EA017074B1 - Ингибиторы hdac - Google Patents

Ингибиторы hdac Download PDF

Info

Publication number
EA017074B1
EA017074B1 EA200900519A EA200900519A EA017074B1 EA 017074 B1 EA017074 B1 EA 017074B1 EA 200900519 A EA200900519 A EA 200900519A EA 200900519 A EA200900519 A EA 200900519A EA 017074 B1 EA017074 B1 EA 017074B1
Authority
EA
Eurasian Patent Office
Prior art keywords
amino
hydroxyamino
alkyl
mmol
nmr
Prior art date
Application number
EA200900519A
Other languages
English (en)
Russian (ru)
Other versions
EA200900519A1 (ru
Inventor
Алан Хорнсби Дэвидсон
Дэвид Фестус Чарльз Моффат
Франческа Энн Дэй
Аластейр Дэвид Грэхем Дональд
Original Assignee
Хрома Терапьютикс Лтд.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Хрома Терапьютикс Лтд. filed Critical Хрома Терапьютикс Лтд.
Publication of EA200900519A1 publication Critical patent/EA200900519A1/ru
Publication of EA017074B1 publication Critical patent/EA017074B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • 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
    • C07D295/08—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 singly bound oxygen or sulfur atoms
    • C07D295/084—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/223—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-aminoacids
    • 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic 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
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • 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
    • 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
    • C07D211/36—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 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • 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
    • 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
    • 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
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
EA200900519A 2006-10-06 2007-09-14 Ингибиторы hdac EA017074B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0619753.7A GB0619753D0 (en) 2006-10-06 2006-10-06 Enzyme inhibitors
PCT/GB2007/003504 WO2008040934A1 (en) 2006-10-06 2007-09-14 Hdac inhibitors

Publications (2)

Publication Number Publication Date
EA200900519A1 EA200900519A1 (ru) 2010-04-30
EA017074B1 true EA017074B1 (ru) 2012-09-28

Family

ID=37454078

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200900519A EA017074B1 (ru) 2006-10-06 2007-09-14 Ингибиторы hdac

Country Status (22)

