RU2021133849A - Улучшенные агонисты апелинового рецептора (apj) и их использование - Google Patents
Улучшенные агонисты апелинового рецептора (apj) и их использование Download PDFInfo
- Publication number
- RU2021133849A RU2021133849A RU2021133849A RU2021133849A RU2021133849A RU 2021133849 A RU2021133849 A RU 2021133849A RU 2021133849 A RU2021133849 A RU 2021133849A RU 2021133849 A RU2021133849 A RU 2021133849A RU 2021133849 A RU2021133849 A RU 2021133849A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- conr
- alkenyl
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 76
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 46
- 125000003118 aryl group Chemical group 0.000 claims 44
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 13
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 8
- 125000005012 alkyl thioether group Chemical group 0.000 claims 8
- 150000001356 alkyl thiols Chemical class 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 239000000651 prodrug Chemical class 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 102100030949 Apelin receptor Human genes 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 108091008803 APLNR Proteins 0.000 claims 4
- 102000016555 Apelin receptors Human genes 0.000 claims 4
- -1 adamantanyl Chemical group 0.000 claims 4
- 125000004171 alkoxy aryl group Chemical group 0.000 claims 4
- 125000005233 alkylalcohol group Chemical group 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 201000011461 pre-eclampsia Diseases 0.000 claims 2
- 230000008085 renal dysfunction Effects 0.000 claims 2
- OUOJIFQQBPKAMU-UHFFFAOYSA-N tetrazol-5-one Chemical compound O=C1N=NN=N1 OUOJIFQQBPKAMU-UHFFFAOYSA-N 0.000 claims 2
- SKMUADUXCABNRO-UHFFFAOYSA-N 3-methyl-2h-1,3-thiazole Chemical compound CN1CSC=C1 SKMUADUXCABNRO-UHFFFAOYSA-N 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 239000002160 alpha blocker Substances 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 229940097320 beta blocking agent Drugs 0.000 claims 1
- 150000001602 bicycloalkyls Chemical group 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
Classifications
-
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/02—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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—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
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D471/08—Bridged 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
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562265177P | 2015-12-09 | 2015-12-09 | |
| US201562265168P | 2015-12-09 | 2015-12-09 | |
| US62/265.168 | 2015-12-09 | ||
| US62/265,177 | 2015-12-09 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018118568A Division RU2766148C1 (ru) | 2015-12-09 | 2016-12-09 | Улучшенные агонисты апелинового рецептора (apj) и их использование |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2021133849A true RU2021133849A (ru) | 2022-03-21 |
Family
ID=57796972
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018118568A RU2766148C1 (ru) | 2015-12-09 | 2016-12-09 | Улучшенные агонисты апелинового рецептора (apj) и их использование |
| RU2021133849A RU2021133849A (ru) | 2015-12-09 | 2016-12-09 | Улучшенные агонисты апелинового рецептора (apj) и их использование |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018118568A RU2766148C1 (ru) | 2015-12-09 | 2016-12-09 | Улучшенные агонисты апелинового рецептора (apj) и их использование |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US10100059B2 (enExample) |
| EP (1) | EP3386976A1 (enExample) |
| JP (2) | JP2019501899A (enExample) |
| KR (1) | KR20180090852A (enExample) |
| CN (1) | CN108602806B (enExample) |
| AU (1) | AU2016366310C1 (enExample) |
| BR (1) | BR112018011784A2 (enExample) |
