CR20150487A - Compuestos de biaril-amida como inhibidores de cinasa - Google Patents

Compuestos de biaril-amida como inhibidores de cinasa

Info

Publication number
CR20150487A
CR20150487A CR20150487A CR20150487A CR20150487A CR 20150487 A CR20150487 A CR 20150487A CR 20150487 A CR20150487 A CR 20150487A CR 20150487 A CR20150487 A CR 20150487A CR 20150487 A CR20150487 A CR 20150487A
Authority
CR
Costa Rica
Prior art keywords
compounds
biaril
cinasa
inhibitors
amida
Prior art date
Application number
CR20150487A
Other languages
English (en)
Spanish (es)
Inventor
Robert Aversa
Paul A Barsanti
Matthew Burger
Michael Patrick Dillon
Alan Dipesa
Cheng Hu
Yan Lou
Gisele Nishiguchi
Yue Pan
Valery Polyakov
Savithri Ramurthy
Alice Rico
Lina Setti
Aaron Smith
Sharadha Subramanian
Benjamin Taft
Huw Tanner
Lifeng Wan
Naeem Yusuff
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of CR20150487A publication Critical patent/CR20150487A/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D213/81—Amides; Imides
    • 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
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • C07D237/10—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 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
    • C07D237/20—Nitrogen 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
    • C07D237/10—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 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
    • C07D237/22—Nitrogen and 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
    • C07D237/10—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 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
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • 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
    • C07D491/08—Bridged 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CR20150487A 2013-03-14 2015-09-14 Compuestos de biaril-amida como inhibidores de cinasa CR20150487A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361783558P 2013-03-14 2013-03-14
PCT/US2014/026107 WO2014151616A1 (en) 2013-03-14 2014-03-13 Biaryl amide compounds as kinase inhibitors

Publications (1)

Publication Number Publication Date
CR20150487A true CR20150487A (es) 2016-01-29

Family

ID=50391541

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20150487A CR20150487A (es) 2013-03-14 2015-09-14 Compuestos de biaril-amida como inhibidores de cinasa

Country Status (45)

Country Link
US (4) US9242969B2 (enExample)
EP (2) EP3299367B1 (enExample)
JP (3) JP6360879B2 (enExample)
KR (1) KR102059545B1 (enExample)
CN (2) CN108467369B (enExample)
AP (1) AP2015008632A0 (enExample)
AR (1) AR095312A1 (enExample)
AU (1) AU2014233657B2 (enExample)
BR (1) BR112015020008B1 (enExample)
CA (1) CA2899967C (enExample)
CL (1) CL2015002151A1 (enExample)
CR (1) CR20150487A (enExample)
CU (1) CU24351B1 (enExample)
CY (1) CY1119707T1 (enExample)
DK (1) DK2970216T3 (enExample)
DO (1) DOP2015000241A (enExample)
EA (1) EA028194B1 (enExample)
EC (1) ECSP15042895A (enExample)
ES (2) ES2657900T3 (enExample)
GE (1) GEP201706692B (enExample)
GT (1) GT201500294A (enExample)
HR (1) HRP20180158T1 (enExample)
HU (1) HUE035932T2 (enExample)
IL (1) IL241165B (enExample)
JO (1) JOP20140104B1 (enExample)
LT (1) LT2970216T (enExample)
MA (1) MA38398B1 (enExample)
MX (1) MX373307B (enExample)
NI (1) NI201500120A (enExample)
NO (1) NO3013169T3 (enExample)
NZ (1) NZ710835A (enExample)
PE (1) PE20160875A1 (enExample)
PH (1) PH12015502116B1 (enExample)
PL (1) PL2970216T3 (enExample)
PT (1) PT2970216T (enExample)
RS (1) RS56774B1 (enExample)
SG (1) SG11201506196SA (enExample)
SI (1) SI2970216T1 (enExample)
SV (1) SV2015005066A (enExample)
TN (1) TN2015000332A1 (enExample)
TW (1) TWI662025B (enExample)
UA (1) UA116644C2 (enExample)
UY (1) UY35398A (enExample)
WO (1) WO2014151616A1 (enExample)
ZA (1) ZA201505438B (enExample)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105050602B (zh) * 2013-01-12 2018-05-25 张大为 作为pi3激酶抑制剂的吡啶化合物
EP3321266A1 (en) 2013-03-14 2018-05-16 Janssen Pharmaceutica NV P2x7 modulators
TWI644671B (zh) 2013-03-14 2018-12-21 比利時商健生藥品公司 Ｐ２ｘ７調節劑
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
MX363936B (es) 2013-03-14 2019-04-09 Boehringer Ingelheim Int (bencil-ciano-metil)-amidas del acido 2-aza-biciclo[2.2.1]heptano- 3-carboxilico sustituidas como inhibidores de catepsina c.
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
ES2689526T3 (es) 2013-03-14 2018-11-14 Janssen Pharmaceutica Nv Moduladores de P2X7
LT3057586T (lt) 2013-10-18 2020-03-10 Celgene Quanticel Research, Inc. Bromodomeno inhibitoriai
US10202373B2 (en) 2014-01-14 2019-02-12 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
MX2016009135A (es) 2014-01-14 2016-10-05 Millennium Pharm Inc Heteroarilos y usos de estos.
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
KR20240110004A (ko) 2014-03-14 2024-07-12 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
US20180118749A1 (en) 2014-09-12 2018-05-03 Janssen Pharmaceutica Nv P2x7 modulators
AU2015315687B2 (en) 2014-09-12 2019-07-11 Janssen Pharmaceutica Nv P2X7 modulators
RS59444B1 (sr) 2014-09-12 2019-11-29 Boehringer Ingelheim Int Spirociklični inhibitori katepsina c
JP6636014B2 (ja) * 2014-09-12 2020-01-29 ノバルティス アーゲー Ｒａｆキナーゼ阻害剤としての化合物および組成物
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
KR102513870B1 (ko) 2014-10-14 2023-03-23 노파르티스 아게 Pd-l1에 대한 항체 분자 및 그의 용도
US20170340733A1 (en) 2014-12-19 2017-11-30 Novartis Ag Combination therapies
CN107530415A (zh) 2015-03-10 2018-01-02 艾杜罗生物科技公司 用于活化“干扰素基因刺激物”依赖性信号传导的组合物和方法
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
WO2017019897A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to tim-3
PT3317301T (pt) 2015-07-29 2021-07-09 Novartis Ag Terapias de associação compreendendo moléculas de anticorpo contra lag-3
CN105153190B (zh) * 2015-08-21 2017-07-21 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶类化合物及其制备方法和应用
MX382526B (es) 2015-10-23 2025-03-13 Array Biopharma Inc Compuestos de 2-piridazin-3(2h)-ona 2-aril sustituidas y 2-heteroaril sustituidas como inhibidores de las tirosina quinasas fgfr
RS63125B1 (sr) 2015-11-03 2022-05-31 Janssen Biotech Inc Antitela koja se specifično vezuju za pd-1 i njihova upotreba
US20180371093A1 (en) 2015-12-17 2018-12-27 Novartis Ag Antibody molecules to pd-1 and uses thereof
CN107021963A (zh) * 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
SI3416945T1 (sl) * 2016-02-19 2020-11-30 Sprint Bioscience Ab Spojine 6-aril-4-(morfolin-4-IL)-1H-piridin-2-ona, uporabne za zdravljenje raka in diabetesa
JP6858984B2 (ja) * 2016-02-19 2021-04-14 スプリント バイオサイエンス アクティエボラーグ がんおよび糖尿病の治療に有用な６−ヘテロシクリル−４−モルホリン−４−イルピリジン−２−オン化合物
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
US20190175609A1 (en) * 2016-06-10 2019-06-13 Novartis Ag Therapeutic uses of a c-raf inhibitor
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
CN106831812B (zh) * 2016-08-09 2019-09-20 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶或吡嗪类化合物及其应用
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
IL292977A (en) 2016-09-09 2022-07-01 Incyte Corp Pyrazolopyridine derivatives as modulators of hpk1 and their use in cancer therapy
TW201811799A (zh) 2016-09-09 2018-04-01 美商英塞特公司 吡唑并嘧啶化合物及其用途
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
WO2018051306A1 (en) * 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
CN110167928A (zh) 2016-12-22 2019-08-23 勃林格殷格翰国际有限公司 作为sos1抑制剂的新型经苄基氨基取代的喹唑啉和衍生物
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
CN106866547B (zh) * 2017-03-15 2020-11-10 江苏省农用激素工程技术研究中心有限公司 2-乙氧基-4,6-二氯嘧啶的合成方法
AU2018258581A1 (en) * 2017-04-28 2019-11-07 Quartz Therapeutics, Inc. RAF-degrading conjugate compounds
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
EP4272740A1 (en) * 2017-05-02 2023-11-08 Novartis AG Combination therapy comprising a raf inhibitor and trametinib
US20200172628A1 (en) 2017-06-22 2020-06-04 Novartis Ag Antibody molecules to cd73 and uses thereof
JP2020529411A (ja) * 2017-08-03 2020-10-08 ノバルティス アーゲー 第三世代ｅｇｆｒチロシンキナーゼ阻害剤とｒａｆ阻害剤の治療用組合せ
CN109384782A (zh) * 2017-08-04 2019-02-26 厦门大学 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
PL3728254T3 (pl) 2017-12-21 2023-06-12 Boehringer Ingelheim International Gmbh Benzyloaminopodstawione pirydopirymidynony i pochodne jako inhibitory sos1
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
WO2019164847A1 (en) 2018-02-20 2019-08-29 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (en) 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US12133841B2 (en) * 2018-05-22 2024-11-05 Js Innomed Holdings Ltd. Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Ｅｎｔｐｄ２抗體、組合療法、及使用該等抗體和組合療法之方法
CN108863884B (zh) * 2018-07-26 2020-07-03 南京富润凯德生物医药有限公司 一种用dast试剂作为消除试剂合成共轭硝基烯取代系列衍生物的方法
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
US12054488B2 (en) 2018-09-27 2024-08-06 Suzhou Raymon Pharmaceuticals Company, Ltd. Pyrazolopyrimidine compound and preparation method therefor and use thereof in preparation of anti-cancer drug
EP3856179A1 (en) 2018-09-28 2021-08-04 Janssen Pharmaceutica N.V. Monoacylglycerol lipase modulators
PE20211773A1 (es) 2018-09-28 2021-09-08 Janssen Pharmaceutica Nv Moduladores de monoacilglicerol lipasa
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
EP3897591A1 (en) 2018-12-20 2021-10-27 Novartis AG Combination therapy with a raf inhibitor and a cdk4/6 inhibitor for use in the treatment of cancer
AU2020244761A1 (en) * 2019-03-22 2021-11-11 Kinnate Biopharma Inc. Inhibitors of RAF kinases
US10927111B2 (en) 2019-05-03 2021-02-23 Kinnate Biopharma Inc. Inhibitors of RAF kinases
JP2022531969A (ja) * 2019-05-13 2022-07-12 ノバルティス アーゲー 癌を治療するためのＲａｆ阻害剤としてのＮ－（３－（２－（２－ヒドロキシエトキシ）－６－モルホリノピリジン－４－イル）－４－メチルフェニル）－２－（トリフルオロメチル）イソニコチンアミドの新規な結晶形態
AU2020326703A1 (en) 2019-08-06 2022-02-17 Incyte Corporation Solid forms of an HPK1 inhibitor
WO2021027943A1 (zh) * 2019-08-14 2021-02-18 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
US10702525B1 (en) 2019-09-04 2020-07-07 United Arab Emirates University Pyrimidine derivatives as anti-diabetic agents
EP4031578A1 (en) 2019-09-18 2022-07-27 Novartis AG Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
KR20220075386A (ko) 2019-09-30 2022-06-08 얀센 파마슈티카 엔.브이. 방사성 표지된 mgl pet 리간드
IL292424A (en) 2019-10-24 2022-06-01 Kinnate Biopharma Inc Inhibitors of raf kinases
JP7214925B2 (ja) * 2019-12-06 2023-01-30 メッドシャイン ディスカバリー インコーポレイテッド Ｐａｎ－ＲＡＦキナーゼ阻害剤としてのビアリール化合物
EP4106756A1 (en) 2020-02-18 2022-12-28 Novartis AG Therapeutic combinations comprising a raf inhibitor for use in treating braf mutant nsclc
TW202146024A (zh) 2020-02-28 2021-12-16 瑞士商諾華公司 包含達拉菲尼、erk抑制劑和raf抑制劑或pd-1抑制劑之三重藥物組合
EP4126860A1 (en) 2020-03-26 2023-02-08 Janssen Pharmaceutica NV Monoacylglycerol lipase modulators
EP4149472A1 (en) 2020-05-12 2023-03-22 Novartis AG Therapeutic combinations comprising a craf inhibitor
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN113912591B (zh) * 2020-07-08 2023-10-20 齐鲁制药有限公司 联芳基化合物
CN111995623A (zh) * 2020-08-18 2020-11-27 上海毕得医药科技有限公司 一种7-溴-4-氯-1-甲基-1H-咪唑并[4,5-c]吡啶的合成方法
WO2022043955A1 (en) 2020-08-31 2022-03-03 Novartis Ag Combination therapy of a raf inhibitor and a mek inhibitor for the treatment of sarcoma
US11407737B2 (en) 2020-09-18 2022-08-09 Kinnate Biopharma Inc. Inhibitors of RAF kinases
WO2022081469A1 (en) * 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibitors of raf kinases
EP4237423B1 (en) 2020-11-02 2024-12-11 Boehringer Ingelheim International GmbH Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors
US12414955B2 (en) 2020-11-25 2025-09-16 Deciphera Pharmaceuticals, Llc Anti-viral activity of VPS34 inhibitors
AU2021409816A1 (en) 2020-12-22 2023-07-06 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
CN114591324B (zh) * 2021-03-30 2023-05-05 深圳微芯生物科技股份有限公司 一类吡嗪酮衍生物、其制备及其应用
IL307908A (en) * 2021-04-23 2023-12-01 Kinnate Biopharma Inc Cancer treatment with a RAF inhibitor
IL307910A (en) * 2021-04-23 2023-12-01 Kinnate Biopharma Inc Solid state forms of (S)-N-(3-(2-(((R)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-methylphenyl)-3-( 2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and its salts
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
WO2022253334A1 (zh) * 2021-06-04 2022-12-08 南京明德新药研发有限公司 一种raf激酶抑制剂的晶型及其制备方法
CA3237812A1 (en) * 2021-11-12 2023-05-19 Biopolar Youtang (Guangdong) Pharmaceutical Co., Ltd. Drak2 inhibitor, and preparation method therefor and use thereof
CN118574836A (zh) 2021-12-01 2024-08-30 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-胺基-3-氰基噻吩及衍生物
CN118613485A (zh) 2021-12-01 2024-09-06 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
PE20241356A1 (es) 2021-12-01 2024-07-03 Boehringer Ingelheim Int Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cancer
US20250313553A1 (en) 2021-12-01 2025-10-09 Boehringer Ingelheim Int'l GmbH Corp. Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4441053A1 (en) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4441051A1 (en) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
IL313417A (en) * 2021-12-09 2024-08-01 Deciphera Pharmaceuticals Llc Anti-RAF kinases and methods of using them
EP4452975A1 (en) 2021-12-23 2024-10-30 Boehringer Ingelheim International GmbH 8-aza quinazolines as brain-penetrant sos1-inhibitors
EP4472968A1 (en) * 2022-02-03 2024-12-11 Pierre Fabre Medicament Inhibitors of raf kinases
CN115947691B (zh) * 2022-03-01 2024-08-16 四川大学 哒嗪砜类衍生物及其用途
US20250179584A1 (en) 2022-03-02 2025-06-05 Novartis Ag Precision therapy for the treatment of cancer
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Ｍｅｋ抑制劑及其用途
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
CA3264293A1 (en) 2022-08-10 2024-02-15 Novartis Ag AMORPHIC SOLID DISPERSIONS COMPRISING NAPORAFENIB
IL320222A (en) 2022-10-26 2025-06-01 Boehringer Ingelheim Int Heterocyclic compounds capable of activating STING
US20240174642A1 (en) 2022-10-26 2024-05-30 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
AU2023370123A1 (en) 2022-10-26 2025-04-17 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
TW202440574A (zh) 2023-02-09 2024-10-16 印度商薩蒂亞製藥創新私人有限公司 作為ｐｋｍｙｔ１抑制劑的雜芳基化合物
WO2024220470A1 (en) 2023-04-17 2024-10-24 Ikena Oncology, Inc. Tead inhibitors and uses thereof in the treatment of proliferative disorders
US20250019385A1 (en) 2023-05-30 2025-01-16 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2024263460A1 (en) * 2023-06-13 2024-12-26 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
AU2024302328A1 (en) * 2023-06-13 2025-11-27 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2024258919A1 (en) * 2023-06-13 2024-12-19 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025032214A1 (en) * 2023-08-09 2025-02-13 Pierre Fabre Medicament Indazole compounds and azaindazole compounds as inhibitors of raf kinases
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
WO2025137105A1 (en) * 2023-12-22 2025-06-26 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
US20250313560A1 (en) 2024-04-03 2025-10-09 Boehringer Ingelheim International Gmbh Novel bicyclic benzylamido pyridine derivatives as SOS1 inhibitors

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
DE3029376A1 (de) 1980-07-31 1982-03-18 Nepera Chemical Co. Inc., Harriman, N.Y. Verfahren zur herstellung von 2,4,5-tris-pyridylimidazolen
DE3486009T2 (de) 1983-09-09 1993-04-15 Takeda Chemical Industries Ltd 5-pyridyl-1,3-thiazol-derivate, ihre herstellung und anwendung.
JP2722586B2 (ja) 1989-01-13 1998-03-04 大正製薬株式会社 インドリルイミダゾール誘導体
JP2808460B2 (ja) 1989-11-16 1998-10-08 大正製薬株式会社 イミダゾール誘導体
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
WO1998008845A1 (en) 1996-08-27 1998-03-05 Novartis Ag Herbicidal s-substituted 1,2,4,6-thiatriazines
CA2282439C (en) 1997-03-05 2010-05-04 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
GB9711650D0 (en) 1997-06-05 1997-07-30 Pfizer Ltd Compounds useful in therapy
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6211177B1 (en) 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
ATE231143T1 (de) 1999-04-09 2003-02-15 Smithkline Beecham Corp Triarylimidazole
CN101481359A (zh) 1999-04-15 2009-07-15 布里斯托尔-迈尔斯斯奎布公司 环状蛋白酪氨酸激酶抑制剂
JP2000302680A (ja) 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
ES2270867T3 (es) 1999-09-23 2007-04-16 Astrazeneca Ab Compuestos de quinazolina terapeuticos.
CA2395564A1 (en) 1999-11-22 2001-05-31 Smithkline Beecham Plc Novel compounds
HK1053984B (zh) 2000-01-18 2006-07-28 沃泰克斯药物股份有限公司 回旋酶抑制剂及其用途
AU2001232809A1 (en) 2000-01-18 2001-07-31 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
ES2218391T3 (es) 2000-03-06 2004-11-16 Smithkline Beecham Plc Derivados de imidazol como inhibidores de raf-cinasa.
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
US7495018B2 (en) 2000-03-30 2009-02-24 Takeda Pharmaceutical Company Limited Substituted 1,3-thiazole compounds, their production and use
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
EP2177520A1 (en) 2000-06-12 2010-04-21 Eisai R&D Management Co., Ltd. 1,5-Di(aryl or heteroaryl)-3-halo-2(1H)-pyridones as intermediates for the preparation of AMPA receptor inhibitors
WO2002042273A2 (en) 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
ATE365730T1 (de) 2000-11-20 2007-07-15 Smithkline Beecham Corp Neuartige verbindungen
EP1341771A2 (en) 2000-11-29 2003-09-10 Glaxo Group Limited Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors
DE60215139T2 (de) 2001-01-26 2007-08-16 Chugai Seiyaku K.K. Malonyl coa-decarboxylase inhibitoren als stoffwechselmodulatoren
CA2437248A1 (en) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Jnk inhibitor
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
MXPA04009541A (es) 2002-03-29 2005-01-25 Chiron Corp Benzazoles sustituidos y uso de los mismos como inhibidores de cinasa raf.
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
CA2498047C (en) 2002-09-18 2009-05-19 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
HRP20050250A2 (en) 2002-09-18 2005-10-31 Pfizer Products Inc. Novel triazole and oxazole compounds as transforming growth factor (tfg) inhibitor
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
CN1863774B (zh) 2003-10-08 2010-12-15 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
WO2005037273A1 (en) 2003-10-16 2005-04-28 Chiron Corporation Substituted benzazoles and use thereof as inhibitors of raf kinase
US8969372B2 (en) 2003-11-14 2015-03-03 Aptose Boisciences Inc. Aryl imidazoles and their use as anti-cancer agents
RU2367661C2 (ru) 2004-03-05 2009-09-20 Тайсо Фармасьютикал Ко., Лтд. Производные тиазола
KR100749566B1 (ko) 2004-04-21 2007-08-16 이화여자대학교 산학협력단 Ａｌｋ5 및/또는 ａｌｋ4 억제제로 유효한 2-피리딜이치환된 이미다졸 유도체
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
PE20060315A1 (es) 2004-05-24 2006-05-15 Irm Llc Compuestos de tiazol como moduladores de ppar
KR20070028536A (ko) * 2004-06-15 2007-03-12 아스트라제네카 아베 항암제로서의 치환된 퀴나졸론
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
GB0415367D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
JP2008511631A (ja) 2004-08-31 2008-04-17 バイオジェン・アイデック・エムエイ・インコーポレイテッド ＴＧＦ−βインヒビターとしてのピリミジニルイミダゾール
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
AU2005295734A1 (en) 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Methods of treating vascular injuries
GB0524814D0 (en) * 2005-12-05 2006-01-11 Glaxo Group Ltd Compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
JP2007246520A (ja) 2006-02-15 2007-09-27 Takeda Yuichiro Ｒａｇｅ阻害剤
BRPI0708813A2 (pt) * 2006-03-17 2011-05-24 Wyeth Corp composto; composição; método de tratamento, inibição do crescimento ou erradicaçõ de neoplasias em um mamìfero necessitado; método de tratamento dse cáncer em um mamìfero necessitado; e mistura
EP2007393B1 (en) 2006-04-07 2013-08-21 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
SI2050749T1 (en) 2006-08-08 2018-04-30 Chugai Seiyaku Kabushiki Kaisha DERIVAT PYRIMIDINE AS A PI3K INHIBITOR AND ITS USE
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
SI2170848T1 (sl) 2007-06-27 2015-01-30 Astrazeneca Ab Derivati pirazinona in njihova uporaba pri zdravljenju bolezni pljuč
JP2010532381A (ja) 2007-06-29 2010-10-07 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用な複素環式化合物
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
EP2176249A2 (en) * 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
WO2009007749A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
RU2474580C2 (ru) 2007-07-19 2013-02-10 Шеринг Корпорейшн Гетероциклические амидные соединения как ингибиторы протеинкиназ
WO2009032667A1 (en) 2007-08-29 2009-03-12 Smithkline Beecham Corporation Thiazole and oxazole kinase inhibitors
UY31322A1 (es) 2007-09-05 2009-04-30 Amidas heterocíclicas y sus métodos de uso-975
WO2009047163A1 (en) 2007-10-10 2009-04-16 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
CA2718936A1 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
US20110144107A1 (en) 2008-06-11 2011-06-16 Irm Llc Compounds and compositions useful for the treatment of malaria
CN102131805A (zh) * 2008-06-20 2011-07-20 百时美施贵宝公司 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物
PT2324008E (pt) 2008-07-24 2012-06-25 Nerviano Medical Sciences Srl 3,4-diarilpirazoles como inibidores da proteína quinase
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
CN102300862B (zh) 2008-12-19 2016-11-23 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
CN102471310A (zh) 2009-09-04 2012-05-23 诺瓦提斯公司 用于治疗增生性疾病的联吡啶化合物
EP2498608A4 (en) 2009-11-10 2013-04-24 Glaxosmithkline Llc BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS
JP5794922B2 (ja) 2009-12-28 2015-10-14 一般社団法人ファルマバレープロジェクト支援機構 １，３，４−オキサジアゾール−２−カルボキサミド化合物
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
EP2585454A1 (en) 2010-06-25 2013-05-01 Novartis AG Heteroaryl compounds and compositions as protein kinase inhibitors
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
SI2672967T1 (sl) 2011-02-07 2018-12-31 Plexxikon Inc. Spojine in postopki za kinazno modulacijo in indikacije zanjo
WO2012125981A2 (en) * 2011-03-17 2012-09-20 Selexagen Therapeutics, Inc. Raf kinase inhibitors
WO2013022766A1 (en) 2011-08-05 2013-02-14 Flynn Gary A Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
WO2013033167A1 (en) 2011-09-01 2013-03-07 Irm Llc Compounds and compositions as c-kit kinase inhibitors
AU2012311458B2 (en) 2011-09-21 2016-02-04 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mTOR inhibitors
CA2871270A1 (en) 2012-05-02 2013-11-07 Lupin Limited Substituted pyridine compounds as crac modulators
KR20150020169A (ko) 2012-05-15 2015-02-25 노파르티스 아게 Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체
TW201414704A (zh) 2012-07-02 2014-04-16 Biogen Idec Inc 作爲ＲＯＲ－γ受體之反向促效劑之含聯芳化合物
WO2014058691A1 (en) 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
WO2016038583A1 (en) 2014-09-12 2016-03-17 Novartis Ag Compounds and compositions as kinase inhibitors
JP6636014B2 (ja) 2014-09-12 2020-01-29 ノバルティス アーゲー Ｒａｆキナーゼ阻害剤としての化合物および組成物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa

Also Published As

Publication number Publication date
DK2970216T3 (da) 2018-01-29
AR095312A1 (es) 2015-10-07
US20160038504A1 (en) 2016-02-11
MA38398A1 (fr) 2018-02-28
AP2015008632A0 (en) 2015-08-31
AU2014233657B2 (en) 2016-08-04
CY1119707T1 (el) 2018-06-27
TN2015000332A1 (en) 2017-01-03
CN105143209B (zh) 2018-03-13
ECSP15042895A (es) 2019-08-30
CU24351B1 (es) 2018-06-05
AU2014233657A1 (en) 2015-08-27
PH12015502116A1 (en) 2016-01-25
NO3013169T3 (enExample) 2018-04-14
HRP20180158T1 (hr) 2018-03-09
RS56774B1 (sr) 2018-04-30
NI201500120A (es) 2015-11-18
CU20150118A7 (es) 2016-03-31
GEP201706692B (en) 2017-06-26
EA028194B1 (ru) 2017-10-31
US10245267B2 (en) 2019-04-02
EP2970216A1 (en) 2016-01-20
CL2015002151A1 (es) 2015-12-18
US10709712B2 (en) 2020-07-14
US9694016B2 (en) 2017-07-04
IL241165B (en) 2019-03-31
US20170260207A1 (en) 2017-09-14
CN108467369A (zh) 2018-08-31
WO2014151616A1 (en) 2014-09-25
SG11201506196SA (en) 2015-09-29
HUE035932T2 (en) 2018-05-28
ES2657900T3 (es) 2018-03-07
UA116644C2 (uk) 2018-04-25
EP3299367A1 (en) 2018-03-28
ZA201505438B (en) 2016-03-30
KR20150133214A (ko) 2015-11-27
CA2899967C (en) 2022-01-18
EP3299367B1 (en) 2019-12-25
KR102059545B1 (ko) 2019-12-26
CN105143209A (zh) 2015-12-09
CA2899967A1 (en) 2014-09-25
JOP20140104B1 (ar) 2021-08-17
LT2970216T (lt) 2018-01-10
PE20160875A1 (es) 2016-09-08
UY35398A (es) 2014-10-31
BR112015020008B1 (pt) 2021-05-11
JP6360879B2 (ja) 2018-07-18
NZ710835A (en) 2016-08-26
JP2020143117A (ja) 2020-09-10
US9242969B2 (en) 2016-01-26
JP6738369B2 (ja) 2020-08-12
GT201500294A (es) 2018-11-27
DOP2015000241A (es) 2015-12-15
MX373307B (es) 2020-04-16
US20140275003A1 (en) 2014-09-18
BR112015020008A2 (pt) 2017-07-18
SV2015005066A (es) 2018-06-12
JP7088983B2 (ja) 2022-06-21
EA201591727A1 (ru) 2016-05-31
MA38398B1 (fr) 2018-09-28
CN108467369B (zh) 2021-08-20
US20190175606A1 (en) 2019-06-13
PL2970216T3 (pl) 2018-04-30
JP2018150319A (ja) 2018-09-27
PH12015502116B1 (en) 2018-08-22
EP2970216B1 (en) 2017-11-01
MX2015012290A (es) 2015-12-16
ES2779673T3 (es) 2020-08-18
PT2970216T (pt) 2018-01-19
SI2970216T1 (en) 2018-01-31
IL241165A0 (en) 2015-11-30
TWI662025B (zh) 2019-06-11
TW201443021A (zh) 2014-11-16
JP2016517417A (ja) 2016-06-16
HK1212692A1 (en) 2016-06-17

Similar Documents

Publication Publication Date Title
CR20150487A (es) Compuestos de biaril-amida como inhibidores de cinasa
DOP2017000066A (es) Compuestos y composiciones como inhibidores de quinasa raf
CU20160052A7 (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
NI201400089A (es) COMPUESTOS DE OXAZOLIDIN - 2 - ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
NI201600058A (es) Compuestos derivados de piridilo bicíclicos fusionados a anillo como inhibidores de fgfr4
CR20150472A (es) USO DE DERIVADOS DE PIRAZOLOPIRIMIDINA PARA EL TRATAMIENTO DE TRANSTORNOS RELACIONADOS CON LA PI3Kd
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
UY35663A (es) Derivados de piperidinil-indol como inhibidores del factor de complemento b y usos de los mismos
MX374452B (es) Inhibidores de glucosilceramida sintasa para el tratamiento de enfermedades.
CR20150425A (es) Compuestos azabencimidazol como inhibidores de las isozimas pde4, para el tratamiento del sistema nervioso central y otros desórdenes
CR20150248A (es) Derivados de oxazolidin-2-ona-pirimidina
UY36875A (es) Composiciones inhibidoras de bromodominios para el tratamiento de diversas enfermedades
CL2017000827A1 (es) Inhibidores de aldosterona sintasa
CU20140107A7 (es) Derivados macrocíclicos para el tratamiento de enfermedades
AR132461A2 (es) Derivados de piperidinil-indol como inhibidores del factor de complemento b y usos de los mismos
CR20160175A (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
CU20140102A7 (es) Compuestos de oxazolidin-2- ona y usos de los mismos como inhibidores de la p13ks
UY35672A (es) Derivados de amino-metil-biarilo como inhibidores del factor de complemento d y usos de los mismos