Country Link
US (4) US8637547B2 (enExample)
EP (2) EP2295410B1 (enExample)
JP (1) JP5395668B2 (enExample)
KR (1) KR101570136B1 (enExample)
CN (2) CN101528677B (enExample)
AU (1) AU2007304022B2 (enExample)
BR (1) BRPI0719204A2 (enExample)
CA (1) CA2665428C (enExample)
CY (1) CY1118881T1 (enExample)
DK (1) DK2295410T3 (enExample)
EA (1) EA017074B1 (enExample)
ES (1) ES2626293T3 (enExample)
GB (1) GB0619753D0 (enExample)
HU (1) HUE033229T2 (enExample)
IL (1) IL197752A0 (enExample)
LT (1) LT2295410T (enExample)
MX (1) MX2009003515A (enExample)
NZ (1) NZ576058A (enExample)
PL (1) PL2295410T3 (enExample)
PT (1) PT2295410T (enExample)
SI (1) SI2295410T1 (enExample)
WO (1) WO2008040934A1 (enExample)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US20030129724A1 (en) 2000-03-03 2003-07-10 Grozinger Christina M. Class II human histone deacetylases, and uses related thereto
US7244853B2 (en) 2001-05-09 2007-07-17 President And Fellows Of Harvard College Dioxanes and uses thereof
EP1861126A4 (en) 2005-03-22 2009-11-18 Harvard College TREATMENT OF PROTEIN REMOVAL TROUBLES
AU2006243000B2 (en) * 2005-05-05 2011-05-26 Macrophage Pharma Limited Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase
GB0509225D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
EP1991247B1 (en) 2006-02-14 2015-10-14 President and Fellows of Harvard College Bifunctional histone deacetylase inhibitors
EP2019674B1 (en) 2006-05-03 2016-11-23 The President and Fellows of Harvard College Histone deacetylase and tubulin deacetylase inhibitors
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
JP5043120B2 (ja) 2006-10-30 2012-10-10 クロマ セラピューティクス リミテッド ヒストンデアセチラーゼの阻害剤としてのヒドロキサメート
GB0803747D0 (en) 2008-02-29 2008-04-09 Martin Enzyme and receptor modulation
CN102164888B (zh) 2008-07-23 2015-06-03 哈佛大学校长及研究员协会 脱乙酰酶抑制剂和其用途
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
GB0903480D0 (en) * 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
WO2011019393A2 (en) 2009-08-11 2011-02-17 President And Fellows Of Harvard College Class- and isoform-specific hdac inhibitors and uses thereof
US20110053925A1 (en) * 2009-08-28 2011-03-03 Novartis Ag Hydroxamate-Based Inhibitors of Deacetylases
US20110245154A1 (en) 2010-03-11 2011-10-06 Hemaquest Pharmaceuticals, Inc. Methods and Compositions for Treating Viral or Virally-Induced Conditions
GB201009853D0 (en) 2010-06-11 2010-07-21 Chroma Therapeutics Ltd HSP90 inhibitors
WO2012025701A1 (en) 2010-08-25 2012-03-01 Chroma Therapeutics Ltd. Alpha, alpha - di substituted glycine ester derivatives and their use as hdac inhibitors
WO2012025155A1 (en) * 2010-08-26 2012-03-01 Novartis Ag Hydroxamate-based inhibitors of deacetylases
EP2609078A1 (en) * 2010-08-27 2013-07-03 Novartis AG Hydroxamate-based inhibitors of deacetylases
CN101967113B (zh) * 2010-09-14 2012-08-22 北京欧凯纳斯科技有限公司 3-Alloc胺基-3-（3-硝基-4-氟苯基）丙酸及其制备方法
CN101985432B (zh) * 2010-09-15 2012-02-22 北京欧凯纳斯科技有限公司 3-Fmoc胺基-3-（3-硝基-4-氟苯基）丙酸及其制备方法
