AU2017212577B2 - Benzimidazole derivatives as modulators of ROR-gamma - Google Patents

Benzimidazole derivatives as modulators of ROR-gamma Download PDF

Info

Publication number
AU2017212577B2
AU2017212577B2 AU2017212577A AU2017212577A AU2017212577B2 AU 2017212577 B2 AU2017212577 B2 AU 2017212577B2 AU 2017212577 A AU2017212577 A AU 2017212577A AU 2017212577 A AU2017212577 A AU 2017212577A AU 2017212577 B2 AU2017212577 B2 AU 2017212577B2
Authority
AU
Australia
Prior art keywords
methyl
benzo
imidazole
dioxol
difluorobenzo
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.)
Ceased
Application number
AU2017212577A
Other languages
English (en)
Other versions
AU2017212577A1 (en
Inventor
David A. Claremon
Lawrence Wayne Dillard
Yi Fan
Stephen D. Lotesta
Suresh B. Singh
Colin M. Tice
Wei Zhao
Linghang Zhuang
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.)
Vitae Pharmaceuticals LLC
Original Assignee
Vitae Pharmaceuticals LLC
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 Vitae Pharmaceuticals LLC filed Critical Vitae Pharmaceuticals LLC
Publication of AU2017212577A1 publication Critical patent/AU2017212577A1/en
Assigned to VITAE PHARMACEUTICALS, LLC reassignment VITAE PHARMACEUTICALS, LLC Alteration of Name(s) of Applicant(s) under S113 Assignors: VITAE PHARMACEUTICALS, INC.
Application granted granted Critical
Publication of AU2017212577B2 publication Critical patent/AU2017212577B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • 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
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/435—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
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a 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
    • A61K31/44—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—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
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/06—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 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
    • C07D405/10—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 carbon chain containing aromatic rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
AU2017212577A 2016-01-29 2017-01-27 Benzimidazole derivatives as modulators of ROR-gamma Ceased AU2017212577B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662288487P 2016-01-29 2016-01-29
US62/288,487 2016-01-29
US201662320893P 2016-04-11 2016-04-11
US62/320,893 2016-04-11
PCT/US2017/015220 WO2017132432A1 (en) 2016-01-29 2017-01-27 Benzimidazole derivatives as modulators of ror-gamma

Publications (2)

Publication Number Publication Date
AU2017212577A1 AU2017212577A1 (en) 2018-08-02
AU2017212577B2 true AU2017212577B2 (en) 2021-05-13

Family

ID=57966225

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017212577A Ceased AU2017212577B2 (en) 2016-01-29 2017-01-27 Benzimidazole derivatives as modulators of ROR-gamma

Country Status (15)

Country Link
US (2) US10829481B2 (enExample)
EP (2) EP3408268B8 (enExample)
JP (2) JP6948333B2 (enExample)
KR (1) KR20180100697A (enExample)
CN (2) CN114230523A (enExample)
AU (1) AU2017212577B2 (enExample)
BR (1) BR112018015273A2 (enExample)
CA (1) CA3011838A1 (enExample)
MA (2) MA55328A (enExample)
MX (1) MX381313B (enExample)
RU (2) RU2021133444A (enExample)
SA (1) SA518392101B1 (enExample)
TW (2) TWI757266B (enExample)
UY (1) UY37098A (enExample)
WO (1) WO2017132432A1 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
KR102702236B1 (ko) 2015-05-15 2024-09-04 오리진 온콜로지 리미티드 Ror 감마 조절제로서의 치환된 테트라하이드로퀴놀리논 화합물
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ROR-γ調節劑
CN115716826A (zh) 2017-07-24 2023-02-28 生命医药有限责任公司 RORγ的抑制剂
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN109593068B (zh) * 2017-09-30 2022-12-27 广东东阳光药业有限公司 一种RORγ抑制剂的中间体及其制备方法
SMT202300212T1 (it) * 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi
CN110483437B (zh) * 2018-05-14 2022-12-06 嘉兴维眸生物科技有限公司 一种含五元环的化合物及其制备和应用
CN112601745B (zh) * 2018-10-24 2023-06-27 上海和誉生物医药科技有限公司 一种氮杂芳基酰胺衍生物及其制备方法和应用
CN121081472A (zh) 2018-12-13 2025-12-09 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
CA3154488A1 (en) 2019-08-23 2021-03-04 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
CA3154391A1 (en) 2019-09-12 2021-03-18 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
BR112022008293A2 (pt) * 2019-10-31 2022-07-26 Jiangsu Hengrui Medicine Co Sal de adição de ácido de regulador de ror?, composições farmacêuticas, uso dos mesmos e métodos para preparar forma cristalina e composição farmacêutica
CN112745268B (zh) * 2019-10-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并咪唑衍生物的晶型及制备方法
TW202136237A (zh) 2020-01-06 2021-10-01 大陸商廣東東陽光藥業有限公司 RORγt抑制劑及其製備方法和用途
CN111333552B (zh) * 2020-04-09 2021-07-20 广州安岩仁医药科技有限公司 β-苯并氨基酸类化合物的合成方法
CN111606868B (zh) * 2020-06-23 2023-02-17 温州大学新材料与产业技术研究院 一种双齿噁唑啉手性配体的制备方法
CN113912563B (zh) * 2020-07-10 2025-05-27 中国科学院广州生物医药与健康研究院 一种苯并五元氮杂环化合物及其应用
JP2024510935A (ja) * 2021-03-03 2024-03-12 ターンズ・ファーマシューティカルズ・インコーポレイテッド 甲状腺ホルモン受容体ベータアゴニスト化合物
EP4412660A1 (en) * 2021-10-04 2024-08-14 Bolt Biotherapeutics, Inc. Asymmetric bis-benzimidazole sting agonist immunoconjugates and uses thereof
PE20252787A1 (es) 2023-04-07 2025-12-22 Terns Pharmaceuticals Inc Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009083526A1 (en) * 2008-01-02 2009-07-09 Smithkline Beecham Corporation Novel compounds
WO2013019682A1 (en) * 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013078233A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-benzylbenzimidazole modulators of pparg
WO2013078240A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-biphenylmethylbenzimidazole modulators of pparg

