CU24341B1 - Compuestos y composiciones orgánicas inhibidores del ácido graso sintetasa (fasn) útiles para el tratamiento del cáncer, infecciones virales, obesidad y diabetes - Google Patents

Compuestos y composiciones orgánicas inhibidores del ácido graso sintetasa (fasn) útiles para el tratamiento del cáncer, infecciones virales, obesidad y diabetes

Info

Publication number
CU24341B1
CU24341B1 CUP2015000120A CU20150120A CU24341B1 CU 24341 B1 CU24341 B1 CU 24341B1 CU P2015000120 A CUP2015000120 A CU P2015000120A CU 20150120 A CU20150120 A CU 20150120A CU 24341 B1 CU24341 B1 CU 24341B1
Authority
CU
Cuba
Prior art keywords
fasn
synthease
obesity
diabetes
cancer
Prior art date
Application number
CUP2015000120A
Other languages
English (en)
Other versions
CU20150120A7 (es
Inventor
Kenneth W Bair
David R Lancia
Hongbin Li
James Loch
Wei Lu
Matthew W Martin
David S Millan
Shawn E R Schiller
Mark J Tebbe
Original Assignee
Forma 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 Forma Therapeutics Inc filed Critical Forma Therapeutics Inc
Publication of CU20150120A7 publication Critical patent/CU20150120A7/es
Publication of CU24341B1 publication Critical patent/CU24341B1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—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
    • 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
    • C07D213/56—Amides
    • 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
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • 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
    • C07D213/69—Two or more oxygen atoms
    • 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
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—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
    • C07D263/57—Aryl or substituted aryl radicals
    • 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
    • C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C07D277/66—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D305/08—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 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
    • 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
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/10—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 carbon chain containing aromatic rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Furan Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

<p>La presente invención se refiere a compuestos y composiciones orgánicas inhibidores del ácido graso sintasa (FASN), su síntesis, aplicaciones y antídotos. A continuación se muestra un compuesto ilustrativo de la invención:</p> <p>ESPACIO PARA FÓRMULA</p>
CUP2015000120A 2013-03-13 2014-03-11 Compuestos y composiciones orgánicas inhibidores del ácido graso sintetasa (fasn) útiles para el tratamiento del cáncer, infecciones virales, obesidad y diabetes CU24341B1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361779908P 2013-03-13 2013-03-13
US201361779962P 2013-03-13 2013-03-13
PCT/US2014/023388 WO2014164749A1 (en) 2013-03-13 2014-03-11 Novel compounds and compositions for inhibition of fasn

Publications (2)

Publication Number Publication Date
CU20150120A7 CU20150120A7 (es) 2016-04-25
CU24341B1 true CU24341B1 (es) 2018-05-08

Family

ID=51658962

Family Applications (1)

Application Number Title Priority Date Filing Date
CUP2015000120A CU24341B1 (es) 2013-03-13 2014-03-11 Compuestos y composiciones orgánicas inhibidores del ácido graso sintetasa (fasn) útiles para el tratamiento del cáncer, infecciones virales, obesidad y diabetes

Country Status (37)

Country Link
US (8) US20160002188A1 (es)
EP (2) EP3587406B1 (es)
JP (2) JP2016517412A (es)
KR (1) KR102194745B1 (es)
CN (2) CN105492008B (es)
AU (3) AU2014249003A1 (es)
BR (1) BR112015023279B1 (es)
CA (1) CA2905751A1 (es)
CL (1) CL2015002698A1 (es)
CR (1) CR20150541A (es)
CU (1) CU24341B1 (es)
CY (1) CY1122244T1 (es)
DK (1) DK2968316T3 (es)
EC (1) ECSP15043280A (es)
ES (2) ES2753386T3 (es)
HR (1) HRP20191860T1 (es)
HU (1) HUE045701T2 (es)
IL (1) IL241699B (es)
LT (1) LT2968316T (es)
ME (1) ME03564B (es)
MX (1) MX364895B (es)
MY (1) MY191366A (es)
NI (1) NI201500141A (es)
NO (1) NO20151329A1 (es)
PE (1) PE20160122A1 (es)
PH (1) PH12015502097B1 (es)
PL (1) PL2968316T3 (es)
PT (1) PT2968316T (es)
RS (1) RS59411B1 (es)
RU (2) RU2686323C2 (es)
SA (1) SA515361086B1 (es)
SG (2) SG11201507486SA (es)
SI (1) SI2968316T1 (es)
SM (1) SMT201900585T1 (es)
TN (1) TN2015000420A1 (es)
WO (2) WO2014164767A1 (es)
ZA (1) ZA201506922B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3587406B1 (en) 2013-03-13 2021-01-27 Forma Therapeutics, Inc. 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-one derivatives and related compounds as fatty acid synthase (fasn) inhibitors for the treatment of cancer
CN105008329B (zh) * 2013-03-21 2018-01-05 默克专利股份公司 作为fasn抑制剂的哌嗪衍生物
CA2964113A1 (en) * 2014-10-14 2016-04-21 La Jolla Institute Of Allergy & Immunology Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
EP3220901B1 (en) 2014-11-20 2020-02-19 VIB vzw Means and methods for treatment of early-onset parkinson's disease
US10919875B2 (en) 2015-06-18 2021-02-16 89Bio Ltd Substituted 4-benzyl and 4-benzoyl piperidine derivatives
BR112017027339A2 (pt) 2015-06-18 2018-09-04 Cephalon, Inc. derivados de piperidina 1,4-substituída
WO2017189613A1 (en) 2016-04-25 2017-11-02 Forma Therapeutics, Inc. Methods of using fasn inhibitors
CN106806371A (zh) * 2017-01-19 2017-06-09 伊希珍 一种化合物在制备治疗发作性睡病药物中的应用
CN107056695A (zh) * 2017-01-26 2017-08-18 青岛辰达生物科技有限公司 一种治疗胃癌药物阿帕替尼的合成方法
US11066420B2 (en) 2017-05-01 2021-07-20 Sanford Burnham Prebys Medical Discovery Institute Inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) and uses thereof
WO2019084300A1 (en) * 2017-10-25 2019-05-02 Forma Therapeutics, Inc. TREATMENT OF GLIOBLASTOMA WITH FASN INHIBITORS
GB201801128D0 (en) 2018-01-24 2018-03-07 Univ Oxford Innovation Ltd Compounds
US12324807B2 (en) 2018-06-01 2025-06-10 Cornell University Combination therapy for PI3K-associated disease or disorder
TWI767148B (zh) * 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
EP3636637A1 (en) * 2018-10-10 2020-04-15 Forma Therapeutics, Inc. Inhibiting fatty acid synthase (fasn)
WO2020092376A1 (en) * 2018-10-29 2020-05-07 Forma Therapeutics, Inc. Treating non-alcoholic steatohepatitis (nash)
CN113382633A (zh) * 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式
BR112021007421A2 (pt) 2018-12-06 2021-08-03 Daiichi Sankyo Company, Limited derivado de cicloalcano-1,3-diamina
US20220400732A1 (en) * 2019-03-21 2022-12-22 Cornell University Anti-fructose therapy for colorectal and small intestine cancers
WO2021127472A1 (en) * 2019-12-20 2021-06-24 Landos Biopharma, Inc. Lanthionine c-like protein 2 ligands, cells prepared therewith, and therapies using same
WO2023093700A1 (zh) * 2021-11-29 2023-06-01 中国海洋大学 咪唑并噻唑衍生物及其制备方法与应用
EP4642451A2 (en) * 2022-12-28 2025-11-05 Seattle Children's Hospital d/b/a Seattle Children's Research Institute N-myristoyltransferase inhibitors and methods of use
CN121085942A (zh) * 2025-08-28 2025-12-09 中国海洋大学 3，5-位取代的咪唑并噻二唑杂环衍生物及其制备方法与应用

Family Cites Families (206)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5759837A (en) 1989-01-17 1998-06-02 John Hopkins University Chemotherapy for cancer by inhibiting the fatty acid biosynthetic pathway
EP0385043A1 (en) * 1989-02-28 1990-09-05 Fabrica Espanola De Productos Quimicos Y Farmaceuticos, S.A. (Faes) New derivatives of 4-substituted piperazines
HU209678B (en) 1992-06-09 1994-10-28 Richter Gedeon Vegyeszet Process for producing biologically active eburnamenin-14-carbonyl-amino derivatives and pharmaceutical compositions containing them
US5376664A (en) 1992-07-27 1994-12-27 The Du Pont Merck Pharmaceutical Company Unsymmetrical mono-3-nitro bis-naphthalimides as anticancer agents
CA2077252C (en) * 1992-08-31 2001-04-10 Khashayar Karimian Methods of making ureas and guanidines, and intermediates therefor
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
WO1997018806A1 (en) 1995-11-17 1997-05-29 The Johns Hopkins University Inhibition of fatty acid synthase as a means to reduce adipocyte mass
US6235878B1 (en) 1996-07-19 2001-05-22 Takeda Chemical Industries, Ltd. Fas ligand-like protein, its production and use
DE19743435A1 (de) 1997-10-01 1999-04-08 Merck Patent Gmbh Benzamidinderivate
US6413974B1 (en) 1998-02-26 2002-07-02 Aventis Pharmaceuticals Inc. 6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines
JP2002512368A (ja) 1998-04-23 2002-04-23 カロ バイオ ユー エス エイ，インコーポレイテッド 受容体の生物活性を調節するための化合物の能力を予測する方法
EP1086122B1 (en) 1998-06-11 2005-08-24 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Pyrazinone protease inhibitors
IL141724A0 (en) 1998-08-28 2002-03-10 Scios Inc INHIBITORS OF P38-α KINASE
WO2000022909A2 (en) 1998-10-19 2000-04-27 Biotech Australia Pty. Limited Systems for oral delivery
CO5180605A1 (es) 1999-06-23 2002-07-30 Smithkline Beecham Corp Compuestos de indol
CO5190665A1 (es) 1999-06-23 2002-08-29 Smithkline Beecham Corp Compuestos de indol
CN1217932C (zh) 1999-08-10 2005-09-07 英国生物技术药物有限公司 抗菌剂
AR029001A1 (es) 1999-08-23 2003-06-04 Smithkline Beecham Corp Derivados de bencil-3,4-metilendioxicinamico y el uso de los mismos para la manufactura de un medicamento
EP1206463A4 (en) 1999-08-23 2003-01-29 Smithkline Beecham Corp FATTY ACID SYNTHASE INHIBITORS
AU6925500A (en) 1999-08-23 2001-03-19 Smithkline Beecham Corporation Fatty acid synthase inhibitors
US6541477B2 (en) * 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
WO2001017942A1 (en) 1999-09-04 2001-03-15 Astrazeneca Ab Amides as inhibitors for pyruvate dehydrogenase
US6486211B1 (en) 1999-10-22 2002-11-26 Smithkline Beecham Corporation Indole compounds
WO2001030752A2 (en) 1999-10-22 2001-05-03 Smithkline Beecham Corporation Indole compounds for treating bacterial infections
EP1255567A1 (en) 1999-11-15 2002-11-13 Drug Innovation &amp; Design, Inc. Selective cellular targeting: multifunctional delivery vehicles
CA2391534A1 (en) 1999-11-15 2001-05-25 Drug Innovation & Design, Inc. Selective cellular targeting: multifunctional delivery vehicles
AU1607501A (en) 1999-11-15 2001-05-30 Drug Innovation & Design, Inc. Selective cellular targeting: multifunctional delivery vehicles
JP2003534340A (ja) 2000-05-24 2003-11-18 スミスクライン・ビーチャム・コーポレイション 脂肪酸シンターゼ阻害剤
EP1164374A1 (en) 2000-06-16 2001-12-19 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Method for identifying apoptosis-modified proteins
US20040022779A1 (en) 2000-06-16 2004-02-05 Thomas Rudel Method for identifying apoptosis-modified proteins
US6608059B1 (en) 2000-06-27 2003-08-19 Smithkline Beecham Corporation Fatty acid synthase inhibitors
WO2002000620A1 (en) 2000-06-27 2002-01-03 Smithkline Beecham Corporation Fatty acid synthase inhibitors
WO2002002119A1 (en) 2000-06-29 2002-01-10 Smithkline Beecham Corporation Fatty acid synthase inhibitors
AU2001281059A1 (en) 2000-08-02 2002-02-13 Smith Kline Beecham Corporation Fatty acid synthase inhibitors
AU2001284705A1 (en) 2000-08-02 2002-02-13 Smith Kline Beecham Corporation Fatty acid synthase inhibitors
EP1318806A4 (en) 2000-09-22 2004-01-21 Smithkline Beecham Corp INHIBITORS OF FATTY ACID SYNTASES
EP1322610A2 (en) * 2000-09-29 2003-07-02 Millennium Pharmaceuticals, Inc. PIPERAZINE BASED INHIBITORS OF FACTOR Xa
CA2423981A1 (en) 2000-09-29 2003-03-28 Kimiko Ichikawa Thienopyrimidine compounds and salts thereof and process for the preparation of the same
US20070208087A1 (en) * 2001-11-02 2007-09-06 Sanders Virginia J Compounds, compositions and methods for the treatment of inflammatory diseases
AU2002243439A1 (en) 2000-11-17 2002-07-24 Smithkline Beecham Corporation Fatty acid synthase inhibitors
EP1401469A2 (en) 2001-04-09 2004-03-31 Lorantis Limited Therapeutic use and identification of modulators of a hedgehog signalling pathway or one of its target pathways
JP2005518332A (ja) 2001-05-23 2005-06-23 デンドレオン コーポレイション 細胞表面のプロテアーゼにより活性化される結合体およびその治療的使用
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
FR2829766A1 (fr) 2001-09-14 2003-03-21 Lipha Derives d'oxamates comportant un heterocycle azote diversement substitue
EP1436283B1 (en) 2001-09-21 2008-01-23 Boryung Pharmaceutical Co., Ltd. Method for preparing pyrimidinone compound and pharmaceutically acceptable salts thereof
EA007468B1 (ru) 2001-12-20 2006-10-27 Оси Фармасьютикалз, Инк. Пиримидиновые соединения, относящиеся к a-селективным антагонистам, их синтез и применение
US20030170244A1 (en) 2001-12-21 2003-09-11 Pluenneke John D. Inhibition of Fas signaling
US20050119251A1 (en) 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
SI1482924T1 (sl) 2002-03-05 2008-12-31 Merck Frosst Canada Ltd Katepsin cistein proteazni inhibitorji
WO2003088975A1 (en) 2002-04-17 2003-10-30 The Burnham Institute Inhibition of fatty acid synthase by beta-lactones and other compounds for inhibition of cellular proliferation
US7728153B2 (en) 2002-04-17 2010-06-01 The Burnham Institute For Medical Research Method for the asymmetric synthesis of beta-lactone compounds
US7662826B2 (en) 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
US20040001801A1 (en) 2002-05-23 2004-01-01 Corvas International, Inc. Conjugates activated by cell surface proteases and therapeutic uses thereof
CN100513404C (zh) 2002-07-09 2009-07-15 法斯根公司 新化合物、含该化合物的药物组合物以及该化合物的应用方法
EP1534074A4 (en) 2002-07-18 2008-01-09 Merck & Co Inc COMBINATION THERAPY FOR THE TREATMENT OF FATIBILITY
AU2003268064A1 (en) 2002-08-09 2004-02-25 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
AU2003268493A1 (en) 2002-09-11 2004-04-30 Merck & Co., Inc. Piperazine urea derivatives as melanocortin-4 receptor agonists
AU2003218462A1 (en) 2002-10-01 2004-04-23 Merck And Co., Inc. Treatment of obesity and other disorders associated with excessive food intake
US20060052597A1 (en) 2002-10-22 2006-03-09 Best Desmond J Aryloxyalkylamine derivatives as h3 receptor ligands
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040122033A1 (en) 2002-12-10 2004-06-24 Nargund Ravi P. Combination therapy for the treatment of obesity
WO2005000217A2 (en) 2003-06-06 2005-01-06 Merck & Co., Inc. Combination therapy for the treatment of dyslipidemia
US20060160834A1 (en) 2003-06-06 2006-07-20 Fong Tung M Combination therapy for the treatment of hypertension
US20070099884A1 (en) 2003-06-06 2007-05-03 Erondu Ngozi E Combination therapy for the treatment of diabetes
WO2005009950A2 (en) 2003-07-22 2005-02-03 Merck & Co., Inc. Piperidine derivatives as melanocortin-4 receptor agonists
EP1663234A1 (en) 2003-08-14 2006-06-07 Pfizer Limited Piperazine derivatives for the treatment of hiv infections
US20050043300A1 (en) * 2003-08-14 2005-02-24 Pfizer Inc. Piperazine derivatives
WO2005035534A1 (ja) 2003-10-08 2005-04-21 Ono Pharmaceutical Co., Ltd. 複素ビシクロ環および複素トリシクロ環化合物およびその医薬
GB0326029D0 (en) * 2003-11-07 2003-12-10 Astrazeneca Ab Chemical compounds
WO2005073186A1 (ja) * 2004-01-29 2005-08-11 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
TW200528101A (en) * 2004-02-03 2005-09-01 Astrazeneca Ab Chemical compounds
BRPI0508514A (pt) 2004-03-10 2007-08-14 Janssen Pharmaceutica Nv aril piperidinas ou piperazinas substituìdas por heterociclos de 5-membros inibidoras de mtp
PE20060285A1 (es) * 2004-03-30 2006-05-08 Aventis Pharma Inc Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp)
JP4777974B2 (ja) 2004-04-01 2011-09-21 イーライ リリー アンド カンパニー ヒスタミンｈ３受容体作用物質、製剤および治療的使用
US8008301B2 (en) 2004-04-01 2011-08-30 Eli Lilly And Company Histamine H3 receptor agents, preparation and therapeutic uses
JP4790704B2 (ja) 2004-04-12 2011-10-12 トレント・ファーマシューティカルズ・リミテッド Ｈｓｐ７０誘発因子としての２−プロペン−１−オン
BRPI0511295A (pt) * 2004-05-18 2007-12-04 Schering Corp 2-quinolil-oxazóis substituìdos úteis como inibidores de pde4
US20050261292A1 (en) 2004-05-19 2005-11-24 Solvay Pharmaceuticals Gmbh Pharmaceutical composition containing N-sulfamoyl-N'-arylpiperazines for the treatment or inhibition of obesity and related conditions
RU2395503C2 (ru) 2004-05-19 2010-07-27 Зольвай Фармасьютиклз Гмбх Лекарственные средства, содержащие n-сульфамоил-n'-арилпиперазины, предназначенные для профилактики или лечения ожирения и связанных с ним состояний
WO2005116006A1 (ja) 2004-05-28 2005-12-08 Riken フラーレン誘導体の製造方法
MX2007002318A (es) 2004-08-26 2007-04-17 Kudos Pharm Ltd Derivados de ftalazinona substituidos con 4-heteroarilmetilo.
WO2006034341A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
JP2008513386A (ja) 2004-09-20 2008-05-01 ４エスシー アーゲー 新規な複素環式ＮＦ−κＢ阻害剤
CA2577821A1 (en) 2004-09-24 2006-04-06 Merck & Co., Inc. Combination therapy for the treatment of obesity
CA2582235A1 (en) 2004-10-04 2006-04-20 Millennium Pharmaceuticals, Inc. Lactam compounds useful as protein kinase inhibitors
WO2006049933A2 (en) 2004-10-29 2006-05-11 Merck & Co., Inc. Compositions and methods for the treatment of obesity and sexual dysfunction
FR2877667B1 (fr) 2004-11-05 2007-03-23 Sod Conseils Rech Applic Derives de 4,7-dioxobenzothiazole-2-carboxamides, leur preparation et leurs applications therapeutiques
MX2007006695A (es) 2004-12-03 2007-08-14 Schering Corp Piperazinas sustituidas como antagonistas de cb1.
FR2879598B1 (fr) 2004-12-17 2007-03-30 Sod Conseils Rech Applic Inhibiteurs de phosphatases cdc25
BRPI0609464A2 (pt) 2005-05-23 2010-04-13 Japan Tobacco Inc composto de pirazol e agente terapêutico para diabetes compreendendo o mesmo
US20060270650A1 (en) 2005-05-26 2006-11-30 Macneil Tanya Combination therapy for the treatment of obesity
ATE450525T1 (de) 2005-06-20 2009-12-15 Schering Corp Kohlenstoffgebundene substituierte piperidine und derivate daraus als histamin-h3-antagonisten
GB0518237D0 (en) 2005-09-07 2005-10-19 Angeletti P Ist Richerche Bio Therapeutic compounds
US7473688B2 (en) 2005-09-13 2009-01-06 Bristol-Myers Squibb Company Indolobenzazepine HCV NS5B inhibitors
BRPI0616575A2 (pt) 2005-09-27 2011-06-21 Irm Llc compostos e composições contendo diarilamina, seu uso como moduladores de receptores de c-kit bem como método para sua produção
CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
CA2627900A1 (en) 2005-11-14 2007-08-16 Irm Llc Compounds and compositions as lxr modulators
ES2334580T3 (es) 2005-12-15 2010-03-12 F. Hoffmann-La Roche Ag Derivados de pirrolo(2,3-c)piridina.
AU2006326067A1 (en) 2005-12-16 2007-06-21 F. Hoffmann-La Roche Ag Pyrrolo [2 , 3-b] pyridine derivatives as H3 receptor modulators
EP1966143A2 (en) 2005-12-21 2008-09-10 Schering Corporation Substituted aniline derivatives useful as histamine h3 antagonists
KR20080087833A (ko) 2005-12-21 2008-10-01 쉐링 코포레이션 히스타민 ｈ３ 길항제로서 유용한 페녹시피페리딘 및 이의유사체
US8008354B2 (en) 2006-01-11 2011-08-30 Burnham Institute For Medical Research Death receptor sensitizing compounds and methods of use therefor
US20070203236A1 (en) 2006-01-11 2007-08-30 Smith Jeffrey W Novel antagonists of the human fatty acid synthase thioesterase
BRPI0707916A2 (pt) 2006-01-13 2011-05-17 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem e uso destes compostos
MX2008009413A (es) 2006-01-20 2008-10-01 Schering Corp Heterociclos como agonistas del receptor de acido nicotinico para el tratamiento de la dislipidemia.
ES2349160T3 (es) 2006-01-23 2010-12-28 F. Hoffmann-La Roche Ag Derivados de la ciclohexil sulfonamida con actividad frente a los receptores h3.
JP2009525278A (ja) 2006-01-30 2009-07-09 メルク エンド カムパニー インコーポレーテッド 脂肪酸シンターゼ（ｆａｓ）のインヒビター
US7807671B2 (en) 2006-04-25 2010-10-05 Bristol-Myers Squibb Company Diketo-piperazine and piperidine derivatives as antiviral agents
US7601716B2 (en) 2006-05-01 2009-10-13 Cephalon, Inc. Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
AU2007267184A1 (en) 2006-05-30 2007-12-06 F. Hoffmann-La Roche Ag Piperidinyl pyrimidine derivatives
CA2652167A1 (en) 2006-05-31 2007-12-06 Philip Jones Pyrrolo[1,2-a]pyrazin-1(2h)-one and pyrrolo[1,2-d][1,2,4]triazin-1(2h)-one derivatives as inhibitors of poly(adp-ribose)polymerase (parp)
GB0610680D0 (en) 2006-05-31 2006-07-12 Istituto Di Ricerche D Biolog Therapeutic compounds
US8088923B2 (en) 2006-07-07 2012-01-03 The Texas A&M University System Cyclic-fused beta-lactones and their synthesis
US7666888B2 (en) * 2006-07-20 2010-02-23 Amgen Inc. Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1
JPWO2008023720A1 (ja) * 2006-08-23 2010-01-14 アステラス製薬株式会社 ウレア化合物又はその塩
CA2662337A1 (en) 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof
EP2698157B1 (en) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
JO2653B1 (en) 2006-10-24 2012-06-17 شركة جانسين فارماسوتيكا ان. في Tetrahydroflavin 1-carboxylic acid substituted with pyridine or pyrazine inhibit MTB
MX2009003823A (es) 2006-11-02 2009-05-11 Sanofi Aventis Deutschland Nueva difenilazetidinona sustituida con acido piperazina-1-sulfonico y que tiene propiedades farmacologicas mejoradas.
WO2008059214A1 (en) 2006-11-13 2008-05-22 Astrazeneca Ab Bisamlde derivatives and use thereof as fatty acid synthase inhibitors
CN101190894A (zh) 2006-11-23 2008-06-04 中国人民解放军军事医学科学院毒物药物研究所 脂肪酸合成酶抑制剂及其制药用途
EP2096923B1 (en) 2006-11-27 2014-01-22 H. Lundbeck A/S Heteroaryl amide derivatives
CN101679297B (zh) 2006-12-08 2012-01-11 埃克塞利希斯股份有限公司 Lxr和fxr调节剂
WO2008075077A1 (en) 2006-12-21 2008-06-26 Astrazeneca Ab Piperidine derivatives for the treatment of obesity
TW200833663A (en) 2006-12-21 2008-08-16 Astrazeneca Ab Therapeutic agents
TW200831092A (en) 2006-12-21 2008-08-01 Astrazeneca Ab Therapeutic agents
US8466150B2 (en) 2006-12-28 2013-06-18 Abbott Laboratories Inhibitors of poly(ADP-ribose)polymerase
DE102007007751A1 (de) 2007-02-16 2008-08-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel
CN101668520A (zh) 2007-02-28 2010-03-10 科内图斯医药公司 使用特定基质金属蛋白酶(mmp)抑制剂治疗肝脏疾病的方法
HRP20110713T1 (hr) 2007-02-28 2011-11-30 Conatus Pharmaceuticals Postupci liječenja kroničnog virusnog hepatitisa c uz upotrebu ro 113-0830
WO2008106167A1 (en) 2007-02-28 2008-09-04 Conatus Pharmaceuticals, Inc. Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases
US7943620B2 (en) 2007-03-07 2011-05-17 Concert Pharmaceuticals, Inc. Anti-anginal compounds
BRPI0809680A2 (pt) 2007-03-30 2014-10-07 Hoffmann La Roche Compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por agonistas de lxr alfa e/ou lxr beta e uso dos compostos.
US7682857B2 (en) 2007-04-16 2010-03-23 Mitsubishi Electric Corporation Method for manufacturing semiconductor optical device
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
CN102317266A (zh) 2007-04-25 2012-01-11 埃克塞利希斯股份有限公司 作为pim调节剂的6-苯基嘧啶酮类
CA2690379A1 (en) 2007-06-13 2008-12-24 Auspex Pharmaceuticals, Inc. Substituted piperazines
EA201000046A1 (ru) 2007-06-21 2011-02-28 Кара Терапеутикс, Инк. Замещенные имидазогетероциклы
EP2019091A1 (en) 2007-06-25 2009-01-28 Fundació Privada Institut d'Investigació Biomédica de Girona - Dr. Josep Trueta Novel polyhydroxylated compounds as Fatty Acid Synthase (FASN) inhibitors
US20090023727A1 (en) 2007-07-05 2009-01-22 Muhammad Hashim Javaid Phthalazinone derivatives
US8314091B2 (en) 2007-08-20 2012-11-20 Msd Oss B.V. N-benzyl,N'-arylcarbonylpiperazine derivatives
MX2010003868A (es) * 2007-10-09 2010-04-27 Hoffmann La Roche Cis-imidazolinas quirales.
CN101939650A (zh) 2007-11-13 2011-01-05 菲思根诊断学有限公司 磷酸化脂肪酸合酶与癌症
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP2011511078A (ja) * 2008-02-06 2011-04-07 レアド トヘラペウトイクス，インコーポレーテッド ポリ（ａｄｐリボース）ポリメラーゼ（ｐａｒｐ）のベンズオキサゾールカルボキサミド阻害剤
WO2009098282A1 (en) * 2008-02-06 2009-08-13 Novasaid Ab Low molecular weight 2,5-disubstituted thiophene derivatives and use thereof in therapy
US8129398B2 (en) 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
US8871753B2 (en) 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
TW201006816A (en) 2008-05-15 2010-02-16 Organon Nv Hexafluoroisopropanol derivatives
US20090325964A1 (en) 2008-05-23 2009-12-31 Wyeth Piperazine Metabotropic Glutamate Receptor 5 (MGLUR5) Negative Allosteric Modulators For Anxiety/Depression
WO2009151910A2 (en) 2008-05-25 2009-12-17 Wyeth Combination product of receptor tyrosine kinase inhibitor and fatty acid synthase inhibitor for treating cancer
EP2767537B1 (en) * 2008-08-06 2017-04-12 Medivation Technologies, Inc. Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
TW201022230A (en) 2008-08-28 2010-06-16 Organon Nv 1-(4-ureidobenzoyl)piperazine derivatives
EP2373315A4 (en) 2008-11-14 2012-06-27 Scripps Research Inst METHOD AND COMPOSITIONS RELATED TO TARGETING OF MONOACYLGLYCEROLLIPASE
US8580807B2 (en) 2009-04-03 2013-11-12 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as GPCR modulators for the treatment of obesity, diabetes and other metabolic disorders
US20120156138A1 (en) 2009-04-14 2012-06-21 Smith Larry J Methods and Compositions for the Treatment of Medical Conditions Involving Cellular Reprogramming
US8173650B2 (en) * 2009-05-27 2012-05-08 Genentech, Inc. Bicyclic pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use
CA2764526A1 (en) 2009-06-24 2010-12-29 Christine Kritikou The use of spinosyns and spinosyn compositions against diseases caused by protozoans, viral infections and cancer
WO2011035018A2 (en) 2009-09-18 2011-03-24 Fate Therapeutics, Inc. Suicide ready cells
US8716482B2 (en) 2009-09-25 2014-05-06 Merck Sharp & Dohme Corp. Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
JP5546636B2 (ja) 2009-09-28 2014-07-09 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ベンゾキセピンｐｉ３ｋ阻害剤化合物及び使用方法
TW201118081A (en) 2009-10-07 2011-06-01 Siena Biotech Spa Wnt pathway antagonists
WO2011056635A1 (en) 2009-10-27 2011-05-12 Glaxosmithkline Llc Benzimidazoles as fatty acid synthase inhibitors
AU2010313282A1 (en) 2009-10-30 2012-05-24 Ocera Therapeutics, Inc. Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
JP2013512245A (ja) 2009-11-24 2013-04-11 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 脂肪酸合成酵素阻害剤としてのアザベンズイミダゾール
JP5805672B2 (ja) 2010-02-22 2015-11-04 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 脂肪酸合成酵素阻害剤としてのトリアゾロン類
WO2011140296A1 (en) 2010-05-05 2011-11-10 Infinity Pharmaceuticals Triazoles as inhibitors of fatty acid synthase
EP3159331A1 (en) 2010-05-05 2017-04-26 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
BR112012032796A2 (pt) 2010-06-24 2016-11-22 Arisaph Pharmaceuticals Inc miméticos niacina, e os métodos de utilização dos mesmos
US8937063B2 (en) 2010-06-24 2015-01-20 Trustees Of Tufts College Niacin mimetics, and methods of use thereof
CA2806341C (en) 2010-07-29 2020-03-24 Rigel Pharmaceuticals, Inc. Ampk-activating heterocyclic compounds and methods for using the same
CN102372698A (zh) 2010-08-10 2012-03-14 江苏恒瑞医药股份有限公司 酞嗪酮类衍生物、其制备方法及其在医药上的应用
EP2615918A4 (en) 2010-09-17 2014-01-29 Glaxosmithkline Ip Dev Ltd INHIBITORS OF ACID GRAS SYNTHASE
WO2012037299A2 (en) 2010-09-17 2012-03-22 Glaxosmithkline Llc Fatty acid synthase inhibitors
US20130237535A1 (en) 2010-11-08 2013-09-12 Nicholas D. Adams Fatty acid synthase inhibitors
US20130345270A1 (en) * 2010-11-12 2013-12-26 Waake Forest University Health Sciences Methods of treating cancer and other disorders
PE20140913A1 (es) 2010-11-15 2014-08-22 Abbvie Inc Inhibidores de nampt y rock
CA2849207A1 (en) 2010-11-24 2012-05-31 Craig Townsend Methods of screening compounds that are cytotoxic to tumor cells and methods of treating tumor cells using such compounds
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
JP2014515345A (ja) 2011-01-10 2014-06-30 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 脂肪酸シンターゼ阻害剤としてのピリミジノン誘導体
WO2012101013A1 (en) 2011-01-28 2012-08-02 Boehringer Ingelheim International Gmbh Substituted pyridinyl-pyrimidines and their use as medicaments
AR086837A1 (es) 2011-03-08 2014-01-29 3 V Biosciences Inc Moduladores heterociclicos de sintesis lipidica
WO2012122391A1 (en) 2011-03-08 2012-09-13 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
EP2686305B1 (en) 2011-03-14 2020-09-16 Impact Therapeutics, Inc. Quinazolinediones and their use
TWI527800B (zh) 2011-04-01 2016-04-01 南京英派藥業有限公司 作為聚（二磷酸腺苷酸－核醣）聚合酶（ｐａｒｐ）之抑制劑之１－（芳基甲基）喹唑啉－２，４（１ｈ，３ｈ）－二酮及其應用
CA2834692A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
ME03074B (me) 2011-05-03 2019-01-20 Agios Pharmaceuticals Inc Akтivatori piruvat kinaze za upotrebu u terapiji
WO2013028495A1 (en) * 2011-08-19 2013-02-28 Biomarin Pharmaceutical Inc. Dihydropyridophthalazinone inhibitors of poly (adp-ribose) polymerase (parp) for the treatment of multiple myeloma
WO2013028445A1 (en) * 2011-08-19 2013-02-28 Glaxosmithkline Llc Fatty acid synthase inhibitors
JP2014525443A (ja) * 2011-08-30 2014-09-29 シーエイチディーアイ ファウンデーション，インコーポレーテッド キヌレニン−３−モノオキシゲナーゼインヒビター、医薬組成物、およびこれらの使用方法
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2771340B1 (en) 2011-10-25 2016-04-13 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9102631B2 (en) 2011-11-01 2015-08-11 Impact Therapeutics, Inc. 1-(arylmethyl)-5,6,7,8-tetrahydroquinazoline-2,4-diones and analogs and the use thereof
CN103130723B (zh) 2011-11-30 2015-01-14 成都地奥制药集团有限公司 一种多聚(adp-核糖)聚合酶抑制剂
CN102627610B (zh) 2012-04-11 2014-06-25 江苏先声药物研究有限公司 一类苯并咪唑类衍生物及其应用
US9096579B2 (en) 2012-04-20 2015-08-04 Boehringer Ingelheim International Gmbh Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
CN103420890B (zh) 2012-05-15 2015-06-24 天津药物研究院 3-吡咯甲酸衍生物及其制备方法和用途
AR092211A1 (es) * 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
EP3587406B1 (en) 2013-03-13 2021-01-27 Forma Therapeutics, Inc. 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-one derivatives and related compounds as fatty acid synthase (fasn) inhibitors for the treatment of cancer
CN105008329B (zh) 2013-03-21 2018-01-05 默克专利股份公司 作为fasn抑制剂的哌嗪衍生物
AU2014298959B2 (en) 2013-07-29 2018-04-05 Merck Patent Gmbh 1,3-disubstituted cyclopentane derivatives
BR112017027339A2 (pt) 2015-06-18 2018-09-04 Cephalon, Inc. derivados de piperidina 1,4-substituída
US10919875B2 (en) 2015-06-18 2021-02-16 89Bio Ltd Substituted 4-benzyl and 4-benzoyl piperidine derivatives
WO2017189613A1 (en) 2016-04-25 2017-11-02 Forma Therapeutics, Inc. Methods of using fasn inhibitors

Also Published As

Publication number Publication date
MX364895B (es) 2019-05-10
NI201500141A (es) 2016-02-16
RU2019111684A3 (es) 2019-11-28
SMT201900585T1 (it) 2019-11-13
NO20151329A1 (en) 2015-10-06
EP2968316A4 (en) 2016-09-21
RU2737434C2 (ru) 2020-11-30
US20190241532A1 (en) 2019-08-08
CA2905751A1 (en) 2014-10-09
US20200347025A1 (en) 2020-11-05
WO2014164767A1 (en) 2014-10-09
MY191366A (en) 2022-06-20
HRP20191860T1 (hr) 2019-12-27
CR20150541A (es) 2016-01-04
US10399951B2 (en) 2019-09-03
RU2015141772A (ru) 2017-04-19
LT2968316T (lt) 2019-10-25
SA515361086B1 (ar) 2021-06-01
CN105492008A (zh) 2016-04-13
MX2015012470A (es) 2016-06-28
RS59411B1 (sr) 2019-11-29
EP2968316B1 (en) 2019-08-07
US20160002188A1 (en) 2016-01-07
ZA201506922B (en) 2019-12-18
EP3587406A1 (en) 2020-01-01
PH12015502097A1 (en) 2016-01-11
BR112015023279A2 (pt) 2017-07-18
PL2968316T3 (pl) 2019-12-31
KR102194745B1 (ko) 2020-12-24
US20180050997A1 (en) 2018-02-22
AU2017268536A1 (en) 2017-12-21
AU2014249003A1 (en) 2015-10-15
CL2015002698A1 (es) 2016-08-19
PT2968316T (pt) 2019-10-29
US10800750B2 (en) 2020-10-13
ES2861180T3 (es) 2021-10-05
US10995078B2 (en) 2021-05-04
SG11201507486SA (en) 2015-10-29
US20190241533A1 (en) 2019-08-08
RU2019111684A (ru) 2019-06-11
RU2686323C2 (ru) 2019-04-25
SG10201707409PA (en) 2017-10-30
TN2015000420A1 (en) 2017-01-03
JP2016517412A (ja) 2016-06-16
IL241699B (en) 2021-09-30
WO2014164749A1 (en) 2014-10-09
ECSP15043280A (es) 2019-03-29
HK1220409A1 (en) 2017-05-05
EP3587406B1 (en) 2021-01-27
CN112521369A (zh) 2021-03-19
CN105492008B (zh) 2020-11-27
US10457655B2 (en) 2019-10-29
JP6790040B2 (ja) 2020-11-25
IL241699A0 (en) 2015-11-30
BR112015023279B1 (pt) 2021-01-19
PH12015502097B1 (en) 2023-02-03
PE20160122A1 (es) 2016-02-12
CY1122244T1 (el) 2020-11-25
ES2753386T3 (es) 2020-04-08
HUE045701T2 (hu) 2020-01-28
US10472342B2 (en) 2019-11-12
US20210214323A1 (en) 2021-07-15
SI2968316T1 (sl) 2019-11-29
ME03564B (me) 2020-07-20
US20180370933A1 (en) 2018-12-27
AU2017268536B2 (en) 2019-07-11
AU2019246753A1 (en) 2019-10-24
KR20150143479A (ko) 2015-12-23
CU20150120A7 (es) 2016-04-25
EP2968316A1 (en) 2016-01-20
US10450286B2 (en) 2019-10-22
US20200017458A1 (en) 2020-01-16
DK2968316T3 (da) 2019-10-07
JP2019048833A (ja) 2019-03-28
AU2019246753B2 (en) 2020-10-22

Similar Documents

Publication Publication Date Title
CU24341B1 (es) Compuestos y composiciones orgánicas inhibidores del ácido graso sintetasa (fasn) útiles para el tratamiento del cáncer, infecciones virales, obesidad y diabetes
MX2013002461A (es) Compuestos y composiciones novedosos para la inhibición de nampt.
IN2013MN02014A (es)
MX2013002358A (es) Compuestos y composiciones de guanidina para la inhibicion de nampt.
CR20200276A (es) Sulfamoilarilamidas y su uso como medicamentos para el tratamientos de la hepatitis b (divisional exp. 2015-0059)
CL2017002483A1 (es) Compuestos heterocíclicos como inhibidores de lsd1
EA201691625A1 (ru) Ароматические гетероциклические соединения как противовоспалительные соединения
BR112014030365A2 (pt) síntese de composto antiviral
CL2017000786A1 (es) Compuestos de heteroarilo como inhibidores de tirosina-cinasa de bruton (btk) y usos de estos.
GT201200230A (es) Inhibidores del virus de la hepatitis c
CO2017013229A2 (es) Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril)piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares
MX2013012760A (es) Nuevos compuestos y composiciones para la inhibicion de nampt.
MX2018003130A (es) Compuestos de heteroarilo como inhibidores de cinasas asociadas a receptor de interleucina-1 (irak) y usos de los mismos.
MX377552B (es) Proceso para preparar un compuesto antiviral de formula i.
BR112014030473A2 (pt) novo diazaespirocicloalcano e azaespirocicloalcano
BR112016028773A2 (pt) processos para preparação de compostos antivirais
AR124083A2 (es) Nuevo inhibidor de sglt1
MX2016007186A (es) Nuevo procedimiento de sintesis de la agomelatina.
MX2020009462A (es) Procesos para la preparación de compuestos de pirimidinilciclopentano.
IN2015DN02514A (es)
PH12016500788A1 (en) Compounds for the treatment of diabetes and disease complications arising from same
NZ751449A (en) Novel compounds and compositions for inhibition of fasn
MA38839B1 (fr) Composés et compositions utiles comme inhibiteurs de mek
CU20110012A7 (es) Derivados de heteroarilo como inhibidores de dgat1