| CO (1) | CO2018005871A2 (enExample) |
| HK (1) | HK1255452A1 (enExample) |
| IL (1) | IL259634A (enExample) |
| MA (1) | MA43417A (enExample) |
| MX (2) | MX391898B (enExample) |
| PE (1) | PE20190258A1 (enExample) |
| RU (2) | RU2766148C1 (enExample) |
| WO (1) | WO2017100558A1 (enExample) |
| ZA (1) | ZA201803301B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112016028119A2 (pt) | 2014-06-06 | 2017-08-22 | Res Triangle Inst | Agonistas receptores de apelina (apj) e usos dos mesmos |
| EA034776B1 (ru) | 2015-05-20 | 2020-03-19 | Эмджен Инк. | Триазоловые агонисты рецептора apj |
| PE20180506A1 (es) | 2015-06-03 | 2018-03-09 | Bristol Myers Squibb Co | Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril) piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares |
| CN108602806B (zh) | 2015-12-09 | 2022-07-12 | 研究三角协会 | 改进的爱帕琳肽受体(apj)激动剂及其用途 |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| AU2017343638B2 (en) * | 2016-10-12 | 2021-12-09 | Research Triangle Institute | Heterocyclic apelin receptor (APJ) agonists and uses thereof |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| US10689367B2 (en) | 2016-11-16 | 2020-06-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the APJ receptor |
| MA46824A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole substitués par alkyle en tant qu'agonistes du récepteur apj |
| WO2018097945A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| MA46827A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole à substitution cycloalkyle en tant qu'agonistes du récepteur apj |
| US11247987B2 (en) | 2017-10-06 | 2022-02-15 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 30 |
| ES2930258T3 (es) | 2017-10-06 | 2022-12-09 | Univ Johns Hopkins | Nuevos antagonistas de glutamina y usos de los mismos |
| US11149040B2 (en) | 2017-11-03 | 2021-10-19 | Amgen Inc. | Fused triazole agonists of the APJ receptor |
| EP3788037A1 (en) | 2018-05-01 | 2021-03-10 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
| IL278291B2 (en) | 2018-05-17 | 2023-10-01 | Forma Therapeutics Inc | Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors |
| LT3860989T (lt) | 2018-10-05 | 2023-06-12 | Forma Therapeutics, Inc. | Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai |
| EP4021447A4 (en) * | 2019-08-29 | 2023-10-11 | Research Triangle Institute | METHODS AND USES FOR APELIN RECEPTOR AGONISTS |
| CA3208025A1 (en) * | 2021-02-25 | 2022-09-01 | Scott P. Runyon | Heteroaryl derivatives as apelin receptor agonists |
| EP4646220A1 (en) | 2023-01-03 | 2025-11-12 | Bioage Labs, Inc. | Combination therapy of apelin receptor agonist and glp-1 receptor agonist for treating a disease or condition associated with weight gain |
| WO2025213190A1 (en) | 2024-04-05 | 2025-10-09 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
| WO2025251084A1 (en) | 2024-05-31 | 2025-12-04 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5998004A (ja) | 1982-11-25 | 1984-06-06 | Kureha Chem Ind Co Ltd | 1,2,4―トリアゾール誘導体及び除草剤 |
| JPS58194866A (ja) | 1982-05-07 | 1983-11-12 | Kureha Chem Ind Co Ltd | トリアゾ−ル誘導体及び該誘導体を含有する除草剤 |
| DE3316300A1 (de) | 1982-05-07 | 1983-11-24 | Kureha Kagaku Kogyo K.K., Tokyo | Heribizide zusammensetzung mit einem gehalt an einem derivat des 1,2,4-triazols als wirkstoff |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5965695A (en) | 1990-05-15 | 1999-10-12 | Chiron Corporation | Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such |
| FR2665898B1 (fr) | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2713225B1 (fr) * | 1993-12-02 | 1996-03-01 | Sanofi Sa | N-pipéridino-3-pyrazolecarboxamide substitué. |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| FR2711140B1 (fr) | 1993-10-12 | 1996-01-05 | Sanofi Sa | 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant. |