Family Cites Families (253)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3751524T2 (de) 1986-07-28 1996-06-13 American Cyanamid Co 5(und/oder6) Substituierte 2-(2-Imidazolin-2-yl)nicotinsäuren, Ester und Salze, verwendbar als herbizide Mittel und Zwischenverbindungen für die Herstellung dieser Nikotinsäuren, Ester und Salze.
FR2624698A1 (fr) 1987-12-18 1989-06-23 Bernard Lyon I Universite Clau Derives heterocycliques de n-carbamoyl-, n-thiocarbamoyl- ou n-amidino-aminomalonyl ou aminosuccinyl amides utiles comme agents edulcorants
AU5175490A (en) 1989-02-27 1990-09-26 Du Pont Merck Pharmaceutical Company, The Novel sulfonamides as radiosensitizers
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
GB8927872D0 (en) 1989-12-08 1990-02-14 Beecham Group Plc Pharmaceuticals
JP2807577B2 (ja) 1990-06-15 1998-10-08 エーザイ株式会社 環状アミド誘導体
EP0520573A1 (en) 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide derivatives
DE4121214A1 (de) 1991-06-27 1993-01-14 Bayer Ag 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
US5416099A (en) 1991-10-29 1995-05-16 Merck & Co., Inc. Fibrinogen receptor antagonists
US5389631A (en) 1991-10-29 1995-02-14 Merck & Co., Inc. Fibrinogen receptor antagonists
US5238950A (en) 1991-12-17 1993-08-24 Schering Corporation Inhibitors of platelet-derived growth factor
US5364869A (en) 1992-03-09 1994-11-15 Abbott Laboratories Heterocycle-substituted benzyaminopyridine angiotensin II receptor antagonists
US5326760A (en) 1992-06-29 1994-07-05 Glaxo, Inc. Aminobutanoic acid compounds having metalloprotease inhibiting properties
JPH06236056A (ja) 1993-02-10 1994-08-23 Fuji Xerox Co Ltd 電子写真感光体
JP3760474B2 (ja) 1993-04-22 2006-03-29 ダイキン工業株式会社 電気エネルギーを発生させる方法、装置およびそれに用いるn−f結合を有する化合物
CA2134192A1 (en) 1993-11-12 1995-05-13 Michael L. Denney 5, 6-bicyclic glycoprotein iib/iiia antagonists
DE4343922A1 (de) 1993-12-22 1995-06-29 Basf Ag Pyridin-2,3-dicarbonsäureimide, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung unerwünschten Pflanzenwuchses
KR970007419B1 (ko) 1993-12-30 1997-05-08 한솔제지 주식회사 승화형 열전사 기록용 색소
FR2725946A1 (fr) 1994-10-24 1996-04-26 Lohr Ind Cale a rapporter sur un plan porteur presentant des perforations
US5719144A (en) 1995-02-22 1998-02-17 Merck & Co., Inc. Fibrinogen receptor antagonists
EP0733632B1 (en) 1995-03-24 2003-06-04 Takeda Chemical Industries, Ltd. Cyclic compounds, their production and use as tachykinin receptor antagonists
US5770590A (en) 1995-03-24 1998-06-23 Takeda Chemical Industries, Ltd. Cyclic compounds, their prudiction and use
EP0882718B1 (en) * 1995-12-28 2005-08-31 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
DE19608791A1 (de) 1996-03-07 1997-09-11 Hoechst Ag Verfahren zur Herstellung von fluorierten Aromaten und fluorierten stickstoffhaltigen Heteroaromaten
DE19702282C2 (de) 1997-01-23 1998-11-19 Hoechst Ag Katalysator für Halex-Reaktionen
US6177443B1 (en) 1997-03-07 2001-01-23 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
EP0973778A1 (en) 1997-03-07 2000-01-26 Novo Nordisk A/S 4,5,6,7-TETRAHYDRO-THIENO 3,2-c]PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE
KR19980074060A (ko) 1997-03-21 1998-11-05 김윤배 신규한 치환된 3,4-디알콕시페닐 유도체
JPH1143489A (ja) 1997-05-30 1999-02-16 Takeda Chem Ind Ltd ヘテロ環化合物、その製造法および剤
US20020132817A1 (en) 1998-03-19 2002-09-19 Hideaki Natsugari Heterocyclic compounds, their production and use
IL136950A0 (en) 1998-03-19 2001-06-14 Takeda Chemical Industries Ltd Heterocyclic compounds, their production and use
FR2778662B1 (fr) 1998-05-12 2000-06-16 Adir Nouveaux composes cycliques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP2000007661A (ja) 1998-06-23 2000-01-11 Nippon Nohyaku Co Ltd 複素環ジカルボン酸ジアミド誘導体及びその中間体並びに除草剤
EP1101758A4 (en) 1998-07-28 2002-04-03 Nihon Nohyaku Co Ltd CONDENSED HETEROCYCLIC DICARBONIC ACID DIAMOND DERIVATIVES OR SALTS THEREOF, HERBICIDES AND THEIR USE
US6348032B1 (en) * 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
EP1145714A4 (en) 1998-11-27 2004-12-15 Takeda Chemical Industries Ltd DRUGS
US6417207B1 (en) 1999-05-12 2002-07-09 Nitromed, Inc. Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
HK1047582B (zh) * 1999-06-23 2005-03-04 萨诺费-阿文蒂斯德国有限公司 取代的苯並咪唑
JP2003505388A (ja) 1999-07-21 2003-02-12 アストラゼネカ・アクチエボラーグ 新規化合物