CN101962349B (zh) * 2010-09-15 2012-08-22 北京欧凯纳斯科技有限公司 3-Boc胺基-3-（3-硝基-4-氟苯基）丙酸及其制备方法
CN102532006A (zh) * 2012-01-31 2012-07-04 江西华士药业有限公司 治疗（类）风湿关节炎药物关键中间体6-甲基吡啶-3-甲醛的制备方法
US20150087687A1 (en) 2012-03-23 2015-03-26 Dennis Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
BR112014025122B1 (pt) 2012-04-10 2022-08-16 Annji Pharmaceutical Co., Ltd Compostos inibidores de histona deacetilases, composição que compreende os mesmos e usos dos ditos compostos e composição para tratar um tumor associado com a desregulação da atividade de histona deacetilases e aumentar a capacidade de aprendizado
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
GB201211310D0 (en) 2012-06-26 2012-08-08 Chroma Therapeutics Ltd CSF-1R kinase inhibitors
MA37700B1 (fr) 2012-06-26 2018-03-30 Bayer Pharma AG N-[4-(quinolin-4-yloxy)cyclohexyl(méthyl)](hétéro)arylcarboxamides utilisables en tant qu'antagonistes des récepteurs aux androgènes, leur production et leur utilisation en tant que médicaments
PL2909175T3 (pl) 2012-10-17 2017-10-31 Macrophage Pharma Ltd N-[2-{4-[6-amino-5-(2,4-difluorobenzoilo)-2-oksopirydyn-1(2h) ylo]-3,5-difluorofenylo}etylo)-l-alaninian tert-butylu lub jego sól, hydrat lub solwat
CN103172540B (zh) * 2013-03-18 2015-07-01 潍坊博创国际生物医药研究院 苯甘氨酸类组蛋白去乙酰酶抑制剂及其制备方法和应用
MX2017011778A (es) 2015-03-13 2017-12-04 Forma Therapeutics Inc Compuestos y composiciones de alfa-cinamida como inhibidores de histona desacetilasa 8 (hdac8).
CN105646297B (zh) * 2015-09-06 2017-12-29 杨东 一种生产贝利司他中间体的工艺方法
CN106496071B (zh) * 2015-09-07 2018-07-31 上海医药工业研究院 肉桂酰胺类化合物、其盐、中间体、制备方法及应用
CA3007767A1 (en) 2015-12-18 2017-06-22 The Procter & Gamble Company Synthesis of cyclohexane ester derivatives useful as sensates in consumer products
WO2017216297A1 (en) 2016-06-16 2017-12-21 Glaxosmithkline Intellectual Property Development Limited Dosage regimen
WO2018013975A1 (en) 2016-07-15 2018-01-18 Viracta Therapeutics, Inc. Hdac inhibitors for use with nk cell based therapies
CA3063111C (en) 2017-05-16 2022-10-11 Annji Pharmaceutical Co., Ltd. Histone deacetylases (hdacs) inhibitors
GB201713975D0 (en) 2017-08-31 2017-10-18 Macrophage Pharma Ltd Medical use
JP2021515767A (ja) 2018-03-07 2021-06-24 バイエル・アクチエンゲゼルシヤフト Ｅｒｋ５阻害剤の同定及び使用
CN212123220U (zh) * 2019-05-17 2020-12-11 依机国际有限公司 快速滑出式户外工具袋
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
EP3976198A4 (en) 2019-05-31 2023-07-19 Viracta Subsidiary, Inc. METHODS OF TREATING VIRUS-ASSOCIATED CANCERS WITH HISTONE DEACETYLASE INHIBITORS
WO2021252475A1 (en) 2020-06-08 2021-12-16 Annji Pharmaceutical Co., Ltd. Quinazoline derivatives useful as selective hdac6 inhibitors
WO2022203429A1 (en) * 2021-03-26 2022-09-29 Chong Kun Dang Pharmaceutical Corp. Composition for preventing or treating multiple sclerosis
CN113582911B (zh) * 2021-08-12 2024-03-12 山东大学 多靶点多奈哌齐-异羟肟酸型化合物及其制备方法和应用
KR20240086748A (ko) 2022-11-29 2024-06-19 숙명여자대학교산학협력단 Ent-7β-하이드록시-15-옥소카우르-16-엔-18-일 아세테이트를 유효성분으로 포함하는 골질환의 예방, 개선 또는 치료용 조성물

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002022577A2 (en) * 2000-09-01 2002-03-21 Novartis Ag Hydroxamate derivatives useful as deacetylase inhibitors

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1099355B (it) 1978-10-12 1985-09-18 Sclavo Inst Sieroterapeut Composizione adatta alla determinazione in cinetica del glucosio
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
US5369108A (en) 1991-10-04 1994-11-29 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and methods of use thereof
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
US6511990B1 (en) 1999-09-08 2003-01-28 Sloan-Kettering Institute For Cancer Research Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
ATE514674T1 (de) 1999-11-23 2011-07-15 Methylgene Inc Inhibitoren für histone-deacetylase
GB0003476D0 (en) 2000-02-16 2000-04-05 British Biotech Pharm Acetal Hydroxylamine compounds
ATE489360T1 (de) 2000-03-24 2010-12-15 Methylgene Inc Inhibitoren der histon-deacetylase
JP2004509941A (ja) 2000-09-29 2004-04-02 プロリフィクス　リミテッド Ｈｄａｃインヒビターとしてのアミド結合を含むカルバミン酸化合物
GB0023983D0 (en) 2000-09-29 2000-11-15 Prolifix Ltd Therapeutic compounds
CA2423744C (en) 2000-09-29 2012-04-03 Prolifix Limited Hydroxamic acid compounds comprising a sulfonamide linkage as hdac inhibitors
WO2002069947A2 (en) 2001-01-12 2002-09-12 Methylgene, Inc. Antisense oligonucleotides and trichostatin analogue histone deacetylase-4 inhibitors against cancer
US6784173B2 (en) 2001-06-15 2004-08-31 Hoffmann-La Roche Inc. Aromatic dicarboxylic acid derivatives
US20040091951A1 (en) 2002-02-07 2004-05-13 Axys Pharmaceuticals, Inc. Assay for measuring acetylation or deacetylation activity of an enzyme
US7501417B2 (en) 2002-03-13 2009-03-10 Janssen Pharmaceutica, N.V. Aminocarbonyl-derivatives as novel inhibitors of histone deacetylase
PL205531B1 (pl) 2002-03-13 2010-04-30 Janssen Pharmaceutica Nv Pochodna karbonyloaminowa, jej zastosowanie i sposób wytwarzania oraz kompozycja farmaceutyczna
CN100445276C (zh) 2002-03-13 2008-12-24 詹森药业有限公司 用作组蛋白去乙酰酶抑制剂的磺酰基衍生物
JP4725945B2 (ja) 2002-03-13 2011-07-13 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な阻害剤としてのスルホニルアミノ誘導体
CA2479906C (en) 2002-04-03 2011-02-08 Topotarget Uk Limited Carbamic acid compounds comprising a piperazine linkage as hdac inhibitors
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
CA2494114A1 (en) 2002-08-02 2004-02-12 Argenta Discovery Limited Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors
US20060032823A1 (en) 2002-09-04 2006-02-16 Harrison Alan D Disinfection of reverse osmosis membrane
US7221775B2 (en) 2002-11-12 2007-05-22 Intellivid Corporation Method and apparatus for computerized image background analysis
TW200418806A (en) * 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
JP4790594B2 (ja) 2003-02-25 2011-10-12 トポターゲット ユーケー リミテッド Ｈｄａｃインヒビターとしての、二環式ヘテロアリール基を含むヒドロキサム酸化合物
WO2004092115A2 (en) 2003-04-07 2004-10-28 Axys Pharmaceuticals Inc. Hydroxamates as therapeutic agents
WO2004110989A1 (en) 2003-05-14 2004-12-23 Bayer Pharmaceuticals Corporation N-hydroxy-7-(arylamino)heptanamide derivatives useful for treating hyper-proliferative disorders
EP1644323B1 (en) 2003-07-07 2015-03-18 Georgetown University Histone deacetylase inhibitors and methods of use thereof
EP1663201A4 (en) 2003-07-15 2009-10-28 Korea Res Inst Of Bioscience USE OF NOVEL 2-OXO-HETEROCYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
WO2005014588A1 (en) 2003-08-01 2005-02-17 Argenta Discovery Limited Substituted thienyl-hydroxamic acids having histone deacetylase activity
JP2007501775A (ja) 2003-08-07 2007-02-01 ノバルティス アクチエンゲゼルシャフト 免疫抑制剤としてのヒストンデアセチラーゼ阻害剤
ATE353319T1 (de) 2003-08-20 2007-02-15 Axys Pharm Inc Acetylenderivate als inhibitoren von histondeacetylase
RU2356547C2 (ru) 2003-08-26 2009-05-27 Мерк ЭйчДиЭйСи Рисерч ЛЛС Способы лечения рака с использованием ингибиторов hdac
MY142589A (en) 2003-09-22 2010-12-15 S Bio Pte Ltd Benzimidazole derivatives : preparation and pharmaceutical applications
AU2004276337B2 (en) 2003-09-24 2009-11-12 Methylgene Inc. Inhibitors of histone deacetylase
CZ2004770A3 (cs) 2004-06-29 2006-02-15 Pavelka@Miloslav Zpusob detekce únavy operátora ze svalové cinnosti a zarízení k provádení tohoto zpusobu
CN101001851B (zh) * 2004-08-09 2011-04-20 安斯泰来制药有限公司 具有作为组蛋白脱乙酰酶(hdac)抑制剂的活性的羟基酰胺化合物
AU2006243000B2 (en) * 2005-05-05 2011-05-26 Macrophage Pharma Limited Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase
GB0509227D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Intracellular enzyme inhibitors
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
GB0510204D0 (en) * 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
WO2006136553A1 (en) * 2005-06-23 2006-12-28 Janssen Pharmaceutica N.V. Imidazolinone and hydantoine derivatives as novel inhibitors of histone deacetylase
GB0608837D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of MAP kinase
GB0608821D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd DHFR enzyme inhibitors
GB0608823D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of P13 kinase
AU2007246869B2 (en) * 2006-05-04 2012-10-18 Macrophage Pharma Limited p38 MAP kinase inhibitors
GB0619753D0 (en) * 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
GB0621203D0 (en) * 2006-10-25 2006-12-06 Chroma Therapeutics Ltd PLK inhibitors
NZ577153A (en) * 2006-10-25 2012-02-24 Chroma Therapeutics Ltd Pteridine derivatives as polo-like kinase inhibitors useful in the treatment of cancer
JP5043120B2 (ja) * 2006-10-30 2012-10-10 クロマ セラピューティクス リミテッド ヒストンデアセチラーゼの阻害剤としてのヒドロキサメート
ATE524454T1 (de) * 2006-11-01 2011-09-15 Chroma Therapeutics Ltd Inhibitoren von ikk-beta serinthreoninproteinkinase
DK2078007T3 (da) * 2006-11-01 2011-12-12 Chroma Therapeutics Ltd Ikk-beta-serin-threonin-proteinkinasehæmmere
GB0622084D0 (en) * 2006-11-06 2006-12-13 Chroma Therapeutics Ltd Inhibitors of HSP90

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002022577A2 (en) * 2000-09-01 2002-03-21 Novartis Ag Hydroxamate derivatives useful as deacetylase inhibitors

Also Published As

Publication number Publication date
GB0619753D0 (en) 2006-11-15
KR20090095560A (ko) 2009-09-09
DK2295410T3 (en) 2017-05-22
ES2626293T3 (es) 2017-07-24
US9273003B2 (en) 2016-03-01
WO2008040934A1 (en) 2008-04-10
IL197752A0 (en) 2009-12-24
EA200900519A1 (ru) 2010-04-30
EP2069291A1 (en) 2009-06-17
LT2295410T (lt) 2017-05-25
PT2295410T (pt) 2017-06-14
HUE033229T2 (hu) 2017-11-28
CN101528677A (zh) 2009-09-09
PL2295410T3 (pl) 2017-10-31
MX2009003515A (es) 2009-04-16
CN101528677B (zh) 2014-07-30
BRPI0719204A2 (pt) 2014-03-04
CN104151200B (zh) 2017-06-20
CN104151200A (zh) 2014-11-19
CA2665428A1 (en) 2008-04-10
EP2295410B1 (en) 2017-03-15
CY1118881T1 (el) 2018-01-10
AU2007304022A1 (en) 2008-04-10
AU2007304022B2 (en) 2012-05-03
KR101570136B1 (ko) 2015-11-18
US20160137594A1 (en) 2016-05-19
EP2069291B1 (en) 2017-12-20
US20130197042A1 (en) 2013-08-01
JP5395668B2 (ja) 2014-01-22
US20100010010A1 (en) 2010-01-14
NZ576058A (en) 2012-01-12
US8637547B2 (en) 2014-01-28
SI2295410T1 (sl) 2017-06-30
EP2295410A1 (en) 2011-03-16
CA2665428C (en) 2014-03-25
US9725407B2 (en) 2017-08-08
US20140323531A1 (en) 2014-10-30
JP2010505802A (ja) 2010-02-25

Similar Documents

Publication Publication Date Title
EA017074B1 (ru) Ингибиторы hdac
EP1877366B1 (en) Hydroxamic acid dervicatives as inhibitors of hdac enzymatic activity
JP5405820B2 (ja) 酵素阻害剤
EA017198B1 (ru) Гидроксаматы в качестве ингибиторов гистон-деацетилазы
US20140155439A1 (en) Enzyme inhibitors
WO2012025701A1 (en) Alpha, alpha - di substituted glycine ester derivatives and their use as hdac inhibitors

Legal Events

Date Code Title Description
PC4A Registration of transfer of a eurasian patent by assignment
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU