NZ620174A - Protein kinase conjugates and inhibitors - Google Patents
Protein kinase conjugates and inhibitorsInfo
- Publication number
- NZ620174A NZ620174A NZ620174A NZ62017410A NZ620174A NZ 620174 A NZ620174 A NZ 620174A NZ 620174 A NZ620174 A NZ 620174A NZ 62017410 A NZ62017410 A NZ 62017410A NZ 620174 A NZ620174 A NZ 620174A
- Authority
- NZ
- New Zealand
- Prior art keywords
- protein kinase
- cysteine residue
- group
- inhibitors
- prot
- Prior art date
Links
- 102000001253 Protein Kinase Human genes 0.000 title abstract 4
- 108060006633 protein kinase Proteins 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 abstract 3
- -1 CYS8 Proteins 0.000 abstract 2
- 101100115718 Arabidopsis thaliana CYS5 gene Proteins 0.000 abstract 1
- 101100115720 Arabidopsis thaliana CYS6 gene Proteins 0.000 abstract 1
- 108010064266 CYS7 Proteins 0.000 abstract 1
- 102100025802 Cystin-1 Human genes 0.000 abstract 1
- 101000855767 Homo sapiens Cystin-1 Proteins 0.000 abstract 1
- 101100426732 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-9 gene Proteins 0.000 abstract 1
- 101100498074 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys11 gene Proteins 0.000 abstract 1
- 101100330293 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys12 gene Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 239000003607 modifier Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 230000000699 topical effect Effects 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
- C07D213/78—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
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with 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
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
- C07D333/68—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
- 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
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- C07D403/14—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 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- 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
- C07D413/12—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
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
- 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
- C07D471/10—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
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biotechnology (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24298809P | 2009-09-16 | 2009-09-16 | |
| NZ598705A NZ598705A (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ620174A true NZ620174A (en) | 2016-08-26 |
Family
ID=43759252
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ620174A NZ620174A (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
| NZ598705A NZ598705A (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ598705A NZ598705A (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9556426B2 (enExample) |
| EP (1) | EP2478361A4 (enExample) |
| JP (4) | JP5806670B2 (enExample) |
| KR (1) | KR20120093220A (enExample) |
| CN (2) | CN102713618B (enExample) |
| AU (2) | AU2010295690B2 (enExample) |
| BR (1) | BR112012005962A8 (enExample) |
| CA (1) | CA2773985A1 (enExample) |
| IL (1) | IL218678A0 (enExample) |
| IN (1) | IN2012DN02534A (enExample) |
| MX (1) | MX339811B (enExample) |
| NZ (2) | NZ620174A (enExample) |
| RU (1) | RU2012114902A (enExample) |
| SG (1) | SG179172A1 (enExample) |
| WO (1) | WO2011034907A2 (enExample) |
Families Citing this family (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA018573B1 (ru) | 2006-09-22 | 2013-09-30 | Фармасайкликс, Инк. | Ингибиторы тирозинкиназы брутона |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| MX2010012703A (es) | 2008-05-21 | 2010-12-21 | Ariad Pharma Inc | Derivados fosforosos como inhibidores de cinasa. |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| CN105362277A (zh) | 2008-07-16 | 2016-03-02 | 药品循环有限公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
| MY156789A (en) * | 2008-09-05 | 2016-03-31 | Celgene Avilomics Res Inc | Algorithm for designing irreversible inhibitors |
| IN2012DN02534A (enExample) | 2009-09-16 | 2015-08-28 | Avila Therapeutics Inc | |
| WO2011060321A1 (en) | 2009-11-16 | 2011-05-19 | Chdi, Inc. | Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| US20110269244A1 (en) | 2009-12-30 | 2011-11-03 | Petter Russell C | Ligand-directed covalent modification of protein |
| CA3007787C (en) | 2010-06-03 | 2020-03-10 | Pharmacyclics Llc | The use of inhibitors of bruton's tyrosine kinase (btk) |
| HUE029196T2 (en) * | 2010-06-04 | 2017-02-28 | Hoffmann La Roche | Aminoprimidine derivatives as LRRK2 modulators |
| SG189043A1 (en) | 2010-11-10 | 2013-05-31 | Hoffmann La Roche | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| BR112013027734A2 (pt) | 2011-05-04 | 2017-08-08 | Ariad Pharma Inc | compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica |
| US8889716B2 (en) | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| WO2013009827A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009812A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc | Methods of treatment |
| WO2013009830A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009810A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| EP2736895B1 (en) | 2011-07-27 | 2016-01-06 | Astrazeneca AB | 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| AR089182A1 (es) * | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| KR20160125527A (ko) * | 2012-04-17 | 2016-10-31 | 후지필름 가부시키가이샤 | 함질소 복소환 화합물 또는 그 염 |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| EA201492082A1 (ru) | 2012-06-04 | 2015-03-31 | Фармасайкликс, Инк. | Кристаллические формы ингибитора тирозинкиназы брутона |
| DK2872491T3 (da) | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
| CA2879570A1 (en) | 2012-07-24 | 2014-01-30 | Pharmacyclics, Inc. | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| MX2015006168A (es) | 2012-11-15 | 2015-08-10 | Pharmacyclics Inc | Compuestos de pirrolopirimidina como inhibidores de quinasas. |
| RU2693480C2 (ru) | 2013-03-14 | 2019-07-03 | Толеро Фармасьютикалз, Инк. | Ингибиторы jak2 и alk2 и способы их использования |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| TWI649081B (zh) | 2013-08-02 | 2019-02-01 | 製藥公司 | 治療固態腫瘤之方法 |
| ES2709509T3 (es) | 2013-08-12 | 2019-04-16 | Pharmacyclics Llc | Procedimientos para el tratamiento de cáncer amplificado por HER2 |
| AU2014318614B2 (en) | 2013-09-12 | 2021-01-07 | Dana-Farber Cancer Institute Inc. | Methods for evaluating and treating Waldenstrom's macroglobulinemia |
| BR112016008849B8 (pt) | 2013-10-25 | 2022-09-06 | Blueprint Medicines Corp | Compostos ou sais farmaceuticamente aceitáveis dos mesmos, uso dos referidos compostos e composições farmacêuticas |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| MA38393B1 (fr) * | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| EP3119910A4 (en) | 2014-03-20 | 2018-02-21 | Pharmacyclics LLC | Phospholipase c gamma 2 and resistance associated mutations |
| LT3126352T (lt) | 2014-04-04 | 2019-01-10 | Syros Pharmaceuticals, Inc. | Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai |
| CN106999494A (zh) | 2014-08-01 | 2017-08-01 | 药品循环有限公司 | 布鲁顿酪氨酸激酶的抑制剂 |
| JP2017523206A (ja) | 2014-08-07 | 2017-08-17 | ファーマサイクリックス エルエルシー | ブルトン型チロシンキナーゼ阻害剤の新規製剤 |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| EP4112618A1 (en) | 2015-06-03 | 2023-01-04 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| NZ743651A (en) | 2015-12-09 | 2023-07-28 | Univ Illinois | Benzothiophene-based selective estrogen receptor downregulators |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| ES2989988T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros heterorocíclicos para la degradación de proteínas diana |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| US11285218B2 (en) | 2016-06-23 | 2022-03-29 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
| EA201990187A1 (ru) | 2016-07-01 | 2019-07-31 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| WO2018187294A1 (en) * | 2017-04-03 | 2018-10-11 | Asana Biosciences, Llc | Pyrimido-pyridazinone compound combinations, methods, kits and formulations thereof |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| EP4455146A3 (en) | 2017-06-29 | 2025-01-01 | G1 Therapeutics, Inc. | Morphic forms of git38 and methods of manufacture thereof |
| WO2019024876A1 (zh) * | 2017-08-04 | 2019-02-07 | 上海和誉生物医药科技有限公司 | 一种具有fgfr4抑制活性的醛基吡啶衍生物、其制备方法和应用 |
| CN111902141A (zh) | 2018-03-26 | 2020-11-06 | C4医药公司 | 用于ikaros降解的羟脑苷脂结合剂 |
| IL259810A (en) * | 2018-06-04 | 2018-07-31 | Yeda Res & Dev | Mitogen-activated protein kinase kinase 7 inhibitors |
| CA3103995A1 (en) | 2018-07-26 | 2020-01-30 | Sumitomo Dainippon Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
| KR102328682B1 (ko) * | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020045941A1 (ko) * | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| WO2020097400A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| US12522583B2 (en) | 2018-11-07 | 2026-01-13 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof |
| US12415816B2 (en) | 2018-11-07 | 2025-09-16 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| CA3124569A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| CN113645976A (zh) | 2019-03-29 | 2021-11-12 | 阿斯利康(瑞典)有限公司 | 用于治疗非小细胞肺癌的奧希替尼 |
| KR20210152515A (ko) | 2019-04-12 | 2021-12-15 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스 및 아이올로스의 트리시클릭 분해제 |
| JP7628108B2 (ja) * | 2019-07-19 | 2025-02-07 | ブリッドジーン バイオサイエンシズ インコーポレイテッド | チロシンキナーゼの阻害剤 |
| MX2022007659A (es) | 2019-12-20 | 2022-07-19 | C4 Therapeutics Inc | Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr). |
| MX2022010952A (es) | 2020-03-05 | 2022-10-07 | C4 Therapeutics Inc | Compuestos para la degradacion dirigida de brd9. |
| TW202204350A (zh) | 2020-05-06 | 2022-02-01 | 美商雅捷可斯治療公司 | 作為jak2抑制劑之6-雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| EP4652997A3 (en) | 2020-05-19 | 2026-03-04 | Pharmacosmos Holding A/s | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| JP2023538517A (ja) | 2020-08-05 | 2023-09-08 | シーフォー セラピューティクス, インコーポレイテッド | Retの標的分解のための化合物 |
| JP7787164B2 (ja) | 2020-09-23 | 2025-12-16 | アキリオン ファーマシューティカルズ, インコーポレーテッド | 補体媒介性障害の治療のための医薬化合物 |
| US12043632B2 (en) | 2020-12-23 | 2024-07-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| CN117940133A (zh) | 2021-06-08 | 2024-04-26 | C4医药公司 | 用于突变braf的降解的治疗剂 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| TW202345806A (zh) | 2022-03-31 | 2023-12-01 | 美商艾伯維有限公司 | 噻唑并〔5,4-b〕吡啶malt-1抑制劑 |
| EP4565585A1 (en) | 2022-08-03 | 2025-06-11 | Bristol-Myers Squibb Company | Compounds for modulating ret protein |
| JP2025540907A (ja) | 2022-11-04 | 2025-12-17 | ブリストル-マイヤーズ スクイブ カンパニー | Ret-lddタンパク質分解誘導剤 |
| CN120530116A (zh) | 2022-11-04 | 2025-08-22 | 百时美施贵宝公司 | Ret-ldd蛋白抑制剂 |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| CN118766549A (zh) * | 2024-06-24 | 2024-10-15 | 重庆医科大学附属第一医院 | 脊柱转移性肿瘤微创切吸治疗系统 |
Family Cites Families (104)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| US5650270A (en) | 1982-02-01 | 1997-07-22 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US4709016A (en) | 1982-02-01 | 1987-11-24 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| US5756466A (en) | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5856116A (en) | 1994-06-17 | 1999-01-05 | Vertex Pharmaceuticals, Incorporated | Crystal structure and mutants of interleukin-1 beta converting enzyme |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| HU228446B1 (en) | 1996-04-12 | 2013-03-28 | Warner Lambert Co | Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof |
| ES2285735T3 (es) | 1996-07-25 | 2007-11-16 | Biogen Idec Inc | Modelo molecular para inhibidores de vla-4. |
| US6686350B1 (en) | 1996-07-25 | 2004-02-03 | Biogen, Inc. | Cell adhesion inhibitors |
| ATE290545T1 (de) | 1996-12-06 | 2005-03-15 | Vertex Pharma | Inhibitoren des interleukin-1beta konvertierenden enzyms |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
| US6251912B1 (en) | 1997-08-01 | 2001-06-26 | American Cyanamid Company | Substituted quinazoline derivatives |
| US6162613A (en) | 1998-02-18 | 2000-12-19 | Vertex Pharmaceuticals, Inc. | Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases |
| US7383135B1 (en) | 1998-05-04 | 2008-06-03 | Vertex Pharmaceuticals Incorporated | Methods of designing inhibitors for JNK kinases |
| US6335155B1 (en) | 1998-06-26 | 2002-01-01 | Sunesis Pharmaceuticals, Inc. | Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules |
| US6919178B2 (en) | 2000-11-21 | 2005-07-19 | Sunesis Pharmaceuticals, Inc. | Extended tethering approach for rapid identification of ligands |
| EP1115847A1 (en) * | 1998-09-25 | 2001-07-18 | Children's Medical Center Corporation | Short peptides which selectively modulate the activity of protein kinases |
| US6288082B1 (en) | 1998-09-29 | 2001-09-11 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| EP1131304B1 (en) | 1998-11-19 | 2002-12-04 | Warner-Lambert Company | N- 4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, an irreversible inhibitor of tyrosine kinases |
| US6569876B1 (en) | 1999-06-17 | 2003-05-27 | John C. Cheronis | Method and structure for inhibiting activity of serine elastases |
| US6420364B1 (en) | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
| AU2001236720A1 (en) | 2000-02-05 | 2001-08-14 | Bemis, Guy | Compositions useful as inhibitors of erk |
| US6384051B1 (en) | 2000-03-13 | 2002-05-07 | American Cyanamid Company | Method of treating or inhibiting colonic polyps |
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| CA2417500C (en) | 2000-07-28 | 2008-11-18 | Georgetown University Medical Center | Erbb-2 selective small molecule kinase inhibitors |
| WO2002014281A1 (en) | 2000-08-11 | 2002-02-21 | Vertex Pharmaceuticals Incorporated | Pyridine derivatives as inhibitors of p38 |
| HUP0400639A3 (en) | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| US7235576B1 (en) | 2001-01-12 | 2007-06-26 | Bayer Pharmaceuticals Corporation | Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| IL144583A0 (en) * | 2001-07-26 | 2002-05-23 | Peptor Ltd | Chimeric protein kinase inhibitors |
| IL161409A0 (en) | 2001-11-21 | 2004-09-27 | Sunesis Pharmaceuticals Inc | Methods for ligand discovery |
| ATE387002T1 (de) | 2001-12-07 | 2008-03-15 | Res Investment Network Inc | Aus festkörper gebildetes mikrooptisches elektromechanisches system (moems) zur wiedergabe eines photonischen diffraktiven speichers |
| CA2472580A1 (en) | 2002-01-07 | 2003-07-17 | Sequoia Pharmaceuticals | Broad spectrum inhibitors |
| US7202033B2 (en) | 2002-03-21 | 2007-04-10 | Sunesis Pharmaceuticals, Inc. | Identification of kinase inhibitors |
| GB0213186D0 (en) | 2002-06-08 | 2002-07-17 | Univ Dundee | Methods |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| EP1375517A1 (en) | 2002-06-21 | 2004-01-02 | Smithkline Beecham Corporation | Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same |
| GB0221169D0 (en) | 2002-09-12 | 2002-10-23 | Univ Bath | Crystal |
| EA200500721A1 (ru) | 2002-11-28 | 2005-12-29 | Шеринг Акциенгезельшафт | Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств |
| PE20040945A1 (es) | 2003-02-05 | 2004-12-14 | Warner Lambert Co | Preparacion de quinazolinas substituidas |
| CA2515688A1 (en) * | 2003-02-11 | 2004-08-26 | Immusol Incorporated | Sirna libraries optimized for predetermined protein families |
| JP4927533B2 (ja) | 2003-02-28 | 2012-05-09 | ニッポネックス インコーポレイテッド | 癌その他の疾患の治療に有用な置換ピリジン誘導体 |
| UY28213A1 (es) | 2003-02-28 | 2004-09-30 | Bayer Pharmaceuticals Corp | Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos. |
| ATE489379T1 (de) | 2003-02-28 | 2010-12-15 | Bayer Healthcare Llc | 2-oxo-1,3,5-perhydrotriazapinderivate, die sich zur behandlung von hyperproliferativen, angiogenen und entzündlichen erkrankungen eignen |
| EP1610808A4 (en) | 2003-03-26 | 2011-04-06 | Sudhir Paul | COVALENT BINDING OF LIGANDS TO NUCLEOPHILIC PROTEINS UNDER GUIDANCE BY NONCOVALENT BINDING |
| WO2007038613A2 (en) | 2005-09-26 | 2007-04-05 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
| US7687506B2 (en) | 2003-04-11 | 2010-03-30 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
| WO2004113274A2 (en) | 2003-05-20 | 2004-12-29 | Bayer Pharmaceuticals Corporation | Diaryl ureas with kinase inhibiting activity |
| EP1648516A2 (en) | 2003-08-01 | 2006-04-26 | Wyeth Holdings Corporation | Use of combination of an epidermal growth factor receptor kinase inhibitor and cytotoxic agents for treatment and inhibition of cancer |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| WO2005034840A2 (en) | 2003-09-17 | 2005-04-21 | Sunesis Pharmaceuticals, Inc. | Identification of kinase inhibitors |
| WO2005043118A2 (en) | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| US7932382B2 (en) | 2004-01-16 | 2011-04-26 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
| AU2005211448A1 (en) * | 2004-01-30 | 2005-08-18 | Merck Patent Gmbh | Bisarylurea derivatives |
| US20080268460A1 (en) | 2004-05-20 | 2008-10-30 | Wyeth | Assays to Identify Irreversibly Binding Inhibitors of Receptor Tyrosine Kinases |
| WO2005115145A2 (en) | 2004-05-20 | 2005-12-08 | Wyeth | Quinone substituted quinazoline and quinoline kinase inhibitors |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| US20060079494A1 (en) | 2004-09-27 | 2006-04-13 | Santi Daniel V | Specific kinase inhibitors |
| JP5089392B2 (ja) | 2004-10-13 | 2012-12-05 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | キナーゼ阻害剤としての複素環式置換ビスアリール尿素誘導体 |
| ZA200706804B (en) | 2005-02-03 | 2008-10-29 | Gen Hospital Corp | Method for treating gefitinib resistant cancer |
| KR20080002826A (ko) | 2005-04-14 | 2008-01-04 | 와이어쓰 | 게피티니브 내성 환자에서의 표피 성장 인자 수용체(egfr) 키나제 억제제의 용도 |
| AR053602A1 (es) | 2005-05-03 | 2007-05-09 | Smithkline Beecham Corp | Compuesto de 2- arilamino -4-oxo-1,3-tiazol-5(4h)- substituido, composicion farmaceutica que lo comprende, proceso para prepararla y uso del compuesto para preparar un medicamento |
| CA2607020C (en) | 2005-05-05 | 2015-01-13 | Chroma Therapeutics Ltd. | Alpha amino acid ester-drug conjugates hydrolysable by carboxylesterases |
| GB0509224D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Inhibitors of intracellular enzymatic activity |
| WO2006125539A2 (en) | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Combination therapy comprising diaryl ureas for treating diseases |
| NZ567851A (en) | 2005-11-01 | 2011-09-30 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| TW200734327A (en) | 2005-11-03 | 2007-09-16 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
| JP2009520038A (ja) | 2005-12-19 | 2009-05-21 | ジェネンテック・インコーポレーテッド | ピリミジンキナーゼインヒビター |
| TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| CA2647271A1 (en) | 2006-04-07 | 2007-10-18 | Modpro Ab | Binder for c-reactive protein |
| CN101054380B (zh) | 2006-04-13 | 2011-07-20 | 沈阳药科大学 | 用作细胞周期依赖性蛋白激酶抑制剂的吡唑并嘧啶类衍生物 |
| US7601852B2 (en) | 2006-05-11 | 2009-10-13 | Kosan Biosciences Incorporated | Macrocyclic kinase inhibitors |
| US8604031B2 (en) * | 2006-05-18 | 2013-12-10 | Mannkind Corporation | Intracellular kinase inhibitors |
| PE20080403A1 (es) * | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| US8217177B2 (en) * | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US8198448B2 (en) * | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| EA018573B1 (ru) * | 2006-09-22 | 2013-09-30 | Фармасайкликс, Инк. | Ингибиторы тирозинкиназы брутона |
| US8193197B2 (en) | 2006-10-19 | 2012-06-05 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| ME00811B (me) | 2006-12-08 | 2012-03-20 | Novartis Ag | JEDINJENJA l KOMPOZICIJE KAO INHIBITORI PROTEIN KINAZE |
| EP2099771A1 (en) | 2006-12-19 | 2009-09-16 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| PT2114900T (pt) | 2007-01-31 | 2019-01-17 | Ym Biosciences Australia Pty | Compostos à base de tiopirimidina e as suas utilizações |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| EP2152079A4 (en) | 2007-06-04 | 2011-03-09 | Avila Therapeutics Inc | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| WO2009030890A1 (en) | 2007-09-03 | 2009-03-12 | University Court Of The University Of Dundee | Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| EP2214486A4 (en) | 2007-10-19 | 2011-03-09 | Avila Therapeutics Inc | HETEROARYL COMPOUNDS AND ITS USES |
| US8293705B2 (en) | 2007-12-21 | 2012-10-23 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
| TWI487522B (zh) | 2007-12-21 | 2015-06-11 | 賽基艾維洛米斯研究股份有限公司 | Hcv蛋白酶抑制劑及其用途(一) |
| US8309685B2 (en) | 2007-12-21 | 2012-11-13 | Celgene Avilomics Research, Inc. | HCV protease inhibitors and uses thereof |
| TW200932255A (en) | 2007-12-21 | 2009-08-01 | Avila Therapeutics Inc | HCV protease inhibitors and uses thereof |
| EP2244721A4 (en) | 2008-01-14 | 2017-01-18 | Bayer Intellectual Property GmbH | Sulfone substituted 2,3-dihydroimidazo ý1,2-c¨quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| SG10201510696RA (en) | 2008-06-27 | 2016-01-28 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| US8188137B2 (en) | 2008-08-15 | 2012-05-29 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
| MY156789A (en) | 2008-09-05 | 2016-03-31 | Celgene Avilomics Res Inc | Algorithm for designing irreversible inhibitors |
| US8603737B2 (en) | 2008-09-19 | 2013-12-10 | Celgene Avilomics Research, Inc. | Methods for identifying HCV protease inhibitors |
| WO2011031896A2 (en) | 2009-09-09 | 2011-03-17 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| IN2012DN02534A (enExample) | 2009-09-16 | 2015-08-28 | Avila Therapeutics Inc | |
| US20110269244A1 (en) | 2009-12-30 | 2011-11-03 | Petter Russell C | Ligand-directed covalent modification of protein |
| MY160734A (en) | 2010-08-10 | 2017-03-15 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
-
2010
- 2010-09-15 IN IN2534DEN2012 patent/IN2012DN02534A/en unknown
- 2010-09-15 WO PCT/US2010/048916 patent/WO2011034907A2/en not_active Ceased
- 2010-09-15 AU AU2010295690A patent/AU2010295690B2/en not_active Ceased
- 2010-09-15 CN CN201080050753.3A patent/CN102713618B/zh not_active Expired - Fee Related
- 2010-09-15 SG SG2012018545A patent/SG179172A1/en unknown
- 2010-09-15 RU RU2012114902/04A patent/RU2012114902A/ru not_active Application Discontinuation
- 2010-09-15 BR BR112012005962A patent/BR112012005962A8/pt not_active IP Right Cessation
- 2010-09-15 CA CA2773985A patent/CA2773985A1/en not_active Abandoned
- 2010-09-15 NZ NZ620174A patent/NZ620174A/en not_active IP Right Cessation
- 2010-09-15 NZ NZ598705A patent/NZ598705A/en not_active IP Right Cessation
- 2010-09-15 KR KR1020127009760A patent/KR20120093220A/ko not_active Ceased
- 2010-09-15 US US12/882,484 patent/US9556426B2/en active Active
- 2010-09-15 MX MX2012003332A patent/MX339811B/es active IP Right Grant
- 2010-09-15 EP EP10817748.6A patent/EP2478361A4/en not_active Withdrawn
- 2010-09-15 JP JP2012529871A patent/JP5806670B2/ja active Active
- 2010-09-15 CN CN201510330338.8A patent/CN105063001A/zh active Pending
-
2012
- 2012-03-15 IL IL218678A patent/IL218678A0/en unknown
-
2015
- 2015-09-04 JP JP2015174949A patent/JP6397389B2/ja not_active Ceased
-
2016
- 2016-07-18 US US15/213,319 patent/US10662195B2/en active Active
- 2016-10-24 AU AU2016250339A patent/AU2016250339A1/en not_active Abandoned
-
2018
- 2018-08-31 JP JP2018163436A patent/JP6889689B2/ja not_active Expired - Fee Related
-
2021
- 2021-05-21 JP JP2021086337A patent/JP2021121219A/ja active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| NZ620174A (en) | Protein kinase conjugates and inhibitors | |
| MY148231A (en) | Leptomycin derivatives | |
| NZ598808A (en) | Pi3 kinase inhibitors and uses thereof | |
| NO20084752L (no) | Konjugater av aziridinayl-epotilonanaloger og farmasoytiske sammensetninger som inneholder disse | |
| WO2007115620A3 (de) | Neuartige cyclobutyl-verbindungen als kinase-inhibitoren | |
| PH12013502192A1 (en) | Antibodies against human angiopoietin 2 | |
| WO2007112193A3 (en) | Camptothecin-binding moiety conjugates | |
| TW200716606A (en) | Chemical compounds | |
| SI1853602T1 (sl) | Kemične spojine | |
| PL1853588T3 (pl) | Związki chemiczne | |
| MY167579A (en) | Glycoconjugation processes and compositions | |
| TW200740776A (en) | N-phenylbenzotriazolyl c-kit inhibitors | |
| WO2007107706A3 (en) | Dimers of heterocyclic compounds for the treatment of copd | |
| WO2009100194A3 (en) | Camptothecin-binding moiety conjugates | |
| MX2011009796A (es) | Inhibidores de la cinasa pi3. | |
| WO2009155121A3 (en) | Inhibitors of pi3 kinase | |
| WO2007038658A3 (en) | Antibody-drug conjugates and methods of use | |
| TW200600518A (en) | Conjugates of hydroxyalkyl starch and a protein | |
| MX2011012122A (es) | Derivados de tiofeno. | |
| TNSN08370A1 (en) | Tetrahydropyridothienopyrimidine compounds and methods of use thereof | |
| WO2009074247A8 (de) | Neue 2-aryl-thiazol-4-carbonsäureamid-derivate, deren herstellung und verwendung als arzneimittel | |
| EA200900261A1 (ru) | Применение эсцина | |
| TW200800993A (en) | Organic compounds | |
| TW200639155A (en) | Thiazolidinones, their production and use as pharmaceutical agents | |
| TW200621260A (en) | Selected fused heterocyclics and uses thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| LAPS | Patent lapsed |