PT1206436E (pt) 1999-08-02 2004-12-31 Hoffmann La Roche Retinoides para o tratamento de enfisema
EP2003134B1 (en) 1999-11-09 2011-03-02 Abbott Laboratories Hydromorphinone compositions
CZ20013424A3 (cs) 1999-12-27 2002-02-13 Japan Tobacco Inc. Sloučeniny s fúzovanými kruhy a jejich pouľití jako léčiva
US6770666B2 (en) 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
US6350755B1 (en) 2000-01-12 2002-02-26 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2001083445A1 (en) 2000-04-25 2001-11-08 Samsung Electronics Co., Ltd. Biphenyl butyric acid derivative as a matrix metalloproteinase inhibitor
CA2354606C (en) 2000-08-03 2005-12-06 Pfizer Products Inc. Azabicycloalkane derivatives and therapeutic uses thereof
US6884782B2 (en) 2000-11-08 2005-04-26 Amgen Inc. STAT modulators
TWI236474B (en) 2001-04-03 2005-07-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
WO2002081447A1 (en) 2001-04-06 2002-10-17 Daewoong Pharmaceutical Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isothiazolinone derivatives and the use thereof
WO2002081443A1 (en) 2001-04-09 2002-10-17 Chiron Corporation Novel guanidino compounds
RU2270192C2 (ru) 2001-04-19 2006-02-20 Эйсай Ко., Лтд. Производные 2-иминопирролидина
SI1397364T1 (sl) 2001-05-24 2007-12-31 Lilly Co Eli Novi pirolni derivati kot farmacevtske uäśinkovine
MXPA04000449A (es) 2001-07-16 2004-03-18 Shionogi & Co Procedimiento para preparacion de derivados de amidina.
JP2003171380A (ja) 2001-09-28 2003-06-20 Takeda Chem Ind Ltd 三環性化合物の製造法
WO2003029254A1 (en) 2001-09-28 2003-04-10 Takeda Chemical Industries, Ltd. Process for preparation of tricyclic compounds
CZ2004408A3 (cs) 2001-10-02 2005-03-16 Pharmacia & Upjohn Company Azabicyklicky substituované kondenzované heteroarylsloučeniny
DE10156719A1 (de) 2001-11-19 2003-05-28 Bayer Ag Heteroarylcarbonsäureamide
TWI263640B (en) 2001-12-19 2006-10-11 Bristol Myers Squibb Co Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
PL372295A1 (en) 2002-02-04 2005-07-11 F.Hoffmann-La Roche Ag Quinoline derivatives as npy antagonists
DE10207037A1 (de) 2002-02-20 2003-08-28 Bayer Cropscience Gmbh 2-Amino-4-bicyclyamino-6H-1,3.5-triazine, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren
US7189851B2 (en) 2002-03-06 2007-03-13 Smithkline Beecham Corporation Condensed heterocyclic compounds as calcitonin agonists
WO2003104216A1 (en) 2002-06-10 2003-12-18 Acadia Pharmaceuticals Inc. Urotensin ii receptor modulators
WO2004014365A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
WO2004026871A1 (en) 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
US8604183B2 (en) 2002-11-05 2013-12-10 Isis Pharmaceuticals, Inc. Compositions comprising alternating 2′-modified nucleosides for use in gene modulation
JP2004203791A (ja) 2002-12-25 2004-07-22 Dai Ichi Seiyaku Co Ltd 芳香族化合物
CN1212674C (zh) 2003-01-08 2005-07-27 东南大学 横向缓冲p型金属氧化物半导体管
TW200503994A (en) 2003-01-24 2005-02-01 Novartis Ag Organic compounds
GB0308025D0 (en) 2003-04-07 2003-05-14 Glaxo Group Ltd Compounds
CN102174042B (zh) 2003-05-19 2013-09-18 Irm有限责任公司 免疫抑制剂化合物和组合物
AU2004240649A1 (en) 2003-05-19 2004-12-02 Irm, Llc Immunosuppressant compounds and compositions
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
EP1628967B1 (en) 2003-05-19 2014-04-09 Irm Llc Immunosuppressant compounds and compositions
US20050004133A1 (en) 2003-06-05 2005-01-06 Makings Lewis R. Modulators of VR1 receptor
CN1566099A (zh) 2003-06-13 2005-01-19 中国科学院上海药物研究所 异喹啉-1,3,4-三酮类化合物、制备方法及其用途
EP1660454A1 (en) 2003-07-07 2006-05-31 Vernalis (R&D) Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
FR2857966A1 (fr) 2003-07-24 2005-01-28 Aventis Pharma Sa Produits aryl-heteroaromatiques, compositions les contenant et utilisation
EP1654260A4 (en) 2003-08-01 2008-09-24 Pfizer Prod Inc 6-LOW HETEROARYL COMPOUNDS FOR THE TREATMENT OF NEURODEEGENERATIVE DISEASES
AU2004274403A1 (en) 2003-09-03 2005-03-31 Aventis Pharmaceuticals Inc. 5-aryl-Pyrazolo(4,3-d)pyrimidines, pyridines, and pyrazines and related compounds
EA200600372A1 (ru) 2003-09-05 2006-08-25 Ньюроджин Корпорейшн Конденсированные с гетероарилом пиридины, пиразины и пиримидины в качестве лигандов рецептора кортикотропин-рилизинг-фактора (crf 1)
US20070088163A1 (en) 2003-09-12 2007-04-19 Kemia, Inc. Modulators of calcitonin and amylin activity
