[go: up one dir, main page]

AR080112A1 - Derivados de fenilalanina y su uso como moduladores de los receptores del glp-1 no peptidicos - Google Patents

Derivados de fenilalanina y su uso como moduladores de los receptores del glp-1 no peptidicos

Info

Publication number
AR080112A1
AR080112A1 ARP110100351A ARP110100351A AR080112A1 AR 080112 A1 AR080112 A1 AR 080112A1 AR P110100351 A ARP110100351 A AR P110100351A AR P110100351 A ARP110100351 A AR P110100351A AR 080112 A1 AR080112 A1 AR 080112A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
nr1br1c
carbocyclyl
nr1as
heteroaryl
Prior art date
Application number
ARP110100351A
Other languages
English (en)
Original Assignee
Argusina Inc
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 Argusina Inc filed Critical Argusina Inc
Publication of AR080112A1 publication Critical patent/AR080112A1/es

Links

Classifications

    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/51—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/87—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
    • C07C323/59—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton with acylated amino groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
    • 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
    • C07D231/04—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C07D233/08—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms
    • C07D233/12—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D233/16—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/40—Radicals substituted by oxygen atoms
    • C07D307/42—Singly bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/08—Hydrogen atoms or radicals containing only hydrogen and carbon atoms
    • C07D333/10—Thiophene
    • 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
    • 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
    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Se proporcionan compuestos moduladores del receptor de GLP-1 no peptídicos, por ejemplo, de Formula 1, composiciones farmacéuticas que comprenden estos compuestos y procesos para su preparacion. También se proporcionan métodos para su uso en el tratamiento de un trastorno metabolico. Reivindicacion 1: Un compuesto de Formula (1): o una sal, solvato o profármaco farmacéuticamente aceptable de aquel; en donde: A es carbociclilo C3-8, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; E es un enlace, alquenileno C2-6, alquinileno C2-6, arileno, heteroarileno, carbociclileno, heterociclileno; con la condicion de que E no es 4-oxo-imidazolidinileno; L3 es un enlace, -C(O)-, -C(O)O-, -OC(O)-, -C(O)NR1a-, -NR1aC(O)-, -O-, -OC(O)O-, -OC(O)NR1a-, -NR1aC(O)O-, -OS(O)-, -S(O)O-, -OS(O)2-, -S(O)2O-, -OS(O)NR1a-, -NR1aS(O)O-, -OS(O)2NR1a-, -NR1aS(O)2O-, -NR1a-, -NR1aC(O)NR1d-, -NR1aS(O)NR1d-, -NR1aS(O)2NR1d-, -S-, -S(O)-, -S(O)2-, -S(O)NR1a-, -NR1aS(O)-, -S(O)2NR1a- o -NR1aS(O)2-; con las siguientes condiciones: (a) E y L3 no son ambos un enlace al mismo tiempo; y (b) cuando L3-E juntos son -O-, R6 no es yodo ni benzoxi; m es un numero entero de 0, 1, 2, 3 o 4; L1 es un bioisostero de carboxilato seleccionado del grupo integrado por -CH2OH, -CONH2, -CO2H, -P(O)(OH)2, -P(OH)2, tetrazolilo o 3-hidroxiisoxazolilo; L2 es -CH2N(R5)-, -N(R5)CH2-, -N(R5)-, -O-, -S-, -C(O)NR5-, -NR5C(O)-, -CH2C(O)NR5-, -NR5C(O)CH2-, -CH=CH-C(O)NR5-, -NR5C(O)-CH=CH-, -C:::C-C(O)NR5-, -NR5C(O)-C:::C-, -S(O)NR5-, -NR5S(O)-, S(O)2NR5-, -NR5S(O)2-, -NR5C(O)NR5a-, -NR5S(O)2NR5a-, -CH2NR5S(O)2NR5a-, -NR5S(O)2NR5aCH2-, -NR5C(O)-alquileno, -NR5S(O)-alquileno, -NR5S(O)2-alquiIeno, -NR5C(O)-alquenileno, -NR5S(O)-alquenileno o -NR5S(O)2-alquenilerio; o alternativamente, L2 y V o W, junto con otros átomos a los cuales están unidos, forman carbociclilo o heterociclilo de 5 a 8 miembros opcionalmente sustituido; o alternativamente, V o W y el átomo de carbono que está unido a R3, L1, y L2, junto con otros átomos a los cuales están unidos, forman carbociclilo o heterociclilo de 5 a 8 miembros opcionalmente sustituido; U, y, W, X e Y son cada uno independientemente C, CH o N; y U, V, W, X e Y, junto con el átomo de carbono al cual V y W están unidos, forman un anillo aromático de 6 miembros; con la condicion de que como máximo tres de U, V, W, X e Y son N o NH; R1, R2, y R3 se seleccionan entre (i), (ii), (iii), y (iv): (i) R1, R2, y R3 son cada uno independientemente (a) hidrogeno, halo o ciano; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-8, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (c) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OR1a, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1cR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -SR1a, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c o -S(O)2NR1bR1c; (ii) R1 o R2 forman un doble enlace con R3 y el otro de R1 y R2 se selecciona igual que en el punto (i); (iii) dos de R1, R2, y R3 se unen para formar carbociclilo C3-8 o heterociclilo de 3 a 8 miembros; y el tercero se selecciona igual que en el punto (i); y (iv) R3 y V o W, junto con los otros átomos a los cuales están unidos, forman carbociclilo C5-8 o heterociclilo de 5 a 8 miembros; y R1 y R2 se seleccionan igual que en el punto (i); R4 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o alternativamente, R4 y R5 junto con el átomo de N al cual están unidos forman heterociclilo; R5 y R5a son cada uno independientemente hidrogeno, alquilo C1-6, -C(O)-alquilo C1-6; alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o alternativamente, R4 y R5 se unen para formar heterociclilo; R6 es ciano, halo, azido, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo, heterociclilo, -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OR1a, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -SR1a, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c o -S(O)2NR1bR1c; cuando U, V, W, X e Y son cada uno independientemente C o CH; R1, R2, y R3 son hidrogeno; L1 es -CONH2 o -CO2H; L2 es -NR5C(O)-; y R4 es -heteroaril-arilo; entonces A-L3-E- es grupo ciano; cada R1a, R1b, R1c, y R1d es independientemente hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o R1a y R1c junto con los átomos de C y N a los cuales están unidos forman heterociclilo; o R1b y R1c junto con el átomo de N al cual están unidos forman heterociclilo; en donde cada alquilo, alquenilo, alquenileno, alquinilo, alquinileno, carbociclilo, carbociclileno, arilo, arileno, aralquilo, heteroarilo, heteroarileno, heterociclilo, y heterociclileno, en R1, R2, R3, R4, R5, R5a, R6, R1a, R1b, R1c, R1d, A, y E están opcionalmente sustituidos con uno o varios sustituyentes Q, donde cada Q se selecciona independientemente entre: (a) ciano, halo, azido y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo, cada uno de los cuales está a su vez opcionalmente sustituido con uno o varios, en una forma de realizacion uno, dos, tres o cuatro, sustituyentes Qa; y (c) -C(O)Ra, -C(O)ORa, -C(O)NRbRc, -C(NRa)NRbRc, -ORa, -OC(O)Ra, -OC(O)ORa, -OC(O)NRbRc, -OC(=NRa)NRbRc, -OS(O)Ra, -OS(O)2Ra, -OS(O)NRbRc, -OS(O)2NRbRc, -NRbRc, -NRaC(O)Rd, -NRaC(O)ORd, -NRaC(O)NRbRc, -NRaC(=NRd)NRbRc, -NRaS(O)Rd, -NRaS(O)2Rd, -NRaS(O)NRbRc, -NRaS(O)2NRbRc, -SRa, -S(O)Ra, -S(O)2Ra, -S(O)NRbRc, y -S(O)2NRbRc, en donde cada Ra, Rb, Rc, y Rd es independientemente (i) hidrogeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno o varios, en una forma de realizacion uno, dos, tres o cuatro, sustituyentes Qa; o (iii) Rb y Rc junto con el átomo de N al cual están unidos forman heterociclilo, opcionalmente sustituido con uno o varios, en una forma de realizacion uno, dos, tres o cuatro, sustituyentes Qa; y en donde cada Qa es independientemente seleccionado del grupo integrado por (a) ciano, halo, y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo; y (c) -C(O)R6, -C(O)ORe, -C(O)NRfRg, -C(NRe)NRfRg, -ORe, -OC(O)Re, -OC(O)ORe, -OC(O)NRfRg, -OC(=NRe)NRfRg, -OS(O)Re, -OS(O)2Re, -OS(O)NRfRg, -OS(O)2NRfRg, -NRfRg, -NReC(O)Rh, -NReC(O)ORf, -NReC(O)NRfRg, -NReC(=NRh)NRfRg, -NReS(O)Rh, -NReS(O)2Rh, -NReS(O)NRfRg, -NReS(O)2NRfRg, -SRe, -S(O)Re, -S(O)2Re, -S(O)NRfRg, y -S(O)2NRfRg; en donde cada Re, Rf, Rg, y Rh es independientemente (i) hidrogeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (iii) Rf y Rg junto con el átomo de N al cual están unidos forman heterociclilo.
ARP110100351A 2010-02-02 2011-02-02 Derivados de fenilalanina y su uso como moduladores de los receptores del glp-1 no peptidicos AR080112A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2010/000141 WO2011094890A1 (en) 2010-02-02 2010-02-02 Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators

Publications (1)

Publication Number Publication Date
AR080112A1 true AR080112A1 (es) 2012-03-14

Family

ID=44354851

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100351A AR080112A1 (es) 2010-02-02 2011-02-02 Derivados de fenilalanina y su uso como moduladores de los receptores del glp-1 no peptidicos

Country Status (6)

Country Link
US (1) US8748412B2 (es)
EP (1) EP2531198A4 (es)
JP (2) JP2013518888A (es)
AR (1) AR080112A1 (es)
CA (1) CA2788782A1 (es)
WO (2) WO2011094890A1 (es)

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP2240451B1 (en) 2008-01-04 2017-08-09 Intellikine, LLC Isoquinolinone derivatives substituted with a purine useful as PI3K inhibitors
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
MX2012012204A (es) 2010-04-22 2012-12-05 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
US8501982B2 (en) 2010-06-09 2013-08-06 Receptos, Inc. GLP-1 receptor stabilizers and modulators
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
AR084824A1 (es) 2011-01-10 2013-06-26 Intellikine Inc Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas
HK1207853A1 (en) * 2011-04-08 2016-02-12 卡尔丹治疗有限公司 Ortho-fluoro substituted compounds for the treatment of metabolic diseases
ES2634716T3 (es) 2011-05-31 2017-09-28 Celgene International Ii Sàrl Nuevos estabilizantes y moduladores del receptor GLP-1
WO2012177896A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
BR112013033316A2 (pt) 2011-06-24 2017-01-31 Amgen Inc antagonista de trpm8 e seu uso em tratamentos
AU2012278976B2 (en) 2011-07-06 2017-05-11 Gilead Sciences, Inc. Compounds for the treatment of HIV
WO2013025733A1 (en) 2011-08-15 2013-02-21 Intermune, Inc. Lysophosphatidic acid receptor antagonists
US8541577B2 (en) * 2011-11-10 2013-09-24 Allergan, Inc. Aryl urea derivatives as N-formyl peptide receptors like-1 (FPRL-1) receptor modulators
CN103917529B (zh) 2011-11-11 2016-08-17 辉瑞大药厂 2-硫代嘧啶酮类
JP6061949B2 (ja) * 2011-12-12 2017-01-18 レセプトス エルエルシー 糖尿病などの疾患の治療のためのｇｌｐ−１受容体モジュレーターとして作用する４つの環を含むカルボン酸誘導体
US8633182B2 (en) 2012-05-30 2014-01-21 Boehringer Ingelheim International Gmbh Indanyloxyphenylcyclopropanecarboxylic acids
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI706945B (zh) 2013-03-01 2020-10-11 美商基利科學股份有限公司 供治療反轉錄病毒科病毒感染之治療性化合物
CA2905726C (en) 2013-03-14 2022-05-31 Janssen Pharmaceutica Nv Gpr120 agonists for the treatment of type ii diabetes
SG10201709565QA (en) 2013-03-14 2017-12-28 Janssen Pharmaceutica Nv Benzo-fused heterocyclic derivatives useful as agonists of gpr120
JP6333355B2 (ja) 2013-03-14 2018-05-30 ヤンセン ファーマシューティカ エヌ．ベー． Ｇｐｒ１２０のアゴニストとして有用な二環式ピロール誘導体
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
CN109867630A (zh) 2013-06-11 2019-06-11 赛尔基因第二国际有限公司 新型glp-1受体调节剂
BR112016014180A2 (pt) 2013-12-18 2017-09-26 Astex Therapeutics Ltd reguladores de nrf2
US10202353B2 (en) 2014-02-28 2019-02-12 Gilead Sciences, Inc. Therapeutic compounds
US8912227B1 (en) 2014-03-07 2014-12-16 Janssen Pharmaceutica Nv Bicyclic pyrrole derivatives useful as agonists of GPR120
EP3114111B1 (en) * 2014-03-07 2019-01-09 Janssen Pharmaceutica NV Bicyclic pyrrole derivatives useful as agonists of gpr120
US9067898B1 (en) 2014-03-07 2015-06-30 Janssen Pharmaceutica Nv Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
DK3925607T3 (da) 2014-04-15 2023-08-21 Vertex Pharma Farmaceutiske sammensætninger til behandlingen af cystisk fibrosetransmembrankonduktansregulator-medierede sygdomme
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
EP3172199B1 (en) 2014-07-25 2020-07-01 Celgene International II Sarl Pyrimidine derivatives as glp-1 receptor modulators
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3230276B1 (en) 2014-12-10 2020-09-02 Celgene International II Sarl Glp-1 receptor modulators
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MA42035A (fr) 2015-05-05 2018-03-14 Pfizer 2-thiopyrimidinones
EP3766878B1 (en) 2015-06-15 2022-03-16 GlaxoSmithKline Intellectual Property Development Limited Nrf2 regulators
CA2988338C (en) 2015-06-15 2024-05-14 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
EP3359532A1 (en) 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
MX384569B (es) 2016-01-15 2025-03-14 Pfizer Ligandos d3 de dopamina 6,7,8,9-tetrahidro-5h-pirido[2,3-d]azepina
CN109640999A (zh) 2016-06-24 2019-04-16 无限药品股份有限公司 组合疗法
PL3347352T3 (pl) 2016-08-19 2019-12-31 Gilead Sciences, Inc. Związki terapeutyczne użyteczne do profilaktycznego lub terapeutycznego leczenia zakażenia wirusem HIV
EP3512839A4 (en) 2016-09-18 2020-03-25 H. Lee Moffitt Cancer Center And Research Institute, Inc. YAP1 INHIBITORS TARGETING THE INTERACTION OF YAP1 WITH OCT4
CN110088089B (zh) 2016-10-25 2023-08-29 勃林格殷格翰国际有限公司 苄基氨基吡啶基环丙烷甲酸、药物组合物及其用途
CN110312706B (zh) 2016-11-28 2023-08-18 勃林格殷格翰国际有限公司 茚满基氨基吡啶基环丙烷甲酸、其药物组合物及用途
WO2018138028A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
CN110312714B (zh) 2017-01-26 2022-12-09 勃林格殷格翰国际有限公司 苄基氧基吡嗪基环丙烷甲酸、其药物组合物和用途
CN110214135B (zh) 2017-01-26 2023-02-21 勃林格殷格翰国际有限公司 茚满基氨基吡嗪基环丙烷羧酸、药物组合物及其用途
JP7050791B2 (ja) 2017-01-26 2022-04-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンジルオキシピリジルシクロプロパンカルボン酸、その医薬組成物及び使用
WO2018138027A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceuticalcompositions and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
AR112413A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas sólidas de un inhibidor de la cápside del vih
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
US10836746B2 (en) 2018-02-15 2020-11-17 Gilead Sciences, Inc. Therapeutic compounds
JP7038843B2 (ja) 2018-02-16 2022-03-18 ギリアード サイエンシーズ， インコーポレイテッド Ｒｅｔｒｏｖｉｒｉｄａｅウイルス感染の処置において有用な治療用化合物を調製するための方法および中間体
EA202092174A1 (ru) 2018-03-14 2021-01-15 Х. Ли Моффитт Кэнсер Сентер Энд Рисерч Инститьют, Инк. Ингибиторы yap1, которые нацелены на взаимодействие yap1 с oct4
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
KR20230141905A (ko) 2018-07-16 2023-10-10 길리애드 사이언시즈, 인코포레이티드 Hiv의 치료를 위한 캡시드 억제제
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
IL282545B2 (en) 2018-10-30 2025-04-01 Gilead Sciences Inc Quinoline derivatives as alpha4beta7 integrin inhibitors
KR102641718B1 (ko) 2018-10-30 2024-02-29 길리애드 사이언시즈, 인코포레이티드 알파4베타7 인테그린 억제제로서의 이미다조피리딘 유도체
CA3115830C (en) 2018-10-30 2023-09-12 Gilead Sciences, Inc. Compounds for inhibition of .alpha.4.beta.7 integrin
WO2020092383A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR102908219B1 (ko) 2019-08-14 2026-01-08 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021108544A1 (en) 2019-11-26 2021-06-03 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN118598916A (zh) 2020-02-18 2024-09-06 吉利德科学公司 抗病毒化合物
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
KR20230035031A (ko) 2020-06-05 2023-03-10 킨네이트 바이오파마 인크. 섬유아세포 성장 인자 수용체 키나아제의 억제제
CA3181690A1 (en) 2020-06-25 2021-12-30 Chienhung CHOU Capsid inhibitors for the treatment of hiv
JP7588224B2 (ja) 2020-10-05 2024-11-21 エンライブン インコーポレイテッド Ｂｃｒ－ａｂｌチロシンキナーゼの阻害のための５－及び６－アザインドール化合物
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
CN117120444A (zh) 2021-04-16 2023-11-24 吉利德科学公司 使用酰胺制备卡巴核苷的方法
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
JP7719954B2 (ja) 2021-08-18 2025-08-06 ギリアード サイエンシーズ， インコーポレイテッド リン脂質化合物並びにその製造方法及び使用方法
CN118369316A (zh) 2021-12-03 2024-07-19 吉利德科学公司 Hiv病毒感染的治疗性化合物
PL4445900T3 (pl) 2021-12-03 2025-09-22 Gilead Sciences, Inc. Związki terapeutyczne przeciwko zakażeniu wirusem hiv
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
WO2025057134A2 (en) 2023-09-14 2025-03-20 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
IT1062206B (it) * 1974-02-01 1983-09-20 Rotta Research Lab S P A A S Derivati della tirosina attivi sulla muscolatura liscia
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
KR890002631B1 (ko) 1984-10-04 1989-07-21 몬산토 캄파니 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5585112A (en) 1989-12-22 1996-12-17 Imarx Pharmaceutical Corp. Method of preparing gas and gaseous precursor-filled microspheres
IT1246382B (it) 1990-04-17 1994-11-18 Eurand Int Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US6274552B1 (en) 1993-03-18 2001-08-14 Cytimmune Sciences, Inc. Composition and method for delivery of biologically-active factors
US5523092A (en) 1993-04-14 1996-06-04 Emory University Device for local drug delivery and methods for using the same
US5985307A (en) 1993-04-14 1999-11-16 Emory University Device and method for non-occlusive localized drug delivery
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6004534A (en) 1993-07-23 1999-12-21 Massachusetts Institute Of Technology Targeted polymerized liposomes for improved drug delivery
US5958458A (en) 1994-06-15 1999-09-28 Dumex-Alpharma A/S Pharmaceutical multiple unit particulate formulation in the form of coated cores
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5759542A (en) 1994-08-05 1998-06-02 New England Deaconess Hospital Corporation Compositions and methods for the delivery of drugs by platelets for the treatment of cardiovascular and other diseases
US5660854A (en) 1994-11-28 1997-08-26 Haynes; Duncan H Drug releasing surgical implant or dressing material
US6316652B1 (en) 1995-06-06 2001-11-13 Kosta Steliou Drug mitochondrial targeting agents
DE69632684T2 (de) 1995-06-27 2005-06-09 Takeda Pharmaceutical Co. Ltd. Verfahren zur herstellung von zubereitungen mit verzögerter freisetzung
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US6039975A (en) 1995-10-17 2000-03-21 Hoffman-La Roche Inc. Colon targeted delivery system
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
TW345603B (en) 1996-05-29 1998-11-21 Gmundner Fertigteile Gmbh A noise control device for tracks
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
US6375987B1 (en) 1996-10-01 2002-04-23 Gattefossé, S.A. Process for the manufacture of pharmaceutical composition with modified release of active principle comprising the matrix
US6139865A (en) 1996-10-01 2000-10-31 Eurand America, Inc. Taste-masked microcapsule compositions and methods of manufacture
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
ATE272394T1 (de) 1996-10-31 2004-08-15 Takeda Chemical Industries Ltd Zubereitung mit verzögerter freisetzung
US6131570A (en) 1998-06-30 2000-10-17 Aradigm Corporation Temperature controlling device for aerosol drug delivery
DE19648576C2 (de) 1996-11-23 1999-08-12 Lohmann Therapie Syst Lts Lutschtablette zur modifizierten Freisetzung von Wirkstoffen im Gastrointestinaltrakt
ZA9711385B (en) 1996-12-20 1999-06-18 Takeda Chemical Industries Ltd Method of producing a sustained-release preparation
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
US6120751A (en) 1997-03-21 2000-09-19 Imarx Pharmaceutical Corp. Charged lipids and uses for the same
US6060082A (en) 1997-04-18 2000-05-09 Massachusetts Institute Of Technology Polymerized liposomes targeted to M cells and useful for oral or mucosal drug delivery
JP2002501518A (ja) * 1997-05-30 2002-01-15 セルテック セラピューティックス リミテッド 抗炎症性チロシン誘導体
ATE249421T1 (de) * 1997-06-23 2003-09-15 Tanabe Seiyaku Co Inhibitoren der alpha4-beta1 vermittelten zelladhäsion
DE69824183T2 (de) 1997-08-22 2005-04-21 Hoffmann La Roche N-alkanoylphenylalaninderivate
US6191171B1 (en) * 1997-11-20 2001-02-20 Merck & Co., Inc. Para-aminomethylaryl carboxamide derivatives
WO1999029640A2 (en) * 1997-12-05 1999-06-17 Eisai Co., Ltd. Compositions and methods for modulating the activity of fibroblast growth factor
US6197794B1 (en) * 1998-01-08 2001-03-06 Celltech Therapeutics Limited Phenylalanine derivatives
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6048736A (en) 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
US7169410B1 (en) 1998-05-19 2007-01-30 Sdg, Inc. Targeted liposomal drug delivery system
CN100444830C (zh) 1998-11-02 2008-12-24 伊兰公司，Plc 多颗粒改进释放组合物
JP2003524614A (ja) * 1998-12-22 2003-08-19 田辺製薬株式会社 α４β１媒介細胞接着のインヒビター
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
KR20020060067A (ko) 1999-04-06 2002-07-16 가와무라 요시부미 α-치환 카르복실산 유도체
US6271359B1 (en) 1999-04-14 2001-08-07 Musc Foundation For Research Development Tissue-specific and pathogen-specific toxic agents and ribozymes
WO2001036376A1 (en) * 1999-11-18 2001-05-25 Ajinomoto Co., Inc. Novel phenylalanine derivatives
US6623756B1 (en) 2000-04-27 2003-09-23 Noveon Ip Holdings Corp. Directly compressed solid dosage articles
US6960597B2 (en) * 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
ATE345127T1 (de) * 2000-09-29 2006-12-15 Ajinomoto Kk Neue phenylalanin-derivate
DE60237826D1 (de) 2001-07-27 2010-11-11 Astellas Pharma Inc Zusammensetzung enthaltend feine Körner mit verzögerter Freisetzung für in der Mundhöhle schnell zerfallende Tabletten
CA2461653A1 (en) 2001-09-28 2003-04-03 Mcneil-Ppc, Inc. Edible composition and dosage form comprising an edible shell
WO2003051340A1 (en) 2001-12-19 2003-06-26 Astrazeneca Ab New film coating
ATE464299T1 (de) * 2002-02-20 2010-04-15 Ajinomoto Kk Neues phenylalaninderivat
US6958161B2 (en) 2002-04-12 2005-10-25 F H Faulding & Co Limited Modified release coated drug preparation
US7485322B2 (en) 2002-12-24 2009-02-03 Lek Pharmaceuticals D.D. Modified release pharmaceutical composition
WO2005056536A1 (en) * 2003-12-10 2005-06-23 Ranbaxy Laboratories Limited Antidiabetic agents which exhibit activity against ppar
RU2390520C2 (ru) * 2003-12-22 2010-05-27 Адзиномото Ко., Инк. Новые производные фенилаланина
BRPI0507574A (pt) * 2004-02-10 2007-07-03 Janssen Pharmaceutica Nv piridazinonas como antagonistas de alfa 4 integrinas
WO2007060408A2 (en) * 2005-11-23 2007-05-31 Astrazeneca Ab L-phenylalanine derivatives and their use as integrin antagonists
US7427414B2 (en) 2006-01-18 2008-09-23 Astron Research Limited Modified release oral dosage form using co-polymer of polyvinyl acetate
US20080200454A1 (en) * 2007-02-15 2008-08-21 Ameriks Michael K Carbon-linked tetrahydro-pyrazolo-pyridine modulators of cathepsin s
BRPI0813105A2 (pt) * 2007-06-20 2015-08-04 Mitsubishi Tanabe Pharma Corp Derivado de sulfonamida de ácido malônico e uso faramacêutico do mesmo

