CY1113483T1 - Παραγωγα βενζαμιδιου χρησιμα ως αναστολεις αποακετυλασης ιστονης - Google Patents

Παραγωγα βενζαμιδιου χρησιμα ως αναστολεις αποακετυλασης ιστονης

Info

Publication number
CY1113483T1
CY1113483T1 CY20121101133T CY121101133T CY1113483T1 CY 1113483 T1 CY1113483 T1 CY 1113483T1 CY 20121101133 T CY20121101133 T CY 20121101133T CY 121101133 T CY121101133 T CY 121101133T CY 1113483 T1 CY1113483 T1 CY 1113483T1
Authority
CY
Cyprus
Prior art keywords
benzamidium
producers
suspends
useful
halo
Prior art date
Application number
CY20121101133T
Other languages
English (en)
Inventor
Elaine Se Stokes
Ca Roberts
Michael J Waring
Original Assignee
Astrazeneca Ab
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
Priority claimed from GB0207863A external-priority patent/GB0207863D0/en
Priority claimed from GB0229930A external-priority patent/GB0229930D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CY1113483T1 publication Critical patent/CY1113483T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—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
    • 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
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
    • 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
    • C07D277/22—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • 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
    • C07D277/22—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—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
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Quinoline Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Η εφεύρεση αφορά μία ένωση του τύπου (I) όπου ο Δακτύλιος Α είναι ετεροκυκλυλ, m είναι 0-4 και κάθε R1 είναι μία ομάδα όπως υδροξυ, αλο, τριφθορομεθυλ και κυανο, R2 είναι αλο και n είναι 0-2, και κάθε R4 είναι μία ομάδα όπως υδροξυ, αλο, τριφθορομεθυλ και κυανό, p είναι 0-4 και R3 είναι αμινο ή υδροξυ, ή φαρμακευτικώς αποδεκτά άλατα ή in vivo υδρολυόμενοι εστέρες ή αμίδια αυτής, τις διαδικασίες παρασκευής τους, τις φαρμακευτικές συνθέσεις που τα περιέχουν και την χρήση τους στην θεραπεία νόσων ή ιατρικών καταστάσεων που προκαλούνται από αποακετυλάση ιστόνης.
CY20121101133T 2002-04-05 2012-11-22 Παραγωγα βενζαμιδιου χρησιμα ως αναστολεις αποακετυλασης ιστονης CY1113483T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0207863A GB0207863D0 (en) 2002-04-05 2002-04-05 Benzamide derivatives
GB0229930A GB0229930D0 (en) 2002-12-21 2002-12-21 Benzamide derivatives
EP03712442A EP1495002B1 (en) 2002-04-05 2003-04-02 Benzamide derivatives useful as histone deacetylase inhibitors

Publications (1)

Publication Number Publication Date
CY1113483T1 true CY1113483T1 (el) 2016-06-22

Family

ID=29252435

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20121101133T CY1113483T1 (el) 2002-04-05 2012-11-22 Παραγωγα βενζαμιδιου χρησιμα ως αναστολεις αποακετυλασης ιστονης

Country Status (26)

Country Link
US (3) US20050171103A1 (el)
EP (1) EP1495002B1 (el)
JP (1) JP4471665B2 (el)
KR (1) KR101066508B1 (el)
CN (2) CN101805309A (el)
AR (1) AR039257A1 (el)
AU (1) AU2003217054B2 (el)
BR (1) BR0308875A (el)
CA (1) CA2480356C (el)
CY (1) CY1113483T1 (el)
DK (1) DK1495002T3 (el)
EG (1) EG25655A (el)
ES (1) ES2392963T3 (el)
HK (1) HK1071359A1 (el)
IL (2) IL164373A0 (el)
IS (1) IS2895B (el)
MX (1) MXPA04009689A (el)
MY (1) MY142177A (el)
NO (1) NO330119B1 (el)
NZ (1) NZ535143A (el)
PL (1) PL372967A1 (el)
PT (1) PT1495002E (el)
RU (1) RU2376287C2 (el)
SI (1) SI1495002T1 (el)
TW (1) TWI319387B (el)
WO (1) WO2003087057A1 (el)

Families Citing this family (151)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04002397A (es) 2001-09-14 2004-12-02 Methylgene Inc Inhibidores de histona deacetilasa.
US7868204B2 (en) 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
AU2003216322A1 (en) 2002-02-15 2003-09-09 Rigel Pharmaceuticals, Inc. Inhibitors of tubulin polymerization
EA007272B1 (ru) 2002-03-13 2006-08-25 Янссен Фармацевтика Н. В. Новые ингибиторы гистондеацетилазы
BR0307606A (pt) 2002-03-13 2004-12-21 Janssen Pharmaceutica Nv Derivados de piperazinila, piperidinila e morfolinila como inibidores de histona desacetilase
EP1547617B1 (en) * 2002-08-20 2010-04-28 Astellas Pharma Inc. Arthrodial cartilage extracellular matrix degradation inhibitor
CN1856489A (zh) * 2003-09-22 2006-11-01 欧洲凯尔特公司 用于治疗疼痛的苯甲酰胺化合物
KR101153335B1 (ko) * 2003-09-24 2012-07-05 메틸진 인코포레이티드 히스톤 데아세틸라제의 억제제
TW200533357A (en) * 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
JP2007519754A (ja) * 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション 化合物
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
WO2005092899A1 (en) 2004-03-26 2005-10-06 Methylgene Inc. Inhibitors of histone deacetylase
ME01058B (me) 2004-07-28 2012-10-20 Janssen Pharmaceutica Nv Supstituisani derivati propenil piperazina kao novi inhibitori histonske deacetilaze
SG156687A1 (en) 2004-07-28 2009-11-26 Janssen Pharmaceutica Nv Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
AR050926A1 (es) * 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
CA2584307A1 (en) * 2004-10-15 2006-06-15 Bayer Pharmaceuticals Corporation Indane amides with antiproliferative activity
ATE502025T1 (de) * 2004-10-19 2011-04-15 Compass Pharmaceuticals Llc Arylcarboxamide und ihre verwendung als antitumormittel
GB0427758D0 (en) * 2004-12-18 2005-01-19 Astrazeneca Ab Novel benzamide compounds
US7968574B2 (en) 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
CA2594345C (en) 2004-12-28 2013-11-05 Kinex Pharmaceuticals, Llc Compositions and methods of treating cell proliferation disorders
GB0500828D0 (en) * 2005-01-15 2005-02-23 Astrazeneca Ab Benzamide derivatives
GB0501146D0 (en) * 2005-01-20 2005-02-23 Astrazeneca Ab Novel benzamide derivatives
NZ599464A (en) 2005-02-03 2014-03-28 Topotarget Uk Ltd Combination therapies using hdac inhibitors
US7872024B2 (en) 2005-04-20 2011-01-18 Merck Sharp & Dohme Corp. Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
EP1874295A4 (en) 2005-04-20 2009-08-12 Merck & Co Inc benzothiophene
AU2006240248A1 (en) 2005-04-20 2006-11-02 Merck Sharp & Dohme Corp. Benzothiophene hydroxamic acid derivatives
GB0509223D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
GB0509225D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
EP1719508A1 (en) * 2005-05-06 2006-11-08 Yih-Lin Chung Use of histone deacetylase inhibitors for the prevention or treatment of joint destruction
DK1901729T3 (da) 2005-05-13 2012-05-14 Topotarget Uk Ltd Farmaceutiske formuleringer af HDAC-inhibitorer
EP1885710B1 (en) 2005-05-18 2015-08-19 Janssen Pharmaceutica N.V. Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase
EP1731911A1 (fr) 2005-06-07 2006-12-13 Institut National De La Sante Et De La Recherche Medicale (Inserm) Procédé utile pour la détection d'encéphalopathies
US8158825B2 (en) 2005-06-24 2012-04-17 Merck Sharp & Dohme Corp. Modified malonate derivatives
US20090176837A1 (en) * 2005-07-12 2009-07-09 Sony Corporation Compounds with activity at retinoic acid receptors
AU2006270322A1 (en) 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase inhibitors
GB0521244D0 (en) * 2005-10-19 2005-11-30 Astrazeneca Ab Benzamide compounds
ATE509920T1 (de) 2005-10-27 2011-06-15 Janssen Pharmaceutica Nv Quadratsäurederivate als inhibitoren von histondeacetylase
JP2009514858A (ja) 2005-11-03 2009-04-09 メルク エンド カムパニー インコーポレーテッド アリール−ピラゾリルモチーフを有するヒストンデアセチラーゼ阻害剤
CA2627923C (en) 2005-11-10 2016-01-12 Topotarget Uk Limited Histone deacetylase (hdac) inhibitors (pxdlol) for the treatment of cancer
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
GB0526352D0 (en) * 2005-12-23 2006-02-01 Astrazeneca Ab Benzamide derivatives
GB0526351D0 (en) * 2005-12-23 2006-02-01 Astrazeneca Ab Novel benzamide derivatives
CN101370803B (zh) 2006-01-19 2012-12-12 詹森药业有限公司 作为组蛋白脱乙酰酶抑制剂的取代的吲哚基-烷基-氨基衍生物
EP1979328B1 (en) 2006-01-19 2012-12-26 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
JP5247470B2 (ja) 2006-01-19 2013-07-24 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒストンデアセチラーゼのインヒビターとしてのピリジン及びピリミジン誘導体
JP5225104B2 (ja) 2006-01-19 2013-07-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 新しい、ヒストンデアセチラーゼのインヒビターとしてのアミノフェニル誘導体
CN101374828B (zh) 2006-01-19 2012-09-19 詹森药业有限公司 作为组蛋白脱乙酰酶抑制剂的杂环烷基衍生物
US8101616B2 (en) 2006-01-19 2012-01-24 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
TW200806292A (en) * 2006-01-25 2008-02-01 Synta Pharmaceuticals Corp Vinyl-phenyl derivatives for inflammation and immune-related uses
US8168658B2 (en) 2006-02-28 2012-05-01 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase
TW200740769A (en) 2006-03-16 2007-11-01 Astrazeneca Ab Novel process
EP2007720B1 (en) 2006-04-07 2013-12-25 MethylGene Inc. Benzamide derivatives as inhibitors of histone deacetylase
JP2009535333A (ja) 2006-04-26 2009-10-01 メルク エンド カムパニー インコーポレーテッド 二置換アニリン化合物
US8119652B2 (en) 2006-05-18 2012-02-21 Merck Sharp & Dohme Corp. Aryl-fused spirocyclic compounds
EP2041071B1 (en) 2006-06-29 2014-06-18 Kinex Pharmaceuticals, LLC Biaryl compositions and methods for modulating a kinase cascade
EP1889830A1 (en) * 2006-07-10 2008-02-20 Pharmeste S.r.l. Biarylcarboxyarylamides as vanilloid-1 receptor modulators
JP2009544611A (ja) 2006-07-20 2009-12-17 メルク エンド カムパニー インコーポレーテッド ヒストン脱アセチル化酵素阻害剤としてのリン誘導体
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
WO2008053131A1 (en) 2006-10-30 2008-05-08 Chroma Therapeutics Ltd. Hydroxamates as inhibitors of histone deacetylase
US7939529B2 (en) 2007-05-17 2011-05-10 Kinex Pharmaceuticals, Llc Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
TWI457336B (zh) 2006-12-28 2014-10-21 Kinex Pharmaceuticals Llc 調節激酶級聯之組成物及方法
US7935697B2 (en) 2006-12-28 2011-05-03 Kinex Pharmaceuticals, Llc Compositions for modulating a kinase cascade and methods of use thereof
US8030344B2 (en) * 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
CA2680838A1 (en) 2007-03-28 2008-10-16 Santen Pharmaceutical Co., Ltd. Intraocular pressure-lowering agent comprising compound having histone deacetylase inhibitory effect as active ingredient
JO2972B1 (en) 2007-06-08 2016-03-15 جانسين فارماسوتيكا ان. في Piperidine / piperazine derivatives
US8835437B2 (en) 2007-06-08 2014-09-16 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
CL2008001671A1 (es) 2007-06-08 2009-07-17 Janssen Pharmaceutica Nv Compuestos derivados de piperidina/piperazina inhibidores de dgat1, composicion farmaceutica que los comprende; y su uso en el tratamiento de enfermedades metabolicas especialmente diabetes.
CA2692153A1 (en) 2007-06-27 2009-01-08 Richard W. Heidebrecht, Jr. Pyridyl and pyrimidinyl derivatives as histone deacetylase inhibitors
WO2009002495A1 (en) 2007-06-27 2008-12-31 Merck & Co., Inc. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8124605B2 (en) 2007-07-06 2012-02-28 Kinex Pharmaceuticals, Llc Compositions and methods for modulating a kinase cascade
CN101765425A (zh) * 2007-08-02 2010-06-30 弗·哈夫曼-拉罗切有限公司 苯甲酰胺衍生物用于治疗cns障碍的用途
MX2010003230A (es) 2007-09-25 2010-04-07 Topotarget Uk Ltd Metodos para la sintesis de ciertos compuestos de acido hidroxamico.
CN101970399A (zh) * 2007-12-14 2011-02-09 乔治敦大学 组蛋白脱乙酰酶抑制剂
JP5564033B2 (ja) 2008-03-27 2014-07-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒストンデアセチラーゼの新規インヒビターとしてのアザ−ビシクロヘキシル置換インドリルアルキルアミノ誘導体
EP2296659B1 (en) 2008-06-05 2016-12-21 Janssen Pharmaceutica, N.V. Drug combinations comprising a DGAT inhibitor and a PPAR-agonist
US9265734B2 (en) 2008-09-03 2016-02-23 Biomarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
MX2011004953A (es) 2008-11-10 2011-12-14 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
KR101745331B1 (ko) 2008-12-19 2017-06-09 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 피라진 유도체
EP2221053A1 (de) * 2009-02-20 2010-08-25 Albert-Ludwigs-Universität Freiburg Pharmazeutische Zusammensetzung enthaltend Hemmstoffe der Proteinmethyltransferase I und deren Verwendung zur Behandlung von Tumorerkrankungen
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
EP2421368A4 (en) * 2009-04-20 2013-01-09 Inst Oneworld Health COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE SULFONAMIDE DERIVATIVES
CN101906076B (zh) * 2009-06-04 2013-03-13 深圳微芯生物科技有限责任公司 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
RU2012109233A (ru) * 2009-09-03 2013-10-10 Аллерган, Инк. Соединения как модуляторы тирозинкиназы
WO2011088181A1 (en) 2010-01-13 2011-07-21 Tempero Pharmaceuticals, Inc. Compounds and methods
JP2013517281A (ja) 2010-01-13 2013-05-16 テンペロ、ファーマシューティカルズ、インコーポレイテッド 化合物及び方法
CN102905700A (zh) 2010-04-16 2013-01-30 金克斯医药品有限公司 用于预防和治疗癌症的组合物以及方法
AU2011253025A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2569289A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
US20130310379A1 (en) * 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
EP2680694B1 (en) 2011-02-28 2019-01-02 BioMarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
EP2694498B1 (en) 2011-04-05 2016-03-30 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
EP2701699B1 (en) 2011-04-28 2019-10-16 The Broad Institute, Inc. Inhibitors of histone deacetylase
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014520161A (ja) 2011-06-22 2014-08-21 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
GB201111630D0 (en) * 2011-07-07 2011-08-24 Cancer Rec Tech Ltd Novel compounds and their use
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
KR102184246B1 (ko) 2011-09-30 2020-12-01 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물의 제조 방법
CA2850564A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
BR112014007690B1 (pt) 2011-09-30 2022-10-04 Vertex Pharmaceuticals Incorporated Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc METHYLATION MODIFICATION ENZYME MODULATORS, COMPOSITIONS AND USES THEREOF
WO2013078320A1 (en) * 2011-11-21 2013-05-30 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
BR112014017762A8 (pt) * 2012-02-09 2017-07-11 Merck Patent Gmbh Derivados de furo[3,2-b]- e tieno[3,2-b]piridina como inibidores de tbk1 e ikk, seus usos, processo para a preparação dos mesmos e medicamentos que os compreendem
AU2013216721B2 (en) 2012-02-10 2017-09-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
RS56673B1 (sr) 2012-04-05 2018-03-30 Vertex Pharma Jedinjenja korisna kao inhibitori atr kinaze i kombinovane terapije koje ih koriste
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
JP6337255B2 (ja) * 2012-07-27 2018-06-06 ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. ヒストンデアセチラーゼの阻害剤
ITRM20120405A1 (it) 2012-08-09 2014-02-10 C N C C S Scarl Collezione Naziona Le Dei Compost Compounds for use in the treatment of disorders that are ameliorated by inhibition of hdac
SI2890680T1 (en) 2012-08-30 2018-08-31 Athenex, Inc. Conventus Building N- (3-FLUOROBENZYL) -2- (5- (4-MORFOLINOPHENYL) PIRIDIN-2-IL) ACETAMIDE AS PROTEIN TIROZINE KINASE PROTECTORS
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN107501275B (zh) 2012-12-07 2019-11-22 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物
EP2970286A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
KR20150132345A (ko) 2013-03-15 2015-11-25 바이오마린 파머수티컬 인크. Hdac 저해제
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003360A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015023915A1 (en) 2013-08-15 2015-02-19 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
ES2862126T3 (es) * 2013-10-10 2021-10-07 Acetylon Pharmaceuticals Inc Compuestos de pirimidín-hidroxiamida como inhibidores de histona desacetilasa
RU2720408C2 (ru) 2013-12-06 2020-04-29 Вертекс Фармасьютикалз Инкорпорейтед Способ получения ингибиторов atr киназы (варианты)
AU2015271030B2 (en) 2014-06-05 2019-05-16 Vertex Pharmaceuticals Incorporated Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof
ES2733847T3 (es) 2014-06-17 2019-12-03 Vertex Pharma Método para tratar cáncer usando una combinación de inhibidores de CHK1 y ATR
US9833466B2 (en) 2014-07-07 2017-12-05 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
US10112939B2 (en) 2014-08-21 2018-10-30 Bristol-Myers Squibb Company Tied-back benzamide derivatives as potent rock inhibitors
WO2016144702A1 (en) 2015-03-06 2016-09-15 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
AU2016229268B2 (en) 2015-03-06 2020-09-10 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
WO2017004522A1 (en) 2015-07-02 2017-01-05 Biomarin Pharmaceutical Inc. Histone deacetylase inhibtors
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
WO2017059357A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
KR102615565B1 (ko) 2016-09-07 2023-12-18 파마케아, 인크. 리실 옥시다제 유사 2 억제제의 용도
CA3039059A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
TWI741040B (zh) * 2016-10-20 2021-10-01 德商拜耳作物科學公司 製備3-烷基硫基-2-氯-n-(1-烷基-1h-四唑-5-基)-4-三氟甲基苯甲醯胺之方法
WO2019134087A1 (zh) * 2018-01-04 2019-07-11 北京大学深圳研究生院 同时抑制lsd1和hdac靶点的化合物及其应用
EA202092328A1 (ru) * 2018-05-11 2021-04-08 Темпл Юниверсити-Оф Зэ Коммонвелс Систем Оф Хаер Эдьюкейшн Новые функционализированные лактамы в качестве модуляторов 5-гидрокситриптаминового рецептора 7 и способ их применения
CN113368114B (zh) * 2020-03-10 2022-04-22 四川大学 一种吗啉嘧啶类化合物的抗肿瘤应用

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH117273A4 (el) * 1973-01-26 1976-07-15
CH187973A4 (de) * 1973-02-09 1977-03-31 Hoechst Ag Verfahren zum optischen Aufhellen von Textilmaterialien
DE2918965A1 (de) * 1979-05-11 1980-11-20 Bayer Ag Benzofuranverbindungen sowie deren verwendung als optische aufheller
IT1232252B (it) * 1989-02-22 1992-01-28 Rotta Research Lab Derivati della n fenil benzamide ad attivita' antiulcera ed antiallerica e procedimento per la loro preparazione
JPH05239069A (ja) * 1992-02-28 1993-09-17 Canon Inc 液晶性化合物、これを含む液晶組成物、それを有する液晶素子、それらを用いた表示方法および表示装置
JP3354090B2 (ja) 1996-09-30 2002-12-09 シエーリング アクチエンゲゼルシャフト 分化誘導剤
US6174905B1 (en) * 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
JPH11269140A (ja) 1998-03-23 1999-10-05 Mitsui Chem Inc 分化誘導剤
JPH11269146A (ja) 1998-03-24 1999-10-05 Mitsui Chem Inc 分化誘導剤
JP4405602B2 (ja) 1998-04-16 2010-01-27 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト ヒストン脱アセチル化酵素阻害剤
JPH11335375A (ja) 1998-05-20 1999-12-07 Mitsui Chem Inc ヒストン脱アセチル化酵素阻害作用を有するベンズアミド誘導体
JP4390024B2 (ja) * 1999-04-23 2009-12-24 アステラス製薬株式会社 新規なジアゼパン誘導体又はその塩
KR20020070285A (ko) 1999-11-23 2002-09-05 메틸진, 인크. 히스톤 디아세틸라제의 억제제
AU776053B2 (en) * 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
JP2002161084A (ja) 2000-11-28 2002-06-04 Sumitomo Pharmaceut Co Ltd 複素環誘導体
MXPA04002397A (es) * 2001-09-14 2004-12-02 Methylgene Inc Inhibidores de histona deacetilasa.
DE10204115A1 (de) * 2002-02-01 2003-08-07 Bayer Cropscience Ag DELTA·1·-Pyrroline
US7148257B2 (en) * 2002-03-04 2006-12-12 Merck Hdac Research, Llc Methods of treating mesothelioma with suberoylanilide hydroxamic acid
CA2632078C (en) 2002-03-04 2012-08-14 Sloan-Kettering Institute For Cancer Research Methods of inducing terminal differentiation
IL163875A0 (en) 2002-03-07 2005-12-18 Univ Delaware Methods, compositions, and kits for enhancing oli gonucleotide mediated nucleic acid sequence alteration using compositions comprising a histone de
NZ534830A (en) 2002-03-13 2005-08-26 Janssen Pharmaceutica Nv Compounds with histone deacetylase HDAC inhibiting activity and oral bioavailability useful for treating proliferative diseases
BR0307606A (pt) 2002-03-13 2004-12-21 Janssen Pharmaceutica Nv Derivados de piperazinila, piperidinila e morfolinila como inibidores de histona desacetilase
EA007272B1 (ru) 2002-03-13 2006-08-25 Янссен Фармацевтика Н. В. Новые ингибиторы гистондеацетилазы
MXPA04007776A (es) 2002-03-13 2004-10-15 Janssen Pharmaceutica Nv Derivados de sulfonilamino como nuevos inhibidores de histona deacetilasa.
ATE398105T1 (de) 2002-03-13 2008-07-15 Janssen Pharmaceutica Nv Carbonylamino- derivativate als neue inhibitoren von histone deacetylase
US20050123397A1 (en) * 2003-12-03 2005-06-09 Mcardle Nathan J. Compressor diffuser

Also Published As

Publication number Publication date
NO330119B1 (no) 2011-02-21
EG25655A (en) 2012-05-02
AU2003217054A1 (en) 2003-10-27
KR20040111478A (ko) 2004-12-31
JP2005533011A (ja) 2005-11-04
ES2392963T3 (es) 2012-12-17
JP4471665B2 (ja) 2010-06-02
CA2480356A1 (en) 2003-10-23
AU2003217054B2 (en) 2009-01-29
KR101066508B1 (ko) 2011-09-21
IS2895B (is) 2014-09-15
IL164373A0 (en) 2005-12-18
US8247562B2 (en) 2012-08-21
PT1495002E (pt) 2012-11-26
TWI319387B (en) 2010-01-11
AR039257A1 (es) 2005-02-16
IS7483A (is) 2004-10-01
TW200400167A (en) 2004-01-01
MY142177A (en) 2010-10-15
BR0308875A (pt) 2005-01-04
HK1071359A1 (en) 2005-07-15
EP1495002A1 (en) 2005-01-12
US20090029991A1 (en) 2009-01-29
RU2376287C2 (ru) 2009-12-20
CN1642915A (zh) 2005-07-20
MXPA04009689A (es) 2005-01-11
WO2003087057A1 (en) 2003-10-23
RU2004132844A (ru) 2005-06-10
CA2480356C (en) 2012-01-03
PL372967A1 (en) 2005-08-08
SI1495002T1 (sl) 2012-12-31
US20100331329A1 (en) 2010-12-30
DK1495002T3 (da) 2012-12-03
IL164373A (en) 2011-02-28
EP1495002B1 (en) 2012-09-05
US20050171103A1 (en) 2005-08-04
NO20044444L (no) 2004-12-28
NZ535143A (en) 2007-04-27
CN101805309A (zh) 2010-08-18

Similar Documents

Publication Publication Date Title
CY1113483T1 (el) Παραγωγα βενζαμιδιου χρησιμα ως αναστολεις αποακετυλασης ιστονης
UY27781A1 (es) Compuestos químicos.
NO20062905L (no) Nye hydroksaminsyreestere og farmasoytisk anvendelse derav
CY1105301T1 (el) Αρυλοσυμπυκνωμενες αζαπολυκυκλικες ενωσεις
CY1113269T1 (el) Παραγωγα ινδαζολυλ αμιδιου για τη θεραπευτικη αγωγη διαταραχων διαμεσολαβουμενων υπο υποδοχεα γλυκοκορτικοειδων
EA200500286A1 (ru) Новые изотиазольные и изоксазольные соединения в качестве ингибиторов трансформирующего фактора роста (тфр)
EA200700099A1 (ru) Производные пиридина
CY1108894T1 (el) Νεα παραγωγα βενζιμιδαζολης
NO20005766L (no) Benzamidderivater for behandling av sykdommer mediert av cytokiner
CY1109376T1 (el) Παραγωγα υδαντοϊνης χρησιμα ως αναστολεις μεταλλοπρωτεϊνασης
MY146662A (en) Novel n-(8-heteroaryltetrahydronaphtalene-2yl) or n-(5-heteroarylchromane-3-yl) carboxamide derivatives for the treatment of pain
ATE286501T1 (de) Pyrimidinderivate
ATE402929T1 (de) Pyrazinverbindungen als inhibitoren des transforming growth factor (tgf)
EA200300776A1 (ru) Производные фенэтаноламина для лечения респираторных заболеваний
PH12021551257A1 (en) Cyclic pantetheine derivatives and uses thereof
CY1110332T1 (el) Παραγωγα βενζιμιδαζολης, συνθεσεις που τα περιεχουν, παρασκευη αυτων και χρηση τους
TW200626553A (en) Novel compounds
CY1114521T1 (el) Ενωσεις βενζαμιδιου χρησιμες ως αναστολεις αποακετυλασων ιστονων
CY1110694T1 (el) Μεθοδος παρασκευης παραγωγων της εχινοκανδινης
EA200400086A1 (ru) Новые производные оксазолидинонов в качестве антибактериальных агентов
DK0669912T3 (da) N-(3-Piperidinylcarbonyl)-beta-alaninderivater som PAF-antagonister
MXPA05013607A (es) Candidatos de farmaco farmaceuticos mejorados y metodos para preparar los mismos.
CY1108238T1 (el) Μεθοδος συνθεσης της περινδοπριλης και των φαρμακευτικως αποδεκτων αλατων της
EA200870223A1 (ru) Производные бензоизоиндола для лечения боли
MY139613A (en) Novel piperazinyl-pyrazinone derivatives for the treatment of 5-ht2a receptor-related disorders