| FR2732967B1 (fr) | 1995-04-11 | 1997-07-04 | Sanofi Sa | 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| FR2741621B1 (fr) | 1995-11-23 | 1998-02-13 | Sanofi Sa | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant |
| FR2757869B1 (fr) | 1996-12-31 | 1999-05-21 | Rhodia Chimie Sa | Utilisation de melanges a base de pt et de composes de metaux de transition autres que le pt pour ameliorer les proprietes de resistance a l'arc des elastomeres silicones |
| US7045532B2 (en) | 1999-04-30 | 2006-05-16 | Millennium Pharmaceuticals, Inc. | ACE-2 modulating compounds and methods of use thereof |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| BR0209325A (pt) | 2001-05-03 | 2004-07-20 | Hoffmann La Roche | Forma de dosagem farmacêutica de mesilato de nelfinavir amorfo |
| US6737042B2 (en) | 2001-05-24 | 2004-05-18 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| TWI231757B (en) | 2001-09-21 | 2005-05-01 | Solvay Pharm Bv | 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
| US7109216B2 (en) | 2001-09-21 | 2006-09-19 | Solvay Pharmaceuticals B.V. | 1H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
| PE20030547A1 (es) | 2001-09-24 | 2003-08-18 | Bayer Corp | Derivados de imidazol para el tratamiento de la obesidad |
| AR038967A1 (es) | 2002-03-18 | 2005-02-02 | Solvay Pharm Bv | Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensina |
| HRP20050053A2 (en) | 2002-09-19 | 2005-04-30 | Solvay Pharmaceuticals B.V. | 1 h-1,2,4-triazole-3-carboxamide derivatives as cannabinoid-cb1 receptor ligands |
| WO2005054204A2 (en) | 2003-11-26 | 2005-06-16 | Synchrony Biosciences, Inc. | Pharmaceutical compounds that regenerate in vivo |
| TW200526641A (en) * | 2003-12-26 | 2005-08-16 | Daiichi Seiyaku Co | Amidopyrazole derivatives |
| WO2005099705A2 (en) | 2004-03-24 | 2005-10-27 | Bayer Pharmaceuticals Corporation | Preparation of imidazole derivatives and methods of use |
| KR20070083839A (ko) | 2004-09-29 | 2007-08-24 | 코디스 코포레이션 | 안정한 무정형 라파마이신 유사 화합물의 약학적 투약 형태 |
| US20080125409A1 (en) | 2004-10-19 | 2008-05-29 | Daiichi Pharmaceutical Co., Ltd. | 1,5-Diheterocycle-1H-Triazole Derivative |
| WO2006133926A1 (en) | 2005-06-17 | 2006-12-21 | Carex Sa | Pyrazole derivates as cannabinoid receptor modulators |
| JP4851546B2 (ja) | 2006-03-10 | 2012-01-11 | ジェンリン ディスカバリー | 肥満治療に有用なカンナビノイド受容体アンタゴニスト/インバースアゴニスト |
| CN106125048B (zh) | 2016-07-11 | 2019-05-24 | 浙江大华技术股份有限公司 | 一种声源定位方法及装置 |
| EP1903052A3 (en) | 2006-07-28 | 2008-04-02 | Faust Pharmaceuticals SA | APJ receptor ligands and uses thereof |
| CA2660261A1 (en) | 2006-08-09 | 2008-02-14 | Pfizer Products Inc. | Heterocycles useful as inhibitors of carbonic anhydrase |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| JP5464395B2 (ja) | 2008-02-01 | 2014-04-09 | 大陽日酸株式会社 | 重水素化された芳香環又は複素環を有する化合物の製造方法 |
| US8354557B2 (en) | 2008-06-17 | 2013-01-15 | Concert Pharmaceuticals, Inc. | Synthesis of deuterated morpholine derivatives |
| EP2334621A1 (en) | 2008-09-16 | 2011-06-22 | Concert Pharmaceuticals, Inc. | Deuterated 2-amino-3-hydroxypropanoic acid derivatives |
| WO2010053545A2 (en) | 2008-11-04 | 2010-05-14 | Anchor Therapeutics, Inc. | Apj receptor compounds |
| JP5621148B2 (ja) * | 2008-11-21 | 2014-11-05 | ラクオリア創薬株式会社 | 5−ht2b受容体拮抗活性を有する新規ピラゾール−3−カルボキサミド誘導体 |
| US20100160323A1 (en) | 2008-12-23 | 2010-06-24 | Alexander Bischoff | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE |
| CN101519430A (zh) | 2009-03-20 | 2009-09-02 | 中国农业大学 | 一类新型保幼激素合成抑制剂-苯丙-甘-亮三肽酰胺类似物 |
| WO2011005052A2 (en) | 2009-07-10 | 2011-01-13 | Green Gross Corporation | Novel arylpiperazine-containing imidazole 4-carboxamide derivatives and pharmaceutical composition comprising same |
| DE102009036604A1 (de) | 2009-07-30 | 2011-02-03 | Aicuris Gmbh & Co. Kg | Substituierte Bis-Arylpyrazolamide mit terminaler primärer Amidfunktionalisierung und ihre Verwendung |
| WO2011156557A2 (en) * | 2010-06-11 | 2011-12-15 | Thomas James B | Compounds active at the neurotensin receptor |
| EP2714624B1 (en) | 2011-05-23 | 2017-12-27 | Sanofi | Process for the preparation of deuterated compounds containing n-alkyl groups |
| CA2835216A1 (en) * | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| CN105646362B (zh) | 2011-07-26 | 2019-07-05 | 赛诺菲 | 3-杂芳酰基氨基-丙酸衍生物及其作为药物的用途 |
| US9815851B2 (en) | 2011-12-02 | 2017-11-14 | Phenex Pharmaceuticals Ag | Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases |
| JP2013231000A (ja) | 2012-04-27 | 2013-11-14 | Dainippon Sumitomo Pharma Co Ltd | 3−アミノメチルピラゾール誘導体 |
| JP6225178B2 (ja) | 2012-05-31 | 2017-11-01 | フェネックス ファーマシューティカルス アーゲー | オーファン核内受容体RORγの調整剤としてのカルボキサミドまたはスルホンアミド置換されたチアゾールおよび関連する誘導体 |
| JO3215B1 (ar) | 2012-08-09 | 2018-03-08 | Phenex Pharmaceuticals Ag | حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy |
| CA2883641C (en) | 2012-09-18 | 2021-09-14 | Auspex Pharmaceuticals, Inc. | Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 |
| PT2897939T (pt) | 2012-09-21 | 2017-05-04 | Sanofi Sa | Derivados de amida do ácido benzoimidazol-carboxílico para tratamento de doenças metabólicas ou cardiovasculares |
| WO2014053533A1 (en) | 2012-10-05 | 2014-04-10 | Sanofi | Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation |
| MX2015008187A (es) | 2012-12-20 | 2016-02-05 | Concert Pharmaceuticals Inc | Inhibidores de alk deuterados. |
| JP6473133B2 (ja) | 2013-03-15 | 2019-02-20 | アラクセス ファーマ エルエルシー | Krasg12cの共有結合性阻害剤 |
| CA2909270A1 (en) | 2013-04-12 | 2014-10-16 | Achillion Pharmaceuticals, Inc. | Highly active nucleoside derivative for the treatment of hcv |
| PL3424920T3 (pl) | 2013-10-17 | 2020-11-16 | Vertex Pharmaceuticals Incorporated | Kokryształy (S)-N-metylo-8-(1-((2'-metylo-4’,6'-dideutero-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK |
| US20170174633A1 (en) * | 2014-03-25 | 2017-06-22 | Research Triangle Institute | Pyrazole compounds selective for neurotensin 2 receptor |
| US10570128B2 (en) | 2014-05-28 | 2020-02-25 | Sanford Burnham Prebys Medical Discovery Institute | Agonists of the apelin receptor and methods of use thereof |
| BR112016028119A2 (pt) | 2014-06-06 | 2017-08-22 | Res Triangle Inst | Agonistas receptores de apelina (apj) e usos dos mesmos |
| CN108602806B (zh) | 2015-12-09 | 2022-07-12 | 研究三角协会 | 改进的爱帕琳肽受体(apj)激动剂及其用途 |
| AU2017343638B2 (en) | 2016-10-12 | 2021-12-09 | Research Triangle Institute | Heterocyclic apelin receptor (APJ) agonists and uses thereof |
| EP4021447A4 (en) | 2019-08-29 | 2023-10-11 | Research Triangle Institute | METHODS AND USES FOR APELIN RECEPTOR AGONISTS |
-
2016
- 2016-12-09 CN CN201680081397.9A patent/CN108602806B/zh not_active Expired - Fee Related
- 2016-12-09 BR BR112018011784A patent/BR112018011784A2/pt not_active Application Discontinuation
- 2016-12-09 MA MA043417A patent/MA43417A/fr unknown
- 2016-12-09 HK HK18114625.4A patent/HK1255452A1/zh unknown
- 2016-12-09 RU RU2018118568A patent/RU2766148C1/ru active
- 2016-12-09 RU RU2021133849A patent/RU2021133849A/ru unknown
- 2016-12-09 JP JP2018530026A patent/JP2019501899A/ja active Pending
- 2016-12-09 MX MX2018006979A patent/MX391898B/es unknown
- 2016-12-09 EP EP16826220.2A patent/EP3386976A1/en active Pending
- 2016-12-09 KR KR1020187018896A patent/KR20180090852A/ko not_active Ceased
- 2016-12-09 US US15/374,386 patent/US10100059B2/en not_active Ceased
- 2016-12-09 AU AU2016366310A patent/AU2016366310C1/en active Active
- 2016-12-09 WO PCT/US2016/065808 patent/WO2017100558A1/en not_active Ceased
- 2016-12-09 PE PE2018001082A patent/PE20190258A1/es unknown
-
2018
- 2018-05-17 ZA ZA2018/03301A patent/ZA201803301B/en unknown
- 2018-05-18 US US15/983,519 patent/US10954247B2/en active Active
- 2018-05-27 IL IL259634A patent/IL259634A/en unknown
- 2018-06-07 MX MX2022002026A patent/MX2022002026A/es unknown
- 2018-06-07 CO CONC2018/0005871A patent/CO2018005871A2/es unknown
-
2020
- 2020-05-04 US US16/974,363 patent/USRE49594E1/en active Active
- 2020-10-28 US US17/082,650 patent/US11535630B2/en active Active
-
2021
- 2021-02-26 JP JP2021029791A patent/JP7195356B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| BR112018011784A2 (pt) | 2018-12-04 |
| PE20190258A1 (es) | 2019-02-25 |
| ZA201803301B (en) | 2019-07-31 |
| CN108602806B (zh) | 2022-07-12 |
| CA3006205A1 (en) | 2017-06-15 |
| WO2017100558A1 (en) | 2017-06-15 |
| USRE49594E1 (en) | 2023-08-01 |
| AU2016366310B8 (en) | 2021-06-03 |
| KR20180090852A (ko) | 2018-08-13 |
| MA43417A (fr) | 2018-10-17 |
| AU2016366310A8 (en) | 2021-06-03 |
| JP7195356B2 (ja) | 2022-12-23 |
| US11535630B2 (en) | 2022-12-27 |
| AU2016366310A1 (en) | 2018-06-07 |
| MX391898B (es) | 2025-03-21 |
| EP3386976A1 (en) | 2018-10-17 |
| AU2016366310C1 (en) | 2021-09-09 |
| MX2018006979A (es) | 2019-05-16 |
| RU2766148C1 (ru) | 2022-02-08 |
| AU2016366310B2 (en) | 2021-05-20 |
| IL259634A (en) | 2018-07-31 |
| US20180265518A1 (en) | 2018-09-20 |
| JP2021100934A (ja) | 2021-07-08 |
| HK1255452A1 (zh) | 2019-08-16 |
| JP2019501899A (ja) | 2019-01-24 |
| MX2022002026A (es) | 2022-03-11 |
| US10954247B2 (en) | 2021-03-23 |
| US10100059B2 (en) | 2018-10-16 |
| CO2018005871A2 (es) | 2018-07-10 |
| US20170166577A1 (en) | 2017-06-15 |
| US20210070767A1 (en) | 2021-03-11 |
| CN108602806A (zh) | 2018-09-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2021133849A (ru) | Улучшенные агонисты апелинового рецептора (apj) и их использование | |
| JP2021100934A5 (enExample) | ||
| RU2016144329A (ru) | Агонисты рецептора апелина (apj) и его применение | |
| EA201390840A1 (ru) | Полициклический lpaантагонист и его применение | |
| AR124662A2 (es) | Formulaciones inmunosupresoras | |
| RU2019123529A (ru) | Соединение хиназолина | |
| JP2014505660A5 (enExample) | ||
| AR074089A1 (es) | Antagonistas de cicloalcano (b) azaindol de los receptores de la postaglandina d2 | |
| CY1119357T1 (el) | Φαρμακευτικες συνθεσεις που περιλαμβανουν συνδετες υποδοχεων σιγμα | |
| PE20140604A1 (es) | Combinacion de panobinostat y ruxolitinib en el tratamiento del cancer tal como una neoplasia mieloproliferativa | |
| RU2019103873A (ru) | Гетероциклические агонисты рецептора апелина (apj) и их применение | |
| AR073551A1 (es) | Pirimidinas macrociclicas como inhibidores de proteina cinasa | |
| EA201100698A1 (ru) | Производные тиенотриазолодиазепина, активные в отношении апо а1 | |
| WO2009143039A3 (en) | Heterocyclic compounds as factor ixa inhibitors | |
| AR127235A1 (es) | Pirazoloquinolinas inhibidoras de kras | |
| EA201071232A1 (ru) | Триазины как ингибиторы киназы pi3 и mtor | |
| SI2820009T1 (en) | Serine / Threonine kinase inhibitors | |
| RU2017134551A (ru) | Новые дигидропиридоизохинолиноны и их фармацевтические композиции для лечения воспалительных расстройств | |
| EA200702331A1 (ru) | Способ получения стробилуринового фунгицида, соединение и композиция | |
| EA201492170A1 (ru) | Новые замещенные в цикле n-пиридиниламиды в качестве ингибиторов киназ | |
| RU2013109138A (ru) | ЛЕКАРСТВЕННАЯ ДОЗИРОВАННАЯ ФОРМА, КОТОРАЯ СОДЕРЖИТ 6'-ФТОР-(N-МЕТИЛ-ИЛИ N,N-ДИМЕТИЛ-)-4-ФЕНИЛ-4',9'-ДИГИДРО-3'Н-СПИРО[ЦИКЛОГЕКСАН-1,1'-ПИРАНО[3,4,b]ИНДОЛ]-4-АМИН | |
| RU2014126646A (ru) | Циклические амидные производные как ингибиторы 11-бета-гидроксистероид-дегидрогеназы и их применение | |
| JP2013500342A5 (enExample) | ||
| RU2014122866A (ru) | Пропеноатные производные бетулина | |
| JP2013522368A5 (enExample) |