ES2650744T3 - Inhibidores de la caseína quinasa 1 delta (CK1delta) - Google Patents

Inhibidores de la caseína quinasa 1 delta (CK1delta) Download PDF

Info

Publication number
ES2650744T3
ES2650744T3 ES14190691.7T ES14190691T ES2650744T3 ES 2650744 T3 ES2650744 T3 ES 2650744T3 ES 14190691 T ES14190691 T ES 14190691T ES 2650744 T3 ES2650744 T3 ES 2650744T3
Authority
ES
Spain
Prior art keywords
compound
disease
alkyl
tau
dementia
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES14190691.7T
Other languages
English (en)
Spanish (es)
Inventor
Joseph M. Sheridan
Jonathan R. Heal
William D.O. Hamilton
Ian Pike
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Proteome Sciences PLC
Original Assignee
Electrophoretics 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
Priority claimed from GBGB1021161.3A external-priority patent/GB201021161D0/en
Priority claimed from GBGB1109162.6A external-priority patent/GB201109162D0/en
Application filed by Electrophoretics Ltd filed Critical Electrophoretics Ltd
Application granted granted Critical
Publication of ES2650744T3 publication Critical patent/ES2650744T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/495—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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—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
    • A61K31/4985—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/495—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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/28—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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Toxicology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ES14190691.7T 2010-12-14 2011-12-14 Inhibidores de la caseína quinasa 1 delta (CK1delta) Active ES2650744T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB1021161.3A GB201021161D0 (en) 2010-12-14 2010-12-14 Casein kinase 1delta (CK1Delta) inhibitors
GB201021161 2010-12-14
GBGB1109162.6A GB201109162D0 (en) 2011-06-01 2011-06-01 Casein kinase 1Delta (CK1Delta) inhibitors
GB201109162 2011-06-01

Publications (1)

Publication Number Publication Date
ES2650744T3 true ES2650744T3 (es) 2018-01-22

Family

ID=45444638

Family Applications (2)

Application Number Title Priority Date Filing Date
ES14190691.7T Active ES2650744T3 (es) 2010-12-14 2011-12-14 Inhibidores de la caseína quinasa 1 delta (CK1delta)
ES11804754.7T Active ES2553610T3 (es) 2010-12-14 2011-12-14 Inhibidores de la caseína cinasa 1 delta (CK1delta)

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES11804754.7T Active ES2553610T3 (es) 2010-12-14 2011-12-14 Inhibidores de la caseína cinasa 1 delta (CK1delta)

Country Status (10)

Country Link
US (5) US20140018540A1 (enExample)
EP (3) EP2651404B1 (enExample)
JP (4) JP5937102B2 (enExample)
CN (3) CN105920010A (enExample)
AU (2) AU2011343039B2 (enExample)
CA (1) CA2818903C (enExample)
DK (1) DK2835131T3 (enExample)
ES (2) ES2650744T3 (enExample)
HK (1) HK1214527A1 (enExample)
WO (2) WO2012080727A2 (enExample)

Families Citing this family (239)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT1993360T (lt) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma
AU2009204483B2 (en) 2008-01-04 2014-03-13 Intellikine, Llc Certain chemical entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2552208A4 (en) * 2010-03-31 2014-07-09 Glaxo Group Ltd IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5937102B2 (ja) * 2010-12-14 2016-06-22 エレクトロフォレティクス リミテッド カゼインキナーゼ１デルタ（ｃｋ１デルタ）阻害剤
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
KR20180080358A (ko) 2011-01-10 2018-07-11 인피니티 파마슈티칼스, 인코포레이티드 이소퀴놀린온 및 이의 고체 형태의 제조 방법
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
AR087701A1 (es) 2011-08-31 2014-04-09 Japan Tobacco Inc Derivados de pirazol con actividad inhibidora de sglt1
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
HUE043171T2 (hu) 2011-10-07 2019-08-28 Takeda Pharmaceuticals Co Neurodegeneratív betegségek kezelésére hasznos 1-arilkarbonil-4-oxi-piperidinvegyületek
KR101987514B1 (ko) 2011-10-18 2019-06-10 아스텔라스세이야쿠 가부시키가이샤 이환식 헤테로환 화합물
AR090037A1 (es) 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
EP2785692B1 (en) 2011-12-01 2017-09-27 ChemoCentryx, Inc. Substituted anilines as ccr(4) antagonists
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
HRP20161774T1 (hr) 2012-06-13 2017-02-24 F. Hoffmann - La Roche Ag Novi diazaspirocikloalkan i azaspirocikloalkan
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9630976B2 (en) 2012-07-03 2017-04-25 Ono Pharmaceutical Co., Ltd. Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes
WO2014009891A1 (en) * 2012-07-11 2014-01-16 Piramal Enterprises Limited Heterocyclic compounds for use in the treatment of cancers
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
CN113679717A (zh) 2012-08-22 2021-11-23 康奈尔大学 用于抑制肌成束蛋白的方法
KR102046499B1 (ko) * 2012-08-24 2019-11-19 트레벤티스 코포레이션 벤조푸라잔 항아밀로이드 화합물 및 방법
CN102850341B (zh) * 2012-09-05 2015-02-18 浙江工业大学 一种噻二唑类化合物及其制备与应用
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
BR112015004111A2 (pt) 2012-09-25 2017-07-04 Hoffmann La Roche novos derivados bicíclicos
CN103739594A (zh) * 2012-10-17 2014-04-23 南京大学 一类含吡嗪环和三氮唑结构的席夫碱类衍生物及其制法
IL291945B2 (en) 2012-11-01 2025-11-01 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
CA2888338C (en) 2012-11-27 2021-07-20 Thomas Helledays Stiftelse For Medicinsk Forskning Mth1 inhibitors for treatment of cancer
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014103801A1 (ja) * 2012-12-28 2014-07-03 株式会社新日本科学 イミダゾピリジン誘導体を有効成分として含むｏｃｔ３活性阻害剤又はｏｃｔ３検出剤
WO2014124458A1 (en) 2013-02-11 2014-08-14 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2014144747A1 (en) * 2013-03-15 2014-09-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
HK1220325A1 (zh) 2013-03-15 2017-05-05 Whitehead Institute For Biomedical Research 苯并咪唑衍生物及其用途
US9045477B2 (en) * 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
US9797882B2 (en) 2013-07-09 2017-10-24 The Translational Genomics Research Institute Method of screening for a compound for inhibitory activity of FN14-tweak interaction
US9238034B2 (en) * 2013-07-09 2016-01-19 The Translational Genomics Research Institute FN14 antagonists and therapeutic uses thereof
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
GB201314452D0 (en) 2013-08-13 2013-09-25 Ostara Biomedical Ltd Embryo implantation
RU2570907C2 (ru) * 2013-10-21 2015-12-20 Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан" Производные 3-ациламинопиридин-2(1h)-она, применимые как ингибиторы серин-треониновой протеинкиназы gsk3b в качестве лекарственных препаратов для лечения диабета ii типа.
KR102254957B1 (ko) 2013-11-22 2021-05-25 씨엘 바이오사이언시즈 엘엘씨 골다공증 치료 및 예방을 위한 가스트린 길항제(ｅｇ ｙｆ476, 네타제피드)
KR20160087900A (ko) 2013-11-26 2016-07-22 에프. 호프만-라 로슈 아게 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일
GB201321738D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
WO2015106025A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
US10087186B2 (en) 2014-01-29 2018-10-02 Glaxosmithkline Intellectual Property Development Limited Compounds as LRRK2 kinase inhibitors
ES2717757T3 (es) 2014-01-29 2019-06-25 Glaxosmithkline Ip Dev Ltd Compuestos
US10167286B2 (en) 2014-02-11 2019-01-01 Mitokinin, Inc. Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PE20161573A1 (es) 2014-02-13 2017-01-19 Incyte Corp Ciclopropilamina como inhibidor de la lsd1
US9493450B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
CA2940144C (en) 2014-02-20 2023-06-13 Cornell University Substituted indazol-3-yl derivatives and pharmaceutical compositions thereof useful as inhibitor of fascin
HUE044999T2 (hu) * 2014-02-27 2019-12-30 Treventis Corp Benzofurazán tartalmú anti-amiloid vegyületek
KR20160128428A (ko) 2014-03-26 2016-11-07 에프. 호프만-라 로슈 아게 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물
SI3122750T1 (sl) 2014-03-26 2019-12-31 F. Hoffmann-La Roche Ag Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA)
WO2015157382A1 (en) * 2014-04-11 2015-10-15 Emory University Treatment of neurodegenerative diseases with asparagine endopeptidase (aep) inhibitors and compositions related thereto
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
US9840482B2 (en) * 2014-04-19 2017-12-12 Sunshine Lake Pharma Co., Ltd. Sulfonamide derivatives and pharmaceutical applications thereof
HUE057317T2 (hu) * 2014-04-23 2022-04-28 Dart Neuroscience Llc Helyettesített [1,2,4]triazolo[1,5-A]pirimidin-7-IL vegyületeket tartalmazó készítmények mint PDE2 inhibítorok
EP3140298A1 (en) 2014-05-07 2017-03-15 Pfizer Inc. Tropomyosin-related kinase inhibitors
CN104059060B (zh) * 2014-05-30 2017-08-01 西安交通大学 一种5‑(1h‑吲哚‑3‑亚甲基)‑1,3‑噻唑烷‑4‑酮类衍生物及其合成方法和应用
EP3152195A4 (en) 2014-06-04 2017-12-13 Thomas Helledays Stiftelse För Medicinsk Forskning Mth1 inhibitors for treatment of cancer
RU2016151390A (ru) 2014-06-04 2018-07-17 Томас Хелледайс Стифтелсе Фёр Медисинск Форскнинг Ингибиторы мтн1 для лечения воспалительных и аутоиммунных заболеваний
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
CA2954681A1 (en) 2014-07-31 2016-02-04 Merck Patent Gmbh Indolizine derivatives and their use in neurodegenerative diseases
EP3189070A4 (en) 2014-08-04 2018-06-27 Drexel University Novel compounds and methods of treating or ameliorating an il-1r-mediated disease or disorder using same
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
EP3204358B1 (en) 2014-10-07 2018-09-19 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
GB201419579D0 (en) * 2014-11-03 2014-12-17 Iomet Pharma Ltd Pharmaceutical compound
TWI568737B (zh) 2014-11-05 2017-02-01 達特神經科學（開曼）有限責任公司 作為ｐｄｅ２抑制劑之經取代的５－甲基－［１，２，４］三唑并［１，５－ａ］嘧啶－２－胺化合物
JP6708130B2 (ja) 2014-12-25 2020-06-10 小野薬品工業株式会社 キノリン誘導体
GB201501302D0 (en) 2015-01-27 2015-03-11 Ostara Biomedical Ltd Embryo implantation
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
EP4591936A3 (en) 2015-03-23 2025-10-15 Tianli Biotech Pty Ltd Treatment of respiratory diseases
PE20180455A1 (es) 2015-04-03 2018-03-05 Incyte Corp Compuestos heterociclicos como inhibidores de lsd1
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
EP3288933B1 (en) * 2015-04-30 2021-10-06 Musc Foundation for Research Development Oxindole compounds and pharmaceutical compositions thereof
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
GB201508276D0 (en) 2015-05-14 2015-06-24 Electrophoretics Ltd A casein kinase 1 delta inhibitor
GB201509134D0 (en) 2015-05-28 2015-07-15 Electrophoretics Ltd Biomolecules involved in Alzheimer's disease
JP6707630B2 (ja) * 2015-06-01 2020-06-10 バンタム、ファーマシューティカル、リミテッド、ライアビリティー、カンパニーＢａｎｔａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌ， Ｌｌｃ 置換ピラゾールおよびピロール化合物、および翻訳開始の阻害およびこれらに関連する疾患および障害の治療のためにこれらを用いる方法
WO2016202758A1 (en) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
WO2016202756A1 (en) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
US10167270B2 (en) * 2015-07-01 2019-01-01 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017000277A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
SG10202001219UA (en) 2015-08-12 2020-03-30 Incyte Corp Salts of an lsd1 inhibitor
CN105061462B (zh) * 2015-08-18 2017-05-24 沈阳药科大学 含有酰胺的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用
JP6886967B2 (ja) * 2015-09-04 2021-06-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ フェノキシメチル誘導体
TWI730002B (zh) 2015-09-18 2021-06-11 日商科研製藥股份有限公司 聯芳系化合物及含有此化合物之醫藥
RU2018112230A (ru) 2015-09-24 2019-10-30 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов atx
CN107635995B (zh) 2015-09-24 2022-08-19 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
JP6877413B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
WO2017062500A2 (en) * 2015-10-05 2017-04-13 The Trustees Of Columbia University In The City Of New York Activators of autophagic flux and phospholipase d and clearance of protein aggregates including tau and treatment of proteinopathies
GB201517523D0 (en) 2015-10-05 2015-11-18 Ostara Biomedical Ltd Methods and compositions for managing reproduction
WO2017063966A1 (en) 2015-10-13 2017-04-20 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-benzothiazole compounds
ES2765738T3 (es) 2015-11-02 2020-06-10 Janssen Pharmaceutica Nv Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo
US10450274B2 (en) * 2015-12-07 2019-10-22 Hinova Pharmaceuticals Inc. Quinoline compounds, preparation methods thereof, and uses thereof as urate transporter inhibitor drug
US20200375996A1 (en) * 2015-12-15 2020-12-03 D.E. Shaw Research, Llc Method of treating neurodegenerative disorders by rescuing alpha-synuclein toxicity
CN107033087B (zh) * 2016-02-04 2020-09-04 西华大学 1h-吲唑-4-胺类化合物及其作为ido抑制剂的用途
WO2017133258A1 (zh) * 2016-02-04 2017-08-10 西华大学 1h-吲唑类衍生物及其作为ido抑制剂的用途
CN107840826B (zh) * 2016-09-19 2021-07-09 西华大学 1h-吲唑类衍生物及其作为ido抑制剂的用途
CN109414410B (zh) 2016-04-22 2022-08-12 因赛特公司 Lsd1抑制剂的制剂
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
EA202092442A3 (ru) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
CA3028718A1 (en) 2016-06-24 2017-12-28 Infinity Pharmaceuticals, Inc. Combination therapies
BR112019000589A2 (pt) 2016-07-14 2019-04-24 Pfizer Inc. pirimidina carboxamidas como inibidores da enzima vanina-1
WO2018030762A1 (ko) * 2016-08-09 2018-02-15 세종대학교산학협력단 Ampk 억제기능에 기반한 뇌졸중 치료용 약학적 조성물
JP7471818B2 (ja) 2016-08-18 2024-04-22 ヴィダック ファーマ リミテッド ピペラジン誘導体、医薬組成物、及びその使用方法
MY199759A (en) 2016-09-02 2023-11-21 Tisento Therapeutics Inc Fused bicyclic sgc stimulators
CN106432235B (zh) * 2016-10-19 2018-02-02 南通大学 靶向CDK和DNA的β‑咔啉衍生物及其制备方法和医药用途
MA46589A (fr) 2016-10-24 2019-08-28 Yumanity Therapeutics Inc Composés et utilisations de ces derniers
EP3535269B1 (en) 2016-11-02 2020-12-09 Janssen Pharmaceutica NV [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors
UA125302C2 (uk) * 2016-11-02 2022-02-16 Янссен Фармацевтика Нв Похідні [1,2,4]триазоло[1,5-a]піримідину як інгібітори pde2
KR20190067788A (ko) * 2016-11-02 2019-06-17 얀센 파마슈티카 엔.브이. Pde2 억제제로서의 [1,2,4]트리아졸로[1,5-a]피리미딘 화합물
US11008325B2 (en) 2016-11-14 2021-05-18 Virginia Commonwealth University Inhibitors of cancer invasion, attachment, and/or metastasis
EP3541378A4 (en) * 2016-11-16 2020-10-07 University of South Florida ALLOSTERIC ANTAGONISTS OF GPRC6A AND THEIR USE IN THE MITIGATION OF PROTEINOPATHIES
EP3566055B1 (en) 2017-01-06 2025-03-12 Janssen Pharmaceutica NV Scd inhibitor for the treatment of neurological disorders
KR102446529B1 (ko) * 2017-01-10 2022-09-23 에테하 취리히 세포 보호 화합물 및 이의 용도
CN106831573B (zh) * 2017-01-23 2019-05-24 南阳师范学院 (n-1,2,3,4-四氢异喹啉基)-阿魏酰胺化合物、制备方法及其应用
UA123810C2 (uk) 2017-01-23 2021-06-02 Цадент Терапеутікс, Інк. Модулятори калієвих каналів
CN106748969B (zh) * 2017-01-23 2019-06-18 南阳师范学院 一种n-(4-苄基哌啶基)-阿魏酰胺化合物、制备方法及其用途
CN119707932A (zh) 2017-01-26 2025-03-28 小野药品工业株式会社 喹啉衍生物的乙磺酸盐
NZ755447A (en) 2017-02-01 2023-05-26 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer
CN106943397B (zh) * 2017-03-01 2020-08-04 浙江大学 雄激素受体拮抗剂及其应用
EP3596059B1 (en) 2017-03-16 2024-04-24 F. Hoffmann-La Roche AG Heterocyclic compounds useful as dual atx/ca inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
PT3448859T (pt) 2017-03-20 2019-10-25 Forma Therapeutics Inc Composições de pirrolopirrole como ativadores de piruvato quinase (pkr).
AU2018239542C1 (en) 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
MX388196B (es) 2017-04-26 2025-03-19 Basilea Pharm Int Ag Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos.
EP3634406B1 (en) * 2017-05-12 2023-09-06 Board of Trustees of The Southern Illinois University on behalf of Southern Illinois University Edwardsville 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JOP20190282A1 (ar) 2017-06-09 2019-12-05 Novartis Ag مركبات وتركيبات لحث تكوّن الغضاريف
CN110997664A (zh) * 2017-06-14 2020-04-10 欧洲分子生物学实验室 用于疗法的苯并呋喃酰胺及其杂芳族类似物
KR20200019228A (ko) 2017-06-21 2020-02-21 미토키닌, 인크. 신경퇴행성 및 미토콘드리아 질환의 치료를 위한 조성물 및 이를 사용하는 방법
GB201710851D0 (en) * 2017-07-06 2017-08-23 Galápagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
WO2019014100A1 (en) 2017-07-10 2019-01-17 Celgene Corporation ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF
CA3069720A1 (en) 2017-07-11 2019-01-17 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
CN111094264A (zh) * 2017-09-11 2020-05-01 保土谷化学工业株式会社 具有嘧啶环结构的化合物及有机电致发光元件
TWI846350B (zh) 2017-09-15 2024-06-21 美商佛瑪治療公司 作為ＣＢＰ／ｐ３００抑制劑之四氫－咪唑並喹啉化合物
JP7223998B2 (ja) 2017-10-13 2023-02-17 小野薬品工業株式会社 Ａｘｌ阻害剤を有効成分として含む固形がん治療剤
CA3079081A1 (en) 2017-10-19 2019-04-25 Michael D. Bartberger Benzimidazole derivatives and their uses
CA3083000A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. Compounds and uses thereof
WO2019123375A1 (en) * 2017-12-21 2019-06-27 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
JP2021507945A (ja) * 2017-12-21 2021-02-25 グリアファーム エスエー 認知症を含む神経障害のための組成物および治療方法
US20190292188A1 (en) 2018-02-27 2019-09-26 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
WO2019173437A1 (en) * 2018-03-06 2019-09-12 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Positive allosteric modulators of dopamine 1 receptor and method of use thereof
EP3543231A1 (en) * 2018-03-19 2019-09-25 ETH Zurich Compounds for treating cns- and neurodegenerative diseases
ES3043183T3 (en) 2018-03-23 2025-11-25 Janssen Pharmaceutica Nv Compounds and uses thereof
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
TWI815887B (zh) * 2018-05-15 2023-09-21 美商愛彼特生物製藥股份有限公司 經取代的2,2'-雙嘧啶基化合物、其類似物及其使用方法
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
MX2023013508A (es) 2018-06-29 2023-12-13 Forma Therapeutics Inc Inhibicion de la proteina de union a creb (cbp).
CN113166153B (zh) 2018-07-05 2024-11-01 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
BR112021002165A2 (pt) * 2018-08-06 2021-05-04 The Board Of Trustees Of The Leland Stanford Junior University composto, composição farmacêutica, e, métodos para tratar uma doença neurodegenerativa e deficiência cognitiva associada ao envelhecimento e neuroinflamação
KR102817790B1 (ko) 2018-08-29 2025-06-05 케모센트릭스, 인크. C-c 케모카인 수용체 4(ccr4) 길항제 및 하나 이상의 면역 체크포인트 억제제를 사용한 병용 요법
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
US11278527B2 (en) 2018-09-04 2022-03-22 Brown University Compositions and methods for the modulation of the corticotropin releasing factor binding protein and the treatment of alcohol use disorder
CN113301900B (zh) * 2018-09-09 2024-11-29 夸纳特制药股份公司 酪蛋白激酶1抑制剂在治疗血管疾病中的应用
CN112996795B (zh) 2018-09-18 2024-11-12 尼坎治疗公司 作为src同源-2磷酸酶抑制剂的稠合的三环衍生物
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
MX2021004647A (es) 2018-10-22 2021-08-16 Novartis Ag Formas cristalinas de moduladores de los canales de potasio.
CN112912139B (zh) * 2018-10-23 2024-07-09 第一三共株式会社 联芳基衍生物
WO2020093098A1 (en) 2018-11-07 2020-05-14 The University Of Melbourne Novel compounds for the treatment of respiratory diseases
CN109503563B (zh) * 2018-12-10 2020-05-12 济南大学 多功能乙酰胆碱酯酶抑制剂及其应用
KR102128509B1 (ko) * 2018-12-19 2020-07-01 한국과학기술연구원 말단 아민기에 아릴 또는 헤테로아릴기가 치환된 신규한 히드라존 유도체 및 이의 용도
EP3906229A4 (en) * 2019-01-04 2022-11-16 Bellbrook Labs, Llc INHIBITORS OF CGAS ACTIVITY AS THERAPEUTIC AGENT
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
MX2021008903A (es) 2019-01-24 2021-11-04 Yumanity Therapeutics Inc Compuestos y usos de los mismos.
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US12351577B2 (en) 2019-03-15 2025-07-08 Forma Therapeutics, Inc. Inhibiting cyclic AMP-responsive element-binding protein (CREB)
US11505548B2 (en) 2019-04-26 2022-11-22 Celgene Corporation Heterocyclic compounds and their use for treatment of helminthic infections and diseases
UY38687A (es) 2019-05-17 2023-05-15 Novartis Ag Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso
LT4299135T (lt) 2019-06-18 2025-09-10 Pfizer Inc. Benzizoksazolo sulfonamido dariniai
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN119431323A (zh) 2019-07-31 2025-02-14 贝林格尔·英格海姆国际有限公司 作为cd38抑制剂的杂双环酰胺
RU2746423C2 (ru) * 2019-09-02 2021-04-13 Общество с ограниченной ответственностью "Научно-исследовательский институт ХимРар" (ООО "НИИ ХимРар") Ингибитор вируса гепатита В (ВГВ)
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
US12343335B2 (en) 2019-11-14 2025-07-01 Zincure Corp. Pharmaceutical composition for treating multiple sclerosis on basis of AMPK inhibitory function and zinc homeostasis control function
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
DK4069691T3 (da) 2019-12-06 2024-10-28 Vertex Pharma Substituerede tetrahydrofuraner som modulatorer af natriumkanaler
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AR122711A1 (es) * 2020-06-25 2022-09-28 Alchemedicine Inc COMPUESTO HETEROCÍCLICO COMO INHIBIDOR DE CASEÍNA QUINASA 1d Y/O QUINASA 5 TIPO RECEPTOR DE ACTIVINA
CA3191164A1 (en) * 2020-08-10 2022-02-17 Dana-Farber Cancer Institute, Inc. Substituted 1,2,4-oxadiazoles as small molecule inhibitors of ubiquitin-specific protease 28
AU2021345564A1 (en) * 2020-09-17 2023-06-01 Janssen Pharmaceutica Nv Casein kinase 1 delta modulators
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
GB202101734D0 (en) * 2021-02-08 2021-03-24 Cerevance Inc Novel Compounds
TW202246232A (zh) 2021-02-19 2022-12-01 英商蘇多生物科學有限公司 Ｔｙｋ２抑制劑及其用途
TW202246233A (zh) 2021-02-19 2022-12-01 英商蘇多生物科學有限公司 Tyk2抑制劑及其用途
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022222963A1 (zh) * 2021-04-21 2022-10-27 长春金赛药业有限责任公司 含咪唑稠环类衍生物、其制备方法及其在医药上的应用
MA64853B1 (fr) 2021-06-04 2025-11-28 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hétéro)aryl) tétrahydrofuran carboxamides utilisés en tant que modulateurs de canaux sodiques
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AU2022364646B2 (en) * 2021-10-15 2025-10-09 Lomond Therapeutics, Inc. SUBSTITUTED 1H-PYRAZOLO [4,3-c] QUINOLINES, METHODS OF PREPARATION, AND USE THEREOF
JP2025513455A (ja) 2022-04-22 2025-04-24 バーテックス ファーマシューティカルズ インコーポレイテッド 疼痛の治療のためのヘテロアリール化合物
CN115466211B (zh) * 2022-06-09 2024-02-23 中国人民解放军空军军医大学 一种n-苯基喹啉-4-胺类化合物及其应用
US20250388584A1 (en) * 2022-07-14 2025-12-25 Shanghai Raising Pharmaceutical Co., Ltd. Tpk agonist and method for treating neurodegenerative diseases using same
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
WO2024083150A1 (zh) * 2022-10-19 2024-04-25 长春金赛药业有限责任公司 一种nk3r拮抗剂的晶型及其制备方法和应用
CN120917015A (zh) * 2023-01-20 2025-11-07 元启(苏州)生物制药有限公司 Srpk1抑制剂和使用方法
WO2024159285A1 (pt) * 2023-01-30 2024-08-08 Eurofarma Laboratórios S.A. Compostos aril piridinas bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits
PY2404641A (es) * 2023-01-30 2024-10-03 Eurofarma Laboratorios S A COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y SUS KITS
IT202400002560A1 (it) * 2024-02-07 2025-08-07 Univ Pisa Inibitori della proteina rock per uso nel trattamento della fibrosi polmonare
CN118666857B (zh) * 2024-06-26 2025-02-25 江西农业大学 一种喹啉类化合物及其在农用杀菌剂中的应用
CN119060061B (zh) * 2024-08-26 2025-09-16 浙江师范大学 一类苯并嘧啶硫醚类化合物作为sting蛋白小分子抑制剂的应用

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9506197D0 (en) 1995-03-27 1995-05-17 Hoffmann La Roche Inhibition of tau-tau association.
US5545656A (en) * 1995-04-05 1996-08-13 Pfizer Inc. 2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease
US20030219427A1 (en) * 1998-08-18 2003-11-27 Allen Hamish J. TPL-2/COT kinase and methods of use
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6087363A (en) * 1999-07-16 2000-07-11 Harbor Branch Oceanographic Institution, Inc. Use of imidazole and indole compounds as inhibitors of nitric oxide synthase
CN100339379C (zh) * 2000-09-01 2007-09-26 圣诺菲-合成实验室公司 2－吡啶基－6,7,8,9－四氢嘧啶并[1,2－а]嘧啶－4－酮和7－吡啶基－2,3－二氢咪唑并[1,2－а]嘧啶－5（1H）酮衍生物
DK1318997T3 (da) * 2000-09-15 2006-09-25 Vertex Pharma Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer
JP2004524289A (ja) * 2000-12-22 2004-08-12 アストラゼネカ・アクチエボラーグ 治療化合物
JP4286146B2 (ja) * 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−５のヘテロアリール置換ピラゾール系調節剤
JP2003212859A (ja) * 2002-01-24 2003-07-30 Nippon Nohyaku Co Ltd 置換フェニルヘテロ環類及びこれを有効成分とする除草剤
IL163777A0 (en) * 2002-03-08 2005-12-18 Lilly Co Eli Kinase inhibitors
FR2836915B1 (fr) * 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
EP1511738A4 (en) * 2002-05-17 2007-05-09 Scios Inc TREATMENT OF FIBROPROLIFERATIVE DISEASES USING TGF BETA INHIBITORS
AU2003242233A1 (en) * 2002-06-12 2003-12-31 Bf Research Institute, Inc. Probe compound for image diagnosis of disease with amyloid accumulation, compound for staining age spots/diffuse age spots, and remedy for disease with amyloid accumulation
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
US7060698B2 (en) * 2003-05-19 2006-06-13 Hoffmann-La Roche Inc. Benzoxazepinone derivatives
JP2006527197A (ja) * 2003-06-06 2006-11-30 ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア ｐ３８キナーゼ阻害剤組成物及びその使用方法
GB0314943D0 (en) 2003-06-25 2003-07-30 Proteome Sciences Plc Screening methods
US7560464B2 (en) * 2004-04-13 2009-07-14 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
SI1791537T1 (sl) * 2004-08-19 2010-02-26 Aventis Pharma Inc 3-ariltioindol-2-karboksamidni derivati in njihovi analogi kot inhibitorji kazein-kinaze I
WO2007015866A2 (en) * 2005-07-20 2007-02-08 Kalypsys, Inc. Inhibitors of p38 kinase and methods of treating inflammatory disorders
EP1842541A1 (en) * 2006-03-29 2007-10-10 G.I.M.-Gesellschaft Für Innovative Medizin Gmbh Nfg Ohg Plant components and extracts and uses thereof
TW200813035A (en) * 2006-06-19 2008-03-16 Astrazeneca Ab Novel heteroaryl substituted benzoxazoles
WO2007149448A2 (en) * 2006-06-21 2007-12-27 E. I. Du Pont De Nemours And Company Pyrazinones as cellular proliferation inhibitors
US7622495B2 (en) * 2006-10-03 2009-11-24 Neurim Pharmaceuticals (1991) Ltd. Substituted aryl-indole compounds and their kynurenine/kynuramine-like metabolites as therapeutic agents
EP2086959B1 (en) * 2006-11-02 2011-11-16 F. Hoffmann-La Roche AG Substituted 2-imidazoles as modulators of the trace amine associated receptors
WO2008058402A1 (en) * 2006-11-17 2008-05-22 Queen's University At Kingston Compounds and methods for treating protein folding disorders
CA2673368C (en) * 2006-12-19 2014-10-28 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
US8445480B2 (en) * 2007-06-20 2013-05-21 Merck Sharp & Dohme Corp. CETP inhibitors derived from benzoxazole arylamides
FR2918061B1 (fr) * 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
FR2918986B1 (fr) 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
GB0715939D0 (en) * 2007-08-15 2007-09-26 Vastox Plc Method of treatment of duchenne muscular dystrophy
AU2008331854A1 (en) * 2007-11-28 2009-06-11 Yale University Nogo receptor binding small molecules to promote axonal growth
US8642660B2 (en) * 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2149551A1 (de) 2008-07-30 2010-02-03 Bayer Schering Pharma AG N-(Indol-3-ylalkyl)-(hetero)arylamidderivate als Modulatoren des EP2-Rezeptors
FR2934994B1 (fr) * 2008-08-12 2010-09-17 Sanofi Aventis Derives de 2-alkyl-6cycloamino-3-(pyridin-4-yl)imidaz°1,2-b! pyridazine, leur preparation et leur application en therapeutique
KR101257695B1 (ko) * 2008-12-24 2013-04-24 제일모직주식회사 신규한 유기광전소자용 화합물 및 이를 포함하는 유기광전소자
FR2945289A1 (fr) * 2009-05-11 2010-11-12 Sanofi Aventis Derives de 2-cycloamino-5-(pyridin-4-yl)imidazo°2,1-b! °1,3,4!thiadiazole, leur preparation et leur application en therapeutique
EP2528441A4 (en) * 2010-01-25 2013-07-10 Chdi Foundation Inc CYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE THEREOF
JP5937102B2 (ja) * 2010-12-14 2016-06-22 エレクトロフォレティクス リミテッド カゼインキナーゼ１デルタ（ｃｋ１デルタ）阻害剤
EP3081568B1 (en) 2011-05-09 2019-11-13 Eip Pharma, LLC Compositions and methods for treating alzheimer's disease

Also Published As

Publication number Publication date
US9789111B2 (en) 2017-10-17
EP2835131B1 (en) 2017-09-06
US20140018540A1 (en) 2014-01-16
WO2012080727A2 (en) 2012-06-21
HK1190622A1 (zh) 2014-07-11
DK2835131T3 (en) 2017-12-04
EP2651405A2 (en) 2013-10-23
US20140031547A1 (en) 2014-01-30
CN103298460B (zh) 2016-06-01
JP2014503528A (ja) 2014-02-13
CN104906103B (zh) 2018-05-18
US20150209368A1 (en) 2015-07-30
CA2818903C (en) 2021-03-23
AU2017200812A1 (en) 2017-03-02
EP2651404A2 (en) 2013-10-23
US20160058745A1 (en) 2016-03-03
AU2011343039A1 (en) 2013-06-27
WO2012080729A3 (en) 2012-08-02
JP5937102B2 (ja) 2016-06-22
EP2651404B1 (en) 2015-10-14
AU2017200812B2 (en) 2019-01-03
US20160354375A1 (en) 2016-12-08
AU2011343039B2 (en) 2017-03-02
EP2835131A1 (en) 2015-02-11
WO2012080727A4 (en) 2012-10-26
CA2818903A1 (en) 2012-06-21
WO2012080729A2 (en) 2012-06-21
JP6243472B2 (ja) 2017-12-06
CN103298460A (zh) 2013-09-11
CN104906103A (zh) 2015-09-16
WO2012080729A4 (en) 2012-11-08
CN105920010A (zh) 2016-09-07
WO2012080727A3 (en) 2012-08-23
JP2017025080A (ja) 2017-02-02
HK1214527A1 (zh) 2016-07-29
US9763947B2 (en) 2017-09-19
ES2553610T3 (es) 2015-12-10
JP2014503527A (ja) 2014-02-13
JP2016172757A (ja) 2016-09-29

Similar Documents

Publication Publication Date Title
ES2650744T3 (es) Inhibidores de la caseína quinasa 1 delta (CK1delta)
ES2446269T3 (es) 3-Benzofuranil-4-indolil-maleimidas como potentes inhibidores de GSK-3 para trastornos neurodegenerativos
ES2927355T3 (es) Compuestos inhibidores de OGA
ES2711453T3 (es) Un derivado de indolinona como inhibidor de tirosina quinasa
WO2025080653A1 (en) Pyrrolo[2,1-f][1,2,4]triazine compounds acting against cancers, inflammatory diseases, and fibrotic disease via interaction with ras superfamily proteins
JP2012522759A (ja) イミダゾ［２，１−ｂ］［１，３，４］チアジアゾール誘導体
US10961254B2 (en) Pyrimidine compounds and methods using the same
CN113557237A (zh) 吡咯并吡啶衍生物及其预防或治疗蛋白激酶相关疾病的用途
CA3187432A1 (en) Compounds and methods for blocking apoptosis and inducing autophagy
JP2023503926A (ja) Ｔａｓｐａｓｅ１阻害剤およびその使用
HK1190622B (en) Casein kinase 1delta (ck1delta) inhibitors
ES2936077T3 (es) Método para producir un derivado de piridona policíclico sustituido y un cristal del mismo
RU2811975C1 (ru) Конденсированное аза-гетероциклическое амидное соединение и его применение
ES2845230T3 (es) Derivados de pirazol[1,5-a]pirimidina como inhibidores de quinasa JAK
ES2659828B1 (es) Uso de los derivados 4H-pirano[2,3-c] pirazol en el tratamiento de enfermedades neurodegenerativas
BR112019019872B1 (pt) Composto, o isômero óptico do mesmo ou o sal farmaceuticamente aceitável do mesmo, método de preparação do mesmo e composição farmacêutica