WO2005039564A1 (en) 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
KR101190912B1 (ko) 2003-11-19 2012-10-12 어레이 바이오파마 인크. Mek의 헤테로시클릭 억제제 및 그의 사용 방법
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
WO2005060958A1 (en) 2003-12-19 2005-07-07 Kalypsys, Inc. (5- (2-phenyl)-thiazol-5-ylmethoxy)-indol-1-yl) -acetic acid derivatives and related compounds as modulators of the human ppar-delta receptor for the treatment of metabolic disorders such as type 2 diabetes
EP1699488A2 (en) 2003-12-23 2006-09-13 Pfizer Products Incorporated Therapeutic combination for cognition enhancement and psychotic disorders
WO2005097129A2 (en) 2004-04-05 2005-10-20 Takeda Pharmaceutical Company Limited 6-azaindole compound
WO2005100334A1 (en) 2004-04-14 2005-10-27 Pfizer Products Inc. Dipeptidyl peptidase-iv inhibitors
GB0412467D0 (en) 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
MX2007003375A (es) 2004-09-22 2007-05-07 Janssen Pharmaceutica Nv Inhibidores de la interaccion entre mdm2 y p53.
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
WO2006065842A2 (en) 2004-12-13 2006-06-22 Synta Pharmaceuticals Corp. 5,6,7,8-tetrahydroquinolines and related compounds and uses thereof
RU2007130077A (ru) 2005-01-07 2009-02-20 Эмори Юниверсити (Us) Антагонисты cxcr4 и их применение для лечения вич-инфекции
WO2006082001A1 (en) 2005-02-07 2006-08-10 F.Hoffmann-La Roche Ag Heterocyclic substituted phenyl methanones as inhibitors of the glycine transporter 1
GB0504556D0 (en) 2005-03-04 2005-04-13 Pfizer Ltd Novel pharmaceuticals
DE102005012872A1 (de) * 2005-03-19 2006-09-28 Sanofi-Aventis Deutschland Gmbh Substituierte, bizyklische 8-Pyrrolidino-benzimidazole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CN101193862B (zh) 2005-04-13 2013-08-21 阿斯特克斯治疗有限公司 羟基苯甲酰胺衍生物和其作为hsp90抑制剂的用途
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
WO2007007054A1 (en) 2005-07-08 2007-01-18 Cancer Research Technology Limited Phthalamides, succinimides and related compounds and their use as pharmaceuticals
EP1940819A1 (en) 2005-08-16 2008-07-09 Memory Pharmaceuticals Corporation Phosphodiesterase 10 inhibitors
US20090131431A1 (en) 2005-09-29 2009-05-21 Christopher David Edlin Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors
RU2428423C2 (ru) 2005-11-10 2011-09-10 Баниу Фармасьютикал Ко., Лтд. Азазамещенные спиропроизводные
PE20071241A1 (es) 2006-01-17 2008-01-14 Schering Corp Compuestos derivados de hidantoina para el tratamiento de trastornos inflamatorios
US20080108611A1 (en) 2006-01-19 2008-05-08 Battista Kathleen A Substituted thienopyrimidine kinase inhibitors
JP5111398B2 (ja) 2006-01-25 2013-01-09 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療又は予防のためのジペプチジルペプチダーゼiv阻害剤としてのアミノシクロヘキサン類
JP5161795B2 (ja) 2006-02-15 2013-03-13 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療又は予防のためのジペプチジルペプチダーゼivインヒビターとしてのアミノテトラヒドロピラン
WO2007101225A2 (en) 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Methods to identify inhibitors of the unfolded protein response
US7977351B2 (en) 2006-03-22 2011-07-12 Allergan, Inc. Heteroaryl dihydroindolones as kinase inhibitors
AU2007228784B2 (en) 2006-03-22 2012-03-08 Janssen Pharmaceutica N.V. Cyclic-alkylaminederivatives as inhibitors of the interaction between MDM2 and p53
EP2023919A4 (en) 2006-05-08 2010-12-22 Molecular Neuroimaging Llc COMPOUNDS AND AMYLOID PROBES FOR THERAPY AND IMAGING USES
PL2051975T3 (pl) 2006-05-16 2013-01-31 Boehringer Ingelheim Int Podstawione prolinamidy, ich wytwarzanie oraz ich zastosowanie jako środków leczniczych
CN1869036A (zh) 2006-06-30 2006-11-29 中国药科大学 7-取代-3-氯吡咯并[3,4-b]吡啶化合物
DE102006032824A1 (de) 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
WO2008010964A1 (en) 2006-07-17 2008-01-24 Merck & Co., Inc. 1-hydroxy naphthyridine compounds as anti-hiv agents
WO2008013963A2 (en) 2006-07-28 2008-01-31 University Of Connecticut Fatty acid amide hydrolase inhibitors
US8389739B1 (en) 2006-10-05 2013-03-05 Orphagen Pharmaceuticals Modulators of retinoid-related orphan receptor gamma
JP5518478B2 (ja) 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
JP5721949B2 (ja) 2006-10-12 2015-05-20 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited 複合薬剤
JP5410285B2 (ja) 2006-10-12 2014-02-05 アステックス、セラピューティックス、リミテッド 医薬化合物
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
PE20080888A1 (es) 2006-10-18 2008-08-26 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE LA ACIL-TRANSFERASA DE ACIL-CoA-DIACIL-GLICEROL 1 (DGAT1)
JP2010512410A (ja) 2006-12-11 2010-04-22 ノバルティス アーゲー 心筋虚血を予防または処置するための方法
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
US20100323953A1 (en) 2007-01-08 2010-12-23 Phenomix Corporation Macrocyclic hepatitis c protease inhibitors
WO2009004496A2 (en) 2007-04-13 2009-01-08 University Of Manitoba Bisanthrapyrazoles as anti-cancer agents
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
US20100129933A1 (en) 2007-04-26 2010-05-27 Forschungszentrum Karlsruhe Gmbh Method for detecting the binding between mdm2 and the proteasome
AR066379A1 (es) 2007-05-02 2009-08-12 Boehringer Ingelheim Int Amidas de acido carboxilico su preparacion y su uso como medicamentos
WO2008135524A2 (en) 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted anthranilamides and analogues, manufacturing and use thereof as medicaments
MX2009012183A (es) 2007-05-10 2010-04-27 Constar Int Inc Moleculas depuradoras del oxigeno, articulos que contienen las mismas y sus metodos de uso.
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
GB0710844D0 (en) 2007-06-06 2007-07-18 Lectus Therapeutics Ltd Potassium ion channel modulators & uses thereof
DE102007034620A1 (de) 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
WO2009026248A2 (en) 2007-08-17 2009-02-26 The Government Of The United States, As Represented By The Secretary Of Health And Human Services, National Institutes Of Health, Office Of Technology Transfer Hydrazide, amide, phthalimide and phthalhydrazide analogs as inhibitors of retroviral integrase
AR070027A1 (es) 2007-09-17 2010-03-10 Abbott Lab Agentes anti-infecciosos contra el virus hcv
US20090076275A1 (en) 2007-09-19 2009-03-19 David Robert Bolin Diacylglycerol acyltransferase inhibitors
EP2217068A4 (en) 2007-10-11 2011-09-14 Glaxosmithkline Llc NOVEL INHIBITORS OF SEH AND THEIR USE
CA2702950A1 (en) 2007-10-16 2009-04-23 Northeastern University Methods and compounds for modulating cannabinoid activity
US20100261679A1 (en) 2007-10-18 2010-10-14 James Sutton CSF-1R, Inhibitors, Compositions, and Methods of Use
BRPI0821102A2 (pt) 2007-11-29 2015-06-16 Hoffmann La Roche Preparação de derivados de di-hidropirrol como intermediários
WO2009073788A1 (en) 2007-12-07 2009-06-11 Firestone Leigh H Compositions and methods for treating menopausal females
US20100273806A1 (en) * 2007-12-18 2010-10-28 Arena Pharmaceuticals, Inc. Tetrahydrocyclopenta[b]indol-3-yl carboxylic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
EP2078711A1 (en) 2007-12-28 2009-07-15 AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A. (Aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor
FR2926554B1 (fr) 2008-01-22 2010-03-12 Sanofi Aventis Derives de carboxamides azabicycliques, leur preparation et leur application en therapeutique
CN101225070B (zh) 2008-01-31 2010-04-14 上海交通大学 用于抗肿瘤的药物
WO2009097972A1 (de) 2008-02-05 2009-08-13 Sanofi-Aventis Sf5-derivate als par1-inhibitoren, ihre herstellung und verwendung als arzneimittel
WO2009112445A1 (en) 2008-03-10 2009-09-17 Novartis Ag Method of increasing cellular phosphatidyl choline by dgat1 inhibition
GB0804702D0 (en) 2008-03-13 2008-04-16 Amura Therapeutics Ltd Compounds
GB0804701D0 (en) 2008-03-13 2008-04-16 Amura Therapeutics Ltd Compounds
WO2009124755A1 (en) 2008-04-08 2009-10-15 European Molecular Biology Laboratory (Embl) Compounds with novel medical uses and method of identifying such compounds
US7863291B2 (en) 2008-04-23 2011-01-04 Bristol-Myers Squibb Company Quinuclidine compounds as alpha-7 nicotinic acetylcholine receptor ligands
US8309577B2 (en) 2008-04-23 2012-11-13 Bristol-Myers Squibb Company Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands
GB0809776D0 (en) 2008-05-29 2008-07-09 Amura Therapeutics Ltd Compounds
JP5615274B2 (ja) 2008-07-01 2014-10-29 ジェネンテック, インコーポレイテッド Mekキナーゼインヒビターとしてのイソインドロン誘導体及びその使用方法
EP2331499B1 (en) 2008-08-19 2016-09-21 Janssen Pharmaceutica NV Cold menthol receptor antagonists
US20110230472A1 (en) 2008-08-29 2011-09-22 Shionogi & Co., Ltd. Ring-fused azole derivative having pi3k-inhibiting activity
CA2741400A1 (en) 2008-09-16 2010-03-25 Merck & Co., Inc. Sulfonamide derivative metabotropic glutamate r4 ligands