Also Published As

Publication number Publication date
EP2531198A4 (en) 2013-06-12
JP2016166182A (ja) 2016-09-15
US8748412B2 (en) 2014-06-10
US20120004198A1 (en) 2012-01-05
WO2011097300A1 (en) 2011-08-11
WO2011094890A1 (en) 2011-08-11
CA2788782A1 (en) 2011-08-11
EP2531198A1 (en) 2012-12-12
JP2013518888A (ja) 2013-05-23

Similar Documents

Publication Publication Date Title
AR080112A1 (es) Derivados de fenilalanina y su uso como moduladores de los receptores del glp-1 no peptidicos
AR080945A1 (es) Pirimidinil y 1,3,5-triazinil benzimidazoles y su uso en la terapia contra el cancer
CY1120342T1 (el) Ανταγωνιστης πολυκυκλικου lpa1 και χρησεις εξ' αυτου
AR075974A1 (es) Pirimidinil y 1,3,5-triazinilbencimidazolsulfonamidas y su uso en terapia del cancer
CY1122624T1 (el) Θεραπεια συνδυασμου του καρκινου
ES2351528T3 (es) Agonistas de orl 1/mi mixtos para el tratamiento del dolor.
AR093038A1 (es) Conjugados de suministro de farmacos que contienen aminoacidos no naturales y metodos para usarlos, composicion y uso
ECSP15039103A (es) Formulación de liberación sostenida de mosapride que proporciona efectos farmacológicos y clínicos con administración una vez al día
BR112022009209A2 (pt) Derivado de amida e método de preparação e uso do mesmo na medicina
NI201500160A (es) Derivados 11-hidroxilo de ácidos biliares y conjugados de aminoácidos de los mismos como moduladores del receptor de farnesoid x
SI2935307T1 (en) Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures
WO2011160136A3 (en) Progesterone containing oral dosage forms and related methods
BRPI0514180A (pt) composto, composição farmacêutica, uso de um composto, kit farmaceuticamente útil adaptado para administração oral diária, e, métodos de preparação de um composto, e de contracepção em um mamìfero
AR087211A1 (es) ANTAGONISTAS DE CRTh2
RU2013109137A (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 ДЛЯ ЛЕЧЕНИЯ НОЦИЦЕПТИВНОЙ БОЛИ
RU2013121788A (ru) Ингибиторы репликации вич
JP2015504871A5 (es)
AR079528A1 (es) Inhibidores de arileno o heteroarileno 5,5-fusionado del virus de la hepatitis c
ECSP077424A (es) Derivados de quinuclidina y su uso como antagonistas del receptor muscarínico m3
UA106636C2 (uk) Морфолінотіазоли як позитивні алостеричні модулятори альфа 7
CA2671904A1 (en) Intermediate duration neuromuscular blocking agents and antagonists thereof
AR100935A1 (es) CONJUGADOS DE FÁRMACO-ANTICUERPO ANTI-RECEPTOR DE FOLATO a (FRA) Y MÉTODOS DE USO DE LOS MISMOS
MX2019002915A (es) Derivado de ?-aminoacido triciclico fusionado, metodo de preparacion, y su uso medico del mismo.
CY1117118T1 (el) Φαρμακευτικος συνδυασμος για την αγωγη του πονου
CY1114163T1 (el) Μεθοδοι χρησεως ανταγωνιστων αγγειοπιεσινης με παραγοντες χημειοθεραπειας ανθρακυκλινης για να μειωνεται καρδιοτοξικοτητα ή/και να βελτιωνεται επιβιωση

Legal Events

Date Code Title Description
FC Refusal