CN101133060B - 酶抑制剂 - Google Patents

酶抑制剂 Download PDF

Info

Publication number
CN101133060B
CN101133060B CN2006800069161A CN200680006916A CN101133060B CN 101133060 B CN101133060 B CN 101133060B CN 2006800069161 A CN2006800069161 A CN 2006800069161A CN 200680006916 A CN200680006916 A CN 200680006916A CN 101133060 B CN101133060 B CN 101133060B
Authority
CN
China
Prior art keywords
mmol
stage
phenyl
acid
group
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN2006800069161A
Other languages
English (en)
Chinese (zh)
Other versions
CN101133060A (zh
Inventor
A·H·戴维森
S·R·佩特尔
F·A·马塞
S·J·戴维斯
A·H·德吕蒙
D·F·C·莫法特
K·W·J·贝克
A·D·G·唐纳尔德
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chroma Therapeutics Ltd
Original Assignee
Chroma Therapeutics Ltd
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 Chroma Therapeutics Ltd filed Critical Chroma Therapeutics Ltd
Publication of CN101133060A publication Critical patent/CN101133060A/zh
Application granted granted Critical
Publication of CN101133060B publication Critical patent/CN101133060B/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to a carbon atom of a six-membered aromatic ring
    • 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
    • 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
    • A61P25/28—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
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/416—2,5-Pyrrolidine-diones 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 other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2006800069161A 2005-05-05 2006-05-04 酶抑制剂 Expired - Fee Related CN101133060B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0509223.4 2005-05-05
GB0509223A GB0509223D0 (en) 2005-05-05 2005-05-05 Enzyme inhibitors
PCT/GB2006/001605 WO2006117549A1 (en) 2005-05-05 2006-05-04 Enzyme inhibitors

Publications (2)

Publication Number Publication Date
CN101133060A CN101133060A (zh) 2008-02-27
CN101133060B true CN101133060B (zh) 2013-06-05

Family

ID=34685155

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2006800069161A Expired - Fee Related CN101133060B (zh) 2005-05-05 2006-05-04 酶抑制剂

Country Status (19)

Country Link
US (3) US7939666B2 (https=)
EP (2) EP1879895B1 (https=)
JP (1) JP5405820B2 (https=)
KR (1) KR101307815B1 (https=)
CN (1) CN101133060B (https=)
AT (1) ATE512150T1 (https=)
AU (1) AU2006243065B2 (https=)
BR (1) BRPI0607410A2 (https=)
CA (1) CA2599411C (https=)
DK (1) DK1879895T3 (https=)
ES (1) ES2367369T3 (https=)
GB (1) GB0509223D0 (https=)
IL (1) IL185580A (https=)
MX (1) MX2007010456A (https=)
NZ (1) NZ560289A (https=)
PL (1) PL1879895T3 (https=)
PT (1) PT1879895E (https=)
WO (1) WO2006117549A1 (https=)
ZA (1) ZA200707091B (https=)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2477604A1 (en) 2002-03-13 2003-09-25 Signum Biosciences, Inc. Modulation of protein methylation and phosphoprotein phosphate
US7923041B2 (en) 2005-02-03 2011-04-12 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
WO2006084033A1 (en) 2005-02-03 2006-08-10 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
GB0509225D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
GB0509223D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
BRPI0610368A8 (pt) * 2005-05-05 2015-09-08 Glaxosmithkline Ip Dev Ltd Modulação de enzima e de receptor
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
GB0619753D0 (en) * 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
US8962825B2 (en) * 2006-10-30 2015-02-24 Glaxosmithkline Intellectual Property Development Limited Hydroxamates as inhibitors of histone deacetylase
GB0803747D0 (en) 2008-02-29 2008-04-09 Martin Enzyme and receptor modulation
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
US8431538B2 (en) 2009-07-22 2013-04-30 The Board Of Trustees Of The University Of Illinois HDAC inhibitors and therapeutic methods of using same
JP5947724B2 (ja) 2009-12-21 2016-07-06 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル シクロフィリンの新しいインヒビター及びその使用
GB201009853D0 (en) 2010-06-11 2010-07-21 Chroma Therapeutics Ltd HSP90 inhibitors
ES2402252B1 (es) * 2011-09-26 2014-03-10 Universidad De Granada Compuesto con actividad antileishmania
JP5771750B2 (ja) * 2011-10-28 2015-09-02 チョン クン ダン ファーマシューティカル コーポレーション Ｈｄａｃ阻害剤用のヒドロキサメート誘導体およびこれを含む薬学的組成物
GB201211310D0 (en) 2012-06-26 2012-08-08 Chroma Therapeutics Ltd CSF-1R kinase inhibitors
HUE046132T2 (hu) 2012-10-17 2020-02-28 Macrophage Pharma Ltd N-[2-{4-[6-amino-5-(2,4-difluor-benzoil)-2-oxopiridin-1(2H)-il]-3,5-difluor-fenil}etil]-l-alanin és annak tercbutil-észtere
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
SG11201708622UA (en) 2015-02-02 2017-11-29 Forma Therapeutics Inc 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors
WO2016126726A1 (en) 2015-02-02 2016-08-11 Forma Therapeutics, Inc. Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors
WO2017162674A1 (en) * 2016-03-22 2017-09-28 Institut National De La Sante Et De La Recherche Medicale (Inserm) Novel derivatives and their use as selective inhibitors of caspase-2
WO2017216297A1 (en) 2016-06-16 2017-12-21 Glaxosmithkline Intellectual Property Development Limited Dosage regimen
EP3472131B1 (en) 2016-06-17 2020-02-19 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors
GB201713975D0 (en) 2017-08-31 2017-10-18 Macrophage Pharma Ltd Medical use
TWI650139B (zh) * 2017-10-11 2019-02-11 行政院原子能委員會核能硏究所 含有放射性同位素氟的異羥肟酸類造影劑、其製備方法及其用途
WO2020013116A1 (ja) * 2018-07-10 2020-01-16 京都薬品工業株式会社 Ｐｔｐ－１ｂ阻害剤およびその用途
CN111393404B (zh) * 2019-01-02 2023-02-17 中国科学院上海药物研究所 一类苯并噻吩类化合物及其药物组合物及应用
CN113121527B (zh) * 2019-12-31 2024-09-06 上海辉启生物医药科技有限公司 三环类化合物及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003066579A2 (en) * 2002-02-07 2003-08-14 Axys Pharmaceuticals Novel bicyclic hydroxamates as inhibitors of histone deacetylase
CN1450991A (zh) * 2000-09-01 2003-10-22 诺瓦提斯公司 脱乙酰酶抑制剂
WO2005037272A1 (en) * 2003-10-22 2005-04-28 Arpida A/S Benzimidazole derivatives and use thereof as peptide deformylase inhibitors

Family Cites Families (40)

* 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
JPS6188884A (ja) 1984-10-04 1986-05-07 Sankyo Co Ltd エンケフアリナ−ゼｂ阻害物質およびその製法
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
IT1264860B1 (it) * 1993-06-21 1996-10-17 Guidotti & C Spa Labor Derivati di acidi cis- e trans-2(((2-(isdrossiammino)-2-ossoetil)- alchilammino)carbonil)cicloesancarbossilici
US6204293B1 (en) * 1995-11-06 2001-03-20 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
AU4249700A (en) 1999-04-19 2000-11-02 Sumitomo Pharmaceuticals Company, Limited Hydroxamic acid derivative
EA200601252A1 (ru) 1999-09-08 2006-10-27 Слоан-Кеттеринг Инститьют Фор Кэнсер Рисёч Новый класс веществ, вызывающих дифференцировку клеток и являющихся ингибиторами гистондеацетилазы, и способы их применения
KR20020070285A (ko) 1999-11-23 2002-09-05 메틸진, 인크. 히스톤 디아세틸라제의 억제제
GB0003476D0 (en) 2000-02-16 2000-04-05 British Biotech Pharm Acetal Hydroxylamine compounds
AU2001248701A1 (en) 2000-03-24 2001-10-03 Methylgene, Inc. Inhibitors of histone deacetylase
EP1335898B1 (en) 2000-09-29 2005-11-23 TopoTarget UK Limited Carbamic acid compounds comprising an amide linkage as hdac inhibitors
CA2423744C (en) 2000-09-29 2012-04-03 Prolifix Limited Hydroxamic acid compounds comprising a sulfonamide linkage as hdac inhibitors
GB0023983D0 (en) 2000-09-29 2000-11-15 Prolifix Ltd Therapeutic compounds
AR035513A1 (es) 2000-12-23 2004-06-02 Hoffmann La Roche Derivados de tetrahidropiridina, proceso para prepararlos, composiciones farmaceuticas que los contienen, y uso de dichos compuestos en la preparacion de medicamentos
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
DE60326436D1 (en) 2002-03-13 2009-04-16 Janssen Pharmaceutica Nv Aminoderivate als histone-deacetylase-inhibitoren
OA12793A (en) 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv Sulfonylamino-derivatives as novel inhibitors of histone deacetylase.
MXPA04008796A (es) 2002-03-13 2004-11-26 Janssen Pharmaceutica Nv Derivados de carbonilamino como novedosos inhibidores de desacetilasa de histona.
ES2306859T3 (es) 2002-03-13 2008-11-16 Janssen Pharmaceutica Nv Derivados de sulfonil como nuevos inhibidores de histona deacetilasa.
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
PL374970A1 (en) 2002-08-02 2005-11-14 Argenta Discovery Limited Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors
US7221775B2 (en) 2002-11-12 2007-05-22 Intellivid Corporation Method and apparatus for computerized image background analysis
SI1611088T1 (sl) 2003-04-07 2009-12-31 Pharmacyclics Inc Hidroksamati kot terapevtska sredstva
WO2004110989A1 (en) 2003-05-14 2004-12-23 Bayer Pharmaceuticals Corporation N-hydroxy-7-(arylamino)heptanamide derivatives useful for treating hyper-proliferative disorders
US20060235012A1 (en) * 2003-06-16 2006-10-19 Chroma Therapeutics Limited Carboline and betacarboline derivatives for use as hdac enzyme inhibitors
EP1644323B1 (en) 2003-07-07 2015-03-18 Georgetown University Histone deacetylase inhibitors and methods of use thereof
WO2005004861A1 (en) 2003-07-15 2005-01-20 Korea Research Institute Of Bioscience And Biotechnology A use of novel 2-oxo-heterocyclic compounds and the pharmaceutical compositions comprising the same
WO2005014588A1 (en) 2003-08-01 2005-02-17 Argenta Discovery Limited Substituted thienyl-hydroxamic acids having histone deacetylase activity
US20060270730A1 (en) 2003-08-07 2006-11-30 Andreas Katopodis Histone deacetylase inhibitors as immunosuppressants
DE602004004665T2 (de) 2003-08-20 2008-01-03 Pharmacyclics, Inc., Sunnyvale Acetylenderivate als inhibitoren von histondeacetylase
KR100924737B1 (ko) 2003-08-26 2009-11-04 슬로안-케테링인스티튜트퍼캔서리서치 Ｈｄａｃ 억제제를 이용한 암의 치료 방법
PT1673349E (pt) 2003-09-22 2010-09-28 S Bio Pte Ltd Derivados benzimidazole: preparação e aplicações farmacêuticas
KR101153335B1 (ko) 2003-09-24 2012-07-05 메틸진 인코포레이티드 히스톤 데아세틸라제의 억제제
WO2005034880A2 (en) 2003-10-09 2005-04-21 Aton Pharma, Inc. Thiophene and benzothiophene hydroxamic acid derivatives
GB0509223D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
BRPI0610368A8 (pt) 2005-05-05 2015-09-08 Glaxosmithkline Ip Dev Ltd Modulação de enzima e de receptor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1450991A (zh) * 2000-09-01 2003-10-22 诺瓦提斯公司 脱乙酰酶抑制剂
WO2003066579A2 (en) * 2002-02-07 2003-08-14 Axys Pharmaceuticals Novel bicyclic hydroxamates as inhibitors of histone deacetylase
WO2005037272A1 (en) * 2003-10-22 2005-04-28 Arpida A/S Benzimidazole derivatives and use thereof as peptide deformylase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Russell L.Wolz.A kinetic comparison of the homologous proteases astacin and meprin A1.Archives biochemistry and biophysics.1994, *

Also Published As

Publication number Publication date
CA2599411C (en) 2013-12-03
US8686032B2 (en) 2014-04-01
IL185580A0 (en) 2008-01-06
ES2367369T3 (es) 2011-11-02
AU2006243065B2 (en) 2012-05-03
AU2006243065A1 (en) 2006-11-09
US20130116318A1 (en) 2013-05-09
GB0509223D0 (en) 2005-06-15
US7939666B2 (en) 2011-05-10
US20140163042A1 (en) 2014-06-12
JP2008540389A (ja) 2008-11-20
KR101307815B1 (ko) 2013-09-12
KR20080015388A (ko) 2008-02-19
BRPI0607410A2 (pt) 2009-09-01
ZA200707091B (en) 2008-10-29
WO2006117549A1 (en) 2006-11-09
EP1879895A1 (en) 2008-01-23
EP2301939A1 (en) 2011-03-30
US9133104B2 (en) 2015-09-15
IL185580A (en) 2012-08-30
EP1879895B1 (en) 2011-06-08
CA2599411A1 (en) 2006-11-09
MX2007010456A (es) 2007-10-11
US20090291978A1 (en) 2009-11-26
JP5405820B2 (ja) 2014-02-05
PL1879895T3 (pl) 2011-11-30
DK1879895T3 (da) 2011-09-19
CN101133060A (zh) 2008-02-27
ATE512150T1 (de) 2011-06-15
NZ560289A (en) 2010-11-26
PT1879895E (pt) 2011-09-06

Similar Documents

Publication Publication Date Title
CN101133060B (zh) 酶抑制剂
CN101528677B (zh) Hdac抑制剂
US7973181B2 (en) Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity
US10172846B2 (en) HCV NS-3 serine protease inhibitors
JP2768554B2 (ja) 金属タンパク質加水分解酵素阻害剤であるヒドロキサム酸誘導体
KR100352199B1 (ko) 매트릭스메탈로프로테아제억제제
JP5340918B2 (ja) ｐ３８ＭＡＰキナーゼ阻害剤
CN101553475B (zh) 作为组蛋白脱乙酰基酶抑制剂的异羟肟酸
SK65097A3 (en) Metalloproteinase inhibitors, manufacturing process thereof and pharmaceutical composition containing the same
EP2401257A1 (en) Enzyme inhibitors
CN102180826A (zh) 含α氨基酸结构的组蛋白去乙酰化酶抑制剂及其用途
US6797730B2 (en) Peptide deformylase inhibitors
JP2004143053A (ja) β−アミノヒドロキサム酸誘導体およびその用途
CN101437799B (zh) p38MAP激酶抑制剂

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20130605

Termination date: 20210504