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
WO2010056194A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
CN101455661B (zh) 2008-11-19 2012-10-10 中国科学院上海有机化学研究所 3-取代苯酞及其类似物的用途
RU2016116516A (ru) 2008-12-08 2018-12-07 Мандифарма Интернэшнл Корпорейшн Лимитед Композиции ингибиторов тирозинкиназных рецепторов белков
BRPI1004930B1 (pt) 2009-01-28 2017-10-17 Bayer Intellectual Property Gmbh Compounds, fungicidal composition and method for controlling phytopathogenic fungi of crops.
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
MX2012007080A (es) * 2009-12-23 2012-07-20 Sanofi Sa [4[4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(1h-pirrolo-pi ri-din-il)-metanonas y sintesis de las mismas.
JP2013517326A (ja) 2010-01-19 2013-05-16 リサーチ・トライアングル・インスティチュート κオピオイド受容体結合リガンド
KR20120117905A (ko) 2010-01-28 2012-10-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 프로테아좀 활성을 향상시키는 조성물 및 방법
EP2368886A1 (en) 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
CN102241621A (zh) 2010-05-11 2011-11-16 江苏恒瑞医药股份有限公司 5,5-双取代-2-亚氨基吡咯烷类衍生物、其制备方法及其在医药上的应用
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
ES2526124T3 (es) 2010-06-16 2015-01-07 Cymabay Therapeutics, Inc. Agonistas del receptor GPR120 y sus usos
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012028100A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
AR082885A1 (es) 2010-09-03 2013-01-16 Genentech Inc Compuestos y composiciones para la inhibicion de nampt
US9266855B2 (en) 2010-09-27 2016-02-23 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
JP2013253019A (ja) 2010-09-28 2013-12-19 Kowa Co 新規なピペリジン誘導体及びこれを含有する医薬
JP6063870B2 (ja) 2010-11-08 2017-01-18 ライセラ・コーポレイション RORγ活性の阻害用のN−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療
JP2013545740A (ja) 2010-11-10 2013-12-26 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング バニロイド受容体リガンドとしての置換された複素芳香族カルボキサミド誘導体および尿素誘導体
WO2012100734A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Compounds useful as retinoid-related orphan receptor gamma modulators
WO2012100732A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
CN102180780A (zh) 2011-03-07 2011-09-14 中国科学技术大学 茚酮类衍生物及其作为淀粉样蛋白沉积物和神经纤维缠结的显像剂和聚集抑制剂的用途
US9090568B2 (en) 2011-03-14 2015-07-28 Impact Therapeutics, Inc. Quinazolinediones and their use
WO2012134943A1 (en) 2011-03-25 2012-10-04 Abbott Laboratories Trpv1 antagonists
CN103459403B (zh) 2011-04-04 2016-08-17 默克专利有限公司 金属络合物
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
WO2012147916A1 (ja) 2011-04-28 2012-11-01 日本たばこ産業株式会社 アミド化合物およびその医薬用途
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
US20140155381A1 (en) 2011-07-29 2014-06-05 Erkan Baloglu Compounds and methods
US20140256740A1 (en) 2011-07-29 2014-09-11 Tempero Pharmaceuticals, Inc. Compounds and methods
EP2738170B1 (en) 2011-07-29 2017-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP2736329A4 (en) 2011-07-29 2015-03-25 Tempero Pharmaceuticals Inc COMPOUNDS AND METHODS
WO2013029338A1 (en) 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
WO2013042782A1 (ja) 2011-09-22 2013-03-28 武田薬品工業株式会社 縮合複素環化合物
GB201116641D0 (en) 2011-09-27 2011-11-09 Glaxo Group Ltd Novel compounds
US20140256767A1 (en) 2011-10-31 2014-09-11 The Broad Institute, Inc. Direct inhibitors of keap1-nrf2 interaction as antioxidant inflammation modulators
WO2013064231A1 (en) 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)
EP2800745B1 (en) 2011-12-02 2020-02-12 Phenex Pharmaceuticals AG Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
US8741892B2 (en) 2011-12-05 2014-06-03 Boehringer Ingelheim International Gmbh Compounds
US8642774B2 (en) 2011-12-08 2014-02-04 Boehringer Ingelheim International Gmbh Compounds
US8796467B2 (en) 2011-12-13 2014-08-05 Boehringer Ingelheim International Gmbh Compounds
WO2013092460A1 (en) 2011-12-20 2013-06-27 Syngenta Participations Ag Cyclic bisoxime microbicides
CA2860382C (en) 2011-12-21 2017-09-12 Allergan, Inc. Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
US20130190356A1 (en) 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
US9216988B2 (en) 2011-12-22 2015-12-22 Genentech, Inc. Benzyl sulfonamide derivatives as RORc modulators
WO2013100027A1 (ja) 2011-12-28 2013-07-04 武田薬品工業株式会社 複素環化合物
WO2013159095A1 (en) 2012-04-20 2013-10-24 Anderson Gaweco Ror modulators and their uses
GB201207406D0 (en) 2012-04-27 2012-06-13 Glaxo Group Ltd Novel compounds
PE20142400A1 (es) 2012-04-27 2015-02-04 Glaxo Group Ltd Compuestos novedosos
WO2013166013A1 (en) 2012-04-30 2013-11-07 Anderson Gaweco Ror modulators and their uses
EP2847198B1 (en) 2012-05-08 2016-12-14 Lycera Corporation Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of ror-gamma and the treatment of disease
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
CA2871504C (en) 2012-05-08 2020-07-21 Merck Sharp & Dohme Corp. Bicyclic sulfone compounds for inhibition of rorgamma activity and the treatment of disease
CN107007597A (zh) 2012-05-31 2017-08-04 菲尼克斯药品股份公司 作为孤儿核受体RORγ调节物的经甲酰胺或磺酰胺取代的噻唑及相关衍生物的制药用途
AR091654A1 (es) 2012-07-02 2015-02-18 Biogen Idec Inc COMPUESTOS QUE CONTIENEN BIARILO COMO AGONISTAS INVERSOS DE RECEPTORES ROR-g
AR092348A1 (es) 2012-07-11 2015-04-15 Hoffmann La Roche DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc
WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014028669A1 (en) 2012-08-15 2014-02-20 Biogen Idec Ma Inc. Novel compounds for modulation of ror-gamma activity
WO2014026329A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026328A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof
LT2897939T (lt) 2012-09-21 2017-05-10 Sanofi Benzimidazolo karboksirūgšties amido dariniai metabolinių arba širdies ir kraujagyslių ligų gydymui
HK1213887A1 (zh) * 2012-10-16 2016-07-15 Janssen Pharmaceutica N.V. RORγt的苯基连接的喹啉基调节剂
WO2014062938A1 (en) 2012-10-19 2014-04-24 Bristol-Myers Squibb Company Rory modulators
SI2928885T1 (sl) 2012-12-06 2017-06-30 Glaxo Group Limited Modulatorji retinoidnemu sorodnega receptorja gama sirote (ror-gama) za uporabo pri zdravljenju avtoimunskih in vnetnih bolezni
WO2013171729A2 (en) 2013-01-08 2013-11-21 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl amide compounds as rorgamat modulator
EP2991994B1 (en) 2013-05-01 2018-08-15 Vitae Pharmaceuticals, Inc. Thiazolopyrrolidine inhibitors of ror-gamma
TWI652014B (zh) 2013-09-13 2019-03-01 美商艾佛艾姆希公司 雜環取代之雙環唑殺蟲劑
ES2841082T3 (es) * 2013-10-15 2021-07-07 Janssen Pharmaceutica Nv Moduladores de quinolinilo enlazados a fenilo de ROR-gamma-t
WO2015083130A1 (en) 2013-12-06 2015-06-11 Aurigene Discovery Technologies Limited Fused pyridine and pyrimidine derivatives as ror gamma modulators
SG11201605178WA (en) 2013-12-24 2016-07-28 Harvard College Cortistatin analogues and syntheses and uses thereof
JP2015124178A (ja) 2013-12-26 2015-07-06 東レ株式会社 環状アミン誘導体及びその医薬用途
WO2015101928A1 (en) 2013-12-31 2015-07-09 Aurigene Discovery Technologies Limited Fused thiophene and thiazole derivatives as ror gamma modulators
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
CN105960395B (zh) 2014-02-03 2020-05-01 巴斯夫欧洲公司 防治无脊椎动物害虫的环戊烯和环戊二烯化合物
WO2015139619A1 (zh) * 2014-03-18 2015-09-24 北京韩美药品有限公司 作为RORγ调节剂的化合物
CR20160418A (es) 2014-03-26 2016-11-07 Hoffmann La Roche Nuevos compuestos biciclicos de 7 eslabones
MA50635A (fr) 2014-03-26 2020-08-12 Hoffmann La Roche Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JP2017515794A (ja) 2014-03-26 2017-06-15 ビーエーエスエフ ソシエタス・ヨーロピアBasf Se 殺菌剤としての置換[1,2,4]トリアゾール及びイミダゾール化合物
CA2942871A1 (en) * 2014-03-27 2015-10-01 Piramal Enterprises Limited Ror-gamma modulators and uses thereof
CA2940264A1 (en) * 2014-04-16 2015-10-22 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl ether compounds as ror gamma modulators
SI3207043T1 (sl) 2014-10-14 2019-04-30 Vitae Pharmaceuticals, Inc. Dihidropirolopiridinovi inhibitorji za ROR-gama
WO2016064970A1 (en) 2014-10-22 2016-04-28 The Board Of Regents Of The University Of Texas System Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
CN107635984B (zh) 2015-03-11 2021-04-13 Fmc公司 杂环取代的二环唑杀有害生物剂
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ROR-γ調節劑
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009083526A1 (en) * 2008-01-02 2009-07-09 Smithkline Beecham Corporation Novel compounds
WO2013019682A1 (en) * 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013078233A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-benzylbenzimidazole modulators of pparg
WO2013078240A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-biphenylmethylbenzimidazole modulators of pparg

