CU24351B1 - Compuestos de biaril-amida como inhibidores de cinasa - Google Patents

Compuestos de biaril-amida como inhibidores de cinasa

Info

Publication number
CU24351B1
CU24351B1 CUP2015000118A CU20150118A CU24351B1 CU 24351 B1 CU24351 B1 CU 24351B1 CU P2015000118 A CUP2015000118 A CU P2015000118A CU 20150118 A CU20150118 A CU 20150118A CU 24351 B1 CU24351 B1 CU 24351B1
Authority
CU
Cuba
Prior art keywords
compounds
biaril
cinasa
inhibitors
amida
Prior art date
Application number
CUP2015000118A
Other languages
English (en)
Other versions
CU20150118A7 (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 C 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 CU20150118A7 publication Critical patent/CU20150118A7/es
Publication of CU24351B1 publication Critical patent/CU24351B1/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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • 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)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

<p>La presente invención proporciona compuestos de la fórmula (I)</p> <p>ESPACIO PARA FORMULA I</p> <p>como se describen en la presente y las sales de los mismos y los usos terapéuticos de estos compuestos para el tratamiento de los trastornos asociados con la actividad de cinasa Raf. La invención proporciona además composiciones farmacéuticas que comprenden estos compuestos y composiciones que comprenden estos compuestos y un co-agente terapéutico.</p>
CUP2015000118A 2013-03-14 2014-03-13 Compuestos de biaril-amida como inhibidores de cinasa CU24351B1 (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 (2)

Publication Number Publication Date
CU20150118A7 CU20150118A7 (es) 2016-03-31
CU24351B1 true CU24351B1 (es) 2018-06-05

Family

ID=50391541

Family Applications (1)

Application Number Title Priority Date Filing Date
CUP2015000118A CU24351B1 (es) 2013-03-14 2014-03-13 Compuestos de biaril-amida como inhibidores de cinasa

Country Status (46)

Country Link
US (4) US9242969B2 (es)
EP (2) EP3299367B1 (es)
JP (3) JP6360879B2 (es)
KR (1) KR102059545B1 (es)
CN (2) CN105143209B (es)
AP (1) AP2015008632A0 (es)
AR (1) AR095312A1 (es)
AU (1) AU2014233657B2 (es)
BR (1) BR112015020008B1 (es)
CA (1) CA2899967C (es)
CL (1) CL2015002151A1 (es)
CR (1) CR20150487A (es)
CU (1) CU24351B1 (es)
CY (1) CY1119707T1 (es)
DK (1) DK2970216T3 (es)
DO (1) DOP2015000241A (es)
EA (1) EA028194B1 (es)
EC (1) ECSP15042895A (es)
ES (2) ES2657900T3 (es)
GE (1) GEP201706692B (es)
GT (1) GT201500294A (es)
HK (1) HK1212692A1 (es)
HR (1) HRP20180158T1 (es)
HU (1) HUE035932T2 (es)
IL (1) IL241165B (es)
JO (1) JOP20140104B1 (es)
LT (1) LT2970216T (es)
MA (1) MA38398B1 (es)
MX (1) MX2015012290A (es)
NI (1) NI201500120A (es)
NO (1) NO3013169T3 (es)
NZ (1) NZ710835A (es)
PE (1) PE20160875A1 (es)
PH (1) PH12015502116B1 (es)
PL (1) PL2970216T3 (es)
PT (1) PT2970216T (es)
RS (1) RS56774B1 (es)
SG (1) SG11201506196SA (es)
SI (1) SI2970216T1 (es)
SV (1) SV2015005066A (es)
TN (1) TN2015000332A1 (es)
TW (1) TWI662025B (es)
UA (1) UA116644C2 (es)
UY (1) UY35398A (es)
WO (1) WO2014151616A1 (es)
ZA (1) ZA201505438B (es)

Families Citing this family (112)

* 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
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
WO2014152537A1 (en) 2013-03-14 2014-09-25 Janssen Pharmaceutica Nv P2x7 modulators
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
AP2015008601A0 (en) 2013-03-14 2015-07-31 Boehringer Ingelheim Int Substituted 2-aza-bicyclo[2.2.1] heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
US9604982B2 (en) 2013-03-14 2017-03-28 Janssen Pharmaceutica Nv P2X7 modulators
HUE048371T2 (hu) 2013-10-18 2020-07-28 Celgene Quanticel Res Inc Bromodomén inhibitorok
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
AU2015206652A1 (en) * 2014-01-14 2016-08-04 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
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
AU2015229103C9 (en) 2014-03-14 2020-11-26 Immutep S.A.S Antibody molecules to LAG-3 and uses thereof
SG11201701633SA (en) 2014-09-12 2017-03-30 Boehringer Ingelheim Int Spirocyclic inhibitors of cathepsin c
CN107074828B (zh) * 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
JP6592510B2 (ja) 2014-09-12 2019-10-16 ヤンセン ファーマシューティカ エヌ．ベー． Ｐ２ｘ７調節因子
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
UY36351A (es) 2014-10-14 2016-06-01 Novartis Ag Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
SG11201706756VA (en) 2015-03-10 2017-09-28 Aduro Biotech Inc Compositions and methods for activating "stimulator of interferon gene" -dependent signalling
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CN114272371A (zh) 2015-07-29 2022-04-05 诺华股份有限公司 包含抗pd-1抗体分子的联合疗法
EP3316902A1 (en) 2015-07-29 2018-05-09 Novartis AG Combination therapies comprising antibody molecules to tim-3
US20180340025A1 (en) 2015-07-29 2018-11-29 Novartis Ag Combination therapies comprising antibody molecules to 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
EP3365335B1 (en) 2015-10-23 2024-02-14 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
CN108697791B (zh) 2015-11-03 2022-08-23 詹森生物科技公司 特异性结合pd-1的抗体及其用途
WO2017106656A1 (en) 2015-12-17 2017-06-22 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
RU2762968C2 (ru) * 2016-02-19 2021-12-24 Спринт Биосайенс Аб 6-гетероциклил-4-морфолин-4-илпиридин-2-оны, пригодные для лечения рака и диабета
RS60898B1 (sr) * 2016-02-19 2020-11-30 Sprint Bioscience Ab Jedinjenja 6-aril-4-(morfolin-4-il)-1h-piridin-2-ona korisna za lečenje kancera i dijabetesa
EP3443114A1 (en) 2016-04-15 2019-02-20 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
MX2018015353A (es) * 2016-06-10 2019-09-09 Novartis Ag Usos terapeuticos de un inhibidor de c-raf.
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds 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
IL292977A (en) 2016-09-09 2022-07-01 Incyte Corp Pyrazolopyridine derivatives as modulators of hpk1 and their use in cancer therapy
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
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
WO2018051306A1 (en) * 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
US20180228786A1 (en) 2017-02-15 2018-08-16 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
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
WO2018200981A1 (en) * 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
FI3618875T3 (fi) * 2017-05-02 2023-07-04 Novartis Ag Raf-inhibiittoria ja trametinibia käsittävä yhdistelmähoito
EP3642240A1 (en) 2017-06-22 2020-04-29 Novartis AG Antibody molecules to cd73 and uses thereof
JOP20200014A1 (ar) * 2017-08-03 2022-10-30 Novartis Ag توليفة علاجية لمثبط كيناز تيروزين egfr من الجيل الثالث ومثبط raf
CA3073073A1 (en) 2017-09-08 2019-03-14 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
AU2018390927B2 (en) 2017-12-21 2023-01-12 Boehringer Ingelheim International Gmbh Novel benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
US20210008047A1 (en) 2018-02-13 2021-01-14 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US10800761B2 (en) 2018-02-20 2020-10-13 Incyte Corporation Carboxamide compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
AU2019272303A1 (en) * 2018-05-22 2021-01-14 Js Innomed Holdings Ltd. Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
UY38247A (es) 2018-05-30 2019-12-31 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
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
US11111247B2 (en) 2018-09-25 2021-09-07 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
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
WO2020065614A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
EA202190886A1 (ru) 2018-09-28 2021-09-07 Янссен Фармацевтика Нв Модуляторы моноацилглицерин-липазы
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
CA3133812A1 (en) * 2019-03-22 2020-10-01 Kinnate Biopharma Inc. Inhibitors of raf kinases
AR118826A1 (es) 2019-05-03 2021-11-03 Kinnate Biopharma Inc Inhibidores de cinasas raf
BR112021022335A2 (pt) * 2019-05-13 2021-12-28 Novartis Ag Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer
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
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Ｅｎｔｐｄ２抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
EP4038070A1 (en) 2019-09-30 2022-08-10 Janssen Pharmaceutica NV Radiolabelled mgl pet ligands
US11098031B1 (en) * 2019-10-24 2021-08-24 Kinnate Biopharma Inc. Inhibitors of RAF kinases
US20230046018A1 (en) * 2019-12-06 2023-02-16 Medshine Discovery Inc. Biaryl compound as pan-raf kinase inhibitor
EP4106756A1 (en) 2020-02-18 2022-12-28 Novartis AG Therapeutic combinations comprising a raf inhibitor for use in treating braf mutant nsclc
KR20220148846A (ko) 2020-02-28 2022-11-07 노파르티스 아게 다브라페닙, erk 억제제, 및 raf 억제제를 포함하는 삼중 약학적 조합물
KR20220157999A (ko) 2020-03-26 2022-11-29 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 조절제
CN115551509A (zh) 2020-05-12 2022-12-30 诺华股份有限公司 包含craf抑制剂的治疗组合
TW202210474A (zh) 2020-06-02 2022-03-16 德商百靈佳殷格翰國際股份有限公司 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
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
TW202227088A (zh) 2020-08-31 2022-07-16 瑞士商諾華公司 組合療法
WO2022060996A1 (en) * 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibitors of raf kinases
US11377431B2 (en) 2020-10-12 2022-07-05 Kinnate Biopharma Inc. Inhibitors of RAF kinases
EP4237423A1 (en) 2020-11-02 2023-09-06 Boehringer Ingelheim International GmbH Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors
CN117396472A (zh) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 Sos1抑制剂及其用途
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
WO2022226221A1 (en) * 2021-04-23 2022-10-27 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 salts thereof
BR112023021913A2 (pt) 2021-04-23 2024-01-16 Kinnate Biopharma Inc Tratamento de câncer com inibidor de raf
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
TWI812259B (zh) * 2021-06-04 2023-08-11 大陸商齊魯製藥有限公司 Raf激酶抑制劑的晶型及其製備方法
EP4431508A1 (en) * 2021-11-12 2024-09-18 Biopolar Youtang (Guangdong) Pharmaceutical Co., Ltd. Drak2 inhibitor, and preparation method therefor and use thereof
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
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
WO2023099612A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099592A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CA3240980A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN118591540A (zh) 2021-12-01 2024-09-03 勃林格殷格翰国际有限公司 包含环状2-氨基-3-氰基噻吩的kras降解化合物
WO2023108108A1 (en) * 2021-12-09 2023-06-15 Deciphera Pharmaceuticals, Llc Raf kinase inhibitors and methods of use thereof
CN118434735A (zh) 2021-12-23 2024-08-02 勃林格殷格翰国际有限公司 8-氮杂喹唑啉作为脑渗透sos1抑制剂
AR128440A1 (es) * 2022-02-03 2024-05-08 Kinnate Biopharma Inc Inhibidores de cinasas raf
CN115947691B (zh) * 2022-03-01 2024-08-16 四川大学 哒嗪砜类衍生物及其用途
AU2023227427A1 (en) 2022-03-02 2024-09-19 Novartis Ag Precision therapy for the treatment of cancer
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
TW202408463A (zh) 2022-08-10 2024-03-01 瑞士商諾華公司 醫藥組合物
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
WO2024089008A1 (en) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
WO2024089006A1 (en) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
US20240166629A1 (en) 2022-10-26 2024-05-23 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
WO2024166131A1 (en) 2023-02-09 2024-08-15 Satyarx Pharma Innovations Private Limited Heteroaryl compounds as pkmyt1 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
JP2001500482A (ja) 1996-08-27 2001-01-16 ノバルティス アクチェンゲゼルシャフト 除草性ｓ置換１，２，４，６―チアトリアジン類
AU743024B2 (en) 1997-03-05 2002-01-17 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
AU4798000A (en) 1999-04-09 2000-11-14 Smithkline Beecham Corporation Triarylimidazoles
DK1169038T3 (da) 1999-04-15 2012-11-26 Bristol Myers Squibb Co Cykliske proteintyrosinkinaseinhibitorer
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
CN1230166C (zh) 2000-01-18 2005-12-07 沃泰克斯药物股份有限公司 回旋酶抑制剂及其用途
WO2001052846A1 (en) 2000-01-18 2001-07-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR029803A1 (es) 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
US7235658B2 (en) 2000-03-06 2007-06-26 Smithkline Beecham P.L.C. Imidazol derivatives as Raf kinase inhibitors
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
AU2001244618A1 (en) 2000-03-30 2001-10-15 Takeda Chemical Industries Ltd. Substituted 1,3-thiazole compounds, their production and use
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
ES2320973T3 (es) 2000-06-12 2009-06-01 EISAI R&amp;D MANAGEMENT CO., LTD. Compuestos de 1,2-dihidropiridina, procedimiento para su preparacion y uso de los mismos.
WO2002042273A2 (en) 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
JP4217480B2 (ja) 2000-11-20 2009-02-04 スミスクライン・ビーチャム・コーポレイション 新規化合物
US7238813B2 (en) 2000-11-29 2007-07-03 Smithkline Beecham Corporation Chemical compounds
US7279477B2 (en) 2001-01-26 2007-10-09 Chugai Seiyaku Kabushiki Kaisha Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
WO2002062792A1 (fr) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Inhibiteur de jnk
WO2002076960A1 (en) 2001-03-22 2002-10-03 Abbott Gmbh & Co. Kg 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
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
NZ535985A (en) 2002-03-29 2007-04-27 Chiron Corp Substituted benzazoles and use thereof as RAF kinase inhibitors
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
EP1542990B1 (en) 2002-09-18 2009-06-17 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
MXPA05002332A (es) 2002-09-18 2005-06-08 Pfizer Prod Inc Nuevos compuestos de oxazol y tiazol como inhibidores del factor de crecimiento transformador (tgf).
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 ｒａｆ 키나아제의 저해제로서 그것의 사용
EP1692113B1 (en) 2003-11-14 2017-09-27 Lorus Therapeutics 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
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
PE20060315A1 (es) 2004-05-24 2006-05-15 Irm Llc Compuestos de tiazol como moduladores de ppar
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
CA2568756A1 (en) * 2004-06-15 2005-12-29 Astrazeneca Ab Substituted quinazolones as anti-cancer agents
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415367D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
CA2578630A1 (en) 2004-08-31 2006-03-09 Wen-Cherng Lee Pyrimidinylimidazoles as tgf-beta inhibitors
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
CA2584248A1 (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
MX2008011853A (es) * 2006-03-17 2008-09-29 Wyeth Corp Derivados de pirazolo[1,5-a]pirimidina y sus metodos de uso.
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
PL2050749T3 (pl) * 2006-08-08 2018-03-30 Chugai Seiyaku Kabushiki Kaisha Pochodna pirymidyny jako inhibitor pi3k i jej zastosowanie
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
CN101842361B (zh) 2007-06-27 2013-06-05 阿斯利康(瑞典)有限公司 吡嗪酮衍生物及其在治疗肺病中的用途
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
AR067354A1 (es) 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc Compuestos utiles como inhibidores de la raf quinasa
WO2009003998A2 (en) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
JP2010533159A (ja) * 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物９４７
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2693967A1 (en) 2007-07-19 2009-01-29 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
JP2010538003A (ja) 2007-08-29 2010-12-09 グラクソスミスクライン エルエルシー チアゾールおよびオキサゾールキナーゼ阻害薬
WO2009030952A2 (en) 2007-09-05 2009-03-12 Astrazeneca Ab Phenylcarboxamide derivatives as inhibitors and effectors of the hedgehog pathway
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
KR101408517B1 (ko) 2008-03-21 2014-06-17 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
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
WO2009152356A2 (en) 2008-06-11 2009-12-17 Irm Llc Compounds and compositions useful for the treatment of malaria
WO2009155388A1 (en) * 2008-06-20 2009-12-23 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
EP2324008B1 (en) 2008-07-24 2012-05-09 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
RU2016141566A (ru) 2008-12-19 2018-12-20 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразина, используемые в качестве ингибиторов киназы atr
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
MX2012002761A (es) 2009-09-04 2012-04-19 Novartis Ag Bipiridinas utiles para el tratamiento de enfermedades proliferativas.
WO2011059610A1 (en) 2009-11-10 2011-05-19 Glaxosmithkline Llc Benzene sulfonamide thiazole and oxazole compounds
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
NZ600837A (en) 2009-12-28 2014-01-31 Gen Inc Ass Pharma Valley Project Supporting Organization 1,3,4-oxadiazole-2-carboxamide compound
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
KR20130048293A (ko) 2010-06-25 2013-05-09 노파르티스 아게 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물
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
WO2012109075A1 (en) 2011-02-07 2012-08-16 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140221374A1 (en) * 2011-03-17 2014-08-07 Ruga Corporation Raf kinase inhibitors
EP2739143B1 (en) 2011-08-05 2018-07-11 Gary A. Flynn Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
US8569283B2 (en) 2011-09-01 2013-10-29 Valentina Molteni Compounds and compositions as c-Kit kinase inhibitors
JP5995975B2 (ja) 2011-09-21 2016-09-21 セルゾーム リミテッド Ｍｔｏｒ阻害剤としてのモルホリノ置換尿素またはカルバメート誘導体
AU2013255437A1 (en) 2012-05-02 2014-11-13 Lupin Limited Substituted pyridine compounds as CRAC modulators
EP2858988B1 (en) 2012-05-15 2018-02-28 Novartis AG Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1
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
EP2903613B1 (en) 2012-10-08 2017-11-22 Merck Sharp & Dohme Corp. Pyrazole derivatives useful as inhibitors of irak4 activity
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN107074828B (zh) 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
WO2016038583A1 (en) 2014-09-12 2016-03-17 Novartis Ag Compounds and compositions as kinase inhibitors

Also Published As

Publication number Publication date
CN108467369A (zh) 2018-08-31
PH12015502116A1 (en) 2016-01-25
JP2016517417A (ja) 2016-06-16
TW201443021A (zh) 2014-11-16
EP2970216B1 (en) 2017-11-01
IL241165B (en) 2019-03-31
CN105143209B (zh) 2018-03-13
JP2020143117A (ja) 2020-09-10
DK2970216T3 (da) 2018-01-29
NO3013169T3 (es) 2018-04-14
PH12015502116B1 (en) 2016-01-25
GEP201706692B (en) 2017-06-26
HUE035932T2 (en) 2018-05-28
SG11201506196SA (en) 2015-09-29
CA2899967C (en) 2022-01-18
CR20150487A (es) 2016-01-29
PE20160875A1 (es) 2016-09-08
US20160038504A1 (en) 2016-02-11
PT2970216T (pt) 2018-01-19
TWI662025B (zh) 2019-06-11
NI201500120A (es) 2015-11-18
US20140275003A1 (en) 2014-09-18
CY1119707T1 (el) 2018-06-27
KR102059545B1 (ko) 2019-12-26
JP6738369B2 (ja) 2020-08-12
US9242969B2 (en) 2016-01-26
ECSP15042895A (es) 2019-08-30
AR095312A1 (es) 2015-10-07
AU2014233657A1 (en) 2015-08-27
CU20150118A7 (es) 2016-03-31
TN2015000332A1 (en) 2017-01-03
HK1212692A1 (zh) 2016-06-17
ES2657900T3 (es) 2018-03-07
RS56774B1 (sr) 2018-04-30
SV2015005066A (es) 2018-06-12
EP3299367A1 (en) 2018-03-28
EP3299367B1 (en) 2019-12-25
BR112015020008A2 (pt) 2017-07-18
HRP20180158T1 (hr) 2018-03-09
JP2018150319A (ja) 2018-09-27
US20190175606A1 (en) 2019-06-13
BR112015020008B1 (pt) 2021-05-11
CL2015002151A1 (es) 2015-12-18
CN105143209A (zh) 2015-12-09
AU2014233657B2 (en) 2016-08-04
LT2970216T (lt) 2018-01-10
UY35398A (es) 2014-10-31
US9694016B2 (en) 2017-07-04
JP7088983B2 (ja) 2022-06-21
AP2015008632A0 (en) 2015-08-31
NZ710835A (en) 2016-08-26
MX2015012290A (es) 2015-12-16
CA2899967A1 (en) 2014-09-25
PL2970216T3 (pl) 2018-04-30
JOP20140104B1 (ar) 2021-08-17
EA028194B1 (ru) 2017-10-31
UA116644C2 (uk) 2018-04-25
EA201591727A1 (ru) 2016-05-31
MA38398B1 (fr) 2018-09-28
US10709712B2 (en) 2020-07-14
ZA201505438B (en) 2016-03-30
SI2970216T1 (en) 2018-01-31
GT201500294A (es) 2018-11-27
US10245267B2 (en) 2019-04-02
KR20150133214A (ko) 2015-11-27
CN108467369B (zh) 2021-08-20
JP6360879B2 (ja) 2018-07-18
EP2970216A1 (en) 2016-01-20
IL241165A0 (en) 2015-11-30
DOP2015000241A (es) 2015-12-15
ES2779673T3 (es) 2020-08-18
MA38398A1 (fr) 2018-02-28
WO2014151616A1 (en) 2014-09-25
US20170260207A1 (en) 2017-09-14

Similar Documents

Publication Publication Date Title
CU24351B1 (es) Compuestos de biaril-amida como inhibidores de cinasa
DOP2017000066A (es) Compuestos y composiciones como inhibidores de quinasa raf
DOP2016000085A (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
ECSP24026455A (es) Compuestos de pirrolotriazina como inhibidores de tam
CU20180006A7 (es) Compuestos de indazaol y azaindazol como inhibidores de irak-4
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
NI201600058A (es) Compuestos derivados de piridilo bicíclicos fusionados a anillo como inhibidores de fgfr4
NI201400089A (es) COMPUESTOS DE OXAZOLIDIN - 2 - ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
CR20150425A (es) Compuestos azabencimidazol como inhibidores de las isozimas pde4, para el tratamiento del sistema nervioso central y otros desórdenes
DOP2018000062A (es) Piridinona dicaboxamidas para uso como inhibidores de bromodominio
CR20150248A (es) Derivados de oxazolidin-2-ona-pirimidina
DOP2016000120A (es) Nuevos inhibidores de dgat2
CL2017000827A1 (es) Inhibidores de aldosterona sintasa
PE20151669A1 (es) Compuestos de azetidiniloxifenilpirrolidina
UY37166A (es) Nucleósidos ánalogos de alquinilo como inhibidores de rinovirus humano
DOP2015000295A (es) Composiciones farmacéuticas de triazolopiridinas sustituidas, metodos para prepararlas y sus usos
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