-06-21
PCT/US2014/043423 WO2015002754A2 (en) 2013-06-21 2014-06-20 Novel bicyclic bromodomain inhibitors
EP14820520.6A EP3010503B1 (en) 2013-06-21 2014-06-20 Novel bicyclic bromodomain inhibitors

Publications (1)

Publication Number Publication Date
HRP20200854T1 true HRP20200854T1 (hr) 2020-08-21

Family

ID=52144263

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20200854TT HRP20200854T1 (hr) 2013-06-21 2020-05-27 Novi biciklički inhibitori bromodomene

Country Status (23)

Country Link
US (5) US9663520B2 (hr)
EP (2) EP3674300B1 (hr)
JP (4) JP6461121B2 (hr)
KR (1) KR102307566B1 (hr)
CN (2) CN105407888B (hr)
AU (2) AU2014284616B2 (hr)
BR (1) BR112015031073B1 (hr)
CA (2) CA2915838C (hr)
DK (1) DK3010503T3 (hr)
EA (1) EA035601B1 (hr)
ES (1) ES2806135T3 (hr)
HK (2) HK1216722A1 (hr)
HR (1) HRP20200854T1 (hr)
HU (1) HUE049469T2 (hr)
IL (1) IL242844B (hr)
MX (1) MX365864B (hr)
NZ (2) NZ714669A (hr)
PL (1) PL3010503T3 (hr)
PT (1) PT3010503T (hr)
SG (2) SG11201510409QA (hr)
SI (1) SI3010503T1 (hr)
WO (1) WO2015002754A2 (hr)
ZA (2) ZA201600272B (hr)

Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX356163B (es) 2011-12-01 2018-05-16 Chemocentryx Inc Anilinas sustituidas como antagonistas de ccr(4).
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
SG10201707487VA (en) 2013-03-15 2017-10-30 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
TWI530499B (zh) * 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
JP6461118B2 (ja) * 2013-06-21 2019-01-30 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての新規の置換された二環式化合物
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EA201690087A1 (ru) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. Новые квиназолиноны как ингибиторы бромодомена
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201608843TA (en) 2014-04-23 2016-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
JP6832846B2 (ja) * 2014-09-15 2021-02-24 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ヘテロ環化合物およびその用途
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
US20190055235A1 (en) * 2014-12-17 2019-02-21 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN107406438B (zh) * 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
CN108135168B (zh) 2015-05-21 2021-07-20 凯莫森特里克斯股份有限公司 Ccr2调节剂
WO2016189042A1 (en) * 2015-05-28 2016-12-01 Bayer Pharma Aktiengesellschaft Method for stratification of melanoma patients by determination of oxygen consumption, ppargc1a, ppargc1b and mitf levels
EP3313818B1 (en) * 2015-06-26 2023-11-08 Celgene Corporation Methods for the treatment of kaposi's sarcoma or kshv-induced lymphoma using immunomodulatory compounds, and uses of biomarkers
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
KR20180039117A (ko) 2015-08-11 2018-04-17 네오메드 인스티튜트 아릴-치환된 디히드로퀴놀리논, 그의 제조법 및 제약으로서의 그의 용도
EP3334719B1 (en) 2015-08-12 2021-09-15 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105198871A (zh) * 2015-11-06 2015-12-30 中国药科大学 一类喹喔啉酮类化合物及其制备方法和用途
CA3005353A1 (en) 2015-11-20 2017-05-26 Forma Therapeutics, Inc. Purinones as ubiquitin-specific protease 1 inhibitors
CA3007168A1 (en) * 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
EA201891514A1 (ru) * 2015-12-24 2019-01-31 Селджен Квонтисел Рисёрч, Инк. Комбинированная терапия ингибитором бромодомена и экстратерминального белка
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN107349193A (zh) * 2016-05-10 2017-11-17 北京市神经外科研究所 蛋白功能抑制剂dapt在制备治疗内分泌疾病的药物中的用途
IL263824B2 (en) 2016-06-20 2023-10-01 Incyte Corp Crystals in solid form in the presence of an inhibitor
US10034861B2 (en) * 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
EP3502099B1 (en) * 2016-08-22 2020-12-09 Medshine Discovery Inc. Cyclic compound acting as pde4 inhibitor
TW201819376A (zh) 2016-10-06 2018-06-01 比利時商健生藥品公司 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途
KR102587839B1 (ko) * 2016-10-27 2023-10-11 셀젠 콴티셀 리서치, 인크. 브로모도메인 및 엑스트라-말단 단백질 억제제 병용 치료요법
WO2018097976A1 (en) * 2016-11-22 2018-05-31 Gilead Sciences, Inc. Synthesis of a compound that modulates the activity of bromodomain-containing proteins
US11261188B2 (en) 2016-11-28 2022-03-01 Praxis Precision Medicines, Inc. Fused heteroaryl compounds, and methods thereof for treating diseases, disorders, and conditions relating to aberrant function of a sodium channel
PT3548033T (pt) 2016-11-28 2024-08-09 Praxis Prec Medicines Inc Compostos e respectivos métodos de utilização
CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
JP7300394B2 (ja) 2017-01-17 2023-06-29 ヘパリジェニックス ゲーエムベーハー 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害
WO2018148745A1 (en) * 2017-02-13 2018-08-16 Praxis Precision Medicines , Inc. Compounds and their methods of use
WO2018187480A1 (en) * 2017-04-04 2018-10-11 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11028058B2 (en) 2017-07-18 2021-06-08 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
MX2020000693A (es) 2017-07-18 2020-07-29 Nuvation Bio Inc Compuestos de 1,8-naftiridinona, y usos de los mismos.
US11278535B2 (en) 2017-08-15 2022-03-22 Praxis Precision Medicines, Inc. Compounds and their methods of use
MA50250A (fr) 2017-09-15 2020-07-22 Forma Therapeutics Inc Compositions de tétrahydroimidazo quinoléine utilisées en tant qu'inhibiteurs de cbp/p300
IL273188B2 (en) 2017-09-25 2023-03-01 Chemocentryx Inc Treatment with a combination of chemokine receptor 2 (ccr2) inhibitors and a pd-1/pd-l1 inhibitor
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
US11332459B2 (en) 2017-10-19 2022-05-17 Teijin Pharma Limited Benzimidazole derivatives and their uses
SG11202005793SA (en) * 2017-12-20 2020-07-29 Betta Pharmaceuticals Co Ltd Compound functioning as bromodomain protein inhibitor, and composition
US20190269664A1 (en) 2018-01-08 2019-09-05 Chemocentryx, Inc. Methods of treating solid tumors with ccr2 antagonists
EP3737367B1 (en) * 2018-01-08 2024-10-02 ChemoCentryx, Inc. Ccr2 antagonists for the treatment of cutaneous t-cell lymphoma
WO2019144970A1 (zh) * 2018-01-29 2019-08-01 石家庄智康弘仁新药开发有限公司 一种1H-咪唑并[4,5-b]吡啶-2(3H)-酮类化合物的晶型及其制备方法
CN110092782B (zh) * 2018-01-30 2022-10-21 中国科学院广州生物医药与健康研究院 一种苯并六元氮杂环化合物及其制备方法和应用
WO2019193516A2 (en) 2018-04-04 2019-10-10 Janssen Pharmaceutica Nv Substituted pyridine and pyrimidines and their use as glun2b receptor modulators
BR112020024379A2 (pt) 2018-05-30 2021-03-02 Praxis Precision Medicines, Inc. moduladores de canais iônicos
SG11202012767UA (en) 2018-06-29 2021-01-28 Forma Therapeutics Inc Inhibiting creb binding protein (cbp)
TWI816881B (zh) * 2018-09-13 2023-10-01 大陸商恒翼生物醫藥（上海）股份有限公司 用於治療三陰性乳癌之組合療法
TWI841598B (zh) * 2018-09-13 2024-05-11 大陸商恒翼生物醫藥（上海）股份有限公司 用於治療雌激素受體陽性乳癌之組合療法
TW202024078A (zh) 2018-09-13 2020-07-01 加拿大商增你智表觀遺傳學公司 Bet溴結構域(bromodomain)抑制劑之固體形式之製備方法
TW202035401A (zh) * 2018-09-13 2020-10-01 加拿大商增你智表觀遺傳學公司 Bet 抑制劑之固體形式
TWI816880B (zh) * 2018-09-13 2023-10-01 大陸商恒翼生物醫藥（上海）股份有限公司 治療前列腺癌之組合療法
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN113939291A (zh) 2019-01-18 2022-01-14 诺维逊生物股份有限公司 1,8-萘啶酮化合物及其用途
KR20210116550A (ko) 2019-01-18 2021-09-27 누베이션 바이오 인크. 아데노신 길항제로서의 헤테로시클릭 화합물
US11773099B2 (en) 2019-05-28 2023-10-03 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11505554B2 (en) 2019-05-31 2022-11-22 Praxis Precision Medicines, Inc. Substituted pyridines as ion channel modulators
US11279700B2 (en) 2019-05-31 2022-03-22 Praxis Precision Medicines, Inc. Ion channel modulators
MX2021015503A (es) 2019-06-14 2022-04-20 Janssen Pharmaceutica Nv Pirazolo piridinas heteroaromáticas sustituidas y su uso como moduladores del receptor glun2b.
JP2022538774A (ja) 2019-06-14 2022-09-06 ヤンセン ファーマシューティカ エヌ．ベー． ピリジンカルバメート及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用
CA3143102A1 (en) * 2019-06-14 2020-12-17 Janssen Pharmaceutica Nv Substituted pyrazolo[4,3-b]pyridines and their use as glun2b receptor modulators
AU2020290772A1 (en) 2019-06-14 2022-01-06 Janssen Pharmaceutica Nv Pyrazine carbamates and their use as GluN2B receptor modulators
CA3142996A1 (en) 2019-06-14 2020-12-17 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators
WO2020249802A1 (en) 2019-06-14 2020-12-17 Janssen Pharmaceutica Nv Substituted pyrazolo-pyrazines and their use as glun2b receptor modulators
BR112021026668A2 (pt) 2019-07-02 2022-02-15 Nuvation Bio Inc Compostos heterocíclicos como inibidores de bet
CN112174945B (zh) * 2019-07-02 2022-06-07 四川大学 具有抗癌作用的吲唑类化合物及其制备方法和用途
US20220372001A1 (en) * 2019-07-04 2022-11-24 Medshine Discovery Inc. Crystal form of benzimidazole-2-one compound, solvate thereof, crystal form of solvate thereof, and preparation method thereof
EP4013756B1 (en) * 2019-09-20 2024-05-08 Novartis AG Mll1 inhibitors and anti-cancer agents
US11767325B2 (en) 2019-11-26 2023-09-26 Praxis Precision Medicines, Inc. Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators
CN111358787B (zh) * 2020-03-26 2021-03-02 四川大学华西医院 一种杂环化合物在制备治疗肺炎药物中的应用
CN111499644B (zh) * 2020-04-24 2021-07-20 苏州大学 咪唑并[1,5-a]喹唑啉-5(4H)-酮类衍生物及其制备方法和用途
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
CN112266386B (zh) * 2020-10-20 2022-03-25 中山大学 一种2-氯腺嘌呤衍生物、制备方法及应用
CN113121531B (zh) * 2021-04-20 2023-06-13 上海药明康德新药开发有限公司 N杂吲哚类化合物、其合成方法和医药上的用途
CN113234078A (zh) * 2021-04-22 2021-08-10 上海阿拉丁生化科技股份有限公司 一种7-甲基-1,5,7-三氮杂二环[4.4.0]癸-5-烯的合成方法
TW202327594A (zh) 2021-09-23 2023-07-16 大陸商恒翼生物醫藥（上海）股份有限公司 用ｂｅｔ溴結構域抑制劑和ｐａｒｐ抑制劑的組合治療預選患者群體的三陰性乳腺癌的方法

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3508258A1 (de) 1985-03-08 1986-09-18 Bayer Ag, 5090 Leverkusen Ss-lactamantibiotika, verfahren zur herstellung und ihre verwendung als und in arzneimitteln
FR2643903A1 (fr) * 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
DE4023369A1 (de) 1990-07-23 1992-01-30 Thomae Gmbh Dr K Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
RU1836357C (ru) * 1990-07-23 1993-08-23 Др.Карл Томэ ГмбХ Производные бензимидазола, их изомеры, смеси изомеров, гидраты или их физиологически переносимые соли, обладающие антагонистическими в отношении ангиотензина свойствами
SI9210098B (sl) * 1991-02-06 2000-06-30 Dr. Karl Thomae Benzimidazoli, zdravila, ki te spojine vsebujejo, in postopek za njihovo pripravo
DE4225756A1 (de) 1992-01-22 1994-03-10 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5614519A (en) 1991-02-06 1997-03-25 Karl Thomae Gmbh (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
DE4224752A1 (de) 1992-04-11 1994-02-03 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5125961A (en) 1991-08-12 1992-06-30 Monsanto Company Substituted pyridine compounds
DE4219534A1 (de) * 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituierte Biphenylylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4408497A1 (de) * 1994-03-14 1995-09-21 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5854268A (en) 1994-08-02 1998-12-29 Merck Sharp & Dohme, Ltd. Azetidine, pyrrolidine and piperidine derivatives
UA54393C2 (uk) 1995-04-21 2003-03-17 Н'Юросерч А/С Сполуки бензимідазолу, фармацевтичні композиції, що містять ці сполуки, та спосіб лікування чутливих до позитивної модуляції гамк-рецепторних комплексів розладів цнс
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
WO2000034248A1 (en) 1998-12-04 2000-06-15 Neurosearch A/S New benzimidazolone-, benzoxazolone-, or benzothiazolone derivatives as ion channel modulating agents
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
US20020019395A1 (en) 2000-02-01 2002-02-14 Bing-Yan Zhu Indalone and benzimidazolone inhibitors of factor Xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
BR0115243B1 (pt) 2000-10-27 2013-09-17 4-5-diidro-1,2-4-triazin-6-onas,1,2,4-triazin-6-onas, composição fungicida ou inseticida, bem como método para controlar fungo ou inseto
PL363245A1 (en) 2000-12-01 2004-11-15 Osi Pharmaceuticals, Inc. Compounds specific to adenosine a1
HUP0400175A2 (en) * 2001-03-01 2007-07-30 Shionogi & Co Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity, their use and pharmaceutical compositions containing them
ES2251582T3 (es) 2001-03-09 2006-05-01 Pfizer Products Inc. Compuestos antiinflamatorios de bencimidazol.
ATE367814T1 (de) 2001-03-15 2007-08-15 Janssen Pharmaceutica Nv Hiv hemmende pyrazinon-derivate
US20030125344A1 (en) 2001-03-23 2003-07-03 Bayer Corporation Rho-kinase inhibitors
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
HUP0400323A2 (hu) 2001-03-28 2005-11-28 Bristol-Myers Squibb Company Tirozin-kináz inhibitorok és a vegyületeket tartalmazó gyógyszerkészítmények
US20050176858A1 (en) 2002-02-15 2005-08-11 Bridgestone Corporation Rubber composition and pneumatic tire made therefrom
TWI276631B (en) 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
US20040166137A1 (en) 2002-11-08 2004-08-26 Lackey John William Hetero-substituted benzimidazole compounds and antiviral uses thereof
AR043063A1 (es) 2002-12-13 2005-07-13 Altana Pharma Ag Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
CL2004000409A1 (es) 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003902860A0 (en) * 2003-06-06 2003-06-26 Daicel Chemical Industries, Ltd Benzimidazole compounds
JP2007501618A (ja) 2003-08-08 2007-02-01 アバニール・ファーマシューティカルズ タンパク質輸送の選択的薬理学的阻害、および関連した、ヒト疾患を治療する方法
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
US7863310B2 (en) * 2004-02-03 2011-01-04 Eli Lilly And Company Kinase inhibitors
WO2005075432A1 (ja) 2004-02-06 2005-08-18 Chugai Seiyaku Kabushiki Kaisha １−（２ｈ）−イソキノロン誘導体およびその抗ガン剤としての使用
WO2005090317A1 (en) 2004-03-23 2005-09-29 F.Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
US20080015196A1 (en) 2004-04-16 2008-01-17 Neurogen Corporation Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands
ES2604197T3 (es) 2004-06-01 2017-03-03 University Of Virginia Patent Foundation Inhibidores dobles de molécula pequeña de cáncer y angiogénesis
EP1604989A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
WO2005121132A1 (ja) * 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗ｈｃｖ作用を有する縮合ヘテロ環化合物
CA2578075A1 (en) 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
WO2006045010A2 (en) 2004-10-20 2006-04-27 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
WO2006084281A1 (en) * 2005-02-04 2006-08-10 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
BRPI0608581A2 (pt) 2005-03-14 2010-01-19 Transtech Pharma Inc derivados de benzazol, composiÇÕes e mÉtodos de uso como inibidores de b-secretase
KR20080013990A (ko) 2005-05-03 2008-02-13 다우 아그로사이언시즈 엘엘씨 치환된 4,5-디하이드로-1,2,4-트리아진-6-온,1,2,4-트리아진-6-온 및 살진균제로서의 이의 용도
EP1909788A2 (en) 2005-07-29 2008-04-16 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
US7968572B2 (en) 2005-10-03 2011-06-28 Ono Pharmaceuticals Co., Ltd. Nitrogen-containing heterocyclic compound and pharmaceutical application thereof
EP1948614A2 (en) * 2005-11-18 2008-07-30 Takeda San Diego, Inc. Glucokinase activators
RU2396269C2 (ru) 2005-12-01 2010-08-10 Ф.Хоффманн-Ля Рош Аг Производные гетероарилзамещенного пиперидина в качестве ингибиторов печеночной карнитин пальмитоилтрансферазы (l-cpt1)
MX2008010611A (es) 2006-02-17 2008-11-12 Pfizer Ltd Derivados de 3-desazapurina como moduladores de receptores similares a toll.
CN101384593A (zh) 2006-02-17 2009-03-11 辉瑞有限公司 用作tlr7调节剂的3-脱氮嘌呤衍生物
PE20071152A1 (es) 2006-04-03 2007-12-16 Glaxo Group Ltd Compuestos derivados de azabiciclo[3.1.0]hex como moduladores de receptores de dopamina d3
CA2700988A1 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
WO2008072784A1 (en) 2006-12-14 2008-06-19 Astellas Pharma Inc. Polycyclic acid compounds useful as crth2 antagonists and antiallergic agents
SG144809A1 (en) 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
WO2008153701A1 (en) * 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
MX2009013753A (es) 2007-06-26 2010-01-26 Sanofi Aventis Una sintesis regioselectiva catalizada por cobre de bencimidazoles y azabencimidazoles.
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
GB0719235D0 (en) 2007-10-02 2007-11-14 Glaxo Group Ltd Novel compounds
WO2009054790A1 (en) 2007-10-26 2009-04-30 Astrazeneca Ab Amide linked heteroaromatic derivatives as modulators of mglur5
JP2011506322A (ja) 2007-12-07 2011-03-03 エラン ファーマシューティカルズ，インコーポレイテッド 液性腫瘍を治療するための方法および組成物
US8084466B2 (en) * 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
WO2009084693A1 (ja) 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009158258A1 (en) 2008-06-25 2009-12-30 E. I. Du Pont De Nemours And Company Herbicidal dihydro oxo six-membered azinyl isoxazolines
US20120040974A1 (en) 2008-08-18 2012-02-16 Yale University Mif modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
US8877772B2 (en) 2008-11-25 2014-11-04 University Of Rochester Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors
EP2370413B1 (en) 2008-12-08 2015-08-05 Arena Pharmaceuticals, Inc. Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
US20120202793A1 (en) 2009-03-09 2012-08-09 Paul Sweetnam Rho kinase inhibitors
CA2992231C (en) 2009-03-18 2022-03-29 Resverlogix Corp. Phenyl-quinazolin-4(3h)-one and phenyl-pyrido[2,3-d]pyrimidin-4(3h)-one derivatives and compositions thereof useful as anti-inflammatory agents
WO2010107739A2 (en) 2009-03-18 2010-09-23 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions of treating a flaviviridae family viral infection
KR20190091564A (ko) 2009-04-22 2019-08-06 리스버로직스 코퍼레이션 신규한 소염제
AU2010244553A1 (en) 2009-05-05 2011-12-01 F. Hoffmann-La Roche Ag Isoxazole-pyridine derivatives
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011054845A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR101424989B1 (ko) 2009-11-05 2014-07-31 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
WO2011062437A2 (ko) 2009-11-20 2011-05-26 에스케이케미칼주식회사 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
KR101165996B1 (ko) 2010-04-23 2012-07-18 주식회사 녹십자 프탈라지논 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
WO2011156626A1 (en) 2010-06-09 2011-12-15 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2011159926A1 (en) 2010-06-16 2011-12-22 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2012003576A1 (en) * 2010-07-06 2012-01-12 Université de Montréal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
WO2012009258A2 (en) 2010-07-13 2012-01-19 Edward Roberts Peptidomimetic galanin receptor modulators
WO2012021382A1 (en) 2010-08-12 2012-02-16 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2
WO2012040499A2 (en) 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
KR101242572B1 (ko) 2010-10-12 2013-03-19 한국화학연구원 5-환 헤테로 아릴로 치환된 프탈라지논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 약학적 조성물
GB201018147D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Method of treatment
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
CN102731409A (zh) 2011-04-08 2012-10-17 中国科学院上海药物研究所 一类哒嗪酮类化合物，其药物组合物、制备方法及用途
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
CN103945848B (zh) 2011-11-01 2016-09-07 雷斯韦洛吉克斯公司 被取代的喹唑啉酮的口服即释制剂
US8685959B2 (en) * 2011-12-01 2014-04-01 Chemocentryx, Inc. Substituted benzimidazoles and benzopyrazoles as CCR(4) antagonists
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
EP2838881B1 (en) 2012-04-20 2018-08-08 AbbVie Inc. Isoindolone derivatives
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
JP6359008B2 (ja) * 2012-06-11 2018-07-18 ユーシービー バイオファルマ エスピーアールエル Ｔｎｆ−アルファ調節ベンゾイミダゾール
WO2014031928A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
JP2015532650A (ja) * 2012-09-05 2015-11-12 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 非生物的植物ストレスに対する活性物質としての置換された２−アミドベンズイミダゾール類、２−アミドベンゾオキサゾール類および２−アミドベンゾチアゾール類またはそれらの塩の使用
WO2014043246A1 (en) 2012-09-11 2014-03-20 The Board Of Trustees Of The University Of Illinois Enoyl reductase inhibitors with antibacterial activity
ES2625945T3 (es) 2012-11-14 2017-07-21 Glaxosmithkline Llc Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
CN104995190A (zh) 2012-12-20 2015-10-21 拜耳医药股份有限公司 Bet蛋白抑制剂二氢喹喔啉酮
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
CA2901799A1 (en) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US10053454B2 (en) 2013-02-27 2018-08-21 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
WO2014164771A1 (en) 2013-03-11 2014-10-09 Abbvie Inc. Bromodomain inhibitors
WO2014165127A1 (en) 2013-03-12 2014-10-09 Abbvie Inc. Pyrrole amide inhibitors
TW201443051A (zh) 2013-03-12 2014-11-16 Abbvie Inc 二氫－吡咯并吡啶酮抑制劑
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
KR20150135359A (ko) 2013-03-14 2015-12-02 컨버진 엘엘씨 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물
WO2014140077A1 (en) 2013-03-14 2014-09-18 Glaxosmithkline Intellectual Property (No.2) Limited Furopyridines as bromodomain inhibitors
MX2015012456A (es) * 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
US20160039842A1 (en) 2013-03-15 2016-02-11 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
SG10201707487VA (en) 2013-03-15 2017-10-30 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
US9199988B2 (en) 2013-03-27 2015-12-01 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues
JP6370368B2 (ja) 2013-03-27 2018-08-08 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 Ｂｒｄ４阻害剤としてのインドリノン類似体
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
JP6388915B2 (ja) 2013-04-26 2018-09-12 ベイジーン，リミテッド 置換５−（３，５−ジメチルイソオキサゾール−４−イル）インドリン−２−オン
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
EP3412675A1 (en) 2013-05-27 2018-12-12 Novartis AG Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
JP2016521722A (ja) 2013-06-17 2016-07-25 バイエル ファーマ アクチエンゲゼルシャフト 置換フェニル−２，３−ベンゾジアゼピン
NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
JP6461118B2 (ja) 2013-06-21 2019-01-30 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての新規の置換された二環式化合物
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
ES2648876T3 (es) 2013-07-23 2018-01-08 Bayer Pharma Aktiengesellschaft Dihidropirido[3,4-b]pirazinonas sustituidas como inhibidores duales de proteínas BET y quinasas tipo polo
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
EA201690087A1 (ru) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. Новые квиназолиноны как ингибиторы бромодомена
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
WO2015074064A2 (en) 2013-11-18 2015-05-21 Bair Kenneth W Tetrahydroquinoline compositions as bet bromodomain inhibitors
EP3071205B1 (en) 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
GB201321739D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US20190055235A1 (en) 2014-12-17 2019-02-21 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors

Also Published As

Publication number Publication date
HK1222335A1 (zh) 2017-06-30
JP2019038839A (ja) 2019-03-14
NZ714669A (en) 2021-07-30
JP2016523259A (ja) 2016-08-08
WO2015002754A3 (en) 2015-03-12
SG10201710705UA (en) 2018-02-27
ZA201800854B (en) 2019-07-31
EA035601B1 (ru) 2020-07-14
US10010556B2 (en) 2018-07-03
EA201592143A1 (ru) 2016-07-29
WO2015002754A2 (en) 2015-01-08
US20180161337A1 (en) 2018-06-14
JP2020073521A (ja) 2020-05-14
CN109939113A (zh) 2019-06-28
AU2014284616A2 (en) 2016-06-09
ES2806135T3 (es) 2021-02-16
MX365864B (es) 2019-06-18
IL242844B (en) 2020-10-29
NZ754629A (en) 2021-07-30
ZA201600272B (en) 2018-07-25
CA2915838A1 (en) 2015-01-08
AU2019201212B2 (en) 2020-11-26
AU2019201212C1 (en) 2021-03-04
AU2014284616B2 (en) 2019-02-28
CN105407888A (zh) 2016-03-16
BR112015031073A2 (pt) 2017-07-25
DK3010503T3 (da) 2020-05-25
PT3010503T (pt) 2020-06-16
US10772892B2 (en) 2020-09-15
CA2915838C (en) 2023-04-18
JP6461121B2 (ja) 2019-01-30
CN105407888B (zh) 2019-05-21
BR112015031073B1 (pt) 2022-11-29
KR102307566B1 (ko) 2021-10-05
SI3010503T1 (sl) 2020-07-31
HUE049469T2 (hu) 2020-09-28
EP3674300A1 (en) 2020-07-01
US20190358237A1 (en) 2019-11-28
US20170216301A1 (en) 2017-08-03
AU2019201212A1 (en) 2019-03-14
JP7037679B2 (ja) 2022-03-16
US10363257B2 (en) 2019-07-30
PL3010503T3 (pl) 2020-08-24
CA3190653A1 (en) 2015-01-08
US20210177855A1 (en) 2021-06-17
EP3674300B1 (en) 2022-10-12
JP6828131B2 (ja) 2021-02-10
HK1216722A1 (zh) 2016-12-02
EP3010503A4 (en) 2017-03-08
KR20160023684A (ko) 2016-03-03
US9663520B2 (en) 2017-05-30
JP6731463B2 (ja) 2020-07-29
US20160159801A1 (en) 2016-06-09
JP2021073231A (ja) 2021-05-13
EP3010503A2 (en) 2016-04-27
MX2015017045A (es) 2016-08-03
AU2014284616A1 (en) 2015-12-24
SG11201510409QA (en) 2016-01-28
EP3010503B1 (en) 2020-03-11
CN109939113B (zh) 2022-02-15
US11446306B2 (en) 2022-09-20

Similar Documents

Publication Publication Date Title
HRP20200854T1 (hr) Novi biciklički inhibitori bromodomene
EP2332940B1 (en) Azaindoles useful as inhibitors of JAK and other protein kinases
CA2968633C (en) 2-aminopyrimidine compound and pharmaceutical composition and use thereof
WO2015015318A4 (en) Novel quinazolinones as bromodomain inhibitors
JP2016522246A5 (hr)
JP6487925B2 (ja) セリン／トレオニンキナーゼ阻害剤
TWI619717B (zh) 三唑并吡
RU2014131378A (ru) Ингибиторы бромдомена
JP2017538721A5 (hr)
TW201202221A (en) Nitrogen containing heteroaryl compounds
JP2016525078A5 (hr)
JP2010503701A (ja) 増殖性疾患の治療に有用なキナーゼ阻害剤
JP2020504747A5 (hr)
TW200827358A (en) Compounds modulating C-FMS and/or C-KIT activity and uses therefor
NZ560402A (en) Imidazo (1,2-A) pyridine compounds as VEGF-R2 inhibitors
CA2671744A1 (en) Compounds and compositions as protein kinase inhibitors
SG194105A1 (en) Pyridine-and pyrazine derivatives
BR112020003254A2 (pt) moduladores da piruvato quinase e uso destes
KR20220028075A (ko) 티로신 키나제 비-수용체 1 (tnk1) 억제제 및 그의 용도
AU2020277541A1 (en) Indole derivative-containing inhibitor, preparation method therefor and application thereof
EP4136073A1 (en) Substituted pyridines for the treatment of inflammatory diseases
AU2018244211A1 (en) Piperidinyl- and piperazinyl-substituted heteroaromatic carboxamides as modulators of GPR6
BR112019007271A2 (pt) compostos de quinoxalina como inibidores do receptor da tirosina quinase do tipo iii
IL274198B2 (en) Use of Nox inhibitors to treat cancer
WO2020065048A1 (en) Novel compounds as nadph oxidase inhibitors