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SIME MAIRI ET AL, "Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPAR[gamma] partial agonist", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, (2011-06-29), vol. 21, no. 18, pages 5568 - 5572 *

Also Published As

Publication number Publication date
US20190352286A1 (en) 2019-11-21
EP3408268B1 (en) 2021-08-04
SA518392101B1 (ar) 2022-03-16
CN109071509B (zh) 2021-11-30
JP6948333B2 (ja) 2021-10-13
MX2018009257A (es) 2018-11-09
TWI757266B (zh) 2022-03-11
JP2019503385A (ja) 2019-02-07
EP3408268B8 (en) 2023-12-06
BR112018015273A2 (pt) 2018-12-18
US10829481B2 (en) 2020-11-10
CA3011838A1 (en) 2017-08-03
UY37098A (es) 2017-08-31
MA45646A (fr) 2021-03-24
WO2017132432A1 (en) 2017-08-03
RU2021133444A (ru) 2021-11-29
WO2017132432A8 (en) 2017-08-31
AU2017212577A1 (en) 2018-08-02
TW201734001A (zh) 2017-10-01
EP3408268A1 (en) 2018-12-05
EP3939974A1 (en) 2022-01-19
MA55328A (fr) 2022-01-19
US20210094940A1 (en) 2021-04-01
CN109071509A (zh) 2018-12-21
CN114230523A (zh) 2022-03-25
MX381313B (es) 2025-03-12
TW202220968A (zh) 2022-06-01
RU2760366C2 (ru) 2021-11-24
JP2021193131A (ja) 2021-12-23
KR20180100697A (ko) 2018-09-11
RU2018127360A3 (enExample) 2020-04-06
RU2018127360A (ru) 2020-03-02

Similar Documents

Publication Publication Date Title
EP3408268B1 (en) Benzimidazole derivatives as modulators of ror-gamma
US10829448B2 (en) Substituted benzoimidazoles as modulators of ROR-γ
AU2015210833B2 (en) Dihydropyrrolopyridine inhibitors of ROR-gamma
US11008340B2 (en) Modulators of ROR-gamma
EA031967B1 (ru) ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ
HK40069627A (en) Modulators of ror-gamma
HK40001214B (en) Benzimidazole derivatives as modulators of ror-gamma
HK40055299A (en) Modulators of ror-gamma
HK1256599B (en) Modulators of ror-gamma
HK40013118B (en) Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating dry eye
HK40013118A (en) Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating dry eye
HK1229788B (en) Dihydropyrrolopyridine inhibitors of ror-gamma
HK1229788A1 (en) Dihydropyrrolopyridine inhibitors of ror-gamma

Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ CLAREMON, DAVID A.; DILLARD, LAWRENCE WAYNE; FAN, YI; LOTESTA, STEPHEN D.; SINGH, SURESH B.; TICE, COLIN M.; ZHAO, WEI AND ZHUANG, LINGHANG

HB Alteration of name in register

Owner name: VITAE PHARMACEUTICALS, LLC

Free format text: FORMER NAME(S): VITAE PHARMACEUTICALS, INC.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired