[go: up one dir, main page]

PE20170004A1 - Inhibidores de biaril cinasa - Google Patents

Inhibidores de biaril cinasa

Info

Publication number
PE20170004A1
PE20170004A1 PE2016001842A PE2016001842A PE20170004A1 PE 20170004 A1 PE20170004 A1 PE 20170004A1 PE 2016001842 A PE2016001842 A PE 2016001842A PE 2016001842 A PE2016001842 A PE 2016001842A PE 20170004 A1 PE20170004 A1 PE 20170004A1
Authority
PE
Peru
Prior art keywords
hydrogen
amino
methyl
biaril
kinase inhibitors
Prior art date
Application number
PE2016001842A
Other languages
English (en)
Inventor
John E Macor
Carolyn Diane Dzierba
Guanglin Luo
Ling Chen
Jonathan L Ditta
Joanne J Bronson
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20170004A1 publication Critical patent/PE20170004A1/es

Links

Classifications

    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • 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
    • C07C233/16—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 singly-bound oxygen atoms
    • C07C233/24—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 singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/25—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 singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur atoms
    • C07D213/34—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/57—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three 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
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/18—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member containing only hydrogen and carbon atoms in addition to the ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/20—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hydrogen atoms and substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D309/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—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 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
    • C07D413/10—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se refiere a un compuesto de formula I, donde: A es piridina, piridazina, entre otros; B es fenilo, piridina, entre otros; R1 es hidrogeno, amino, -CO2H, entre otros; R2 es hidrogeno, ciano, -CH2OH, halo y metilo; R3 es hidrogeno, ciano, ciclopropilo, entre otros; R4 es hidrogeno, halo y metilo; R5 es 3-(2-metilpropil)-azetidin-metil-oxo-; 2,4-dimetilpentan-2-ol-oxo-; entre otros. Son compuestos preferidos: (S)-N-(4-(4-((2-amino-4-metilpentil)oxi)-3-fluorofenil)piridin-2-il)acetamida; (S)-N-(4-(4-((2-amino-4-metilpentil)oxi)-3-metoxifenil)piridin-2-il)acetamida; entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tratamiento. Dichos compuestos son inhibidores de AAK1 (cinasa asociada al adaptador 1), siendo utiles en el tratamiento de la enfermedad de Alzheimer, trastorno bipolar, entre otros
PE2016001842A 2014-04-02 2015-04-01 Inhibidores de biaril cinasa PE20170004A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461973942P 2014-04-02 2014-04-02
US201462061591P 2014-10-08 2014-10-08

Publications (1)

Publication Number Publication Date
PE20170004A1 true PE20170004A1 (es) 2017-03-04

Family

ID=52988448

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001842A PE20170004A1 (es) 2014-04-02 2015-04-01 Inhibidores de biaril cinasa

Country Status (27)

Country Link
US (7) US9902722B2 (es)
EP (1) EP3126351B1 (es)
JP (1) JP6411541B2 (es)
KR (1) KR102379518B1 (es)
CN (1) CN106458994B (es)
AU (1) AU2015240869B2 (es)
BR (1) BR112016022298B1 (es)
CA (1) CA2944466C (es)
CL (1) CL2016002502A1 (es)
CY (1) CY1120988T1 (es)
DK (1) DK3126351T3 (es)
EA (1) EA028942B1 (es)
ES (1) ES2700549T3 (es)
HR (1) HRP20181899T1 (es)
HU (1) HUE041457T2 (es)
IL (1) IL248086B (es)
LT (1) LT3126351T (es)
MX (1) MX2016012829A (es)
PE (1) PE20170004A1 (es)
PL (1) PL3126351T3 (es)
PT (1) PT3126351T (es)
RS (1) RS58062B1 (es)
SG (1) SG11201608195QA (es)
SI (1) SI3126351T1 (es)
SM (1) SMT201800665T1 (es)
WO (1) WO2015153720A1 (es)
ZA (1) ZA201606767B (es)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016523963A (ja) 2013-07-08 2016-08-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールアミドキナーゼ阻害剤
JP6473146B2 (ja) 2013-10-11 2019-02-20 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ピロロトリアジンキナーゼ阻害剤
PL3105218T3 (pl) 2014-02-13 2020-03-31 Incyte Corporation Cyklopropyloaminy jako inhibitory lsd1
SMT201900620T1 (it) 2014-02-13 2020-01-14 Incyte Corp Ciclopropilammine come inibitori di lsd1
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
HUE041457T2 (hu) * 2014-04-02 2019-05-28 Bristol Myers Squibb Co Biaril kináz inhibitorok
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
ES2757948T3 (es) 2015-04-03 2020-04-30 Incyte Corp Compuestos heterocíclicos como inhibidores LSD1
WO2016164295A2 (en) * 2015-04-10 2016-10-13 Bristol-Myers Squibb Company Fused pyridines as kinase inhibitors
AU2016306555B2 (en) 2015-08-12 2021-01-28 Incyte Holdings Corporation Salts of an LSD1 inhibitor
JP6864674B2 (ja) * 2015-10-01 2021-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ビアリールキナーゼ阻害剤
CN112142655A (zh) 2015-10-01 2020-12-29 百时美施贵宝公司 联芳基激酶抑制剂
JP7190906B2 (ja) 2017-01-24 2022-12-16 住友化学株式会社 縮合複素環化合物及びそれを含有する組成物
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
TW202120495A (zh) * 2019-08-02 2021-06-01 美商愛彼特生物製藥股份有限公司 經取代環丙基—２，２＇—聯嘧啶基化合物、其類似物及其使用方法
CN115484951A (zh) * 2020-04-21 2022-12-16 莱西肯医药有限公司 用于治疗病毒感染的aak1抑制剂
EP4138844A1 (en) 2020-04-21 2023-03-01 Lexicon Pharmaceuticals, Inc. 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections
EP4159719A4 (en) * 2020-05-28 2024-07-17 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Preparation method for (s)-2-amino-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)methyl propionate diacid salt
TW202210462A (zh) * 2020-05-28 2022-03-16 中國大陸商杭州中美華東製藥有限公司 （ｓ）－２－胺基－３－（４－（２，３－二甲基吡啶－４－基）苯基丙酸甲酯及其鹽的製備方法
JP2024527618A (ja) * 2021-07-15 2024-07-25 シーザン ハイスーク ファーマシューティカル カンパニー リミテッド Ａａｋ１阻害剤及びその用途
WO2023051749A1 (zh) * 2021-09-30 2023-04-06 武汉人福创新药物研发中心有限公司 Aak1抑制剂及其用途
CN119095826A (zh) * 2022-03-01 2024-12-06 莱西肯医药有限公司 用于合成aak1抑制剂的方法和化合物
KR20240155293A (ko) * 2022-03-01 2024-10-28 렉시컨 파마슈티컬스 인코퍼레이티드 고체 형태의 (s)-1-((2',6-비스(디플루오로메틸)-[2,4'-바이피리딘]-5-일)옥시)-2,4-디메틸펜탄-2-아민 및 이의 염
WO2023183443A1 (en) 2022-03-23 2023-09-28 Teva Pharmaceuticals International Gmbh Solid state forms of lx9211 and salts thereof
WO2024099430A1 (zh) * 2022-11-10 2024-05-16 西藏海思科制药有限公司 一种含aak1抑制剂的药物组合物
WO2024125668A1 (zh) * 2022-12-13 2024-06-20 上海海雁医药科技有限公司 杂环取代的五并六元杂芳基衍生物、其药物组合物及应用与制备方法
WO2024153067A1 (zh) * 2023-01-16 2024-07-25 上海海雁医药科技有限公司 杂环取代的含氮杂环衍生物、其药物组合物及应用与制备方法
WO2024207945A1 (zh) * 2023-04-07 2024-10-10 艾立康药业股份有限公司 作为aak1抑制剂的氮杂环类化合物

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5464764A (en) 1989-08-22 1995-11-07 University Of Utah Research Foundation Positive-negative selection methods and vectors
AU2515992A (en) 1991-08-20 1993-03-16 Genpharm International, Inc. Gene targeting in animal cells using isogenic dna constructs
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US7348335B2 (en) * 2002-11-05 2008-03-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
JP2007526324A (ja) * 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
CA2649302A1 (en) * 2006-04-12 2007-10-25 Wyeth Anilino-pyrimidine phenyl and benzothiophene analogs
AU2008210455A1 (en) * 2007-01-31 2008-08-07 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as kinase inhibitors
EP3235499A3 (en) * 2012-03-09 2018-01-17 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
US8703953B2 (en) * 2012-03-09 2014-04-22 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
US8901305B2 (en) 2012-07-31 2014-12-02 Bristol-Myers Squibb Company Aryl lactam kinase inhibitors
EP2958924B1 (en) 2013-02-22 2016-12-28 Bristol-Myers Squibb Company 5h-chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase 1 (aak1)
JP2016523963A (ja) 2013-07-08 2016-08-12 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールアミドキナーゼ阻害剤
JP6243539B2 (ja) 2013-09-11 2017-12-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールエーテルをベースとするキナーゼ阻害剤
JP6276865B2 (ja) 2014-01-29 2018-02-07 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリールラクタムキナーゼ阻害剤
CA2937501A1 (en) 2014-01-31 2015-08-06 Bristol-Myers Squibb Company Quinoline-based kinase inhibitors
HUE041457T2 (hu) 2014-04-02 2019-05-28 Bristol Myers Squibb Co Biaril kináz inhibitorok
EP3200797A1 (en) 2014-09-30 2017-08-09 Bristol-Myers Squibb Company Quinazoline-based kinase inhibitors
WO2016164295A2 (en) 2015-04-10 2016-10-13 Bristol-Myers Squibb Company Fused pyridines as kinase inhibitors
JP6864674B2 (ja) 2015-10-01 2021-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ビアリールキナーゼ阻害剤
CN112142655A (zh) * 2015-10-01 2020-12-29 百时美施贵宝公司 联芳基激酶抑制剂
WO2020010295A1 (en) 2018-07-06 2020-01-09 Liqui-Box Corporation Dispensing probe for dispensing flowable material

Also Published As

Publication number Publication date
EA028942B1 (ru) 2018-01-31
JP2017511329A (ja) 2017-04-20
MX2016012829A (es) 2017-01-05
US20190367508A1 (en) 2019-12-05
CA2944466C (en) 2020-06-09
CN106458994A (zh) 2017-02-22
US20180134704A1 (en) 2018-05-17
IL248086A0 (en) 2016-11-30
RS58062B1 (sr) 2019-02-28
HRP20181899T1 (hr) 2019-01-11
PL3126351T3 (pl) 2019-03-29
LT3126351T (lt) 2018-11-26
US10723734B2 (en) 2020-07-28
US20170183340A1 (en) 2017-06-29
WO2015153720A1 (en) 2015-10-08
AU2015240869B2 (en) 2018-11-08
CA2944466A1 (en) 2015-10-08
AU2015240869A1 (en) 2016-11-17
SI3126351T1 (sl) 2018-11-30
BR112016022298A2 (es) 2017-08-15
US10351563B2 (en) 2019-07-16
EP3126351A1 (en) 2017-02-08
JP6411541B2 (ja) 2018-10-24
PT3126351T (pt) 2018-12-04
US12065437B2 (en) 2024-08-20
ES2700549T3 (es) 2019-02-18
US10155760B2 (en) 2018-12-18
SG11201608195QA (en) 2016-10-28
KR102379518B1 (ko) 2022-03-25
KR20160132491A (ko) 2016-11-18
CN106458994B (zh) 2019-09-13
EA201691916A1 (ru) 2017-02-28
CL2016002502A1 (es) 2017-06-23
US9902722B2 (en) 2018-02-27
DK3126351T3 (en) 2019-01-14
US20190048006A1 (en) 2019-02-14
US10981910B2 (en) 2021-04-20
EP3126351B1 (en) 2018-09-19
BR112016022298B1 (pt) 2022-09-20
CY1120988T1 (el) 2019-12-11
US20200317671A1 (en) 2020-10-08
NZ725814A (en) 2021-06-25
ZA201606767B (en) 2018-05-30
US20210277001A1 (en) 2021-09-09
SMT201800665T1 (it) 2019-01-11
US20240360131A1 (en) 2024-10-31
IL248086B (en) 2019-09-26
HUE041457T2 (hu) 2019-05-28

Similar Documents

Publication Publication Date Title
PE20170004A1 (es) Inhibidores de biaril cinasa
PE20161438A1 (es) Inhibidores de desmetilasa 1 especifica a lisina
PE20170695A1 (es) Compuestos de indol carboxamida utiles como inhibidores de cinasas
PE20190395A1 (es) Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
CU20170087A7 (es) Formas cristalinas de 5-(4-ciclopropil-1 h-imidazol-1-il)-n-(6-(4-isopropil-4h-1 , 2, 4- triazol-3-il)piridin-2-il)-2-fluoro-4-metilbenzamida
PE20161368A1 (es) Inhibidores de diacilglicerol aciltranferasa 2
PE20141535A1 (es) Inhibidores de pde10 de pirimidina
EA201591908A1 (ru) Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
PE20160686A1 (es) Nuevas dihidroquinolizinonas para el tratamiento y profilaxis de la infeccion por virus de la hepatitis b
PE20171341A1 (es) Compuestos de pirazina para el tratamiento de enfermedades infecciosas
PE20171338A1 (es) Compuestos y composiciones como inhibidores de quinasa raf
PE20140626A1 (es) Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona
PE20170666A1 (es) 2-(morfolin-4-il)-1,7-naftiridinas
EA201592200A1 (ru) Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
PE20130405A1 (es) Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
EA201790246A1 (ru) Гетероциклические карбоновые кислоты в качестве активаторов растворимой гуанилатциклазы
PE20140609A1 (es) Diazacarbazoles y metodos de uso
PE20160521A1 (es) Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida
PE20152032A1 (es) Compuestos de 3,4-dihidroisoquinolin-2(1h)-il
PE20151001A1 (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
AR100818A1 (es) N-(cianometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida
MX2021015102A (es) Inhibidores del receptor del factor estimulante de colonias 1 (csf-1r).
EA202091120A2 (ru) Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы
MX2017004950A (es) Composiciones y metodos para tratar el insomnio.
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk