[go: up one dir, main page]

PE20200834A1 - Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas - Google Patents

Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas

Info

Publication number
PE20200834A1
PE20200834A1 PE2020000174A PE2020000174A PE20200834A1 PE 20200834 A1 PE20200834 A1 PE 20200834A1 PE 2020000174 A PE2020000174 A PE 2020000174A PE 2020000174 A PE2020000174 A PE 2020000174A PE 20200834 A1 PE20200834 A1 PE 20200834A1
Authority
PE
Peru
Prior art keywords
alkyl
modulators
alkenyl
initiation factor
pentane
Prior art date
Application number
PE2020000174A
Other languages
English (en)
Inventor
Robert A Ii Craig
Anthony A Estrada
Jianwen A Feng
Brian Fox
Christopher R H Hale
Katrina W Lexa
Maksim Osipov
Travis Remarchuk
Zachary K Sweeney
Vicente Fidalgo Javier De
Original Assignee
Denali Therapeutics 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 Denali Therapeutics Inc filed Critical Denali Therapeutics Inc
Publication of PE20200834A1 publication Critical patent/PE20200834A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/14—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic 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
    • A61K31/4164—1,3-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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—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 two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/38—2-Pyrrolones
    • 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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D233/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/36—One oxygen atom with hydrocarbon radicals, substituted by nitrogen atoms, attached to ring nitrogen atoms
    • 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
    • C07D233/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • 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
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
    • 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
    • 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
    • C07D263/34—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 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
    • C07D263/36—One oxygen atom
    • C07D263/38—One oxygen atom attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • 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
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
    • C07D291/02—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms not condensed with other rings
    • C07D291/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—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
    • C07D403/12—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
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings 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
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/38—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing five carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable, un analogo isotopicamente enriquecido, una mezcla de estereoisomeros o profarmaco de este; en donde: L es heteroalquileno opcionalmente sustituido con 1 a 6 R10 o heterociclilo opcionalmente sustituido, entre otros; x es 1 o 2; z es 0 o 1; X1 es O, NR9 o un enlace; R1 es H, alquilo C1-12, alquenilo C2-12, entre otros; R2 es H, alquilo C1-12, alquenilo C2-12, entre otros; R3 H, alquilo C1-12, alquenilo C2-12, entre otros; cada R4 y R5 es independientemente H, alquilo C1-12, alquenilo C2-12, entre otros; cada R10 es independientemente halo, alquilo C1-12 o haloalquilo C1-12; y es 1, 2, 3, 4, 5, 6, 7 o 8. Estos compuestos son moduladores del factor de iniciacion eucariota 2B, en donde se utiliza para tratar una enfermedad o afeccion neurodegenerativa, tal como enfermedad de Alper, Alzheimer, Parkinson, entre otros. Tambien se refiere a compuestos intermedios y a metodos de preparacion de dichos compuestos.
PE2020000174A 2017-08-09 2018-08-08 Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas PE20200834A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762543307P 2017-08-09 2017-08-09
US201762553728P 2017-09-01 2017-09-01
US201762608504P 2017-12-20 2017-12-20
PCT/US2018/045868 WO2019032743A1 (en) 2017-08-09 2018-08-08 COMPOUNDS, COMPOSITIONS AND METHODS

Publications (1)

Publication Number Publication Date
PE20200834A1 true PE20200834A1 (es) 2020-08-13

Family

ID=65272557

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020000174A PE20200834A1 (es) 2017-08-09 2018-08-08 Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas

Country Status (20)

Country Link
US (3) US11236100B2 (es)
EP (1) EP3665156A4 (es)
JP (3) JP2020530446A (es)
KR (2) KR20250017299A (es)
CN (3) CN118239937A (es)
AU (3) AU2018313850B2 (es)
CA (1) CA3071024A1 (es)
CL (1) CL2020000299A1 (es)
CO (1) CO2020001220A2 (es)
CR (1) CR20200054A (es)
IL (2) IL301709B2 (es)
MA (1) MA49858A (es)
MX (2) MX2020001352A (es)
MY (1) MY201438A (es)
PE (1) PE20200834A1 (es)
PH (1) PH12020550028B1 (es)
SA (1) SA520411222B1 (es)
SG (1) SG11202000532SA (es)
TW (1) TW201920115A (es)
WO (1) WO2019032743A1 (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110730777A (zh) * 2017-06-07 2020-01-24 葛兰素史密斯克莱知识产权发展有限公司 作为atf4通路抑制剂的化学化合物
CR20200054A (es) 2017-08-09 2020-03-21 Denali Therapeutics Inc Compuestos, composiciones y métodos
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
MX2020004557A (es) 2017-11-02 2020-10-05 Calico Life Sciences Llc Moduladores de la vía de estrés integrada.
CN111757739A (zh) 2017-12-13 2020-10-09 普拉西斯生物技术有限责任公司 整合应激反应路径抑制剂
SG11202011014VA (en) 2018-06-05 2020-12-30 Praxis Biotech LLC Inhibitors of integrated stress response pathway
TWI832295B (zh) 2018-10-11 2024-02-11 美商嘉來克生命科學有限責任公司 整合應激路徑之前藥調節劑
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
TWI877136B (zh) 2019-02-13 2025-03-21 美商戴納立製藥公司 化合物、組合物及方法
US12091392B2 (en) 2019-02-13 2024-09-17 Denali Therapeutics Inc. Compounds, compositions and methods
PE20220961A1 (es) 2019-04-23 2022-06-10 Evotec Int Gmbh Moduladores de la via de respuesta integrada al estres
BR112021020106A2 (pt) 2019-04-23 2021-12-07 Evotec Int Gmbh Moduladores da via de resposta ao estresse inte-grado
US20200347043A1 (en) * 2019-04-30 2020-11-05 Calico Life Sciences Llc Modulators of the integrated stress pathway
CA3142748A1 (en) 2019-06-12 2020-12-17 Praxis Biotech LLC Modulators of integrated stress response pathway
CA3162526A1 (en) 2020-01-28 2021-08-05 Christopher John Brown Modulators of the integrated stress response pathway
MX2022011143A (es) 2020-03-11 2022-10-13 Evotec Int Gmbh Moduladores de la via de respuesta integrada al estres.
MX2023004623A (es) 2020-10-22 2023-05-12 Evotec Int Gmbh Moduladores de la via integrada de respuesta al estres.
US20230391725A1 (en) 2020-10-22 2023-12-07 Evotec International Gmbh Modulators of the integrated stress response pathway
KR20230110510A (ko) 2020-10-22 2023-07-24 에보텍 인터내셔널 게엠베하 통합 스트레스 반응 경로의 조절제
TW202233580A (zh) * 2020-10-30 2022-09-01 美商嘉來克生命科學有限責任公司 整合應激路徑之調節劑
CN116507608A (zh) * 2020-11-20 2023-07-28 戴纳立制药公司 化合物、组合物和方法
CN116323620A (zh) * 2020-11-25 2023-06-23 豪夫迈·罗氏有限公司 用于治疗和预防乙型肝炎病毒感染的芳香族桥环酰胺衍生物
TW202241857A (zh) * 2020-12-18 2022-11-01 美商戴納立製藥公司 化合物之固體形式
CN119630634A (zh) * 2022-06-23 2025-03-14 戴纳立制药公司 用于制备真核起始因子2b的调节剂的方法
JP2025539152A (ja) * 2022-11-21 2025-12-03 シェンチェン チョンゲ バイオロジカル テクノロジー カンパニー リミテッド 化合物、それを含む医薬組成物及びその合成方法と使用
WO2025019827A1 (en) * 2023-07-20 2025-01-23 Denali Therapeutics Inc. Formulation, solid dosage form, and methods
WO2025230528A1 (en) * 2024-05-01 2025-11-06 Calico Life Sciences Llc Methods of treating amyotrophic lateral sclerosis
WO2026004939A1 (ja) * 2024-06-28 2026-01-02 キッセイ薬品工業株式会社 ジ置換ビシクロ［１．１．１］ペンタン化合物

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6429207B1 (en) 1997-11-21 2002-08-06 Nps Pharmaceuticals, Inc. Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
AU762345B2 (en) 1998-10-16 2003-06-26 Asubio Pharma Co., Ltd. Aminophenoxyacetic acid derivatives as neuroprotectants
AR024077A1 (es) 1999-05-25 2002-09-04 Smithkline Beecham Corp Compuestos antibacterianos
US20010047100A1 (en) 2000-04-26 2001-11-29 Kjaersgaard Hans Joergen Chiral imidazoyl intermediates for the synthesis of 2-(4-imidazoyl)-cyclopropyl derivatives
CA2443108A1 (en) 2001-04-03 2002-10-17 Merck & Co. Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
MX2007002582A (es) 2004-09-02 2008-01-14 Vertex Pharma Quinazolinas utiles como moduladores de canales ionicos.
CN101258157A (zh) 2005-05-24 2008-09-03 阿斯利康(瑞典)有限公司 具有抗菌活性的氨基哌啶喹啉及其氮杂等构类似物
CA2634743C (en) 2005-12-23 2014-07-29 Zealand Pharma A/S Modified lysine-mimetic compounds
CA2666482A1 (en) 2006-10-20 2008-05-02 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors
CA2689102C (en) 2007-06-15 2016-07-26 Actelion Pharmaceuticals Ltd 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives
MX2011005905A (es) 2008-12-12 2011-06-20 Actelion Pharmaceuticals Ltd Derivados de 5-amino-2-(1-hidroxi-etil)-tetrahidropirano.
US9421211B2 (en) 2009-05-28 2016-08-23 President And Fellows Of Harvard College N,N′-diarylurea compounds and N,N′-diarylthiourea compounds as inhibitors of translation initiation
KR102050712B1 (ko) 2009-06-17 2019-12-02 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제의 억제제
AR084457A1 (es) 2010-12-22 2013-05-15 Lundbeck & Co As H Derivados de biciclo[3,2,1]octilamida
ES2580961T3 (es) 2011-02-24 2016-08-30 Nerviano Medical Sciences S.R.L. Derivados Tiazolilfenil-bencenosulfonamido como Inhibidores de Cinasa
TWI494312B (zh) 2011-03-10 2015-08-01 Daiichi Sankyo Co Ltd 二螺吡咯啶衍生物
RU2625309C2 (ru) 2011-04-22 2017-07-13 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Замещенные диаминокарбоксамидные и диаминокарбонитрильные производные пиримидинов, их композиции и способы лечения с их помощью
WO2013120940A2 (en) 2012-02-14 2013-08-22 Syngenta Participations Ag Novel compounds
KR20150064098A (ko) 2012-10-02 2015-06-10 다이닛본 스미토모 세이야꾸 가부시끼가이샤 이미다졸 유도체
KR102243637B1 (ko) * 2013-03-14 2021-04-26 리커리엄 아이피 홀딩스, 엘엘씨 바이사이클릭 진통 화합물
US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
AU2014233520B2 (en) 2013-03-15 2019-02-21 The Regents Of The University Of California Modulators of the eIF2alpha pathway
US20160318856A1 (en) 2013-09-11 2016-11-03 The Brigham And Women's Hospital, Inc. Substituted Urea eIF2alpha Kinase Activators
ES2702951T3 (es) * 2014-04-04 2019-03-06 Syros Pharmaceuticals Inc Inhibidores de quinasas dependientes de ciclina 7 (cdk7)
CA2961605C (en) 2014-09-17 2023-01-10 Kalyra Pharmaceuticals, Inc. Bicyclic compounds
CN107108561B (zh) * 2014-11-20 2020-08-28 默克专利有限公司 用作irak抑制剂的杂芳基化合物及其用途
EP3623371A1 (en) 2014-12-16 2020-03-18 Axovant Sciences GmbH Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors
EA201791896A1 (ru) 2015-02-25 2018-02-28 Уильям Марш Райс Юниверсити Дезацетокситубулизин н и его аналоги
GB201506894D0 (en) 2015-04-23 2015-06-10 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
BR112017023764A2 (pt) 2015-05-05 2018-07-31 Bayer Pharma AG derivados de ciclohexano substituído por amido
TW201718557A (zh) 2015-10-08 2017-06-01 歌林達有限公司 經吡唑基取代之四氫吡喃基碸
TW202506629A (zh) * 2016-05-05 2025-02-16 美商嘉來克生命科學有限責任公司 整合應激途徑之調節劑
TW201808903A (zh) 2016-05-05 2018-03-16 嘉來克生命科學有限責任公司 整合應激途徑之調節劑
TW201808914A (zh) * 2016-05-05 2018-03-16 嘉來克生命科學有限責任公司 整合應激途徑之調節劑
TW201808888A (zh) * 2016-05-05 2018-03-16 嘉來克生命科學有限責任公司 整合應激途徑之調節劑
US10851053B2 (en) 2016-06-08 2020-12-01 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
EP3468960B1 (en) 2016-06-08 2022-03-23 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds as atf4 pathway inhibitors
WO2018009615A1 (en) * 2016-07-06 2018-01-11 Acquist Llc Compounds and their use for reducing uric acid levels
JOP20190072A1 (ar) 2016-10-13 2019-04-07 Glaxosmithkline Ip Dev Ltd مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم
JP7128816B2 (ja) 2016-12-08 2022-08-31 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム 疾患の治療のための二重ロイシンジッパー（ｄｌｋ）キナーゼのビシクロ［１．１．１］ペンタン阻害剤
WO2018225093A1 (en) 2017-06-07 2018-12-13 Glaxosmithkline Intellectual Property Development Limited Chemical compounds as atf4 pathway inhibitors
CN110730777A (zh) * 2017-06-07 2020-01-24 葛兰素史密斯克莱知识产权发展有限公司 作为atf4通路抑制剂的化学化合物
EP3649108A1 (en) 2017-07-03 2020-05-13 GlaxoSmithKline Intellectual Property Development Limited 2-(4-chlorophenoxy)-n-((1 -(2-(4-chlorophenoxy)ethynazetidin-3-yl)methyl)acetamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases
JP2020525513A (ja) * 2017-07-03 2020-08-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 癌および他の疾患を治療するためのａｔｆ４阻害剤としてのｎ−（３−（２−（４−クロロフェノキシ）アセトアミドビシクロ［１．１．１］ペンタン−１−イル）−２−シクロブタン−１−カルボキサミド誘導体および関連化合物
CR20200054A (es) 2017-08-09 2020-03-21 Denali Therapeutics Inc Compuestos, composiciones y métodos
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
WO2019054430A1 (ja) 2017-09-14 2019-03-21 第一三共株式会社 芳香族複素環を有するアミド化合物
IL274367B2 (en) 2017-11-02 2023-10-01 Calico Life Sciences Llc Combined pressure pathway modulators
EP3704091B1 (en) 2017-11-02 2025-12-31 Calico Life Sciences LLC INTEGRATED STRESS RESPONSE PATH MODULATORS
CA3080964A1 (en) 2017-11-02 2019-05-09 Calico Life Sciences Llc Modulators of the integrated stress pathway
UY37957A (es) 2017-11-02 2019-05-31 Abbvie Inc Moduladores de la vía de estrés integrada
BR112020008827A2 (pt) 2017-11-02 2020-10-20 Calico Life Sciences Llc moduladores da via de estresse integrada
MX2020004557A (es) 2017-11-02 2020-10-05 Calico Life Sciences Llc Moduladores de la vía de estrés integrada.
UY37956A (es) 2017-11-02 2019-05-31 Abbvie Inc Moduladores de la vía de estrés integrada
US20230192712A1 (en) 2017-11-02 2023-06-22 Calico Life Sciences Llc Modulators of the integrated stress pathway
UY37958A (es) 2017-11-02 2019-05-31 Abbvie Inc Moduladores de la vía de estrés integrada
CN111757739A (zh) 2017-12-13 2020-10-09 普拉西斯生物技术有限责任公司 整合应激反应路径抑制剂
EP3768660A1 (en) 2018-03-23 2021-01-27 Denali Therapeutics Inc. Modulators of eukaryotic initiation factor 2
WO2019193541A1 (en) 2018-04-06 2019-10-10 Glaxosmithkline Intellectual Property Development Limited Bicyclic aromatic ring derivatives of formula (i) as atf4 inhibitors
WO2019193540A1 (en) 2018-04-06 2019-10-10 Glaxosmithkline Intellectual Property Development Limited Heteroaryl derivatives of formula (i) as atf4 inhibitors
CA3105942A1 (en) 2018-07-09 2020-01-16 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
WO2020031107A1 (en) 2018-08-08 2020-02-13 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
TWI832295B (zh) 2018-10-11 2024-02-11 美商嘉來克生命科學有限責任公司 整合應激路徑之前藥調節劑
US12091392B2 (en) 2019-02-13 2024-09-17 Denali Therapeutics Inc. Compounds, compositions and methods
TWI877136B (zh) 2019-02-13 2025-03-21 美商戴納立製藥公司 化合物、組合物及方法
US20220177456A1 (en) 2019-03-06 2022-06-09 Denali Therapeutics Inc. Compounds, compositions and methods
US20200347043A1 (en) 2019-04-30 2020-11-05 Calico Life Sciences Llc Modulators of the integrated stress pathway
SG11202111970WA (en) 2019-04-30 2021-11-29 Calico Life Sciences Llc Substituted cyclolakyls as modulators of the integrated stress pathway
TW202241857A (zh) 2020-12-18 2022-11-01 美商戴納立製藥公司 化合物之固體形式

Also Published As

Publication number Publication date
AU2018313850A1 (en) 2020-02-06
CN118239938A (zh) 2024-06-25
TW201920115A (zh) 2019-06-01
CN111094233A (zh) 2020-05-01
MY201438A (en) 2024-02-22
US20250388595A1 (en) 2025-12-25
PH12020550028A1 (en) 2021-02-08
US20220411433A1 (en) 2022-12-29
SA520411222B1 (ar) 2023-12-11
IL301709A (en) 2023-05-01
BR112020001591A2 (pt) 2020-07-21
CN118239937A (zh) 2024-06-25
IL272089B1 (en) 2023-05-01
KR102757890B1 (ko) 2025-01-23
EP3665156A1 (en) 2020-06-17
US11236100B2 (en) 2022-02-01
JP2020530446A (ja) 2020-10-22
CN111094233B (zh) 2024-03-15
KR20200037830A (ko) 2020-04-09
IL301709B1 (en) 2025-03-01
PH12020550028B1 (en) 2024-05-24
EP3665156A4 (en) 2021-04-28
IL272089A (en) 2020-03-31
SG11202000532SA (en) 2020-02-27
AU2018313850B2 (en) 2022-12-22
CL2020000299A1 (es) 2020-07-24
AU2025200658A1 (en) 2025-02-20
IL301709B2 (en) 2025-07-01
US11851440B2 (en) 2023-12-26
AU2023201775A1 (en) 2023-04-20
IL272089B2 (en) 2023-09-01
CR20200054A (es) 2020-03-21
KR20250017299A (ko) 2025-02-04
NZ760919A (en) 2024-02-23
MX2023003989A (es) 2023-04-24
CO2020001220A2 (es) 2020-02-18
JP2023052166A (ja) 2023-04-11
JP2025031810A (ja) 2025-03-07
WO2019032743A1 (en) 2019-02-14
CA3071024A1 (en) 2019-02-14
MA49858A (fr) 2021-04-28
MX2020001352A (es) 2020-03-20
US20210147435A1 (en) 2021-05-20

Similar Documents

Publication Publication Date Title
PE20200834A1 (es) Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas
PE20212023A1 (es) Compuestos, composiciones y metodos
PE20210454A1 (es) Macrociclos como moduladores del regulador de conductancia transmembrana de la fibrosis quistica, composiciones farmaceuticas de estos, su uso en el tratamiento de la fibrosis quistica y procesos para elaborarlos
PE20171341A1 (es) Compuestos de pirazina para el tratamiento de enfermedades infecciosas
PE20181010A1 (es) Derivados de n-[2-(1-benzilpiperidin-4-il)etil]-4-(pirazin-2-il)-piperazina-1-carboxamida y compuestos relacionados como antagonistas del receptor muscarinico 4 (m4) para tratar trastornos neurologicos
PE20210140A1 (es) Moduladores de la proteina reguladora de conductancia transmembrana de la fibrosis quistica y metodos de uso
CL2020001343A1 (es) Nuevos profármacos de catecolamina para uso en el tratamiento de la enfermedad de parkinson.
PE20161443A1 (es) Compuestos
SA518391307B1 (ar) مركبات ومشتقات سبيرو [ إندول -3، 2- بيروليدين h3] أون جديدة على هيئة مثبطات الدقيقة المزدوجة للفأر(1h)2 بي2-53
AR040773A1 (es) Pirazoles utiles como inhibidores de gsk-3
AR094300A1 (es) Derivados de quinolonas
AR036374A1 (es) Pirrolo pirimidinas.
AR100714A1 (es) Derivados de alquilo y arilo de compuestos de 1-oxa-4,9-diazaespiro undecano que tienen actividad multimodal contra el dolor
AR065654A1 (es) 3-ciano-4-(4-tetrahidropiran-fenil)-piridin-2-ona derivados,composiciones farmaceuticas que los contienen,metodo de preparacion de los mismos,y usos para prevenir o tratar trastornos neurologicos y psiquiatricos.
CY1119326T1 (el) Φαινυλο-3-αζα-δικυκλο[3.1.0]εξ-3-υλο-μεθανονες και η χρηση αυτων ως φαρμακο
AR090955A1 (es) Aminas biciclicas c-17 de triterpenoides con actividad inhibidora de la maduracion del vih
PE20240886A1 (es) Compuestos espirociclicos
EA201791802A1 (ru) СШИТЫЕ ДИГИДРО-4H-ПИРАЗОЛО[5,1-c][1,4]ОКСАЗИНИЛОВЫЕ СОЕДИНЕНИЯ И АНАЛОГИ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦНС
SA521430330B1 (ar) Eed و rc2 مشتقات آزولوبيريدين كبيرة الحلقة كمعدلات
AR100713A1 (es) Derivados de amida de compuestos de 1-oxa-4,9-diazaespiro undeceno que tienen actividad multimodal contra el dolor
PE20242071A1 (es) Compuestos moduladores de diacilglicerol quinasa
PE20210183A1 (es) Tiofenocarboxamidas sustituidas y analogos de las mismas
UY36257A (es) “compuestos de imidazopiridazina”.
CY1124708T1 (el) Φαρμακολογικως δραστικα αλικυκλικα υποκατεστημενα παραγωγα πυραζολο[1,5-a] πυριμιδινης
ECSP10010606A (es) Derivados de quinuclidina como antagonistas de receptores muscarinicos m3