AR103574A1 - Compuestos tricíclicos y usos de lo mismos en medicina - Google Patents

Compuestos tricíclicos y usos de lo mismos en medicina

Info

Publication number
AR103574A1
AR103574A1 ARP160100271A ARP160100271A AR103574A1 AR 103574 A1 AR103574 A1 AR 103574A1 AR P160100271 A ARP160100271 A AR P160100271A AR P160100271 A ARP160100271 A AR P160100271A AR 103574 A1 AR103574 A1 AR 103574A1
Authority
AR
Argentina
Prior art keywords
independently
heterocyclyl
aryl
cycloalkyl
alkyl
Prior art date
Application number
ARP160100271A
Other languages
English (en)
Original Assignee
Sunshine Lake Pharma Co 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 Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Publication of AR103574A1 publication Critical patent/AR103574A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/4192—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
    • A61K31/42—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
    • A61K31/422—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
    • A61K31/435—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
    • 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
    • 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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/5025—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
    • A61K31/519—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
    • A61K31/55—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
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P1/04—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
    • 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
    • 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
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • 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
    • A61P7/06—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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)

Abstract

Un método para el tratamiento de enfermedades y/o estados mediados por FXR que comprende administrar el compuesto o la composición farmacéutica. Reivindicación 1: Un compuesto caracterizado porque presenta la fórmula (1) o un estereoisómero, un isómero geométrico, un tautómero, un N-óxido, un hidrato, un solvato, un metabolito, una sal aceptable para uso farmacéutico o un profármaco del mismo, en la que: X es N, CH o ÅN-O&#⁹²⁰;; el anillo D es un anillo heteroaromático de cinco miembros o un heterociclo de cinco miembros; L es un enlace, -(CR³R⁴)ᶠ-, -(CR³R⁴)ᶠ-O-, -(CR³R⁴)ᶠ-NH- o -(CR³R⁴)ᶠ-S(=O)ₜ-; R es un triciclilo fusionado o un heterotriclililo fusionado, en el que R está sustituido opcionalmente con uno, dos, tres, cuatro o cinco R⁸; cada R¹ es de modo independiente H, deuterio, F, Cl, Br, l, hidroxi, amino, nitro, ciano, alquilo, haloalquilo, haloalcoxi, cicloalquilo, heterociclilo, alquenilo, alquinilo, alquilamino, alcoxi, arilo o heteroarilo; R² es H, deuterio, F, Cl, Br, I, hidroxi, amino, nitro, ciano, alquilo, haloalquilo, haloalcoxi, alcoxialquilo, cicloalquilo, hidroxialquilo, heterociclilo, alquilamino o alcoxi; cada uno de R³ y R⁴ es de modo independiente H, deuterio, alquilo C₁₋₄, F, Cₗ, Bʳ, ₗₒ ₕₐₗₒₐₗqᵘⁱₗₒ C₁₋₄; cada R⁸ es de modo independiente H, deuterio, F, Cl, Br, I, hidroxi, nitro, amino, aminoalquilo, alquilamino, alquilo, hidroxialquilo, alcoxi, haloalquilo, haloalcoxi, cicloalquilo, cicloalcoxi, alquenilo, alquinilo, arilo, arilo halo sustituido, arilalquilo, oxo (=O), -L¹-C(=O)OR¹⁵, -L¹-S(=O)ₜR¹⁶, -O-L²-C(=O)OR¹⁵, -O-L²-S(=O)ₜR¹⁶, -C(=O)NR¹⁷R¹⁸, -C(=O)N(R¹⁷)S(=O)₂R¹⁶, -C(=NR¹⁷)NR¹⁷R¹⁸, -C(=O)N(R¹⁷)-L³-S(=O)₂OR¹⁵, -C(=O)N(R¹⁷)C(=O)OR¹⁵, -C(=O)N(R¹⁷)-L³-C(=O)OR¹⁵, ciano, heterociclilo o heteroarilo; o dos R⁸, junto con el mismo átomo C al que están unidos, de modo independiente y opcional forman cicloalquilo o heterociclilo; o dos R⁸, junto con los átomos C adyacentes al que están unidos, de modo independiente y opcional forman cicloalquilo, heterociclilo, arilo o heteroarilo; en la que R⁸ está sustituido de modo independiente y opcional con uno o más R¹⁹; cada R¹⁵ es de modo independiente H, deuterio, alquilo, aminoalquilo, alquenilo, alquinilo, haloalquilo, cicloalquilo, heterociclilo o arilo; cada R¹⁶ es de modo independiente H, deuterio, hidroxi, amino, alquilo, aminoalquilo, alquenilo, alquinilo, haloalquilo, cicloalquilo, heterociclilo, arilo o -NR¹⁷R¹⁸; cada uno de R¹⁷ y R¹⁸ es de modo independiente H, deuterio, alquilo, aminoalquilo, alquenilo, alquinilo, haloalquilo, cicloalquilo, heterociclilo o arilo; o R¹⁷ y R¹⁸, junto con el átomo N al que están unidos, de modo independiente, y opcional forman heterociclilo o heteroarilo; cada L¹ es de modo independiente un enlace, -C(=O)-, alquileno C₁₋₆, alquenileno C₂₋₆ o alquinileno C₂₋₆; cada L² es de modo independiente alquileno C₁₋₆, alquenileno C₂₋₆ o alquinileno C₂₋₆; cada L³ es de modo independiente un enlace o alquileno C₁₋₄; n es 0, 1, 2, 3 ó 4; cada f es de modo independiente 0, 1 ó 2; cada t es de modo independiente 0, 1, ó 2; donde cada uno de dicho hidroxi, amino, alquilo, hidroxialquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, haloalquilo, alquilamino, alcoxi, alcoxialquilo, cicloalquiloxi, haloalcoxi, heterociclilo, arilo, heteroarilo, arilo halosustituido, arilalquilo, haloalquilo C₁₋₄, alquileno C₁₋₆, alquenileno C₂₋₆, alquinileno C₂₋₆ y alquileno C₁₋₄ de R¹, R², R³, R⁴, R⁸, R¹⁵, R¹⁶, R¹⁷, R¹⁸, L¹, L² y L³ está sustituido de modo independiente y opcional con uno o más R⁹; y cada uno de R⁹ y R¹⁹ es de modo independiente H, deuterio, F, Cl, Br, l, ciano, oxo (=O), hidroxi, alquilo, alquilamino, amino, arilo, heterociclilo, heteroarilo, alquenilo, alquinilo, cicloalquilo, alcoxi o haloalquilo.
ARP160100271A 2015-02-13 2016-01-29 Compuestos tricíclicos y usos de lo mismos en medicina AR103574A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201510083621 2015-02-13

Publications (1)

Publication Number Publication Date
AR103574A1 true AR103574A1 (es) 2017-05-17

Family

ID=56614145

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160100271A AR103574A1 (es) 2015-02-13 2016-01-29 Compuestos tricíclicos y usos de lo mismos en medicina

Country Status (17)

Country Link
US (1) US10183917B2 (es)
EP (1) EP3256468B1 (es)
JP (1) JP6661070B2 (es)
KR (1) KR102577823B1 (es)
CN (1) CN105884758B (es)
AR (1) AR103574A1 (es)
AU (1) AU2016218701B2 (es)
BR (1) BR112017017078B1 (es)
CA (1) CA2976294C (es)
DK (1) DK3256468T3 (es)
ES (1) ES2791401T3 (es)
HK (1) HK1244279A1 (es)
HU (1) HUE050173T2 (es)
MX (1) MX2017010477A (es)
RU (1) RU2724100C9 (es)
TW (1) TWI698430B (es)
WO (1) WO2016127924A1 (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
DK3277286T3 (da) 2015-03-31 2021-07-05 Enanta Pharm Inc Galdesydererivater som fxr/tgr5-agonister og anvendelsesmetoder deraf
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017201150A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
US10138228B2 (en) 2016-05-18 2018-11-27 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use therof
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
EP3730487B1 (en) 2016-06-13 2022-04-27 Gilead Sciences, Inc. Azetidine derivatives as fxr (nr1h4) modulators
TW201808283A (zh) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
CN110177783B (zh) * 2016-08-23 2023-06-06 阿德利克斯股份有限公司 用于治疗代谢病状和病症的激素受体调节剂
US11091482B2 (en) 2016-08-23 2021-08-17 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators
WO2018067704A1 (en) 2016-10-04 2018-04-12 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
US10654797B2 (en) 2016-11-03 2020-05-19 North & South Brother Pharmacy Investment Company Limited Solid forms of an adamantyl compound, compositions and uses thereof
CN106631991B (zh) * 2016-12-16 2021-04-16 常州南京大学高新技术研究院 一种n-丁基-2,2,6,6-四甲基-4-哌啶胺的简便合成方法
CN108329330B (zh) * 2017-01-20 2021-05-04 复旦大学 2-苄氧苯基噁唑并吡啶类化合物及其药物用途
EP4122464B1 (en) 2017-03-28 2024-05-15 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
CA3066217A1 (en) * 2017-06-05 2018-12-13 National University Of Singapore Compounds useful in inhibiting human trefoil factor 3
UY37847A (es) 2017-08-15 2019-03-29 Inflazome Ltd Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3
UY37848A (es) 2017-08-15 2019-03-29 Inflazome Ltd Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3
US11926600B2 (en) 2017-08-15 2024-03-12 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
JP7271513B2 (ja) 2017-09-14 2023-05-11 アルデリックス， インコーポレイテッド 代謝関連の突然変異誘発性及び線維性の症状及び障害を治療するためのホルモン受容体調節薬
WO2019118571A1 (en) 2017-12-12 2019-06-20 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
CN110128432B (zh) * 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
EP3759077A1 (en) 2018-03-02 2021-01-06 Inflazome Limited Novel compounds
EP4360632A2 (en) 2019-01-15 2024-05-01 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
AU2020225225B2 (en) 2019-02-19 2022-12-22 Gilead Sciences, Inc. Solid forms of FXR agonists
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
CN110028443B (zh) * 2019-05-29 2022-03-04 济南周行医药科技有限公司 一种调节fxr活性的三环化合物类药物中间体的制备方法
CA3142904A1 (en) 2019-07-23 2021-01-28 Novartis Ag Treatment comprising fxr agonists
KR20220038368A (ko) 2019-07-23 2022-03-28 노파르티스 아게 Fxr 작용제를 이용하는 간 질환의 병용 치료
CN112300120B (zh) * 2019-07-31 2023-04-14 北京四环制药有限公司 一种用于制备巴罗萨韦或其衍生物的化合物及其制备方法和其应用
JOP20220057A1 (ar) 2019-09-03 2023-01-30 Novartis Ag علاج أمراض أو اضطرابات الكبد تشتمل على مضادات مستقبل actrii
CN114401745A (zh) 2019-09-19 2022-04-26 诺华股份有限公司 包含fxr激动剂的治疗
US20220331341A1 (en) 2019-09-30 2022-10-20 Novartis Ag Treatment comprising the use of fxr agonists
EP4061364A4 (en) * 2019-11-20 2023-09-13 Vivace Therapeutics, Inc. HETEROARYL COMPOUNDS
JP2023504427A (ja) * 2019-11-29 2023-02-03 ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 三環式含窒素化合物の非晶質及びその用途
CN112876492B (zh) * 2019-11-29 2023-07-18 广东东阳光药业有限公司 含氮三环化合物的晶型及其用途
CN112876490A (zh) * 2019-11-29 2021-06-01 广东东阳光药业有限公司 含氮三环化合物的晶型及其用途
CA3164941A1 (en) 2019-12-20 2021-06-24 Novartis Ag Combination treatment of liver diseases using integrin inhibitors
WO2022101853A1 (en) 2020-11-16 2022-05-19 Novartis Ag Method of determining liver fibrosis
CN114235976B (zh) * 2021-11-09 2023-11-03 暨南大学 一种含氮杂环有机化合物中间产物的合成和分析方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR002459A1 (es) * 1995-01-17 1998-03-25 American Cyanamid Co Antagonistas de vasopresina de benzacepina triciclicos, una composicion farmaceutica que los contiene, un metodo para tratar enfermedades y unprocedimiento para su preparacion.
EP1140079B1 (en) 1998-12-23 2009-06-03 Glaxo Group Limited Assays for ligands for nuclear receptors
CZ20014261A3 (cs) 1999-06-03 2002-06-12 Nippon Suisan Kaisha, Ltd. Tricyklické fúzované heterocyklické sloučeniny, způsob jejich přípravy a pouľití
ATE381542T1 (de) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
CN1681388A (zh) * 2002-09-18 2005-10-12 Fmc有限公司 三环衍生物杀虫剂
WO2004048349A1 (en) 2002-11-22 2004-06-10 Smithkline Beecham Corporation Farnesoid x receptor agonists
BRPI0412262A (pt) * 2003-07-23 2006-09-19 X Ceptor Therapeutics Inc derivados de azepina como agentes farmacêuticos
ATE526318T1 (de) 2005-12-19 2011-10-15 Glaxosmithkline Llc Farnesoid-x-rezeptor-agonisten
JP5301286B2 (ja) 2006-02-03 2013-09-25 イーライ リリー アンド カンパニー Ｆｘ受容体を調節するための化合物及び方法
WO2007144785A2 (en) * 2006-03-26 2007-12-21 Uti Limited Partnership Ryanodine receptor inhibitors and methods relating thereto
ATE460403T1 (de) 2006-05-24 2010-03-15 Lilly Co Eli Verbindungen und verfahren zur modulierung von fx-rezeptoren
ATE465996T1 (de) 2006-05-24 2010-05-15 Lilly Co Eli Fxr-agonisten
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
CL2007003035A1 (es) 2006-10-24 2008-05-16 Smithkline Beechman Corp Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
EP2121621B1 (en) * 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
US20100249179A1 (en) 2007-06-13 2010-09-30 Smithkline Beecham Corporation Farnesoid X Receptor Agonists
EP2173174A4 (en) 2007-07-02 2010-08-04 Glaxosmithkline Llc FARNESOID X RECEPTOR AGONISTS
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
WO2010011375A2 (en) 2008-04-21 2010-01-28 Merck & Co., Inc. Inhibitors of janus kinases
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
JP2012503654A (ja) 2008-09-26 2012-02-09 ワイス・エルエルシー １，２，３，６−テトラヒドロアゼピノ［４，５−ｂ］インドール−５−カルボキシレート核内受容体阻害剤
CA2740366A1 (en) 2008-10-21 2010-04-29 Metabolex, Inc. Aryl gpr120 receptor agonists and uses thereof
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
PT3124481T (pt) 2010-02-16 2018-06-18 Aragon Pharmaceuticals Inc Moduladores do receptor de androgénios e suas utilizações
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
US20140039007A1 (en) 2010-12-20 2014-02-06 David C. Tully Compositions and methods for modulating farnesoid x receptors
US20130261108A1 (en) 2010-12-20 2013-10-03 Irm Llc Compositions and methods for modulating farnesoid x receptors
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
EA031003B1 (ru) 2013-09-11 2018-10-31 Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль) Способы и фармацевтические композиции для лечения вызванных вирусом гепатита в инфекций
CN104513213A (zh) 2013-09-28 2015-04-15 山东亨利医药科技有限责任公司 Fxr激动剂
TR201807321T4 (tr) 2013-11-05 2018-06-21 Novartis Ag Farnesoid x reseptörlerinin modüle edilmesi için bileşimler ve yöntemler.
KR20160132111A (ko) 2014-03-13 2016-11-16 더 솔크 인스티튜트 포 바이올로지칼 스터디즈 Fxr 작용제와 제조방법 및 용도
CN104045635A (zh) 2014-06-23 2014-09-17 华东理工大学 3,4,5-三取代异恶唑类化合物及其用途
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
BR112017013568A2 (pt) 2014-12-22 2018-03-06 Akarna Therapeutics Ltd compostos bicíclicos fundidos para o tratamento de doenças

Also Published As

Publication number Publication date
CA2976294A1 (en) 2016-08-18
BR112017017078A2 (pt) 2018-04-10
HK1244279A1 (zh) 2018-08-03
CN105884758B (zh) 2019-12-10
AU2016218701B2 (en) 2019-08-08
US10183917B2 (en) 2019-01-22
RU2724100C2 (ru) 2020-06-22
KR20170117489A (ko) 2017-10-23
CN105884758A (zh) 2016-08-24
CA2976294C (en) 2024-01-16
AU2016218701A1 (en) 2017-07-20
MX2017010477A (es) 2018-05-01
RU2017131875A (ru) 2019-03-14
WO2016127924A1 (en) 2016-08-18
TWI698430B (zh) 2020-07-11
ES2791401T3 (es) 2020-11-04
RU2724100C9 (ru) 2020-11-03
EP3256468B1 (en) 2020-04-08
TW201629022A (zh) 2016-08-16
US20180030003A1 (en) 2018-02-01
JP6661070B2 (ja) 2020-03-11
KR102577823B1 (ko) 2023-09-13
DK3256468T3 (da) 2020-05-11
JP2018505203A (ja) 2018-02-22
EP3256468A4 (en) 2018-07-25
HUE050173T2 (hu) 2020-11-30
BR112017017078B1 (pt) 2023-04-04
RU2017131875A3 (es) 2019-08-07
EP3256468A1 (en) 2017-12-20

Similar Documents

Publication Publication Date Title
AR103574A1 (es) Compuestos tricíclicos y usos de lo mismos en medicina
AR109295A1 (es) Compuestos tricíclicos que contienen nitrógeno y usos de los mismos en medicina
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR105845A1 (es) Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4
AR110139A1 (es) COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV
NI201600170A (es) Pirazolopiridinas y pirazolopirimidinas
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR103252A1 (es) Compuestos de quinazolina
AR103828A1 (es) INHIBIDORES DEL FACTOR TRANSFORMADOR DEL CRECIMIENTO b
AR100691A1 (es) Esteroides neuroactivos, composiciones, y usos de los mismos
AR087348A1 (es) Indazoles, composiciones farmaceuticas que comprenden tales compuestos y su uso como medicamentos
AR100886A1 (es) 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas
AR049300A1 (es) Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos
AR095198A1 (es) Derivados de triazolona de piridinilo y piridinilo fusionado
AR090994A1 (es) Uracilos sustituidos biciclicamente y uso de los mismos
AR091261A1 (es) Derivados de alcoholes 1-fenil-2-piridinilalquilicos como inhibidores de la fosfodiesterasa
BR112016019462B8 (pt) Compostos heterocïclicos tricïclicos como inibidores de fosfoinosotida 3-cinase
AR099937A1 (es) Compuestos de isoindolinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados
AR095359A1 (es) Compuestos heteroaromáticos y su uso como ligandos d1 de dopamina
AR092809A1 (es) 3,5-diaminopirazol como inhibidor de quinasa
AR097755A1 (es) Derivados sustituidos de fenilalanina como moduladores del factor xia
AR097403A1 (es) Derivados de benzamida como antagonistas de lpar1 y/o lpar5 y un proceso para su preparación
AR092288A1 (es) Ligandos del receptor ep1
AR097756A1 (es) Derivados de fenilalanina sustituidos
AR116424A1 (es) Moduladores de la somatostatina y usos de los mismos